Lecoptin coated tablets 40 mg. №50

Description

Lecoptin Composition
active substance: verapamil;

1 tablet contains verapamil hydrochloride 40 mg or 80 mg;

Excipients

40 mg tablets: corn starch, lactose, potato starch, croscarmellose sodium, talc, colloidal silicon dioxide, magnesium stearate, povidone, sodium carmellose, sucrose, polysorbate 80, calcium carbonate, quinoline yellow dye (E 104), titanium dioxide (E 171), capol 600.

Lecoptin Dosage form
Film-coated tablets.

Basic physical and chemical properties: yellow, round, biconvex film-coated tablets.

Lecoptin Pharmacotherapeutic group
Selective calcium channel blockers with direct effects on the heart. Phenylalkylamine derivatives. ATX code С08D A01.

Lecoptin Pharmacodynamics
Verapamil blocks the transmembrane flow of calcium ions into cardiomyocytes and vascular smooth muscle cells. It directly reduces myocardial oxygen demand by affecting energy-consuming metabolic processes in myocardial cells and indirectly affects a decrease in afterload. By blocking the calcium channels of the smooth muscle cells of the coronary arteries, blood flow to the myocardium increases even in the post-stenotic areas and the spasm of the coronary arteries is eliminated. The antihypertensive efficacy of verapamil is due to a decrease in peripheral vascular resistance without an increase in heart rate as a reflex response.

No undesirable changes in the physiological values ​​of blood pressure are observed. Verapamil has a pronounced antiarrhythmic effect, especially in supraventricular arrhythmias. It delays the conduction of the impulse in the atrioventricular node, as a result of which, depending on the type of arrhythmia, the sinus rhythm is restored and / or the ventricular rate is normalized. The normal heart rate level does not change or decreases slightly.

Pharmacokinetics
Verapamil hydrochloride is a racemic mixture consisting of equal parts of the R-enantiomer and the S-enantiomer. Verapamil is actively metabolized. Norrapamil is one of 12 metabolites that are detected in urine, has 10-20% of the pharmacological activity of verapamil and accounts for 6% of the excreted drug. Equilibrium plasma concentrations of norverapamil and verapamil are the same. Equilibrium concentration is achieved 3-4 days after repeated administration of the drug once a day.

Absorption

More than 90% of verapamil after administration is rapidly and almost completely absorbed in the small intestine. The average bioavailability in healthy volunteers after a single dose of the drug is 22%, which is explained by the extensive hepatic metabolism of the first pass. Bioavailability doubles after repeated administration.

The maximum concentration of verapamil in blood plasma (C max) is achieved within 1-2 hours after taking the immediate-release tablets, norverapamil – after 1 hour. Food intake does not affect the bioavailability of verapamil.

Distribution

Verapamil is widely distributed in body tissues, in healthy volunteers the volume of distribution is from 1.8 to 6.8 l / kg. Plasma protein binding of verapamil is approximately 90%.

Metabolism

Verapamil is actively metabolized. In the course of in vitro metabolic studies, it was found that verapamil is metabolized by cytochrome P450 CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18. It was found that after taking the drug by healthy male volunteers, verapamil hydrochloride undergoes intensive metabolism in the liver with the formation of 12 metabolites, most of which were detected in trace amounts. Major metabolites have been identified as the various N- and O-dealkylation products of verapamil. Among these metabolites, only norverapamil has a pharmacological effect (approximately 20% of the parent compound), as shown in studies in dogs.