Amitraz appears as white monoclinic crystals. Melting point 187-189°F (86-87°C). Insoluble in water. Used as an acaricide, insecticide and treatment of demodectic mange in dogs.
Analysis of urine obtained from volunteers dosed with (14)C-amitraz indicated that the metabolism of amitraz was qualitatively similar to that in the other species. The major metabolites were 4-formamido- meta-toluic acid, 4-acetamido- meta-toluic acid and N-methyl- N'-(2,4-xylyl)formamidine. In addition, 40-60% of the metabolites excreted in urine were accounted for by a polar fraction containing conjugates of 4-formamido- meta-toluic acid and 4-acetamido- meta-toluic acid. The minor metabolites included 4-amino- meta-toluic acid and form-2',4'-xylidide. Excretion of N-methyl- N'-(2,4-xylyl)formamidine was dose-dependent. The metabolites identified in the volunteers were 4-formamido- meta-toluic acid plus 4-acetamido- meta-toluic acid (27% of the total radiolabel in urine), N-methyl- N'-(2,4-xylyl)formamidine (6%), 4-amino- meta-toluic acid (4%), form-2',4'-xylidide (4 %), the product of acid hydrolysis of N-methyl- N'-(2,4-xylyl)formamidine and form-2',4'-xylidide (1%), and polar material (57%).
When (14)C-amitraz was applied to Boophilus microplus, penetration occurred readily. Cleavage to 2,4-dimethylformanilide and N-2,4-dimethylphenyl N'-methylformamidine and large amounts of polar material occurred. 2,4-dimethylaniline adn CO2 were also produced.
... Pear samples were extracted with ethyl acetate and anhydrous sodium sulphate. Amitraz was found to be rapidly decomposed into four related compounds, of which N-(2,4-dimethylphenyl)formamidine (DMPF) was the most abundant and persistent. N,N'-bisdimethylphenylformamidine (BDMPF), 2,4-dimethylformamidine (DMF) and 2,4-dimethyl aniline (DMA) were also main metabolites of amitraz.
In separate studies, groups of two male and two female beagle dogs were dosed orally (4 mg/kg bw by capsule) or dermally (20-21 mg on an area of 400-500 cm sq) with (14)C-amitraz (specific activity, 8.6 mCi/g). ... /The/ metabolism of amitraz was essentially the same after oral and dermal administration. 4-Formamido- meta-toluic acid was the predominant residue in both blood and urine. The parent compound and the first hydrolysis products, N-methyl- N'-(2,4-xylyl)formamidine and form-2',4'-xylidide, were not observed at measurable concentrations in either blood or urine.
The hydrolyzed metabolic products of amitraz include 2,4-dimethylaniline, and N-(2,4-dimethylphenyl)-N'-methylformamidine. These metabolites are further metabolized to 2,4-dimethylaniline and ultimately to 4-amino-3-methylbenzoic acid, the principal amitraz metabolite found in the urine and liver.
The pharmacological activity of amitraz includes different mechanisms of action leading to toxic effects in humans as well as in animals. Many of these effects and most of the effects on humans are caused by its alpha-adrenergic agonist activity. Furthermore amitraz inhibits prostaglandin synthesis, interacts with the octopamine receptors of the central nervous system and inhibits monoamine oxidases. Animal studies revealed that damages due to amitraz poisoning can be recovered even after exposure to a potentially lethal dose. This could mean that amitraz' effects are reversible or at least are recoverable. When an amitraz poisoning is lethal, death results from respiratory depression. (Wikipedia)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌性证据
癌症分类：C组可能的人类致癌物
Cancer Classification: Group C Possible Human Carcinogen
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
对人类不具有致癌性（未被国际癌症研究机构IARC列名）。
No indication of carcinogenicity to humans (not listed by IARC).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
该物质可以通过吸入和摄入被身体吸收。
The substance can be absorbed into the body by inhalation and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
The toxic effects to humans following on amitraz-uptake include loss of consciousness, vomiting, respiratory failure, miosis, hypothermia, bradycardia, hyperglycemia and central nervous system depression. (Wikipedia)
In all species examined, urine was the major route of excretion, accounting for 65-84% of the dose (55-76% within the first 24 hr). ... In both rats and mice, increasing the dose of amitraz from 1 to 100 mg/kg bw increased the excretion of N-methyl- N'-(2,4-xylyl)formamidine from approximately 5 to 30% of the total excretion.
In separate studies, groups of two male and two female beagle dogs were dosed orally (4 mg/kg bw by capsule) or dermally (20-21 mg on an area of 400-500 cm sq) with (14)C-amitraz (specific activity, 8.6 mCi/g). Peak blood concentrations of radiolabel were observed during the first 8 hr after oral administration. About 80% of the oral dose was excreted within the first 24 hr and 100% within 72 hr, preferentially in the urine. After dermal treatment, peak blood concentrations occurred within 24-72 hr, and only 25-40% was recovered in urine and feces over a 10-day collection period, demonstrating the poor dermal absorption of amitraz.
