Tolerance to anticholinesterase compounds in mammals

Toxicology. 1982;25(2-3):79-97. doi: 10.1016/0300-483x(82)90021-x.

Abstract

Administration of multiple, sublethal doses of organophosphorus insecticides induces the development of tolerance to their toxicity. Among the different hypotheses investigated to explain the mechanism of this phenomenon, the one which has received the greatest experimental support is a downregulation of the muscarinic cholinergic receptors. Subsensitivity to cholinergic agonist has been demonstrated in vivo and in vitro in isolated organ preparations. Receptor binding experiments using muscarinic antagonists and agonists revealed a decrease of cholinergic receptors in central and peripheral tissues. Tolerance to another class of acetylcholinesterase inhibitors, carbamates has also been demonstrated. Differences from and similarities to organophosphate tolerance are discussed.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Carbamates
  • Cholinesterase Inhibitors / toxicity*
  • Drug Tolerance
  • Insecticides / toxicity
  • Organophosphorus Compounds
  • Parasympathetic Nervous System / drug effects
  • Parasympathomimetics / pharmacology
  • Receptors, Muscarinic / drug effects
  • Receptors, Nicotinic / drug effects

Substances

  • Carbamates
  • Cholinesterase Inhibitors
  • Insecticides
  • Organophosphorus Compounds
  • Parasympathomimetics
  • Receptors, Muscarinic
  • Receptors, Nicotinic