engleski

Efficiency of Phenyl-Imidazolium and Quinuclidinium Oximes in Organophosphorus and Carbamates Intoxication

Organophosphorus compounds (Ops) and carbamates are widely used as pesticides in agriculture, drugs in treatment of cholinergic disorders and chemical warfare agent. In this paper the efficiency of new compounds bis-phenyl-imidazolium (2B) and imidazolium-quinuclidinium oximes (BM-1) were tested on OPs and carbamates intoxicated mice in vivo, and on human erythrocytes acethylcholinesterase (AChE ; 3.1.1.7) in vitro. Oxime 2B strongly inhibits the AChE, and has good reactivation potency, while the oxime BM-1 weakly inhibits AChE and its in vitro activity against OPs and carbamates inhibited AChE is negligible. In in vivo experiment tested compounds were applied intraperitoneally at 1/4 of their respective LD50 dose together with atropine (10 mg/kg body weight) immediately after subcutaneous administration of OPs or carbamates. Both oximes were highly effective in the therapy of mice intoxicated with dichlorvos and propoxur, whereas BM-1 provided a 100% protection of mice against 4 x LD50 of soman, 3.2 x LD50 of tabun, and 20 x LD50 of RO 2-0683, respectively. The results indicate that in vivo efficiency of BM-1, and its ineffectivness in vitro must be attributed to mechanism not yet well defined. Very good in vivo action of tested oximes is especially interesting in the carbamate intoxication, because actually the drug of choice is atropine only.

Oximes; organophosphorus; carbamates

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