Lercanidipine

Uses

Lercanidipine is used for the treatment of mild to moderate essential hypertension.

Lercanidipine is also used to associated treatment for these conditions: High Blood Pressure (Hypertension), Mild Hypertension, Moderate Essential Hypertension

How Lercanidipine works

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Lercanidipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Dosage

Lercanidipine 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.

Should be taken on an empty stomach. Take at least 15 min before meals.

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.

Precaution

Special care should be exercised when Lercanidipine is used in patients with sick sinus syndrome, left ventricular dysfunction and ischaemic heart disease.

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.

Food Interaction

• Avoid alcohol. Alcohol may increase the vasodilatory effects of lercanidipine, which may lead to hypotension.
• Avoid grapefruit products. Grapefruit inhibits the metabolism of lercanidipine through CYP3A4, which causes increased serum levels of lercanidipine, and may increase the risk of hypotension.
• Exercise caution with St. John's Wort. Lercanidipine is metabolized by CYP3A4, and St. John's Wort is a CYP3A4 inducer.
• Take on an empty stomach. Taking lercanidipine after meals increases its bioavailability, therefore lercanidipine should be taken least 15 minutes before meals.

Pregnancy & Breastfeeding use

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.

Contraindication

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.

Special Warning

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.

Acute Overdose

There have been no recorded cases of Lercanidipine overdosage. As with other dihydropyridines, overdosage might be expected to cause excessive peripheral vasodilatation with marked hypotension and reflex tachycardia.

Storage Condition

Should be stored in cool and dry place

Innovators Monograph

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