Overview
Exforge is a fixed-dose combination of amlodipine (a dihydropyridine calcium channel blocker) and valsartan (an angiotensin II receptor blocker) used for the treatment of hypertension. It works through complementary mechanisms to reduce peripheral vascular resistance and lower blood pressure. This combination may provide additive antihypertensive effects compared to monotherapy.
Mechanism of Action
Amlodipine inhibits calcium influx through L-type calcium channels in vascular smooth muscle, causing vasodilation and reduced peripheral resistance. Valsartan selectively blocks angiotensin II binding to AT1 receptors, inhibiting angiotensin II-induced vasoconstriction, aldosterone secretion, and sodium retention. These complementary mechanisms provide additive blood pressure reduction.
Indications
- Treatment of hypertension
- May be used in patients whose blood pressure is not adequately controlled on amlodipine or valsartan monotherapy
Common Doses
- 5 mg/160 mg
- 10 mg/160 mg
- 5 mg/320 mg
- 10 mg/320 mg
Dosage
Initial dose typically 5/160 mg once daily. Titration may be made after 1-2 weeks. Maximum recommended dose is 10/320 mg once daily. Dose should be individualized based on blood pressure response.
Contraindications
- Known hypersensitivity to any component
- Coadministration with aliskiren in patients with diabetes
Side Effects
- Peripheral edema
- Dizziness
- Headache
- Fatigue
- Flushing
- Hyperkalemia
- Hypotension
- Angioedema (rare)
Interactions
- CYP3A inhibitors: Increase amlodipine exposure, monitor for hypotension and edema
- CYP3A inducers: May decrease amlodipine efficacy, monitor blood pressure
- Simvastatin: Limit dose to 20 mg daily when coadministered
- Potassium-sparing diuretics/potassium supplements: Increased risk of hyperkalemia
- NSAIDs/COX-2 inhibitors: May reduce antihypertensive effect and worsen renal function
- Other RAS inhibitors: Increased risk of hypotension, hyperkalemia, and renal impairment
Counseling Points
- Take once daily with or without food
- Do not stop abruptly; consult healthcare provider before discontinuing
- Report swelling of face, lips, tongue, or difficulty breathing immediately
- Monitor blood pressure regularly
- Avoid potassium supplements or salt substitutes unless directed by physician
- Use effective contraception during treatment
- Report dizziness, lightheadedness, or fainting
- Maintain regular follow-up appointments