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Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans

✍ Scribed by T. Thomsen; U. Bickel; J. P. Fischer; H. Kewitz

Publisher
Springer
Year
1990
Tongue
English
Weight
252 KB
Volume
39
Category
Article
ISSN
0031-6970

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✦ Synopsis

The effect of galanthamine (GAL) and its 2 major metabolites on human cholinesterases has been explored. Epigalanthamine, a diastereomer of GAL, was 130-times less potent in vitro in its effect on acetylcholinesterase (AChE) in erythrocytes than the parent compound, and it did not differ significantly from the ketone galanthaminone. In vivo, the maximal 36-55% inhibition of AChE was approached 30 min after oral administration of 10 mg GAL. The duration of the catalytic inhibition corresponded to an elimination half-life of approximately 5-7 h. GAL was well tolerated in 8/8 healthy volunteers, and 3/4 Alzheimer patients tolerated the drug up to a daily dose of 40 mg.

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