Valsartan is an orally active, nonpeptide angiotensin II receptor antagonist (ARB), selective for the AT1 receptor. It blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor subtype in many tissues (eg, vascular smooth muscle, adrenal gland). Its action is independent of the pathways for angiotensin II synthesis. It has no agonist activity of AT1 and its affinity for the AT1 receptor is approximately 20,000 times greater than for the AT2 receptor.
藥動學
Elimination half-life: 6 hrs
Excretion: primarily as unchanged drug in the urine (13%) and feces (83%)
禁忌症
Concomitant Aliskiren use in diabetic patients; Hypersensitivity to valsartan or other angiotensin receptor antagonists.
懷孕分類
D
哺乳分類
Infant risk cannot be ruled out
副作用
Hypertension, headache, dizziness, serum BUN raised, serum creatinine raised, cough
劑量和給藥方法
80 to 160mg PO QD, maintenance dose can be up to 320mg QD