Metabolic actions of angiotensin receptor antagonists: PPAR-gamma agonist actions or a class effect?
Accumulating basic and clinical data support the hypothesis that angiotensin receptor blockers have beneficial effects on glucose and lipid metabolism that are not shared by other classes of antihypertensive agents. These metabolic actions might only partially be shared by angiotensin-converting enzyme inhibitors. Specific benefits beyond those of other angiotensin receptor blockers have been claimed for telemesartan and, to a lesser extent, irbesartan based on a partial agonist action on PPAR-gamma receptors. Although the evidence is strong in vitro, specific actions not shared by other angiotensin receptor blockers have not yet been convincingly demonstrated in vivo or in clinical trials. In many cases, a full range of doses has not been compared, and the apparent superiority of telmesartan could be an artifact of its higher receptor binding affinity, greater tissue penetration owing to lipophilicity, and longer half life.
Ernsberger
Paul
P
Department of Nutrition, Case Western Reserve University, School of Medicine, Cleveland, OH 44106-4906, USA. pre@po.cwru.edu
Koletsky
Richard J
RJ
D047228:Angiotensin II Type 1 Receptor Blockers / Q000493:pharmacokinetics / Q000494:pharmacology*; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D001562:Benzimidazoles / Q000493:pharmacokinetics / Q000494:pharmacology; D001565:Benzoates / Q000493:pharmacokinetics / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D006973:Hypertension / Q000188:drug therapy; D000077405:Irbesartan; D047495:PPAR gamma / Q000819:agonists*; D011945:Receptors, Angiotensin / Q000378:metabolism; D012084:Renin-Angiotensin System / Q000187:drug effects / Q000502:physiology; D000077333:Telmisartan; D013777:Tetrazoles / Q000493:pharmacokinetics / Q000494:pharmacology
D047228:Angiotensin II Type 1 Receptor Blockers; D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001565:Benzoates; D001713:Biphenyl Compounds; D047495:PPAR gamma; D011945:Receptors, Angiotensin; D013777:Tetrazoles; D000077405:Irbesartan; D000077333:Telmisartan