2,4,5-T:  Position Document 1
           2,4,5-T Working Group
           U.S. Environmental Protection Agency

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             2,4,5-T:   Position Document 1

                       •                          •   Page
  I.  Background	   1
      A*  Chemical/Physical Characteristics..	   1
      B.  Manufacturing Process and Contaminants...   1
      C.  Formulation  and Class	,..   5
      D.  Registered Uses and Production	   5
      E.  Metabolism in Experimental Systems	,   7
      F.  Environmental Fate	   10
          (1)  Persistence:  Soils	   10
          (2)  Persistence:  Water	   12
          (3)  Transport	   15
          (4)  Bioaccumulation	   15
      G.  Residues	   19
          (1)  Soil	   19
          (2)  Water	   20
          (3)  Air	   23
          (4)  Animals	,...   24
          (5)  Plants	   27
          (6)  Humans	   29
          (.7)  Animal  Products	   32
          (8)  Food	   37
          (9)  Human Exposure Via Industrial
               Accidents	,	   38
      E*.  Tolerances	,»..	   42
      I.  Pesticide Episode Reports System (PERS)..   43

 II.  Regulatory History	   45

III.  Summary, of Scientific Evidence Relating  to
      Rebuttable Presumption.	   50
      A." . Oncogenic Effects....	   50
          (1)  2,4,5-T	   51
               (a)  Effects of Dietary 2,4,5-T
               '  .   «0.05 ppm TCDD) on Rodents....   51
               (b)  Effects of Subcutaneous Injec-
                    tion and Oral Administration of
                    2,4,5-T (30 ppm TCDD) on
             —-—   Rodents	   54
          (2)  TCDD	   56
               (a)  Oncogenic Effects of Low
                    Levels of TCDD on Rodents	   56
               (b)  Effects Closely. Related to
                    Oncogenicity in Test Animals...   62
          (3)  Preliminary Epidemiological
               Studies	   64
      B.  Other Chronic or Delayed Toxic Effects...   66
          (1)  Pesticide-free TCDD	   68
               (a)  Studies in which TCDD Produced
                    Teratogenic and/or Fetotoxic
                    Effects in Mice	   68
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                                                    Page
               (b)  Studies in Which TCDD Produced
                    Teratogenic and/or Fetotoxic
                    Effects in Rats	  7 1
               (c)  Summary	  79
          (2)  2>M,5-T (TCDD Contamination Ranging
               From Undetectable to 30 ppm)	  80
               (a)  Teratogenic and Fetotoxic Ef-
                    fects in Rodents	  80
               (b)  Adverse Reproductive Effects
                    in Other Mammalian Test
                    Systems..	  98
               (c)  Adverse Effects in Avian
                    Species	  99
               (d)  Studies in Avian Species in
                    Which Adverse Effects Were Hot
                    Observed...........*•••••••••••  101
               (e)  Summary....	  101
          (3)  Exposure Analysis	  101
               (a)  Oral Exposure	  102
               (b)  Dermal Exposure	  *35
                  (i)   Spray Applicator:  Back-
                        pack Sprayer	  105
                  tii--)  Spray Applicator:  Trac-
                        tor-mounted, Low-boom
                        Spray Equipment	  108
                  (iii) Aerial Application:  Ex-
                       . posed Population Directly
                >: .;     Beneath Spray Plane	  110
               (c)  Inhalation Exposure:  Aerial
                    Application	  113
               (d)  Cumulative Exposure....	  116

 IV.  Studies Relating to Possibe Adverse Effects..  118
      A.  Mutagenicity	.....*  118
,---.      (D  2,1,5-T	.'	  118
               (a)  Positive Study	  118
               (b)  Negative Studies	  119.
          (2)  TCDD	..  121
              	(a)  Positive Studies	  121
            "' (b)  Negative Studies	:	  123
          (3)  Chromosomal Damage	  124
      B.  Toxicity to Humans;  TCDD	•  125
          CD  Chloracne.	  125
    :      (2)  Porphyria cutanea tarda and
               £-Amino-levulinic Acid Synthetase...  127

References	  129


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               2,4,5-T: POSITION DOCUMENT 1


I.  BACKGROUND


     A* Chemical/Physical Characteristics

       The herbicide commonly known as 2,H,5-T (chemical

name, 2,iJ,5-Trichlorophenoxyacetic Acid) has an empirical

formula -of CgH5Cl,0,»  The pure acid form occurs as white

crystals and has a molecular weight of 255»^9»  The melt-

ing point is 156.6°C.  Its solubility in water is 278 parts

per million (ppm) at 25°C; it is also soluble in acetone,

ethanol, ether, and alkaline solutions (1).  The esters of

2|4,5-T are formulated to be emulsifiable in water and

soluble in most oils, while its anine salts are soluble in

water but insoluble in petroleum oils (2, 3)»


     -B-4  -Ma-nufacturing Process and Contaminants


       2,4,5-T is produced commercially by a process using

1,2,4,5-tetrachlorobenzene as the starting material which is

reacted with methanol and sodium hydroxide under high temper-

ature and high"pressure to give the sodium salt of 2,^,5-tri-

chlorophenol (2,4,5-TCP).-'
    2,1,5-TCP is the subject of a separate Rebuttable
Presumption Against Registration (RPAR) Position Document*
It is discussed in this document because both it and its
contaminant 2 ,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) may
be present in some commercial 2,4,5-T and in 2,4,5-T samples
used in animal experiments.
                             -1-

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       This product is reacted with chloroacetie acid under



mildly alkaline conditions,  Sulfuric acid (H SOJ Is then





added to the product of this step to produce 2,4,5-T.  The



acid forn of 2,4,5-T can be readily reacted with a variety



of alcohols to produce a large selection of esters and with



amines to produce amine salts (3)*





       During the first step in the manufacturing process



of 2,4,5-T, if temperature and pressure are not carefully



controlled, highly toxic contaminants, polychlorinated



dibenzo-p-dioxins, may be formed in large quantities*  The



particular dioxin formed is dependent on the chlorophenols



present (4),  The terra dioxin does not apply to any one



compound but to a group of related substances, which are



distinguished by the number and orientation of chlorine



atoms they contain.  Dioxin toxicity also varies with the



position and numbers of chlorines attached to the phenol



rings.





       In the 2,4,5-T manufacturing process an especially



toxic dioxin, 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), is



formed when the reaction temperature is excessive (8, 9, 10,




11, 12), most commonly at temperatures above 160°C.



Halogens at the 2, 3, and 7 positions are known to produce



toxic dioxins (13)*  In the case of TCDD, the chlorine atoms





                             -2-

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are attached at the 2, 3» 7» and 8 positions which are
                                                    \

considered the most toxic positions -possible (HO.   The "

dioxin contaminant in 2,1,5-T is of particular concern

because of its extremely high toxicity, and because of the

apparent inability of manufacturers to produce 2,^,5-T
       •        »
                                  2/
without the contaminant, TCDD (7).


       TCDD occurs as a white crystalline solid.  It is

99.5$ decomposed at 800°C.  TCDD has the following solubility

in various solvents at 25°C (7).

                            • •

     • .Solvent                Solubility (wt. per cent)

     Acetone                  0.011                .
     Benzene                  0.057
     Dimethylsulfoxide       <0.01
     Methanol                 0.001
     Water     .   "  *'        0.00000002 (0.2 ppb)


       It has been recognized for quite some time that

chlorinated dibenzo-p-dioxins occur as possible byproducts

(contaminants) in the manufacturing of chlorinated phenols

(15).  The formation-of TCDD during production of 2,^,5-TCP

was demonstrated by Kimmig and Schulz (16).  TCDD was

obtained from the pyrolyzing of 2,4,5-TCP by Higginbotham
2.1  Since manufacturers are unable to produce 2,4,5-T
without TCDD, all references to 2,4,5-T in this docu-
ment refer to 2,4,5-T contaminated with some level of
TCDD.
                           -3-

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et al» (11).  They noted that the specific dioxin formed
depended on the chlorophenol pyrolyzed.  Kearney et al.
(17), however, reported that TCDD is historically associated
with any pesticide derived from 2,1,5-TCP.  A number of
researchers (12, 18, 19, 20, 21) have reported on the
formation of TCDD by thermal decomposition of the sodium
salt of 2,U,5-TCP under alkaline conditions during the
manufacturing process.

       Since 1950, most of the chemical industry has known
that large quantities of TCDD may be formed as a byproduct
of the 2,1,5-TCP manufacturing process if the procedures are
not carefully controlled."" At one time 2,4,5-T was produced
which contained between 30 to 40 ppm of TCDD (7, 22, 55).
Between 1968 and 1969, one manufacturer had a 90$ decrease
in the amount of TCDD present in the 2,4,5-T it produced.
Different manufacturers produced 2,H,5-T with different TCDD
contents (17).                              -    ;
       After concern arose in 1969 about the extremely toxic
effects of TCDD, manufacturing methods were changed and
carefully controlled b.y manufacturers.  By 1971 industry
had reduced TCDD content in commercial samples of 2,U,5-T to
less than 1 ppm (9, 23, 2*0.  Current U.S» manufacturing
                                        • .  . -
specifications require 2,M,5-T presently being sold to

                            -n-

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contain less than 0.1 ppm TCDD (7).  Several countries now

produce commercial 2,4,5-T containing less than.0.05 ppm
                                               •
TCDD (25).


     C. formulation and Class


       2,4,5-T is classed and used as a selective herbicide,
                                                             <
especially for brush control (2).  It is formulated in many

forms of salts and esters which are available as emulsifiable

concentrates containing 2, 4, or 6 pounds actual acid

equivalent per gallon and as oil soluble concentrates with 4

or 6 pounds active ingredient (AI) per gallon.  The most

commonly used formulations are the low volatile esters (26),
                                                         i
2,4,5-T also occurs in registrations mixed with 2,4-D,

Dicamba, Picloram, Silvex, and 2-(2-methyl-4-chlorophenoxy)

propiOTiic acid (27)«


 . .   D*  Registered Uses and Production


 	    2.,4,5-T has been produced as a registered pesticide in

the United States since 1948,  According to EPA records,

approximately 122 companies hold Federal registrations and .

formulate 424 registered products; eleven companies have

former state registrations-^ and formulate 21 products.
2i/  Pesticide products formerly registered under state
pesticide registration laws and shipped*or distributed
for sale solely within intrastate commerce are subject
to Federal pesticide regulations under  40 CFR Section
I62.1?(a).  Application has been made to obtain Federal
registration for intrastate use of these products.  For
a list of trade names under which 2,4,5-T is marketed,
see the registrant/product list.attached to this document.
                            -5-

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       Section 7(c) of FIFRA requires manufacturers and
formulators to submit to EPA information on production,
sales, and distribution.  Under FIFRA sections .7(c) and
10, this information may not be made available to the
public.  A confidential memorandum containing this informa-
tion has been sent to the Deputy Assistant Administrator for
Pesticides (28).  The Pesticide Review  (29) reported that
11,626,000 pounds of 2,4,5-T acid, esters, and salts were
produced in the United States in 1969 and 12,335,000 pounds
in 1970.  The Pesticide Review  (29) also reported that tl.>
United States imported 738,907 pounds of 2,4,5-T during
1971 through 1974.-^ Of this total 155,342 pounds were
imported in 1974.  This was down from nearly 392,000 pounds
in 1973 but up from the 5-year average  of 148,000 pounds.
While The Pesticide Review  (29) does not report export
figures for 2,4,5-T alone,  it does report exports of 2,4-D
and 2,4,5-T together.  Export of 2,4-D  and 2,4,5-T was
reported at 6.8 million pounds  in 1972; 21 million pounds in
1973; and almost 22 million pounds in 1974.     ;
       A great deal of variability exists in reports on
usage of 2,4,5-T.  Agricultural end-use data obtained
from the National Study of Agricultural, Governmental,
4/ The level of TCDD in the imported 2,4,5-T was not
reported.
                           -6-

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and Industrial Uses of Pesticides, conducted by this

Agency  (30), indicated the following uses of 2,4,5-T in

the United States in 1974.
Crop
Rangeland
Rice-
1
1
1
and Pastures 1

1
iKursery Crop I

[Turf and

1
Ornamentals 1
1
Blueberries- 1
1
[Estimated
I
total use 1
pounds AI
applied
968,000
..
16,000

12,000

200
.
8

996,000
in aqriculture for 1974 I
% total
aqriculture
97.24
1.54

1.20

0.02

-

100.00

a/  The Agency has looked at effects on aquatic organ-
isms representative of species likely to be exposed
from application of the triethylam.ine formulation of
2,4,5-1*to rice.  The calculated concentration of this
formulation in e 6-inch layer of water at the highest
recommended use rate is 0.9 ppm.  The LC-50 bioassay
values for bluegill and catfish are well above this
level (ranging from a 24-hcur LC-50 of 53 ppm for
bluegill to a 96-hour LC-50 of >72 ppm for bluegill
and channel catfish).  Rainbow trout, which cannot be
considered "representative of the organisms likely to
be exposed" in the geographic areas where rice is grown,
have a 9-6-hour LC-50 ranging from 0.7 to 0.07 ppm.
b/  This is no longer a registered use.

       In addition, this survey reported that 324,491

pounds of active 2,4,5-T were used by federal and state

agencies and 659,463 pounds by industry.


       Other sources have reported usages for 1974 as

follow: rights-of-way, 4 million pounds; rangeland, 1.5 to

2.3 million pounds; rice, 220,000 pounds; and forestry,

50,000 pounds.

                        -7-

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     E.  Metabolism in Experimental Systems

       Several studies have demonstrated that 2,4,5-TCP is
the primary degradation product or metabolite formed in the
breakdown of 2,4,5-T, by either physical or biological
mechanisms. Crosby and Wong (31) found that 2,4,5-TCP
was one of the major decomposition products in the photode-
composition of 2,4,5-T in water.  Sharpee  (32) found that
rcicrobial degradation of 2,4,5-T in culture, soil, and
aquatic ecosystems resulted in the formation of small
amounts of 2,4,5-TCP.
                             -7 a-

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       Shafik et al. (33) dosed Sprague-Dawley rats by

gavage with 2,4,5-T at 50, 5, 0.05, .and 0.005 mg/kg for

three days.  Two rats were dosed at each level.  The authors

found that, at 0.005 mg/kg, excretion of 2,1,5-T in urine

was complete two days after the final dose.  They also found
      *
2,^,5-TCP excreted as a metabolite in the urine of rats

given 50 mg/kg, but no detectable 2,4,5-TCP was found at the

two lowest dose levels.  A hydroxylated trichlorophenoxyacetic

acid and a hydroxylated trichlorophenol were identified, by

unconfirmed mass spectrometric analysis, as possibly being
                  • *  *
two additional metabolites of 2,4,5-T.


       Grunow et al. (3*0 studied seven male Wistar rats fed

a single 2,4,5-T dose at 50 mg/kg.body weight.  They found

that the daily renal excretion of free 2,4,5-T was, in

general, at its maximum on the second day after feeding.

After seven days, free 2,1,5-T in the urine decreased to a

value below 2% for all animals.  In addition to 2,4,5-T

excreted in the free form, the authors found it to be
                                                         •
excreted as derivatives which could be converted into

2,4,5-T by acid hydrolysis.  They were able to identify one

of these as N(2,4,5-trichlorophenoxyacetyl) glycine.


       Grunow and Bohme  (35), in a study using Wistar .rats

and KMRI mice, fed doses of 2,4,5-T at 200 mg/kg body

weight.  These authors isolated N(2,4,5-trichlorophenoxy

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acetyl) taurine as a metabolite of 2,4,5-T, in addition to


the metabolites named above.
                                   •



       Clark et al. (36) found residues of 2,4,5-TCP in the


muscle, liver, and kidney of sheep which were fed rations


containing 2,000 ppm of 2,4,5-T for 28 days.  The 2,4,5-T
      •

used in this study had a purity of 39% and contained no


detectable dioxin (detection limit!  0*5 ppm). -




       Leng (37) conducted a feeding study during 1969 and


1970, in which dairy and beef cattle and sheep were given


2,4,5-T at levels from 10 to 2,000 ppm in the total diet for


intervals of two to four weeks at each level tested.  The


author reported that no residues «0.05 ppm) occurred in


milk or cream of cows ingesting 10 to 30 ppm 2,4,5-T. At 100


ppm 2,^,5-T in the diet, traces of 2,4,5-TCP (0.06 ppm)
  ".*-..'•                        *

appeared in milk and cream.  When given high 'levels of


2,4,5-T, equivalent to 300 and 1,000 ppm in the total diet,


residues of 2,4,5-T and 2,4,5-TCP ranged from 0.05 to 0.5


ppm in the milk of individual cows*




       Fitzgerald et al. (38), studying the degradation


of 2,4,5-T in woody plants, reported that colorimetric


analysis suggested, and chromatographic analyses confirmed,


that the n-butyl ester of 2,4,5-T is degraded in sweet


gum CLlquidarobap stvraciflua) and southern red oak  (Ouercus


falcata) to yield 2,4,5-TCP.

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     F*   Environmental Fate

     (1)  £ e r 3 i s t e n c e ;   Soils
      *
       Soil surface and foliage are the major recipients of
phenoxy herbicides (39) whether applied by ground spray
systems or from aircraft.  Once 2,4,5-T reaches the soil it
Bay be degraded chemically or biologically, volatilized and
moved  to other areas, absorbed on soil colloids or in
organic matter, or leached to depths or locations where
it cannot be absorbed by plant roots (47),

       Norris et al. (176) reported on the persistence
of 2,4,5-T in a Pacific Northwest forest.  The authors
found  that six months after application of 2,4,5-T at 2.24
kg/ha  (2 pounds/acre),  the level of herbicide in the forest
floor  declined 90$; after one year, less than 0.02 kg/ha
remained in the forest floor*  The authors found little
leaching of 2,4,5-T from the forest floor into soil, and
no residues were found deeper than 15 cm (maximum residue
found  was 0.08 ppm) despite rainfall of 24 cm the first
month  and 70 cm the first three months after application.
Norris et al, (176) stated that the rapid disappearance
of 2,4,5-T from the forest floor suggests abundant mi-
crobial activity.  Norris (40) reported microbial ac-
tivity to be important in the disappearance of 2,4,5-T
from forest-floor material in the laboratory.

                           -10-

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       Wiese and Davis (11) found that, in an agricultural

soil, 2,1,5-T remained in the upper .six inches even after

application of 1.5 inches of water over a short period of

time.     ,
                                            \

      «
       Helling et al. (39) found that 2,4,5-T is relatively

mobile in sandy soils but that movement decreases as organic

content increases.  Thus 2,1,5-T is moderately mobile in

clay soils and only slightly mobile in muck (12).


       Yoshido and Castro (13) studied the degradation

of 2,1-D, 2,1,5-T, and Picloram in two Philippine soils

•under upland and submerged conditions. . The authors found the

degradation of 2,1,5-T to be rapid in Maahas clay.  Slightly

more 2,1,5-T residues were recovered in submerged than

in upland Maahas soil.   In Luisiana soil under submerged

conditions, 2,1,5-T degraded rapidly in eight weeks after a

four-week lag period, while it degraded gradually under

upland conditions, with only about 10? of the 2,1,5-T

recovered after 12 weeks.                        .


       Morton et al. (11), using technical grade 2,1,5-T

labeled in the carboxyl position with carbon-11, found that

its apparent half-life averaged 1.6 weeks in green tissues

of native grasses at College Station and Spur, Texas, and

1.7 weeks in litter tissue.  The authors stated that the


                           -11-

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amount and frequency of rainfall were conducive both to

leaching and microbial decomposition of the herbicide, and

to growth of sideoats gramma plants, all of which were

factors contributing to rapid reduction of herbicide concen-

trations.

     • * -                    .             '
       When considering the persistence of 2,4,5-T, the.

persistence of  its  manufacturing contaminant,  TCDD, must

also be considered.  Helling et al«  (39) found that TCDD  was

not  photodecoaposed on soil.  TCDD  was  found  to be immobile

in Norfolk and  Lakeland sandy loams, Hagerstown silty  clay

•loam, Barnes clay  loam, and Celeryville muck,  and was  not

.leached  further into soil  by rainfall  or irrigation.

During  surface  erosion .of  soil, however, lateral  trans-

port of TCDD could  occur.


        The  persistence  of  TCDD  in  Lakeland  loamy  sand  and

Hagerstown  silty clay  loam at  1,  10,  and 100  ppm  was  studied

by Kearney  et  al.  (46)  for 360  days.   After  one year  these

researchers  recovered  56  and  63$  of the originally  applied

TCDD in  Hagerstown and  Lakeland soils,  respectively.

Helling  et  al.  (39) observed  that  TCDD's persistence  was

predictable  since  it is  insoluble  in water.


      (2)   Persistence:   Water


        Current information indicates that,  although some

2,4,5-T  may  enter  streams  flowing through  or adjacent to


                            -12-

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areas being sprayed, residue levels in streams will be


very low.  Norris (47) reported the results of an intensive


study of stream contamination from spray projects on range


and forest lands in Oregon which showed that peak concentra-


tions of phenoxy herbicides seldom exceeded 0,1 ppm and that


herbicide residues persisted for only a few hours in nearly


all streams.  Norris (47) speculated, however, that applica-


tion of herbicides to marshy areas may result in high-level,


long persistence of chemical residues in nearby streams*



       The Report of the Advisory Committee on 2,4,5-T


to the Administrator of the Environmental Protection


Agency (48) stated that all available data indicated that


the amount of 2,4,5-T entering water is small and does not


persist long.  It is adsorbed on clay or absorbed by biota


within "a matter of days.                           ;



._. .     .Phenoxy chemicals entering water may be lost by


volatilization, degradation', adsorption on sediment, adsorp-


tion by biota, and dilution as additional stream water


passes through the site.  Almost all authorities agree that


there is adsorption on bottom sediment (48, 49, 50).



       Kenaga (51) stated that esters of 2,4,5-T in most
 •

kinds of water, except highly acidic waters, are usually


hydrolyzed within a matter of days.  When the 2-ethylhexyl




                           -13-

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'ester of 2,4,5-T was applied to water in the laboratory at a



concentration of 1 ppm for an hydrolysis study, 58% remained



after 4 hours; 33? after 8 hours; and \2% after 16 hours.





       Trichell et al. (52), studying the loss of herbicides



in runoff water, found 2 ug/ml of 2,4,5-T in runoff water 24



hours after it was applied at 2.24 kg/ha, after which 1.3 cm



of rainfall was simulated on sod-covered plots of 3% slope.



Four months after application, concentrations of 2,4,5-T in



runoff water had diminished to 0.04 ug/ml%






       Edwards and Glass (53) monitored runoff and percola-



tion of 2,4,5-T at Coshocton, Ohio, for 14 months following



application of 11.2 kg/ha of 2,4,5-T and found that 5»5



g/ha, or over 0»05? of the herbicide, was lost from the



treated area.  Host of the 2,4,5-T was removed in runoff



water during the first four months after application, and



more than half of the loss occurred the first month after



treatment.





       Kearney et al. (46) concluded that contamination



of underground water supplies with TCDD seemed very unlikely,



since vertical movement of TCDD did not occur in a wide



range of soil types.  The fact that no leaching occurred,



however, would not preclude runoff loss when soil erosion is



significant (39).





                            -14-

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     (3)  Jjraiisport


       Isensee and Jones (54) measured uptake of TCDD from

soil by two crop species.  Oats (Ayena sativa)- and soybeans

(Glvcine max) were grown in Lakeland sandy loam soil treated

with 0.06 ppm TCDD.  The concentration of TCDD in soil

was approximately 4,000 times greater than the amount that
                                         •
would be deposited in soil from an application of 2,4,5-T

(with 1 ppm TCDD) at a rate of 2 pounds/acre in the top

1/3 inch of the soil surface.  The tops of these plants

were harvested at intervals to maturity.  Mature oats and

soybean tops contained less than 1 part per billion (ppb)
                  •
TCDD.  TCDD vars detected (with a detection limit of 1 ppb)

in mature oat grain, while no TCDD was found in the bean of

soybeans.  The authors concluded that soil uptake of TCDD by

plants was highly unlikely, since little or no TCDD was

taken up by oats or soybeans under the conditions of this

experiment (54).


     (4)  Bioaccumulatjon


       Woolson et al. (55) conducted a study to determine if

TCDD residues could be detected in bald eagle (ftaljaectas

leucooephalys) tissue extracts, as a representative of the

top of a food chain.  Scientists at the Patuxent Wildlife
                                   t
Center (U.S. Department of the Interior, Laurel, Maryland)

collected, and furnished to these researchers, 19 bald eagle


                           -15-

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      r                                  •

carcasses from Alaska, Maine, North Dakota, Wisconsin,



Michigan, Minnesota, Arkansas, Illinois, Missouri, Maryland,



Virginia, Iowa, New York, New Jersey, and Florida between



1966 and 1971.  These states were selected as sampling



sites in order to provide a widely dispersed sample population.



The eagle tissues were prepared and extracted as described
     *


by Mulhearn et al« (56).  Woolson et al. (55) detected no



dioxin residues at a level of 0,05 ppm TCDD, the lower limit



of detection for most pesticides in tissue samples .run by



the Patuxent Wildlife Research Center at that time.  The



authors stated that the non-detection of dioxin residues



could imply that there was no dioxin build-up in the food



chain;  that the build-up was less than the [then] current



detectable level of 0.05 ppm [50 ppb]; that the eagles



examined were not contaminated although other samples might



be; or that other species could feed on a different .food



chain to accumulate dioxins.




       Isensee and Jones (57) exposed several organisms in



a model aquatic ecosystem to 1**C-labeled TCDD for up to 31



days to determine the distribution and bioacumulation



potential in the aquatic environment.  Soil containing from



                            1 J|
0.0001 to 7.^5 ppm adsorbed   C-TCDD was placed in  aquaria,



containing eight snails fPhvsa sp,), a few strands of algae



(pedogonium c_ardi_a_c.um_), and 10 ml of old aquarium water
                          -16-

-------
  containing various diatoms, protozoa, and rotifers.  Fifteen



  duckweed (L_emna minor) plants were also added to one aquarium,



  Samples of daphnids were taken for analysis at 30 days, and



  two aosquito fish (Gambusia affinis) were added to each



  .tank.  Three days later all of the organisms were removed



  for analysis, and two fingerling channel catfish (Ictalurus



  ounctatus) were'added to' each tank and exposed for six



  days*        .






         The authors stated that all organisms in both treat-



  ment and control tanks prospered during this exposure



 . period, indicating that TCDD was not toxic at the concentra-



  tions used*  TCDD ac-c'Officiated in all organisms.  At the



  highest TCDD concentration  (7*45 ppm) algae accumulated



 '. 6»690 ± 960 ppb TCDD; snails, 1,820 ± 170 ppb; daphnids,



  10,400 ± 480 ppbj and Gambusia, 1,380 i 220 ppb.  Catfish



^ were not analyzed for TCDD  residues*  At the second highest



  TCDD concentration (3.17 ppn), however, catfish accumulated



  720 ± 130 ppb TCDD.  The authors stated that accumulation in



  all of the test organisms from soil containing 0.1 ppb TCDD



  is important since this concentration approaches the concen-



  tration which would occur under normal field use of 2,4,5-T.



  The authors concluded that  the data  suggested that under



  certain circumstances (discharge of storm runoff from





                              -17-

-------
recently treated rangeland into a small pond), water-eroded


surface soil or debris may contain enough TCDD for measurable


residues (parts per thousand [ppt] quantities) to accumulate


in fish or other aquatic organisms.  However, the authors


speculated that TCDD, orginating from 2,4,5-T applications,


discharged into large lakes, streams, or estuaries would


probably become -sufficiently diluted so that no measurable


accumulation would occur.

                 • ^       '      '

       As part of a broad study to determine whether 2,4,5-T


use leads to TCDD accumulation in the environment, Shadoff


et al. (58) collected samples of fish, mud, water, and human
nilk from areas in Texas and Arkansas.  The Texas samples


of water, mud, catfish, and walleyed pike were collected


from the San Angelo Reservoir, an impoundment of the North


Concho River.  The authors stated that this watershed has
  "                        .                 - *

large acreages that have been sprayed with 2,H,5-T at 0.5


pounds/acre (2,4,5-T acid equivalent) for brush control.


These researchers also obtained six samples of human milk


from mothers residing in the general area of the San Angelo


Reservoir.  In addition, bass from a 125-acre pond in the


heart of the Arkansas rice-growing area were collec.ted..-


Water from this pond is- used to flood rice fields treated


with the equivalent of 1.25 pounds/acre of 2,4,5-T acid,


four to eight weeks prior to flooding.  The water is



                          -18-

-------
1 later drawn off the fields and pumped back into  the  pond  for



 re-use.  In addition, the pond i3  supplemented by water from



 wells and by water collected as .run-off  fron  surrounding



 rice fields during the rainy season.  The authors stated



 that this cycle had been in use  (including the proper  use of



 2,4,5-T) for 18 years up to the  time of  their study.



 The authors stated that no TCDD  was detected  in  the  tissues



 sampled, using a Gas Chromatography-Mass Spectrometry



 procedure with a detection limit which averaged  less than 10



 ppt. No  evidence was found that  TCDD is  accumulating in the



 environment from the use of 2,4,5-T described in this



 study*





      G«  Residues



      (1)  Soil





        Koolson et  al»  (55) studied Lakeland  sandy soil



 to determine if TCDD residues  could be detected  in  soil



 receiving exceedingly  large application  of 2,4-D and 2,4,5-T,



 The heaviest rate  of 2,4,5-T application was  947 pounds/acre



 applied  aerially during  1962 through  1964, while the



 lightest rate  was_jj50  pounds/acre  applied aerially  during



  1968 and 1969.  .During  this period, it was not uncommon



  for commercial samples  of 2,4,5-T  to  contain  levels  of



 30 to  40 ppm TCDD.





                             -19-

-------
       The authors were able to detect small amounts of



2,4,5-T in the soil samples.  They observed that the residue




level decreased with time after application and stated




that leaching and microbial decomposition cpuld account for




this decrease.  Using a detection limit of less than 1 ppb,




the authors did not detect any TCDD at any depth in 36-inch



core samples of the soil.






     (2)  Water






       In October 1965, the U.S. Geological Survey initiated



*a limited program of pesticide monitoring on 11 waterways




in the western United States (59)*  The streams, representing



agricultural areas where the probability of observing



pesticide residues would be greater, included the Missouri,



Brazos, Yellowstone, Sacramento, Colorado, Arkansas, Yakima,



Rio Grande, and Snake Rivers*  Pesticides chosen for analysis



included the insecticides aldrin, DDD, DDE, DDT, dieldrin,



endrin, heptachlor, heptachlor  epoxide, and lindane, and



the herbicides 2,4-D, 2,H,5-T, and silvex.  The authors



reported that no herbicide was found at any time at any



station during the first year of the sampling program*  The



lower limit of sensitivity (detection) was 5 ppt.






       Manigold and Schulze (60), reporting on the results



of the U.S. Geological Survey stream monitoring program for






                              -20-

-------
the two-year period October 1966 to September 1968f observed



that beginning in August 196? 2,4-D, silvex, and 2,4,5-T had



been detected frequently*  2,4,5-T was found in 28 of the



320 samples and ranged from  0,01 to 0,07 ppb.  The authors



stated that the established criteria permitted 100 ug/liter




(ppb) for herbicides.  These authors reported that the



analytical procedures were changed from the preceding report



to use Law's sample clean-up procedure, which permits



routine detection of pesticides at 0.005 ug/liter in most



waters*





       Norris (47) observed that peak concentrations of



phenoxy herbicides seldom exceeded 0*1 ppm in streams



contaminated from spray projects on range and forest lands



in Oregon,





       Lawson (61) studied 2,4,5-T residues in storm runoff



from three small watersheds in Arkansas*  Two watersheds,



one cleared and the other partially cut, were sprayed with



the isooctyl ester of 2,4,5-T,  A third watershed, adjacent



to the two treated ones, was used as a control.  Spraying



was done in September 1971, June 1972, and July 1973, either



to control woody sprouts and broadleaf vegetation or just to



provide herbicide application for-monitoring.  The cleared



watershed was treated with 4 pounds acid equivalent per acre



and the partially cut site with 2 pounds/acre,





                               -21-

-------
       In water samples taken after the first runoff-producing
storm in October 1971| Lawson (61) detected an average
of 2*1 ppm 2,4,5-T from the cleared watershed and 1*0 ppm
from the partially cut site.  Maximum amounts detected were
2«2 and 1.3 pptn for the two areas.  No 2,4,5-T was detected
from the control site*                    •

       Only trace amounts (less than 0*2 ppm) were detected
from each of the two treated sites after the next runoff-
producing storms in November 1971»  None was detected from
the control.

       In approximately 90 samples taken after storms during
the period December 1971 through September 1973, no 2,4,5-T
was detected by Lawson (61) in the runoff from the treated
or control water sheds,             .   '.'•'" :r

       Since TCDD is immobile in soil (39) and soluble in
water at only 0.2 ppb (7), the possibility of ground water
contamination is virtually nonexistent (.46)•  TCDD could be
present in runoff when soil erosion is significant (39), and
thus TCDD contamination of water bodies could occur.
       A recent National Academy of Sciences report on
drinking water stated that 2,4,5-T and TCDD have never b.een
detected in drinking water; the limit of detection was in
                            -22-

-------
the parts per trillion^  However, the report did project the



toxicity of 2,^,5-T and TCDD, their acceptable daily intake,




and suggested no-adverse-effect levels (62).






     (3)  lin





       Prior to 1970, phenoxy herbicides were widely



used for early postemergence control of weeds in wheat*



Johnson (63) reported that air samples collected during



spring and summer in the state of Washington where these




crops are grown contained as much as 0.06 ug/m^ 2,4-D. and




2,4,5-1* Assuming that a man—inhales about 30 m' of air per




day, the authors estimated that exposure to 0*06 ug/m  would



amount to inhalation of 1.8 ug phenoxy herbicide/day



or 0*025 ug/kg of body weight per day for a 70 kg man.





	   --Ambient air monitoring for pesticides in predominantly



agricultural areas of 28 states was conducted by the



National Air Monitoring Program in calendar years (CY) 1970



'through 1972 using ethylene glycol impinger type samples.



Table 1 records the arithmetic mean of residues of 2,4,5-T



detected in this program (6*0.
                            .23-

-------
Table 1.  Air Monitoring Data for 2,M,5-T in 28 State
1
\ Name of
\ State or Citv
1 Louisana
{Montana
{New Mexico
{Idaho
{Illinois
{Oregon
{Tennessee
{Tennessee
i Qklahoma
2,H,5-T Ester I
Monitored For !
Isopropyl esterl
i
i
i
BOEE {
{
{
Isooctyl ester {
!
•a
ng/m
CY -1970
-
ND
- .
ND
ND
ND
1.1
ND
ND
ng/m3
CY iq?l
ND
ND
ND
• ND
3.6
0.5
ND
2.7
in. 6
ng/m3
CY 1Q72
1.9
0.8
1.0
1.7
ND
ND
ND
ND
ND
ND = Not Detected,





     (H)  Animals               ;  .      .-





       Phenoxy acetic acids are relatively strong acids,



and animals rapidly excrete them unchanged in their urine



(36).  In their study of the fate of atrazine, kuron,



ailvex, and 2,U,5-T in the dairy cow, St.  John et al. (65)



found that dairy cows given 2,1,5-T and silvex in their feed



at 5 ppm for four days, completely eliminated both 2,1,5-T



and silvex as soluble salts in the urine two days after



dosing stopped.                  .





       Zielinski and Fishbein (66)  treated female C57BL/6



mice with a single subcutaneous injection of 100 mg/kg body



weight of 2,M,5-T in dimethylsulfoxide solution.  They



sacrificed the animals at various intervals after injection



and analyzed JLT^ toto for 2,U,5-T.  The amounts recovered as



percentage of the amount injected indicated decreasing



levels at the following time intervals after dosing:  at 0



hours, 77.1 ± 5.0J; at 16 hours, 56.9 ±. M.2%; and at 2M



hours 23.7 ±. 3.6J,

-------
       In a preliminary report of a two-year chronic


toxicity feeding study, Dow Chemical USA (110)'reported


the following residue data for rats fed indicated TCDD


doses:  24,000 ppt in liver and 8,100 ppt in fat of females


ingesting 2,200 ppt/day; 5,100 ppt in liver and 1,700


ppt in fat of females ingesting 220 ppt/day; and 540 ppt in


liver and fat of females ingesting 22 ppt/day*  The pre-


liminary report gives no residue data for treated males,


or for controls of either sex,




       Piper et al. (67) studied the fate of 2,4,5-T follow-


ing oral administration to rats and dogs*  Four groups of


three male and three female Sprague-Dawley rats (Spartan


strain) and two male and two female adult beagle dogs were


          '             14   • '  "   '
given single doses of   C-labeled 2,4,5-T by intubation


at 5, 50, 100, and 200 mg/kg body weight in rats and


5 mg/kg body weight in dogs.  The authors combined  data


obtained for males and females since the pharmacokinetics of


2,4,5-T were essentially the same in each sex»  In this


study, the clearance half-life for 5 mg/kg 2,4,5-T from dog


plasma  was 77.0 hours; in rats the half-life was 4.7


hours at 5 mg/kg anff" ^.^'hours at 50 mg/kg.  At doses of


100 and 200 mg/kg  body weight, the clearance half-life  for


rats increased to  19i4 and 25.2 hours,  showing  that the

-------
pharmacokinetics of 2,H,5-T varies with dose as well as with

species*  The authors suggested that the half-life values

at 100 and 200 ng/kg body weight indicated that these doses

may have exceeded the excretory capacity of the rats»



       Zitko (68) assayed  chlorinated dibenzodioxin residues

in aquatic animals, but was unable to detect these compounds

(detection limit:  0»04 ug/g [ppm] for TCDD) in any of

several aquatic animals from Canadian locations.  The author

had selected  species from high trophic levels of the

aquatic food web to measure  cumulative pesticide contamination*

More recently, using improved analytical methods for detection

of dioxin at ppt levels, Baughman and Meselson (69) found

mean TCDD levels ranging from 18 ppt to 810 ppt in fish and

crustaceans taken from Vietnamese rivers in August and

September 1970.  TCDD levels tended to be higher in fish
                                  *
from interior rivers than in those from seacoast locations.

In comparison, Baughman and Meselson found less than 3 ppt

TCDD in fish obtained in a market in Cape Cod, Massachusetts.

In another study, Matsumura and Benezet (70) placed TCDD-

coated sand directly in an aquarium containing brine shrimp,

mosquito larvae, and fish (silverside).  TCDD pickup was low

in fish (2 ppb) and brine shrimp (157 ppb) under the experi-

mental conditions.  But mosquito larvae, which are bottom



                              -26-

-------
feeders, showed a surprisingly high rate of pickup (4,150



ppb)«  The authors concluded that TCDD was not likely to



accumulate in as many biological systems as DDT because of



TCDD1s low solubility in water and lipids, as well as its



low partition coefficient in lipids,





     (5) Plants





       Clark et al* (36) reported that, when herbicides



are applied to rangeland, the levels of phenoxy herbicides



available for ingestion by grazing livestock depend upon



the nature and degree of cover, the rate and mode of applica-



tion, time after application, and climate conditions.



Studies by Morton et al. (44) showed that residues on grass



immediately after application of 2,4,5-T are not likely



to exceed 100 to 150 ppm for each pound of actual herbicide



applied per acre.                               '.'••...'-





       Leng (37) stated that herbicide residues in or on



plants declined rapidly, with a half-life of one to two



weeks, due to photodecomposition by sunlight, wash-off



by rain, metabolism by plants, and dilution from growth of



plants,  2,4,5-T was applied to grass in four states at an



application rate of 4 pounds/gallon, 3 gallons/acre;



initial residues immediately after treatment in California



averaged 684 ppm (or 57 ppm/pound applied per acre); 1,668






                              -27-

-------
ppm (or 139 ppn/pound) in Michigan; 1,H6H ppm (or 122



ppm/pound) in North Carolina; and 1,332 ppm or (111 ppn/pound)



in Texas.  After two weeks, residues in the four locations



averaged 26 to 3H ppm/pound per acre*  After 16 weeks, all



residues had declined to an average 3 ppm/pound applied per

     *                    •                        '

acre*
                   •                     .               *




       Baur et al. (71) treated grass species indigenous



to Victoria County, Texas, with 2 pounds/acre 2,1-,5-T ester.



One month after application the concentration averaged



4,060 ng/g (ppb) for 2,A,5-T acid and 2,890 ng/g (ppb) for



2,4,5-T ester*  Six months after application the concentra-



tion averaged 60 and 170 ng/g (ppb) for 2,M,5-T acid and


ester, respectively,              •





 •"'.     Getzendaner and Hummel (72)"*  described a 1969



study in which a 2,4,5-T propylene glycol butyl ether ester



formulation was sprayed on Texas-grass at an application



rate equivalent to 12 pounds of 2,M,5-T per acre; this rate



was 6 to 24 times the usual rate applied to grazing lands



for brush control. At this time, manufacturing  specifications
    Studies submitted by registrants as part of petitions

for residue tolerances are classified confidential, pending

outcome of litigation in U.S. District Court,
                           •28-

-------
for no detectable TCDD in 2,H,5-T used a method sensitive to

1 ppm.   The authors found that residues of TCDD decreased

rapidly from about 500 ppt TCDD within one day of application,

to about 35 ppt TCDD after four weeks, and about 15 ppt TCDD

after 16 weeks.  The TCDD decrease roughly paralleled the

loss of 2,1,5-T from the same grass,
  '''•-.'••*"*.•    •   *"
     (6) Humans-                          '

       Matsumura (73) studied 2,4,5-T in the blood and urine

of human male volunteers who had ingested the chemical*

After ingesting 150 mg (2.2 mg/kg),  the  plasma concentration

of 2,1»,5-T in one subject reached a peak of 2U1 ug/ml after

four hours.  A linear, semi-logarithmic concentration-time  .

curve (a gradient of -0.065) four hours post-treatment
indicated first order elimination and absorption kinetics,


       In a second part of this study, Matsumura gave
two male volunteers single oral doses of 100 mg 2,4,5-T»

Urine samples were collected over 72 hours.  About H5% of

the original dose was found in urine collected during

the first 21 hours after treatment;  60$ had been recovered

36 hours after treatment; and after 72 hours, more than 80%

of the original dose-of 2,4,5-T had been recovered,

       Gehring et al, (7^) also studied the fate of 2,4,5-T

following oral administration to man.  Five male volunteers,

                             -29-

-------
ages 31 to 58 years, each ingested a single 5 mg/kg oral .

dose of analytical grade 2,4,5-T, with a purity greater than

99J and less than the detectable level (0.05 ppm) TCDD,
directly or as a slurry in milk.  Blood, urine, and feces
were collected at intervals for up to  96 hours after
ingestion.  Essentially all (88.5 ± 5.1$) of the 2,4,5-T   .•
ingested by these subjects was excreted unchanged in the
urine after 96 hours*  The plasma 2,4,5-T concentration
increased rapidly following ingestion and after 7 hours -
reached a peak of approximately 57 ug/ml, after which the
plasma contained 65J of the 2,4,5-T in the body, of which
99? was bound reversibly to protein,
                                   *     .    .       -
       Kohli et al. (75) also studied absorption and
excretion of 2,4,5-T in man.  Eight male volunteers, age 25
to 35 years, received a single oral dose (2, 3, or 5       •
.mg/kg) analytical grade 2,4,5-T with a purity greater than
99£*  Urine was collected up to 96 hours, and blood samples
were collected up to 168 hours,   2,4,5-T was detected  in
some two-hour urine samples, indicating rapid excretion of
the compound.  More than half of the 2,4,5-T was excreted  in
.the urine in the first 48 hours, although small quantities
were still being excreted at 96  hours.
                             -30-

-------
       2,1,5-T appeared in all plasma samples  one hour




after  2,4,5-T ingestion, indicating rapid absorption.




Maximum concentration (approximately 25 ug/ml for the 5




mg/kg dose) was reached between 7 and 24 hours  after
                                       /



ingestion and began to decline at a first-order rate

                              »


after 32 hours,                         .

     *              ...        '"".."




       These investigators concluded that 2,4,5-T was



readily absorbed from the gastrointestinal tract, that it



was eliminated unchanged in the urine, and that the half-life



for plasma clearance was 18.8 ± 3,1 hours.  These authors



pointed out that, in general, higher recoveries were reported



by Gehring et al. (7*0 who used an electron capture detector,




.instead of the flame-ionization detector used in their



study.     .          •••;.'  .         -...••..
       The National Hunan Monitoring Program for Pesticides,



through its cooperative arrangement with the Health and



Nutritional Examination Survey II (Hanes II project), is



currently analyzing human urine samples for silvex, 2,4,5-T,



and 2,4,5-TCP (64),  The survey is scheduled for completion



in 1979, but some extremely tentative results are available.



No quantifiable 2,4,5-T residues have been detected in the



first  400 samples; however, trace amounts (<10 ppb) have



been found in a few samples,        :





       Dougherty and Piotrowska (177) reported on screening



of human urine for environmental contamination with toxic
                             -31-

-------
residues by negative chemical ionization mass -spectrometry.


The procedure is based on solvent extraction with minimal


clean-up followed by examination with negative chemical


ionization mass spectrometry for organochlorine residues and



related compounds with masses greater than 130 daltons*



Urine' for the screening procedure was obtained from students



at Florida State University (25 dorm residents; 21 football



team members; and 11 swimming team members).  The authors


reported that the limited survey of human urines indicates   *


contamination of the subjects with 2,4,5-T, pentachlorophenol,
                                                          •

other polychlorophenoxy acids, and numerous unknown compounds.


The authors indicated that 2,4,5-T was found in 36% (9/25) of


the dorm residents; 24? (5/21) of the football team; and 9%


(1/11) of the swimming team.  The authors attempted to define


the source of the contamination by applying the same


screening procedure to environmental substrates and suggested
                         *


the food chain (beef fat in the case of 2,4,5-T) as one


significant source of the contamination.                    .




     (7) Animal Products                 '              •.




       Kocher et al. (76) surveyed  beef fat from cattle


grazing on land where 2,4,5-T had been applied to determine


if TCDD was present in this tissue*   None of the 2,4,5-T


samples used were available for analysis for TCDD content.




                            -32-

-------
The authors did not know whether the samples were produced



before 1972 (when maximum allowable TCDD content was 1  ppzn)



or after 1972 (when maximum allowable TCDD content was 0.1


ppm).  None of the 16 samples from Sugarland, Texas, Missouri,



and Oklahoma showed TCDD residues when analyzed by a gas



chroaatography-mass spectrometry detection technique (detection



limits!  3 to 6 ppt).  Three of the eight samples from



Mertzon, Texas, where animals had grazed for 30 days in a


fenced pasture sprayed in its entirety with 2,4,5-T, gave


positive responses at the detection limit of 3 to 4 ppt TCDD.




        In another surveillance study, Mahle et al* (77)



analyzed milk from cows grazing on grass treated with


2,4,5-T in accord with normal agricultural practices.



Twenty-five samples were collected from different farms


in Oklahoma, Arkansas, and Missouri; these areas were


selected as representative of those where 2,4,5-T is used to


control broadleaf weeds and brush in pasture and rangeland.


Milk purchased in Midland, Michigan, an area where 2,5,5-T


is not used, provided control samples*  Based on gas


chromatography-mass spectrometry data (detection limit:-  1
                                         •

ppt), the authors stated that control samples were indistin-


guishable from the samples from treated areas and concluded


that TCDD was not present.
                               -33-

-------
         The residue levels reported in animal products in


  the studies cited below were obtained in laboratory

  feeding studies and not from animals grazing on pastures

  and rangelands treated at dosage rates recommended on


 .registered product labels.  Nevertheless, residues obtained


  in these feeding studies could occur in the environment and

  at these same levels since animals grazing on forage plants

  immediately after treatment at recommended rates of applica-

  tion could ingest 2,4,5-T in amounts similar to those fed in

  the studies.         _.       —


                           •  '       ~ .
         Leng (37) found no residues greater than 0.05 ppm in

.milk or cream of cows ingesting 10 to 30 ppm 2,4,5-T.  A.t

  100 ppm 2,4,5-T in the diet, traces of 2,4,5-TCP (0.06 ppm) -

  were found in milk and cream.   When the diet contained high
                             -34-

-------
levels of 2,M,5-T,  equivalent to 300 and 1,000 ppn in the
total diet, residues of 2,4,5-T and 2,4,5-TCP ranged from
0,15 to 0.5 ppm in  milk of individual cows.

       Leng T37)>  reporting on residues in meat and meat
byproducts, stated  that calves slaughtered after ingesting
     t
300 ppm 2,4,5-T in  the total diet contained average residues
of 0.12 to 0.28 ppm in muscle, fat, and liver, and 3.3 ppm
in kidney*  Animals fed 900 to 2,000 ppm 2,4,5-T in the
total diet and slaughtered without withdrawal had propor-
tionally higher average residues in tissue.  No residues rfer
detected (detection limit:  0*05 ppm) in most tissues when
animals were given  untreated feed for one week after they
had been on the highest levels (1,800 and 2,000 ppm) of
2,4,5-T for four weeks.  Residues of 2,^,5-T declined
rapidly in tissues  as soon as animals started to eat
untreated feed.

       Clark and Palmer (78) found 0.08 ppm 2,4,5-T in
omental fat of each of two sheep given four oral doses of
either 0.15 or 0,75 mg/kg of the propylene glycol butyl
ester of 2,4,5-T.   They also  found 368 ppm 2,4,5-T in
kidneys of animals  killed by four daily 250 mg/kg doses of a
2,4,5-T ester.

       Clark et al. (36) found 2,4,5-T no higher than 0.05
ppm in muscle or fat of sheep held one week on untreated
                               1
                            •35-

-------
feed. Residues of the metabolite 2,4,5-TCP wer-e not detected



in the fat of any of the aniraals4  They also found that the



2|4,5-T level in liver and kidneys was less than 0.05 ppm



after the animals were on untreated feed for seven days*






       Leng (79) found low levels of 2,4,5-T in muscle and




fat of calves .receiving 300 to 900 ppm 2,4,5-T in the diet



and much higher residues  in tissues of animals fed 1,800



ppm 2,4,5-T for 28 days*  Calves fed 300 ppm 2,4,5-T showed



0.12 and 0.28 ppm 2,4,5-T in muscle and fat, respectively.



Calves fed 900 ppm showed 0.24 and 0*38 ppm in muscle and



fat, respectively.  And at 1,800 ppm in the diet, calves



showed 1*2 and 2*0 ppm in muscle and fat, respectively.  In



this same study, Leng found relatively low residues of



2|JJ,5-T in liver at feeding levels of 300 and 900 ppm (0»2



and 1.0 ppm, respectively) and sharply increased residues



(7*9 ppm) at 1,800 ppm, indicating that the threshold level.



may have been exceeded at this higher dosage level*  Residues



of 2,4,5-T in kidney appeared to be proportional to the



level in the diet.





       Eighty-five samples of beef fat were analyzed



for TCDD content under the auspices of the EPA Dioxin



Implementation Plan (see Section II).  These beef fat
                            -36-

-------
 samples  included  18  samples  from  control  areas  and  67

 samples  from  areas previously  treated  with  2,4,5-T.

 Hone  of  the  18  control  samples had  detectable amounts

 of TCDD  at a  detection  limit of 10  ppt.   Of the 67  samples

 from  areas previously exposed  to  2,4,5-T, one showed a

 positive TCDD level  of  60  ppt;  two  appeared to  have TCDD  at

 20 ppt;  and  fiv.e  may have  had  TCDD  levels which ranged  from

 5 to  10  ppt»  The values for these  five  samples were at or

 below, the limits  of  detection  of  10 ppt.  Forty-three beef

 liver samples were analyzed  and showed no TCDD  residues at a

 detection limit of 10 ppt»


      (8) Food


       Evidence that very  little  2,4,5-T  gets into  food is

 seen  in  results of Market  Basket  Surveys  conducted  by

 'the Food ajxd Drug Administration  (FDA),   Of the 134 total

"diet  samples  involving  1,600 food composites (Market Basket
         <
 Survey)  analyzed  from 1964 through  April  1969,  only three

 contained 2,4,5-T*   Two were dairy  products containing  8  to

 13$ fat  with  0.008 and  0»19  ppm in  the fat.  A  single

 meat, fish,  and poultry composite from Boston consisting  of

 17 to 23? fat was found to contain  0.003  ppm 2,4,5-T on

 a fat basis  (81,  82, 83, 84)..                            •


       FDA Market Basket Survey samples  from 1969 through

 July  1974 showed  no  2,4,5-T  residues (detection limit:  0.02



                               -37-

-------
ppn) in 155 total diet samples involving 1,869 food composites




(85, 86, 87, 88, 89).





     (9)  Human Exposure via Industrial Accidents





       There have been a number of industrial accidents



during manufacture of chlorinated phenols that have resulted



in human exposure to TCDD.





       Whiteside (90) reported on a 19^9 explosion at a



chemical'plant producing 2,^,5-T in Nitro, West Virginia*



The release -of intermediate chemicals led to 228 cases of
                             \


chloracne among exposed workers,  Whiteside stated that



symptoms of effected workers-included skin eruptions,



shortness of breath, intolerance to cold, palpable and



tender liver, loss of sensation in extremities, damage to



peripheral nerves, fatigue, nervousness, irritability,



insomnia, Toss of libido, and vertigo*





       Goldmann (91) reported on a 1953 accident at a



2,^,5-TCP production plant in Germany.  Temperature and



pressure rose explosively in the autoclave, forming previously



unknown, very toxic chlorinated hydrocarbons; H2 persons



contracted serious cases of dermatitis, in which Hi persons



suffered consequent damage to internal organs, and seven



persons  experienced disturbances of the nervous system.
                          -38-

-------
A similar accident  occurred in Amsterdam in 1963 when an



explosion in a 2,4,5-T factory resulted in 50 workers



contracting chloracne (90).





       In 1954, 31 workers in a Hamburg,  Germany, chemical



plant producing 2,4,5-T from technical 2,4,5-TCP contracted



chloracne (10, 16, 92) and suffered the physical and psycho- .



logical symptoms associated with it (93)• Kimmig and Schulz



(10) extensively investigated the workers' conditions



and conducted experiments treating the skin of a rabbit's



ear with chemicals to which workers had been exposed.



These researchers tentatively identified  the causative agent



of the chloracne as TCDD.Bauer et al. .(15) conclusively



identified TCDD as the cause of chloracne,





       In 1964 workers in a 2,4-D and 2,4,5-T plant in



the United States developed chloracne (93> 9*0.  Eleiberg



et al. (94) found evidence of porphyria cutanea tarda (PCT)



of varying'degrees of severity in 11 out  of 29 workers.  PCT



had never before been described as related to chloracne, nor



had it been ascribed to industrial exposure in the United



States.  The authors stated- that either the finished chemicals



or some intermediate were responsible for both diseases.





       The Fine Chemicals Unit of Coalite and Chemical



Products Limited located at Bolsover, Derbyshire, in England



had been producing 2,4,5-TCP for nearly three years without





                          '  -39-

-------
 .Incident when an explosion occurred  at  midnight on April 23>



 1968*   As a result of this exothermal  reaction, TCDD had



 accidentally been produced*   Workers at this'plant were



 accidentally exposed to TCDD,  and  79 cases of chloracne were



 recorded, many of them severe  (9»  95K





        Beginning in May 1971  an accidental poisoning episode



 occurred in the United States  that affected humans,  horses,



 and other animals*  The exposure was related to the  spraying



 of waste oil, contaminated with TCDD,  on riding arenas  to



 control dust%  Three days after spraying,  sparrows and



 other  birds were found dead  on the arena floor*  Of  85



 horses exercised within the  arena, 62  became ill,  and 48



 died*   The first horse died  on June  20, 1971%   Horses



 continued to die as late as  January  1974,   Human illnesses



 were less severe, but did include  one  case of hemorrhagic



 cystitis in a 6-year-old girl  who  frequently played  in  the



-ar«na.  Analysis showed the  arena  contained 31.8 to  33,0



 ug/g TCDD (96, 97, 162),                              .





        Beale et al, (98) presented follow-up information on



 the 6-year-old girl involved  in this accidental poisoning.



 These  authors stated that the  girl's symptoms resolved  in



 three  to four days and did not recur.   Results of a  repeat



 voiding cystogram three months later appeared normal,



 Cystoscopy at this time did,  however,  demonstrate numerous



 punctate haemorrhagic.areas  in the bladder, especially  in





                          :   -HO-

-------
the region of the trigone*  Five years later, an investiga-




tion showed that this girl had grown normally;- results of a



physical examination, including a detailed neurological



examination, were normal,  Cystogram and liver-function



tests were also normal, as was the urinary excretion of



uroporphyrins, coproporphyrins, and thyroid function,






       On July 10} 1976, an accident at the ICMESA chemical



plant in the Seveso Region of Italy released 2 to 10 pounds



of TCDD over a wide area (90, 99» 100)»  Hundreds of animals



died, many area residents reported skin disorders, and an



area of 110 hectares was evacuated (101),  Reports of the



immediate symptom^ _and^indications of many long-term effects



are just becoming available.





       Seveso inhabitants initially experienced numerous,



burnlike skin lesions which gradually  receded; Whiteside



(90) believed this type of lesion was probably due to direct



contact with the sodium hydroxide and phenolic components of



the fallout.  Two and a half months after the explosion,



however, children and young people in the zone most affected



by the fallout developed symptoms of true chl.oracne, a sign



of dioxin poisoning, on their faces,-arms, and bodies*  By



November 1976, 28 people had developed confirmed cases of



chloracne, and the number rose to 38 by December 1976; one



year later, the number of confirmed cases of chloracne was



130.

-------
       A number of Seveso women were pregnant at the

time of the accident,  Whiteside (90) reported that the

number of legal and illegal abortions performed after the

accident probably totalled 90» Results of a survey by an

epidemological commission showed that 183 babies were

delivered in the two months following the accident, and that

there were 51 spontaneous abortions as distinct from induced

abortions (approximately double the rate of spontaneous

abortions previously reported for the area)^  Whiteside

(SO) reported that eight cases of birth abnormalities have

been noted to. date among babies born to women in the Seveso

area who were pregnant at the time of the explosion.

Physicians in the Seveso~~area have had difficulty relating

this directly to the explosion, however, since this incidence

of birth abnormalities was not disproportionate to the usual

incidence of abnormal births,



     H,  Tolerances


       There are no tolerances established for 2,4,5-T in or

on food crops. Likewise, no tolerances have been set

specifically far—TCDD--i-a—or--on food crops.  However, 40 CFR

Section 180,302 does establish a tolerance of 0.05 ppm for

hexachlorophene on cotton seed (a nonhuman dietary food
• *
item), with a stated limitation that the technical grade


                            -42-

-------
 hexachlorophene  used  in  the  formulation  shall  not  contain

 more  than  0»1  ppn  TCDD«   The limitation  does hot  constitute

 a  tolerance  (102).


      1. •" pesticide Episode Reports  System  (PERS)


       EPA's Pesticide Episode  Response  Branch of  'the  Office

 of Pesticide Programs maintains a Pesticide Episode  Reports

 System  (PERS)  which collects reports  of  pestibide  exposure

 affecting  humans,  domestic animals, livestock, and wildlife

 (103)%   According  to  their records, there  were 96  episodes

 from  1966  to April 1977  involving 2,4,5-T*


       Many  of these  96  episodes recorded  effects  in more

 than  one area  of the  environment*   Plant damage was  reported

 60 times,  effects  on  humans  16  times,  water contamination

 .14 times,  effects  on  domestic animals  and  soil contamination

 7  times  each,  general environmental contamination  3  times,
                                                    V"-V. *•
-an-d fish kills and complaints against  use  of 2,4,5-T twice

 each.


        There was substantial evidence  in 13 of the 96

 episodes link-ing 2,4,5-T to  the episode's  effects; there was

 circumstantial evidence  in 20 of the  episodes  for  involvement

 of 2,4,5-T;  there  was insufficient  evidence in 62  of the

 episodes to  prove  or  disprove involvement  of 2,^,5-T;  and

 one episode  had no verification status listed.


                             -H3-

-------
        Of the 13 episodes for which there was substantial




 evidence linking 2,4,5-T to the episode's effects, two



. involved humans (including one suicide); 2,4-D was also



 involved in both episodes.  Three episodes involved plant



 damage from drift of herbicides; 2,4,5-T residues were



 found in plant samples in two episodes; 2,4-D was also



 involved in one of these episodes.  Two episodes involved



 fish kills resulting from accidental spills into streams,



 with 2,4-D involved in both incidents; in one of these



 episodes, 6,000 fish (90$ juvenile salmon) were killed;



 residues of both 2,4-D and 2,4,5-T were found in these fish,



 Two incidents involved soil contamination when two warehouses



 were destroyed by a tornado and fire; many other pesticides



 were Involved In both instances. Two episodes involved



 domestic animals; in one, 24 cows died after herbicide



 application.  Arsenic residues were found in two cows,



 and arsenic contamination of the herbicide mioc was suspected,



 In the other instance, 8 cows drank water contaminated with



 2,4,5-T; residue levels of 0.03 and 0.02 ppm were found in



 the milk five and eight days, respectively, after the



 incident.  Two hundred and forty gallons of milk were



 dumped.  One incident involved water contamination as a



 result of a warehouse fire; many other pesticides were also



 involved*

-------
 II.  KECULATORY HISTORY



        2,4,5-T was developed during World War-II and was



 first registered as a pesticide on March 2,  19^8 (3)»  Since



 then, it has been the subject of several Federal regulatory




 actions.





        On April 13, 1966, the United States  Department of



 Agriculture (USDA) and the Food and Drug Administration



 (FDA) published an announcement in the Federal  Register



 abolishing the "No Residue and Zero Tolerance"  concepts as



 scientifically untenable*  Future registrations would be



 granted on the basis of either "Negligible Residue" or



 "Permissible Residue,"  Industry was given until December



 31, 1967, to comply by obtaining tolerances  for residues of



 2,^,5-T in all treated food, feed products,  and byproducts



*.(in addition no registrations would be continued beyond



 December 31, 1970).





        Following this action, a series of Pesticide Registra-



tion (PR) Notices were issued over several years, extending



 certain "no residue" and "zero tolerance" registrations



 beyond the December 31, 1967, deadline for obtaining



 residue tolerance,  (These and all following PR Notices



 are cited in Reference 104,)  Among uses of 2,4,5-T extended



 beyond the deadline were uses on pasture grasses and



 rangeland; on apples (Mclntosh), blueberries (low bush),



 cereal grains (undesignated), rice, and sugarcane; and in



 lakes and ponds*

-------
       PR Notice 70-8 issued by the USDA on March 10, 1970,




identified data needs for certain compounds* .'2,4,5-T




was identified as one of the compounds requiring further




teratogenic studies*






       PR Notice 70-11 published on April 20, 1970, suspended




2,4,5-T products bearing certain directions for use.



The suspended uses were all uses in lakes, ponds,' or on



ditch banks; and liquid formulations for use around the




home, recreation areas, and similar sites*






       PR Notice 70-13 issued by the USDA on Hay 1, 1970,




cancelled 2,4,5-T products bearing certain directions




for use.  The cancelled uses were all granular 2,4,5-T



formulations for use around the home, recreational areas,



and similar sites; and all 2,4,5-T uses on food crops



intended for human consumption.                           -





       All registrants wera advised of these actions, and



two of the 2,4,5-T registrants, Dow Chemical and Hercules



Incorporated,- excercised their right under Section 4(e) of



the Federal Insecticide, Fungicide, and Rodenticide Act



(FIFRA) [7 U.S.C. 135 et seq.] to petition for referral of



the cancellation (rice use only) to an Advisory Committee.






       As provided by Section 4(c) of FIFRA (1964 amendment),



& nine-member Advisory Committee of scientists was appointed






                            -46-

-------
to consider all relevant facts, submit a report and recommen-


dations regarding registration for certain uses of 2,4,5-T,


and state the reasons or bases for these recommendations.


Their report was submitted to the Administrator of the


Environmental Protection Agency on May 7, 1971 (48)*  The


Committee recommended that use of 2,4,5-T be permitted in


forestry, range land, and rights-of-way providing that the


limit of 0.1 ppm of contamination with TCDD be set for all


future production of 2,4,5-T; that 2,4,5-T be applied no


more than once a year at any one site; and that 2,4,5-T be


applied with proper caution so that it will not contaminate


other areas where it may come into contact with humans,



       The Committee also recommended that this action be


reviewed again when existing deficiencies in information


about possible magnification of TCDD in the food chain


have been'rectified by  specific research.



       In the meantime, PR Notice 70-22, published by the


USDA on September 28, 1970, addressed the presence of


chlorodioxin contaminants in economic poisons.  This notice


stated that  the BJS.DA had determined that certain toxic


chlorodioxins  (such as  TCDD) may be present as contaminants


in the basic materials  used in formulating 2,4,5-T and


silvex.  The notice also stated that  the presence of such
                                           f



                            -47-

-------
chlorodioxins constituted a possible hazard to nan since they



had been found to be extremely toxic to laboratory animals,



and that appropriate regulatory action would be taken under



provisions of FIFRA since products containing chlorodioxins



are considered to be in violation of FIFRA%






       Dow Chemical obtained an injunction against EPA in



July 1972, enjoining further administrative action against



2,4,5-T*  The United States Court of Appeals for the Eighth



Circuit overturned the injunction in 1973, and administrative



proceedings were allowed to go forward.






       On July 20, 1973, a notice of intent to hold public



hearings on all uses "o'f ~2,4,5-T was filed with the EPA



Hearing Clerk under Section 6(b)(2) of FIFRA, as amended



1972*  All federally approved uses of 2,4,5-T were to be



explored in a public hearing scheduled for April 1974,



following completion of an intensive monitoring program for



detecting dioxin in the ppt range (38 FR 19869, July 29,



1973)*





       On May 10, 1974, the information hearing was expanded



to include all ins-ecticides and herbicides having 2,4,5-TCP



In their manufacturing process.  These included silvex,



erbon, and ronnel, as well as 2,4,5-T and 2,4,5-TCP, all



of which may contain TCDD.





                               -48-

-------
       On June 24, 1974, EPA withdrew cancellation and




information-gathering proceedings initiated against 2,4,5-T



and related compounds because of its inability to monitor



food for TCDD residues with the necessary analytical



precision.  Although the 2,4,5-T notice of hearing was



withdrawn, the Agency stated that it "will continue its TCDD



residue monitoring program and will take such further action



as it deems appropriate once the results of the monitoring



project are available" (39 FR 24050 June 28, 1974).



       On July 25-26, 1974, the Agency held a Dioxin Planning



Conference in Washington, D.C., primarily for those parties



having an interest in the withdrawn 2,4,5-T/dioxin hearings,



to address data analysis and retrieval (in the areas of



analytical methodolgy, toxicology, and monitoring) with



emphasis on analytical methodology for TCDD at the ppt



level.  As a result, the Agency established a Dioxin Implemen-



tation Pla-n (DIP) intended to identify a preferable analytical



methodology to monitor human and environmental samples for



JCDD.



       On-going TCDD studies under the DIP include:  an



analytical method validation study to produce statistically



defensible data; monitoring for resioues in human milk in



the Pacific northwest; additional beef fat residue studies;



                        -49-

-------
additional technical pesticide residue studies; and an




environmental monitoring program for TCDD residues in soil,



water, and biota*






III.  SUMMARY OF SCIENTIFIC EVIDENCE RELATING TO




               E PRESUMPTION                  '
       The following adverse effects of 2,4,5-T and/or



TCDD have been found to exceed the criteria for issuance of



a rebuttable presumption as stated in Section 162.11 of the



Code of Federal Regulations (CFR 40)«  Because of industry's



apparent inability to produce 2,4,5-T without TCDD contamina-



tion, none of the studies cited are for pure 2,4,5-T.  The



effects of TCDD must also be considered when assessing



2,4,5-T by the Agency's risk criteria*





'•' ..  A»  pncogenic Effects         .'    .. '_ ' .





       40 CFR Section I62.11(a) (3) (ii) (A) provides that a



rebuttable presumption shall arise "if a pesticide's



ingredient(s)... (i)nduces oncogenic effects in experi-



mental mammalian species or in man as a result of oral,



inhalation or dermal exposure...."  Section 162.3(bb)



defines the term oncogenic as "the property of a substance



or a mixture of substances to produce or induce benign



or malignant tumor formation in living animals."
                         -50-

-------
       The studies summarized below indicate that 2,4,5-T

containing less than 0.05 ppm TCDD and/or TCDD alone have

oncogenic effects in two mouse strains  and one rat strain.

Since 2)4,5-1, as currently formulated, contains TCDD (at a

maximum amount of 0.099 ppm), a rebuttable presumption

against the registration of 2,4,5-T products has arisen

because of the oncogenic effect of 2, 4,5-1 and its contami-

nant, TCDD,


     (1)
       (a)  Effects of Dietary _2,ltf5-T «0.05 ppm TCDD)

            on Rodents



       In their bioassy of 2,4,5-T for carcinogenicity in
                               .«z
mice, Muranyi-Kovacs et al* (105) administered 2,4,5-T


(containing <0.05 ppm TCDD^'to inbred C3Hf and XVII/G mice.

The mice were given 100 mg/liter of 2,4,5-T in the drinking

water for two months beginning at six weeks of age.  During

the succeeding 15 to 20 months, the mice were given 2,4, 5-T

mixed in the diet at a concentration of 80 ppm ad libitum.


      ' In C3Hf mice, 48* of the treated females (12/25)  and

55$ of the treated males (12/22) developed tumors, compared

with control values of 21 J (9/44) and 49* (21/43), respec-

tively (Table 2)%  The differences between the number of

tumors observed and the number expected were significant for

female mice at all sites (p < 0.03) and for the combined sexes
    This TCDD level is less than the 0.1 ppm TCDD currently
found in most commercial formulations (see Section I.B).
                           -51-

-------
                     7/
         (p < 0.01).     For  non-incidental tumors,  the differences

         were significant  for   each sex  and the  combination;  no

                                                                      8/
         significant  differences were  found in incidental tumors.

         No other  strain-sex combination yielded  statistically

         significant  values  (106).  Rare types of tumors, not seen in

         the control  animals,  were observed in the  treated C3Hf

         females.

               Table 2.  "Oncogenic Effects  of 2.4.5-T on Mix



•t^ain
C3HF


•
VII/G


^^
*
| ! Dietary!
I j Level !
i ; i

i M i 0 ,'
i i 80 !
i F i 0 i
! ! so i
IM! o j
! i so i
IF! c !
II 1
1 i On '
i i OU i
Mean
Survi-
val Timej
fdavs)
630
51lJc/
680
620
521 -
583
569
. •
641^
Mice with
and Lung
Leukemia
and Liver
Tuaors !
No/Total
21/43
12/22
9/44
-^272-.
25/32
15/20
21/40

16/1Q
No^i *
149
!55
121
	 (48
J78
i
}75
,'53
1
!8a






Incidence of
Total
• 22
13
9
n
27
16
24

16
i i
! Lunc 1
i 2 j
i - i
! 5 !
! - i
j 22 j
1 1
! 20 !
I |
f 15 f
i
Liver !
19 I
10 i
3 i
4 !
4 i
-- |
— i
1
__ i


Tunors
i
Leuker">.a !
t
— — i
2 1
1 !
I
T t
- 1
1 i
2 j
i
"1 f
i
i
:
Other1
id/ ;
• i
1-' I
— !
6£/ |
\&/ i
• i
217 i
i
_— '
  Data from Kuranyi-Kovacs (105).
  Estimated daily oral  dose = 12 mg/kg body weight.
  Effective number of mice are mice surviving longer than 300 days or developing a tumor
fore 300 days of age.
 J>leomorphic salivary  gland tumor.                '                      •
  ribrosarcoma; one hyperplastic urinary bladder and one hyperplastic forestomach not
eluded.
  One osteogenic sarcoma; two sarcomas; two cutaneous tumors; one cervical tumor.
  Forestomach tumor.
  Urinary bladder papilloma; two hyperplastic lesions of'urinary bladder not included.
 ^"wo hemangiomas.	^	t_. _^__  __            .'            •
  p < 0.01 compared with controls.     ~~ '   ""-.        	
  p < 0.001 compared with controls.
   The investigators found  no significant sex-related
   Incidental  tumors are  tumors discovered at necropsy
  an  animal which died from  some other  cancer; non-
 eidental tumors  are tumors  diagnosed during life  or
 Ich  caused the  death of  the animal.
                        -52-

-------
       A decrease in survival time for mice with tumors was




noted in both male and female treated C3Hf mice when compared




with controls.  C3Hf treated male mice survived an average



of 511 days compared with 630 days for control male mice.



According to the evaluation by EPA's Carcinogen Assessment



Group [CAG] (106), this difference was significant (p <0.001)



Treated female C3Hf mice survived 620 days compared with 680




days for control females.  Chemically induced oncogenic



effects typically show long latency periods.  The finding




of reduced longevity among treated animals as compared




with controls complicates the assessment of the potential




oncogenic effects of 2,4,5-T.






       In XVII/G mice, 84? of the treated females (16/19)



and 75? of the treated males (15/20) developed tumors,



compared with control values of 53? (21/40) and 78? (25/32),



respectively.       •        ~.        .    .       .   '. - .   .   •_"






       An increase in survival time for mice with tumors



over controls was noted among the XVII/G treated animals.



There was an average survival time of 583 days for treated



male mice compared with 521 days for control male mice.



Treated females survived 641 days compared with 569 days for



control females.  According to CAG (106), the difference



was significant (p < 0.01) in females.






                        -53-

-------
       (b)  Effects of. Subcutaneous Injection and Oral

            Administration of 2.4.B-T (30 Dom TCDD)
                 *
            on Rodents


       Innes et al, (107) studied the tumorigenicity of

2,i7.5-Tf containing about 30 ppm TCDD, in two hybrid

strains of mice, designated as "Xn and "Y", after Oral or

subcutaneous administration of the maximum tolerated dose

(Table 3)»  The testing was performed at Bionetics Research

Laboratories, under contract from the National Institutes

of Health*  Results of the studies were calculated comparing

treated groups with matched and pooled controls.%/


       In the subcutaneous study, mice were given a single

injection of 21,5 mg/kg of 2,4,5-T in a dimethyl sulfoxide

(DMSO) solution at approximately 18 months of ageo  Seventeen

percent (3/18) of the treated "Y" males developed pulmonary

adenomas, compared with 1J (1/71) of the matched controls and

3% (1/122) of the pooled controls*  This increased incidence

of pulmonary adenomas was significant relative to -both con-

trol groups [p = 0.024 matched and p = 0,04 pooled] (106)»


       In'the oral study, 21.5 mg/kg of 2,4,5-T in gelatin
                                      /
was administered daily by stomach tube, beginning at seven
Si/  Because this was a large scale screening study,
several control groups were used.  No significant dif-
ferences were found among these groups*
                          -54-

-------
days of age.  After weaning, 60 ppm of 2,4,5-T  was mixed



In the diet and provided ad Xi_bi_t_um until  the end of  the



study at approximately 18 months.  Gross and histological



examinations were made of all major organs  and  visible'



lesions; thyroid glands were not examined.  According to



CAG's evaluation (106), there were no significant differences



between 2,1,5-T treated and control groups  of mice with



respect to tumors at specific sites or total number of



tumor-bearing animals*
Table
                  Tumors in Mice Ineestine_


StrairL
X


•






Y









1 ! ! Mice with Specific Tusors
jDose
S3x! (orn)
M ! 0
S (matched)
1 o
! (pooled)
! 60
F ! 0
! (matched)
; o
{(pooled)
! 60
M i 0
! (matched)
! 0
!( pooled)
! 60
F j 0
\ (matched)
i 0
! (pooled)
Mice with Tumors iReticulum Cell! Tumor Tvpe Pumonaryj
No/Total Mo! 5 ! Sarcoca ! Adenoma & Carcinoma iHeoatoma
5/15 ! 33 i 0
! !
22/79 ! 28 ! 5
! i .
6/18 ! 33 ! 1
2/18 ! 11 ! 1
i i ;;
8/87 ! 9 i 4
! !
1/81 ! 6 ! —
3/18 ! 17 i —
! !
16/90 i 18 ! 1
i !
3/18 ! 17 i 2
1/15 I 7 i 1
i !
7/82 ! 9 i 3
\ \
! 60 ! 2/18 ! 11 ! 1
2 i 3

5
' .-- ' •- .':."•
1
1

3

1
3

10

' ~_
— —
"
3

—

8

4
• _
•



—

5

1
—

1

— !
                      -55-

-------
    . (2)  TCPP



       (a)  Qncqgenlc Effects of Low Levels of

            on Rodents              .



       Van Miller et al» (109) recently reported the results

of a two-year feeding study with male Sprague-Dawley rats.
                                       t
Ten groups of ten animals per group were  fed ground chow


containing  0, 1, 5, 50, or 500 ppt (= 10"12 gram TCDD/gram


food), and 1, 5, 50, 500, or 1,000 ppb ( = 10   gram TCDD/gram

food) TCDD.



       Food intake (10 i 4 g/day) was significantly lower in

rats ingesting the three highest dose levels (50, 500, or

1,000 ppb TCDD) than in controls (21 ± 2  g/day), and none of

the rats in these' three groups gained weight after the start

of the experimental diet.  All rats receiving these three

dose levels died between the second and fourth week of

treatment*          .  .

                                      1
       On the other hand, food intake for rats on other dose

levels was similar to controls "(20 ± 2 g/day)»  Weight

gain was significantly less only for rats given 5 ppb TCDD

(391 ± 54 g) as compared to controls (531 ± 44 g)»  In these



                               -56-

-------
seven groups only one animal died before the 30th week, and

that death occurred in the 500-ppt group at the l?th week.

In the 5- and 1-ppb groups, all animals died by the 90th

week of the experiment.  Table U shows the mortality figures

for all groups.
)>./
Si/
£/
£./
Jl/
j./
      Table 4.  Mortality in Rats Ingesting
                        Levels of TCDD
!
Dose I
J2/ i
1 ppt*7 1
5 ppt" !
50 ppf2-7 !
5 0 0 p p u !
1 ppb*7 i
ii/ J
5 ppb i
4 / 1
50. ppb i
500 ppb-17 !
1 , 000 t>ob~" !
^Veek of ..
First Death
68
86
33
69
it".
31
31

• • '-'3 ..."
2 - •"• '-
2
iNo, Rats Dead
! at QSth Week-7
I 6/10 (60*)
! 2/10 (20*)
! 4/10 (40*)
! 4/10 (40*)
5/10 (50*)
! 10/10 (100*)
! 10/10 (100*)
i
j. 10/10 (100*)
i 10/10 (loo*)
1 10/1.0 (100?)
I
1
t
1
i
1
1

1
j
1
1
1
1
1
1
Surviving animals sacrificed at 95 weeks.
Control group.  Diet contained no TCDD.
Approximate weekly dose was 0.0003 ug/kg body wt,
                              001 ug/kg body wt.
                              01 ug/kg body wt.
                              1 ug/kg body wt.
                              4 ug/kg body wt.
                              0 ug/kg body wt.
    Approximate weekly dose was
    Approximate weekly dose was
    Approximate weekly dose was
    Approximate weekly dose was
    Approximate weekly dose
    Approximate weekly dose
                                0
                                0
                                0
                                0
                            was 2
                            was 24 ug/kg body wt.
    Approximate weekly dose was 240 ug/kg body wt.
    Approximate weekly dose was 500 ug/kg body wt.
                       -57-

-------
      ' Laparotomies were performed on all rats surviving


through the 65th week, and all tumors observed were biopsied.

Rats were maintained on these diets until the 78th week and

were then placed on the control diet.  Surviving animals

were killed at 95 weeks.  Complete necropsies were done at

death or sacrifice, and tissue samples were microscop-

ically examined.  Special staining methods were used to "aid

in the diagnosis of neoplasms*"



       Tumorigenic and toxic effects were observed  in rats

in the six lowest dose groups.  The overall incidence

of neoplasms in the six experimental groups was 38? (23/60),

compared with 0% Co /TO ) In—the control group.  The difference

is statistically significant (106).  Neoplastic nodules and

cholangiocarcinomas of the liver were observed in 40? (4/10)

6f the rats ingesting 5 ppb TCDD; two animals had both

neoplastic nodules of the liver and cholangiocarcinomas.
.                " i
One rat (10J) in the 1 ppb group had hepatic carcinoma

compared to none of the controls.  Hepatic tumors were not

found in other dose groups (Table 5).
    Table 5.  Liver'Togror's 'In Rats Ingestin
1
JDose (orb)
i 0
I 1
i ,
{ Rats With
I Neoplastic
! Nodules
! No. ! ?
! 0/10 i o
I 0/10 ! o
| | h/
fiats With
Cholangio-
carcinoma's
No . ! I
0/10 ! 0
1/10 j 10
2/10 I 20-k'
Nodules plus
Carcinomas
No. i ?
0/10 ! o !
1/10 ! 10 j
a/io ! 4o-x 1 '
    Data  from Van Miller  (109).
Jb_/  Two animals had  both  neoplastic nodules of  the liver
and cholangiocarcinomas,


                           -58-

-------
       Tumors developed in M6J (23/50) of the rats ingesting




5, 50, or 500 ppt and 1 or 5 ppb TCDD, compared to none



(0/10) in the control rats*  Van Miller et al* noted that



"nineteen (57?) Csic - Agency calculation is 5W (19/35)3



of the animals that died in the six groups fed subacute



levels of TCDD had neoplastic alterations."  Carcinomas were



observed in the ear duct,  kidney, and liver.  Three retriperi-



toneal histiocytomas were  described as metastasizing to the



"lungs, kidney, liver, and skeletal musculature*"  According



to CAG's evaluation (106), statistically significant increases



in tumors at all sites were found in rats fed 5, 500, 1,000,



and 5,000 ppt as compared  with control'animals (p=0.05)



[Table 6],  Three .of the ten deaths which occurred in the



5-ppb dose group were attributed to apiastic anemia.  One



animal in the 500-ppt group had a severe liver infarction,





  ;     Dow Chemical USA (110) has provided EPA with a



preliminary report of a study of TCDD's chronic toxic effects



in Sprague-Dawley rats* Groups of 50 rats of each sex were



fed 0.1, 0«01, or 0.001 ug TCDD/kg body weight daily for two



years*  To provide these dose levels, the concentrations of



TCDD in the diet were approximately 2,200, 210, and 22 ppt*



Eighty-six animals of each sex were used as controls.





       Dow (110) reported "discernible increases" in the



incidence of hepato.cellular carcinomas of the liver



and of squamous cell carcinomas of the lung, hard palate/nasal






                           -59-

-------
Table
1 I
1 &/ !
!Dose !
i o . !
! 1 PPt !
!
I 5 ppt !
150 ppt 1
1500 ppt !
I 1 ppb i
i 5 DDb i
6.
Total
Tumors in Rats .Ii
Destine: T
C1 T\ TY^^
I Rats With

Beni
0
0

1
2
2
b
8

en
i
1


,1
j


Tumors
Halicnant Total
o i o
0 ! 0
! A /
5 i 6s"'
1 1 f
2 ! #>•
5 j 5A/
2 ! 10
' Tumors
! No.
! o/io
1 o/io
i
! 5/10
i 3/10
1 4/10
! 4/10
! 7/10

{
o^x
0?
e/
50$-'
30J
40?^
40J
70?

i
i
i
i
i
•
!
!
1
i
I
    Data from Van Miller  (109).
Ji/  Rats administered 50, 500, and  1,000  ppb  were  all
dead within four weeks.
£/  Forty male rats used  as  controls  for  another study  '.
were received at the same time and  kept under identical
conditions did not have neoplasms when killed at 18 months.
jj/  One rat had ear duct  carcinoma  and lymphocytic leukemia,
The following tumor "types were each observed  in one rat:
adenocarcinomas (kidney), malignant histiocytoiaa (retroperi-
toneal), angiosarcoma (skin), and Leydig  cell adenoma  (testis)
£/  Three rats died with  aplastic anemia.
£/  The following tumor types were  each observed in one rat:
fibrosarcona  (muscle), squamous  cell  tumor  (skin), and
astrocytoma (brain).
£./  The following tumor types were  each observed in one rat:
fibroma (striated muscle), carcinoma  (skin),  sclerosing
seminoma (testis), and adenocarcinoma (kidney)*
JL/  One rat had a severe  liver infarction,
i/  One rat .had cholangiocarcinoma  and malignant histio-
cytomas (retriperitoneal)»   The  following tumor types  were
each observed in one rat:  angiosarcoma (skin), glioblastoma
(brain), and malignant histiocytoma (retroperitioneal).
J./  One rat had squamous  cell tumor (lung)  and neoplastic
nodule  (liver).  Two rats had cholangiocarcinoma and neo-
plas-tic nodule diver)*   Three rats had squamous cell  tumors
(lung)* One rat had neoplastic nodule.
                           -60-

-------
turbinates, and tongue in rats at 0*1 ug/kg.  They also



reported decreased incidences of  pituitary, uterine,



mammary gland, pancreatic, and adrenal gland tumors at this



dose level,  Dow also reported that this dose level produced



increased mortality, decreased body weight gain, and changes



in blood chemistry values which  suggested severe toxicity,




Hepatocellular nodules and  alveolar hyperplasia were



observed.in the 0.01 ug/kg group* A squamous cell carcinoma



of the hard palate was observed in one female receiving this



dose; Dow considered this unrelated to TCDD treatment



because a similar tumor occurred in "other concurrent



studies,"  At 0,001 ug/kg there were no "discernible effects



in male rats and an increased incidence of [reversible]



swollen hepatocytes in female rats,"





    •';.'.  Dow's preliminary report does not include control



data, quantitative data on tumor incidence, or statistical



analyses.  CAG has not evaluated this study.  Table 7



describes the available tumor information.  Dow has submitted



the final report for this study, which CAG is currently



reviewing.
                            -61-

-------
     Table 7«  Tumors in Sprague-Dawley Rats
                             a/
  	Ingesting TCDD 	
J_	pose	L                             1
         v i   pot   I  Tumors	L
10      ; I    0   i  	                       I
lo.ooi -   !   22   !  	                       1
10.01      1  210   !  Hepatocellular Nodules     !
I          I        I  Squamous Cell Carcinoma-^-'  I
j          I        I  Alveolar Hyperplasia       \

JO.I       I 2,220  !  Hepatocellular Carcinoma""  !
                      Sauanous Cell Carcinoma
                                             -^-
    Data from Dow Chemical USA (110), a preliminary report,
    Hardpalate squamous cell carcinoma observed  in only
one female rat»
    Observed only in females.
    Squamous cell carcinoma observed in lungs, hardpalate/-
nasal turbinate, or tongue.
     (b)  Effects Closely Related__to Oncogenicitv in Test

     .'"^'>>. Animals          _                 .


       Many chemically non-reactive carcinogens are

enzymatically converted to  biologically active carcinogens,

The  eazyme aryl hydrocarbon hydroxylase (AHH) is strongly

implicated in this process  (112).  For example, the incidence

of bronchiogenic carcinomas in humans (113) and mouse

sarcomas induced by 3-methyl-cholanthrene  (II1*) have been

related to the level of inducibility of AHH (99).


       Kouri et al» (11M) studied AHH induction in human

lymphocyte cultures by TCDD. The authors stated, "TCDD

itself is not a potent carcinogen in mice; however, the

synergistic action of TCDD  with 3-methylcholanthrene (MC)

produces cancer in different strains of mice in direct


                          -62-

-------
proportion to the degree of elevation of the induced hydroxy-


lase activity and associated cytochrome pj-450 content,"



Their study showed a positive correlation between basal


enzyme activity and enzyme levels maximally inducible by


either TCDD or MC»  They also found that TCDD is about 40 to
    i

60 times more potent than MC as an inducer of hydroxylase


activity in cultured human lymphocytes*  These authors


further suggested that, because of the relatively high


levels of TCDD in certain parts of the world, TCDD
  •

may also present considerable long-term risk because of


possible synergism in chemically initiated oncogenesis, in


addition to short-term risks posed by its toxic and terato-


genic properties.               .




       The implication of TCDD in AHH inducibility has


also been reported by Poland and Glover (115, 116) and


Poland et al. (117)«  In their studies on chick embryo


livers, Poland and Glover (115) found that all dioxins


which are potent inducers have halogens at three of the


four lateral ring positions and at least one nonhalogenated


carbon atom,  Poland and Glover (116) compared the po-


tency of TCDD as an inducer of hepatic AHH with that of


MC, the most commonly employed inducing agent.  They


stated that analysis of the data by a computer program


for bioassay showed that TCDD was 28,640 times as potent




                            -63-

-------
as MC on a molar basis,  (The 95? confidence interval

                                         ji
of the potency ratio,is 2,07 .to 3,95 X 10 ,)  The index of


precision, A , was 0,18.  Poland et al. (117) suggested that


a hepatic cytosol species which binds TCDD is the receptor


for the induction of hepatic aryl hydrocarbon hydroxylase.



       Allen et al. (118) conducted a study in which female


rhesus monkeys were fed diets containing 500 ppt TCDD for


nine months. Anemia, thrombocytopenia, and leukopenia were


the most debilitating changes*  The altered lymphopoiesis


could be associated .with immune suppression.  The authors


reported widespread hypertrophy, hyperplasia, and metaplasia


in the epithelium of monkeys exposed to TCDD, and related


this to data showing increased tumor frequency in TCDD fed


rats*  .       ,/...--.   • •..    '.'-..:"••-.   . •    ..-.-'.•       /••.-..



     (-3)  preliminary Epideniolo.gical Studies



       Two epidemiolgical studies lend -support to a finding


of~in<;reased tumorigenicity due to 2,4,5-T exposure.  The


English summary of a Swedish paper by Hardell (108) stated


that "there were seven cases of malignant mesenchymal tumors


in [87] persons [who had been] exposed to 2,^,5-T over a



                           -64-

-------
period of 10-20 years." In five of the cases, exposure had

been direct and comparatively massive*  The latent period of


10 to 20 years is in agreement with that assumed for chemical

carcinogenesis.  The statistical distribution of 7 of the

87 patients deviated from the national average with a

dominance of humors in males,



       Tung (120) reported an elevated incidence of primary

liver cancers among Vietnamese following the Hide application
                                             s

of "Agent Orange" as a defoliant during the years 1961 to

1962,  "Agent Orange" is composed of equal parts 2,4,5-T and

2,4-D (2,4-dichlorophenoxyacetic acid) and is contaminated

With TCDD.  During 1962 to 1968, 10J (791/7911) of all

cancers were liver cancers, compared with 3$ (159/5*142)

during 1955 to 1961,  The latent period involved is shorter

than that normally assumed for chemical carcinogenesis; the

possibility of a shorter latent period for some chemicals,

however, cannot be eliminated.  Neither of these studies is

sufficient to be the basis of any firm conclusions concerning

a causal connection between 2,4,5-T and cancer.  But in view

of the results obtained in experimental animals, they
                                                    •
warrant noting.
                            -65-

-------
       The Working Group concludes that there is sufficient

evidence to indicate that 2,4,5-T, containing TCDD at

levels as low as 0»05 ppm, and TCDD alone can produce

oncogenic effects in mammalian species.  Since 2,4,5-T, as

currently formulated, contains TCDD (at a maximum amount of

0*099 ppm), a rebuttable presumption against registration of

2,4,5-T products has arisen because of the oncogenic effects

of 2,4,5-T~and TCDD.
                                •v-.

     B«  Other Chronic or Delayed Toxio Effects


       40 CFH Section 162.11(a)(3)(ii)(B) provides that "a

rebuttable presumption shall arise if a pesticide's

ingredient(s)..,(p)roduces any other chronic or delayed

toxic effect in test animals at any dosage up to a level, as

determined by the Administrator, which is substantially

higher than that to which humans can reasonably be anticipated

to be exposed, taking into account ample margins of safety."

This section reflects concern that chronic exposure to

chemicals may result in injury to the reproductive system

and/or the fetus and provides that a rebut'table presumption

shall arise if chronic chemical exposure in test animals

produces such results.


       The studies summarized below show that 2,4,5-T

containing 0.5 ppm or less TCCD produces teratogenic and/or

fetotoxic effects in mice at 30 mg/kg, in rats at lOO.mg/kg,

in hamsters at 40 mg/kg, and in birds at 1 mg/kg.  Other

-------
studies show that pesticide-free TCDD is fetotoxic and/or



teratogenic at doses as low as 0»125 ug TCDD/kg in rats and



0»1 ug TCDD/kg in nice.  Specifically, these studies



show that exposure to TCDD and/or 2,4,5-T containing TCDD



during pregnancy is associated with statistically significant



increases in the incidence of cleft palate, kidney anomalies,



skeletal and intestinal tract anomalies, and embryonic



resorption.  (Maternal toxicity has also been observed in



many of these studies, primarily in the form of reduced



weight gain and increased liver-to-body weight ratio.



Whenever it has appeared particularly relevant, details have



been cited in the individual studies*)





       The Working Group has concluded from these studies



that 2,4,5-T containing TCDD, 2,4,5-T without detectable



dioxin, and TCDD alone produce fetotoxic and teratogenic



effects in mammals.  The Working Group has also concluded



that an ample margin of safety does not exist for the



population at risk (women of child-bearing age) for dermal



and inhalation exposure and for cumulative oral, dermal, and



inhalation exposure to both 2,^,5-T and/or TCDD.  For these
reasons, the Working Group irecommencLa issuance of a rebuttable



presumption based on the fetotoxic and teratogenic effects



of 2,U,5-T and/or TCDD.






                          -67-

-------
      (1)  Pesticide-free  TCDD






       A Bionetics Research Institute  study  on  2,^,5-T




provided the  first indication  that  TCDD  adversely  affected




mammalian development  (123)• In  this study,  detailed  with



later confirming  studies  in Section III,B.(2) below,  2,4,5-T



significantly increased the frequency  of cleft  palate,



kidney anomalies, and  fetal mortality  in the litters  of



treated dams.   The 2,4,5-T used  in  this  study contained




approximately 30  ppm TCDD*  Subsequent studies,  detailed in



this  section,  using pesticide-free  TCDD  have established



that  TCDD alone produces  these effects,  and  that the  TCDD




contaminant may be the principal  chemical  determinant




of  the fetotoxic  and teratogenic  effects in  mammals exposed



to  the pesticide  2,4,5-T.






       (a)  Jgtudles _ln which TCDD Produced Tera'togenlc



'.-•'••"      and/or Fetotoxic Effects in  Mice





       Courtney and Moore (128)  studied  TCDD's  embryotoxic



and teratogenic effects in three  mouse strains  (Table 8).



Test  animals  were administered 1  or 3  ug TCDD/kg body



•weight subcutaneous!^  in_.s£lutions  of  100? dimethylsulfoxide



(DMSO) on days  6  to 15 of gestation.   DMSO was  administered as



the control.   TCDD produced cleft palates  in all three



strains.  At  3  ug/kg,  30J (3/10)  of the  CD-I litters  had



fetuses with  cleft palates compared to OJ  (0/9)  of the



controls; 71% (5/7) of the C57BL/6  litters had  cleft  palates






                            -68-

-------
   , ...»•-                        ,
  .:,....-"•"•*:.....'-'•'"   .„...'•-•"
                       -- — "
of
                .69-

-------
    TCDD was administered  orally  at  25  to 400 ug/kg body weight
   r
    and subcutaneously at  25  to 200  ug/kg.



           Mortality  per litter increased .with the dose and

    reached 97?  (oral) and 76?  (subcutaneous) in the litters

    administered TCDD, as  compared with a mortality of 6 and

    14? in the oral and subcutaneous control groups, respec-

    tively.  The most common  anomalies  observed were cleft

    palates and  malformed  kidneys.   All of the fetuses in

    the 200 and  400 ug/kg  (oral)  and 200 ug/kg (subcutaneous)

    groups exhibited  cleft palates as compared to 0? of the

    controls.  Of  the fetuses in  the 200 ug/kg (oral) group,

    100? had kidney malformations as compared to 1? of the

    controls.  Other  anomalies  observed were hydrocephalus,

    open eye, and  club foot.   Edema  and petechiae were also

    .observed in  fetuses administered the high doses.


  Table Q.  Fetotoxic  and Teratogenio Effects of TCDD in CD-I Mice"
i : i
i Dose !
Uug/kg i Route of Ad-
Joer dav) J ministration
! 25 i Oral
! 50 i Oral
MOO i Oral
! 200 i Oral
1^400 ! Oral
25 I Subcutaneous
50 ! Subcutaneous
100 iSuhcutaenous
200 iSubcutaenous
5f i Oral
corn oil,1
(0.1 ml)!
_DKSO~ J Subcutaneous
-
% Average Fetal
Mortal itv/Litterj
. 6
13
14
87
o? ...
36
56
72
76
6
14
Average # j
Abnormal
Fetuses
ner Litter
. 4.6
8.1
8.3
1.5
.0.4
6.7
5.0
3.5
0.8
0.2
Abnormal i
Cleft
Palate
a
K
O
19
66
100
100
82
79
85
100
0
i o
Anomalies/Total
Kidney
Anomalies
34
72
71
100
•50
53
58
95
1
1
' 0
Fetuses
Club
Foot
*
3
7
13
14
50
11
17
0
18
4
i i
! 1 !
Data from Courtney (133)
DMSO r dimethylsulfoxide
                                  -70-

-------
       Moore et al.  (174)  also fpund that TCDD caused

fetotoxic and teratogenic  responses in C57BL/6 mice at

1 ug/kg administered on days 10 through 13 of gestation.

Compared with 0? incidence (0/27) in the control litters,
   t
94? (15/16) of the treated litters exhibited kidney

anomalies, and 19? (3/16)  -had cleft palates.  At 3 ug/kg,

the incidence of these anomalies was 100? (14/14) and 86$

(12/14), respectively.


       Neubert and Dillman (127) tested the embryotoxic

and teratogenic effects of TCDD in NMRI mice (Table 10).

In one test, pregnant mice were given varying doses of TCDD

(0»3 to 9 ug/kg) by intubation on days 6 to 15 of gestation*

At 9 ug/kg, 100? (3/3) of the viable litters had resorptions;
                                           •
67? (6/9) of all litters had total resorptions*  Oil control

values were 32 and 0? for litters with resorptions and

litters vith total resorptions, respectively.  Cleft palate

was observed in all of the litters and 82? of the fetuses

at 9 ug/kg; comparable oil control values were 6 and 0.7?,

respectively* Statistically significant (p < 0.01)

proportions of the fetuses evidenced cleft palate at 3, 4.5,

and 9 ug/kg (3, 13,  and 82?, respectively) when compared

with the oil control.
                          -71-
                                                                        r
                                                                        ?-,

-------
 Table  10.   Ecabryotoxic  and  Teratogenic

            Effects  of  TCDD  on  KMRI  Mice3-7
!
         iLitters  Af fectqd/ Viable  Litters!
         l   Resorptions  I   Cleft  Palate   I
!(u*/k>?)
; o
oil
0.3
3.0
4.5
9.0
! Q.O
# !
23/95!
21/65!
7/13!
16/24!
5/12!
3/3 !
V6 !
%
24
32
' 54
67
42
100
50
! f
! 6/95
! 4/65
! 0/13
i 7/24
! 6/12
! 3/3
! <5/6
I
6
6
0
29
50
100
8?
i
i
\
\
i
!
!
i
     Data fron  Neubert  and  Dillnan (127).
     All  doses  administered on  days  6  to  15,
 except  second  9.0  ug/kg  dose which  was
 administered on  days  9 to  13.

        In this study,  a  single oral dose  of  45  ug/kg TCDD  on

 day 6 produced resorption  in 100$ of  the  viable litters; 23

 ug/kg on day 10  led  to 50$ resorptions.   Seventy-one per

 cent of  the. viable litters had embryos with  cleft  palate

 when 45  ug/kg  was  given  as a single dose  on  day 11.  Control

 values  were 24$  for  litters with  resorption  and 6$ for

 litters  with cleft palates. -

 ;..     Smit-h et  al.  (135)  administered 0.001, 0.01,  0.1,

 i.O, and 3.0 ug  TCDD/kg  body weight per day  to  CF-1  mice by

 garage  from days 6 through 15  of  gestation  (Table  11).  The

 percentage  of  resorptions  per  implantation was  significantly

 higher  in treated  mice than in the  controls  only in  the 1.0

 ug/kg group.   Cleft  palate occurred in 71$ of the  litters

 treated  at  3.0 ug/kg  and in 21$ of  the litters  treated at

.1.0 ug/kg;  bilateral  dilated renal  pelvises  occurred in 28$
                         -72-

-------
  of  the litters treated at  3,0 ug/kg,  and  in  5% of  the

  'litters  treated at  1,0 ug/kg.  No  significant increase in

  either cleft palate or dilated renal  pelvis  was observed at

  0*1|  0.01,  or 0.001 ug/kg.   None  (0/3*0 of  the control

  litters  had cleft  palate or  abnormal  kidneys.


Table  11.  • Fetotoxic- and  Teratog°nic_Effects of TCDD in CF-1 Mice
{Incidence of Cleft!
{Palate in Litters i
Dose 'per Live Litters !
( utr/ke) ! *
0 i 0/34
0.001 i 2/41
0.01 ! 0/19
0*1 i 1/17
I 1.0 ! 4/19
^o ho/u
• * 1
ff 1
0 i
5 i
o !
6 i
2& \
7& i
Litters With
Resorbed Fetuses
tier Live Litters
* i *
25/34 i 74
30/41 ! 73
17/19 i 89
16/17 ! 94
18/19 I 95
11/14 ! 78
Litters With Dilated
Renal Pelvis. per
Live Litters
# . ! i
0/34 0
0/41 0 I
0/19 0 !
0/17 0
1/19 \ 5
1 4/14 ! 2&k/ i
%J  Data fron Smith et al.
.by  Statistically different
probability test (p < 0,05)
(135).
 from controls by the Fishers exact
       Neubert et al. (175) estimated the ED-50 for cleft

palate in fetuses to be 40 ug TCDD/kg per day (Table 12).

The no-effect-level during days 6 to 15 of gestation was

estimated to  be 2 ug/kg per day for NMRI mice.  No pronounced

fetal mortality was observed when 3 ug TCDD/kg body weight

was administered on days 6 to 15 of pregnancy.



Table 12.  Occurrence of Cleft Palate in Offspring of Hloe Fed
!
{Strain!
CD-1 j
1
DBA !
1
NMRI \
1
IC57B1 j
1 !
Dose
(ue/ke)
0
3
0
?
0
?
0
1
% Cleft Palates per {Affected Litters/Total Litters
Total Fetuses Exanined !
<0.3 1 '
? !
<1 !
U !
0.7 !
3 !
<1 !
1 22 !
*
0/29
V10
0/23
2/9
10/160
7/2>4
0/23
5/7
! *
! o
! 30
i - 0
! 22
i 6
! 2Q
i 0'!
! 71 !
JEL/  Data from Neubert et al.  (175)»
                                 -73-

-------
       Khera and Ruddick (6)  studied the perinatal ef-


fects of TCDD in Wistar rats. In one test,  rats were orally


administered 0.125,  0»25,  0.5,  and KO ug TCDD/kg per day on


days 6 through 15 of gestation  (Table 14),   Visceral


lesions were observed at 0.25 ug/kg and above;  slight


decreases in fetal weight were  also seen. Postnatal effects


of prenatal exposure to TCDD  were studied by allowing


offspring of treated dams to  be reared by untreated dams .

until weaning.  Reduced survival, body weight gain, and


reproductive ability in the progeny were observed after


maternal treatment with 0.5 and 1*0 ug/kg«   No  fetotoxic


effects were observed at 0*125  ug/kg.



       In a second experiment,  rats were treated orally

with 1, 2, 4, 8, and 16 ug TCDD/kg body weight  per day


on days 6 through 15 of gestation.  TCDD treatment reduced

Tetal weight^ and the number  of live fetuses per litter, and
     •   • "                        "
produced visceral lesions in  50? (3/6) of the 1,0 ug/kg

fe~tus-es and 1*3$ (3/7) of the  2.0 mg/kg fetuses, as compared

to none (0/10) in the controls*  The incidence  of skeletal

anomalies was comparable to that in the controls at all dose

levels*  Doses of 1  ug/kg or  more produced maternal toxicity;

 4 ug/kg or more produced 100J  embryomortality.  The authors

concluded that oral treatment of pregnant Wistar rats with

0«25 ug (or more)/kg per day on days 6 to 15 of gestation


adversely effected rat development,



                          -75-

-------
                    Teratogenic Effects of TCDD in Wistar Rats2-
1
i
ise I
VkR) !
S-l I
Un- I
eated i
.ntrol i
•eated!
jutrol i
17125 i
3.25 I
0.5 I

est 2 !
41n- I
-reated I
Control !
s'reated !
control!
1.0 i
6*0 S
4.0 i
8.0 I
16.0 T


Avg." tf Live
Fetuses/Litter

10.7


11.0
10.6
10,9
10.5
P. "3

11.5


9.8

6.5
6.0
0
0
0

Avg. Fetal
Weight
( eratns)

4.82


4.51
4.64
4.79
4.46
u:io

4.68


4.77

4.17
3.31
. .


Fetuses with
Skeletal Anomalies/-
Total tf Examined
#

5/107


21/116
3/121
6/109
10/105
6/81

8/116


9/89

7/80
7/57
*„

5


18
2
6
10
7

7"


10

9
12
h
1
i
[Fetuses with Micro-
iscopic Visceral
i Lesions/Total tf
! * !
i >
I 0/13 !
I
i i
i 0/11 I
i i
! 0/38 i
! 1/33 !
3/31 !
! V10 i
i i
! 0/10 l
Ii
I
I i
! 0/10 !
! i
} 3/6 I
3/7
i
i
I i

Examined
%

0


0
0
3
10
?0

0


0

50
43
I
]

J  Data from Khsra and Ruddick (6); treated controls given anisole-corn oil.





               Courtney and Moore (128) administered TCDD to CD rats



       subcirfrane-ously  in solutions of 100?  DMSO  on days  6 through



       15 of  gestation (Table 8).  DMSO was administered as the



       control.  'Kidney anomalies were found in  four  of  the six



       litters (67?) whose dams were administered 0,5 ug/kg as



       compared to  OJ	(_0/9) in the controls.  TCDD did not affect



       fetal  mortality, fetal weight, or cleft palates in the



       fetuses,






               Dow Chemical USA (110) conducted a three-generation



       reproductive study on Sprague-Dawley rats continuously fed



       the equivalent  of 0,001, 0.01, or 0,1 ug  TCDD/kg  per day.
                                  -76-

-------
A preliminary report cites reduced fertility and litter

survival in f  rats as the reasons for discontinuing the

0.1 ug/kg dose level; significantly reduced fertility was

also observed at 0.01 ug/kg.  "Clearly evident" indications

of toxicity at 0.01 ug/kg among f  and f  litters included

smaller litter size at birth, plus decreased survival and

growth of neonates.  Dilated renal pelvis was observed in

each of the three f  rats at 0,1 ug/kg which survived to

adulthood*  Increased frequency of this anomaly was also

seen among weanlings at lower doses; however a dose-

related or generational correlation could not be made.

In summary, Dow conclu-ded thart~nthe reproductive capacity

~of rats ingesting TCDD was clearly affected at dose levels

of 0.01 and 0.1 ug/kg per day, but not at 0,001 ug/kg per

day , through three successive generations,"  The pre-

liminary report did not include the numerical data neces-
 ~— ™. -    . .                                                ^
sary for Agency evaluation.  Analysis will continue as

these become available.
                        -77 & 78-

-------
       Adverse  reproductive effects due to TCDD.have also




 been  observed in  hamsters and chickens*  Gastrointestinal



 hemorrhage was  noted  in hamster  fetuses after administra-




 tion  of  TCDD at 0.5 ug/kg per day on days 6 to  10 of gesta-



 tion  (48; 62).  Buu Hoi et al, (111) established that



 0.02  ug/kg TCDD caused teratogenic effects in chick embryos,



 Bowes et al. (137) and Verrett (136) confirmed  these




 results. They  found  abnormalities in the beaks, eyes,



 and feet of chick embryos after  TCDD exposure.               !






       (c)  Summary                                  •






       Studies  have established  that TCDD is fetotoxic




•and teratogenic at doses as low  as 0.125 ug/kg  in rats



 (129)  and at 0,3  ug/kg in mice (127); preliminary data from



 Dow (110) indicates that TCDD may have effects  at 0.01 ug/kg



 in rats. Cleft palate and kidney anomalies have been



 observed in rats, mice, and hamsters.  No fetotoxic or



 teratogenic effects have been observed at doses of 0,03



 ug/kg in rats (129) and 0,1 ug/kg in mice (135), Table 15



 lists the no-effect-levels in rats and mice for teratogenicity



 from  TCDD,                       -
                          -79-

-------
Table 15.  Ho-Effeet-Levels for Teratogenesis from TCDD
        (Route of Ad-
 Soe c i e s 1 ci i n i s t_p at ion
Wo-Effect-Level!
      per dav
Reference
        i Subcutaneous
        I    Oral
        !    Oral
  House {Subcutaneous
  • i.Y-WJv. Or.ai"V
        I    Oral	
    <0.5       .'Courtney and Moore (128)
     0.125     {Khera and Ruddick (6)
     0,03      iSparschu et al« (129)
    <1»0       {Courtney and Moore (128)
    <0.3       iNeubert and Dillman (127)
     0. 1	.'Smith et al. (US)	
     (2)  £, 4, 5-T f TCDD _Contaplnatlo_n_ Ranging Fron"T?ndeteotable

          to ^0 ppm)                           .'     .       .


       (a)  Teratogenic and, Fetotoxlc .Effects In RodgnJbs


       Courtney et al* (123) developed the first evidence

that a 2,4,5-T pesticide product was teratogenic and fetotoxic
(Table 16). -    The 2,4,5-T used in this study contained

approximately 30 ppn TCDD.  The pesticide was administered

daily either orally or subcutaneously on days 6 to 14 of

gestation in C57BL/6 mice, days 6 to 15 in AKR mice, and

d-aya 10 to 15 in Sprague-Dawley rats.  Subcutaneous adminis-

tration of, 113 mg/kg body weight resulted in significant

increases in the incidence of cleft palate and cystic

kidneys — ^  in the embryos of both strains  of mice, and

fetal mortality in the C57BL/6 mice. Oral administration  of
_Lfi/  Results of this study were published by the Department  of
Health, Education, and Welfare (121) and by Clegg  (122)*
JJ/  In a recent report on studies measuring renal alkaline
phosphatase in fetal mice, Highman et al, (45) attributed
the increased incidence of "cystic kidneys" in the offspring
of 2,4,5-T treated animals to retarded development,  rather
than true teratogenesis.  Reduction in fetal weight  and
increased incidence of cleft palate were also observed
among the fetuses of treated dams.
                            -80-

-------
           Table 16.  Teratocenic Evaluation of
                   In
1
! Route of
£se {Adtninis-
."sin Itration
j7BL/6£/ i
•ntreated! 	
>ntrol {Subcutaneous
>*trol i Stomach tube
i
'eated {Subcutaneous
^eated {Subcutaneous
i
^eated ! Stomach tube
i
fated j Stomach tube


^7BL/6 !
>ntreated{ 	
introl {Subcutaneous
i
'•ated {Subcutaneous
i
i
:RJ/ j
^treated i 	
>ntrol 'Subcutaneous
i^rol {Stomach tube
•eated {Subcutaneous
-eated (Stomach tube
i
!
i
Dose If Lit"
\
— ! 72
£/ ! 106
&./ ! 32
21.5^: 6
ns.o^7! 18
46.4i/| 6
113.CT1 1 12
i

i
— ! 8
L/ \ 10
ns.o^7! 10
i
i
i
	 { 58
£/ ! 72
&/ ! 12
113.0117! 14
m.o^! 7
Per Litter
Avg. # Live! Abnormal
Fetuses {Fetuses
i *
i
j
5.8 ! 11
5.5 ! 12
7.1 i 14
7.7 ! 12
4.4 ! 5^
8.5 j yf
4.8 ! 7017
i
i
i
5.1 ! 31
6.1 ! 8
7.7 ! 7717
i
i
j
7.1 ! 5
6.9 ! 4
8.8 ! 0
6.9 i 2917
^_? ! 551/-
% Fetuses
with
Cleft {Cystic
Palate iKidnev
1
<1 } 1
<1 { 2
0 ! 1
0 ! 0
4 / J i /
221/| ^J/
2 ! 3317
23l/j ^
i
I
i
0 i 7
0 { 0
29^7{ 60^-7
1
I
j

<1 { <1
0 { 0
28^7| 1
5^\ 0
Fetal
Mortality

26
29
15
3
42
8
47i/
'


36
23
11



16
15
9
23
4-JJ/
Abnormal
Litters

38
42
41
50
86^7
10C;
100"^



71
30
100i/



19
24
0
71 i
10017
 Contained approximately 30 ppa TCDD.
 Data from Courtney et al» (123).
 Jreated from day 6 through 14 of pregnancy.  Killed on day 18 of gestation.
 Treated from day 9 through 17 of pregnancy.  Killed on day 18 of gestation.
 Treated from day 6 through 15 of pregnancy.  Killed on day 19 of gestation.
 Dose, 100 ul DMSO per mouse,
 Dose, 100 ul honey solution (honey to water, 1:1) per mouse.
 Administered as a solution of 2,4,5-T in 100? DMSO in a volume of 100 ul per mouse,
 0?,4,5-T was suspended in a honey solution (honey to water, 1:1) in a volume of 100
j mouse.
 P = 0.01.                                                         ,              .
 P = 0.05.
                                              ul
-81-

-------
the same dose caused increased incidence of cleft palate and

fetal mortality in both strains and cystic kidneys in

C57BL/6 mice*  Courtney et al. also reported increases in

liver-to-body weight ratios in fetal mice,

       «
       These investigators also found that 4,6, 10, or 46.4

ing/kg 2,4,5-T given orally to Sprague-Dawley rats produced

kidney anomalies and other embryotoxic effects at all levels

(Table !?)«  The occurrence of hemorragic gastrointestinal

tracts in rat fetuses was also reported* •


       Roll (125) found embryotoxic and teratogenic effects

in NMRI mice after prenatal exposure to 2,4,5-T containing

0.05 jt 0.02 ppm dioxin (Table 18),  2,4,5-T at 20 to 130

ing/kg body weight was administered orally to the dams on

each of days 6 to 15 of gestation.  At 90 or 130 mg/kg,

the percentage of resorptions and/or dead fetuses was

markedly increased relative to the controls; however,

maternal toxic effects were also observed at these dose

levels.-^  Statistically significant, dose-related

reductions in fetal weight were observed at 20 mg/kg

and above.       .
JL2/  Although the LD-50 for female NMRI mice had been
previously determined to be 778 ing/kg, an increased maternal
mortality rate was seen at 130 mg/kg and weight gain was
depressed at doses above 60 mg/kg (125),
                        .82-

-------
Table 17. Terato.cenic Evaluation of g.U.S-T^in Rats^7
• !
1
!
{Route of
st ' lAdminis-
irnal Itration
tV 1
ntreated! 	
ntrol {Stomach tube
eated j Stomach tube
1
0ted {Stomach tube




Dose
(icc/k^)

...

-------
three of the litters treated with 90 mg/kg of sample (B);


none was seen in the controls. Fetal weight was significantly


depressed in all treated groups compared with the oil


control.                                 •




       The percentage of fetuses with cleft palate was


significantly higher than the .control group in all 2,^,5-T


groups treated with ^5 tig/kg or more. In the group treated


vith 120 mg/kg 2,H,5-T containing <0.02 ppm dioxin, 5M$


(7/13) of the litters and 11* (U/145) of the fetuses


exhibited cleft palate compared with oil control values of
                                             s

6$ (A/65) and 0»7*_(5/669V,__respectively.



       These investigators also tested the butyl ester


of.2,4,5-T and found similar effects.  In experiments


combining 2,4,5-T and TCDD, potentiation of teratogenic


effects was observed.  Sixty mg/kg of 2,4,5-T (sample


A) combined with 0«3 ug/kg TCDD increased cleft palate


frequency among fetuses from 5 to 1MJ,  In this study no


cleft palates were observed among fetuses treated only with


0.3 ug/kg TCDD,
                           -85-

-------
              Tabl» TQ.  Esbrvntoylo Effects of 2.'
1
1
i
iPioxin
{Content
stsent Ifonn)
JNone I —
ion
|2 4
I'
1
1
1
1
1
J2 i
I
1
i?,4
control! —
,5-T U)! <0.02
i
1
1
1
i
j
,5-T (B)| 0.05
i -
1
! 1 Resoortion (PESJ
'Dose
i
! 0.4 nl
[ 8.0
Il5.0
Iso.o
1 45.0
[60.0
Iso.o
1 120.0
J30.0
I
I60.0
i
190.0
i i
,5-T fC)!unknowr.!QO.O
\% Litters!? EES/Inplan-
iwith RES Station Sites
1 1
i ' i
1 24
i 32
! 35
! 38
! 56
1 55
! 63
1 53
! 54
! 44
1

! 71
I 71
i
1
j
j
j
i
1
i
i
i
i
I
t
4
4
3
5
7
6
11
8
10
6
7
8-
n
! RES/Single
! Litter w/RES
! fM)
! 0.6
I 0.5
1 0.4
1. 0.5
! 0.8
i 0.6
i 1.2"
! 1.1"
! 1.3^
! 0.6
! 0.4
i ,.0^
! i.iX
i i
i Fetal !
! Weight i
if crass)!
! 1.26^1
! 1.30 !
! i^l
I ..«"!
I 1.09^1
! 0.98*/!
1 1.01^1
1 1.02^1
1 0.95^1
i 1.11^!
i I.IT^I
I 0.99^1
! ^.o^• 1
Cleft Palat
J Litters!?
with C? Iwi
6 i
6 !
<7 1
8 |
• 11 I
16 |
20 i
35 i
54 |
22 !
71 |
86 {
i
72 f
e fCP)
Fetuses
th C?
0.6
0.7
<1
1
,
3^
5^
8&/
1tli/
2
9^
23^
•><£•'
Pata from Neubert and Pi11nan (127); 2,4,5-T sample (b) received from Roll (125).
p^ 0.01.  .                          .


      '•'--•    Bage et al. (132) injected  NMRI  mice subcutaneously

      with 50 and 110 ng/kg 2,4,5-T  (<1.0  ppm dioxin) on each of

      days 6  through 14 of gestation*  At  110 mg/kg, 2,4,5-T was

      teratogenic,  causing fetal death,  cleft palate, and  other

      anomalies.             .


              Courtney and Moore (128)  studied the effects  of

      2,4,5-T Urn  LTD-T 'fiindom-b'red mice,  two  strains of inbred

      Bice, DBA/2J and C57BL/6J, and CO  rats  (Table 20).


                               -86-

-------

J
9
1
1
(Soecies
I CD-1
| House
i£xpt. 1
1
!
1
1
i
I
Table 20. Eabrvotoxlc
I
1
}
! Coanound
!
1
I DMSO
12.4,5-T
KTech.)
12,4,5-T
KTech.)
|2,4,5-T
If Tech.)
lErpt. 2! DMSO
i
I
jExpt. 3
i
1
I
1
I
J
|
1 DBA/2
I Mouse
j
IC57B1/6
I House
i
!2,4,5-T
j(Analy.)
! DMSO
12,4,5-T
KTech.)
i2,4,5-T
KAnaly.)
}
!2,4,5-T
!(Analv.)
i DMSO
12,4,5-T
!(T°ch.)
! DMSO
!2,4,5-T
i
iCTech.)
! CD fiat [Sucrose
I
t
I
1
|
I
I
1
12,4,5-T
KTech.)
!2,4,5-T
KTech.)
12,4,5-T
KTech.)
|2,4,5-T
KTech.)


Dose
(nc/lre)



50

100

150^


100


100—

100


125

...
100

—

100
—
10

21.5

46.4

80.0s/


% Fetal
Mortality
Effects of Analytical and Techr

[Fetal
[Weight
!?er Litter Ksraas)


6.6
6.6

7.5

51.7

8.8
9.6

8.4
.

11.6


12.9

25.1
27.0

10.8

15. P
3.4
1.8

1.4

3.8

52.1

i
\
\ 1.35
! 1.26
|
i 1.00
I
! 0.91
t
! U02
i 0.73"
t
t
i 1.09
J 0.85"
i
I 0.86"
I
! JS/
! 0.71
1
t
i o.as
! 0.6T"
i
i 0.99
i
| o 7«^7
i 2.48
i 2.40
t
! 2.54
t
i
! 2.20
-W
I 2.30
i
£\eft Palate (C?)
% Litters!
Affected !
!
{
i
0 i
0 !
[
33 !
{
100 !
|
0 i
89 I
!
0 !
40 !
- !
40 |
I
!
78 !
!
o :
27 !
i
0 i
J
HO \
0 i
0 !
j
o :

o i
i
o -!
!
1
1
if C? per!J
ij«a 2
. l|,5-T
Kidnev A
a.'
no~alies
Littersi* Affected F
Affected [Affected
Litter


0
0

3.0

5.3

0
4.4

0
2.0

2.0


5.4

0
1.0

0

1.3
0
0

0

0

0

1
.1-..
i
i
!
I
1
1
i
1
!
i
i
i
[
i
i
i
|
1
1
1
!
I
i
t
I
I
i
!
I
i
i
i
i

i
j
i
i
1
j
I



0
0

0

0

33
78

63
80

100


67

13
9

9

0
0
20

38

14

50

[per
!Litt
i
i
1
1
!
i
S
]
1
!
1
j
l
i
i
1
|
1
1
s
j
i
1
!
i
I
i
}
j
!

I
•
i
i
i
{
Affected
AT*


0
0

0

0

1.0
1.7

2.0
2.4

4.2


4.3

1.0
1.0

1.0

o
0
1.0

1.3

2.0

4.0


i
i
etusesj
!
i
i
i
!
!
s
i
I
}
1
\
I
i
i
1
{
I
!
j
i
!
j
{
!
J
!
i
I
i

j
{
i
i
|

3j  Data  fron Courtney and Moore  (128).
J>/  Investigators  thought this data  to be  close  to  a maternal toxic dose.
SJ  Maternal LD-40.
Jj/  p  < 0.05.
                                     -87-

-------
2,4,5-T containing 0.5 ppm (technical) or 0.05 ppm (analytical)
TCDD was administered subcutaneously to mice at 50 to 150
eg/kg in DMSO and orally to rats at 10 to 80 mg/kg in
sucrose on each of days 6 to 15 of gestation.  At 100 mg/kg
or more, both 2,4,5-T samples produced significant reductions,
which appeared to be dose related, in fetal weight in all
strains of mice; rats were not affected.  2,1,5-T was
fetocidal at two doses, but the investigators considered
this effect to be due to maternal toxicity.

       Both 2,U,5-T samples produced cleft palate in mice.
For CD-I dams treated with 100 mg/kg of either 2,4,5-T
sample, 40$ of the1 I'l-t-^er-s—and two fetuses per affected
litter evidenced cleft palate compared with 0? in the
control (Expt, 3)«  No cleft palates were observed among the
rat fetuses.  To verify this observation, a second group
of rats was given two 150 mg/kg doses of technical 2,^,5-T
subcutaneously at the time of palate closure (days 13
to 1*0.  Again, no cleft palates were observed; however,
there was a significant increase in fetal mortality among
treated animals (1*1$) when compared with the controls
(OJ).           ""     *""""^"^       _

       Fetuses of CD-1 mice treated with analytical 2,4,"5-T
also showed increased incidences of kidney anomalies;
the'response to technical 2,4,5-T was not as great.  At 100
ttg/kg, 100$ of the litters and *U2 fetuses per affected
litter of dams treated with analytical 2,4,5-T displayed
                             -88-

-------
kidney anomalies, compared with 80$ and 2.4 for technical


2,4,5-T and 63? and 2.0 for controls (Expt. 3)*  The effect


in inbred strains of nice was comparable with control


values.   In rats, technical 2,4,5-T at all dose levels


produced higher incidences of litters affected and numbers


of fetuses per litter affected than seen in the control


animals.  The maximum effects on kidney anomalies in rats '


were 50$ of. the litters and 4.0 fetuses per litter at 80


mg/kg, compared with 0$ in the control litters.


       In another study using CD-1 mice, Courtney (134)


administered 0.45 to 1.0 mM/kg body weight per day of
•

2,4,5-T  (0.05 ppm dioxin) either orally or subcutaneously



during various segments o"f the gestation period (Table 21).


Cleft  palate was  seen in all groups treated with 2,4,5-T;


there  were no instances of this anomaly within the control


groups.  At 0.8 mM/kg, 48? of total fetuses and 37$ of the


litters . evidenced this malformation.  Statistically signifi-


cant  (p  S. 0.05)  increases in the percentage of fetuses dead


and/or resorbed were observed at the highest  doses.  All


dose  levels had  adverse effects on  fetal weight. The author


noted  that by  slightly altering experimental  conditions, the


cleft  palate effect and the effects on- fetal  mor-tality and


fetal  weight could be produced independently.
J_3./   Maternal  toxicity  was  also  observed,  evidenced  by
reductions  in  maternal  weight  gain and  increased  liver-
to-body  weight ratios  (134).        •  "


                        -89-

-------
          DOS*
;/
              'Days
         '#/tot
                       al #•
                  73)
             ?"-'«/  21/59



            /'«•«' Sr
            I 4 ^
              /
a  p.
                               siu«
                  89
                                   ;SFe^  ;;.*
                                   .Monf-,-,.,  . ~
                                 /Fetal
                                    72
                                   !igftt
                    IPs
                                         tusea
6
t7
13
17
U

29£/
/ n ^^~~
/ °»95 /
0.94
1.07
0.89
1 /N A '
• 0.8? i
i •°' i
/0.87 /
— — ^.


16
lin
1
— i
1 —
/
/
/
1
/
1
«**t
	 -_

6
U
                                     :/
                                           •03
                                                              :ers;
                               37
 «•
                                -
             .„,
                                   -    ,


       -
.-
               «.
                          -90-
                                               • •-

-------
 per litterT"*    The  larger proportion of malformed fetuses

 in the  treated  groups resulted from either an increased

 incidence  of  skeletal anomalies also seen in the controls  or

 a low incidence of  abnormalities not observed in the controls.

 The former category included wavy ribs, retarded ossification,

 extra ribs, and a variety of sternal defects; the latter

 included  fused  ribs,  small-sized distorted scapula, malformed

 humerus shaft,  and  bent radius or ulna. Abnormal kidneys

. were observed in 7  to 45$ of the examined fetuses treated

 with sample T-1, compared with a control value of 20 to 3-5J.
Table 22. Effects of 2.4.S-T on Wistar Hat Fetuses2-7
iCompundjDose
! |(mg/kg)
! !
! T-1 {Treated
1- } Control
! 50
! 100
T-2 ! Treated
{Control
! 25
.J 50 __
	 ! 100

•Treated
{Control
! 25
--"- \ 50
{ 100
! ISO
T-3 {.Treated
{ Control-
! 25
! 50
! 100
! 1SO
! T-4^7 ! SO
tf of
Litters
14
1
Q
10
13
12
Q
10
11
14
10
s
10
14
2
12
1
8
Avg. # p
Viable
Fetuses
11.1
12.9
9.2
10.5
11.7
8.6
12.6
12.7
11.5
11.0
•11.6
11.8
12.2
11.0
12.6
11.0
11.3
>er Litter
Dead
Fetuses
0.6
1.3
1.P '
0.6
0.8
0.5
' 2.4
0.7
0.5
1.4
0.6
2.2
0.7
•
0.9
0.5
0.9
1.0
1.1
Fetal
Weight
4.65
4.84
5.34
5.06
5.15
4.S7
4.67
5.15
4.91
4.35
5.31
5.00
4.75
5.00
3.00
4 04
Avg. % Mal-
formed Fetuses
oer Litter^-
15
24
10
15
9
26
10
28
36
17
11
56
37
P1
in i
   Data from Khera.and HcKinley (130).
   One or more skeletal malformation (viable fetuses).
   No treated control given.                .
  14/   Statistical significance was determined using  the
  average  value per dose level.  Data from T-4 were not
  used  in  this analysis.
                          -91-

-------
     ,  In the postnatal portion of the study, after

normal delivery, survival rate, sex ratio, and pup weight
         /
on days 1 and 21 were compared.  Although treated pups

surviving from day 2 to 21 were slightly smaller at some

dose levels, there were no significant differences from

controls for any variable.  In some experiments, litters

were standardized at 8 pups on day 2, and the remaining

littermates examined for defects.  The increased incidences

of malformations among treated groups were comparable

to those found in the prenatal study.  Assuming the same

incidence for pups not examined, the investigators con-

cluded that there we.r§_np_re.al differences in survival

rates among control and treated groups* The butyl ester of

2,4,5-T produced similar toxic effects.             :


       Sokolik  (131) orally administered 100 and 400 mg/kg

and 50 and 200 mg/kg of 2,4,5-T and its butyl ester to rats

of the Rappolovo line on each of days 1 to 14 or 1 to 16 of

pregnancy.  At  TOO mg/kg, 2,4,5-T produced embryos with a

combination of  deformities including absence of lower jaw,

abnormal hind limbs, and exophthalmos.  At 400 mg/kg, the

embryos of treated rats evidenced cleft palate, hydrocephalus,

hydronephrosis, and abnormalities of the upper limbs which

included tridactyly, webbed toes, and abnormal shortness*


                          -92-

-------
       The butyl ester of 2,4,5-T was more toxic than
the parent compound, causing more than 30$ embryonic mortality
at 200 mg/kg.  The lower dose, 50 ng/kg,  also caused
high mortality among the embryos.  Cleft  palate, hydronephro-
sis, hydrocephalus, and extensive gastrointestinal hemorrhages
were also observed within the treated groups.  From these
results, the author concluded that 2,4,5-T and its derivatives
have a high potential 'for teratogenic activity,

       Collins and Williams (124) tested  seven samples
of 2,4,5-T from different sources for embryotoxic effects in
golden Syrian hamsters (Mesocric.e.tu.s auratus) [Table 23].
The dioxin contents ranged from not detectable (detection
limit < 0.1 ppm) to 45 ppm.  Daily oral doses of 20 to 100
og/kg body weight were administered in acetone:corn oil:car-
boxymethyl cellulose (1:5*8:10) on days 6 to 10 of gestation.
2,4,5-T with no detectable dioxin significantly (p < 0.05)
reduced fetal weight and fetal viability per litter at all
levels tested*

       Total fetal mortality was greatly increased at all
levels when compared with controls and was dose-dependent,
as was the effect on fetal viability.  The increased
incidence o-f gastrointestinal hemorrhage also appeared to be
dose related.  At 100 mg/kg, "pure" 2,4,5-T caused increased
incidences of malformations and reductions in the number
of live fetuses per litter.  One "pure" sample, F, at
100 mg/kg significantly reduced fetal weight from 1.8

                            -93-

-------
fable 23.
i
i
•i
}
fCoEDOund
{Control
/ A
f ••
^
i
! B



-
C



•
D



m




F
4*
Ezbrvotoxic Effects of
i
i
i
i
|
i
i
i
i
i
I
1
j
j
f
f

i
j
j
i
!
i
i

|


i
j
i
i
j

Dioxin
Content
(DOS)
—
45



2.9



0.5




0.1



NI^7


•

ND
ND
>
i
i
i
J
i
i
i
1
i
i
i
j
i
i1
i
i
j
j
I
i
f
i
i
i
f
i
i
i
I
i
J
i
f
i
i


Dose
(n£/k£)
	
20
40
80
100
40
80

100
20
40
80

100
40
80

100
40

80

100
100
100

1
% Total,'
Mortal-,'
itv
3 U '
32.3 I
74.3 /
94.4 /
100.0 !
7.2 }
9.8 }
1
11.4 !
8.5 i
4.0 !
43.6 j
j
57.2 !
2.4 {
33.3 i
j
47. 1 /
•10.7 •'
i
29.9 i
i
56.3 1
31.3 /
30,0' I
2,4,5-T in
Fetuses
i
Avg # Live}
per Litter}
i
11.0 !
7.3 /
3.7 i
0.8 j
0 !
9.1 !
10.4 j
i
12,8 /
12.6 j
13.4 /
6.6 i
I
5.1 !
11.4 }
7.8 j
,
6.0 /
11.2 i
j
8.7 i
1
6.3 !
7.3 /
8.4 ,'
Kansters"^

u
Avg Weigh t-^
(grams )

1.8
1.7
1.7
1.6
••»•.
1.7
1.7

1.7
I.T^
1.647
u^
$J
1.5
1.8
1.7
' ^J /'
i » O
1.5^
j /
1.5~
&/
1.5
1.6-7
1.6—
,
_L? Fetal Via-
/ 1
.'bility per
{Litter
i
96.7
/ 68. 117
I 25.8^
I 5.3"
( Ci*
• 93. 1
/ 90.1^
i » t
\ DO cS-'
, 00, ~
/ on p£/
i yo.<>
•' 95.9
/ 58,3^
{ jj/
' 40,2
97.8
/ 68.3d7
| J M
\ 57.2s-
/ 88. 217
| . *
1 69.1
I ji/
% Abnor-
malities
per Live
Litter
3.5
25.0"
33.3SL/
100.0"

0
12.5
. /
50,-Cr-
0
11.1
40.0^
A/
40.0
0
0

0
0

0
d/

' Hemorrhages!
per Total
Live Fetuses

O.3.?
28.4
75.7
42.9

0
2.4

13.0
8.6
2.5
12.5

7.6
0
2.1

5.6
1.5

4.2

I 53. 1 ' 36. 4 I 0
i 71. $•' 1 40. O^7 J 6.8
I 68.3d7 I 0 / 16.7
i
•
i
i
I
i
i
i
i
i
i
i
i
i
i
i
i
r
i
1
i
i
i
/
|
|
/
|
/
i
/
i
i
i
')ata from Collins and Williams (124).
ipparently normal weights for samples A and B attributed to edema.
'ot detected.
  < 0.05.
                                     -94-

-------
 to  1.6  grams,  reduced  fetal  viability  from  96.7  to 71.4?,

 and  increased  abnormalities  from  3.5 to  40J.   The anomalies
•
 associated  with  2,4,5-T  containing no  dioxin  were exencephaly,

 eye  abnormalities,  delayed  head ossification,  and hind

 limb deformities.

        Increasing  the  level  of dioxin  contamination increased

 fetal mortality  and the  incidence of abnormalities per

 litter; fetal  viability  was  reduced,   A  clear correlation

 was  found between  the  level  of dioxin  and abnormalities per

 litter.  Although  the  incidence of hemorrhages also increased,

 no  relationship  between  it  and dioxin  level could be found.

 Bulging eyes (ab-s-eno-e .-of .eyelid)  and delayed  ossification

 were'the most  common anomalies seen among fetuses exposed

 to  dioxin-contaminated 2,4,5-T; exencephaly,  edema, cleft

 palate, ectopic  heart, and  fused  ribs  were  also observed.

        Emerson et  al.  (141)  found no adverse  effects of

 commercial 2,4,5-T, containing 0.5 ppm TCDD,  on fetal
                    \
 development in Sprague-Dawley derived  rats  and New Zealand

 white rabbits.  Daily  oral  doses  of 2,4,5-T in gelatin were

 administered to  the rats at 1 to  24 mg/kg on  days 6 to 15 of

 gestation;  to  t"R=e~r"aT5i1t:S~~a'€":::3b to 40jng/kg on days 6 to 18

 of  gestation.   The investigators  found no maternal or

 embryonic toxic  effects  in  either species,  nor was 2,4,5-T


                         -95-

-------
considered teratogenic under the conditions of these experi-

ments.  The most frequently observed abnormalities were

accessory ribs, hydronephrosis, and retardation in the

development of the sternebrae. With the exception of partial-

ly ossified sternebrae in both species and bilateral accessory

ribs in the rabbit, the incidence of these anomalies was

greater in the control animals than in the examined treated

groups.

       Sparschu et al. (140) orally administered 2,4,5-T,

containing 0.5 ppm TCDD, to rats in daily doses of 50
              %
and 100 mg/kg on days 6 to 15 and 6 to 10 of gestation,

respectively.  Results-are given in Table 24.  At 50 mg/kg,

there were no significant maternal or embryonic toxic

effects attributable to 2,4,5-T except for an increased

incidence of delayed skull ossification, and a single fetus

with intestinal hemorrhage.  At 100 mg/kg, 2,4,5-T was toxic


to both dams and fetuses.^""*
JL5./  The high rate of maternal mortality caused dosing
to be stopped on day 10, instead of day 15.  Significant
reductions in weight gain were also observed.
                        -96-

-------
Table 24.  Kffgefcs of 2.4.5-T on Fetal Devlopnent of Rats
I
1
u
i
j
\%
I
JL

Parameter
Viable fetuses
Total
Mean oer litter
Resorptions
Litters
Total fetuses
j
t
i
I
i
I
i
jFetal weight (grams) j
! Male i
1 Female 1
jSex Ratio (M:F)
i
i
i Abnormalities !
{(} fetuses examined) !
j Poorly ossified sternebrae!
! Fifth 1
!
I
!
-1
i
1
I
a/
JL/
£/
Second and fifth
Multiple
Malaligned sternebrae
Delayed ossification
Interparietal
Parietals :
Frontals
Data from Sparschu et al
All viab-le fetuses from
• p < 0.05
1
i
T
j
i
i
i
. (1
one

Dose (
0
252
11
68
6.7
4.41
4. 17
53:47
15.2
3.0
8.3
0.8

3.8
3.0
0.8
40).
litter.

mg/kK oer dav)
! 50
i
! 203
! 11
I
i 61
i 12.1
I 4.38
I 4.15
! 44:56
1
! 22.1
! 4.2
j 12.6
i 2.1
{
J16.85./
il6.8^
1 7.4-a/
100
13* '
100
3.57^
2^:77
57.1^
14.3
14.3
28.6^X

2B.6^\
K'J l£./ !
D I . I i
I I *l * T



 	   Resorptions  were  observed  in  all  litters;  75? were



 totally resorbed.   Fetal weight was  significantly (p <



 0.001)  reduced  in both sexes  and  the sex ratio  was  shifted



 in  favor of  females.  Abnormalities  observed  which  had



 significantly  (p <  0.05) higher incidences  than in  the
                            -97-

-------
controls were poorly ossified and malaligned sternebrae and



delayed skull ossification. The investigators concluded that



the delayed ossification observed in this study was a



reversible manifestation, rather than a true teratogenic



effect,



       (b)  .Adverse Reproductive Effects in. Other Mam-



            mal Jan., Test Systems



       Adverse reproductive effects of 2,4,5~T exposure



have been observed in other mammalian test  systems.



Lloyd  et al»  (173) reported on In vivo enzymatic studies



showing reduced uptake and metabolism of testosterone



by the prostate gland in male nice treated  orally with



doses  of 2,4,5-T  (6.25, 12.5,. pi* 25 mg/kg,  ten times



-daily)*



       lefiaenko  (151) reported on the effects of acute



and chronic exposure to the butyl ester of  2,4,5-T on



gonadal and somatic tissue in an jn vivo cytogenetic



study  in male albino rats.  Chronic effects on the go-



nads were observed after exposure to 0,1 ug/kg for two



and one half  months.  Adverse effects (seen at seven months,



when the experiment was terminated), which  were considered



persistent effects, included testicular atrophy, decreased



sperm  count,  desquamated tubules, and aberrant cells



in the germinal epithelium.  Chromosomal aberrations



were also observed during  the chronic phase of the ex-



periment.  EPA .evaluation  of this study found inadequacies



in the methodology which would prevent the  drawing of



firm conclusions  from this data (106).




                           -98-

-------
       Recent studies in rats by Sjoden and Soderberg



[cited in (25)3 appear to show that prenatal exposure.



to 2,4,5-T leads to behavioral abnormalities and changes



in thyroid activity and brain seritonin levels in the



progeny.  Single oral doses of TOO mg/kg were administered



to the dams on days 7» 8, or 9 of pregnancy.



       (c)  Adverse Effects in, Avian Species



       Embryotoxic effects in avian species due to 2,4,5-T



exposure have been reported.  Verrett  (136) studied the



effects of 2,4,5-T, containing either  27 or 0.5 ppm TCDD,



on chicken eggs.  The 2,4,5-T was injected through the



air cell of the eggs, either preincubation or on the



fourth day of incubation.  The sample  containing 27 ppm



TCDD was found  to be more lethal  (LD-50 = 25 ug/egg) than



tOie less contaminated sample  (LD-50 a  100 ug/egg).  Both



samples produced teratogenic  effects,  including chick



edema,  eye defects, beak defects  (primarily cleft palate),



and short, twisted feet resulting from tendon slippage.



Teratogenic  effects were observed at doses as low as



.1  ppn  (50  ug/egg) with  the sample containing 0.5 ppm



TCDD  and as  low as 0.125 ppm  (6.25  ug/egg) with the sample



containing 27  ppm TCDD.



        Lutz  and Lutz-Ostertag (138) studied the action



of 2,4,5-T,  in  aqueous  solution afc  a concentration of



2  to  10 g/liter, on  the  embryonic development of quail



(Coturnix  coturnix japonica), chicken  (Sallus gall.u.s),




                         -99-

-------
pheasant (Phasianus .colchicus), and two partridge species



(Alectoris ru.fa and Perdrix; perdrix).  The 2,4,5-T was



adoinistered by dipping, spraying, and organo-typic cultures.



Abnormal genital tracts were observed in all species,



indicating abnormal sexual differentiation.  Further,



morphological changes in the tastes often gave the appearance



of true testicular atrophy.  In another study, 2,4,5-T



affected fertility in birds of both sexes (139).
                       -100-

-------
       (d)  Studies in Avian Species in Which.Adverse




            Effects Were Not Observed






       Using 2,U,5-T contaminated with less than 0»1 ppm




dioxin, Strange and Kerr (112) found no abnormal development




in chicken embryos.  Doses of 12,5, 25, 50, 75, 100, and 125



mg/kg were injected into eggs on days 0 and 5 of incubation;




observations were made HB hours later*  At this, developmental




stage, kidneys were not sufficiently developed to detect the




tubule lesions reported by Bjorklund and Erne (143)*






       (e)  Summary






       Studies have established that 2,4,5-T is fetotoxic



and teratogenic at doses as low as 35 mg/kg (0.05 ±. 0.02



ppm TCDD) in mice (125); *1.6 mg/kg (approximately 30 ppm



TCDD) in rats (123); and 20 mg/kg (0,5 ppm TCDD) in hamsters



(12*0 »  Cleft palate and kidney anomalies have been .observed



in mice, rats, and hamsters.  No fetotoxic or teratogenic



effects (no-effect levels) have been observed at doses of



20 mg/kg (0.05 ± 0.02 ppm TCDD) in mice (125) and 25 to 150



mg/kg (0.05 ± 0.02 ppm TCDD) in rats (125).





     (3)  Exposure Analysis






       In order to determine whether a rebuttable presumption



should be issued based on reproductive and fetotoxic effects,



pursuant to Section 162.11 (a)(3)(ii)(B), the Working Group



must determine whether or not an ample margin of safety






                          -101-

-------
exists between the levels of 2,4,5-T and/or TCDD which



produce reproductive and fetotoxic effects, and the level(s)



to which humans can reasonably be anticipated to be exposed.





       The cancellation of uses of 2,^1,5-T on food crops



intended for human consumption and for use around the



home, recreation sites, aquatic areas, and ditch banks in



1970 was thought to have eliminated the potential exposure



to that portion of the population at risk (women of child-



bearing age).
                            -lOla-

-------
       Social changes over the last few years,  however,



have given wonen the opportunity for employment in areas



that once were considered open only to men.  Since women



of child-bearing age are now employed in occupations such



as pesticide applicators, operators of highway construc-



tion and maintenance equipment, foresters, and chemical



formulators, they have become part of the population at



risk with potential exposure to 2,4,5-T and/or TCDD.





       In order to determine whether an ample margin of



safety exists, the Working Group must first determine



how much 2,4,5-T a woman could be exposed to through



oral, dermal, or inhalation erposure.  For each of these



analyses, the Working Group assumes a woman to weigh



60 kg.  The  following calculations are based on an exposure



analysis for 2,4,5-T and TCDD performed by EPA's Criteria



and Evaluation Division  [CED] (164).





       (a)  •Oral Exposure                       .





       For  purposes of this analysis, the Working Group



considered  currently registered uses where the possibility



of oral exposure to 2,4,5-T and/or TCDD existed.  Treat-



ment of range and pasture land could result in oral  ex-



posure through ingestion of meat and milk  from animals



grazing on  the treated area.  Since actual data on residues



of 2,4,5-T  in animals grazing on treated  rangeland is





                         -102-

-------
unavailable, for purposes of the 2,4,5-T oral exposure

analysis, the Working Group used residue information

obtained in a feeding study (37) in which cattle were

fed. considerably higher amounts of 2,4,5~T than they

would normally be exposed to in grazing on treated land.
      «
The following calculations are based on the average quanti-"

ties of food eaten per day (1.5 kg), as reported by Lehman

(144, 165).
  Table 25.  2.4r5-T Oral Exposure Analysis
{                    Whole Milk  Meat (Beef).'
{No-adverse-effeet    20 mg/kg    20 mg/kg   j
{level for terato-
jgenicity in mice

{Average level of     0.103 ppm"2"  0.2
{2,4,5-T identified

\% of food item in    19.6%       4,6?
{total human diet                : '

{Average amount of    1.5 kg      1.5 kg
{food eaten per day
I
{Exposure to 2,4,5-T  0.0005      0.0002     !
'per dav	rag/kg	mg/kg	{.
£./  Animals were fed at 300 ppm 2,4,5-T in the diet for 2 to
3 weeks.  This is a worst case assumption for cows grazing
on freshly-treated pasture without a withdrawal period; all
milk and meat was obtained from such cows.  Meat (beef)
includes muscle, fat, and liver tissues which constitute the
major portion of edible meat*
       To find the average daily intake of a single food

item, multiply the average daily food intake by the percent

of that item in the total diet:  for milk, 1.5 kg X 19.6?

=0.294 kg; and for meat (beef), 1.5 kg X 4.6? s 0.069 kg.


                            -103-

-------
       The quantity of 2,4,5-T in .the average daily diet


equals the average daily intake of each food item multi-


plied by the level of 2,4,5-T in the food item:   for


milk, 0.294 kg X 0,103 ppm = 0.03 og; and for meat (beef),


0.069 kg X 0.2 ppm =0,014 mg.
      *                               .



       The theoretical exposure of an average woman equals


the amount of 2,4,5-T in the daily diet divided by the


weight of the average woman:  for milk, 0.03 og / 60 kg


= 0.0005 mg/kg; and for meat (beef), 0.014 mg / 60 kg


s 0.0002 mg/kg; total exposure from milk and beef products


could be 0,0007 mg/kg per day,




x       Existing data on TCDD residues in animals grazing


on treated rangeland are too meager to use for an analysis


of TCDD exposure to humans through ingestion of meat or


milk  from animals  so exposed.




       The W.orking Group considers that the difference


between the no-adverse-effect level of 2,4,5-T for terato-


genic effects  (20 mg/kg) and the calculated oral exposure


level for 2,4,5-T  (0,0007 mg/kg  per day) does constitute an


ample margin of safety.  Since this risk criterion for other


chronic adverse effects has not  been met or exceeded, a .


rebuttable presumption does not  arise,




                         -104-

-------
       (b)  D'errsal Exposure


       In order to conduct these analyses, the Working

Group nust determine the amount of 2,4,5-T and/or TCDD

which would come in contact with the skin and the amount

that would be absorbed.
      *         '

       (i)  Sprav Applicator;   Back-pack, Sprayer


       For purposes of this analysis, the Working Group

assumes the applicator to be a 60-kg woman of child-

bearing age, and the site of application either a right-

of-way or spot treatment of pasture or rangeland.  The

equipment is a back-pack sprayer (166K  The following

calculations of exposure are based on dilution for spray-

ing of three pints of formulated product- per 32 pints of

water. Typical 2,4,5-T formulations, based on inspection of

a large number of registered labels (164), range from 4 to 6

pounds active ingredient (acid equivalent) per gallon.  The

product used in this exposure analysis has an assumed

concentration of 4 pounds 2,4,5-T per gallon.  Label recommen-

dations vary from a recommended dilution of 0.094 to 4

pounds acid equivalent per 32 pints of water.  A dilution

rate of 1.6 pounds per 32 pints has been selected as represen-

tative of a typically-used spray mixture.          .


       Wolfe et al. (166) studied dermal exposure to

fenthion during hand back-pack spraying for mosquitoes


                          -105-

-------
for ten situationsi  Exposure ranged  from 0.1  to  6.3 mg/hr,

with a mean value of 3»6 mg/hr (6 ml/hr).  Method of applica-

tion was a hand pressure sprayer, using a 0,06$ spray.

Workers wore short-sleeved, open-necked shirts with no

gloves or hat.  Based on Wolfe's data, CED (164)  calculated

a dermal exposure of approximately 0.177 pints per day.  CED

(16M also determined that approximately 10? of the 2,4,5-T

and TCDD coming in contact with the skin of the applicators

would be absorbed even after washing, based on absorption

studies with other pesticides (1H5, 1^6, 163).


	Table 26.  Back-pack Spraver Dermal Exposure,Data	
                                             TCDD
jUse Dilution rate  — — — 5 pints            3 pints
I              '           (U6 pounds        (0,00000016
j                         2,4,5-T) per       pounds TCDD)
I •-••-.               32 pints           per 32 pints
{                         water              water
I      '<"-•        '  '• -  ~   .           •
{Amount of diluted        0,18 pint         0*18 pint
I material gotten         .....              r •;
|-on skin daily            .                 :
I                            .         •   v   .-.  -.   :
\% Diluted material       10$                10J
labsorbed
!                               •    '•  ••• .   , .
lExposure level           409 ng             O.OM09 ug
!
iDose level               6,8 mg/kg          0.0007 ug/kg
I
.lNo-Adverse-Ef fec.t, ____ ..^^^.Q.JDLg/kg           0,03 ug/kg
I level for terato-            :^-        —
Jeenic effects
       The following calculations (see Table 27  for mathe-

matics) will give the daily dermal exposure for  both 2,4,5-T


                             •106-

-------
and TCDD:  1) convert the dilution rate to grams; 2) multi-

ply this figure by 1,000 (for 2,4,5-T) to convert to milli-

grams and by 1,000,000 (for TCDD) to convert to micrograms;

3) multiply this figure by the daily dermal dose of diluted

material; 4) multiply this figure by the percent absorbed;

and 5) divide this figure by the weight of the applicator

for the daily exposure to 2,4,5-T or TCDD per 8-hour working

day,


 	Table 27	
I         2,4,5-T
11) 1.6 pounds/32 pt X 454 g/-
{   pound s 22*70 g/pt;
I
|2) 22.70 g/pt X 1,-9.04X-ttg/g =
I   22,700 mg/pt;
!
!3) 22,700 mg/pt X 0.18 pt =
I   4,086 mg;
!4) 4,086 mg X 10$ = 408.6 mg
         TCDD
1) 0.00000016 pounds/-
   32 pt X 454 g/pound -•
   0*00000227 g/pt;
2) 0.00000227 g/pt X
   1,000,000 ug/g =
   2.27 ug/pt;
3) 2.27 ug/pt X 0.18 pt
   0.41 ug;
4) 0.41 ug X 10? s
! '                             j   0,041 ug;
!5) 408.6 mg / 60 kg =         !5) 0.041 ug / 60 kg =
I   6.8 mg/kg per day	I   0.0007 ug/kg per dav
       The Working Group considers" that the difference

between the no-adverse-effect level of 2,4,5-T for tera-

togenic effects (20 mg/kg) and this calculated dermal

exposure level for 2,4,5-T (6.8 mg/kg), as well as the

difference between the no-adverse-effect level of TCDD for

teratogenic effects (0.03 ug/kg) and this calculated expo-

sure level for TCDD (0.0007 ug/kg), do not constitute an

ample margin of safety.  The Working Group therefore recom-

mends issuance of a rebuttable presumption against pesticide


                           -10 7-.

-------
products contaanj.u& &,-.,., . ....




Section 162.11(a)(3)(ii)(B).






       (ii)  Sprav Applicator:  Tractor-mountedf  Low-boon



             Spray Equipment






       For the purpose of this analysis, the Working Group



assumes the applicator to be a 60-kg female of child-




bearing age clearing brush on either rangeland or rights-




of-way.  The same product cited above (2,4,5-T at 4 pounds/gal)




is being used, and the dilution rate is 1.6 pounds of




formulation to 32 pints of water1 (equal to 4 pounds of




2,4,5-T per 10 gallons of water). Based on exposure studies



using similar equipment but a different herbicide (14?)»  the



Working Group determined that, during an eight-hour working




day, the applicator would get  0*048 pints of diluted



material on her skin.  The Working Group determined that 10J



of the pesticide on the skin would be absorbed (145, 1*16, 163).



Table 28*  Dermal Exposure Data (Tractor Mounted  Equipment)
I
SUse Dilution rate
|
lAmount of diluted
imaterial gotten
|on skin daily
i
1$ Diluted material
{absorbed
I
lExposure level
1 :
{Dose level
i
i
1 No-Ad verse-Effect
llevel for terato-
Ipenic effects
2T4r<5-T TCDD
3 pints 3 pints
(1.6 pounds (0.00000016
2,4,5-T) per pounds TCDD)
32 pints per 32 pints
viater „ water
0.048 pint 0.048 pint
'


10$ 10$
• • .

109 mg 0.0109 ug

1.8 ing/kg 0.00018 ug/kg


20 mg/kg 0.03 ug/kg

j
                            -108-

-------
       The following calculations (see Table 29.for mathe-
                                                 .»
matics) will give the daily dermal exposure for both <2,4,5-T

and TCDD:  1) convert the dilution rate to grams; 2) multi-

ply this figure by 1,000 (for 2,4,5-T) to convert to milli-

grams and by 1,000,000 (for TCDD) to convert to nicrograms-;

3) multiply this figure by the daily dermal dose of diluted
                                                 \
material; 4) -multiply this figure by the percent absorbed;

and 5) divide this figure by the weight of the applicator

for the daily exposure to 2,4,5-T or TCDD per 8-hour working

day.


	      .         	Table 2Q   	1
          2f 4.5-T      	_!.
 1) 1.6 pounds/32 pt X 454 g/-
    pound = 22.70 g/pt;

 2) 22.70 g/pt X 1,000 mg/g =
    22,700 mg/pt;

 3) 22,700 mg/pt X 0.048 pt r
    1,089.6 mg;
 4) 1,089.6 mg X 10J =
    108.96 mg;
 5) 108.96 mg / 60 kg  =
    1.8 ffig/kg per.day	
           TCDD
  1)  0.00000016  pounds/-
     32  pt  X  454 g/pound  =
     0,00000227  g/pt;
  2)  0.00000227  g/pt  X
     1,000,000 ug/g =
     2.27 ug/pt;
  3)  2.27 ug/pt  X 0.048  pt
     0.109  ug;
  4)  0.109  ug X  10$ =
     0.011  ug;
' 15)  0.011  ug /  60 kg  s
...'..   0.00018  ug/kg per, day
       The Working Group considers  that the difference

between  the no-adverse-effect  level of 2,4,5-T  for tera-

togenic  effects  (20 mg/kg) and this calculated  dermal

exposure  level for 2,4,5-T (1.8 mg/kg), as well as the

difference between the  no-adverse-effect  level  of TCDD  for

teratogenic effects (0.03 ug/kg) and  this calculated expo-

sure level for TCDD (0,00018 ug/kg),  do not constitute  an
                            -109-

-------
ample margin of safety.  The Working Group therefore recom-



mends issuance of a rebuttable presumption against pesticide



products containing 2,4,5-T and/or TCDD pursuant to 40 CFR




Section 162.11(a)(3)(ii)(B).






       (iii)  Aerial Applicat ion;  EXPOs_e d.,P_opu 1 ation



              Directly Beneath Spray Plane






       Caplan et al. (167), working with aerially applied



malathion in oil sprays applied at 0,46 pounds per 0.76



gallons water/acre, determined a dermal exposure to persons



directly beneath the spray plane for bare skin (head, neck,



shoulders, forearms, hands, and thighs) of 3*556 mg/day.



With these data, an equivalent dermal exposure for 2,4,5-T



and TCDD, aerially applied at 4 pounds acid equivalent



2,U,5-T per  TO gallons water/acre, can be determined,





   Table ?0.  Dermal Exposure Pat?. (Agrj.g.1 fit? plication^
jDermal exposure to
{aerially applied
{malathion
\
i
lUse Dilution rate
!
1
! •
\
I
\% Diluted materiaT*"
jabsorbed
I
{Exposure level
1 ' . ."
I Dose level
1
1
! No-Ad verse-Effect
{level for terato-
jKenic effects
3.556 mg/0.46
per acre


2f4T5-T
4 pounds
2,4,5-T per
10 gallons of
water/acre


---TO? - •
.
• • ' - . - .- . ..
3«1 mg

0.051 mg/kg
" ' . •

20 mg/kg


pounds malathion



TCDD
0.0000004
pounds TCDD
per 10 gal-
lons of water
per acre

10$

.-•
0,0003 ug

5 X 10"6
ug/kg

0.03 ug/kg
!
I
                            -110-

-------
       The following calculations (see Table 31. for .mathe-

matics) will give the daily dermal exposure for both 2,4, 5-T

and TCDD:  1) divide the dermal exposure to malathion

by the malathion application rate and multiply by the

application rate of 2, 4, 5-T and TCDD to obtain the dermal

exposure; for TCDD, multiply this figure by 1,000 to convert

to microgramsj 2) multiply this figure by the percent

absorbed; and 3) divide this figure by the weight of the

applicator for the daily exposure to 2,4, 5-T or TCDD per

8-hour working day.
 	Table 31	
          2f 4r5-T            - j   •       TCDD             |
 1) 3.556 mg/0.46 pounds X     SD.3.556 mg/0.46 pounds X f
    4 pounds = 31 ng;          j    0.0000004 pounds =
                           .1    0.000003 mg X 1,000 =
                               I    0.003 ug;
 2) 31 mg X 102 = 3.1 mg;      !2) O.OC3 ug X 10$ =
                               j    0.0003 ug;
 3) 3.1 mg/ 60 kg =            J3) 0.0003 ug / 60 kg r
    0.051 mg/kg per day        {    _ v ,--6   ..        ,   ,
 		!    5 X 10   ug/kg per day !
   •    The Working Group considers that the difference

between the no-adverse-effect level of TCDD for teratogenic

effects (0.03 ug/kg) and this calculated dermal exposure

level for TCDD (5 X 10   ug/kg) does constitute an ample

nargin of safety.  The Working Group also considers,

however, that the difference between the no-adverse-effect

level of 2, 4, 5-T for teratogenic effects (20 mg/kg) and this

calculated dermal exposure level for 2,4, 5-T (0.051 mg/kg)


                          -111 & 112-

-------
does not constitute an ample margin of safety.  The Working

Group therefore recommends issuance of a rebuttable presumption

against pesticide products containing 2,4,5-T pursuant to

40 CFR Section 162.11(a)(3)(ii)(B).


       (c)  Inhalation.. Exposure;  Aerial Application


       There are no studies available on inhalation exposure

of 2,4,5-T.  There are, however, several studies on inhala-

tion exposure to malathion (167, 168) which CED used as a

model for this 2,4,5-T exposure analysis (164)*  Caplan et

al. (167) determined an air concentration, for unprotected

persons directly beneath the spray plane during application

and for two hours afterward, of 0*067 mg malathion/m^ from

aerial application of 0.46 pounds Al/gallon per acre.  The

collection period spanned the course of the actual application

time plus two hours thereafter.  The authors considered the-sam-

p.ling technique to be equivalent to average inspiration through

the nostrils.  This inhalation exposure (amount available for

inhalation) was 12$ of the applied malathion,  Caplan et al.

further reported that the average median diameter  ( = volume

median diameter, or vmd-^1 was 109 microns.  Based on work

by Akesson and Yates (168), CED (164) estimated that the

size of the malathion droplets which could be inhaled was
16/  The vmd is that droplet size-which divides the total
volume of drops in half, i.e», 50? of the volume is in
drops above the vmd size and 50? below it»
                          -113-

-------
under 60 micron?.  Since 2,4,5-1 is typically applied as a

medium or coarse spray, while malathion is applied as a fine

spray, the percent of 2,4,5-T droplets small enough to be

inhaled (under 60 microns) would be less than the percent of

malathion droplets small enough to be inhaled.  According to

Akesson and Yates (168), 2% of Z,4,5-T spray droplets would

be available for. inhalation (or 1/6 the amount of malathion

droplets available for inhalation), on a "worst case" basis.
  T a b 1 e 32»  Inhalation Exposure Data (Aerial Application)
JAir concentration of
{aerially applied
Imalathion
{Use Dilution rate
I
{Lung Absorption
{Rate
 Breathing Rate
\
{Exposure level

!         ..._,_
 Dose level

I
{No-Adverse-Effect
{level for terato-
'genic effects
                          0.067  mg/m    with application
                          rate  of 0.46  pounds  malathion
                          per -gallon  per  acre
                          2,4T5-T
                          4 pounds
                          2,4,5-T per
                          10 gallons  of
                          viater/acre
                          100?
                          1.8  nr/hr

                          0.34 mg
                          per  2 hr
0.023 mg/kg
per 8 hr

20 mg/kg
                   ?CDD
                   0.0000004
                   pounds TCDD
                   per 10 gal-
                   lons of water
                   per acre

                   10055
                   1.8 m°/hr

                   0.000032
                   ug per 2 hr
                                             2 X 10  ug/kg!
                                             per 8 hr
                                                          5
                                             0.03 ug/kg
                             .114-

-------
    1   The following calculations (see Table 33 for mathe-

matics) will give the daily inhalation exposure for both

2,4,5-T and TCDD:  1) multiply the air concentration of

malathion by the amount of 2,4,5-T and TCDD applied, then

multiply this figure by 1/6 for the inhalation exposure to

2,4,5-f and'TCDD; for TCDD, multiply this figure by 1,000 to

convert to micrograms; 2) multiply this figure by the

breathing rate; 3) multiply this figure by eight [8] to

get the 8-hour exposure total;'and 4) divide this figure

by the weight of the applicator for the inhalation exposure

to 2,4,5-T or TCDD per 8-hours exposure.


   •	Table 33.    	'
          2. /I.5-T
 1) 0.067 mg/cu m per 0.46
    pounds X 4 pounds = 0.58
    mg/cu m X 1/6 s 0.097
  -  mg/cu m;               ;
 2) 0.097 mg/cu m X 1.8 cu m/-
    h'r = 0.17 mg/hr;

 3) 0.17 mg/hr X 8 = 1.36 mg;
         TCDD
1) 0.067 mg/cu m per 0.46
   pounds X 0,0000004
   pounds = 0.000000058
   ng/cu n X 1/6 s
   0.000000009 ng/cu m X
 1,000 = 0.000009 ug/cu m;
2) 0.000009 ug/cu m X
   1.8 cu ra/hr =
  • 0.000016 ug/hr;
3) 0.000016 ug/hr X
                                   8 = 0,000128 ug;
!4) 1.36 mg / 60 kg =          !4) 0.000128 / 60 kg =
I   0.026 mg/kg exposure       }          -6
J _   per day	.	I    2 X 10   ug/kg -per
       The Working Group considers that the difference

between the no-adverse-effect level of TCDD for teratogenic

effects (0«03 ug/kg) and this calculated dermal exposure

level for TCDD (2 X 10   ug/kg) does constitute an ample

margin of safety.  The Working Group also considers,


                        -115-

-------
 however,  that  the  difference  between  the  no-adverse-effect

 level  of  2,4,5-T for  teratogenic  effects  (20 ag/kg) and  this


 calculated  dermal  exposure  level  for  2,4,5-T (0.026 mg/kg-^-M

 does not  constitute an  ample  margin of  safety.   The Working

 Group  therefore recommends  issuance of  a  rebuttable presumption

 against pesticide  products  containing 2,4,5-T  pursuant to i|0

 CFR Section 162.11(a)(3)(ii)(B).              .

        (d)   Cumulative  Exposure              '

       The  Working Group  has  also considered the possibility

 of a single individual  being  exposed  through two or more of

 the above routes.  The results (derived  from Tables 27> 29»

 and 31) are shown  in  Table  3^.  The Working Group also notes

 that possible  cumulative  exposure to  several dioxin-containing

 pesticides  could increase the total body  burden  and increase

 total  risk  from dioxin  exposure.  .            :
V    .        •         -      .          '             ''-'.-     •  • :
       The  Working Group  considers that the differences

 between the no-adverse-effect level of  TCDD for  terato-

 genic  ef.fects  (0.03 ug/kg)  and  the calculated  cumulative

 exposure  levels for TCDD  in Situations  2   and  3  (see  Table

 34) do constitute  an  ample  margin of  safety.   The Working
     Johnson  (63)  [see  Section  I.G.(3)],  in  a  review  article,
 calculated a  daily  inhalation  exposure  to phenoxy  herbicides
 of 0.025  ug/kg  for  a 70-kg  adult.   The  calculations  were
 based  on  actual  air monitoring data of  air  samples collected
.in two wheat-growing areas  in  the  state  of  Washington  during
 spring and summer and  analyzed for phenoxy  herbicides.   The
 author did not  specify how  soon after application  the
 samples were  taken.

                        -116-

-------
  Table .34. ._.Cumulative Exposure to 2,4f5-T and TCDD
I   Situation #1 ;   2.4.5-T  i     Situation # i :  TCDD
(Oral-   0.0007 mg/kg      }0ral-      	
JDermal- 6.8 mg/kg         IDermal- 0.0007  ug/kg
*                    4       |                     •
llnhal.- 0.2 mg/kg5-        llnhal.- negligible3-
ICum. =  7.0 mg/kg         iCum. =  0.0007  ug/kg
i                           i
I   Situation *2;   2.4.5-T  i     Situation #2:  TCDD
SOral-   0.0007 mg/kg      !Oral-      	
iDermal- 1,8 lag/kg      •   iDermal- 0.00018 ug/kg
llnhal.- Oi.05a/            llnhal.- negligible-7
{Cum. =  1.85 mg/kg        |Cum. =  0.00018 ug/kg

!   Situation #?:   2.4.5-T  i     Situation ?n;  TCDD
JOral-   0.0007 mg/kg      iOral-    .  	
                           !i                 g
 Dermal- 0.051 mg/kg       IDermal- 5 X 10   ug/kg
llnhal.- 0.026 mg/kg       llnhal.- 2 X 10~6 ug/kg
I                           I                 £
{Gun. =  0.0777 nz/ke	!• Cua. r  7 Y 10   ug/kg	
&/  Calculations were made on a worst-case  basis as 3$
of dermal exposure based on Wolfe (179) who states, "over
97$ of the pesticide to which the body is subjected during
most exposure situations, and especially to applicators of
liquid sprays, is deposited on  the skin."   TCDD inhalation
exposure values were negligible:  Situation #1, 21 X 10~
ug/kg; Situation #2, 54 X 10~7  ug/kg.
Croup also considers, however, that the differences between

the no-adverse-effect levels of 2,4,5-T and TCDD for terato-

genie effects (20 mg/kg and 0.03 ug/kg, respectively) and

the calculated cumulative exposure levels for 2,4,5-T in

Situations 1, 2, and 3 and TCDD in Situation 1 (see Table

34) do not constitute an ample margin of safety.  The

Working Group th~er~efore- recommends issuance of a rebuttable

presumption against pesticide products containing 2,4,5-T

pursuant to 40 CFR Section 162.1 1 (a)(3)(ii)(B).


                        -117-

-------
IV.  STUDIES RELATING TO POSSIBLE ADVERSE EFFECTS






       This section addresses other types of adverse




effects of 2,-^,5-T for which the Working Group has deter-




mined that insufficient evidence exists to initiate a



rebuttable presumption.  The Agency solicits comments




from registrants and other interested parties on the




evidence listed below, and requests submission of any




additional studies or relevant information on 2,4,5-T




and/or TCDD relative to these potential adverse effects.






     A.  Mutaggnicitv    _                  .        ....






       Section 162.11(a)(3)(ii)(A) provides that a rebuttable



•presumption shall arise if a pesticide's ingredient(s),



aetabolitefs), or degradation product(s) induce mutagenic



effects, as determined by multitest evidence.                .






     (1)  2f 4.5-T






       (a) .' positive Study






       Majumdar and Golia (178) fed male Pro soph 11 a me1ano-



jgaster either 250 or 1,000 ppm dioxin free 2,4,5-T (obtained



from Eastman Kodak) for 15 days.  They were then mated to



sets of virgin females to generate three 4-day broods of



offspring.  F  flies were allowed to mate, and F  flies were



scored for X-linked recessive lethals.  No differences among






                               -118-

-------
 broods were  noted, and  data  from all  broods were  pooled.



 The  percent  lethals  in  controls, 250  and  1,000  ppm  groups



 were dose-related  and were 0.05> 0.26,  and 0.66$, respectively.



 The  control  vs,  1,000 ppm lethal rates  were significantly



 different  from  one another (p  < 0,01),  Ethyl methane



 sulfonate  (250  ppm)  was included as  a positive  control;



 it yielded 13.70?  lethals.   The total number of flies



 in each  experimental group was no  larger  than 2,000.
                                                        *



        (b)  Negative Studies,





        The mutagenicity of 2,4,5-T was evaluated by Ercegovich



 et al»  (148),  employing the  procedure of  Ames,  using five



 strains  of galmonella  typhimurium  without activation.   They



 concluded  that  2,4,5-T  is not.mutagenic.

 •- ••'*-   • "            .                     ' "



        Fujita et al. (149) reported chromosomal abnormalities



 in Jji vitro cytogenetic studies  of human  lymphocytes


             • -7      -4
 exposed to 10   to 10   M of 2,4,5-T, which  contained 0.09



 ppm TCDD.   Breaks, deletions,  and  rings were  observed.



,.£hromatid  breaks increased with  increasing concentrations



 of 2,4,5-T%  It was  not possible  to distinguish whether this



 was a toxic effect or a potential  genetic effect (150).
                            .119-

-------
       Majundar and Hall (169) reported on .the cyto-

genetic effects of 2,4,5-T—^  on in vivo bone-marrow

cells of Mongolian gerbils.  The animals were injected

with total amounts of 2,4,5-T at the rate of 50, 150,

250, 350, or 500 mg/kg body weight over the 5-day period

of the study.  Increasing numbers of chromatic gaps,

breaks, and fragments were observed at 250, 350, and

500 mg/kg doses.  No exchange figures or isochromosozne

gaps or breaks were observed.  This is not a definitive

experiment for indicating the potential of 2,4,5-T for

causing heritable chromosome damage (170)»  Toxicity

effects of the chemical could give similar results (170).


       Davring and Hultgren (171) reported on an JLn

ylvo study on the cytogenetic effects on bone-marrow

cells of tyu_4 musculus (male mice) induced by a Swedish
                                    TO/
commercial 2,4,5-T ester formulation-^  and its compo-

nents.  The study showed that 2,4,5-T commercial pro-

ducts can affect chromosomal and reproductive mechanisms,

Two different strains of mice were used with similar

results for both.  These results correlated with effects

seen in Drosophila.  The authors stated that chromatid
     The 2,4,5-T used in this study was purchased from
Eastman Kodak Company, Rochester, N.Y,, and contained
no measurable amount of TCDD.  The authors do not indi-
cate the limit of sensitivity.
JL2/  The concentration of TCDD was guaranteed to be  .
less than 0.1 ppm in the product,

                        -120-

-------
protocol were given,  and statistical methods were apparently




not employed in assessing the data.






       The second test by Hussain et al. (24) studied



reverse mutation from histidine dependence to histidine




independence in Salmonella tvphimurlum (Strains TA 1532 and




TA 1530).  TCDD was positive in TA 1532 but negative in TA




1530.  This indicated that TCDD acts as a frameshift mutagen.




ICR-170 was used as a positive control in the test with TA




1532.  No positive or negative controls were tested in IA




1530*






       In the third test Hussain et al, (24) observed slight



prophage induction in £» o o1i K-39.   However, data from this



test were difficult to evaluate because the solvent used,



dimethyl sulfoxide, causes cellular effects,






       A preliminary report on the chromosomal analysis of



hospital.patients exposed to TCDD in the accident at the



Seveso, Italy, factory was presented at the Department of



Health, Education, and Welfare meeting on October 12, 1976



(152).  An increased number of chromosomal lesions (gaps,



chromatidic and chromosomal breaks,  and rearrangements) were



observed in  somatic cells of the 2- to 28-year-old males



and females tested.  Cytogenetic studies of tissues from



therapeutic abortions performed on women who were exposed to



TCDD during the accident indicated that there was chromosomal






                             -122-

-------
damage to cells in maternal peripheral blood, and placental




and fetal tissues.  These preliminary results were based on



a small number of samples, and no specific data are available




at this time (150).






       (b) Negative Studies






       Khera and Ruddick (6) conducted dominant lethal tests




in which male Wistar rats received TCDD at dosages of 4 and



8 ug/kg per day. The studies indicated that no dominant



lethal mutations arose during the 35 days after treatment.



The period examined corresponded to postmeiotic stages of




spermatogenesis,






       A cytogenetic screening study of the effects of TCDD



on bone marrow cells of male Osborne-Mendel rats was per-



formed by the Food and Drug Administration (119). Two



separate experiments were performed. The first was a multiple



dose test in which 10 ug TCDD/kg per day was administered by



intubation for 5 consecutive days* In the second test,



single doses of 5, 10, and 15 ug TCDD/kg were administered



intraperitoneally and 20 ug/kg (the highest dose) was



administered orally.  There was no evidence "-•from these



studies to indicate that TCDD produced cytogenetic damage in



the bone marrow of these male rats.  Toxicity, which was



indicated by a slight weight loss, was noted in  rats that



received a single dose of 15 or 20 ug/kg (the highest



dose levels).




                          -123-

-------
       Green (119) conducted a short-term investigation of




several dioxins, using male Osborne-Mendel rats, to determine




what potential these substances had to produce cytogenetic




damage in rat bone-marrow.   In one study all of the dioxins




were tested by being intubated in the rats for five consecu-




tive days at 10 ug/kg per day.  A second study involved TCDD




alone administered orally at 20 ug/kg and intraperitoneally




at 5, 10, and 15 ug/kg.  The author found no evidence that



any of the substances tested produced cytogenetic damage in



the bone marrow of male rats,






       In conclusion, although Hussain et al» (2*0  have



demonstrated that TCDD does appear to act as a point .(gene)



mutagen, the evidence is weak for heritable genetic effects




since the level of mutagenic testing is meager and  there




were some major deficiences in some tests. However, the




study by Hussain et al. does not fulfill the criterion of



multitest•evidence as prescribed in HO CFR 162.11.  Although



TCDD does appear to have the potential to act as a  chromosomal



mutagen from the In vivo cytogenetic studies (152), specific



data are not yet available from the Seveso accident.








     (3)  Chromosomal Damage






       The Working Group also wishes to call attention



to three studies [previously discussed in Sections  III.B.(2)(b),



IV. (1), and IV.(2Mb)], which indicate that 2,H,5-T and/or

-------
TCDD may cause chrooosomal damage.  Fujita et al. (



reported chromosomal abnormalities in jLn, vitro- tests on




human lymphocytes exposed to 2,4,5-T; abnormalities included




breaks, deletions, and rings.  Yefimenko (16?) reported




damage.to bone-marrow cell chromosomes (including breaks,




true aberrations, or rearrangements) in jjl vivo tests on rat




gonadal and somatic tissue exposed to butyl ester 2,4,5-T.




The preliminary HEW report (152) on the Seveso incident



indicated an increased number of chromosomal lesions (gaps,



chromatic breaks, and rearrangements) in somatic cells of 2-




to 28-year-old humans exposed to TODD.




       The Working Group concludes that there is a data gap




on mutagenic -effects and that further evidence and testing



is needed on the mutagenicity of 2,4,5-T and TCDD.  The



Working Group would like to evaluate more detailed and



specific information as it becomes available from the Seveso



.accident.  Relevant information or studies on the mutagenetic



effects' of 2,4,5-T and/or TCDD should be submitted to the



Agency, and the option for re-evaluating their mutagenic



properties must be left open should more conclusive evidence



become available.                  •         .



     B.  Toxicitv to Humans:  TCDD



     (t)  Chloracne



       A number of researchers have reported illness ascribed



to TCDD (90, 93, 95, 153).  Most of these toxic effects have



                        -125-

-------
occurred in chemical plant workers after accidental exposure




to the dioxin.  While a number of ill effects have been




reported, the most widely known is chloracne,






       Chloracne is a severe skin disease resulting from




exposure to highly chlorinated dibenzo dioxins.  It is a




disease of the follicular and sebaceous glands.  Its




symptoms and signs include skin lesions, follicular hyper-
                                                 •



keratosis, and the formation of large sebaceous cysts,




inflammed tubercles, and pustules.  In addition to these




symptoms, chloracne is often accompanied by a brownish




keratinization of the skin, cystitis, pyelonephritis,




depression, hirsutism, fatigue, neurological disturbances,




raised cholesterol levels, liver damage, and psychological




manifestations (10, 15, 16, 154, 155, 156,  157).   Several



researchers have observed that chloracne is not only irritat-




ing and persistent but also very difficult  t'o cure.  It is




one of the most frequently contracted forms of occupational




dermatitis, occurring primarily in chemical plant employees


      «

engaged in the production of 2,4,5-T and 2,4,5-TCP (16, 95,




155, 156, 158).


        • • •   '         • '      '             .    *


       The first report on a toxic material being the




causative agent for an occupational skin disease appears to




have been by Dr. Karl Herxheimer in 1899.  Dr. Herxheimer




diagnosed the cause of dermatological problems in a German






                           -126-

-------
factory worker as exposure to chlorine ions in the produc-



tion of caustic potash (159).  It is from, this early



diagnosis that we get the name chloracne.  During the early



1950's there were a series of industrial accidents in



Germany resulting in an outbreak of chloracne in the



employees of chemical plants manufacturing 2,4,5-T and



2,4,5-TCP.  The. symptoms of the employees of one of these



factories in Hamburg, Germany, were extensively ' investigated



by Kimming and Schulz (16)*  These researchers, using



the rabbit ear test, proved that the cause of the chloracne



was a contaminant found in crude 2,4,5-TCP and not the



formulated 2,4,5-TCP.  Later on, Bauer et al, (15) conclusively



identified TCDD as the causative agent of chloracne,





   '•."- (2)  Porr>hvrla cutanea tarda and P -Aminolevulinic



••'.-.-."•:'•' " Acid Svnthetase            ..       ' -.   • '.  .'''•'.





 _ '.... .  Porphyria cutanea tarda (PCT) , a form of hepatic



porphyria, is another disease caused by exposure to TCDD



and often accompanies chloracne.  PCT occurs primarily in



industrial workers associated with the manufacture of



'2,4,5-T (93,~9T
       The symptoms of porphyria cutanea tarda, a defect in



hepatic metabolism of porphyrins, are fragility of the



skin, photosensitivity of the skin, hyperpigmentation,



over-production of porphyrins, hirsutism, and neurological






                            -127-

-------
and intestinal disorders (9^i 160).  It is also characterized




biochemically by an increase in the activity of the mitochon-




drial enzyme  6-aminolevulinic acid (ALA) synthetase, which




is the first and rate-limiting enzyme in heme biosynthesis




(160)»  TCDD was thought to be a potent inducer of ALA




activity in chick embryo liver (115)* Goldstein et al. (161)
                                                            r—



reported that TCDD was found to induce ALA synthetase and




hepatic prophyria in mice.  These researchers stated that at




that time [1973] TCDD was the most potent porphyrogenic



chemical known*   Poland and Kende 1976 (*J) found that the



duration of ALA induction from TCDD exposure is prolonged,




most likely due to the long biological half-life of TCDD,




These researchers also found that ALA synthetase inducers



have halogen atoms occupying at least three of the four




lateral ring positions (positions 2, 3> 7, and 8), and that



there is at least one free, nonhalogenated ring position.



TCDD fulfills all of these requirements.
                           »128-

-------
             2,4,5-T:   Position Document 1

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                              .131-

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*33.  Shafik, M.T., H^C. Sullivan, and H.F, Enos.  1971*
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*-36»  Clark, D,E., J.S. Palmer, R.D. Radeleff, H.R.
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                              -132-

-------
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*45,  Highman, B., T.B, Gaines, and H.J. Schumacher.
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                            -133-

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«»51.  Kenaga, E.E.  1974,  2,4,5-T and  derivatives:
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C57«  Isensee, A.R., and G.E.  Jones,   1975»   Distri-
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C59.  Brown, E., and Y.A. Nishioka,  1967.   Pesticides
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                            -134-

-------
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*62»  National Research Council, Safe Drinking Water
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*66.  Zielinski, W,L», Jr., and L. Fishbein.  1967*  Gas
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*67»  Piper, W*N., J.Q. Rose, M.L. Leng, and P,J, Gehring.
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