Molecular and cellular actions of galantamine: clinical implications for treatment of organophosphorus poisoning

J Mol Neurosci. 2010 Jan;40(1-2):196-203. doi: 10.1007/s12031-009-9234-3. Epub 2009 Aug 19.

Abstract

There have been continued efforts to develop effective antidotal therapies against poisoning with organophosphorus (OP) compounds, including nerve agents and pesticides. We reported recently that galantamine, a drug used to treat Alzheimer's disease, administered before (up to 3 h) or soon after (up to 5 min) an exposure of guinea pigs to 1.5-2 x LD50 soman or sarin effectively counteracted the acute toxicity and lethality of the nerve agents provided that the animals were also post-treated with atropine. Here, we demonstrate that administered to guinea pigs at 30 min before or up to 15 min after an acute challenge with 1 x LD50 soman, galantamine (8 mg/kg, intramuscular) alone is sufficient to counteract the lethality and acute toxicity of the nerve agent. Evidence is also provided that 100% survival can be attained when the association of appropriate doses of galantamine and atropine is administered 30-45 min after the challenge of the guinea pigs with 1 x LD50 soman. Galantamine counteracts the neurodegeneration and the changes in the nicotinic cholinergic system that result from an acute exposure of guinea pigs to 1 x LD50 soman. The results presented herein corroborate that galantamine is an effective antidote against OP poisoning.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Acetylcholinesterase / drug effects
  • Acetylcholinesterase / metabolism
  • Animals
  • Atropine / pharmacology
  • Brain / drug effects
  • Brain / metabolism
  • Brain / pathology
  • Chemical Warfare Agents / toxicity
  • Cholinergic Fibers / drug effects
  • Cholinergic Fibers / metabolism
  • Cholinergic Fibers / pathology
  • Cholinesterase Inhibitors / pharmacology*
  • Cholinesterase Inhibitors / therapeutic use
  • Cholinesterase Reactivators / pharmacology*
  • Cholinesterase Reactivators / therapeutic use
  • Drug Interactions / physiology
  • Female
  • Galantamine / pharmacology*
  • Galantamine / therapeutic use
  • Guinea Pigs
  • Lethal Dose 50
  • Male
  • Muscarinic Antagonists / pharmacology
  • Nerve Degeneration / chemically induced
  • Nerve Degeneration / drug therapy
  • Nerve Degeneration / prevention & control
  • Organ Culture Techniques
  • Organophosphate Poisoning*
  • Organophosphorus Compounds / antagonists & inhibitors*
  • Sarin / antagonists & inhibitors
  • Sarin / toxicity
  • Soman / antagonists & inhibitors
  • Soman / toxicity
  • Treatment Outcome

Substances

  • Chemical Warfare Agents
  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators
  • Muscarinic Antagonists
  • Organophosphorus Compounds
  • Galantamine
  • Atropine
  • Soman
  • Sarin
  • Acetylcholinesterase