Zanidip^®-Recordati (Tablets) Instructions for Use

Marketing Authorization Holder

Recordati Ireland Ltd. (Ireland)

Manufactured By

Recordati Industria Chimica E Farmaceutica S.p.A. (Italy)

Recordati Ilac Sanayi Ve Ticaret A.S. (Turkey)

ATC Code

C08CA13 (Lercanidipine)

Active Substance

Lercanidipine (Rec.INN registered by WHO)

Dosage Forms

	Zanidip^®-Recordati	Film-coated tablets, 10 mg: 7, 10, 14, 15, 20, 21, 25, 28, 30, 35, 40, 42, 45, 49, 50, 56, 60, 70, 75, 80, 84, 90, 98, 100, 105, 112, 120, 125, 140, 150, 168, 175, 180, 196 or 210 pcs.
		Film-coated tablets, 20 mg: 7, 10, 14, 15, 20, 21, 25, 28, 30, 35, 40, 42, 45, 49, 50, 56, 60, 70, 75, 80, 84, 90, 98, 100, 105, 112, 120, 125, 140, 150, 168, 175, 180, 196 or 210 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light yellow in color, round, biconvex, with a score on one side; light yellow at the fracture.

	1 tab.
Lercanidipine hydrochloride	10.0 mg

Excipients: lactose monohydrate, microcrystalline cellulose (type 101), sodium carboxymethyl starch (type A), povidone-K30, magnesium stearate.

Shell composition ready film coating [hypromellose, talc, titanium dioxide (E171), macrogol-6000, iron oxide yellow dye (E172)].

7 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
10 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
14 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
15 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
20 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
25 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
28 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.
30 pcs. – blisters (1, 2, 3, 4, 5, 6, 7) – cardboard packs.

Film-coated tablets, from pink to dark pink in color, round, biconvex, with a score on one side, light yellow at the fracture.

	1 tab.
Lercanidipine hydrochloride	20.0 mg

Excipients: lactose monohydrate, microcrystalline cellulose (type 101), sodium carboxymethyl starch (type A), povidone-K30, magnesium stearate.

Shell composition ready film coating [hypromellose, talc, titanium dioxide (E171), macrogol-6000, iron oxide red dye (E172)].

Clinical-Pharmacological Group

“Slow” calcium channel blocker. Antihypertensive drug

Pharmacotherapeutic Group

BMCC (Bone Mineral Crystal Complex)

Pharmacological Action

It is a slow calcium channel blocker, a dihydropyridine derivative. It inhibits the transmembrane calcium current into cardiomyocytes and smooth muscle cells.

The mechanism of the antihypertensive effect is due to a direct relaxing action on vascular smooth muscles, resulting in a decrease in total peripheral vascular resistance.

It has a prolonged antihypertensive effect. Due to high selectivity, it does not have a negative inotropic effect.

The duration of the therapeutic action is 24 hours.

Pharmacokinetics

After oral administration at a dose of 10-20 mg, it is completely absorbed.

The 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 average T_1/2 is 8-10 hours.

Indications

Mild to moderate essential arterial hypertension.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
I10	Essential [primary] hypertension

ICD-11 code	Indication
BA00.Z	Essential hypertension, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Take orally once daily.

Initiate therapy at 10 mg.

Administer at least 15 minutes before a meal, preferably in the morning.

If the therapeutic effect is insufficient after two weeks, increase the dose to 20 mg once daily.

Do not exceed the maximum daily dose of 20 mg.

For patients with mild to moderate hepatic or renal impairment, use with caution and consider a lower initial dose.

In elderly patients, initiate treatment at the recommended starting dose and monitor closely.

The tablet is scored and can be divided for dose titration only; do not crush or chew.

Swallow the tablet whole with a glass of water.

Regular blood pressure monitoring is essential to assess therapeutic response.

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose; in that case, continue with the regular schedule and do not take a double dose.

Adverse Reactions

From the cardiovascular system: effects associated with vasodilating 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 age 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.

Grapefruit juice may enhance the hypotensive effect of lercanidipine.

Ethanol may potentiate the effect of lercanidipine.

When used concomitantly with metoprolol, the bioavailability of lercanidipine decreases by 50%. This effect may also occur with concomitant 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 20 mg is used concomitantly with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40%.

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

When lercanidipine 20 mg was used concomitantly 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 observed 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 concomitantly.

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

When lercanidipine (20 mg) and simvastatin (40 mg) were used concomitantly, the AUC value for simvastatin increased by 56%, and the same value for its active metabolite, β-hydroxy acid, increased by 28% . Unwanted interaction can be avoided by taking the drugs at different times of the day (Lercanidipine – in the morning, simvastatin – in the evening).

Grapefruit juice may enhance the antihypertensive effect when taken concomitantly with 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.

Medical Disclaimer