An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists.

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van Zwieten PA

An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists.

Drugs. 1993 Apr;45(4):509-17.

PubMed ID

7684671 [ View in PubMed

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Abstract

Haemodynamically, the combination of alpha 1- and beta-adrenoceptor antagonists is a logical one. alpha 1-Adrenoceptor blockade causes vasodilatation and hence counteracts elevated peripheral vascular resistance, the most consistent haemodynamic derangement in established essential hypertension. beta-Blockers, which lower elevated blood pressure by a different (not yet clearly understood) mechanism, suppress the reflex tachycardia triggered by vasodilatation. Combined alpha/beta-adrenoceptor blockade can be obtained by the simultaneous administration of both types of adrenoceptor antagonists, but also by giving drugs that possess alpha- and beta-adrenoceptor antagonistic activity in the same molecule. Carvedilol and labetalol are the best known examples of such combined alpha/beta-adrenoceptor antagonists, although their pharmacodynamic profile is a result of different receptor selectivity of their component stereoisomers, rather than combined alpha/beta-blocking activity in a single chemical entity. Both compounds have been investigated clinically in the treatment of essential hypertension in moderate-to-large scale trials. A few newer combined alpha/beta-adrenoceptor antagonists, such as amosulalol, arotinolol and medroxalol have been developed, but clinical data on these compounds are relatively scarce.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Labetalol	Alpha-1 adrenergic receptors (Protein Group)	Protein group	Humans	Yes	Antagonist	Details
Labetalol	Beta-1 adrenergic receptor	Protein	Humans	Yes	Antagonist	Details
Labetalol	Beta-2 adrenergic receptor	Protein	Humans	Yes	Antagonist	Details