EFFECT OF CELIPROLOL ON HEMODYNAMICS DURING EXERCISE LOADING AND THE RESPONSES CAUSED BY SYMPATHOMIMETIC DRUGS IN ESSENTIAL-HYPERTENSION

Celiprolol is a beta1-selective beta-adrenoreceptor antagonist with intrinsic sympathomimetic activity. The hemodynamic effects of celiprolol during exercise loading as well as responses to adrenergic drugs (norepinephrine and isoproterenol) and changes in body position (electric tilt table) were investigated in nine patients with mild to moderate essential hypertension. Patients were treated with celiprolol 200 mg once daily for 4 to 6 weeks, followed by 400 mg for 12 to 14 weeks. Hemodynamics during exercise loading were measured in the supine position using a bicycle ergometer with a constant load of 1.25 W/kg for 6 minutes. Celiprolol significantly reduced the increase in blood pressure and heart rate associated with exercise loading, but the reduction in the increase in cardiac output was not significant. Total peripheral resistance did not change significantly during exercise loading. Celiprolol did not affect the increase in blood pressure caused by norepinephrine, but the increase in systolic blood pressure and heart rate caused by isoproterenol was significantly suppressed. Celiprolol had no apparent effect on the blood pressure and heart rate response caused by standing. The results of this study suggest that the hemodynamic mechanism for the hypotensive effect of celiprolol is different during the effort and resting states and that celiprolol is a unique beta-adrenoreceptor antagonist.