Intravenous diltiazem and CYP3A-mediated metabolism

A. L. Masica, N. E. Azie, D. C. Brater, S. D. Hall, D. R. Jones

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Aims: To study whether intravenous diltiazem, a calcium channel blocker commonly prescribed for hypertension and stable angina, is an inhibitor of the CYP3A enzymes by using oral lovastatin, an HMG Co-A reductase inhibitor, as a substrate. Methods: Ten healthy volunteers were studied in a randomized two-way crossover design. The two arms were 1) administration of a 20 mg dosage of lovastatin orally and 2) administration of a 20 mg dosage of lovastatin orally 1 h after an intravenous loading dosage and constant infusion of diltiazem. Blood samples were collected up to 25 h in order to quantify lovastatin and diltiazem concentrations in the separated serum. Lovastatin and diltiazem concentrations were quantified by GC-MS and h.p.l.c., respectively. Results: Intravenous diltiazem did not significantly affect the oral AUC, C(max), t( 1/2 ) or t(max) of lovastatin. Conclusions: These data suggest that the interaction of lovastatin with diltiazem does not occur systemically and is primarily a first-pass effect. Thus, drug interactions with diltiazem may become evident when a patient is moved from intravenous to oral dosing.

Original languageEnglish
Pages (from-to)273-276
Number of pages4
JournalBritish Journal of Clinical Pharmacology
Volume50
Issue number3
DOIs
StatePublished - 2000

Fingerprint

Cytochrome P-450 CYP3A
Lovastatin
Diltiazem
Stable Angina
Calcium Channel Blockers
Enzyme Inhibitors
Drug Interactions
Cross-Over Studies
Area Under Curve
Healthy Volunteers
Oxidoreductases
Hypertension
Serum

Keywords

  • Calcium channel blockers
  • CYP3A
  • Diltiazem
  • Drug interactions
  • Lovastatin

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Masica, A. L., Azie, N. E., Brater, D. C., Hall, S. D., & Jones, D. R. (2000). Intravenous diltiazem and CYP3A-mediated metabolism. British Journal of Clinical Pharmacology, 50(3), 273-276. https://doi.org/10.1046/j.1365-2125.2000.00249.x

Intravenous diltiazem and CYP3A-mediated metabolism. / Masica, A. L.; Azie, N. E.; Brater, D. C.; Hall, S. D.; Jones, D. R.

In: British Journal of Clinical Pharmacology, Vol. 50, No. 3, 2000, p. 273-276.

Research output: Contribution to journalArticle

Masica, AL, Azie, NE, Brater, DC, Hall, SD & Jones, DR 2000, 'Intravenous diltiazem and CYP3A-mediated metabolism', British Journal of Clinical Pharmacology, vol. 50, no. 3, pp. 273-276. https://doi.org/10.1046/j.1365-2125.2000.00249.x
Masica, A. L. ; Azie, N. E. ; Brater, D. C. ; Hall, S. D. ; Jones, D. R. / Intravenous diltiazem and CYP3A-mediated metabolism. In: British Journal of Clinical Pharmacology. 2000 ; Vol. 50, No. 3. pp. 273-276.
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