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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4A
pubmed:dateCreated
1983-12-17
pubmed:abstractText
Labetalol represents the culmination of an effort to enhance the antihypertensive efficacy and to improve the hemodynamic profile of beta-adrenoceptor blockers by incorporating an additional anti-hypertensive action, that is, alpha blockade, into its pharmacologic mechanism. Reviewed here are the major aspects of the animal pharmacology of labetalol. The compound blocks beta1 and beta2-adrenoceptors nonselectively. Its blockade of alpha receptors is selective and directed at the alpha1 subset. Labetalol also dilates blood vessels independently of these mechanisms. This action is mediated by activation of vascular beta2 adrenoceptors. Thus, labetalol acts as a partial agonist on vascular smooth muscle. However, it differs markedly from other beta blockers with intrinsic sympathomimetic activity in that its agonism is directed specifically at beta2 receptors. Labetalol lowers blood pressure in a variety of animal models of hypertension. Unlike pure beta blockers, the compound reduces peripheral vascular resistance. On the basis of this profile, it is proposed that labetalol lowers blood pressure in human subjects by three independent mechanisms: (1) beta blockade, (2) alpha blockade, and (3) direct vasodilatation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
AIM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0002-9343
pubmed:author
pubmed:issnType
Print
pubmed:day
17
pubmed:volume
75
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
15-23
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
1983
pubmed:articleTitle
Pharmacology of labetalol in experimental animals.
pubmed:publicationType
Journal Article