Telmisartan, a long-lasting angiotensin II type-1 receptor antagonist, provides comparable antihypertensive activity to other major classes with placebo-like safety for essential hypertension.
Does telmisartan provide effective and safe antihypertensive activity in patients with essential hypertension?
Telmisartan is a long-acting, highly lipophilic AT1 receptor antagonist that provides effective once-daily blood pressure control with a favorable safety profile.
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 cardio‐and renoprotective 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.
Wienen et al. (Thu,) conducted a review in Essential hypertension. Telmisartan vs. ACE inhibitors, beta blockers, calcium antagonists, other sartans was evaluated. Telmisartan, a long-lasting angiotensin II type-1 receptor antagonist, provides comparable antihypertensive activity to other major classes with placebo-like safety for essential hypertension.