Dynamics of beta-adrenoceptor blockade with cetamolol.

Abstract

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.

• Authors: J Coelho, K Schnelle, L Joubert, D Ventura, J Mullane
• Journal: British journal of clinical pharmacology (Br J Clin Pharmacol) Vol. 19 Issue 4 Pg. 411-6 (Apr 1985) ISSN: 0306-5251 [Print] England
• PMID: 2859872 (Publication Type: Journal Article)

Chemical References

• Acetamides
• Adrenergic beta-Antagonists
• cetamolol

Topics

• Acetamides (blood, pharmacology)
• Adolescent
• Adrenergic beta-Antagonists
• Adult
• Blood Pressure (drug effects)
• Double-Blind Method
• Heart Rate (drug effects)
• Humans
• Male
• Physical Exertion
• Radioligand Assay