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

Nicardipine HCl 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. St...

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Bibliographic Details
Published in:Biopharmaceutics & drug disposition Vol. 8; no. 2; p. 133
Main Authors: Wagner, J G, Ling, T L, Mroszczak, E J, Freedman, D, Wu, A, Huang, B, Massey, I J, Roe, R R
Format: Journal Article
Language:English
Published: England 01-03-1987
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Summary:Nicardipine HCl 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 HCl) 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. Other metabolic pathways are responsible for the saturable first-pass metabolism observed for nicardipine.
ISSN:0142-2782
DOI:10.1002/bdd.2510080205