Verapamil - instructions for use, dose, side effects, contraindications

Excipients (core): lactose monohydrate (sugar milk) - 40.90 mg, potato starch - 5.00 mg, povidone - 3.10 mg, microcrystalline cellulose - 10.00 mg, calcium stearate - 1.00 mg.

Excipients (shell): hypromellose - 1.80 mg, polysorbate-80 - 0.35 mg, titanium dioxide - 0.80 mg, talc - 0.05 mg.

Each 80 mg tablet contains active substance: verapamil hydrochloride 80 mg.

Excipients (core): lactose monohydrate (sugar milk) - 81,80 mg, potato starch - 10,00 mg, povidone - 6,20 mg, microcrystalline cellulose - 20,00 mg, calcium stearate - 2,00 mg.

Excipients (shell): hypromellose - 3.60 mg, polysorbate-80 - 0.70 mg, titanium dioxide - 1.60 mg, dye quinoline yellow - 0.10 mg.

Description:

Tablets with a dosage of 40 mg.

Biconvex tablets covered with a white sheath, on the fracture core and shell of uniform color.

Tablets with a dosage of 80 mg.

Biconvex tablets covered with a film coating of yellow color, on the fracture are visible two layers - the core of white color and a film coating of yellow color.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.D.A.01 Verapamil

C.08.D.A Phenylalkylamine derivatives

Pharmacodynamics:

Verapamil is one of the main drugs group of blockers of "slow" calcium channels. It has antiarrhythmic, anti-anginal and antihypertensive activity. The drug reduces the need for myocardium in oxygen by decreasing myocardial contractility and reducing the heart rate. Causes the enlargement of the coronary vessels of the heart and increases coronary blood flow; reduces the tone of the smooth muscles of peripheral arteries and the general peripheral vascular resistance. Verapamil significantly slows the atrioventricular conduction, depresses the automatism of the sinus node, which allows the use of the drug for the treatment of supraventricular arrhythmias. Verapamil is the drug of choice for the treatment of angina of vasospastic genesis (Prinzmetal angina). Has an effect with angina pectoris.

Pharmacokinetics:

When ingested absorbed more than 90 % of the dose. Bioavailability - 10 - 20%. The maximum concentration of the drug in the blood plasma is achieved 1-2 hours after oral administration (80 - 400 mg / ml). Verapamil penetrates through blood-brain and placental barriers. It is metabolized by the "first pass" through the liver. The main metabolites are norverapamil, N-dealkylnorverapamil. Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. Connection with blood plasma proteins - 90%. The half-life for a single dose is 2.8 - 7.4 hours; when taking repeated doses - 4,5 - 12 hours. Is displayed in small quantities in unaltered form (3-4 %), the rest - in the form of metabolites (70%) kidneys, about 25% - with bile. The secretion of breast milk is low.

Indications:

1. Treatment and prevention of cardiac arrhythmias:

paroxysmal supraventricular tachycardia;
flutter and atrial fibrillation (tachyarrhythmic variant);
supraventricular extrasystole.

2 Treatment and prevention:

chronic stable angina (stress angina);
unstable angina;
vasospastic angina (Prinzmetal angina, variant angina).

3. Treatment of arterial hypertension.

Contraindications:

Hypersensitivity to the components of the drug, pronounced bradycardia, chronic heart failure II B - III stage, severe arterial hypotension, cardiogenic shock (except for caused by arrhythmia), sinoauric blockade, atrioventricular blockade of II and III degree (excluding patients with an artificial pacemaker); acute myocardial infarction, sinus node weakness syndrome, aortic aortic stenosis, Wolff-Parkinson-White syndrome, Morgagni-Adams-Stokes syndrome, acute heart failure, simultaneous use of beta-blockers (intravenously), pregnancy, lactation, age 18 years.

Carefully:

With caution, it is necessary to prescribe the drug to patients with atrioventricular blockade of the 1st degree, chronic heart failure, expressed violations of the liver function, renal insufficiency, in old age, mild or moderate degree of arterial hypotension, myocardial infarction with left ventricular failure, bradycardia.

Dosing and Administration:

Verapamil is taken orally during or after a meal, with a small amount of water. The dosage regimen and duration of treatment are set individually, depending on the patient's condition, severity, the features of the course of the disease and the effectiveness of therapy.

To prevent attacks of angina pectoris, arrhythmia and in the treatment of hypertension, the drug is prescribed to adults at an initial dose of 40 to 80 mg 3 to 4 times a day. If necessary, increase the single dose to 120-160 mg. The maximum daily dose of the drug is 480 mg.

In patients with severe hepatic impairment, withdrawal of verapamil from the body is slow, so it is advisable to start treatment with minimal doses. The daily dose of the drug should not exceed 120 mg.

Side effects:

With the use of verapamil possible:

From the cardiovascular system: possible reddening of the face, pronounced bradycardia, atrioventricular block, marked decrease in blood pressure, development or worsening of heart failure, tachycardia; rarely - angina, up to the development of myocardial infarction (especially in patients with severe obstructive lesions of the coronary arteries), arrhythmias (including fibrillation and flutter of the ventricles).

From the gastrointestinal tract: nausea, vomiting, constipation (rarely - diarrhea), gingival hyperplasia, increased appetite; in some cases - a transient increase in "hepatic" transaminases and alkaline phosphatase in the blood plasma.

From the central nervous system: dizziness, headache, fainting, anxiety, retardation, fatigue, asthenia, drowsiness, depression, extrapyramidal disorders.

Allergic reactions: skin itch, skin rash, hyperemia of the facial skin, multiforme exudative erythema (including Stevens-Johnson syndrome).

Other: weight gain, very rarely - agranulocytosis, gynecomastia, hyperprolactinemia, galactorrhea, arthritis, transient loss of vision in the background of Cmah, pulmonary edema, thrombocytopenia, asymptomatic, peripheral edema.

Overdose:

Symptoms: sinus bradycardia, passing into atrioventricular blockade, sometimes asystole, marked decrease in arterial pressure, heart failure, shock.

Treatment for early detection - gastric lavage, Activated carbon; with rhythm and conduction disturbances - intravenous injection of isoprenaline, norepinephrine, atropine, 10 - 20 ml of 10% calcium gluconate solution, artificial pacemaker; IV infusion of plasma-substituting solutions. Hemodialysis is not effective.

Interaction:

At simultaneous reception of verapamil with:

· antiarrhythmic agents, beta-blockers and inhalation anesthetics observedincreased cardiotoxic effect (increased risk of atrioventricular blockade, a sharp decrease in heart rate, the development of heart failure, a sharp drop in blood pressure);

· antihypertensive agents and diuretics - it is possible to strengthen the hypotensive effect of verpamil;

· digoxin may increase the level of digoxin concentration in the blood plasma due to the deterioration of its excretion by the kidneys (therefore it is necessary to monitor the level of digoxin in the blood plasma in order to determine its optimal dosage and prevent intoxication);

· cimetidine and ranitidine elevates the level of concentration of verapamil in blood plasma;

· rifampicin, phenobarbital may reduce the concentration in the blood plasma and weaken the action of verapamil;

· theophylline, prazosin, cyclosporin, an increase in the concentration of these substances in the blood plasma is possible;

· muscle relaxants may enhance the muscle relaxant effect;

· Acetylsalicylic acid increases the possibility of bleeding;

· quinidine increases the level of concentration of quinidine in blood plasma, increases the threat of lowering blood pressure,and in patients with hypertrophic cardiomyopathy, the occurrence of severe arterial hypotension is possible;

· carbamazepine and lithium, the risk of neurotoxic effects increases;

· increases the concentration in the blood of valproic acid due to the suppression of metabolism involving cytochrome P450; .

· Calcium preparations reduce the effectiveness of verapamil;

· nicotine, accelerating metabolism in the liver, leads to a decrease in the concentration of verapamil in the blood;

· procainamide, quinidine and other drugs that cause lengthening of the interval QT, increase the risk of its significant lengthening;

· prazosin and other alpha-adrenoblockers increase the hypotensive effect;

· Non-steroidal anti-inflammatory drugs (NSAIDs) reduce the hypotensive effect due to suppression of prostaglandin synthesis, sodium retention and fluid in the body;

· increase the concentration of cardiac glycosides (requires careful monitoring and reduction of the dose of glycosides);

· sympathomimetics reduce the hypotensive effect of verapamil; disopyramide and flecainide should not be administered within 48 hours before or 24 hours after the use of verapamil (summation of a negative inotropic effect,up to a fatal outcome);

· exstrogens reduce the hypotensive effect due to fluid retention in the body;

· it is possible to increase the plasma concentrations of drugs characterized by a high degree of binding to proteins (including coumarin and indanedione derivatives, NSAIDs, quinine, salicylates, sulfinpyrazone).

Special instructions:

With an increase in blood pressure in patients with hypertrophic cardiomyopathy, alpha-adrenergic stimulants (phenylephrine); Do not use isoprenaline. Before starting therapy for heart failure, it is necessary to achieve a state of compensation. In the treatment it is necessary to monitor the function of the cardiovascular and respiratory systems, the content of glucose and blood electrolytes, the volume of circulating blood and the amount of urine released.

It is not recommended to stop treatment suddenly.

Effect on the ability to drive transp. cf. and fur:

Form release / dosage:

Tablets, film-coated 40 mg and 80 mg.

Packaging:10, 25, 30, 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50, 60 or 100 tablets into a polymer container for medicines.

One container or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002541

Date of registration:12.03.2012 / 21.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp29.01.2017

Illustrated instructions

Instructions

Verapamil (Verapamil)