The clinical profile of the angiotensin II receptor blocker eprosartan.
Angiotensin II receptor antagonists block angiotensin II type 1 (AT1) receptors and reduce the pressor effects of angiotensin in the vasculature. By this mechanism, they induce similar pharmacological effects to angiotensin-converting enzyme (ACE) inhibitors, resulting in a lowering of blood pressure (BP). However, AT1 antagonists differ from ACE inhibitors with respect to side effects, and induce less cough, which is related to bradykinin activation. Within the class of angiotensin II antagonists, eprosartan differs from other currently clinically available agents in terms of its chemical structure and its dual pharmacological mode of action. Eprosartan acts not only at vascular AT1 receptors but also at presynaptic AT1 receptors, causing inhibition of sympathetically stimulated noradrenaline release. Eprosartan is not metabolized by cytochrome P450 enzymes and therefore has a low potential for metabolic drug interactions, which may be of importance when treating the elderly and patients on multiple drugs. In clinical trials eprosartan has proven to be at least as effective as the ACE inhibitor enalapril in reducing BP, but with a significantly lower incidence of side effects. Eprosartan is safe, effective and well tolerated in long-term treatment, either as monotherapy or in combination with other antihypertensive drugs such as hydrochlorothiazide.
Hedner
Thomas
T
Department of Clinical Pharmacology, Sahlgrenska University Hospital, 41345 Göteborg, Sweden. thomas.hedner@pharm.gu.se
D000179:Acrylates / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D007093:Imidazoles / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D044140:Receptor, Angiotensin, Type 1; D013876:Thiophenes
D000179:Acrylates; D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D007093:Imidazoles; D044140:Receptor, Angiotensin, Type 1; D013876:Thiophenes; C068373:eprosartan