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

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Dosage form: & nbspsolution for intravenous administration

Composition:

Each ampoule with 2 ml of the drug contains:

Active substance: verapamil hydrochloride 5.00 mg

Excipients: sodium chloride - 17.00 mg, citric acid monohydrate - 42.00 mg; sodium hydroxide - 16.80 mg; hydrochloric acid concentrated - 0.0054 ml; water for injections - up to 2.00 ml.

Description:

A clear, colorless solution.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

Pharmacodynamics:

Verapamil belongs to the group of blockers of "slow" calcium channels. Has antiarrhythmic, anti-anginal and antihypertensive activity.

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.

Has an effect in angina pectoris, as well as in the treatment of angina with supraventricular rhythm disorders.Suppresses metabolism involving cytochrome P450.

Pharmacokinetics:

It binds to blood plasma proteins by 90%. Penetrates through the blood-brain and placental barrier and into breast milk (in small amounts). Rapidly metabolized in the liver by N-dealkylation and O-demethylation with the formation of several metabolites. Accumulation of the drug and its metabolites in the body explains the increase in the effect of course treatment. The most significant metabolite is pharmacologically active norverapamil (20% of the hypotensive activity of verapamil). In the metabolism of the drug involved enzyme system CYP3A4, CYP3A5 and CYP3A7. The half-life period is biphasic: about 4 minutes-early and 2-5 hours-the final one. It is excreted by the kidneys 70% (unchanged 3-5%), with bile 25%. It is not excreted by hemodialysis.

Indications:

Suppression of seizures of supraventricular paroxysmal tachycardia; paroxysms of flicker and atrial flutter, atrial extrasystole.

Contraindications:

Hypersensitivity to the components of the drug, chronic heart failure IIB - grade III, arterial hypotension, acute myocardial infarction,sinoatrial block, sick sinus syndrome, aortic stenosis syndrome Morgagni-Adams-Stokes, digitalis intoxication, atrioventricular block II and III degree, ventricular tachycardia, cardiogenic shock, Wolff-Parkinson-White syndrome or Lown-Ganong-Levine combined with atrial flutter or atrial fibrillation (except for patients with a pacemaker), porphyria, pregnancy, lactation, parenteral administration during the previous 2 hours of a beta blocker, age 18 years (efficiency and security is not established).

Carefully:

Atrioventricular block I degree, bradycardia, patients taking beta-blockers, myocardial infarction with left ventricular failure, advanced age, chronic heart failure, and I II A degree, expressed violations of the liver and kidneys.

Dosing and Administration:

Administered intravenously, slowly, over at least 2 minutes in a continuous, monitoring of the electrocardiogram, heart rate and blood pressure. In elderly patients, the administration is carried out for at least 3 minutes to reduce the risk of unwanted effects.

To arrest paroxysmal arrhythmias of the heart rhythm, intravenously, struyno, (under the control of ECG and AD) for 2-4 ml of 0.25% solution (5-10 mg). If there is no effect, re-administration after 30 minutes at the same dose is possible.

A solution of verapamil is prepared by diluting 2 ml of 0.25% solution of the drug in 100-150 ml of a 0.9% solution of sodium chloride.

Side effects:

From the cardiovascular system: pronounced bradycardia (not less than 50d / min), pronounced decrease in arterial pressure, development or exacerbation of heart failure, tachycardia; possibly the development of angina pectoris, up to myocardial infarction (especially in patients with severe obstructive lesions of the coronary arteries), arrhythmias (including fibrillation and flutter of the ventricles); with rapid introduction - atrioventricular blockade III degree, asystole, collapse.

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

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

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

Other: transient loss of vision against the background of maximum concentration, pulmonary edema, thrombocytopenia asymptomatic, peripheral edema (swelling of the ankles, feet and shins).

Overdose:

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

Giving help: with bradycardia and conduction disorders - intravenous injection of isoprenaline, atropine, 10-20 ml of 10% calcium gluconate solution, artificial pacemaker; intravenous infusion of plasma-substituting solutions.

To increase blood pressure in patients with hypertrophic obstructive cardiomyopathy, alpha-adrenostimulators are prescribed (phenylephrine); do not use isoprenaline and norepinephrine. Hemodialysis is not effective.

Interaction:

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

Cimetidine increases bioavailability of verapamil by almost 40 % (due to a decrease in metabolism in the liver), in connection with which, it may be necessary to reduce the dose of the latter.

Calcium preparations reduce the effectiveness of verapamil.

Rifampicin, barbiturates, nicotine, accelerating the 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 bradycardia, atrioventricular blockade, and heart failure increases. Procainamide, quinidine and other drugs that cause lengthening of the interval QT, increase the risk of significant lengthening of the latter.

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-adrenoblockers increase the hypotensive effect. Nonsteroidal anti-inflammatory drugs reduce the hypotensive effect due to suppression of prostaglandin synthesis, delay of sodium ions and fluid in the body.

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

Sympathomimetics reduce the hypotensive effect of verapamil.

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

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

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

Increases the risk of neurotoxic effect of lithium drugs.

Strengthens the activity of peripheral muscle relaxants (may require a change in the dosage regimen).

Special instructions:

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. Can extend the interval PQ at a concentration in the blood plasma above 30 ng / ml. It is not recommended to stop treatment suddenly.

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

With caution apply during work drivers of vehicles and people whose profession is associated with increased concentration of attention (reduces the reaction rate).

Form release / dosage:

Solution for intravenous administration 2.5 mg / ml

Packaging:

2 ml of the drug in an ampoule of colorless neutral glass (I hydrolytic group) with a white stripe in place of the fault. For 5 ampoules in a contour squeeze box made of PVC, covered with aluminum foil. 2 contour packs (10 ampoules) or 10 out-of-round cell packs (50 ampoules), along with the instructions for use, are placed in a cardboard box.

Storage conditions:

In the dark place at a temperature of 15-25 ° 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:П N011991 / 02

Date of registration:18.07.2011

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)