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
Bioavailability: 25%
Metabolism: CYP2C9
Excretion: Renal, mainly as unchanged drug
Elimination Half Life: 6 hours
禁忌症
Concomitant aliskiren use in diabetic patients.
Hypersensitivity to valsartan or any component of the product
Heart failure:
1. Initial: 40 mg ORALLY twice daily
2. Maintenance: 80 to 160 mg ORALLY twice daily as tolerated; MAX 320 mg daily Hypertension:
1. Initial: 80 to 160 mg ORALLY once daily
2. Maintenance: 80 to 320 mg ORALLY once daily Myocardial infarction:
1. Initial: 20 mg ORALLY twice daily
2. May be increased within 7 days to 40 mg twice daily ; titrate to 160 mg twice a day as tolerated
小兒調整劑量
Hypertension: (6 to 16 years old)
1. Initial 1.3 mg/kg once daily; MAX 40 mg/day
2. Maintenance: up to 2.7 mg/kg once daily; MAX 160 mg/day