Effect of different durations and formulations of diltiazem on the single-dose pharmacokinetics of midazolam: How long do we go?

Journal of Clinical Pharmacology

Volumn 51, Issue 11, 2011, Pages 1561-1570

  Friedman, Evan J ^a   Fraser, Iain P ^a   Wang, Ying Hong ^a   Bergman, Arthur J ^a   Li, Chi Chung ^a   Larson, Patrick J ^a   Chodakewitz, Jeffrey ^a   Wagner, John A ^a   Stoch, S Aubrey ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

cytochrome P450 3A; diltiazem; drug drug interactions; Midazolam; Simcyp

Indexed keywords

CYTOCHROME P450 3A; DILTIAZEM; KETOCONAZOLE; MIDAZOLAM;

ADULT; AREA UNDER THE CURVE; ARTICLE; COMPUTER PROGRAM; CONVENTIONAL RELEASE FORMULATION; DIZZINESS; DRUG BLOOD LEVEL; DRUG DEGRADATION; DRUG FORMULATION; EXTENDED RELEASE FORMULATION; FEMALE; FEVER; HUMAN; HUMAN EXPERIMENT; LETHARGY; MALE; NORMAL HUMAN; PAIN; SINGLE DRUG DOSE; TREATMENT DURATION; VOMITING;

ADULT; AREA UNDER CURVE; CHEMISTRY, PHARMACEUTICAL; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP3A; DILTIAZEM; DRUG INTERACTIONS; FEMALE; HUMANS; KETOCONAZOLE; MALE; MIDAZOLAM; MIDDLE AGED; SENSITIVITY AND SPECIFICITY; YOUNG ADULT;

EID: 80054751099     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270010387141     Document Type: Article

References (20)

1. Böttiger Y, Säwe J, Brattström C, Tollemar J, Burke JT, Häss G, et al. Pharmacokinetic interaction between single oral doses of diltiazem and sirolimus in healthy volunteers. Clin Pharmacol Ther. 2001 ; 69: 32-40 (Pubitemid 32108669)
2. Lamberg TS, Kivisto KT, Nuevonen PJ. Effects of verapamil and diltiazem on the pharmacokinetics of buspirone. Clin Pharmacol Ther. 1998 ; 63: 640-645 (Pubitemid 28327891)
3. Backman JT, Olkkola KT, Aranko K, Himberg JJ, Neuvonen PJ. Dose of midazolam should be reduced during diltiazem and verapamil treatments. Br J Clin Pharmacol. 1994 ; 37: 221-225 (Pubitemid 24212179)
4. Stoch SA, Friedman E, Maes A, Yee K, Xu Y, Larson P, et al. Effect of different durations of ketoconazole dosing on the single-dose pharmacokinetics of midazolam: shortening the paradigm. J Clin Pharmacol. 2009 ; 49: 398-406
5. Jamei M, Marciniak S, Feng K, Barnett A, Tucker G, Rostami-Hodjegan A. The Simcyp population-based ADME simulator. Expert Opin Drug Metab Toxicol. 2009 ; 5: 211-223
6. Ochs HR, Knuchel M. Pharmacokinetics and absolute bioavailability of diltiazem in humans. Klin Wochenschr. 1994 ; 62: 303-306
7. Wang Y-H. Confidence assessment of the Simcyp time-based approach and a static mathematic model in predicting clinical drug-drug interactions for mechanism-based CYP3A inhibitors. Drug Metab Dispos. 2010 ; 38: 1094-1104
8. Robbins-Weilert DK, Giesing DH, Weir SJ. Steady-state pharmacokinetics of high-dose diltiazem hydrochloride (Cardizem CD) administered once daily in healthy volunteers. Am J Ther. 1999 ; 6: 211-216 (Pubitemid 29342880)
9. Zhou S, Yung Chan S, Cher Goh B, Chan E, Duan W, et al. Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs. Clin Pharmacokinet. 2005 ; 44: 279-304 (Pubitemid 40477790)
10. Guidance for Industry: Drug Interaction Studies-Study Design, Data Analysis, and Implications for Dosing and Labeling. Rockville, MD: US Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER), Center for Biologics Evaluation and Research (CBER) ; 2006 :
11. Jones DR, Gorski JC, Hamman MA, Mayhew BS, Rider S, Hall SD. Diltiazem inhibition of cytochrome P-450 3A activity is due to metabolite intermediate complex formation. J Pharmacol Exp Ther. 1999 ; 290: 1116-1125 (Pubitemid 29400251)
12. Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, et al. The conduct of in vitro and in vivo drug-drug interaction studies: a PhRMA perspective. J Clin Pharmacol. 2003 ; 43: 443-469 (Pubitemid 36506147)
13. Chen M, Nafziger AN, Bertino JS. Drug-metabolizing enzyme inhibition by ketoconazole does not reduce interindividual variability of CYP3A activity as measured by oral midazolam. Drug Metab Dispos. 2006 ; 34: 2079-2082 (Pubitemid 44837769)
14. Cranbury, NJ: Kos Pharmaceuticals ; 2006 :
15. Venkatakrishnan K, Obach RS, Rostami-Hodjegan A. Mechanism-based inactivation of human cytochrome P450 enzymes: strategies for diagnosis and drug-drug interaction risk assessment. Xenobiotica. 2007 ; 37: 1225-1256 (Pubitemid 350035532)
16. Thummel KE, O'Shea D, Paine MF, Shen DD, Kunze KL, Perkins JD, et al. Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism. Clin Pharmacol Ther. 1996 ; 49: 491-502 (Pubitemid 26193889)
17. Masica AL, Mayo G, Wilkinson GR. In vivo comparison of constitutive cytochrome P450 3A activity assessed by alprazolam, triazolam, and midazolam. Clin Pharmacol Ther. 2004 ; 76: 341-349 (Pubitemid 39313124)
18. Gorski JC, Jones DR, Haehner-Daniels BD, Hamman MA, O'Mara EM, Hall SD. The contribution of intestinal and hepatic CYP3A to the interaction between midazolam and clarithromycin. Clin Pharmacol Ther. 1998 ; 64: 133-143 (Pubitemid 28423848)
19. Wang Y-H, Gorski JC, Hamman MA, Hall SD. Age and sex effect on duration of CYP3A inhibition by clarithromycin. Meeting abstract: 7th International ISSX meeting. Drug Metab Rev. 2004 ; 36 (suppl 1). 287
20. Yang J, Liao M, Shou M, Jamei M, Yeo KR, Tucker GT, et al. Cytochrome p450 turnover: regulation of synthesis and degradation, methods for determining rates, and implications for the prediction of drug interactions. Curr Drug Metab. 2008 ; 9: 384-394