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

Excipients: lactose monohydrate, corn starch, microcrystalline cellulose, silica colloidal anhydrous, magnesium stearate, sodium carboxymethyl starch, talc, giproloza, sucrose dioxide E 171 Titanium, povidone, Macrogol 6000, acacia gum, dye quinoline yellow E 104 opaglos white 6000.

Description:

Yellow, round, shiny, biconvex coated tablets.

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 anti-arthritic, anti-anginal and antihypertensive activity.

The drug reduces myocardial oxygen demand by reducing myocardial contractility and heart rate deceleration.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 vital slows atrioventricular conduction, inhibits sinus node automaticity, allowing to use 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:

If ingested, more than 90% of the dose taken is absorbed. Bioavailability is 10-20%. The maximum concentration of the drug in the blood plasma is achieved 1-2 hours after ingestion (80-400 ng / ml). Penetrates through blood-brain and placental barriers. Verapamil 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. Binding to 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. It is excreted in a small amount in unchanged 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 pectoris (Prinzmetal angina).

3. Treatment of arterial hypertension.

Contraindications:

Hypersensitivity to the components of the drug, pronounced bradycardia, cardiac insufficiency II B - III stage, 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 , syndrome of weakness of the sinus node, stenosis of the aortic estuary, Wolff-Parkinson-White syndrome,Morgagni-Adams-Stokes syndrome, acute heart failure, simultaneous use of beta-blockers (intravenously), pregnancy, lactation, age under 18 years (efficacy and safety not established).

Carefully:

Carefully it is necessary to appoint patients with atrioventricular blockade of I degree, chronic heart failure I-II degree, expressed violations of liver function, bradycardia, mild or moderate degree of arterial hypotension, myocardial infarction with left ventricular failure, renal failure, elderly age.

Dosing and Administration:

Verapamil is taken orally, during or after a meal,shekm 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 40-80 mg 3-4 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, excretion of verapamil from the body is slowed, so it is advisable to start treatment with minimal doses. The daily dose of the drug should not exceed 120 mg.

Side effects:

From the cardiovascular system: possible reddening of the face, expressed bradycardia, atrioventricular block, marked decrease in blood pressure, development or progression of heart failure, tachycardia; rarely - angina pectoris 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 the activity of "hepatic" enzymes 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 rash, skin itching, hyperemia of the skin of the face, multiforme exudative erythema (including syndrome Stevens-Johnson)

Other: an increase in body weight, very rarely - agranulocytosis, gynecomastia,

hyperprolactinemia, galactorrhea, arthritis, transient loss of vision against the background of the maximum concentration of the drug in the blood plasma (Cmah), pulmonary edema, thrombocytopenia (without clinical manifestations), peripheral edema.

Overdose:

Symptoms: sinus bradycardia, turning into atrioventricular blockade, sometimes asystole, marked decrease in blood pressure, heart failure, shock. Treatment: with 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; intravenous infusion of plasma-substituting solutions. Hemodialysis is not effective.

Interaction:

With the simultaneous use of verapamil with:

- antiarrhythmics, beta-blockers and inhalation anesthetics, there is an increase in 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 intensify the hypotensive effect of verapamil;

- 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 increases the risk of neurotoxic effects Verapamil the concentration in the blood of carbamazepine, muscle relaxants, 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, reduces the severity of antianginal, hypotensive and antiarrhythmic actions. Procainamide, quinidine and other drugs that cause lengthening of the interval QT, increase the risk of 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. Sympathomimetics reduce the hypotensive effect of verapamil.

Dysopyramide 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 lethal outcome).It is possible to increase the plasma concentrations of drugs characterized by a high degree of binding to proteins (in g.ch. derivatives of coumarin and indanedione, NSAIDs, quinine, salicylates, sulfinpyrazone).

Special instructions:

In order to increase blood pressure in patients with hypertrophic cardiomyopathy, alpha-adrenergic stimulants (phenylephrine); do not use isoprenaline and norepinephrine.

Before starting therapy for heart failure, it is necessary to achieve a state of compensation.

In the treatment it is necessary to control the function of the cardiovascular and respiratory systems, the level of glucose and blood electrolytes, the volume of circulating blood and the amount of excreted urine.

It is not recommended to stop treatment suddenly.

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

Form release / dosage:

The tablets covered with a cover, on 40 mg and 80 mg.

Packaging:

For 15 tablets in a blister is perforated from aluminum foil and PVC film.

2 blisters (30 tablets) together with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of 15-25 ° C. Keep out of the reach of children.

Shelf life:

5 years.Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N011991 / 01

Date of registration:05.09.2007 / 12.02.2010

Expiration Date:Unlimited

The owner of the registration certificate:Alkaloid, JSCAlkaloid, JSC Macedonia

Manufacturer: & nbsp

Alkaloid AO The Republic of Macedonia

Information update date: & nbsp28.01.2017

Illustrated instructions

Instructions

Verapamil (Verapamil)