Trade Names:Diovan- Tablets 40 mg- Tablets 80 mg- Tablets 160 mg- Tablets 320 mg
Antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the binding of angiotensin II to the AT 1 receptor in vascular smooth muscle and the adrenal gland, producing decreased BP.
T max is 2 to 4 h after dosing. Bioavailability is about 10% to 35%. Food decreases AUC about 40% and decreases C max about 50%.
Vd is about 17 L. Highly bound to albumin (about 95%).
The major metabolite, valeryl 4-hydroxy valsartan, accounts for about 9% of the dose.
Half-life is about 6 h. Valsartan is primarily recovered in the feces (about 83%) and urine (about 13%). Recovery is mainly unchanged drug, with only about 20% of the dose recovered as metabolite. The plasma Cl is about 2 L/h.
No correlation between renal function and exposure to the drug.Hepatic Function Impairment
Patients with mild to moderate chronic liver disease have about twice the AUC value.Elderly
AUC is about 70% higher and t ½ is about 35% longer in elderly patients.
Treatment of hypertension; treatment of heart failure; reduction of CV mortality in clinically stable patients with left ventricular failure or dysfunction after MI.
PO Initial dosage: 80 or 160 mg once daily. Maintenance dosage: 80 to 320 mg once daily.Children 6 to 16 yr of age
PO Initial dosage: 1.3 mg/kg (up to 40 mg) once daily. Adjust dose based on BP response. Dosages higher than 2.7 mg/kg (up to 160 mg) once daily have not been studied in children.Heart FailureAdults
PO Initial dosage: 40 mg twice daily; titration to 80 and 160 mg twice daily should be done to the highest dose, as tolerated by the patient (max dose, 320 mg/day).Post-myocardial infarctionAdults
PO Initiate 12 h after MI at 20 mg twice daily. Titrate within 7 days to 40 mg twice daily with additional titrations to a target maintenance dosage of 160 mg twice daily, as tolerated by the patient.Hepatic/Renal Function Impairment
Exercise care with dosing in patients with hepatic or severe renal function impairment.
May be administered with or without food.
Store at 59° to 86°F in tightly closed container. Protect from moisture.
May increase valsartan plasma concentrations.Lithium
Plasma concentrations may be increased by valsartan, resulting in an increase in the pharmacologic and adverse reactions of lithium.Potassium-sparing diuretics (eg, spironolactone), potassium supplements
Coadministration may cause elevated serum potassium concentrations in certain high-risk patients.
None well documented.
Hypotension (7%); postural hypotension (2%); syncope (at least 1%).
Dizziness (17%); fatigue (3%); postural dizziness (2%); headache, vertigo (at least 1%).
Blurred vision (at least 1%).
Diarrhea (5%); abdominal pain (2%); nausea, upper abdominal pain (at least 1%).
Renal function impairment (at least 1%).
Elevated liver enzymes, hepatitis (postmarketing).
Arthralgia, back pain (3%); rhabdomyolysis (postmarketing).
Dry cough (3%).
Viral infection (3%); hypersensitivity (postmarketing).
When used in pregnancy, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.
Assess renal function in heart failure or post-MI patients.
Category D .
Safety and efficacy not established in children younger than 6 yr of age.Heart failure or post-MI patients
Use caution when initiating therapy; hypotension may occur.
Patients with renal artery stenosis may experience acute renal failure. Use caution in treating patients whose renal function may depend on the activity of renin-angiotensin-aldosterone system (eg, severe CHF).
Use with caution.
Symptomatic hypotension may occur after initiation of valsartan therapy in patients who are intravascularly volume depleted (eg, those treated with diuretics). Correct these conditions prior to administration of valsartan or start treatment under close medical supervision.
Bradycardia, hypotension, tachycardia.
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