Galantamine, a cholinesterase inhibitor
that allosterically modulates nicotinic receptors: effects on the course of
Alzheimer's disease
Coyle, Kershaw
Biol Psychiatry 2001 Feb; 49 (3) 289-299
Abstract
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.