valsartan and lercanidipine

C09DB08

Forms & Strengths

Adult Dosing

Hypertension: One tablet once daily, taken at least 15 minutes before a meal
Titration: Increase dose after 2 to 4 weeks if blood pressure is inadequately controlled
Max daily dose: Valsartan 160 mg / Lercanidipine 20 mg
Renal impairment: Caution in mild-to-moderate; contraindicated in severe (CrCl < 30 mL/min)
Hepatic impairment: Contraindicated in severe hepatic impairment

Pediatric Dosing

Safety and efficacy in pediatric patients below 18 years of age have not been established
Not recommended for use in children and adolescents

Indications

Treatment of essential hypertension
indicado as replacement therapy in patients whose blood pressure is adequately controlled by the individual components given concurrently at the same dose level

Mechanism of Action

Valsartan is a selective, reversible angiotensin II receptor blocker (ARB) acting on the AT1 subtype
Lercanidipine is a dihydropyridine calcium channel blocker (CCB) that inhibits transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle
Combination provides additive antihypertensive efficacy through complementary mechanisms of vasodilation and RAAS blockade

Contraindications

Hypersensitivity to valsartan, lercanidipine, or any dihydropyridines
Second and third trimesters of pregnancy due to fetal and neonatal toxicity
Severe hepatic impairment
Severe renal impairment (CrCl < 30 mL/min) and patients undergoing dialysis
Obstruction of the outflow tract of the left ventricle (including severe aortic stenosis)
Untreated congestive heart failure
Unstable angina pectoris or within 1 month of a myocardial infarction
Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, erythromycin)
Co-administration with cyclosporine
Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment

Adverse Reactions

Common: Dizziness, headache, peripheral edema, flushing, palpitations
Uncommon: Hypotension, orthostatic hypotension, tachycardia, fatigue, asthenia, nausea, dyspepsia, rash
Rare: Somnolence, muscle cramps, pollakiuria, chest pain
Post-marketing: Angioedema, hyperkalemia, elevated liver function tests, renal impairment, hypersensitivity reactions

Drug Interactions

Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, grapefruit juice): Increase lercanidipine plasma concentrations, contraindicated
CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, St. John's wort): Decrease lercanidipine efficacy
Cyclosporine: Increases plasma levels of both lercanidipine and valsartan, contraindicated
Potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium: May lead to increases in serum potassium
Lithium: Reversible increases in serum lithium concentrations and toxicity reported during concomitant use with ARBs
NSAIDs including selective COX-2 inhibitors: May reduce antihypertensive effect and increase risk of worsening renal function
Other antihypertensive agents: May potentiate the blood pressure-lowering effect

Curated Content: Needs Vetting Before Put to Clinical Use