The safety and efficacy of orally administered
celiprolol, a new beta 1-selective
adrenergic blocking
drug with peripheral beta 2-agonist properties, were assessed in 91 patients with mild to moderate systemic
hypertension (supine diastolic blood pressure [BP] 95 to 114 mm Hg without medication) using a placebo-controlled, double-blind, randomized, titration-to-effect study design. All patients received placebo for 4 weeks and were then randomized to receive placebo (n = 46) or once-daily
celiprolol (n = 45), which was titrated every 2 weeks (200, 400, 600 mg/day) over a 6-week period to achieve a reduction in supine diastolic BP to less than or equal to 90 mm Hg. Plasma
lipids and
lipoproteins were also assessed at baseline, during placebo and after randomization to active
therapy in a subgroup of patients. Compared with placebo,
celiprolol reduced supine and standing BP (reduction of supine BP -0.4/-2.1 mm Hg with placebo, -5.7/-6.4 with
celiprolol, p less than 0.05; reduction of standing BP -1.7/-1.0 with placebo, -7.2/-4.9 with
celiprolol, p less than 0.05). Supine heart rate was reduced by 6.8 beats/min with
celiprolol compared with 2.0 beats/min with placebo (p less than 0.05). No differences were seen when the effects of placebo and
celiprolol on plasma
lipoproteins were compared.
Celiprolol is a safe, effective and well tolerated once-daily
antihypertensive drug and has no detrimental effects on plasma
lipids.