[Importance of reactivation of fosdrin-inhibited acetylcholinesterase in the brain and diaphragm for the in vivo therapeutic effect of oximes in rats poisoned with fosdrin].
BACKGROUND
The composition of the causal antidotal therapy of subjects, poisoned with organophosphorus insecticides, has not been satisfactorily solved till now in spite of the knowledge of the basic mechanism of action of these toxic substances. The purpose of this study is to evaluate which of currently used or perspective acetylcholinesterase reactivators seems to be the most efficacious to protect poisoned subjects.


RESULTS
In experiments on white laboratory rats, the reactivating efficacy of selected acetylcholinesterase reactivators (oximes), administered at equimolar doses, was evaluated in target tissue of toxic effects of organophosphorus insecticides (diaphragm, brain) and compared with their therapeutic efficacy in the case of prophylactic administration with the help of the evaluation of mean efficacy dose of oximes, possible to protect rats exposed to supralethal dose of organophosphorus insecticide fosdrin for 24 hours. Our findings confirm that there are not statistically significant differences in reactivating and therapeutic efficacy of oximes tested against fosdrin in rats.


CONCLUSIONS
The perspective acetylcholinesterase reactivators (H oximes) seem to be as suitable as currently used oximes for the therapy of acute poisonings with organophosphorus insecticides although they are not significantly more efficacious than currently used oximes as in the case of the treatment of poisoning with highly toxic organophosphorus compounds.
Vojenská lékarská akademie JEP, Hradec Králové.
J
J
Kassa
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000201:enzymology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology / Q000506:poisoning* / Q000627:therapeutic use*; D003964:Diaphragm / Q000201:enzymology*; D004789:Enzyme Activation / Q000187:drug effects; D007306:Insecticides / Q000494:pharmacology / Q000506:poisoning*; D008297:Male; D008799:Mevinphos / Q000494:pharmacology / Q000506:poisoning*; D010091:Oximes / Q000627:therapeutic use*; D011041:Poisoning / Q000188:drug therapy / Q000201:enzymology; D051381:Rats; D017208:Rats, Wistar
D002800:Cholinesterase Inhibitors; D007306:Insecticides; D010091:Oximes; D008799:Mevinphos; D000110:Acetylcholinesterase