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Lack of relationship between quinidine pharmacokinetics and the sparteine oxidation polymorphism.

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.

journal_name

Eur J Clin Pharmacol

journal_title

European journal of clinical pharmacology

authors

Nielsen F,Rosholm JU,Brøsen K

doi

10.1007/BF00194341

subject

Has Abstract

pub_date

1995-01-01 00:00:00

pages

501-4

issue

6

eissn

0031-6970

issn

1432-1041

journal_volume

48

pub_type

临床试验,杂志文章

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