ARITMIL [Verapamil] 5 mg Solution for IV injection

ARITMIL

instructions for medical use of the medicinal product

Tradename

Aritmil, Aritmil

International non-proprietary name

Composition

Each ampoule (2 ml solution) contains:

active ingredient: verapamil USP ( as verapamil ) hydrochloride 5 mg

excipients: water for injection, sodium chloride, hydrochloric acid as a pH regulator.

Dosage form

Solution for injection .

Pharmacotherapeutic group

Slow calcium channel blocker.

Pharmacological properties

Aritmil - belongs to the group of blockers of "slow" calcium channels. It has antiarrhythmic, antianginal and antihypertensive activity. The active substance is verapamil.

Pharmacodynamics

Verapamil blocks the transmembrane flow of calcium ions in cardiomyocytes and vascular smooth muscle cells. Verapamil reduces automatism, reduces the speed of impulse conduction and increases the refractory period in the cells of the conduction system of the heart. It delays the conduction of an impulse in the atrioventricular node and inhibits the automatism of the sinus node, which allows the drug to be used to treat supraventricular arrhythmias.

Pharmacokinetics

Verapamil is widely distributed in various tissues of the body, penetrates the blood-brain and placental barriers, into breast milk. Plasma protein binding is approximately 90%.

Verapamil is actively metabolized in the liver with the participation of cytochromes P450 CYP3A4, CYP1A2, CYP2C8, CYP2C9, CYP2C18. Norverapamil, one of 12 urinary metabolites, accounts for 10% to 20% of the hypothetical pharmacological activity of verapamil.

The elimination half-life is biphasic: the early period is about 4 minutes; final - 2-5 hours. Excreted by the kidneys 70% (unchanged 3-5%), with bile 25%. Not excreted by hemodialysis.

Indications for use

Relief of attacks of supraventricular paroxysmal tachycardia, paroxysms of atrial fibrillation and flutter, atrial extrasystole.

Contraindications

•          hypersensitivity to verapamil;

•          myocardial infarction complicated by bradycardia;

•          sick sinus syndrome;

•          cardiogenic shock;

•          atrioventricular block II and III degree;

•          Wolff-Parkinson-White syndrome;

•          severe arterial hypotension or left ventricular failure;

•          chronic heart failure IIB-III stage;

•          acute heart failure;

•          bradycardia less than 50 beats / min;

•          hypotension - systolic blood pressure less than 90 mm Hg;

•          simultaneous intravenous administration of beta-blockers.

Dosage and administration

Enter intravenously, stream, slowly over 2 minutes (under the control of blood pressure, heart rate and ECG) , 2-4 ml of solution (5-10 mg). Re-introduction can be carried out after 30 minutes. Maintenance drip administration is prepared by diluting 2 ml of the drug solution in 100-150 ml of isotonic sodium chloride solution.

At   elderly patients, the introduction is carried out for 3 minutes to reduce the risk of undesirable effects.

Special instructions and precautions

The drug is used with caution in patients with severe impaired liver and kidney function, atrioventricular blockade of the 1st degree, while taking beta-blockers, myocardial infarction with left ventricular failure, chronic heart failure stages I and IIA, old age.

Influence on the ability to drive vehicles and mechanisms

Use with caution in patients whose activities are associated with the need for a high concentration of attention (the reaction rate decreases).

Use during pregnancy and during breastfeeding

Use during pregnancy and during breastfeeding is contraindicated.

Interaction with other drugs

Increases the blood concentration of digoxin, theophylline, prazosin, cyclosporine, carbamazepine, muscle relaxants, quinidine, valproic acid due to the suppression of metabolism involving cytochrome P450.

Cimetidine increases the bioavailability of verapamil by almost 40% (by reducing metabolism in the liver), and therefore, it may be necessary to reduce the dose of the latter.

Calcium preparations reduce the effectiveness of verapamil. Rifampicin, barbiturates, nicotine, accelerating metabolism in the liver, lead to a decrease in the concentration of verapamil in the blood, reduce the severity of antianginal, hypotensive and antiarrhythmic action.

With simultaneous use with inhalation anesthetics, the risk of developing bradycardia, atrioventricular blockade, and heart failure increases. Procainamide, quinidine, and other drugs that prolong the QT interval increase the risk of a significant prolongation of the latter.

The combination with beta-blockers can lead to an increase in the negative inotropic effect, an increase in the risk of developing atrioventricular conduction disorders, bradycardia (the introduction of verapamil and beta-blockers must be carried out at intervals of several hours).

Prazosin and other alpha-blockers enhance the hypotensive effect. Non-steroidal anti-inflammatory drugs reduce the hypotensive effect due to the suppression of prostaglandin synthesis, retention of sodium ions and fluid in the body.

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

Sympathomimetics reduce the hypotensive effect of verapamil.

Disopyramide and flecainide should not be administered within 48 hours before and 24 hours after the use of verapamil (summation of negative inotropic effect, up to death).

Estrogens reduce the hypotensive effect due to fluid retention in the body. It is possible to increase plasma concentrations of drugs characterized by a high degree of protein binding (including coumarin and indandione derivatives, non-steroidal anti-inflammatory drugs, quinine, salicylates, sulfinpyrazone).

Drugs that reduce blood pressure increase the hypotensive effect of verapamil.

Increases the risk of a neurotoxic effect of lithium preparations. Enhances the activity of peripheral muscle relaxants (may require a change in dosing regimen).

Side effect

From the side of the cardiovascular system: severe bradycardia (at least 50 beats / min), a pronounced decrease in blood pressure, the development or aggravation of heart failure, tachycardia; it is possible to develop angina pectoris, up to myocardial infarction (especially in patients with severe obstructive lesions of the coronary arteries), arrhythmias (including ventricular fibrillation and flutter); with rapid administration - atrioventricular blockade of the III degree, asystole, collapse.

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

From the digestive system: nausea, increased activity of "liver" transaminases and alkaline phosphatase.

Allergic reactions: pruritus, rash, flushing of the skin of the face, erythema multiforme exudative (including Stevens-Johnson syndrome).

Other: pulmonary edema, asymptomatic thrombocytopenia, peripheral edema (swelling of the ankles, feet and legs).

Overdose

Symptoms: sinus bradycardia, turning into atrioventricular block, sometimes asystole, marked decrease in blood pressure, heart failure, shock, sinoatrial block.

Assistance: with bradycardia and conduction disorders - in / in the introduction of isoprenaline, atropine, 10-20 ml of a 10% solution of calcium gluconate, an artificial pacemaker; intravenous infusion of plasma-substituting solutions. To increase blood pressure in patients with hypertrophic obstructive cardiomyopathy, alpha-adrenergic stimulants (phenylephrine) are prescribed; isoprenaline and norepinephrine should not be used. Hemodialysis is not effective.

Storage conditions

Store in a dry place, at a temperature not exceeding 30°C.

Keep out of the reach of children!

Best before date

3 years. Do not use after the expiry date stated on the packaging.

Holiday conditions

Released by prescription.

Release form

5 ampoules of 2 ml in a blister pack. 2 packs together with instructions for use in a cardboard box.