Presartan, the first of a new class of antihypertensives, is a specific and selective antagonist of angiotensin II at the AT1 sites. Angitensin II is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. Presartan and its principal active metabolite block the vasoconstriction and aldosterone secreting effects of angiotensin II to the AT1 receptor found in many tissues. Presartan is now regarded as the first-line therapy option for treating high blood pressue.