STUDIES ON THE THERAPEUTIC EFFECT OF 2-PYRIDINE ALDOXIME METHIODIDE (2-PAM) IN MAMMALS FOLLOWING ORGANOPHOSPHORUS COMPOUND-POISONING (REPORT III):DISTRIBUTION AND ANTIDOTAL EFFECT OF 2-PAM IN RATS

The metabolic fate of 2-PAM and its antidotal effect on organophosphorus compound poisoning in rats were studied. When 14C-2-PAM was administered intravenously, the amount of 14C reaching the brain was small. Following administration by intramedullary injection, 14C was present in high concentration...

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Veröffentlicht in:	Journal of toxicological sciences 1993/11/25, Vol.18(4), pp.265-275
Hauptverfasser:	UEHARA, Sachiko, HIROMORI, Toshihiko, ISOBE, Naohiko, SUZUKI, Takashi, KATO, Terushige, MIYAMOTO, Junshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antidotal study Antidotes - administration & dosage Antidotes - pharmacokinetics Antidotes - therapeutic use Biological and medical sciences Brain - enzymology Brain - metabolism Chemical and industrial products toxicology. Toxic occupational diseases Cholinesterase Reactivators - administration & dosage Cholinesterase Reactivators - pharmacokinetics Cholinesterase Reactivators - therapeutic use Cholinesterases - metabolism Enzyme Activation Fenitrothion - poisoning Half-Life Injections Injections, Intravenous Malathion - poisoning Male Medical sciences Organophosphate Poisoning Poisoning - drug therapy Pralidoxime Compounds - administration & dosage Pralidoxime Compounds - pharmacokinetics Pralidoxime Compounds - therapeutic use Rats Rats, Sprague-Dawley Subarachnoid Space Tissue Distribution Toxicology Various organic compounds
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Zusammenfassung:	The metabolic fate of 2-PAM and its antidotal effect on organophosphorus compound poisoning in rats were studied. When 14C-2-PAM was administered intravenously, the amount of 14C reaching the brain was small. Following administration by intramedullary injection, 14C was present in high concentrations in the brain, and 72-90% of the 14C present in the brain corresponded to the unchanged form of 2-PAM. 2-PAM was rapidly excreted into the urine and feces following either intramedullary or intravenous administration. The half-life of 2-PAM in the brain following intramedullary administration was 1.52 hr. Intramedullary administration of 2-PAM to rats poisoned with fenitrothion or malathion enabled their survival and induced reactivation of brain cholinesterase.
ISSN:	0388-1350 1880-3989
DOI:	10.2131/jts.18.4_265