Amlodipine / Valsartan

Trade Names:Exforge- Tablets amlodipine 5 mg/valsartan 160 mg- Tablets amlodipine 10 mg/valsartan 160 mg- Tablets amlodipine 5 mg/valsartan 320 mg- Tablets amlodipine 10 mg/valsartan 320 mg

Pharmacology

Inhibits movement of calcium ions across cell membranes in systemic and coronary vascular smooth muscle.

Antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the angiotensin II receptor (AT ₁ receptor) in vascular smooth muscle and the adrenal gland, producing decreased blood pressure.

Indications and Usage

Treatment of hypertension.

Contraindications

Standard considerations.

Dosage and Administration

Titrate slowly in patients with severe renal function impairment.

Titrate slowly.

PO 5 mg/160 mg once daily in patients who are not volume-depleted is the usual starting dose. Increase after 1 to 2 wk to a max of 10 mg/320 mg once daily.

PO Initially, 2.5 mg of amlodipine once daily.

General Advice

• May be taken with or without food.
• May be administered with other antihypertensive agents.
• Patients not adequately controlled on amlodipine (or another dihydropyridine calcium channel blocker) alone or valsartan (or another angiotensin II receptor blocker) alone may be switched to amlodipine/valsartan tablets.
• May be substituted for individually titrated components.

Storage/Stability

Store at 59° to 86°F; protect from moisture.

Drug Interactions

Amlodipine plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.

Plasma concentrations may be elevated by valsartan, increasing the pharmacologic and toxic effects of lithium.

Coadministration with valsartan may cause elevated potassium concentrations and, in heart failure patients, increased serum creatinine. Amlodipine plasma concentrations may be elevated.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension.

CNS

Dizziness (2%); syncope.

Dermatologic

Exanthema.

EENT

Nasopharyngitis (4%); tinnitus, visual disturbance.

Metabolic

Peripheral edema (5%); increased potassium (3%).

Respiratory

Upper respiratory tract infection (3%).

Miscellaneous

Increased BUN (6%); increased creatinine (4%); elevated liver function tests, hypersensitivity.

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

In patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (eg, patients with severe CHF), valsartan treatment may be associated with oliguria and/or progressive azotemia, which may rarely result in acute renal failure and death.

Use with caution.

Hepatic Function

Use with caution.

Cardiovascular

Increased frequency, duration, or severity of angina or acute MI may occur. Use with caution in patients with heart failure or severe aortic stenosis.

Hypotension/Volume-depleted patients

Symptomatic hypotension may occur after initiation of valsartan 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.

Surgery

Use with caution in patients undergoing surgery.

Overdosage

Symptoms

Bradycardia, circulatory shock, depressed consciousness, hypotension, peripheral vasodilation, shock, tachycardia.

Patient Information

• Advise patient to take once daily as prescribed without regard to meals, but to take with food if GI upset occurs.
• Advise patient to try to take each dose at about the same time each day.
• Inform patient that drug controls, but does not cure, hypertension and to continue taking drug as prescribed even when BP is not elevated.
• Instruct patient to avoid the use of supplements or salt substitutes containing potassium without first consulting health care provider.
• Advise patient to monitor and record BP and pulse at home and to inform health care provider if abnormal measurements are noted.
• Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
• Inform women of childbearing age to report pregnancy to health care provider as soon as possible.
• Advise women not to breast-feed while taking this medication.

Copyright © 2009 Wolters Kluwer Health.