Mechanism of action and metabolism of acetylcholinesterase inhibitors: Implications for treatment

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8 Scopus citations


Alzheimer's disease is characterized by substantial loss of cholinergic neurons and choline acetyl transferase, correlating with deficits in memory and other aspects of cognition. Elevation of levels of acetylcholine in the brain should potentiate cholinergic function, and a number of modalities have been designed to test this hypothesis. One approach which is emerging as an important therapy for mild to moderate AD is that of acetylcholinesterase inhibition. The first acetylcholinesterase inhibitors (AChEIs) produced modest clinical improvement in a minority of patients with Alzheimer's disease, but were associated with significant toxicity. However, the second generation AChEIs have improved tolerability and the use of donepezil, which has been licensed in the United States for the past two years, has led to a wider acceptance of AChEI therapy by physicians and their patients. There are differences between these new AChEIs in enzyme selectivity, site specificity, half-life, and metabolism, indicating possible distinctions in clinical utility. The future acceptance and use of each new AChEI will depend on clarification of the clinical implications of their differing properties, as well as the long-term interactions of AChEIs with commonly-prescribed drugs such as nonsteroidal anti-inflammatory agents, estrogens, and free radical inhibitors.

Original languageEnglish (US)
Pages (from-to)S2-S6
JournalInternational Journal of Geriatric Psychopharmacology
Issue numberSUPPL. 1
StatePublished - Jan 1 1998


  • Acetylcholinesterase inhibitors
  • Alzheimer's disease
  • Pharmacodynamics
  • Pharmacokinetics

ASJC Scopus subject areas

  • Geriatrics and Gerontology
  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Neuropsychology and Physiological Psychology

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