Essential hypertension of mild or moderate severity.
LERCAMEN-20 TABLETS COMPOSITION
active substance: 1 coated tablet contains 20 mg lercanidipine hydrochloride, which corresponds to 18.8 mg lercanidipine
excipients: lactose, microcrystalline cellulose, sodium starch (type A), povidone K 30, magnesium stearate
shell: Opadry 02F25077 (hypromellose, talc, titanium dioxide (E 171), macrogol 6000, iron oxide (E172)).
LERCAMEN-20 TABLETS DOSAGE FORM
Basic physical and chemical properties: pink-colored round biconvex film-coated tablets with a notch for division on one side.
LERCAMEN-20 TABLETS PHARMACOLOGICAL GROUP
Selective calcium antagonists with a predominant effect on blood vessels. Derivatives of dihydropyridine.
ATX code С08С А13.
LERCAMEN-20 TABLETS PHARMACOLOGICAL PROPERTIES
Lercanidipine is a calcium antagonist of the dihydropyridine group that inhibits the transmembrane flow of calcium into heart cells and smooth muscle cells. The mechanism of the antihypertensive action of lercanidipine is due to a direct relaxing effect on the vascular muscles, as a result of which the total vascular peripheral resistance decreases. Despite the short half-life of lercanidipine, it has a prolonged hypotensive effect due to a high membrane separation coefficient and is devoid of negative inotropic action due to its high vascular selectivity. Since vasodilation caused by lercanidipine occurs gradually, acute arterial hypotension with reflex tachycardia in patients with arterial hypertension is rare.
Pharmacokinetics. Lercanidipine is completely absorbed after oral administration, and the maximum plasma concentration is reached after 1.5-3 hours.
Due to the high metabolism during the first passage through the liver, the bioavailability of lercanidipine taken by the patient after meals is approximately 10%, while it decreases to ⅓ of this value if the drug was used in 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 2:00 after eating very fatty foods, so it is advisable to take the drug on an empty stomach.
Distribution from blood plasma to tissues and organs is rapid and extensive. The degree of binding of lercanidipine to blood plasma proteins exceeds 98%. The free fraction of the drug may increase in patients with severely impaired renal and hepatic function, as this decreases the level of protein in the blood plasma.
Lercanidipine hydrochloride is extensively metabolized by the CYP 3A4 enzyme, the drug is not detected unchanged in urine and feces. It is mainly converted into inactive metabolites, about 50% of the dose taken is excreted in the urine. Excretion takes place mainly by biotransformation. The half-life is 8-10 hours, and the therapeutic effect lasts 24 hours due to the high degree of binding of lercanidipine to cell membrane lipids. With repeated application, no cumulation was observed.