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Hi:
I would appreciate to receive information on which CYP450 isoenzymes are
repsonsible for the metabolism of glyburide and glipizide in humans. I
have searcheed the Medlin with very little information. thank you.
Poe-Hirr Hsyu
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Please read our paper in PHARMACOGENETICS, 9:71-80 (1999).
"Pharmacokinetics of chlorpheniramine, phenytoin, glipizide and nifedipine
in an individual homozygous for CYP2C9*3 allele"
Arthur B. Straughn
UT Memphis College of Pharmacy
EMAIL ASTRAUGHN.aaa.UTMEM.EDU
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[Two replies - db]
From: "HILBERT, JAMES "
To: "'PharmPK.at.pharm.cpb.uokhsc.edu'"
Subject: RE: PharmPK metabolism of glyburide and glipizide
Date: Mon, 5 Apr 1999 10:23:11 -0400
MIME-Version: 1.0
Try http://www.dml.georgetown.edu/depts/pharmacology/davetab.html
Jim Hilbert
Pfizer, Inc.
mailto: james_hilbert.-a-.groton.pfizer.com
---
Date: Mon, 05 Apr 1999 16:01:23 -0500
From: "Charlie Fisher, Ph.D."
Reply-To: cfisher.at.cortex.ama.ttuhsc.edu
Organization: Texas Tech Health Science Center School of Pharmacy
X-Accept-Language: en
MIME-Version: 1.0
To: PharmPK.-at-.pharm.cpb.uokhsc.edu
Subject: Re: PharmPK metabolism of glyburide and glipizide
Glibenclamide is excreted in the urine as trans-4- and
cis-3-hydroxyglibenclamide. 36 +/- 6% of the given dose of glibenclamide was
excreted in 48 h urine as hydroxylated metabolites, 27 +/- 4% as
trans-4-hydroxyglibenclamide and 8+/- 2% as cis-3-hydroxyglibenclamide (1)
It is apparently not metabolized by CYP2D6 or CYP2C19 since there is a lack
of association with the debrisoquine and mephenytoin phenotypes (1). The
unimodal distribution of metabolism also suggests that CYP2C9 is not involved
as it is with tolbutamide (2). Drug-drug interactions with cyclosporin
metabolism suggest it may be metabolized by CYP3A4 (3).
(1) Br J Clin Pharmacol 1990 Sep;30(3):476-80 Lack of relationship between
glibenclamide metabolism and debrisoquine or mephenytoin hydroxylation
phenotypes. Dahl-Puustinen ML, Alm C, Bertilsson L, Christenson I, Ostman J,
Thunberg E, Wikstrom I
(2) Arzneimittelforschung 1989 Nov;39(11):1449-50 Uniform elimination pattern
for glibenclamide in healthy Caucasian males. Spraul M, Streeck A, Nieradzik,
M, Berger M
(3) Ther Drug Monit 1996 Oct;18(5):624-6 Possible interaction between
cyclosporine and glibenclamide in posttransplant diabetic patients. Islam SI,
Masuda QN, Bolaji OO, Shaheen FM,
Sheikh IA
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Copyright 1995-2010 David W. A. Bourne (david@boomer.org)