Verapamil-LekT 80 mg tablets 50
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Active substance: Verapamila hydrochloride - 80 mg. Excipients of the nucleus: Lactose monohydrate (milk sugar) - 30 mg, potato starch - 43.6 mg, calcium stearate - 1.6 mg, talc - 4.8 mg,
Excipients of the shell: polysorbate-80 - 0.76 mg, titanium dioxide - 0.36 mg, methyl cellulose MC-15 - 2.512 mg, beeswax - 0.162 mg, petroleum jelly - 0.2 mg, dye tropeolin-O, or quinoline yellow E-104 - 0.006 mg.
Blocker of "slow" calcium channels (inhibits transmembrane transport of calcium ions to the contractile fibers of smooth muscle cells of the myocardium and coronary vessels). Has antianginal, antiarrhythmic, antihypertensive and hypotensive effect. The antianginal effect is associated both with a direct effect on the myocardium at the level of cellular metabolic processes, and with an indirect effect on the heart muscle by reducing the afterload. Blocking the flow of calcium ions to the contractile fibers of the smooth muscle cells of the coronary arteries, increases myocardial perfusion, even in post-stenotic areas, and eliminates, stops coronary spasm. The hypotensive effect of verapamil is due to a decrease in the total resistance of peripheral vessels without a compensatory increase in heart rate (HEART rate). Verapamil does not affect normal blood pressure (BP). Verapamil has a pronounced antiarrhythmic effect, especially with supraventricular arrhythmia, delays the conduction of the impulse in the atrioventricular (AV) node, as a result of which the sinus rhythm is restored and / or the frequency of ventricular contractions is normalized depending on the type of arrhythmia. Verapamil does not affect or slightly reduces heart rate. The onset of action when taken orally - after 1-2 hours, the maximum effect develops after 30-90 minutes, the duration of action is 8-10 hours.
When taken orally, it is rapidly absorbed in the small intestine, absorption - 90-92%, bioavailability after a single dose - 24-35% due to intensive metabolism during the initial passage through the liver and increases by 1.5-2 times with prolonged use. With prolonged use in increasing doses, bioavailability may increase. The time to reach the maximum concentration (TCmax) when ingested - 1-2 h. Maximum concentration - 80-400 ng / ml. Binding with plasma proteins - 90%. It penetrates the blood-brain barrier, the placental barrier and into breast milk (in low concentrations). It is rapidly metabolized in the liver by N-dealkylation and O-demethylation, with the formation of several metabolites (identified in humans 12). The accumulation of the drug and its metabolites in the body explains the increased action during the course of treatment. The main pharmacologically active metabolite is norvirapamil (20% of the hypotensive activity of verapamil). The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in the metabolism of verapamil. The half-life when ingested is 3-7 hours with a single dose, 4-12 hours - with prolonged use (due to the saturation of the enzyme systems of the liver and an increase in plasma concentrations, the half-life increases by almost 2 times). With liver failure, bioavailability increases and the half-life increases. It is excreted by 70% of the kidneys (3-5% unchanged), 16-25% - through the intestines. It is not excreted in hemodialysis.
Indications for use
- Treatment and prevention: chronic stable angina pectoris (angina pectoris); unstable angina; vasospastic angina (Prinzmetal angina, variant angina);
- Treatment of arterial hypertension.
With caution: Atrioventricular blockade of the first degree, chronic heart failure, arterial hypotension, bradycardia, hypertrophic obstructive cardiomyopathy, severe impairment of liver or kidney function, slowing of neuromuscular transmission (myasthenia gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy), advanced age. Pregnancy and lactation: Data on the clinical use of Verapamil-Ect during pregnancy are insufficient, so the drug should not be used during pregnancy. When using the drug Verapamil-LekT during lactation, it is necessary to stop breastfeeding.
Dosage and Administration
- Dosage form
- 80 mg
- Number of tablets
- INN Russian