Lack of relationship between quinidine pharmacokinetics and the sparteine oxidation polymorphism

European Journal of Clinical Pharmacology
F NielsenK Brøsen

Abstract

Quinidine is a very potent inhibitor of CYP2D6, but the role of the enzyme in the biotransformation of quinidine has only been investigated in a single in vitro study and in two small in vivo experiments, with contradictory results. The present investigation was designed to present definite evaluation of whether quinidine is metabolised by CYP2D6. Eight poor metabolizers (PM) and 8 extensive metabolizers (EM) of sparteine each took one oral dose of 200 mg quinidine. In the EM, the total clearance, the clearance via 3-hydroxylation and the clearance via N-oxidation, were 33, 3.7 and 0.23 l.h-1, respectively. In the PM, the corresponding values were 29, 3.1 and 0.18 l.h-1, respectively. There were no statistically significant differences between EM and PM in any of these pharmacokinetic parameters. It is concluded that CYP2D6 is not an important enzyme for the oxidation of quinidine.

Citations

Dec 9, 1997·Clinical Pharmacology and Therapeutics·K M KaukonenP J Neuvonen
Jan 1, 1999·Clinical Pharmacology and Therapeutics·T HeiskanenE Kalso
Jul 4, 2001·Clinical Pharmacokinetics·P T Giao, P J de Vries
May 25, 2012·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Howard J BurtAleksandra Galetin
Feb 15, 2000·British Journal of Clinical Pharmacology·P DalénL Bertilsson

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