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A review of the human metabolism and pharmacokinetics of nicardipine hydrochloride
Author(s) -
DOW R. J.,
GRAHAM D. J. M.
Publication year - 1986
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1986.tb00322.x
Subject(s) - nicardipine , pharmacokinetics , bioavailability , pharmacology , first pass effect , oral administration , dosing , medicine , half life , chemistry , calcium
1 A series of studies has been conducted to investigate the disposition of nicardipine following oral and intravenous administration to human subjects. 2 Nicardipine is rapidly absorbed, rapidly and extensively metabolised and rapidly eliminated from plasma. 3 Nicardipine is subject to extensive pre‐systemic elimination. This is partially saturable by increasing dose or duration of dosing. 4 Because of nicardipine's saturable pre‐systemic elimination, steady‐state plasma levels and bioavailability show a non‐linear relationship with dose over the range 10 to 40 mg three times daily. 5 On repeated oral administration steady‐state levels are apparently achieved within 3 days without subsequent change. This is consistent with the measured terminal elimination half‐life of 11.8 h, and a demonstrated absence of effect on hepatic microsomal enzyme systems. 6 Consumption of food before nicardipine administration reduces its bioavailability. 7 Studies in the elderly have demonstrated that increased hypotensive effects with age cannot be attributed to pharmacokinetic changes. 8 Studies in renally impaired subjects have demonstrated that dosage at the lower end of the recommended range is appropriate.