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

talc - 1.90 mg or 3.80 mg, magnesium stearate - 0.82 mg or 1.64 mg; Excipients (shell): macrogol 4000, 0.29 or 0.72 mg, talc 0.29 mg or 0.72 mg, titanium dioxide 0.16 mg or 0.42 mg, quinoline yellow color 0.01 mg

or 0.02 mg, hypromellose 1.25 mg or 3.12 mg.

Description:The tablets covered with a cover from light yellow up to yellow-orange color, round, biconcave.

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 decreasing the frequency. heartbeats.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 in angina pectoris, as well as in the treatment of angina with supraventricular rhythm disorders.

Pharmacokinetics:

When ingested, more than 90% of the dose taken is absorbed. Bioavailability - 10-20%. The maximum concentration (Cmah) of the drug in the blood plasma is achieved 1 to 2 hours after ingestion (80-400 mg / ml). Verapamil permeates through blood-brain and placental barriers. It is metabolized by the "first pass" through the liver. The main metabolites are norverapamil, N-dialkylverapamil and 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 period / half-life with a single dose is 2.8 - 7.4 hours; at 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%) by the kidneys, about 25% - with bile. The secretion of breast milk is low.

Indications:

1. Treatment and prevention of cardiac arrhythmias:

paroxysmal supraventricular tachycardia;
chronic form of 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 verapamil and other components of the drug, pronounced bradycardia, chronic heart failure of 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, or Lawn syndrome-Ganonga-Levine (except for patients with a pacemaker), Morgagni syndrome - Adams - Stokes expressed by left ventricular dysfunction, atrial flutter or atrial fibrillation, congestive heart failure, the simultaneous use of beta blockers (iv), pregnancy, lactation, children under 18 years (efficacy and safety not established), simultaneous reception of colchicine.

Carefully:

With caution, it is necessary to appoint patients with atrioventricular blockade of I degree, idiopathic hypertrophic subaortic stenosis, chronic heart failure I-II A stage, expressed by violations of the liver and / or kidney function, arterial hypotension, bradycardia, in old age, with delayed neuromuscular transmission.

Dosing and Administration:

Verapamil is taken orally during or after a meal without rassasyvaya and not chewing, squeezed 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 40-80 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 for patients with severe hepatic insufficiency.

Side effects:

When using Verapamil, the following are possible:

- from the cardiovascular system: possible reddening of the face, pronounced bradycardia, atrioventricular blockade, a marked decrease in blood pressure, the appearance of symptoms of heart failure when using the drug in high doses, especially in predisposed patients, tachycardia; rarely - angina pectoris up to the development of myocardial infarction (especially in patients with severe obstructive lesions of the coronary arteries), arrhythmia (including fibrillation and flutter of the ventricles);

- from the gastrointestinal tract: nausea, vomiting, constipation, increased appetite, rarely - diarrhea; in some cases - a transient increase in the activity of "hepatic" transaminases and alkaline phosphatase in the blood plasma;

- from the central nervous system: dizziness, headache, fainting, anxiety, asthenia, drowsiness, depression, extrapyramidal disorders (ataxia, masky face, shuffling gait, stiffness of hands or feet, trembling of hands and fingers, difficulty swallowing), in rare cases - increased nervous excitability, inhibition , fatigue;

- allergic reactions: skin rash, itching, hyperemia of the skin of the face, multiforme exudative erythema (including Stevens-Johnson syndrome);

- Other: gynecomastia, hyperprolactinemia, gingival hyperplasia, weight gain, very rarely - agranulocytosis, galactorrhea, arthritis, transient loss of vision, pulmonary edema, thrombocytopenia asymptomatic, peripheral edema.

Overdose:

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

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 simultaneous application:

- enhances AUC (area under the concentration-time curve) of carbamazepine in patients with stable partial epilepsy (risk of side effects such as diplopia, headache, ataxia and dizziness).

- enhances AUC, Css (ground clearance) and Cmah (the maximum concentration of the drug) of cyclosporine.

- enhances AUC and Cmah of glibenclamide.

- increases the concentration of sirolimus and tacrolimus.

- significantly increases AUC and Cmbuspirone and midazolam.

- increases the concentration of theophylline (due to lower clearance), ethanol (and lengthens its effect), the concentration of quinidine (the risk of pronounced reduction in blood pressure).

- can increase the concentration of atorvastatin and lovastatin.

- increases significantly AUC and Cmah simvastatin.

- enhances AUC and Cmah almotriptan.

- increases the concentration of cardiac glycosides (requires careful monitoring and reduction of the dose of glycosides).

- enhances AUC and Cmmetoprolol and propranolol in patients with angina pectoris.

-increases the plasma concentration of colchicine (substrate for CYP3A and p-glycoprotein).

- when ingested significantly increases AUC and Cmah doxorubicin.

- slightly increases AUC imipramina; does not affect the concentration of the active metabolite, desipramine.

-increases Cmah prazosin and terazoand AUC terazosin.

- inhibitors CYP3A (including erythromycin, ritonavir and other antiviral HIV drugs), teligromycin increase plasma concentrations of verapamil.

- grapefruit juice increases AUC and CmOh R- and S- isomer of verapamil.

- cimetidine increases the bioavailability of verapamil by almost 40-50% (due to a decrease in liver metabolism), so it may be necessary to reduce the dose of the latter.

- rifampicin can significantly reduce bioavailability (up to 92%), and AUC and Cmah verapamil.

- Phenobarbital increases the clearance of verapamil 5 times.

- sulfinpyrazone increases the clearance of verapamil by about 3 times and reduces bioavailability (60%).

- preparations of St. John's wort penetrate lower AUC R- and S- isomer of verapamil and CmOh.

- while simultaneous use with inhalation anesthetics increases the risk of bradycardia, atrioventricular blockade, heart failure.

- combination with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of developing atrioventricular conduction disorders, bradycardia (the administration of verapamil and beta-blockers should be performed at intervals of several hours).

- prazosin and other alpha-blockers, as well as other antihypertensive drugs (ATP inhibitors, vasodilators, diuretics, beta-adrenoblockers) increase the hypotensive effect.

- disopyramide and flecainide should not be administered within 48 hours or 24 hours after the use of verapamil (summation of a negative inotropic effect, up to a lethal outcome).

- increases the risk of neurotoxic effect of lithium preparations.

- strengthens the action of peripheral muscle relaxants (a change in the dosage regimen may be required)

- while simultaneous use with acetylsalicylic acid (ASA), there was a slightly greater increase in bleeding time than with ASA alone.

- carbamazepine and lithium increases the risk of neurotoxic effects.

Special instructions:

To increase 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 compensated state.

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

It is not recommended to stop treatment suddenly.

Form release / dosage:

Tablets, film-coated, 40 mg and 80 mg.

Packaging:

10 tablets per contour cell pack.

50 tablets per can of polymeric materials.

2 or 5 contour mesh packages or 1 can of polymeric materials together with instructions for medical 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 date shown on the packaging.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008214/08

Date of registration:17.10.2008 / 11.02.2015

Expiration Date:Unlimited

The owner of the registration certificate:AVEKSIMA, JSC AVEKSIMA, JSC Russia

Manufacturer: & nbsp

IRBITSK HFZ, OJSC Russia

Information update date: & nbsp28.01.2017

Illustrated instructions

Instructions

Verapamil (Verapamil)