Actions and interactions of cholinolytics and cholinesterase reactivators in the treatment of acute organophosphorus toxicity

Drug Chem Toxicol. 1991;14(3):283-91. doi: 10.3109/01480549109002190.

Abstract

Different drug combinations consisting of cholinolytic and a cholinesterase (ChE) reactivator provide greater therapeutic efficacy in acute organophosphorus (OP) poisoning in mice than when used alone. Maximum protection, as determined by a shift of the LD50 for the two OP agents, was observed with the cholinolytic benactyzine. A protection index (P.I.) of 42 was obtained when benactyzine was given along with obidoxime in diisopropylphosphorofluoridate (DFP) intoxication. With the more toxic OP agent soman (o-pinacolylmethylphosphonofluoridate), the same cholinolytic only offered a maximum P.I. of 3.2 when administered with HS-6, another bispyridinium ChE reactivator. This beneficial effect of benactyzine is possibly due to its greater antimuscarinic effect in the central nervous system than atropine or dexetimide.

MeSH terms

  • Acute Disease
  • Animals
  • Benactyzine / therapeutic use
  • Cholinesterase Reactivators / therapeutic use*
  • Male
  • Mice
  • Obidoxime Chloride / therapeutic use
  • Organophosphate Poisoning*
  • Parasympatholytics / therapeutic use*
  • Poisoning / drug therapy
  • Pralidoxime Compounds / therapeutic use

Substances

  • Cholinesterase Reactivators
  • Parasympatholytics
  • Pralidoxime Compounds
  • HS 6
  • Obidoxime Chloride
  • Benactyzine