[Pharmacokinetic and pharmacodynamic aspects of angiotensin II antagonists. Focus on arterial hypertension].
The major pharmacokinetic and pharmacodynamic properties of angiotensin II receptor antagonists in humans are reviewed, this analysis being focused on its antihypertensive effect. Common characteristics of the members of this new therapeutic class: nonpeptidic nature, lipophilia, oral intermediate bioavailability and selectivity for AT1 receptor are discussed. The liver metabolism and the presence of active metabolites of some of these molecules are specially stressed. Angiotensin II antagonists block the blood pressure response to angiotensin II, reduce the high baseline blood pressure in hypertensive patients, increase the plasma renin activity and endogenous angiotensin II plasma levels, have natriuretic effects and increase the renal blood flow without altering the glomerular filtration rate. These and other dose-dependent effects of angiotensin II receptor antagonists are discussed and criticized, in an attempt to characterize their pharmacokinetic profile and to define the pharmacodynamic relation able to support its therapeutical use.
da Silva
P M
PM
Serviço de Medicina, Hospital de Santa Marta.
D000804:Angiotensin II / Q000037:antagonists & inhibitors*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000493:pharmacokinetics*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D014662:Vasoconstrictor Agents / Q000037:antagonists & inhibitors*
D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D014662:Vasoconstrictor Agents; D000804:Angiotensin II