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Single intravenous dose and steady‐state oral dose pharmacokinetics of nicardipine in healthy subjects
Author(s) -
Wagner John G.,
Ling Teck L.,
Mroszczak Edward J.,
Freedman Donna,
Wu Ann,
Huang Bee,
Massey Ian J.,
Roe Robert R.
Publication year - 1987
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510080205
Subject(s) - nicardipine , pharmacokinetics , bioavailability , oral administration , pharmacology , steady state (chemistry) , oral dose , first pass effect , medicine , regimen , anesthesia , chemistry , calcium
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.