Dynamics of beta-adrenoceptor blockade with cetamolol.
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.
Coelho
J
J
Schnelle
K
K
Joubert
L
L
Ventura
D
D
Mullane
J
J
D000081:Acetamides / Q000097:blood / Q000494:pharmacology*; D000293:Adolescent; D000319:Adrenergic beta-Antagonists; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D004311:Double-Blind Method; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D005082:Physical Exertion; D011869:Radioligand Assay
D000081:Acetamides; D000319:Adrenergic beta-Antagonists; C038931:cetamolol