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At least 19 recordsLinked to original sources

PubMed1990

[Studies on dichlorvos (DDVP). III. Testing of dichlorvos for cocarcinogenic activity in mice].

In order to clarify whether or not Dichlorvos (DDVP)--which did not exert carcinogenic effects in mice in our experiments--is cocarcinogenic, male and female mice of the strain C57Bl/6/Bln were subcutaneously injected with the carcinogen N-Nitrosodiethylamine (NDEA) and received in addition DDVP orally. For comparison NDEA and DDVP alone was administered to other groups of mice. The combined application (NDEA + DDVP) did not result in increased incidences of tumors and preneoplastic lesions as compared with the NDEA-treated groups of mice. The incidence of focal (transitional cell) hyperplasias of the urinary bladder epithelium was increased in the groups treated with NDEA + DDVP as compared to the groups with single compound treatment. There were no development of tumors and no differences in the latency periods of tumors which could be attributed to the combined treatment with NDEA + DDVP. Under these experimental conditions DDVP was not cocarcinogenic in mice.

Administration, Oral↗

PubMed1991

Schistosoma mansoni: glutathione S-transferase-catalyzed detoxication of dichlorvos.

Dialyzed cytosol of adult Schistosoma mansoni worm pairs catalyzed the glutathione-dependent O-demethylation of dichlorvos (2,2-dichlorovinyl dimethylphosphate), the active form of the antischistosomal drug metrifonate, to form a thioether conjugate, S-methylglutathione, and desmethyl dichlorvos. The reaction rate was dependent on both time and protein concentration, and no product was formed when either dichlorvos or glutathione was omitted from the reaction mixture. Female worm cytosols were about 2.5-fold more active per milligram of protein that those of males. Partial purification of glutathione S-transferases from male worms by affinity chromatography on glutathione-agarose showed that the reaction could be catalyzed by a preparation containing the three major isoenzymes, but that the unbound fraction, which contains at least one additional form of the enzyme that is particularly active with epoxide substrates, was 16-fold more active toward dichlorvos than the bound fraction. S-Methylglutathione also was formed by S. mansoni worm pairs incubated in the presence but not in the absence of dichlorvos. Because GSH S-transferase-catalyzed metabolism of dichlorvos results in the formation of desmethyldichlorvos, which unlike the parent compound is not an effective acetylcholinesterase inhibitor, the reaction represents a pathway of detoxication in schistosomes. It is the first example of a clinically used schistosomicide shown to be detoxicated by a conjugation pathway. These results raise the possibility that dichlorvos detoxication by S. mansoni may help explain why this species is normally refractory to metrifonate.

Animals↗

PubMed1992

Hepatotoxicity of trichlorfon and dichlorvos in isolated rat hepatocytes.

Hepatotoxicity of organophosphorus insecticides, trichlorofon and dichlorvos, a dechlorinated form of the former, was examined in isolated hepatocytes from untreated control and phenobarbital-pretreated (80 mg/kg, i.p., for 3 days) rats. These compounds produced toxic effects on hepatocytes as evidenced by malondialdehyde production and lactate dehydrogenase leakage in a dose-dependent manner up to the concentration of 2 mM, dichlorvos being more toxic than trichlorfon. Hepatocytes from phenobarbital-pretreated rats were more sensitive to these organophosphates than those from control rats. Dichloroacetaldehyde and dichloroacetic acid, metabolites of dichlorvos, did not injure hepatocytes. The toxic effects of dichlorvos on hepatocytes were enhanced by increasing oxygen concentration during the incubation, or by addition of glycolytic substrates (pyruvate, lactate or fructose) to the incubation mixtures. On the other hand, addition of antioxidants (diethyldithiocarbamate or N,N'-diphenyl-p-phenylenediamine), or cytochrome P-450 inhibitors (SKF-525A or metyrapone) to the incubation mixtures attenuated malondialdehyde production caused by dichlorvos and protected cells from death. Addition of dichlorvos to the incubation mixtures of hepatic microsomes stimulated lipid peroxidation in the presence of NADPH, which was inhibited by further addition of superoxide dismutase but not catalase. These results suggest that hepatotoxicity of trichlorfon and dichlorvos are related to their peroxidative property in microsomes which is accelerated by oxygen.

Animals↗

PubMed1992

The influence of single topical application of dichlorvos on blood esterases and toxicity in male calves.

The effect of dichlorvos on inducing changes in blood esterase activities and systemic toxicity was investigated following single topical applications of 1, 3 or 6% dichlorvos concentrations to male calves. Dichlorvos at 1% concentration did not produce any signs of toxicity, whereas 3 and 6% concentrations induced mild to severe toxicity characteristic of anticholinesterase poisoning. Dichlorvos at all concentrations significantly inhibited erythrocyte cholinesterase (25-75%), plasma cholinesterase (30-85%), and serum carboxylesterase (15-51%) activities in male calves. The dose-dependent inhibition was maximum 12 h after insecticide exposure. The extent of inactivation of blood esterases was not correlated with the severity of toxicity. Inhibition of blood cholinesterases by the 6% dichlorvos was still present 21 d after the dichlorvos exposure.

Administration, Cutaneous↗

PubMed1979

The chemical and biochemical reactivity of dichlorvos.

The chemical structure, reactivity and metabolic fate of the insecticide dichlorvos (2,2-dichlorovinyl dimethyl phosphate) are discussed in relation to the possible genotoxicity of this and other methyl phosphate triesters. Recent attempts to demonstrate the methylation of DNA following exposure of bacteria and animals to dichlorvos are reviewed. On the basis of comparative data relating mutagenesis to methylation reactions, it seems entirely appropriate to conclude that the mutagenicity of dichlorvos to bacteria is due solely to methylation of the bacterial DNA under the conditions of these tests. However, the methylation of mammalian DNA could not be demonstrated under realistic exposure conditions (when the alkylating mutagen methyl methanesulphonate afforded clearly measurable methylation). The failure to detect methylation by dichlorvos in vivo is attributed to the operation of highly efficient enzyme-catalysed biotransformations which rely largely on the phosphorylating reactivity of dichlorvos. The biotransformation pathways, characterised mostly in the rat, appear to be common also to pig, mouse, hamster, and man.

Animals↗

PubMed1991

The therapeutic effects of 2,3-butanedione monoxime and atropine in severe dichlorvos intoxication in buffalo calves.

2,3-Butanedione monoxime and atropine alone or in combination were evaluated for their ability to alleviate the toxicity and to reverse the biochemical changes induced by dichlorvos in the blood of buffalo calves. Treatment with 2,3-butanedione monoxime plus atropine 30 min after oral administration of dichlorvos (160 mg/kg) eliminated the apparent toxic signs within 10-15 min, completely prevented lethality, and reversed the dichlorvos-induced alterations in the concentrations of serum carboxylesterase, total plasma proteins, blood glucose and plasma cholinesterase within 2, 4, 12 and 168 h, respectively. Treatment with either 2,3-butanedione monoxime or atropine alone was less effective but the former was the more potent of the two in counteracting the biochemical effects of dichlorvos. These antidotal studies suggest that 2,3-butanedione monoxime in conjunction with atropine would provide effective therapy against severe dichlorvos intoxication in buffalo.

Animals↗

PubMed1978

Mutagenicity of dichlorvos and other structurally related pesticides in Salmonella and Streptomyces.

The following pesticides: azinphosmethyl, diallate, dichlorvos, EPTC, fenchlorphos, mevinphos, monocrotophos, noruron, parathionmethyl, triallate, trichlorphon and vegadex were tested for the ability to induce his+ revertants in four histidines requiring strains of Salmonella typhimurium--TAI 535(missense), TAI 536, TAI 537 and TAI 538 (frame-shift)- and resistance to low levels of streptomycin in Streptomyces coelicolor. Dichlorvos, which is a phosphoric ester with a dichlorovinyl group as side chain, and trichlorphon, which is known for its spontaneous conversion in dichlorvos, are both mutagenic in Salmonella (strain TAI535) and Streptomyces. Five organophosphorus pesticides similar to dichlorvos but devoid of the vinyl group are not mutagenic. Three carbamates, diallate, triallate and vegadex, which contain a chloroallyl group similar to the vinyl group of dichlorvos are mutagenic in Streptomyes; triallate and vegadex are powerful mutagens also in Salmonella (strain TAI535); two other carbamates devoid of the chlorinated group are not mutagenic. The results suggest that the presence of a vinyl chloride or allyl chloride group in the molecule of these pesticides is responsible for the ability to induce point mutations in Salmonella and Streptomyces.

Animals↗

PubMed1992

Neurotoxicity of dichlorvos: effect on antioxidant defense system in the rat central nervous system.

The effect of dichlorvos exposure (5 mg kg-1 body wt, ip) on lipid peroxidation and antioxidant defense system in different regions of the rat central nervous system was studied. In the present paper an inhibition of acetylcholinesterase activity was used as an index of dichlorvos neurotoxicity. We observed significant increases in the activities of the antioxidant enzymes superoxide dismutase (SOD) and catalase which were accompanied by a decrease in the values of lipid peroxidation. Dichlorvos exposure also resulted in a significant decrease in glutathione peroxidase activity. The decreased levels of both reduced and oxidized glutathione as observed on dichlorvos exposure affected the GSH/GSSG ratio. These results indicate that the enzymes SOD and catalase may enhance the disposal of potentially toxic radicals. Furthermore, the decrease in GSH levels may be a mechanism for the detoxification of dichlorvos in the brain.

Acetylcholinesterase↗

PubMedDate not supplied

Effects of repeated topical application of dichlorvos on blood enzymes and its toxicity in buffalo calves (Bubalus bubalis).

Dichlorvos was applied as spray at 1 and 2% concentrations daily for a period of 28 and 21 consecutive days, respectively to buffalo calves. Animals sprayed with 1% dichlorvos displayed mild to moderate clinical signs of toxicosis during the 4th week of exposure. The higher concentration (2%) produced clinical signs of poisoning after 12-16 applications, and was lethal to one of three animals. Daily spraying of dichlorvos at both concentrations inactivated erythrocyte cholinesterase (ChE) (15-21%), plasma ChE (17-20%) and serum carboxylesterase (5-10%) within 3 days. The extent of inhibition of esterases was increased with repeated treatment and maximal inhibition of erythrocyte ChE (80-89%), plasma ChE (81-91%) and serum carboxylesterase (33-54%) with 1 and 2% concentrations was observed on the 28th and 21st day after start of application, respectively. In surviving animals, blood esterases remained inactivated to the extent of 14-65% on the 14th day after the termination of treatment. Dichlorvos at both concentrations significantly (P less than 0.01) elevated the serum levels of aspartate aminotransferase, alanine aminotransferase, acid phosphatase and alkaline phosphatase. The activities of these enzymes in surviving animals recovered to control values within 14 days after the final application of dichlorvos.

Administration, Topical↗

PubMed1991

Micronuclei induction by dichlorvos in the mouse skin.

Micronucleus (MN) induction in cultured keratinocytes was investigated following skin painting of HRA/Skh mice with the pesticide, dichlorvos. Whole skin and partially-purified epidermal cells from 5-6 week old male animals were cultured for 4 days in vitro after single topical applications of various concentrations of dichlorvos in vivo. Appropriate doses, allowing optimum survival of keratinocytes, were selected following an initial range-finding experiment. To evaluate MN induction in dividing cells, the cytokinesis-block method was employed. Results showed statistically significant MN at all dose levels in partially-purified epidermal cells and a positive trend with respect to dose from 51 to 1033 nmol dichlorvos. A significant increase in MN was also detectable in cultured cells from whole skin, dissociated within as little as 1 h after application of dichlorvos. Although a number of technical difficulties are associated with the skin micronucleus method, it has been used successfully in this laboratory to detect several skin carcinogens of both high and low potency. Since dichlorvos is rapidly absorbed through the skin, and can induce MN in skin cells of treated mice, this compound may therefore be considered to pose a contact hazard for exposed humans.

Administration, Topical↗

PubMed1991

Carcinogenesis studies of dichlorvos in Fischer rats and B6C3F1 mice.

Dichlorvos (dichlorovinyl dimethyl phosphoric acid ester) is a cholinesterase inhibitor used widely as a contact and stomach insecticide for control of internal and external parasites. Carcinogenesis studies were conducted by administering dichlorvos in corn oil by gavage 5 times a week for 103 weeks to groups of 50 male and 50 female Fischer rats at 0, 4, or 8 mg/kg body weight, to groups of 50 male B6C3F1 mice at 0, 10, or 20 mg/kg, and to groups of 50 female B6C3F1 mice at 0, 20, or 40 mg/kg. During the course of the studies, body weights and survival rates of the male and female rats and mice were not different from those of their respective controls; females of both species appeared to gain more weight than controls. Neoplasms induced by dichlorvos included adenomas of the exocrine pancreas (male rats), mononuclear cell leukemia (male rats), and squamous cell papilloma of the forestomach (male and female mice; two other female mice had squamous cell carcinomas). Lesions observed in female rats that may have been due to dichlorvos administration included adenomas of the exocrine pancreas and fibroadenomas of the mammary gland. The results demonstrated that dichlorvos is carcinogenic for Fischer rats and B6C3F1 mice.

Adenoma↗

PubMed1978

Activities of dichlorvos or disophenol against the hookworm (Uncinaria lucasi) and sucking lice of northern fur seal pups (Callorhinus ursinus) on St. Paul Island, Alaska.

One controlled and six critical tests were conducted in July, 1977 with northern fur seal pups (Callorhinus ursinus) to determine the efficacies of a single dose of dichlorvos capsules at 29.3 to 32.8 mg/kg, tablets at 10.5 to 11.5 mg/kg, or disophenol at 9.9 mg/kg given subcutaneously against natural infections of adult Uncinaria lucasi. In the controlled test, 20 pups were treated and 10 pups were nontreated. Removal of hookworms in this test was 99% for five pups receiving dichlorvos capsules, 99% for five pups receiving dichlorvos tablets, and 77% for 10 pups receiving disophenol. Also, both formulations of dichlorvos and the formulation of disophenol were highly active against natural infestations of two species of sucking lice (Proechinophthirus fluctus and Antarctopthirus callorhini). In critical tests with four pups treated with dichlorvos capsules at 28.6 to 30.6 mg/kg, removal of hookworms was uniformly 100%. Disophenol at 9.9 mg/kg removed 100% and less than 1% of hookworms in two pups, respectively, in critical tests.

Alaska↗

PubMed1991

Pharmacokinetics of metrifonate and its rearrangement product dichlorvos in whole blood.

Six male healthy volunteers were given single oral doses of 7.5 mg/kg of metrifonate and concentrations of metrifonate and dichlorvos were determined in whole blood using a standardized sampling procedure. Blood was collected in test tubes containing equal volumes of 0.74 M phosphoric acid for the determinations of metrifonate and dichlorvos with gas chromatography and mass spectrometry at different time points for up to 24 hr. Cholinesterases were also determined in blood haemolyzed with water. Metrifonate was quickly absorbed with a Cmax of 50.5 +/- 18.9 mumol/l which was obtained between 0.17 to 1 hr after drug intake. Mean whole blood t1/2, Clo and AUC were 2.07 +/- 0.24 hr, 0.34 +/- 0.06 l/hr/kg and 89.2 +/- 16 mumol.hr/l respectively. The concentrations of dichlorvos closely followed those of metrifonate with a constant ratio of 0.01 to 0.02. The concentrations of metrifonate were detectable for up to 8 hr but those of dichlorvos had fallen below the level of determination by this time. Both plasma and red blood cell cholinesterases were readily inhibited and were still low after 24 hr. None of the volunteers complained of side effects.

Adult↗

PubMed1992

The influence of 2,3-butanedione monoxime on dichlorvos-induced enzymatic changes in buffalo calves.

The effects of administration of 2,3-butanedione monoxime (2,3-BM) or atropine alone and in combination were determined on the blood enzymatic activities of dichlorvos-exposed buffalo calves. Dichlorvos given po at 160 mg/kg body weight produced pronounced inhibition of erythrocyte acetylcholinesterase (AChE) and elevation in serum aminotransferases and phosphatases within 30 min. 2,3-BM administered alone or in conjunction with atropine to dichlorvos-exposed calves significantly reactivated erythrocyte AChE activity whereas atropine was ineffective. The effect of 2,3-BM plus atropine on other enzymatic activities was comparatively greater than that of either drug alone. The results indicated that combined treatment with 2,3-BM and atropine was most effective in reversing dichlorvos-induced enzymatic alterations.

Animals↗

PubMed1991

Utilization of dichlorvos and trichlorfon in salmonid farming in Norway during 1981-1988.

The main objectives of this investigation were to quantify the use of dichlorvos and trichlorfon in the treatment of salmon lice infestations, to evaluate the prescribing of these drugs, and to estimate possible changes in the salmon lice problem by use of drug statistics. This study has shown that the use of trichlorfon increased from 4.9 tons in 1981 to 28.3 tons in 1985. This figure declined to 3.2 tons in 1988. The use of dichlorvos increased from 0.3 tons in 1986 to 3.2 tons in 1988. The change in the prescribing from trichlorfon to dichlorvos has dramatically reduced the pollution caused by these substances in the marine environment. Moreover, if necessary safety rules are observed, this change reduces the exposure of the workers on fish farms to these drugs, and also reduces the possibilities of intoxications of the fish during the treatment procedure. The sales figures of dichlorvos and trichlorfon, related to the calculated biomass of farmed salmonids in the sea, indicate a dramatic increase in the salmon lice problem.

Agriculture↗

PubMed1990

Effects of dichlorvos treatment on mouse reproduction.

To test whether exposure to dichlorvos vapors for treatment of mouse ectoparasites resulted in temporary cessation of breeding, we exposed harem breeding groups of mice to varying concentrations of dichlorvos vapors and examined the effects of exposure on litter frequency and litter size. All exposure levels resulted in decreased plasma cholinesterase concentrations in treated mice for up to 10 days following the completion of exposure. Litter frequency and size were unaffected by dichlorvos exposure, and gestation times were not prolonged. Therefore, treatment with dichlorvos vapors during breeding did not affect reproduction in exposed mice.

Administration, Inhalation↗

PubMed1979

Teratogenic potential of dichlorvos given by inhalation and gavage to mice and rabbits.

Dichlorvos (2,2-dichlorovinyl dimethyl phosphate) is an important organophosphate insecticide and anthelmintic with widespread use. The purpose of this study was to evaluate the teratogenic potential of dichlorvos given orally at the maximum tolerated dose to mice (60 mg/kg/day) and rabbits (5 mg/kg/day) and by inhalation in both species at a concentration of 4 microgram/l seven hours daily. Dichlorvos was not found to be teratogenic in either species by either route of administration.

Administration, Oral↗

PubMed1976

Dichlorvos -- a 2-year inhalation carcinogenesis study in rats.

To determine the effects of dichlorvos vapour on the tumour incidence in rats, 5 week old Carworth Farm E strain rats weighing between 94 and 150 g were exposed to 0, 0.05, 0.5 and 5.0 mg/m3 in a 2-year inhalation study. The growth rate of all treated rats was depressed, particularly in the males. There was increased survival of the rats exposed to 5 mg/m3. There were no consistent differences in food intakes, organ weights, haematological or blood chemistry estimations, except in cholinesterase activites, amongst the various groups of rats. No compound-related differences were seen in acetylcholine and choline estimations carried out on a small number of female rats' brain tissues after two years' exposure. There were no gross or microscopical compound-related changes in the rats' tissues. Ultrastructural examination of the respiratory tissues of the rats from the control and 5 mg/m3 group showed no changes attributable to dichlorvos. The results of a relative risk analysis of the tumour data showed that no dose-related increase in tumour risk was established for rats of either sex. These data confirm the results of earlier st.udies supporting the safety of insecticidal uses of dichlorvos.

Animals↗