Portal de Periódicos da CAPES

Improved left ventricular function during exercise: A comparison of celiprolol and atenolol

1988; Elsevier BV; Volume: 116; Issue: 5 Linguagem: Inglês

10.1016/0002-8703(88)90136-6

1097-6744

James M. McLenachan, John T. Wilson, Henry Dargie,

Pharmacological Effects and Assays

The clinical pharmacology of β-adrenoceptor blockers is summarized. They have a variety of pharmacological actions on the β-adrenoceptors. For example, propranolol is a nonselective β-blocker with antagonist effects on both β1 and β2 receptors, atenolol is a selective β1-antagonist, and celiprolol is a selective β1-antagonist, partial β2-agonist. β1-Receptor blockade tends to reduce heart rate, cardiac output, and arterial pressure while increasing peripheral vascular resistance, whereas β2-receptor blockade tends to be disadvantageous in causing bronchoconstriction and peripheral vasoconstriction. Selective β1-antagonist, β2-agonist activity would, therefore, appear to be particularly beneficial in offering the advantages of β1 blockade plus peripheral vasodilation. The β1- and β2-receptor actions of drugs are not always clearly identifiable, as in the demonstration of celiprolol's partial β2-agonist activity in human beings. This is because, in vivo, cardiovascular reflexes are intact and it has not, so far, been possible to remove endogenous catecholamines. This review summarizes various studies to investigate partial agonist activity, with particular emphasis on celiprolol.