Effective treatment of hypertension by AT₁ receptor antagonism: the past and future of telmisartan

Abstract

Lowering blood pressure is the most effective treatment method to ensure a reduction in the total risk for cardiovascular morbidity and mortality. The renin–angiotensin system plays an important role in volume homeostasis and blood pressure regulation and is a target for several groups of pharmaceutical agents. Angiotensin II receptor blockers represent the newest class of antihypertensive compounds. They prevent the binding of angiotensin II to the subtype 1 receptor (AT₁), which is believed to mediate most of the physiological actions relevant to the regulation of blood pressure. Telmisartan, a widely used AT₁ receptor antagonist, is a highly selective compound with high potency, a long duration of action and a tolerability profile similar to placebo. Numerous randomized clinical trials and community-based studies have demonstrated that oral telmisartan and combinations of telmisartan with hydrochlorothiazide are at least as effective in lowering blood pressure as all other hypertensive medications. This has been demonstrated in different populations of adult patients with mild-to-moderate essential hypertension, including patients with coexisting Type 2 diabetes, metabolic syndrome or renal impairment. Several large-scale, long-term, clinical endpoint studies are in progress to assess the beneficial effects of telmisartan on hypertension-related end-organ damage in patients at high risk of renal, cardiac and vascular damage whose blood pressure is well controlled. The most recent data from clinical trials and latest research regarding telmisartan will be reviewed in this article.

Keywords::

• angiotensin II receptor blocker
• diabetes
• hypertension
• metabolic syndrome
• renin-angiotensin system
• telmisartan