Reference

In vivo inhibition of rabbit whole blood cholinesterase with organophosphate inhibitors and reactivation with oximes

In vivo inhibition of rabbit whole blood cholinesterase with organophosphate inhibitors and reactivation with oximes. Gough, B. J.; Shellenberger, T. E. (Gulf South Res. Inst., New Iberia, La., USA). Drug Chem. Toxicol., 1(1), 25-43 (English) 1978. CODEN: DCTODJ. DOCUMENT TYPE: Journal CA Section: 4 (Toxicology) The di-Me phosphates, Bidrin [141-66-2], C 2307 [25601-84-7], DDVP [62-73-7], Gutoxon (I) [961-22-8], and the oxygen analog [7533-78-0] of C 9491 produced dose- and time-related inhibition of cholinesterase [9001-08-5] during infusion into rabbits; inhibited enzyme recovered spontaneously to 60-80% of normal activity within 60-90 min after infusion. Azodrin [6923-22-4]-induced inhibition was dose- and time-related, but immediate spontaneous recovery was negligible. Injection of 2-pyridinealdoxime methiodide (2-PAM) [94-63-3] immediately following infusion produced rapid almost complete reactivation of cholinesterase (progressively less reactivation was seen at 1-3 h following infusion of all di-Me phosphates). Enzyme inhibited with SD 1652 [72-00-4], a di-Et phosphate, was reactivated by 2-PAM up to at least 48 h following inhibitor infusion. 1,1'-Trimethylenebis[4-(hydroxyiminomethyl)pyridinium bromide] [56-97-3] and 2-pyridinealdoxime Me methanesulfonate [154-97-2] produced marked enzyme reactivation when injected immediately following inhibitor infusion; isonitrosoacetone [306-44-5] and diacetyl monoxime [57-71-6] were not effective at doses 3100 mg/kg. Results suggest that spontaneous reactivation of inhibited cholinesterase may be due partially to a reversal of the enzyme inhibitor complex as well as to hydrolysis of the dialkyl phosphorylated enzyme.

Antidote for organophosphorus intoxication

Antidote for organophosphorus intoxication. Popa, Ioan; Popescu, Maria (Ministerul Apararii Nationale, Rom.). Rom. RO 59391 10 Nov 1975, 2 pp. (Romanian). (Romania). CODEN: RUXXA3. CLASS: IC: A61K023-06. APPLICATION: RO 71-67336 17 Jun 1971. DOCUMENT TYPE: Patent CA Section: 4 (Toxicology) An antidote is given for poisoning by organophosphorus compds., contg. benactyzine-HCl [57-37-4], phenacyl oxime g-picolinium chloride [67037-55-2], and diacetyl monoxime [57-71-6]. Thus, 1 antidote dragee contains benactyzine-HCl 0.002, diacetyl monoxime 0.198, phenacyl oxime g-picolinium chloride 0.2 and other inert materials. Two dragees completely prevented the poisoning of dogs by parathion [56-38-2] (3 times the LD50 dose).