PMID: 2095347Jan 1, 1990Paper

Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans

European Journal of Clinical Pharmacology
T ThomsenH Kewitz

Abstract

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.

References

May 1, 1989·Neuropathology and Applied Neurobiology·C DuyckaertsJ J Hauw
Jul 1, 1988·Journal of Clinical Chemistry and Clinical Biochemistry. Zeitschrift Für Klinische Chemie Und Klinische Biochemie·T ThomsenO Pleul
Jan 26, 1966·Annals of the New York Academy of Sciences·F F Foldes, J C Smith

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Citations

Feb 26, 2013·Archives of Pharmacal Research·Preet Anand, Baldev Singh
Jan 1, 1995·Pharmacology & Therapeutics·A L Harvey
Mar 1, 1996·Journal of Ethnopharmacology·P A De Smet
Jan 4, 2012·Nature Reviews. Drug Discovery·Daniel A Bachovchin, Benjamin F Cravatt
Feb 21, 2002·Biological & Pharmaceutical Bulletin·Motoh MutsugaMakoto Inoue
Aug 1, 1991·European Journal of Clinical Chemistry and Clinical Biochemistry : Journal of the Forum of European Clinical Chemistry Societies·T ThomsenH Kewitz
Dec 17, 2003·Clinical Pharmacokinetics·Martin R Farlow
Feb 9, 2011·Journal of Pharmaceutical and Biomedical Analysis·Lygia Azevedo MarquesMartin Giera
Mar 16, 2004·Fundamental & Clinical Pharmacology·Carla PettenatiCarlo Caltagirone
Jun 9, 2001·Clinical Therapeutics·A Maelicke
Jul 30, 2015·Neurochemistry International·Yu Pong NgNancy Y Ip
Nov 4, 2000·Expert Opinion on Investigational Drugs·J J SramekN R Cutler
Jan 27, 2006·The Cochrane Database of Systematic Reviews·C Loy, L Schneider
Dec 10, 1999·Journal of Clinical Psychopharmacology·J S KennedyM H Ebert
Aug 4, 2009·Toxicology and Applied Pharmacology·Corey J HilmasPatrick T Williams

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