ATC Group: C09C Angiotensin II antagonists, plain

Azilsartan medoxomil is an orally active prodrug that is rapidly converted to the active moiety, azilsartan, which selectively antagonises the effects of angiotensin II by blocking its binding to the AT₁ receptor in multiple tissues. Angiotensin II is the principal pressor agent of the RAAS, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium.

Candesartan is an AIIRA, selective for AT₁ receptors, with tight binding to and slow dissociation from the receptor. It has no agonist activity. The antagonism of the angiotensin II (AT₁) receptors results in dose related increases in plasma renin levels, angiotensin I and angiotensin II levels, and a decrease in plasma aldosterone concentration.

Eprosartan is a potent, synthetic, orally active non-biphenyl non-tetrazole angiotensin II receptor antagonist, which binds selectively to the AT₁ receptor.

Fimasartan, an angiotensin II receptor antagonist with selectivity for the AT1 receptor subtype, is a pyrimidinone-related heterocyclic compound.

Irbesartan is a potent, orally active, selective angiotensin-II receptor (type AT₁) antagonist. It is expected to block all actions of angiotensin-II mediated by the AT₁ receptor, regardless of the source or route of synthesis of angiotensin-II. The selective antagonism of the angiotensin-II (AT₁) receptors results in increases in plasma renin levels and angiotensin-II levels, and a decrease in plasma aldosterone concentration.

Losartan is a synthetic oral angiotensin-II receptor (type AT₁) antagonist. Antihypertensive activity and suppression of plasma aldosterone concentration are maintained, indicating effective angiotensin II receptor blockade.

Olmesartan medoxomil is a potent, orally active, selective angiotensin II receptor (type AT₁) antagonist. It is expected to block all actions of angiotensin II mediated by the AT₁ receptor, regardless of the source or route of synthesis of angiotensin II. The selective antagonism of the angiotensin II (AT₁) receptors results in increases in plasma renin levels and angiotensin I and II concentrations, and some decrease in plasma aldosterone concentrations.

Telmisartan is an orally active and specific angiotensin II receptor (type AT₁) antagonist. Telmisartan selectively binds the AT₁ receptor. The binding is long-lasting.

Valsartan is an orally active, potent, and specific angiotensin II (Ang II) receptor antagonist. It acts selectively on the AT₁-receptor subtype, which is responsible for the known actions of angiotensin II.