PharmPK Discussion - Diltiazem - a substrate of OATP

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On 20 Mar 2006 at 15:38:14, "Saiprasad Boddu" (saiprasadb.-at-.glenmarkpharma.com) sent the message


The following message was posted to: PharmPK

Hello,
I am doing a project on Diltiazem. I am not getting
information whether Diltiazem is a substrate of OATP (organic anion
transporting polypeptide).
Please cite me the articles also.
Thank you,
Saiprasad b

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On 20 Mar 2006 at 13:15:36, "Louis Ptak" (lptak.-at-.pharmresource.com) sent the message


The following message was posted to: PharmPK

Dear Saliprasad,
Here is an article I found using Google [use 'Diltiazem OATP' - db].
Hope this helps.

DOI:10.1111/j.1365-2125.2006.02613.x
British Journal of Clinical Pharmacology

Effects of itraconazole and diltiazem on the pharmacokinetics of
fexofenadine, a substrate of  P-glycoprotein

Mikiko Shimizu, 1 Tsukasa Uno, 1 Kazunobu Sugawara 2 & Tomonori
Tateishi 1
1 Department of Clinical Pharmacology, Hirosaki University School of
Medicine and
2 Department of Pharmacy, Hirosaki University Hospital, Hirosaki, Japan

Here is another article.  Michael D. Perloff, Lisa L. von Moltke,
Michael H. Court, Tsutomu Kotegawa, Richard I. Shader, and David J.
Greenblatt
Midazolam and Triazolam Biotransformation in Mouse and Human Liver
Microsomes: Relative Contribution of CYP3A and CYP2C Isoforms
J Pharmacol Exp Ther 2000 292: 618-628. [Abstract] [Full Text] [PDF]

And Life-Threatening Interaction of Mibefradil and -Blockers With
Dihydropyridine Calcium Channel Blockers
Michael E. Mullins, MD; B. Zane Horowitz, MD; Dennis H. J. Linden, MD;
Gregory W. Smith, RPh; Robert L. Norton, MD; Jack Stump, MD

JAMA. 1998;280:157-158.

Mibefradil is a T-type and L-type calcium channel blocker (CCB) released
in the United States in 1997 for management of hypertension and chronic
stable angina. Postmarketing surveillance revealed a potential serious
interaction between mibefradil and -blockers, digoxin, verapamil, and
diltiazem, especially in elderly patients. The manufacturer voluntarily
withdrew mibefradil on June 8, 1998. We describe 4 cases of cardiogenic
shock in patients taking mibefradil and -blockers who began taking
dihydropyridine CCBs. One case resulted in death; the other 3 survived
episodes of cardiogenic shock with intensive support of heart rate and
blood pressure. Physicians who are preparing to switch patients'
medications from mibefradil to other antihypertensive agents should be
aware of these potentially life-threatening drug-drug interactions.

Regards,

Louis Ptak

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