Verapamil of / x t п / about 0,08 g No. 50

General characteristics. Structure:

Active agent – verapamil of a hydrochloride of 0,08 g (80 mg) and excipients: sugar milk, potato starch, talc, calcium stearate, an oksipropiltsellyuloza or methyl cellulose water-soluble, titanium dioxide, the twin – 80, tropeolin O or the KF yellow water-soluble dye – 6001.

Description: Tablets, coated yellow color, round biconvex form. On cross section two layers are visible.

Pharmacological properties:

Pharmacodynamics. Verapamil is one of the main drugs of group of blockers of "slow" calcium channels. It has antiarrhytmic, anti-anginal and anti-hypertensive activity. Drug reduces the need of a myocardium for oxygen due to decrease in contractility of a myocardium and reduction of heart rate. Causes expansion of coronary vessels of heart and increases a coronary blood stream; reduces a tone of smooth muscles of peripheral arteries and the general peripheric vascular resistance. Verapamil significantly slows down atrioventricular conductivity, automatism of a sinus node oppresses that allows to use drug for treatment of supraventricular arrhythmias. Verapamil is choice drug for treatment of stenocardia of vasospastic genesis (Printsmetal's stenocardia). Renders effect at an angina of exertion, and also at treatment of stenocardia with supraventricular disturbances of a rhythm.

Pharmacokinetics. At intake more than 90% of the accepted dose are soaked up. Bioavailability – 10-20%. The maximum concentration of drug in a blood plasma is reached in 1-2 hours after intake (80-400 ng/ml). Verapamil gets through hematoencephalic and placental barriers. Is exposed to metabolism at the first passing through a liver. The main metabolites are norverapamit, N-dealkilverapamil, N-dealkilnorverapamil. Accumulation of drug and its metabolites in an organism explains strengthening of action at course treatment. Linkng with proteins of a blood plasma – 90%. The elimination half-life at reception of a single dose makes 2,8-7,4 hours; at reception of repeated doses – 4,5 – 12 hours. Other part – in the form of metabolites (70%) by kidneys, about 25% - with bile is removed in a small amount in not changed look (3 – 4%). Secretion with breast milk low.

Indications to use:

1. Treatment and prevention of disturbances of a cordial rhythm:
- Bouveret's supraventricular disease;
- tremblings and atrial fibrillations (takhiaritmichesky option);
- supraventricular premature ventricular contraction;
2. Treatment and prevention:
- chronic stable stenocardia (angina of exertion);
- unstable stenocardia;
- vasospastic stenocardia (Printsmetal's stenocardia, alternative stenocardia);
3. Treatment of arterial hypertension.

Route of administration and doses:

The mode of dosing and duration of treatment are established individually depending on a condition of the patient, severity, features of a course of a disease and efficiency of therapy. For prevention of attacks of stenocardia, arrhythmia and at treatment of arterial hypertension drug is appointed by the adult in an initial dose on 40-80 mg by 3-4 times a day. If necessary increase a single dose to 120-160 mg.

Features of use:

For increase in arterial pressure at patients with a hypertrophic cardiomyopathy appoint alpha адреностимуляторы (Phenylephrinum); it is not necessary to apply изопреналин. Before therapy at heart failure it is necessary to reach the compensated state. At treatment control of function cardiovascular and respiratory systems, behind the content of glucose and electrolytes of blood, OTsK and amount of the emitted urine is necessary. It is not recommended to stop treatment suddenly.

Side effects:

- from cardiovascular system: face reddening, the expressed bradycardia, an atrioventricular block, the expressed lowering of arterial pressure, emergence of symptoms of heart failure when using drug in high doses, especially at predisposed patients is possible;
- from digestive tract: nausea, vomiting, locks; in some cases – tranzitorny increase in activity of "hepatic" transaminases and an alkaline phosphatase in a blood plasma;
- from TsNS: dizziness, a headache, in rare instances – the increased nervous irritability, block, fatigue;
- allergic reactions: skin rash, itch;
- others: development of peripheral hypostases, gynecomastia, giperprolaktinemiya, hyperplasia of gums.

Interaction with other medicines:

- antiarrhytmic means, beta adrenoblockers and inhalation anesthetics observe strengthening of cardiotoxic effect (increase in danger of emergence of an atrioventricular block, sharp decrease in heart rate, development of heart failure, sharp falling of arterial pressure);
- anti-hypertensive means and diuretics – strengthening of hypotensive effect of verapamil is possible; - digoxin increase in level of concentration of digoxin in a blood plasma in connection with deterioration in its removal by kidneys is possible (therefore it is necessary to carry out control of level of digoxin in a blood plasma for the purpose of identification of its optimum dosage and prevention of intoxication);
- Cimetidinum and ranitidine the level of concentration of verapamil in a blood plasma increases; - rifampicin, phenobarbital decrease in concentration in a blood plasma and weakening of effect of verapamil is possible; - theophylline, Prazozinum, cyclosporine increase in concentration of these substances in a blood plasma is possible;
- muscle relaxants strengthening of myorelaxation action is possible;
- acetylsalicylic acid possibility of bleedings amplifies;
- quinidine the level of concentration of quinidine in a blood plasma increases, the threat of a lowering of arterial pressure amplifies, and at patients with a hypertrophic cardiomyopathy developing of the expressed arterial hypotension is possible;
- carbamazepine and lithium danger of emergence of neurotoxic effects increases.

Contraindications:

Hypersensitivity to drug components, the expressed bradycardia, chronic heart failure of the II B – the III stages, arterial hypotension, cardiogenic shock (except for caused by arrhythmia), a sinoauricular block, an atrioventricular block of II and III degrees (excepting patients with an artificial pacemaker); an acute myocardial infarction, a sick sinus syndrome, a stenosis of the mouth of an aorta, a WPW-syndrome, Morganyi-Adams-Stokes's syndrome, an acute heart failure, simultaneous use of beta adrenoblockers (intravenously), pregnancy, the lactation period, age up to 18 years.
With care it is necessary to appoint drug sick with the atrioventricular block of the I degree, chronic heart failure expressed by abnormal liver functions. Route of administration and doses: Verapamil is accepted inside in time or after food, washing down with a small amount of water.

Overdose:

Overdose by drug: Symptoms: a sinus bradycardia, passing into an atrioventricular block, sometimes an asystolia, the expressed lowering of arterial pressure, heart failure, shock, sinuatrial blockade;
 Treatment: at early identification – a gastric lavage, absorbent carbon; at disturbance of a rhythm and conductivity – intravenous administration of an izoprenalin, Norepinephrinum, atropine, 10-20 ml of 10% of solution of calcium of a gluconate, an artificial pacemaker; in/in infusion of plasma substituting solutions. The hemodialysis is not effective.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C. Drug should be stored in the places unavailable to children. Period of validity: 3 years. Not to apply medicine after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 80 mg. On 50 tablets in bank of orange glass, or bank polymeric, or in a bottle polyethylene medical, or on 10 tablets in a blister strip packaging. Each can or a bottle, or on 1, 2 or 5 blister strip packagings together with the application instruction place in a pack from a cardboard.