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. 1989 Sep;28(3):362-5.
doi: 10.1111/j.1365-2125.1989.tb05439.x.

Calcium channel antagonists and cyclosporine metabolism: in vitro studies with human liver microsomes

J F Tjia  1 , D J Back, A M Breckenridge
Affiliations

Calcium channel antagonists and cyclosporine metabolism: in vitro studies with human liver microsomes

J F Tjia et al. Br J Clin Pharmacol. 1989 Sep.

Abstract

The effects of four Ca2+ channel antagonists on the metabolism of cyclosporine (CsA) by human liver microsomes (n = 4) in vitro have been examined. Nicardipine produced marked inhibition of both M17 and M21 (IC50 = 7.0 microM) formation. In contrast nifedipine produced less than 20% inhibition of M17 and M21 even at the highest concentration examined (50 microM). Diltiazem data were comparable to those for nifedipine. Verapamil (50 microM) produced 30 and 28% inhibition of M17 and M21 formation, respectively. These findings give a basis to the increase in CsA blood concentrations seen in transplant patients who are also given nicardipine.

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