Rectal Administration of Nifedipine: Haemodynamic Effects and Pharmacokinetics in Hypertensives

Abstract

The haemodynamic effects and pharmacokinetics of nifedipine suppositories, used mainly for hypertensive emergencies, were studied in 10 severely hypertensive patients. Following rectal administration, significant hypotensive effects occurred after 0.5 h and lasted until 7 h after administration. The mean (±SE) maximum decreases in systolic and diastolic blood pressures 1.5 h after administration were: systolic, 61.8 ± 7.9 mmHg (P<0.001); and diastolic, 30.8 ± 4.0 mmHg (P<0.001). No serious side-effects were reported and heart rate did not change significantly. Mean nifedipine concentration in the blood peaked at 52.4 ng/ml, 1 h after administration and, after 7 h, was still 14.3 ng/ml which is higher than the minimum plasma concentration required for hypotensive effects to occur. There was a close correlation between nifedipine concentration in the blood and hypotensive effects. These results indicate that rectal administration of nifedipine should be regarded as a useful alternative treatment in hypertensive emergencies.