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PubMed2003

Dizocilpine improves beneficial effects of cholinergic antagonists in anticholinesterase-treated mice.

Mice were administered anticholinesterase pesticides dichlorvos (DDVP) or methomyl (MET). Both DDVP and MET induced dose-dependent seizures and lethality in mice. The muscarinic antagonist atropine (ATR, 1.8 mg/kg) did not prevent seizures but diminished the lethality induced by DDVP or MET. The nicotinic antagonist mecamylamine (MEC, 1 mg/kg) affected neither DDVP-induced seizures nor DDVP- and MET-induced lethality, but diminished MET-induced seizures. At a higher dose (10 mg/kg), MEC attenuated seizures produced by MET, but not DDVP, and decreased lethality of both anticholinesterases. The N-methyl-D-aspartate (NMDA) antagonist dizocilpine (MK-801, 1 mg/kg) prevented DDVP-, but not MET-induced seizures. MK-801 did not affect DDVP- or MET-induced lethality. Concurrent administration of ATR and MK-801 prevented the occurrence of DDVP- but not MET-induced seizures. MK-801 coadministered with ATR enhanced its protective effect against DDVP- or MET-induced lethality in mice. Coinjection of MEC (at both doses studied) and MK-801 completely prevented seizures produced by both acetylcholinesterase (AChE) inhibitors. Coadministration of MEC (1 mg/kg) and MK-801 protected mice against DDVP or MET lethality. MK-801 administered along with MEC at 10 mg/kg enhanced antilethal effects of the nicotinic antagonist in DDVP- or MET-treated mice. With respect to the mechanism underlying anticholinesterase-induced neurotoxicity, muscarinic and nicotinic, as well as NMDA receptors, seem to play major roles. The results suggest that combined treatment with cholinergic and NMDA antagonists might be beneficial in anticholinesterase-induced poisonings.

Animals↗
PubMed2006

A method to determine precise benchmark doses for carbamate anticholinesterases.

In determining benchmark doses for risk assessment and regulation of carbamate anticholinesterase pesticides like formetanate, oxamyl, and methomyl, one needs to quantitate low levels of cholinesterase inhibition. For improved accuracy while using fewer subjects, we developed an assay based on the recognized ability of carbamates to protect cholinesterase from irreversible inactivation. This assay measures enzyme that survives diisopropylfluorophosphate exposure in vitro and then reactivates by decarbamylation after small molecules are removed with size-exclusion centrifugation. The 99% silencing of unprotected cholinesterase yields a low background. Comparisons of recovered activity with initial activity (representing carbamate-free enzyme) use each sample as its own control. As a result, carbamate-protection assays can demonstrate a statistically significant 2-3% inhibition of brain cholinesterase in a single experimental group of modest size. When applied to brain samples from formetanate-treated rats, such an assay predicted a benchmark dose of 0.19 mg/kg for 10% inhibition (BMD10), with a lower 95% confidence limit of 0.15 mg/kg (BMDL10). Protection assays should enable precise determinations of benchmark doses for other carbamates, as well as accurate assessment of in vivo inhibition half-lives under low-dose scenarios.

Animals↗
PubMed2000

Citrus leafminer (Lepidoptera: Gracillariidae) density: effect on yield of 'Tahiti' lime.

The relationship between damage by citrus leafminer, Phyllocnistis citrella Stainton, and 'Tahiti' lime yield were investigated in a 15-yr-old and a 5-yr-old lime orchard. Citrus leafminer population densities were controlled by insecticide applications of abamectin plus FC 435 oil, abamectin plus FC435 oil plus imidacloprid, and methomyl. The control was not treated. To ensure adequate citrus leafminer densities, adult citrus leafminer were periodically released in the experimental plots during fall and winter. For the 15-yr-old trees, the least amount of leaf area damage occurred in the abamectin plus FC 435 oil plus imidacloprid (1.9%) and the abamectin plus FC435 oil (2.3%) treatments compared with the control treatment (10-21%). In the 5-yr-old orchard, the least amount of leaf area damaged occurred in the abamectin plus FC 435 oil plus imidacloprid (0.4%) and the imidacloprid (0.1%) treatments compared with the control (20.85%). The percentage of leaf area damaged was linearly correlated with the average number of mines per leaf, average mine days, and cumulative mine days in both orchards. In both orchards, the percentage of leaf area damaged and cumulative mine days was linearly correlated with the number of fruit per tree and total fruit weight per tree. Calculating the economic injury levels indicated that 16-23% and 18-85% of leaf area damaged caused significant yield reductions in 15-yr-old and 5-yr-old trees, respectively.

Animals↗
PubMed1997

Carbamate poisoning in early childhood and in adults.

OBJECTIVE: Retrospective evaluation of the clinical course of carbamate poisoning in young children and adults. DESIGN: Thirty-six children aged 1 to 8 years (median 2.5 years) and 24 adults aged 17 to 41 years (median 22 years) ingested rat poison resulting in carbamate poisoning. The ingested poisons in all cases were positively identified as methomyl or aldicarb by gas chromatography-mass spectrometry. RESULTS: Symptoms of intoxication in children were compared to those in adults with similar depression of the serum cholinesterase. The predominant symptoms in young children were central nervous system depression and hypotonia. The most common muscarinic effect was diarrhea. In adults, the main signs were miosis and fasciculations. Fasciculations in children were less frequent. Central nervous system depression, hypotonia, and diarrhea were uncommon in adults. CONCLUSION: Based on a relatively large number of carbamate poisonings in young children, we conclude that the clinical presentation differs from adult poisoning manifestations. The absence of classic muscarinic effects does not exclude the possibility of carbamate poisoning in young children with central nervous system depression.

Adolescent↗
PubMed1977

Poisoning by carbamate pesticides.

In recent years the number of carbamate pesticides registered for use in New South Wales has increased. Some of the newer carbamates are very toxic and have cholinergic properties similar to those of the organic phosphates, though the effect is of much shorter duration. Because of this, separate tests for plasma and red blood cell levels of cholinesterase should be conducted as soon as possible after exposure in order to obtain meaningful results. A typical case of carbamate poisoning is described in which both plasma and red blood cell cholinesterase values were lowered. The substitution of a liquid pesticide formulation for the original powder formulation has reduced the operator inhalation hazard in the case of methomyl.

Agricultural Workers' Diseases↗
PubMed2001

[A case of carbamate poisoning in which GCMS was useful to identify causal substance and to decide the appropriate treatment].

We often have cases of insecticide poisoning where the patient is unconscious and the causal substances are unknown. We report an 83-year-old unconscious man who had apparently ingested several agricultural chemicals, possibly organophosphate or carbamate. According to his family, there were three kinds of containers of agricultural chemicals with their caps opened around him. When he was transferred to our hospital, he presented hypertension, hypersalivation, and muscle fasciculation. His pupils were markedly miotic. In order to identify the substances ingested we used a gas chromatographymass spectrometer (GCMS) using his gastric content. Within 30 minutes we were able to identify the causal substance as methomyl, one of the popular carbamates, thereby eliminating the need to use pralidoxime (PAM). GCMS makes it possible to identify unknown substances quickly and accurately and is therefore extremely useful in deciding the appropriate treatment.

Aged↗
PubMed2002

[Stimulation single fiber electromyography in rats with myasthenia induced by organophosphorus insecticides and their mixtures poisoning].

OBJECTIVE: To study the neuromuscular function and its relation with the occurrence of myasthenia in rats poisoned by dimethoate (D), phoxim (P), methomyl (M), M + D and M + P respectively. METHODS: The stimulation single fiber electromyography(SSFEMG) at different stimulus frequencies(5, 10 and 20 Hz) was used. The whole blood cholinesterase (ChE) activity was measured 1 h before and after poisoning. RESULTS: (1) Myasthenia occurred in 5 out of 9.5 out of 10.5 out of 5, and 8 rats poisoned by D, P, M + D, and M + P, respectively. (2) The average mean consecutive differences(MCD) at 5, 10, and 20 Hz in myasthenic rats were significantly higher than those of poisoned rats without myasthenia and the control ones. (3) SSFEMG changes at 5, 10 and 20 Hz were significantly consistent with the clinical manifestation of myasthenia, especially at 10 Hz and 20 Hz. (4) ChE activity was significantly lower in rats with P or D poisoning while ChE inhibition was of no difference in rats with M, M + D, and M + P poisoning. In the D poisoning and P poisoning groups, there was no significant difference in ChE inhibition between the rats with and without myasthenia. CONCLUSION: Muscle weakness was associated with neuromuscular transmission dysfunction, but not well correlated with ChE inhibition. The SSFEMG with stimulus frequency at 10 Hz or 20 Hz could be used to detect the neuromuscular dysfunction during myasthenia induced by organophosphate insecticides and their mixtures poisoning.

Animals↗
PubMedDate not supplied

Determination of pesticides in soy-based infant formula using liquid chromatography with electrospray ionization tandem mass spectrometry.

A sensitive method using liquid chromatography with electrospray ionization tandem mass spectrometry (LC/ESI-MS/MS) was developed and validated to quantify and confirm 13 pesticides, including aldicarb sulfoxide, aldicarb sulfone, oxamyl, methomyl, formetanate, 3-hydroxycarbofuran, carbendazim, thiabendazole, aldicarb, propoxur, carbofuran, carbaryl, and methiocarb, in soy-based infant formula. Data acquisition under MS/MS was achieved by applying multiple reaction monitoring of 2 fragment ion transitions to provide a high degree of sensitivity and selectivity for both quantitation and confirmation. Different approaches to constructing calibration curves were compared and discussed to address issues of the extraction efficiency or recovery, and matrix effects. Matrix-matched standard calibration curves with the use of isoprocarb as an internal standard were finally used to achieve the best accuracy of the method. Under most circumstances, recoveries of 13 pesticides, spiked at 5.0, 25.0, and 45.0 microg/kg, were close to 100%. The method detection limits (signal-to-noise ratio > or =3:1; microg/kg) of 13 pesticides were 0.2 for thiabendazole and methiocarb, 0.6 for aldicarb, and 0.1 for the others.

Aldicarb↗
PubMed1991

Kinetic study on inhibition of earthworm acetylcholinesterase by carbamate insecticides.

The specific activity parameters of Acetylcholinesterase (AChE) in adult and immature stages of earthworm (Lumbricus terrestris) were determined. The results show that the tissues of immature and adult stages differ in their affinity rate (Ka) to substrate and maximum enzymic hydrolysis (Vmax). The AChE form of adult stage had higher Vmax value, while the most higher Ka value was shown in the AChE of the immature stage. The studies of inhibition power on the two sources of ACChE indicated that the highest bimolecular inhibition constant value (Ki) was obtained by carbofuran on the AChE of the adult tissues, while aldicarb was the most potent on the immature tissues. The inhibition progress of the AChE by aldicarb was relatively rapid more than the other two tested inhibitors: carbofuran and methomyl.

Aldicarb↗
PubMed1975

[Thin layer chromatographic separation and enzymatic detection of carbamate pesticides in plant extracts].

The authors developed a thin-layer chromatographic technique for the separation of carbamate pesticides from plant material and an enzymatic method for their determination. The cellulose plates were impregnated with polar substances (ethylene glycol, triethylene glycol and beta,beta'-oxydipropionitrile). n-Heptane/chloroform and iso-octane/dioxane served as solvents. The slight enzyme-inhibiting effect and the colouration of the plant extracts render the detection of the pesticides difficult. Nevertheless, the separation and the enzymatic detection of Methomyl, Carbaryl, Baygon and Aldicarb could be achieved. The Rf values of the carbamates are not influenced by the kind (apples, pears, onions) and the quantity (50--200 mg) of the plant material.

Aldicarb↗
PubMed1997

A modified electrometric method for measurement of erythrocyte acetylcholinesterase activity in sheep.

A modified method was compared with an original electrometric method for measurement of erythrocyte acetylcholinesterase (EChE) activity in sheep. The mean +/- SD (pH/30 min) of EChE activity of 8 sheep measured by the modified procedure (0.70 +/- 0.15) was not significantly different from that of the original method (0.64 +/- 0.12). The inherently low plasma cholinesterase activity of the sheep as measured by the 2 methods were also not significantly different from each other (0.09 +/- 0.04 vs 0.10 +/- 0.04). The coefficient of variation of the modified method in measuring EChE activity was 8%. The method was used to demonstrate in vitro inhibition of sheep EChE activity by the organophosphorus and carbamate insecticides dichlorvos and methomyl, respectively. The method could be well-suited for rapid measurement of EChE activity in sheep, especially in cases of organophosphate and possibly carbamate poisoning.

Acetylcholinesterase↗
PubMed1999

Acute carbamate and organochlorine toxicity causing convulsions in an agricultural pilot: a case report.

Agricultural pilots are involved in a particularly hazardous occupation with a high occupational mortality rate. They face many risks, not least of which is exposure to the agricultural chemicals that they spray. Many accidents and illnesses have been reported previously in the literature, attributable to the acute and chronic effects of chemical exposure, most notably the organophosphate family of insecticides. There are few reports of post-crash exposure to carbamate and organochlorine insecticides. This report documents the case of a professional agricultural pilot who, following an emergency landing, was soaked with Methomyl (a carbamate) and Endosulfan (an organochlorine) leaking from his aircraft. He developed cholinergic symptoms within an hour of the accident, which settled spontaneously, but suffered a tonic-clonic seizure some 6 h later while in the hospital. The seizure was attributed to exposure to the organochlorine, however, subsequent EEG recordings demonstrated a non-specific epileptiform focus in the frontal lobes. The pilot made a full recovery and has remained seizure-free without treatment. The pathophysiology of carbamate and organochlorine poisoning is reviewed, and the differential diagnoses of seizures in this pilot discussed. The difficulty facing a licensing authority in determining the aeromedical disposition of a pilot who has suffered a provoked seizure is also highlighted.

Adult↗
PubMed1989

Cholinesterase activity depression among California agricultural pesticide applicators.

Cholinesterase activity measurements for 542 California agricultural pesticide applicators under medical supervision during the first 9 months of 1985 were analyzed. Twenty-six workers, 4.8% of the sample, had cholinesterase values at or below the California threshold values for removal from continued exposure to cholinesterase-inhibiting pesticides (60% of baseline for red blood cell cholinesterase and 50% of baseline for plasma cholinesterase activity). Eight of these 26 workers, 31.5%, had pesticide-related illnesses. Pesticides most frequently associated with cholinesterase depressions exceeding California threshold values included mevinphos (Phosdrin), oxydemeton methyl (Metasystox-R), methomyl (Lannate), and acephate (Orthene); these pesticides included organophosphates in toxicity categories I and II and one carbamate in toxicity category I.

Agricultural Workers' Diseases↗
PubMed2005

Liquid chromatographic determination of nine N-methylcarbamates in drinking water.

A multi-residue method for the simultaneous extraction from drinking water using solid-phase extraction on LiChrolut EN [poly(styrene-divinylbenzene), PSDVB] and determination of nine N-methylcarbamate pesticides (NMCs) (aldicarb, its metabolites i.e. aldicarb sulfone and aldicarb sulfoxide and carbaryl, carbofuran, dioxacarb, ethiofencarb, methomyl and propoxur) using reversed-phase liquid chromatography was studied. A 1000-fold pre-concentration was achieved and the method was used for determination of the nine pesticides in water, with limits of detection in the range 3-15 ng L(-1). For all compounds the recoveries determined at the 0.1 and 1 microg L(-1) level generally ranged from 85 to 104% with relative standard deviations (RSD) of 1.4-8.8%.

Carbamates↗
PubMed2006

Ammonium perfluorooctanoate as a volatile surfactant for the analysis of N-methylcarbamates by MEKC-ESI-MS.

Ammonium perfluorooctanoate (APFOA) was investigated as an MS-friendly surfactant for the analysis of a mixture of ten N-methylcarbamates with MEKC-ESI-MS. Because of the relatively low boiling point of perfluorooctanoic acid ( approximately 190 degrees C), APFOA can be introduced into a mass spectrometer without the adverse effects of less volatile surfactants such as SDS. With a BGE consisting of 50 mM APFOA/isopropanol (IPA) 98:2 and with 30 kV applied, a very fast separation ( approximately 6 min) was possible with only one pair of analytes comigrating. Using an experimental design with four factors (voltage, nebulizer pressure, concentration of APFOA, and concentration of IPA) we were able to resolve all analytes in just over 11 min. Sheath liquid composition and flow rate, drying gas temperature and flow rate, and fragmentor voltage were then optimized for maximum signal intensity and S/N. It was found that the faster method gave better S/N because of narrower peak widths, and detection limits in SIM mode were between 0.01 (aldicarb) and 0.08 mg/L (methomyl). Calibration curves were prepared with standards of 0.50, 1.00, and 2.00 mg/L for the analysis of samples obtained after SPE of tap water spiked with the ten N-methylcarbamates at a level of 10 microg/L. All analytes showed very good recoveries (>86%), except for the most polar analyte aldicarb sulfone (recovery of 73%), testifying for the potential use of APFOA for this kind of analyses.

Caprylates↗
PubMed2001

Activity of the botanical aphicides 1,5-diphenyl-1-pentanone and 1,5-diphenyl-2-penten-1-one on two species of Aphididnae.

1,5-Diphenyl-1-pentanone (A) and 1,5-diphenyl-2-penten-1-one (B) are natural products extracted for the first time from Stellera chamaejasme. Laboratory bioassay showed that the two products have strong contact activity and very good anti-feedant activity against Aphis gossypii and Schizaphis graminum. Both products showed dose-dependent relationships for both forms of activity against the two aphids, the contact activity of B being about twice that of A. Both products were inferior to methomyl in contact activity but superior in anti-feedant activity against the two aphids. This is the first report of aphicidal activity in these two compounds, which may represent a new class of aphicide.

Animals↗
PubMed2001

Monitoring insecticide resistance in house flies (Diptera: Muscidae) from New York dairies.

House flies were collected from dairies across New York state and the levels of resistance to seven insecticides were measured using standard laboratory assays with three to five diagnostic concentrations. The highest levels of resistance were found for tetrachlorvinphos, permethrin and cyfluthrin. Although levels of resistance to methomyl were somewhat lower, they were among the highest ever reported for field-collected house flies. Resistance to pyrethrins was limited primarily to the lowest diagnostic concentration. House flies were susceptible to fipronil at all dairies, suggesting that this material would be highly effective for fly control. The levels of resistance were similar at all the dairies, irrespective of their insecticide use, suggesting substantial movement of flies between facilities. Relative to resistance levels found at New York dairies in 1987, resistance levels had increased for permethrin, were unchanged for tetrachlorvinphos and had decreased for dimethoate. To identify a single diagnostic concentration that could be used in the laboratory assays to assess accurately resistance levels in future studies, we carried out a 'simulated' field bioassay using formulated materials. A diagnostic concentration for each insecticide is proposed on the basis of a comparison of our bioassays.

Adaptation, Physiological↗
PubMed2001

Sex-related response to organophosphorus and carbamate insecticides in adult Oriental fruit moth, Grapholita molesta.

During the development of a resistance-monitoring bioassay that uses males as the life-stage tested, the relationship of adult female and male susceptibility of Grapholita molesta to different classes of insecticides was investigated. Preliminary results indicated that more males survived diagnostic doses of azinphos-methyl than females. Additional research revealed that, although the body mass of adult male G molesta was only 69% of that of female moths (5.67 and 8.20 mg, respectively), their LC50 values were 2.6, 4.1 and 10.3 times higher than those of females for azinphosmethyl, malathion and parathion-methyl, respectively. However, female G molesta moths were more tolerant to methomyl than were male moths. There was no indication that this sex-related response occurred in G molesta larvae. The results presented here raise concerns regarding the use of pheromone traps for determining whether insecticide treatments are required and as part of resistance monitoring programs.

Animals↗