Prizidilol, an antihypertensive with precapillary vasodilator and β-adrenoceptor blocking actions, in primary hypertension

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Abstract
Single oral doses of 1.5, 3.0, 4.5 and 6.0 mg/kg prizidilol HCl (SK&F 92657, dl-3[2-(3-tert-butylamino-2-hydroxy-propoxy)phenyl]6-hydrazinopyridazine hydrochloride) an antihypertensive with vasodilator and .beta.-adrenoceptor blocking actions, were given to 12 patients with primary hypertension on separate days. Systolic and diastolic blood pressure (BP) decreased after 4.5 and 6.0 mg/kg and systolic BP also after 3.0 mg/kg. The antihypertensive effect was evident in 1-2 h with maximum effect in 4-5 h (supine systolic BP 20 and diastolic 13 mm Hg after 6.0 mg/kg); the effect was sustained for > 8 h. An initial slight reduction in heart rate (HR) after 1-2 h was followed by a slight rise after 6-8 h. There were higher plasma drug levels and greater antihypertensive effects after the 6.0 mg/kg dose in slow acetylators (n = 5) than in rapid acetylators (n = 7). Due to its hydrazine moiety, prizidilol, like hydralazine, seems to be a substrate for the polymorphic N-acetyltransferase enzyme system.

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