Nicardipine: pharmacokinetics and effects on carotid and brachial blood flows in normal volunteers.
The effects of nicardipine, 20 mg, three times daily, nicardipine slow release, 30 mg, twice daily and a placebo on brachial and carotid arteries diameters and flows have been investigated by the pulsed Doppler technique during a single blind and cross-over study performed in six healthy volunteers. Simultaneously, nicardipine plasma levels and relative bioavailability were determined. Nicardipine significantly increased brachial and carotid arteries diameters (by 16 and 10% respectively) and flows (by 60 and 35% respectively). These effects peaked after 4 h and lasted no longer than 6 h. Forearm vascular resistance was significantly decreased. Hence nicardipine dilated both large and small arteries. Nicardipine slow release elicited the same effects on brachial and carotid arteries diameters and flows as nicardipine. These effects peaked at 6 h and lasted up to 10 h. Although the profiles of the pharmacodynamic effects and of the kinetics of nicardipine were almost parallel in each individual after administration of both nicardipine formulations, there was no correlation between the nicardipine plasma relative bioavailability and its effects on brachial and carotid arteries blood flows when considering all subjects together.
D000328:Adult; D000450:Aldosterone / Q000097:blood; D001916:Brachial Artery / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000378:metabolism / Q000494:pharmacology*; D002339:Carotid Arteries / Q000187:drug effects; D004837:Epinephrine / Q000097:blood; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D009529:Nicardipine; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D009638:Norepinephrine / Q000097:blood; D011863:Radioimmunoassay / Q000379:methods; D012039:Regional Blood Flow / Q000187:drug effects*; D012083:Renin / Q000097:blood
D002121:Calcium Channel Blockers; D000450:Aldosterone; D009529:Nicardipine; D012083:Renin; D009543:Nifedipine; D009638:Norepinephrine; D004837:Epinephrine