Tacrine

Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was first synthesised at the Department of Pharmacology at the University of Sydney.

Clinical uses

Tacrine was the prototypical cholinesterase inhibitor for the treatment of Alzheimer's disease. Its clinical effectiveness was hindered by poor oral bioavailability and considerable adverse drug reactions (including nausea, diarrhoea, urinary incontinence, and hepatotoxicity) such that few patients could tolerate therapeutic doses. Indeed there is some doubt as to its efficacy in humans at all. Other newer cholinesterase inhibitors, such as donepezil, are now preferred over tacrine.

Sources

  • Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6

 

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