Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors: effects on the course of Alzheimer's disease

Biol Psychiatry. 2001 Feb 1;49(3):289-99. doi: 10.1016/s0006-3223(00)01101-x.


Despite the proven efficacy of acetylcholinesterase inhibitors in Alzheimer's disease, there is a need for new and more effective treatments. Galantamine is a novel treatment for Alzheimer's disease that inhibits acetylcholinesterase and modulates nicotinic receptors. In randomized, double-blind, placebo-controlled studies of up to 6 months duration, galantamine significantly improved cognitive function. Galantamine also had beneficial effects on instrumental and basic activities of daily living, and postponed the progression of behavioral symptoms. Patients who completed one of the 6-month, placebo-controlled studies were eligible to enter a 6-month, open-extension study of the 24-mg/day dose of galantamine. At the end of 12 months, cognitive function and activities of daily living were preserved in those patients who had been treated throughout the study with galantamine 24 mg/day. At 12 months, this group of patients had significantly better cognitive functions than patients who had been treated with a placebo for 6 months before receiving galantamine. These studies indicate that galantamine postpones the progression of symptoms in Alzheimer's disease. Since galantamine shows the greatest benefits when treatment is started early, its long-term benefits may result from an effect on the underlying disease process; such an effect might be mediated by galantamine's concomitant action on nicotinic receptors.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Aged
  • Allosteric Regulation / drug effects
  • Allosteric Site / drug effects*
  • Alzheimer Disease / diagnosis
  • Alzheimer Disease / drug therapy*
  • Brain / drug effects
  • Cholinesterase Inhibitors / administration & dosage*
  • Cholinesterase Inhibitors / adverse effects
  • Clinical Trials, Phase III as Topic
  • Disease Progression
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Drug Administration Schedule
  • Galantamine / administration & dosage*
  • Galantamine / adverse effects
  • Humans
  • Multicenter Studies as Topic
  • Randomized Controlled Trials as Topic
  • Receptors, Nicotinic / drug effects*


  • Cholinesterase Inhibitors
  • Receptors, Nicotinic
  • Galantamine