Indications
Lercanidipine is indicated for the treatment of mild to moderate essential hypertension.
Therapeutic Class
Calcium-channel blockers
Pharmacology
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.
Dosage
Use in elderly: The recommended dosage is 10 mg orally once a day at least 15 minutes before meals; the dose may be increased to 20 mg depending on the individual patient’s response. It may take about 2 weeks before the maximal anti-hypertensive effect is apparent. Some individuals, not adequately controlled on a single antihypertensive agent, may benefit from the addition of Lercanidipine to therapy with a beta-adrenoceptor blocking drug (atenolol), a diuretic (hydrochlorothiazide) or an ACE inhibitor (ramipril).Use in children: Since there is no clinical data in patients under the age of 18 years, use in children is not currently recommended.
Use in renal or hepatic dysfunction: Special care should be exercised in patients with mild to moderate renal or hepatic dysfunction. Dosage above 20 mg daily must be approached with caution. Lercanidipine is not recommended for use in patients with severe hepatic or renal dysfunction.
Administration
Should be taken on an empty stomach. Take at least 15 min before meals.
Interaction
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.
Contraindications
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.
Side Effects
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; GI disturbances such as dyspepsia, nausea, vomiting, epigastric pain and diarrhea, polyurea, rash, somnolence and myalgia.
Pregnancy & Lactation
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.
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.
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