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In order to clarify the interrelationships between hemodynamic changes and pharmacokinetics following oral administration of a single dose of nifedipine (5 and 10 mg capsules), blood pressure (BP), heart rate (HR) and plasma concentration of nifedipine were measured in 5 healthy volunteers (NT) and in 5 patients with essential hypertension (EHT).<BR>Acute oral administration of nifedipine caused a rapid dose dependent reduction of BP in EHT, whereas no significant fall of BP was found in NT. No significant change of HR after nifedipine administration was observed in both EHT and NT. The results may suggest that the BP reduction is caused mainly by an attenuated sensitivity of the baroreceptor mechanism in EHT.<BR>Plasma concentration of nifedipine promptly rose reaching the maximum level after .1 hour in both groups. The mean value of maximum plasma concentration in healthy volunteers was 55.4 ng/ml receiving 5 mg nifedipine and 124.5 ng/ml receiving 10 mg nifedipine respectively. 67.1 ng/ml and 132.4 ng/ml in EHT was measured after 5 mg and 10 mg. No significant difference of the maximum plasma concentrations in nifedipine or other pharmacokinetic parameters was observed between the two groups.<BR>The minimum plasma concentration of nifedipine required for an effective BP fall (over 13 mmHg reduction in mean arterial pressure) in EHT is about 12 ng/ml and this hypotensive effect lasted 6 hours after the administration of 10 mg nifedipine.<BR>These findings indicate that nifedipine is effective in lowering BP without an increase of HR in EHT, and also suggest that effective plasma concentration of nifedipine may be about 12 ng/ml.
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