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PubMed1992

Reduction by pyridostigmine pretreatment of the efficacy of atropine and 2-PAM treatment of sarin and VX poisoning in rodents.

This study concerned the effect of pyridostigmine pretreatment on (a) the antidotal efficacy of atropine and 2-PAM in sarin, tabun, and VX poisoning in mice and guinea pigs and on (b) the oxime-induced reactivation of VX-inhibited whole blood acetylcholinesterase (AChE) of guinea pigs. One hour prior to organophosphate (OP) challenge with sarin, tabun, or VX, animals were given oral doses of pyridostigmine to induce approximately 30 and 60% inhibition of whole blood AChE; controls received vehicle. Mice were challenged im and guinea pigs sc with the OP compounds. Treatment with atropine (11.2 mg/kg to mice; 32 mg/kg to guinea pigs) plus 2-PAM (25 mg/kg) was given im at 10 sec postchallenge in mice and 1 min postchallenge in guinea pigs. In the reactivation experiments, pyridostigmine or saline was given im to guinea pigs 30 min prior to VX (8.24 micrograms/kg, sc), atropine (16 mg/kg) was given im at 1 min, and 2-PAM (25 mg/kg) at 16 min postchallenge. Pyridostigmine significantly enhanced the efficacy of atropine and 2-PAM against tabun in both species. In contrast, pyridostigmine reduced or did not increase the efficacy of atropine and 2-PAM against sarin or VX in both species. Recovery of VX-inhibited AChE by 2-PAM was decreased significantly in pyridostigmine pretreated animals. The results suggest that pyridostigmine pretreatment may adversely effect the efficacy of atropine and 2-PAM as antidotes for VX and sarin intoxication.

Acetylcholinesterase↗
PubMed1997

Evaluation of combined toxic effects of GB/GF and efficacy of jielin injection against combined poisoning in mice.

A computer program (Q-test) was used to evaluate the combined toxic effects of nerve agent GF and its combined form with sarin (GB/GF) in mice. Efficacy of Jielin Injection, the 2-PAM-containing antidote used successfully in China for the treatment of organophosphate pesticide poisoning, was also evaluated and compared with HI-6 against single and combined poisonings. The two agents were basically additive in toxicity when combined. However, toxic signs (convulsions) appeared later in combined poisoning than after exposure to each agent alone. The protective ratio of Jielin Injection against GF poisoning was low but significantly higher when against poisoning by GB or combined agent. When HI-6 was substituted for 2-PAM, the antidote was more effective against poisoning by both single and combined agents. Results of in vitro reactivation of GF-inhibited human erythrocyte acetylcholinesterase by these oximes agreed with the in vivo antidotal efficacy.

Animals↗
PubMedDate not supplied

Carbamate derivatives of 2-arylimidazo[1,2-a]pyridinium salts as acetylcholinesterase inhibitors and protective agents against organophosphorus compounds.

A series of 2-arylimidazo[1,2-a]pyridinium salts with (N,N-dimethylcarbamoyl)oxy or (N-methylcarbamoyl)oxy groups at the 3'- or 4'-position on the phenyl substituent and various substituents on the imidazo[1,2-a]pyridine ring have been synthesized. The compounds show in vitro inhibitory activity against electric eel acetylcholinesterase (AChE), type III, and several of the compounds show protective effects toward the organophosphorus AChE inhibitor soman in mice. The possible structural relationship of these compounds to physostigmine and pyridostigmine is considered.

Animals↗
PubMed1980

Organophosphate pesticide inhibition of cholinesterase in laboratory animals and man and effects of oxime reactivators.

The responses of rabbit whole blood cholinesterase following intravenous infusion or percutaneous application of dialkylphosphate inhibitors and injection of oxime enzyme reactivators. The experiments were conducted to determine the structure-activity relationships of the inhibitors and the reactivators, establish the mechanisms of enzyme inhibition, and investigate other factors affecting the toxicity of organophosphate esters including percutaneous absorption and conversion of dithioates to the more reactive respective ozones. Intravenous infusion of dialkylphosphate esters produced dose and time dependent inhibition, followed by a spontaneous, but incomplete recovery. The lack of complete recovery was not totally due to the "aging" phenomona as measurable enzyme reactivation could be induced subsequent to the spontaneous recovery. The need for revision of the enzyme inhibition model is discussed.

Animals↗
PubMed1983

Persistence of symptoms after mild to moderate acute organophosphate poisoning among 19 farm field workers.

Exposure to 2 organophosphate pesticides occurred when entry into a cauliflower field was permitted 4 h after application of highly toxic chemicals. It resulted in acute illness of mild to moderate degree in 19 farm workers, including 3 children and 1 pregnant woman. There were no fatalities. Two to three months were required for recovery from major symptoms and return to normal acetylcholinesterase levels. An exception was the persistence of eye symptoms in the majority 4 mo after the day of exposure.

Adolescent↗
PubMedDate not supplied

Toxicological properties of O,O,S-trialkyl phosphorothioates.

The effect of atropine, 2-pyridine aldoxime methiodide (2-PAM), and several O,O,O-trialkylphosphorothioates on poisoning of rats by a series of O,O-dimethyl and O,O-diethyl S-alkyl phosphorothioates was investigated. Atropine and 2-PAM successfully protected rats treated with O,O-diethyl S-n-propyl and S-i-propyl phosphorothioates, while the O,O,O-trialkyl phosphorothioates were effective in protecting rats treated with O,O-dimethyl S-methyl and S-ethyl phosphorothioates. O,O-Dimethyl and O,O-diethyl S-i-propyl phosphorothioates also were examined for in vitro and in vivo inhibition of rat plasma, red blood cell, and brain cholinesterase. Overall, the results indicated that two different mechanisms, cholinergic and noncholinergic, are involved in intoxication by the O,O,S-trialkyl phosphorothioates.

Animals↗
PubMed1985

Organophosphate insecticide poisoning.

Organophosphate insecticides are widely used agents which are quickly absorbed through the skin and mucous membranes. The effects of acute exposure to these agents can be severe and intensive therapy may be required. Specific drugs are available to reverse the muscarinic, nicotinic and central effects of these poisons. When given early they are very effective and early diagnosis and treatment may therefore be life-saving. A case of acute poisoning with an organophosphate anticholinesterase insecticide is reported. The signs and symptoms of acute poisoning are described and a rational approach to specific treatment is discussed.

Acute Disease↗
PubMed1975

Delivery of a quaternary pyridinium salt across the blood-brain barrier by its dihydropyridine derivative.

A dihydropyridine-pyridine type redox system was successfully applied for delivering a quaternary pyridinium salt, N-methylpyridinium-2-aldoxime chloride (2-PAM), through the blood-brain barrier. The dihydropyridine derivative of 2-PAM was quickly oxidized to 2-PAM after crossing the blood-brain barrier. As a result of this approach, the brain cholinesterase blocked by organophosphates could be reactivated. The new method should be useful in delivering numerous drugs which are otherwise inaccessible to the brain because of their polar ionic character.

Animals↗