Lercanidipine is indicated for the treatment of mild to moderate essential hypertension.
Calcium-channel blockers
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.
Concomitant treatment of Lercanidipine with cyclosporin, phenytoin, carbamazepine, rifampicin, ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin, and midazolam should be avoided. Caution should be exercised when Lercanidipine is co-prescribed with astemizole, amiodarone, quinidine, cimetidine, metoprolol and simvastatin.
Lercanidipine is contraindicated in patients with left ventricular outflow tract obstruction, untreated congestive cardiac failure, unstable angina pectoris, within 1 month of a myocardial infarction and known hypersensitivity to any dihydropyridine. Lercanidipine should not be taken with grapefruit juice.
Treatment with Lercanidipine is generally well tolerated. The most common side effects are related to the vasodilatory properties of Lercanidipine such as flushing, peripheral edema, headache, dizziness and asthenia. Other side effects, which occurred in less than 1% of patients include fatigue; Gl disturbances such as dyspepsia, nausea, vomiting, epigastric pain and diarrhea, polyurea, rash, somnolence and myalgia.
Pregnancy Category C. There is no clinical experience with lercanidipine in pregnancy, but other dihydropyridine compounds have been found to cause irreversible malformations in animals. Therefore, lercanidipine should not be administered during pregnancy or to women with child-bearing potential unless effective contraception is used.Use in lactation: There is no clinical experience with lercanidipine in lactation. Distribution into milk may be expected, due to the high lipophilicity of lercanidipine. Therefore, lercanidipine should not be administered to lactating women.
Special care should be exercised when Lercanidipine is used in patients with sick sinus syndrome, left ventricular dysfunction and ischaemic heart disease.
There is no data with Lercanidipine overdosage. As with other dihydropyridines, overdosage might be expected to cause excessive peripheral vasodilation with marked hypotension and reflex tachycardia. Since the drug is highly lipophilic, it is most probable that plasma levels are no guide to the duration of the period of risk and dialysis may not be effective.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Calcium-channel blockers
Lercanidipine is a selective calcium channel blocker of the dihydropyridine group and it inhibits the transmembrane influx of calcium into smooth muscle. The mechanism of its antihypertensive action is due to a direct relaxant effect on vascular smooth muscle, thus lowering total peripheral resistance. Lercanidipine is endowed with a prolonged antihypertensive activity because of its high membrane partition coefficient and is devoid of negative inotropic effects due to its high vascular selectivity.
Since there is no clinical data with Lercanidipine in pregnancy, it should not be administered during pregnancy or to woman with child bearing potential unless effective contraception is used. Lercanidipine is highly lipophilic and distribution in milk may be expected. Therefore, it should not be administered to nursing mother.
