Tacrine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in Alzheimer's disease

Drugs & Aging
A J Wagstaff, D McTavish

Abstract

Tacrine is a centrally acting cholinesterase inhibitor with additional pharmacological activity on monoamine levels and ion channels. It has been postulated that some or all of these additional properties may also be relevant to the mode of action of the drug. There are wide interindividual variations in pharmacological and clinical response to tacrine, possibly related to interindividual variation in bioavailability. Tacrine appears to improve cognitive function and behavioural deficits in a proportion of patients with Alzheimer's disease, at dosages of 80 to 160 mg/day. In the best designed trials, 30 to 51% of evaluable patients showed an improvement of at least 4 points on the cognitive subscale of the Alzheimer's Disease Assessment Scale, versus 16 to 25% of placebo recipients. A similar proportion of tacrine recipients were judged to have improved when global assessment scales were used. There was a significant dose-response relationship up to 160 mg/day. However, large numbers of patients were withdrawn during the trials, many because of tacrine-associated increases in transaminase levels. Elevated liver enzyme levels occurred in about 50% of tacrine recipients (reaching clinical significance in about 25%). Cholinergic s...Continue Reading

Citations

May 1, 1997·Journal of the American Geriatrics Society·F LandiG Gambassi
Jan 1, 1996·Acta Neurologica Scandinavica. Supplementum·A Nordberg
Jan 15, 2005·Pharmaceutical Research·Rashmi S Upasani, Ajay K Banga
Jul 11, 2006·Drugs & Aging·Lorenzo PrianoAlessandro Mauro
Jul 24, 2015·Toxicological Sciences : an Official Journal of the Society of Toxicology·Sehan Lee, Mace G Barron
May 20, 1999·The Annals of Pharmacotherapy·W J KrallN R Cutler
Dec 5, 1998·British Journal of Clinical Pharmacology·P J TiseoL T Friedhoff
Jun 30, 2010·Journal of Enzyme Inhibition and Medicinal Chemistry·Stevan PecicWayne W Harding
Jan 1, 2020·Biomolecules·Gabriela Dumitrita StanciuDaniela Carmen Ababei
Oct 27, 2001·Journal of Autonomic Pharmacology·M A BecerraE Marhuenda
Aug 7, 2002·Clinical Pharmacokinetics·Michael W JannGary W Small
Apr 1, 1996·Clinical Pharmacology and Therapeutics·S T ForgueT M deVries
Feb 11, 2020·Biochemical and Biophysical Research Communications·Valery M DembitskyVladimir D'yakonov
Nov 19, 1997·The Medical Journal of Australia·H Brodaty, P S Sachdev
Oct 10, 2020·Neuropharmacology·Gabriella MarucciFrancesco Amenta
Oct 26, 2002·European Journal of Pharmacology·Gary L WenkBeatrice Hauss-Wegrzyniak

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