United States
Environmental Protection
Agency
Health Effects Research
Laboratory
Cincinnati OH 45268
Research and Development
EPA-600/S1 -81 -068  Dec. 1981
Project  Summary
Study  of  Chlorine  Dioxide and
Its  Metabolites  in  Man

Joseph R. Bianchine, Judith R. Lubbers, Sudha Chauhan, and Judy Miller
  To assess the relative  safety of
chronically   administered   chlorine
water disinfectants in man, a control-
led study was undertaken.  The study
was conducted in three phases. Phase
I,  a rising, single dose  tolerance
investigation examined the effects of
chlorine  disinfectants  in  normal
healthy adult male volunteers. Phase II
considered the effect on normal sub-
jects of daily ingestion of disinfectants
at a concentration of 5 mg/L  over a
12 week period. In phase III, chlorite,
at a concentration  of 5 mg/L,  was
administered daily to a limited number
(3)  of  gIucose-6 -phosphate
dehydrogenase  (G-6-PO)   deficient
subjects. Physiological  impact  was
assessed by  evaluation of a  large
battery of qualitative and quantitative
tests.
  In  general, the study affirmed the
relative safety and tolerance of normal
healthy  adult  males  and  normal
healthy  adult male G-6-PD deficient
individuals to the daily ingestion of 2.5
mg of chlorite for a  12 week period.
  This Project Summary was develop-
ed by EPA's Health  Effects Research
Laboratory,  Cincinnati,   OH,  to
announce key findings of the research
project that is fully  documented in a
separate report of the same title (see
Project Report ordering information at
back).
Introduction

  Chlorine dioxide  (CIO2J  has  been
identified as a potential water disinfect-
ant alternative to chlorination. A three-
phase  human  investigation  was
undertaken to assess the safety of ClOa
and its metabolites.
  In  Phase  I.  Rising-Dose Tolerance
Study, a controlled double-blind study
was  initiated to assess the safety of
single dose  administration of CI02
and its metabolites over a broad range of
concentrations. Normal  healthy adult
males were treated  with  successive
increasing doses of chlorine dioxide,
chlorite, chlorate, chloramine, chlorine
or  untreated   water  (control).  The
concentration ranges examined were as
follows: chlorine dioxide,  0.1 to 24.0
ppm;  chlorite,  0.01  to  12.0  ppm;
chlorate, 0.01 to 1 2.0 ppm; chloramine,
0.01  to 24.0 ppm; and chlorine, 0.01 to
24.0 ppm
  In Phase II: Chronic Administration to
Normal Subjects. Sixty volunteers were
divided, at random, into six double-blind
treatment groups of 10  subjects each
for the administration  of CIO2, CI02
metabolites,  chlorite  (CIC)2~)  and
chlorate  (ClOs"); chloramine (NH2CI);
chlorine; and control, distilled  water.
The  20-week protocol involved a  12
week period of daily oral administration
of 500 mL of treated water followed by
an 8-week observation period. The con-
centration of water disinfectants was 5
mg/L. Urine and blood samples col-
lected at  weekly intervals  were sub-
jected to  complete  routine  clinical
analysis and to  special determinations
for methemoglobm, glutathione, G-6-
PD  and  thyroid function.  Subjective
evaluation  of  the qualitative clinical
tests was coupled with  the statistical
evaluation of all quantitative chemical
parameters.
  In Phase III. Chronic Administration to
G-6-PD  Deficient Subjects.  Three

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healthy male  volunteers found to be
deficient in G-6-PD were chosen for the
study.   All  three   subjects  ingested
chlorite; no concurrent control study
was performed The study protocol was
identical to that of Phase II in temporal
design  and  evaluatipn  procedures.
Volunteers  received 500 ml_ daily  of
sodium chlorite at  a concentration of 5
mg/L chlorite.

Materials and Methods

Subject Selection
  Normal healthy adult male volunteers
selected for inclusion in this study were
required to satisfy the following criteria:

  1.  Subjects were between 21  and
     45 years of  age and  were not
     confined to an institution.

  2.  Subjects   had   no   significant
     abnormal physical findings at the
     pretreatment physical  examina-
     tion.

  3.  Subj'ects had no laboratory values
     significantly  outside  the normal
     range at the pretreatment evalua-
     tion.

  4.  Subjects weighed at the time of
     the  pretreatment evaluation
     within ± 10% of the normal body
     weight for their frame and stature
     based on a standard weight table.

  5.  All subjects gave written consent
     to participate in the study.

Subjects were  excluded from the study
if they.

  1.  Had  symptoms  of   significant
     clinical illness in the two weeks
     preceding the study;

  2.  received any drugs in  the  four
     weeks preceding  the initiation of
     this study;

  3.  required any concomitant medi-
     cation;

  4.  had  one  or  more  surgical or
     medical  condition which  might
     interfere  with the  absorption,
     metabolism or excretion of sub-
     stances by the body;

  5.  -had a known hypersensitivity to
     drugs,  food   or  environmental
     factors;
  6.   had a history of cardiac, renal,
      hepatic,  neurologic, hematologic
      or gastrointestinal disease; and

  7.   had a history of drug addiction

  For Phase III, volunteers were defined
as G-6-PD deficient on the basis of a
hemoglobin G-6-PD level of less than
5.0 IU/GM hemoglobin in the pre-study
screening.  Phase  III  subjects  were
normal in all other respects
  No  subject who entered this study
was   undergoing  concurrent  drug
therapy.  However, once on  study, a
record was kept  of the  occasional
episode of any physician-administered
drug therapy that was required because
of intercurrent illness. No subject was
dropped from the study because of any
intercurrent  illness   that  developed
during this study.


Discussion

   During the course of the three phase
study, a  massive volume of raw data
was acquired. For each of the partici-
pants,  subjective  information   was
collected at regular intervals concern-
ing  general medical  well-being. The
interpretation of physical examinations,
electrocardiograms. Coombs tests, and
hemoglobin electrophoresis increased
the  amount of  available information
Vital  signs (blood pressure, heart rate,
body temperature and respiratory rate)
for each study subject were determined
and compiled. Qualitative examinations
of individual blood and  urine samples
were made.  Further, 47  quantitative
chemical  parameters derived from the
extensive battery of  blood  and  urine
testing   procedures   were   recorded
regularly. The conclusions drawn in this
report were drawn from this body of
information.
   The incidence of  minor illnesses,
such as "colds" and the "flu" were
evenly  distributed  among  treatment
groups  and control  groups. Physical
examinations  revealed  no  treatment-
related pathology. Coombs test results
were consistently normal throughout
the study for the treatment groups and
the  control groups.  The incidence of
borderline abnormal hemoglobin
electrophoresis was greatest during the
posttreatment observation  period; no
relationship between treatment and the
presence  of   abnormal,  hemoglobin
electrophoresis  could  be  established.
Examination  of individual  vital  sign
parameters and statistical evaluation of
those parameters failed to identify any
changes in vital signs  which could be
attributed to treatment  with any of the
water  disinfectants.  Abnormalities  in
the qualitative blood and urine analyses
were few and,  again,  appeared  to be
randomly distributed.

Conclusion
  All three phases of this large control-
led and double  blinded  clinical evalua-
tion of ClOaand its potential metabolites
m human male volunteer subjects were
completed uneventfully, There were no
obvious undesirable clinical  sequellae
noted by any of the participating sub-
jects or the observing medical team. In
several cases  statistically  significant
trends in certain biochemical or physio-
logical  parameters were  associated
with treatment; however, none of these
trends were judged to have physiolog-
ical consequence. One  cannot rule out
the possibility that, over a longer treat-
ment period, these trends might indeed
achieve clinical importance.  However,
within the limits of the  study, the rela-
tive safety of orgal ingestion of ClC^and
its metabolites,  chlorite and chlorate,
was demonstrated.

Recommendations
  This  study was  limited  in  some
respects:

   1.  Only  male  volunteers  partici-
      pated.

  2.  Treatment  was  limited to  12
      weeks

  3.  The number of G-6-PD deficient
      subjects was very small.

  4   The dose of disinfectants  was
      fairly low.

  With this in mind,  we make several
recommendations. In  use of chlorine
dioxide as a water  disinfectant, the
entire population will ingest  the disin-
fectant and its  byproducts over a long
period of time. The safety of ingestion in
women and children must be assessed.
The length of study should be increased.
Furthermore, on the basis of Phase III,
the absence  of detrimental effects on
potentially  susceptible individuals
cannot be ascertained with confidence;
the sample  size  was  limited and no
concurrent control was run. If chlorine
dioxide is to be used as  a primary disin-
fectant,  human  invegtigations  at

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increased dose levels ought to be con-
ducted.
  Supplementary information including
computer printouts, tables, figures, vital
sign tabulations, subject histories, and
clinical/chemical parameters are on file
at the Health Effects Research Labora-
tory, Cincinnati, Ohio.
Joseph Ft. Bianchine, Judith Ft. Lubbers. Sudha Chauhan, and Judy Miller are
  with  the  Department of  Pharmacology,  Ohio  State  University,
  Columbus, OH 43210.
Richard Bull is the EPA Project Officer (see below).
The complete report, entitled "Study of Chlorine Dioxide and Its Metabolites in
  Man."  (Order No. PB 82-109 356: Cost: $9.50, subject to change) will be
  available only from:
          National Technical Information Service
          5285 Port Royal Road
          Springfield, VA 22161
          Telephone: 703-487-4650
The EPA  Project Officer can be contacted at:
          Health Effects Research Laboratory
          U.S.  Environmental Protection Agency
          Cincinnati,  OH 45268
                                                                            ti US GOVERNMENT PRINTING OFFICE 1981—559-017/7403

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United States
Environmental Protection
Agency
Center for Environmental Research
Information
Cincinnati OH 45268
Postage and
Fees Paid
Environmental
Protection
Agency
EPA 335
Official Business
Penalty for Private Use $300

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