Lercanidipine (Tablets) Instructions for Use

ATC Code

C08CA13 (Lercanidipine)

Active Substance

Lercanidipine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

“Slow” calcium channel blocker. Antihypertensive drug

Pharmacotherapeutic Group

Calcium channel blockers; selective calcium channel blockers with predominant vascular action; dihydropyridine derivatives

Pharmacological Action

A blocker of slow calcium channels, a derivative of the dihydropyridine series. It inhibits the transmembrane flow of calcium into cardiomyocytes and smooth muscle cells.

The mechanism of the antihypertensive effect is due to a direct relaxing effect on vascular smooth muscles, resulting in a decrease in total peripheral vascular resistance. It has a prolonged antihypertensive action. Due to high selectivity, a negative inotropic effect is absent.

The duration of the therapeutic action is 24 hours.

Pharmacokinetics

After oral administration in a dose of 10-20 mg, it is completely absorbed. C_max in blood plasma is detected after 1.5-3 hours and is 3.3 ng/ml and 7.66 ng/ml, respectively.

Distribution from blood plasma to tissues and organs occurs rapidly. Plasma protein binding exceeds 98%. No accumulation is observed upon repeated administration. It undergoes metabolism. The mean T_1/2 is 8-10 hours.

Indications

Mild to moderate essential arterial hypertension.

ICD codes

Dosage Regimen

Take orally, once daily. Swallow the tablet whole with a glass of water. Do not chew or crush the tablet.

Initiate therapy at 10 mg once daily. Take the dose at least 15 minutes before a meal, preferably in the morning. Food significantly increases drug absorption.

If adequate blood pressure control is not achieved after two weeks, the dose may be increased to 20 mg once daily. This is the maximum recommended dose.

Do not exceed the 20 mg daily dose. The therapeutic effect is dose-dependent. Titrate the dose gradually based on individual patient response and tolerability.

In elderly patients and patients with mild to moderate hepatic or renal impairment, use the same initial 10 mg dose. Exercise caution during subsequent dose titration. Monitor blood pressure closely.

The drug is contraindicated in patients with severe renal impairment (creatinine clearance less than 10 mL/min) or severe liver dysfunction.

Adverse Reactions

From the cardiovascular system: effects associated with the vasodilatory action were rarely noted – peripheral edema, sensation of “flushing” of blood to the face, palpitations, tachycardia, chest pain, decreased blood pressure, angina pectoris, myocardial infarction, asthenia, fatigue, headache, dizziness.

From the digestive system: very rarely – dyspepsia, nausea, vomiting, epigastric pain, diarrhea, reversible increase in liver enzyme activity, gingival hyperplasia.

Other: very rarely – polyuria, skin rash, drowsiness, myalgia.

Contraindications

Chronic heart failure in the stage of decompensation; unstable angina; aortic stenosis; within 1 month after myocardial infarction; severe liver dysfunction; renal impairment (creatinine clearance less than 10 ml/min); lactose intolerance; pregnancy; lactation (breastfeeding) period; women of childbearing potential not using reliable contraception; children and adolescents under 18 years of age; hypersensitivity to the active substance; hypersensitivity to other dihydropyridine derivatives.

Use in Pregnancy and Lactation

Use during pregnancy and lactation (breastfeeding) is contraindicated.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction. Use with caution in mild to moderate hepatic insufficiency.

Use in Renal Impairment

Contraindicated in severe renal impairment (creatinine clearance less than 10 ml/min). Use with caution in mild to moderate renal insufficiency.

Pediatric Use

Contraindicated in children and adolescents under 18 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Use with caution in mild to moderate renal and/or hepatic insufficiency, in elderly patients, in sick sinus syndrome (without a pacemaker), coronary artery disease, left ventricular dysfunction.

Drug Interactions

When used concomitantly with CYP3A4 inhibitors (including ketoconazole, itraconazole, erythromycin), manifestations of drug interaction are possible (combinations should be used with caution).

When used concomitantly with CYP3A4 inducers (including antidepressants, rifampicin), a decrease in the antihypertensive effect of lercanidipine is possible.

Enhancement of the hypotensive effect of lercanidipine is possible when consuming grapefruit juice.

Ethanol may potentiate the action of lercanidipine.

With simultaneous use with metoprolol, the bioavailability of lercanidipine decreases by 50%. This effect may also occur with simultaneous use with other beta-blockers, so dose adjustment of lercanidipine may be required to achieve a therapeutic effect with this combination.

Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme, therefore inhibitors and inducers of this isoenzyme, when used concomitantly, may affect the metabolism and excretion of lercanidipine. Concomitant use of lercanidipine with CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is not recommended.

Concomitant use of cyclosporine and lercanidipine is not recommended, as an increase in the plasma concentration of both substances is observed.

Caution should be exercised when lercanidipine is used concomitantly with other CYP3A4 substrates (terfenadine, astemizole, class III antiarrhythmic drugs, e.g., amiodarone, quinidine).

When lercanidipine is used concomitantly at a dose of 20 mg with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40%.

Lercanidipine should be prescribed with caution simultaneously with CYP3A4 inducers, for example, anticonvulsants (phenytoin, carbamazepine) and rifampicin, as a decrease in the antihypertensive effect of the drug is possible. Regular monitoring of blood pressure is necessary.

When lercanidipine was used concomitantly at a dose of 20 mg in patients continuously taking beta-methyldigoxin, no pharmacokinetic interaction was noted, while in healthy volunteers treated with digoxin, an increase in the C_max value for digoxin by an average of 33% was noted after taking 20 mg of lercanidipine on an empty stomach, while AUC and renal clearance changed insignificantly. It is necessary to monitor for signs of digoxin intoxication in patients taking digoxin and Lercanidipine simultaneously.

Concomitant use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in the plasma concentration of lercanidipine. With high doses of cimetidine, the bioavailability and antihypertensive effect of lercanidipine may increase.

With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), the AUC value for simvastatin increased by 56%, and the same value for its active metabolite – β-hydroxy acid – by 28% . Taking the drugs at different times of the day (Lercanidipine – in the morning, simvastatin – in the evening) can avoid unwanted interaction.

Enhancement of the antihypertensive effect is possible with simultaneous intake of grapefruit juice and lercanidipine.

Ethanol may potentiate the antihypertensive effect of lercanidipine.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.