Affiliation:
1. Department of Chemistry, Government College University Lahore, Lahore, Pakistan
2. Department of Pharmacy,
Lahore College of Women University, Lahore, Pakistan
3. Punjab University College of Pharmacy, University of the
Punjab, Lahore, Pakistan
Abstract
Background:
Warfarin (WAR) is an anticoagulant with a narrow therapeutic index and
is principally metabolized by CYP3A4 and CYP2C9 enzymes. The inhibitors of these enzymes
may alter the systemic exposure to WAR. Quercetin (QUE), a bioflavonoid, may modify the bioavailability
of drugs used concurrently by inhibiting CYP3A4, CYP2C8, CYP2C9, CYP1A2, and Pglycoprotein
(P-gp).
Objective:
The current study scrutinized the influence of QUE on WAR pharmacokinetics in rats.
Method:
QUE was orally administered to animals for 14 consecutive days, followed by WAR as a
single oral dose on the 15th day in the pre-treatment group. The co-administration group received a
single dose of QUE and WAR concomitantly. Only carboxymethylcellulose (CMC) 0.5% was administered
as a vehicle to control group.
Result:
In the pre-treated group, WAR’s Cmax was increased by 30.43%, AUC0-∞ by 62.94%, and t1/2 by
10.54%, while Cl decreased by 41.35%, relative to control. In co-administered animals, WAR’s Cmax increased
by 10.98%, AUC0-∞ by 20.20%, and t1/2 by 8.87%, while Cl declined by 16.40%.
Conclusion:
QUE alters the pharmacokinetics of WAR, warranting possibly WAR dose adjustment
after confirmatory clinical investigations, specifically in patients with thrombotic disorders
and a pre-treatment history of QUE or its product.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology (medical),Pharmacology,Toxicology
Cited by
2 articles.
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