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Prizidilol, an antihypertensive with precapillary vasodilator and β‐adrenoceptor blocking actions, in primary hypertension
Author(s) -
Larsson R,
Karlberg B E,
Norlander B,
Wirsén A
Publication year - 1981
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1981.82
Subject(s) - hydralazine , blood pressure , vasodilation , medicine , heart rate , antihypertensive drug , diastole , pharmacology , supine position , endocrinology , cardiology
Single oral doses of 1.5, 3.0, 4.5, and 6.0 mg/kg prizidilol HCl, an antihypertensive with vasodilator and β‐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 to 2 hr with maximum effect in 4 to 5 hr (supine systolic BP 20 and diastolic 13 mm H g after 6.0 mg/kg); the effect was sustained for more than 8 hr. An initial slight reduction in heart rate (HR) after 1 to 2 hr was followed by a slight rise after 6 to 8 hr. 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. Clinical Pharmacology and Therapeutics (1981) 29, 588–593; doi: 10.1038/clpt.1981.82