Angiotensin II Type 1 Receptor Blockers

Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS.
DrugDrug NameDrug Indication
DB00177Valsartan**Monotherapy** Valsartan may be used alone for the management of hypertension [FDA label] **Combination therapy** Valsartan is indicated for the management of hypertension in patients for whom combination therapy is deemed appropriate [F3139]. It is combined with other anthypertensive agents such as hydrochlorothiazide, amlodipine, nevibolol and sacubitril [F3139], [F3136], [F3145], [F3148]. **Heart Failure** Valsartan is indicated for the treatment of heart failure (NYHA class II-IV) in patients who are intolerant to angiotensin-converting enzyme inhibitors (ACE inhibitors) for various reasons, including those who experience ACE inhibitor adverse effects. In a clinical study of 5010 patients, hospitalizations due to heart failure were markedly decreased when valsartan was taken regularly over a 2-year span [FDA label].
DB00678LosartanMay be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Losartan may be also used as a second line agent in the treatment of congestive heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.
DB00966TelmisartanUsed alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart failure (only in patients who cannot tolerate ACE inhibitors).
DB01342ForasartanFor the treatment of hypertension.
DB01347SaprisartanSaprisartan is used in the treatment of hypertension and heart failure.
DB08822Azilsartan medoxomilTreatment of hypertension (alone or as an adjunct).
DB00876EprosartanFor the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).
DrugDrug NameTargetType
DB00177ValsartanType-1 angiotensin II receptortarget
DB00177ValsartanCytochrome P450 2C9enzyme
DB00177ValsartanSolute carrier organic anion transporter family member 1B3transporter
DB00177ValsartanSolute carrier organic anion transporter family member 1B1transporter
DB00177ValsartanCanalicular multispecific organic anion transporter 1transporter
DB00678LosartanType-1 angiotensin II receptortarget
DB00678LosartanCytochrome P450 3A4enzyme
DB00678LosartanCytochrome P450 2C9enzyme
DB00678LosartanCytochrome P450 2C8enzyme
DB00678LosartanMultidrug resistance protein 1transporter
DB00678LosartanSolute carrier family 22 member 6transporter
DB00678LosartanUDP-glucuronosyltransferase 1-1enzyme
DB00678LosartanUDP-glucuronosyltransferase 1-3enzyme
DB00678LosartanUDP-glucuronosyltransferase 1-10enzyme
DB00678LosartanUDP-glucuronosyltransferase 2B7enzyme
DB00678LosartanUDP-glucuronosyltransferase 2B17enzyme
DB00678LosartanCytochrome P450 2C19enzyme
DB00678LosartanSerum albumincarrier
DB00678LosartanSolute carrier family 22 member 12transporter
DB00678LosartanSolute carrier family 2, facilitated glucose transporter member 9transporter
DB00678LosartanBile salt export pumptransporter
DB00966TelmisartanType-1 angiotensin II receptortarget
DB00966TelmisartanPeroxisome proliferator-activated receptor gammatarget
DB00966TelmisartanMultidrug resistance protein 1transporter
DB00966TelmisartanCanalicular multispecific organic anion transporter 1transporter
DB00966TelmisartanATP-binding cassette sub-family G member 2transporter
DB00966TelmisartanCytochrome P450 2C19enzyme
DB00966TelmisartanBile salt export pumptransporter
DB00966TelmisartanUDP-glucuronosyltransferase 1-3enzyme
DB01342ForasartanType-1 angiotensin II receptortarget
DB01347SaprisartanType-1 angiotensin II receptortarget
DB08822Azilsartan medoxomilType-1 angiotensin II receptortarget
DB00876EprosartanType-1 angiotensin II receptortarget
DB00876EprosartanCanalicular multispecific organic anion transporter 1transporter