Effects of celiprolol on plasma renin, aldosterone, norepinephrine and epinephrine in primary hypertension

Celiprolol is a newly developed cardioselective β-blocking agent with mild β 2-agonist and weak α 2-antagonist properties. To evaluate the acute (2.5 hours) and chronic (2 weeks) effects of celiprolol (400 mg once a day) on plasma renin, aldosterone, norepinephrine and epinephrine, 20 patients with mild to moderate primary hypertension were studied in a double-blind placebo-controlled crossover trial. Two and one-half hours after the first dose of both placebo and celiprolol, supine and standing measurements of blood pressure showed a significant reduction, whereas plasma norepinephrine increases were comparable with baseline values. Placebo and celiprolol produced similar changes on supine blood pressure and plasma norepinephrine. In 9 patients celiprolol decreased plasma renin (from a mean ± standard deviation of 1.09 ± 0.35 to 0.77 ± 0.52 ng/ml/hr, p < 0.05) and aldosterone (from 9.2 ± 3.7 to 6.7 ± 3.9 ng/dl, p < 0.05) acutely both supine and standing, but placebo did not change these parameters. Celiprolol increased pulse rate supine (but not standing) as compared with baseline values. After 2 weeks of celiprolol therapy, blood pressure was decreased both supine and standing compared with placebo in 18 patients (140 ± 18/88 ± 8 vs 149 ± 18/94 ± 7, 136 ± 18/ 91 ± 6 vs 142 ± 20/97 ± 9 mm Hg, respectively, each p < 0.05), without a change of pulse rate when supine and with a reduction when standing. There were no significant changes of plasma renin, aldosterone, norepinephrine and epinephrine levels during chronic therapy compared with placebo.