NIDEXIF 10 mg

Indications

• Hypertension
• Chronic stable angina pectoris
• Prinzmetal's variant angina

Dosage

Children: Lercanidipine is not recommended for use in children and adolescents under 18 years of age due to insufficient safety and efficacy data.

Adults: The usual initial adult dose is 10 mg once daily, which may be increased to a maximum of 20 mg once daily if necessary.

Mechanism of action

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

Pharmacodynamics

As a calcium channel blocker, Lercanidipine decreases peripheral vascular resistance and myocardial oxygen demand, making it effective in managing hypertension and chronic stable angina. Its selectivity for vascular smooth muscle over cardiac muscle reduces the likelihood of reflex tachycardia, a common side effect of other antihypertensive agents.

Pharmacokinetics

Lercanidipine is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 1 to 2 hours post-administration. It has a high protein binding rate and a long half-life, allowing for once-daily dosing. The drug is extensively metabolized in the liver and excreted primarily in the feces, with a smaller portion eliminated in the urine. Its pharmacokinetics can be affected by food, with high-fat meals increasing its absorption.

Contra-indications

• Severe hypotension
• Cardiogenic shock
• Severe aortic stenosis
• Concurrent use with other dihydropyridine calcium channel blockers

Adverse effects

• Peripheral edema
• Flushing
• Headache
• Dizziness
• Palpitations
• Gingival hyperplasia
• Abdominal pain

Interactions

• cobicistat+lercanidipine: Severe (increases exposure)
• grapefruit juice+lercanidipine: Severe (increases exposure)
• idelalisib+lercanidipine: Severe (increases exposure)
• enzalutamide+lercanidipine: Moderate (decreases exposure)
• apalutamide+lercanidipine: Moderate (decreases exposure)
• dronedarone+lercanidipine: Moderate (increases exposure)
• antifungals, azoles+lercanidipine: Moderate (increases exposure)
• miconazole+lercanidipine: Moderate (increases exposure)
• cenobamate+lercanidipine: Moderate (decreases exposure)
• ciclosporin+lercanidipine: Moderate (increases exposure)

Precautions

• Monitor blood pressure regularly
• Use with caution in patients with liver impairment
• Consider potential interactions with other antihypertensive medications

Pregnancy

Not recommended during pregnancy unless the benefits outweigh the risks. Consult healthcare professionals for individual assessment.

Breast-feeding

Lercanidipine is excreted in breast milk; caution is advised when administered to nursing women.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• Tablets

Indications

• Hypertension
• Mild to moderate hypertension

Dosage

Adults: Initially 10 mg once daily; may be increased to 20 mg daily if necessary. Doses should be adjusted at intervals of 3–4 weeks, and it is recommended to take the medication in the morning.

Mechanism of action

Lercanidipine acts by selectively blocking L-type calcium channels in the vascular smooth muscle, resulting in decreased intracellular calcium concentrations. This mechanism causes relaxation of vascular smooth muscle, leading to vasodilation and a subsequent decrease in blood pressure. It has a preferential effect on the peripheral vasculature, reducing systemic vascular resistance.

Pharmacodynamics

The antihypertensive effects of lercanidipine are characterized by a reduction in arterial pressure, which is sustained over a 24-hour period. It is noted for its relatively low incidence of reflex tachycardia compared to other calcium channel blockers, making it favorable for long-term management of hypertension. Clinical studies have shown lercanidipine to be effective in reducing both systolic and diastolic blood pressure.

Pharmacokinetics

Lercanidipine is well absorbed from the gastrointestinal tract, although its bioavailability is approximately 10% due to extensive first-pass metabolism. Peak plasma concentrations occur about 1-2 hours after oral administration. It has a long elimination half-life of approximately 8-12 hours, allowing for once-daily dosing. The drug is metabolized primarily in the liver via cytochrome P450 enzymes, particularly CYP3A4, with metabolites excreted mainly in the urine. Renal impairment does not significantly affect its clearance, but caution is advised in patients with hepatic impairment.

Contra-indications

• Cardiac outflow obstruction
• Acute porphyrias
• Severe left ventricular failure
• Within 1 month of myocardial infarction

Adverse effects

• Gingivitis
• Hypersensitivity reactions
• Muscle cramps
• Tremor
• Asthenia
• Abdominal discomfort
• Increased urinary frequency
• Ischaemic heart disease
• Photosensitivity reactions
• Sexual dysfunction
• Atrial fibrillation
• Myalgia

Interactions

• Other calcium channel blockers
• CYP3A4 inhibitors and inducers
• Beta-blockers
• Diuretics
• ACE inhibitors

Precautions

• Caution in patients with hepatic impairment
• Monitor for hypotension
• Dose adjustments may be necessary in elderly patients

Pregnancy

Manufacturer advises avoiding use, as it may inhibit labor.

Breast-feeding

Manufacturer advises avoiding use; no specific information available.

Storage

Store at room temperature, protected from light and moisture.

Formulations

• Lercanidipine hydrochloride 10 mg tablet
• Lercanidipine hydrochloride 20 mg tablet
• Modified-release formulations may be available

Mechanism of action

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.

Pharmacodynamics

Lercanidipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Lercanidipine is similar to other peripheral vasodilators. Lercanidipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. 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.