UnH«i Sttt« Office of Pesticides end Toxic Sut»tanee> EiiKliuniiuitil Protection Office of Pesticide Programs (TS-766C) Agency Washington. DC 20460 &EPA Pesticide Fact Sheet Name of Chemical: Paraquat Reason for Issuance: Registration Standard Date Issued: Jfe It W 9HQPv w *^ ^V^P* Fact Sheet Number: 131 1. Description of Chemical Generic Name: 1 ,1'-dimethyl-4-41-bipyridinium ion Common Name: Paraquat Trade Names: Actor Cekuquat, Crisquat, Dextrone, Dexuron, Esgrara, Gramanol, Gramoxone, Gramuron, Hebaxon, Herboxone, Goldquat 276, Paracol Paraquat CL, Pillarquat, Pillarxone, Sweep, PP148 (dichloride) and Dextrone X. EPA Shaughnessy Code: 061601 (dichloride) Chemical Abstracts Service (CAS) Number: 1910-42-5 (dichloride) Year of Initial Registration: 1964 Pesticide Type: Herbicide, defoliant, desiccant, and plant growth regulator Chemical Family: Bipyridylnium or dipyridylnium U.S. and Foreign Producers: ICI Americas, Inc.; Taiwan by Comlets Chemical Industrial Company, Ltd., and Shinung Corp., Italy by VisplantChriraiasero S.p.I.; Spain by Hightex S.A.; Great Britain by ICI Plant Protection Division. 2. Use Patterns and Formulations Application Sites: Terrestrial food crops; terrestrial nonfood crops; terrestrial noncrop, forestry and domestic outdoor sites. Major Crops Treated: Field crops (corn and soybeans), and fruit and nut crops. Types and Method of Application: Foliarly applied by broadcast, band, or directed spray by ground equipment or broadcast by aircraft. It may be applied preplant, preemergence, or preharvest in relation to the crop. ------- —2— Application Rates: 0.25 lb active ingredient/A to 1.0 lb active ingredient/A (0.28 to 1.12 kg active ingredient/ha). Types of Formulation: Aqueous solution containing 2 lbs (0.24 kg) paraquat cation per gal (L). Usual Carrier: Water. 3. Science Findings Summary Science Statement: Paraquat is extremely toxic (Category I) via oral, dermal, and inhalation exposure routes to mammals. It is not teratogenic to mice or rats. Paraquat is not oncogenic to mice but is oncogenic to rats. Paraquat is weakly genotoxic - it was negative for mutagenicity in eight studies, weakly positive in four studies and positive in four studies. Paraquat is moderately toxic to birds, slightly toxic to freshwater fish, moderately toxic to aquatic invertebrates, and relatively nontoxic to honeybees. Paraquat is not believed to cause problems 1th stable wildlife populations but may be hazardous to unstable or endangered populations of plants and animals. Paraquat dichioride was stable to hydrolysis and photo- lysis in soil, preliminary data indicate that paraquat has a half-life of greater than 2 weeks in water plus soil, is immobile in silt loam and silty clay loam, and slightly mobile in sandy loam and potentially mobile in sandy soils extremely low in organic matter. The half- life of paraquat in water is approximately 23 weeks. Paraquat is not readily desorbed from the soil and is not likely to contaminate ground water in agricultural soils. Preliminary data indicate that the paraquat degradate 14 C-carboxy-1-methyl pyridiniuni (QINA) chloride is loosely absorbed in the soil and is potentially mobile and has a leaching potential. Chemical Characteristics: Analytical grade of paraquat dichioride is a colorless odorless hygroscopic powder, whereas the technical product is yellow. Paraquat is very soluble in water, slightly soluble in alcohols and insoluble in hydrocarbons. It is nonvolatile, corrosive to metals, stable at room temperature (either as a solid or an aqueous solution at neutral or acidic pH), but is hydrolyzed by alkali, decomposes photocheTnically , and melts (with decomposition) at 300 °C. ------- —3— Toxicology Characteristics: Acute Toxicology Acute Oral Toxicity = 100 and 126 mg paraquat cation/kg (rat) for males; 112-150 mg paraquat cation/kg for females Toxicity Category II Acute Oral Toxicity = 22 mg paraquat cation/kg for (guinea pig) males and females Toxicity Category I Acute Dermal Toxicity = 59.9 mg paraquat cation/kg (rabbit) Toxicity Category I Acute Inhalation = 0.6 to 1.4 ug paraquat ion/L (rat) Toxicity Category I Eye Irritation = Severe Eye Irritant (rabbit) Toxicity Category I Primary Derraal Irritation = Primary irritation score of (rabbit) 2.1 - Toxicity Category III Skin Sensitization = Not a sensitizer (guinea pig) Major Routes of Exposure: Acute Inhalation: Two inhalation studies were submitted. One study had an inhalation toxicity of about 1.0 ugfL (Toxicity Category I) with 90 percent of the particle diameters below 0.3 urn. A second study was performed with particles of median diameter of 21.5 to 23 urn. The inhalation toxicity for this study was 3.5 ugiL (Toxicity Category 1). These studies show that inhala- tion toxicity is highly dependent on particle size. Information received on particle size of paraquat droplets formed during aerial application and during knapsack spraying indicate that virtually no droplets smaller than 15 urn were formed during either method of application. Subchronic Dermal Exposure: A 21-day dermal toxicity study in rabbits was submitted with a NOEL of 1.15 mg paraquat cation/kg body weight (bwt) for local skin effects and a NOEL for systemic toxicity of 6 mg paraquat cation/kg bwt. Data are available indicating that a dermal absorption rate for humans is about 0.5 percent. These data are ------- -4- preferable to dermal data from other species, therefore, the dermal data in rabbits are not of cond ern. Combination of Acute Inhalation and Dermal Exposure: Mar- gins of safety were calculated for combined inhalation and dermal exposure of workers repeatedly exposed to paraquat. Combined inhalation and dermal exposures of several groups of workers were then compared to a NOEL of 0.5 mg paraquat cation/kg/day derived from a 90-day dog-feeding study. The lowest effect level (LEL) for this study was 1.5 mg paraquat cation/kg/day, at which dosage level toxic effects in the lung were observed. All but two of the margins of safety are greater than 100. Chronic Toxicology: Teratology and Reproduction Paraquat was not teratogenic to mice. The fetotoxic NOEL is 5 ing paraquat cation/kg bwt and the maternal NOEL is 1.0 mg paraquat cation/kg bwt. Paraquat was not teratogenic to rats. Both the feto- toxic and maternal NOEL are 1.0 mg paraquat cation/kg bwt. Paraquat had no effect on reproduction in rats. The systemic NOEL for reproduction is 25 parts per million (ppm). The teratology and reproduction studies are acceptable and show no reason to place paraquat in Special Review. Chronic Feeding - Oncogenic Studies In the rat chronic feeding study, the systemic NOEL is 25 ppm of paraquat cation per kilogram of body weight and the systemic LEL is 75 ppm. In the 1-year dog study the systemic NOEL Is 15 ppm paraquat cation per kilogram of body weight. The systemic LEL is 30 ppm. Paraquat was not oncogenic to mice. The systemic NOEL is 12.5 ppm of paraquat cation per kilogram of body weight. This study is acceptable. Paraquat was oncogenic to rats. Squamous cell carci- noma occurred in 51.6 percent of all rats having tumors of the skin and suhcutis in the head region. In high ------- -5- dose males, the incidence was significantly increased over concurrent controls. Mutagenicity: Paraquat was negative in eight studies (mostly in gene mutation and chromosomal aberration assays); weakly positive in two gene mutations, one chromosomal aberration and one DNA damage/repair assays; and positive in four DNA damage/repair assays. Physiological and Biochemical Behavior Characteristics: Foliar Absorption: Very rapidly absorbed by the foliage. Translocation: Can occur via the xylem under certain conditions. Mechanism of Pesticidal Action: Lipid peroxidation result- ing in disruption of cell membrane. Metabolism and Persistence in Plants: In sunlight, limit- ed photochemical breakdown occurs for paraquat which remains on the outside of treated plants. Since plants are killed rapidly in bright sunlight, signifi- cant quantities of the breakdown products are formed only on surfaces of dead tissues and there is no movement of these substances from the dead tissues to other parts of the plant. Environmental Characteristics: Absorption and Leaching in Basic Soil Types: Langmuir adsorption maxima values (m) ranged from 17 to 46.8 mg/100 grams on seven clay soils and one silty clay loam soil. Adsorption is positively correlated with soil cation exchange capacity (CEC). Paraquat is not readily desorbed from the soil and is not likely to contaminate ground water in agricultural soils. Data are required to determine the potential for the QINA degradate to leach in soils. Microbial Breakdown: Bound paraquat is degraded with difficulty or not at all. Loss from Photodecomposition and/or Volatilization: Does not volatilize; limited photodecomposition may occur on sprayed leaf surfaces and dead vegetation. Contamination of Ground and Surface Water: Paraquat binds tightly to the soil and does not leach in agricultural soils. ------- -6 Exposure of Humans and Nontarget Organisms to Chemical or Degradates: Margins of safety for humans appear ade- quate when product is used according to label direc- tions. Use of paraquat nay have an effect on a few mammals or ground nesting birds under unusual circum- stances. Wildlife populations should not be adversely affected when paraquat is used according to label directions. Exposure During Reentry: Current precautionary labeling and worker safety rules adequately protect worker, mixer, loader, applicator. Ecological Characteristics: Paraquat is moderately toxic to birds and aquatic invertebrates and slightly toxic to freshwater fish. Avian Acute Oral Toxicity with Bobwhite quail: 176 mg/kg Aviari Dietary Toxicity with Bobwhite quail: 981 ppm Ring-neck pheasant: 1468 ppm Mallard duck: 4048 ppm Avian Reproduction Studies: Bobwhite quail: 100 ppm Mallard duck: 30 ppm Acute Toxicology: Freshwater Fish: Rainbow trout: 15-38.7 ppm Bluegill sunfish: 13-156 ppm Acute Toxicity to Invertebrates (Daphnia): 1.2 to 4.0 mg/L Endangered Species: Although paraquat is not believed to cause problems with stable wildlife populations, its acute and subacute toxicity may be hazardous to unstable or endangered populations (primarily plant species). Tolerance Reassessment: Tolerances are established for residues of the plant regulator, desiccant, defoliant, and herbicide paraquat (1 ,1-dimethyl-4,4’-bipyridinium ion) derived from application of either the his(methyl- sulfate) or dichioride salt (both calculated as the cation) in or on the following raw agricultural commodities (40 CFR 180.205): ------- —7- Commodities Parts Per Million Acerola 0.05 Alfalfa 5.0 Almond hulls 0.5 Apples 0.05 Apricots 0.05 Asparagus 0.5 Avocados 0.05 Bananas 0.05 Barley, grain 0.05 Beans, forage 0.1 Beans, hay 0.4 Beans, lima (succulent) 0.05 Beans, snap (succulent) 0.05 Beets, sugar 0.5 Beets, sugar (tops) 0.5 Birdsfoot trefoil 5.0 Broccoli 0.05 Cabbage 0.05 Carrots 0.05 Cattle, fat - 0.01 Cattle, meat 0.01 Cattle, meat byproducts 0.01 Cauliflower 0.05 Cherries 0.05 Chinese Cabbage 0.05 Citrus fruit 0.05 Clover 5.0 Coffee beans 0.05 Collards 0.05 Corn, fresh, inc. sweet corn (K + CWHR) 0.05 Corn, fodder 0.05 Corn forage 0.05 Corn grain 0.05 Cottonseed 0.5 Cucurbits 0.05 Eggs 0.01 Figs 0.05 Goats, fat 0.01 Goats, meat 0.01 Goats, meat byproducts 0.01 Grass, pasture 5.0 Grass, range 5.0 Guar beans 0.5 Guava 0.05 Hogs, fat 0.01 Hogs, meat 0.01 Hogs, meat byproducts 0.01 Hops, fresh 0.1 ------- —8- Commodities Parts Per Million Hops vines 0.5 Horses, fat 0.01 Horses, meat 0.01 Horses, meat byproducts 0.01 Kiwifruit 0.05 Lettuce 0.05 Milk 0.01 Mint, hay 0.5 Nectarines 0.05 Nuts 0.05 Oat grain 0.05 Olives 0.05 Onions, dry bulb 0.05 Onions, green 0.05 Papayas 0.05 Passion fruit 0.2 Peaches 0.05 Pears 0.05 Peas, succulent 0.05 Peas, hay 0.8 Pineapples 0.05 Pistachio nuts 0.05 Plums (fresh prunes) 0.05 Potatoes 0.5 Poultry, fat 0.01 Poultry, meat 0.01 Poultry, meat byproducts 0.01 Rhubarb 0.05 Rye grain 0.05 Safflower seed 0.05 Sheep, fat 0.01 Sheep, meat 0.01 Sheep, meat byproducts 0.01 Small fruit 0.05 Sorghum forage 0.05 Sorghum grain 0.05 Soybeans 0.05 Soybean forage 0.05 Strawberries 0.25 Sugarcane 0.5 Sunflower seeds 2.0 Turnips (roots) 0.05 Turnips (tops) 0.05 Vegetables, fruiting 0.05 Wheat grain 0.05 A food additive tolerance of 0.2 ppm is established for residues of the defoliant, desiccant, and herbicide paraquat (1,1’_dimethyl-4,4’-bipyridifliUm ion) derived ------- -9 from the application of either the bis(methylsulfate) or dichioride salt (both calculated as the cation) in or on dried hops resulting from application of the pesticide to growing hops (21 CFR 193.331). Feed additive tolerances are established for residues of the defoliant, desiccant, and herbicide paraquat (1,l’dimethyl4-4’-bipyridifliUlfl ion) derived from the application of either the bis(methylsulfate) or dichioride salt (both calculated as the cation) in the following processed feeds when present therein as a result of application of paraquat to growing crops (21 CFR 561.289): Feeds Parts Per Million Mint, hay, spent 3.0 Sunflower, seed, hulls 6.0 The acceptable daily intake (ADI) based on the 1-year dog study (NOEL of 0.45 mg/kg/day) and using a safety factor of 100 is calculated to be 0.0045 mg/kg/day. The maximum permitted intake (MPI) for a 60-kg human is calculated to be 0.27 mg/day. The theoretical maximum residue contribution (TMRC) for paraquat, based on published tolerances is 0.1134 mg/day. The TMRC constitutes 42 percent of the MPI. Reported Pesticide Incidents: The Agency’s Pesticide Incident Monitoring System (PIMS) indicated that the majority of the poisoning incidents involving paraquat resulted from the purposeful ingestion of the chemical in apparent suicide attempts. 4. Summary of Regulatory Position and Rationale The Agency has classified paraquat as a Group C oncogen (Possible Human Carcinogen). However, after considering applicator exposure to paraquat, the Agency has concluded that the risks posed by paraquat are not of concern in terms of the magnitude of risk to the individual appli- cators. The Agency is continuing to require that an emetic cleared under 40 CFR 180.1001 be incorporated into all manufacturing-use products (MUP’s) and end-use products containing paraquat. The emetic is needed in the formu- lations to induce rapid vomiting thereby reducing absorp- tion of paraquat if swallowed. ------- — 10 - The Agency is requiring those agricultural products contain- ing paraquat already classified as “Restricted Use” maintain this classification. Based on submitted acute toxicity and subchronic toxicity data the “Restricted Use” classification and current precautionary statements are necessary to protect mixer-loaders and applicators from effects of derrnal toxicity. The Agency has determined that the homeowner product contain- ing 0.276 percent paraquat presently unrestricted will remain unrestricted. The Agency believes that this relatively dilute formulation, when used according to label directions, is not likely to present a significant health hazard to humans. The Agency is requiring additional residue data on several crops and processed commodities as well as some changes in the tolerance listings. The Agency is requiring certain label revisions pertaining to application and grazing restric- tions, as determined by review of available residue data. The Agency is requiring labeling to protect endangered species. This labeling is addressed in Pesticide Regis- tration (PR) Notices 87-4 and 87-5. The Agency will issue registrations for substantially similar products while data gaps are being filled. Significant new uses for paraquat will be considered on a case-by-case basis. 5. Summary of Major Data Gaps Date due (from issuance of Standard ) Environmental fate data 9-50 months Subchronic inhalation toxicity 15 months Residue chemistry data 24 months Product chemistry 6 months 6. Contact Person at EPA : Robert J. Taylor Office of Pesticide Programs, EPA Registration Division (TS-767C) 401 M Street SW. Washington, DC 20460 Phone: (703) 557-1800 Disclaimer : The information presented in this Pesticide Fact Sheet is for informational purposes only and may not be used to fulfill data requirements for pesticide registration and reregistration. ------- |