Acute and long-term hypotensive effects and plasma concentrations of nifedipine in patients with essential hypertension.

The acute and long-term hypotensive effects of low doses of nifedipine, and the correlation between the fall in the blood pressure (BP) and the plasma nifedipine concentration, were investigated in patients with essential hypertension. The oral administration of nifedipine 5 mg rapidly decreased BP from 163 +/- 22/101 +/- 10 to 127 +/- 12/82 +/- 9 mmHg (mean +/- SD; p less than 0.001), and increased heart rate from 72 +/- 8 to 76 +/- 6 beats/min (p less than 0.05), plasma renin activity rose from 1.2 +/- 0.6 to 1.4 +/- 0.8 ng/ml/h (p less than 0.05), and plasma nifedipine concentration was 75.6 +/- 22.0 ng/ml 30 min after administration (n = 7). The nifedipine concentration was significantly correlated both with the fall in BP (r = 0.410, p less than 0.02, n = 31) and the rise in the heart rate (r = 0.412, p less than 0.02, n = 31). Treatment with nifedipine 5 mg t.d.s. alone or in combination either with propranolol 10 mg t.d.s., or thiazide 1 tablet daily, or propranolol and thiazide, controlled BP in 36 patients during the 22 week study period. During the long-term nifedipine therapy, the plasma nifedipine level was significantly correlated with the fall in systolic (r = 0.577, p less than 0.01, n = 20) and diastolic (r = 0.595, p less than 0.01, n = 20) BP. It was concluded that the plasma nifedipine concentration could be correlated with the fall in BP, and that low doses of nifedipine, either as monotherapy or in combination, were effective in the acute and long-term treatment of patients with essential hypertension.