Lercamen-10 coated tablets 10 mg. №60

Description

Lercamen-10 tablets Storage

active substance: 1 film-coated tablet contains 10 mg of lercanidipine hydrochloride, which is equivalent to 9.4 mg of lercanidipine;

excipients: lactose monohydrate; microcrystalline cellulose; sodium starch glycolate (type A); povidone; magnesium stearate; shell Opadry OY-SR-6497; which includes: hypromellose, talc, titanium dioxide (E 171), polyethylene glycol, iron oxide (E 172).

Lercamen-10 tablets Dosage form

Film-coated tablets.

Main physical and chemical properties: yellow round biconvex tablets, film-coated, with a score line on one side.

Pharmacotherapeutic group. Selective calcium antagonists with the main effect on blood vessels. ATX code C08C A13.

Lercamen-10 tablets Pharmacological properties

Pharmacodynamics

Lercanidipine is a calcium antagonist of the dihydropyridine group, which inhibits the transmembrane influx of calcium into heart and smooth muscle cells. The mechanism of its action is due to the direct relaxing effect on the vascular muscles, which reduces the total peripheral vascular resistance. Despite the short half-life of lercanidipine, it has a prolonged antihypertensive effect due to the high coefficient of membrane distribution and is devoid of negative inotropic action due to its high vascular selectivity. Because lercanidipine-induced vasodilation occurs gradually, acute hypotension with reflex tachycardia in patients with hypertension is rare.

Pharmacokinetics

Lercanidipine is completely absorbed after oral administration, and the maximum concentration in blood plasma is reached in 1.5-3 hours. Due to the high metabolism during the first pass through the liver, the absolute bioavailability of lercanidipine taken by the patient after a meal is approximately 10%, and it decreases to 1/3 of this value if the drug was used by healthy volunteers on an empty stomach. The bioavailability of lercanidipine after oral administration is increased by 4 times if it is taken no later than 2 hours after eating a very fatty food, so the drug should be taken before meals. The degree of binding of lercanidipine to serum proteins exceeds 98%. Elimination occurs mainly through biotransformation. The mean half-life is 8-10 hours and the therapeutic effect lasts 24 hours due to the high degree of binding of lercanidipine to the lipid membrane. No accumulation was observed with repeated use. When lercanidipine is administered orally, its plasma concentration is not directly proportional to the dose taken (nonlinear kinetics). After taking 10, 20 and 40 mg, the maximum plasma concentrations observed were 1: 3: 8, and the areas under the plasma concentration-time curves were 1: 4: 18, indicating a gradual saturation of metabolism in first pass. Thus, the bioavailability of lercanidipine increases with increasing dose. The pharmacokinetics of lercanidipine in elderly patients and in patients with mild or moderate renal or hepatic impairment have been shown to be similar to those observed in the general population. In patients with severe renal dysfunction or in patients undergoing hemodialysis sessions, drug concentrations were higher (approximately 70%). In patients with moderate or severe hepatic impairment, the systemic bioavailability of lercanidipine is likely to increase because it is metabolised mainly in the liver.

Clinical characteristics

Indication.

Essential hypertension of mild or moderate severity.

Lercamen-10 tablets Contraindication

Hypersensitivity to the active substance, to other dihydropyridines or to any component of the drug. Women of childbearing potential if they do not use contraception. Obstruction of the vessels coming out of the left ventricle. Untreated congestive heart failure. Unstable angina. Severe hepatic or renal impairment. Within 1 month after myocardial infarction. Concomitant use with: strong CYP 3A4 inhibitors, cyclosporine and grapefruit juice.