Lercanidipine

Indications
 Oral
Hypertension
Adult: As hydrochloride: 10 mg once daily, increased after 2 wk to 20 mg daily if necessary.
Renal impairment: Dosage may need to be reduced in mild to moderate renal impairment. Avoid in patients with CrCl <12 ml/min.
Contraindications
 Severe hepatic or renal impairment; aortic stenosis, unstable angina, uncontrolled heart failure, within 1 mth of MI; lactation, pregnancy.
Warnings / Precautions
 Left ventricular dysfunction, sick sinus syndrome (if pacemaker not fitted).
Adverse Reactions
 Tachycardia, oedema, flushing, headache, dizziness, asthenia, rash, diarrhoea, polyuria, palpitations, hypotension, drowsiness, myalgia.
Drug Interactions
 Plasma concentration reduced by inducers of CYP3A4 eg rifampicin, phenytoin, carbamazepine. Bioavailability also reduced by metoprolol and possibly propranolol. Plasma concentrations increased by inhibitors of CYP3A4 eg imidazole antifungals, erythromycin, ritonavir, fluoxetine. Alcohol may potentiate vasodilating effect.
Potentially Fatal: Significantly increased plasma levels of both lercanidipine and ciclosporin when administered together.
See Below for More lercanidipine Drug Interactions
Food Interactions
 Grapefruit juice may inhibit metabolism.
Mechanism of Actions
 Lercanidipine is a dihydropyridine calcium-channel blocker which acts by inhibiting the influx of calcium ions through the slow channels of the vascular smooth muscle and myocardium during depolarization. Its main effect is vasodilatation because it has greater selectivity for vascular smooth muscle than cardiac smooth muscle.
Absorption: Fully absorbed from the GI tract. Peak plasma levels occur in 1.5-3 hr.
Distribution: Extensively distributed in tissues and organs. >98% protein bound.
Metabolism: Undergoes extensive hepatic metabolism to inactive metabolites via CYP3A4 isoenzyme.
Excretion: Mean elimination half life is approx 8-10 hr.
Administration
 Should be taken on an empty stomach. (Take on an empty stomach at least 15 min before meals.)
ATC Classification
 C08CA13 - lercanidipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Available As
  • Lercanidipine 10 mg
  • Lercanidipine 20 mg

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