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Dynamics of beta‐adrenoceptor blockade with cetamolol.
Author(s) -
Coelho J,
Schnelle K,
Joubert L,
Ventura D,
Mullane J
Publication year - 1985
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1985.tb02663.x
Subject(s) - blockade , beta (programming language) , crossover study , blood pressure , partial agonist , pharmacology , agonist , medicine , endocrinology , receptor , alternative medicine , pathology , computer science , programming language , placebo
Cetamolol is a new beta‐adrenoceptor blocking agent shown in animals to have moderate beta 1‐adrenoceptor selectivity and partial agonist activity. In healthy normal volunteers, beta 1‐adrenoceptor blockade was measured as the reduction of exercise‐induced tachycardia, systolic blood pressure, and double product at 2, 8, and 24 h after a single oral dose of 10, 25, and 50 mg cetamolol. beta 1‐adrenoceptor blockade was significantly linearly related to log serum cetamolol level, was maximal at 2 h, and was still clinically significant at 24 h. A crossover study of single 0, 10, and 25 mg doses confirmed these findings.