A Review on Telmisartan: A Novel, Long‐Acting Angiotensin II‐Receptor Antagonist

Abstract

Telmisartan is a potent, long-lasting, nonpeptide antagonist of the angiotensin II type-1 (AT 1 ) receptor that is indicated for the treatment of essential hypertension. It selectively and insurmountably inhibits stimulation of the AT 1 receptor by angiotensin II without affecting other receptor systems involved in cardiovascular regulation. Very high lipophilicity, a unique feature of telmisartan, coupled with a high volume of distribution, indicate that the compound offers the clinically important advantage of good tissue penetration. Telmisartan is not a prodrug and has a longer terminal elimination half-life than other commercially available sartans (~24 h), making it suitable for once-daily dosing. The compound is not metabolized by cytochrome P450 isoenzymes and has a low risk for P450-based drug interactions. In animal models, telmisartan exhibits pronounced cardioand reno-protective effects in animals with severe, essential hypertension. In clinical studies, telmisartan shows comparable antihypertensive activity to members of other major antihypertensive classes, such as ACE inhibitors, beta blockers and calcium antagonists. These trials have confirmed the placebo-like safety and tolerability of telmisartan in hypertensive patients. Based on these data, telmisartan offers advantages over other sartans and represents an important new treatment option for hypertension.

Current status of angiotensin receptor blockers for the treatment of cardiovascular diseases: focus on telmisartan

“…In addition, it is an insurmountable drug with respect to its AT 1 receptor attachment, leading to slow dissociation from the receptor and thus prolongation of its effect. 38,39 Telmisartan is highly selective for the AT 1 receptor and has no affinity for the AT 2 receptor. By attaching itself to the AT 1 receptor and leaving the AT 2 receptor free, it exerts a dual effect.…”

Comparative Effects of Telmisartan and Valsartan on Insulin Resistance in Hypertensive Patients with Metabolic Syndrome

“…E f f e c t s o f T e l mi s a r t a n a n d Va l s a r t a n o n S e r u m L i p i d P r o f i l e file might be involved in the strong insulin-sensitizing effect of telmisartan (14).…”

Significance of angiotensin II receptor blockers with high affinity to angiotensin II type 1 receptors for vascular protection in rats

“…For example, although ARBs vary in their binding affinities in in vitro experiments, the significance of the different binding affinities of the various ARBs has rarely been discussed in in vivo studies. 4,5 In in vitro experiments that studied the angiotensin II time-dependent dissociation of telmisartan, olmesartan, candesartan, Exp3174 (an active metabolite of losartan) and valsartan from membrane components containing human AT 1 receptors, the dissociation rate constant of each ARB was 0.003248, 0.004171, 0.005203, 0.008561 and 0.009946 min À1 , respectively, with corresponding half-lives of 213, 166, 133, 81 and 70 min, respectively. 4 In another study assessing binding to cultured Chinese hamster ovary cells expressing human AT 1 receptors, the dissociation rate constant of olmesartan and telmisartan was 0.0096 and 0.0237 min À1 , respectively, with corresponding half-lives of 65 and 29 min, respectively.…”

“…4,5 In in vitro experiments that studied the angiotensin II time-dependent dissociation of telmisartan, olmesartan, candesartan, Exp3174 (an active metabolite of losartan) and valsartan from membrane components containing human AT 1 receptors, the dissociation rate constant of each ARB was 0.003248, 0.004171, 0.005203, 0.008561 and 0.009946 min À1 , respectively, with corresponding half-lives of 213, 166, 133, 81 and 70 min, respectively. 4 In another study assessing binding to cultured Chinese hamster ovary cells expressing human AT 1 receptors, the dissociation rate constant of olmesartan and telmisartan was 0.0096 and 0.0237 min À1 , respectively, with corresponding half-lives of 65 and 29 min, respectively. 5 Miura et al 6 reported structural differences among ARBs, and these differences may explain why olmesartan can block AT 1 receptors to a greater degree than other ARBs.…”