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PubMed2006

Analytical study of trichlorfon residues in Kaki fruit and cauliflower samples by liquid chromatography-electrospray tandem mass spectrometry.

A detailed analytical study on trichlorfon residues in selected vegetables samples has been carried out, focused on the reliable quantification and confirmation of this compound, and on stability of residues under storage. As a consequence, a rapid and sensitive LC-ESI-MS/MS method has been developed for the determination of residues of this insecticide in kaki fruit (flesh and peel) and cauliflower samples. Extraction was performed with acetonitrile using a high-speed blender. After 4-fold dilution of the extract with water, 20 microL was directly injected in the LC-ESI-MS/MS system (triple quadrupole), using matrix-matched standards calibration for quantification. Under optimized MS/MS conditions, limit of detections between 0.006 and 0.013 mg/kg were reached, and a limit of quantification of 0.05 mg/kg was established, with a runtime of only 15 min. Recoveries from spiked blank samples at 0.05 and 0.5 mg/kg were in the range 83-101% with relative standard deviations lower than 10%. The method was applied to treated and untreated samples collected from field residues trials, using quality control samples analysis for the evaluation of the method. Despite the acquisition of two MS/MS transitions in selected reaction monitoring mode, the analysis of treated samples revealed the presence of a chromatographic peak close to the analyte that corresponded to a trichlorfon isobaric compound that shared the same MS/MS transitions. This unusual situation in LC-MS/MS-based procedures required the application of an efficient chromatographic separation to avoid this interference. All experiments have been made in compliance with the principles of Good Laboratory Practices (GLP) and following the European SANCO guidelines for pesticides residue analysis (PRA).

Brassica↗
PubMed1984

Intermittent chemotherapy with trichlorfon (metrifonate) reverses proteinuria, hematuria, and leukocyturia in urinary schistosomiasis: results of a three-year field study.

Trichlorfon (metrifonate) was given intermittently to 37 schoolboys with urinary schistosomiasis living in a hyperendemic area of the Sudan. Patients were followed up for three years. Initially, 10 mg of trichlorfon/kg of body weight was administered; this dosage was repeated 14 days and 16 months later. Patients still excreting eggs after 24 months received a fourth dose. At month 24, 61% and at month 36, 56% of the patients had no detectable egg excretion; the others showed severe reduction of egg output. The number of ova excreted was always paralleled by a combined scale of hematuria, leukocyturia , and proteinuria, as assessed by urine analysis reagent strips. Quantitative urine analysis at month 36 revealed pathological findings in only eight individuals. Thus, trichlorfon given three or four times in a dose of 10 mg/kg of body weight spaced over a period of two years was highly effective in reducing parasite load and disease in children living under hyperendemic conditions.

Child↗
PubMed1989

The effect of the organophosphate trichlorfon on the neuromuscular blocking activity of atracurium in halothane-anesthetized horses.

To determine whether cholinesterase inhibition by an organophosphate would influence atracurium's neuromuscular blockade, six horses were anesthetized and paralyzed with atracurium (total of five injections per horse) on experimental Day 1, then were given trichlorfon (64 mg/kg per os) 6 days later. On Day 7, horses were anesthetized and paralyzed in the same manner as on experimental Day 1. Blood was taken to measure serum cholinesterase activity prior to anesthesia on Days 1 and 7. No significant difference was noted in atracurium's neuromuscular blocking activity between the 2 experimental days (P less than 0.05), despite Day 7 cholinesterase activity that was 16% of pre-trichlorfon values. For atracurium Injections 1 and 2-5, 85 and 43 micrograms/kg of atracurium, respectively, were required to produce a 95-99% reduction in hoof twitch. The time from injection to maximum twitch reduction was approximately 9 min after Injection 1 and 5 min after subsequent injections. Time from injection to maximum twitch reduction was significantly longer for Injection 1 than Injections 2-5 on both experimental days. The time from maximum twitch reduction until 10% recovery was approximately 8 min, with no significant difference between experimental days. The time for twitch recovery from 10 to 75% was approximately 17 min for all injections. Antagonism of atracurium with edrophonium caused the twitch height to return to pre-atracurium strength in approximately 7 min. Edrophonium caused a significant increase in arterial blood pressure. Heart rate change was variable after edrophonium.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1981

Changes in carbohydrate metabolism in various organs of the snail, Lymnaea acuminata following exposure to trichlorfon.

Several aspects of carbohydrate metabolism following 24 hr and 48 hr treatment with 10 and 20 mg/l of trichlorfon, were studied in hepatopancreas, mantle, intestine and foot of the snail. Lymnaea acuminata. Following treatment with the pesticide, the rate of oxygen consumption and concentration of glycogen were reduced, while the levels of lactic acid and reducing sugars were enhanced. Withdrawal of pesticide for 7 days following trichlorfon treatment (10 mg/l for 48 hrs) could not reverse these changes.

Animals↗
PubMed1977

Trichlorfon toxicity in pigs.

A field outbreak of suspected poisoning is recorded from feed medicated with the organophosphorus insecticide trichlorfon. A controlled experiment showed that toxicity could occur when trichlorfon was fed from 3-5 days at levels greater than that recommended. Signs recorded were inappetence, muscle tremor, ataxia and deaths. Attention is drawn to conditions which could result in overdosage and toxicity when used on the farm.

Animals↗
PubMed1976

Influence of trichlorfon and fractionated irradiation on hydroproteolytic activity of pancreas and intestinal tissues of rats.

Investigations into the hydroproteolytic activity of pancreas and intestinal tissues (small intestine and colon) of rats after fractionated irradiation (5 X 150 R) were carried out. There was found marked postirradiation enhancement of lipase activity in pancreas and duodenal part of intestine and increase of B-glucuronidase and acid phosphatase activity in nearly all parts of the examined intestinal tissues. Fractionated irradiation resulted in an increase of pancreatic catheptic (proteolytic) activity causing simultaneous decrease of proteolytic activity in intestine and colon. Preventive administration of Trichlorfon (ten days before irradiation) in the dose of 10 mg or 30 mg/kg evoked modification of hydroproteolytic activity in intestinal tissues of healthy and irradiated rats. Trichlorfon applied in the dose of 30 mg/kg exerted antilipolytic and anticatheptic effects in pancreas and intestinal tissues of irradiated rats.

Acid Phosphatase↗
PubMedDate not supplied

Analysis of pharmaceutical dosage forms for oxfendazole: II. Simultaneous liquid chromatographic determination of oxfendazole and trichlorfon in equine paste.

A reverse phase liquid chromatographic procedure is described for the simultaneous determination of oxfendazole [2-(methoxycarbonylamino)-5-phenylsulfinylbenzimidazole] and trichlorfon [(2,2,2-trichloro-1-hydroxyethyl)phosphonic acid dimethyl ester] in equine paste. The sample is extracted by sonication in methanol. Insoluble excipients are removed by centrifugation and an aliquot plus internal standard are diluted with dilution solvent (water-acetonitrile-phosphoric acid, 80 + 20 + 1). The samples are filtered and injected onto a Partisil-5 ODS-3 column with acetonitrile-0.01 M phosphate buffer pH 6.0 (20 + 80) as mobile phase. Method specificity is confirmed using an absorbance rationing technique. The method yields mean recoveries of 100.9 and 100.0% for trichlorfon and oxfendazole, respectively. Dependence of chromatographic performance characteristics on mobile phase organic content, pH, and buffer concentration is also reported.

Animals↗
PubMed1975

Repeated oral administration of coumaphos in sheep: interactions of coumaphos with bishydroxycoumarin, trichlorfon, and phenobarbital sodium.

Interactions between treatments with coumaphos, bishydroxycoumarin (an anticoagulane), trichlorfon (an organophosphorous compound), and phenobarbital sodium (an inducer of microsomal enzymes) were investigated in sheep. A daily dose of 2 mg of coumaphos/kg of body weight for 6 days did not affect the plasma enzymes or the antiprothrombinemic effect of bishydroxy-coumarin in wethers. The treatment of ewes with an intravenous (IV) injection of trichlorfon, insufficient to produce significant inhibition of erythrocyte acetylcholinesterase (AChE) activity, appeared to produce additive effects with those produced by subsequent treatment with 4 mg of coumaphos/kg/day. In ewes given 40 mg of phenobarbital sodium/kg for 5 days intraperitoneally (IP), the anticholinesterase effect of 4 mg of coumaphos/kg was significantly reduced and signs of toxicity were not present. Treatment with daily doses of 2 mg of coumaphos/kg for 6 days did not modify the anticholinesterase effect of a 2nd series of treatments given 6 weeks later.

Acetylcholinesterase↗
PubMed1984

Critical test evaluations of oxfendazole and trichlorfon: effectiveness of a paste formulation in the horse.

Critical tests were performed on 6 horses to evaluate the antiparasitic effectiveness of oxfendazole given in combination with trichlorfon in a paste formulation. Treatments were given orally as a single dose. The rates of active ingredient administration were 2.5 and 40 mg/kg of body weight for oxfendazole and trichlorfon, respectively. The combined activities of the 2 antiparasitic compounds proved 100% efficacious in the removal of adult Strongylus vulgaris, S edentatus, Oxyuris equi, and Parascaris equorum. Fourth stage O equi, and 2nd and 3rd instars of Gasterophilus nasalis also were completely removed. Second and 3rd stage instars of G intestinalis were removed at the rates of 98.1% and 98.8%, respectively. Nematodes of the "small strongyle" category were removed at the combined rate of 97.0%. Pronounced larvicidal effects of the test formulation were demonstrated via culturing fecal nematode eggs during the trial. Untoward effects of treatment were not seen in any of the trial animals.

Animals↗
PubMed1981

Clinical toxicosis and erythrocyte cholinesterase inhibition of trichlorfon combined with mebendazole in horses.

Thirty adult horses were used to compare the toxicity and cholinesterase (ChE) inhibition of various dosages of a combination anthelmintic, trichlorfon + mebendazole. Single oral doses of up to 5 times the effective dosage (39.7 mg of trichlorfon and 8.8 mg of mebendazole/kg of body weight) did not result in deaths. Horses given a placebo and horses treated at the recommended dosage rate showed few or no side effects, whereas horses given higher dosages showed dosage-related increases in the severity of clinical signs of organophosphate toxicosis. Dosage-related inhibition of erythrocyte ChE activity was also detected. A 2nd treatment of some of the horses at the recommended dosage 35 days after the initial treatment resulted in minimal or no side effects, despite the fact that erythrocyte ChE activity was still depressed before the repeat treatment. Changes indicating organ toxicosis were not detected in any of the clinical pathologic determinations in any of the dosage groups.

Administration, Oral↗
PubMed1986

Distribution and placental transfer of trichlorfon in guinea pigs.

Radiolabelled trichlorfon, dimethyl-(2,2,2-trichloro-1-hydroxyethyl)phosphonate, was administered by stomach tube to pregnant guinea pigs on days 37 and 52 of gestation and examined by the whole body autoradiography method. The results showed that the radiolabelled compound was rapidly distributed to the main organs of the dam with the highest concentrations in the liver, the kidney and the lung. No substantial concentration of radioactivity occurred in the fetuses until 30 min after administration. The uptake in the fetuses was more pronounced at the later gestational stage when the concentration in the fetal liver equalled that of the placenta.

Animals↗
PubMed1986

Prenatal effects of trichlorfon on the guinea pig brain.

The organophosphorus compound trichlorfon, dimethyl (2,2,2-trichloro-1-hydroxyethyl) phosphonate, was administered by stomach tube (100 mg/kg) to pregnant guinea pigs at two different stages of gestation (days 36, 37, 38 and 51, 52, 53). The pups developed locomotory disturbances, and post mortem examination revealed significantly decreased weights of the total brain and the cerebellum, as compared to controls. There was also a significant weight reduction particularly of the medulla oblongata, but also of the hippocampus, the thalamus, and the colliculi. Histological examination of the cerebellum revealed reduction of the external granular layer and the molecular layer, and regional absence of Purkinje cells. The activities of the neurotransmitter enzymes choline acetyltransferase (ChAT), and glutamate decarboxylase (GAD) in cerebellum were reduced as compared to the control values.

Animals↗
PubMed1993

Environmental trichlorfon and cluster of congenital abnormalities.

Of 15 live births in one Hungarian village in 1989-90, 11 (73%) were affected by congenital abnormalities and 6 were twins. Of the 11, 4 had Down syndrome. Likely causes of such clusters (known teratogenic factors, familial inheritance, consanguinity) were excluded. A case-control study and environmental investigations pointed the finger of suspicion at the excessive use of trichlorfon at local fish farms. The content of this chemical was very high in fish (100 mg/kg) and several pregnant women, including all mothers of babies with Down syndrome, had consumed contaminated fish in the critical period for the congenital abnormalities observed.

Abnormalities, Drug-Induced↗
PubMed1991

Effects of organophosphorus insecticides: effects of trichlorfon and dichlorvos on the immune response of carp (Cyprinus carpio). III. In vitro effects on lymphocyte proliferation and phagocytosis and in vivo effects on humoral response.

Cells isolated from the pronephros of carp were incubated in vitro with the organophosphorus insecticide trichlorfon or dichlorvos, each of which is used in aquaculture to eliminate fish ectoparasites. Dose-dependent suppressive effects were observed in assays for lymphocyte proliferation and myeloid cell respiratory burst activities. Dichlorvos given by bath in vivo did not affect antibody production against Yersinia ruckeri even if the spleen and kidney were obviously contaminated according to acetylcholinesterase activity analysis. Some blood parameters of nonspecific immunity (ceruloplasmin, lysozyme, hemagglutinins) were slightly affected.

Animals↗
PubMed2004

Trichlorfon predisposes to aneuploidy and interferes with spindle formation in in vitro maturing mouse oocytes.

The pesticide trichlorfon (TCF) has been implicated in human trisomy 21, and in errors in chromosome segregation at male meiosis II in the mouse. We previously provided evidence that TCF interferes with spindle integrity and cell-cycle control during murine oogenesis. To assess the aneugenic activity of TCF in oogenesis, we presently analysed maturation, spindle assembly, and chromosome constitution in mouse oocytes maturing in vitro in the presence of 50 or 100 microg/ml TCF for 16 h or in pulse-chase experiments. TCF stimulated maturation to meiosis II at 50 microg/ml, but arrested meiosis in some oocytes at 100 microg/ml. TCF at 100 microg/ml was aneugenic causing non-disjunction of homologous chromosomes at meiosis I, a significant increase of the hyperploidy rate at metaphase II, and a significant rise in the numbers of oocytes that contained a 'diploid' set of metaphase II chromosomes (dyads). TCF elevated the rate of precocious chromatid segregation (predivision) at 50 and 100 microg/ml. Pulse-chase experiments with 100 microg/ml TCF present during the first 7 h or the last 9 h of maturation in vitro did not affect meiotic progression and induced intermediate levels of hyperploidy at metaphase II. Exposure to > or =50 microg/ml TCF throughout maturation in vitro induced severe spindle aberrations at metaphase II, and over one-third of the oocytes failed to align all chromosomes at the spindle equator (congression failure). These observations suggest that exposure to high concentrations of TCF induces non-disjunction at meiosis I of oogenesis, while lower doses may preferentially cause errors in chromosome segregation at meiosis II due to disturbances in spindle function, and chromosome congression as well as precocious separation of chromatids prior to anaphase II. The data support evidence from other studies that TCF has to be regarded as a germ cell aneugen.

Aneuploidy↗
PubMedDate not supplied

Teratogenic effects of trichlorfon (Metrifonate) on the guinea-pig brain. Determination of the effective dose and the sensitive period.

The conditions (sensitive period and doses) for producing hypoplasia in guinea-pig offspring after treatment of pregnant guinea-pigs with the organophosphorous agent trichlorfon (metrifonate, 0,0-dimethyl 2,2,2-trichloro-1-hydroxyethylphosphonate) were examined. The results showed that the minimal dose required was 100 mg/kg on three consecutive days. For the cerebellum the most sensitive period was 42-44 day of gestation, for cortex the most vulnerable period was gestational days 48-50. The doses could be given either per os or subcutaneously. Almost all regions of the brain were reduced in weight. Cerebellum was the most vulnerable region, but also the medulla and hypothalamus were greatly reduced in weight. The mechanism behind the teratogenic effect is not known, but alkylation of DNA or an effect on its repair mechanism are possible effects.

Animals↗
PubMed1986

Assessment of teratogenic potential of trichlorfon in mice and rats.

Trichlorfon was evaluated for its teratogenic potential in the CD-1 mouse at doses of 200, 300 or 400 mg/kg/day administered by gavage on days 7-16 of gestation. In the CD-1 mouse, TCF was teratogenic, fetotoxic and lethal at the two highest dose levels which were also maternally lethal. At the lowest dose level which was not maternally lethal, there was a significant decrease in the number of calcified centers in the forepaws and hindpaws indicating fetotoxicity and a delay in maturation. TCF was administered at doses of 50, 100 or 200 mg/kg/day to CD rats by gavage on gestational days 7-19 (study I) or 8-20 (study II). In the CD rat in body study I and II, the highest dose level was maternally lethal. In study I, TCF was teratogenic with a shift in rib profile. In study II, TCF was teratogenic with an increased incidence in malformations of the urinary system. Additionally, TCF was fetotoxic with reduced ossification of the skulls at the lowest and highest dose levels.

Animals↗
PubMed1990

[Polyneuropathy caused by trichlorfon: report of a case with electrophysiologic and histopathologic study of the sural nerve].

The authors observed a patient who worked in a farm and suffered an organophosphate intoxication (trichlorfon). The immediate effect was manifested by vomiting and abdominal cramps. Three months later he presented a distal symmetric sensorimotor (predominantly motor) neuropathy with distal muscle atrophy. Electromyography has revealed denervation changes in every muscle studied and the sensory and motor nerve conduction was slowed in arms and legs. The sural nerve biopsy specimen studied by light microscopy with semi-thin section and teased fiber preparation showed axonal degeneration. The ultrastructural studies of the axonal alterations consisted of degeneration of the neurofilaments and the neurotubules with granular appearance of the axoplasm.

Aged↗