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Single intravenous dose and steady-state oral dose pharmacokinetics of nicardipine in healthy subjects

✍ Scribed by John G. Wagner; Teck L. Ling; Edward J. Mroszczak; Donna Freedman; Ann Wu; Bee Huang; Ian J. Massey; Robert R. Roe

Publisher: John Wiley and Sons
Year: 1987
Tongue: English
Weight: 617 KB
Volume: 8
Category: Article
ISSN: 0142-2782
DOI: 10.1002/bdd.2510080205

No coin nor oath required. For personal study only.

✦ Synopsis

Nicardipine HCI oral doses (10-40 mg) were administered sequentially to six healthy subjects. For each regimen the capsule dose was administered every 8 hours (q 8 h) for 3 days and the plasma profiles of nicardipine and its pyridine analogue (M5) were determined following the last dose on day 4. Steady-state plasma concentrations of nicardipine for each subject were fitted very well by the Michaelis-Menten equation. An intravenous tracer dose (0.885 mg nicardipine HCI) was administered simultaneously with the final oral dose on the fourth day of the 30 mg q 8 h regimen. The steady-state bioavailability of nicardipine was shown to be dose-dependent and averaged 19 per cent (10 mg), 22 per cent (20 mg), 28 per cent (30 mg), and 38 per cent (40 mg). Nicardipine undergoes linear first-pass metabolism to M5. Qther metabolic pathways are responsible for the saturable first-pass metabolism observed for nicardipine.

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