Verapamil. Instructions for the drug, indications for use, price, analogs, release forms

The date: 04.11.2019

Description of the dosage form

Verapamil

Latin name
Release form

Pills

Compound

Verapamil hydrochloride

Package
pharmachologic effect

Verapamil is a class I selective calcium channel blocker, a diphenylalkylamine derivative. It has antianginal, antiarrhythmic and antihypertensive effects.

The antianginal effect is associated both with a direct effect on the myocardium and with an effect on peripheral hemodynamics (reduces the tone of peripheral arteries, OPSS). The blockade of calcium entry into the cell leads to a decrease in the transformation of energy contained in the macroergic ATP bonds into mechanical work, and a decrease in myocardial contractility. Reduces myocardial oxygen demand, has a vasodilating, negative foreign and chronotropic effect.

Verapamil significantly reduces AV conduction, lengthens the refractory period and suppresses the automatism of the sinus node. Increases the period of diastolic relaxation of the left ventricle, reduces the tone of the myocardial wall (is an adjunct for the treatment of hypertrophic obstructive cardiomyopathy). It has an antiarrhythmic effect in supraventricular arrhythmias.

Indications

Angina pectoris (tension, stable without angiospasm, stable vasospastic), supraventricular tachycardia (including paroxysmal, with WPW syndrome, Laun-Ganong-Levin syndrome), sinus tachycardia, atrial tachyarrhythmia, atrial flutter, atrial hypodermis hypertensive crisis (intravenous injection), hypertrophic obstructive cardiomyopathy, primary hypertension in the pulmonary circulation.

Contraindications

Severe arterial hypotension, AV block II and III degree, sinoatrial blockade and SSSU (except for patients with a pacemaker), WPW syndrome or Laun-Ganong-Levin syndrome in combination with atrial flutter or atrial fibrillation (except for patients with a pacemaker), pregnancy, period lactation, hypersensitivity to verapamil.

Method of administration and dosage

If necessary verapamil can be injected into / in a jet (slowly, under the control of blood pressure, heart rate and ECG). A single dose for adults is 5-10 mg, if there is no effect after 20 minutes, repeated administration at the same dose is possible. A single dose for children aged 6-14 years is 2.5-3.5 mg, 1-5 years old - 2-3 mg, up to 1 year old - 0.75-2 mg. For patients with severely impaired liver function, the daily dose of verapamil should not exceed 120 mg.

Maximum daily dose for adults when taken orally is 480 mg.

Shelf life
"

Selective Class I calcium channel blocker, diphenylalkylamine derivative
Drug: VERAPAMIL

The active substance of the drug: verapamil
ATX encoding: C08DA01
KFG: Calcium channel blocker
Registration number: P No. 013974/01
Date of registration: 14.08.08
Owner reg. ID: SHREYA LIFE SCIENCES Pvt. Ltd. (India)

Verapamil release form, drug packaging and composition.

Film-coated tablets 1 tab. verapamil hydrochloride 40 mg - "- 80 mg
Excipients: dibasic calcium phosphate, starch, butylhydroxyanisole, purified talc, magnesium stearate, gelatin, methylparaben, hydroxypropyl methylcellulose, titanium dioxide, indigo carmine.
10 pieces. - blisters (1) - cardboard packs.
10 pieces. - blisters (5) - cardboard packs.

DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information provided is presented only for familiarization with the drug, you should consult your doctor about the possibility of use.

Pharmacological action Verapamil

Selective class I calcium channel blocker derived from diphenylalkylamine. It has antianginal, antiarrhythmic and antihypertensive effects.
The antianginal effect is associated both with a direct effect on the myocardium and with an effect on peripheral hemodynamics (reduces the tone of peripheral arteries, OPSS). The blockade of calcium entry into the cell leads to a decrease in the transformation of the energy contained in the macroergic bonds of ATP into mechanical work, and a decrease in myocardial contractility. Reduces myocardial oxygen demand, has a vasodilating, negative foreign and chronotropic effect.
Verapamil significantly reduces AV conduction, lengthens the refractory period and suppresses the automatism of the sinus node. Increases the period of diastolic relaxation of the left ventricle, reduces the tone of the myocardial wall (is an adjunct for the treatment of hypertrophic obstructive cardiomyopathy). It has an antiarrhythmic effect in supraventricular arrhythmias.

Pharmacokinetics of the drug.

When taken orally, more than 90% of the dose is absorbed. Protein binding - 90%. Metabolized during the "first pass" through the liver. The main metabolite is norverapamil, which has less pronounced hypotensive activity than unchanged verapamil.
T1 / 2 when taking a single dose is 2.8-7.4 hours, when taking repeated doses - 4.5-12 hours (due to saturation of the liver enzyme systems and an increase in the concentration of verapamil in the blood plasma). After intravenous administration, the initial T1 / 2 is about 4 minutes, the final one is 2-5 hours.
It is excreted mainly by the kidneys and 9-16% through the intestines.

Indications for use:

Dosage and method of administration of the drug.

Individual. Inside for adults - at an initial dose of 40-80 mg 3 times / day. For dosage forms of prolonged action, the single dose should be increased and the frequency of administration should be decreased. Children aged 6-14 years old - 80-360 mg / day, up to 6 years old - 40-60 mg / day; the frequency of admission is 3-4 times / day.
If necessary, verapamil can be injected intravenously in a jet (slowly, under the control of blood pressure, heart rate and ECG). A single dose for adults is 5-10 mg, if there is no effect after 20 minutes, repeated administration at the same dose is possible. A single dose for children aged 6-14 years is 2.5-3.5 mg, 1-5 years - 2-3 mg, up to 1 year - 0.75-2 mg. For patients with severely impaired liver function, the daily dose of verapamil should not exceed 120 mg.
Maximum dose: for adults when taken orally - 480 mg / day.

Side effects of Verapamil:

From the side of the cardiovascular system: bradycardia (less than 50 beats / min), a marked decrease in blood pressure, development or worsening of heart failure, tachycardia; rarely - angina pectoris, up to the development of myocardial infarction (especially in patients with severe obstructive coronary artery disease), arrhythmia (including fibrillation and flutter of the ventricles); with rapid intravenous administration - AV block of the III degree, asystole, collapse.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, fainting, anxiety, lethargy, fatigue, asthenia, drowsiness, depression, extrapyramidal disorders (ataxia, mask-like face, shuffling gait, stiffness of the hands or feet, trembling of the hands and fingers, difficulty swallowing).
From the digestive system: nausea, constipation (rarely diarrhea), gingival hyperplasia (bleeding, soreness, swelling), increased appetite, increased activity of hepatic transaminases and alkaline phosphatase.
Allergic reactions: pruritus, skin rash, facial flushing, erythema multiforme exudative (including Stevens-Johnson syndrome).
Others: weight gain, very rarely - agranulocytosis, gynecomastia, hyperprolactinemia, galactorrhea, arthritis, transient loss of vision against the background of Cmax, pulmonary edema, asymptomatic thrombocytopenia, peripheral edema.

Contraindications to the drug:

Application during pregnancy and lactation.

Verapamil is contraindicated during pregnancy and lactation.

Special instructions for the use of Verapamil.

It should be used with caution in case of AV blockade of the 1st degree, bradycardia, severe stenosis of the aortic orifice, chronic heart failure, with mild or moderate arterial hypotension, myocardial infarction with left ventricular failure, hepatic and / or renal failure, in elderly patients, in children and adolescents under the age of 18 (efficacy and safety of use have not been studied).
If necessary, combined therapy of angina pectoris and arterial hypertension with verapamil and beta-blockers is possible. However, intravenous administration of beta-blockers should be avoided while using verapamil.
Influence on the ability to drive vehicles and control mechanisms
After taking verapamil, individual reactions (drowsiness, dizziness) are possible, affecting the patient's ability to perform work that requires a high concentration of attention and the speed of psychomotor reactions.

Interaction of Verapamil with other drugs.

With simultaneous use with antihypertensive drugs (vasodilators, thiazide diuretics, ACE inhibitors), there is a mutual strengthening of the antihypertensive effect.
With simultaneous use with beta-blockers, antiarrhythmic agents, agents for inhalation anesthesia, the risk of developing bradycardia, AV blockade, severe arterial hypotension, heart failure increases, due to the mutual strengthening of the inhibitory effect on the automatism of the sinoatrial node and AV conduction, contractility and conductivity myocardium.
With parenteral administration of verapamil to patients who have recently received beta-blockers, there is a risk of arterial hypotension and asystole.
With simultaneous use with nitrates, the antianginal effect of verapamil is enhanced.
With simultaneous use with amiodarone, the negative inotropic effect, bradycardia, conduction disturbances, AV blockade are enhanced.
Since verapamil inhibits the isoenzyme CYP3A4, which is involved in the metabolism of atorvastatin, lovastatin and simvastatin, drug interactions are theoretically possible due to an increase in plasma concentrations of statins. Cases of the development of rhabdomyolysis are described.
With simultaneous use with acetylsalicylic acid, cases of an increase in bleeding time due to an additive antiplatelet effect have been described.
With simultaneous use with buspirone, the concentration of buspirone in the blood plasma increases, its therapeutic and side effects increase.
With simultaneous use, cases of an increase in the concentration of digitoxin in the blood plasma have been described.
With simultaneous use with digoxin, the concentration of digoxin in the blood plasma increases.
With simultaneous use with disopyramide, severe arterial hypotension and collapse are possible, especially in patients with cardiomyopathy or decompensated heart failure. The risk of developing severe manifestations of drug interactions is apparently associated with an increase in the negative inotropic effect.
With simultaneous use with diclofenac, the concentration of verapamil in the blood plasma decreases; with doxorubicin - the concentration of doxorubicin in the blood plasma increases and its effectiveness increases.
With simultaneous use with imipramine, the concentration of imipramine in the blood plasma increases and there is a risk of developing unwanted changes on the ECG. Verapamil increases the bioavailability of imipramine by decreasing its clearance. Changes in the ECG are due to an increase in the concentration of imipramine in the blood plasma and the additive inhibitory effect of verapamil and imipramine on AV conduction.
With simultaneous use with carbamazepine, the effect of carbamazepine increases and the risk of side effects from the central nervous system increases due to inhibition of the metabolism of carbamazepine in the liver under the influence of verapamil.
With simultaneous use with clonidine, cases of cardiac arrest in patients with arterial hypertension have been described.
When used simultaneously with lithium carbonate, the manifestations of drug interactions are ambiguous and unpredictable. Cases of increased effects of lithium and the development of neurotoxicity, a decrease in the concentration of lithium in the blood plasma, and severe bradycardia are described.
The vasodilating effect of alpha-blockers and calcium channel blockers can be additive or synergistic. With the simultaneous use of terazosin or prazosin and verapamil, the development of severe arterial hypotension is partially due to pharmacokinetic interaction: an increase in Cmax and AUC of terazosin and prazosin.
With simultaneous use, rifampicin induces the activity of liver enzymes, accelerating the metabolism of verapamil, which leads to a decrease in its clinical efficacy.
With simultaneous use, the concentration of theophylline in the blood plasma increases.
With simultaneous use with tubocurarine chloride, vecuronium chloride, it is possible to enhance the muscle relaxant effect.
With simultaneous use with phenytoin, phenobarbital, a significant decrease in the concentration of verapamil in the blood plasma is possible.
With simultaneous use with fluoxetine, the side effects of verapamil are enhanced due to a slowdown in its metabolism under the influence of fluoxetine.
With simultaneous use, the clearance of quinidine decreases, its concentration in the blood plasma increases and the risk of side effects increases. Cases of arterial hypotension have been observed.
With the simultaneous use of verapamil inhibits the metabolism of cyclosporine in the liver, which leads to a decrease in its excretion and an increase in plasma concentration. This is accompanied by an increase in the immunosuppressive effect, a decrease in the manifestations of nephrotoxicity is noted.
With simultaneous use with cimetidine, the effects of verapamil are enhanced.
With simultaneous use with enflurane, prolongation of anesthesia is possible.
When used simultaneously with etomidate, the duration of anesthesia increases.

Content

At the present time, a huge number of medicines for various diseases are sold, but ordinary people without medical education can find it very difficult to deal with them. Many experts prescribe Verapamil - the instructions for the use of which explain why this drug is prescribed for the treatment, what effect it has. If you are going to buy and use this medicine, read about all its features.

What is Verapamil

This medicine belongs to the group of antiarrhythmic, antianginal. Verapamil is a slow calcium channel blocker. Its action is aimed at slowing down the pulse and reducing the load on the heart. The drug is sold by a doctor's prescription, which is indicated by its instructions for use. The medicine is prescribed for various pathologies of a vascular nature, some types of arrhythmias.

Compound

Verapamil is available in tablets, dragees and ampoules. The composition depends on the shape you choose. One tablet contains the following:

40 or 80 mg of verapamil hydrochloride;
potato starch, polyethylene glycol, lactose, paraffin, avicel, polyvidone K 25, magnesium stearate, talc, gum arabic, silicon dioxide, gelatin, sucrose.

One tablet of the drug contains:

40, 80, 120 or 240 mg of verapamil hydrochloride;
methylparaben, indigo carmine, dibasic calcium phosphate, gelatin, hydroxypropyl methylcellulose, magnesium stearate, starch, butylhydroxyanisole, purified talc, titanium dioxide.

A 2 ml ampoule of the drug contains:

5 mg verapamil hydrochloride;
citric acid monohydrate, water for injection, sodium chloride, sodium hydroxide, concentrated hydrochloric acid.

Release form

You can buy these types of drugs:

Verapamil tablets in a film shell with a concentration of 40, 80, 120 mg. 10 pieces in a blister. 2, 5 or 10 records in one cardboard box.
Verapamil in 2 ml ampoules. 10 pieces per pack.
Verapamil retard. Extended-release tablets with a dosage of 240 mg. Pack of 20.
Dragee with a dosage of 40 or 80 mg. Pack of 20, 30 or 50.

Mechanism of action

The drug blocks calcium channels. This provides three effects:

coronary vessels dilate;
blood pressure decreases;
the heart rate is normalized.

Thanks to the drug, the myocardium contracts less often. The drug reduces the tone of the smooth muscles of the peripheral arteries and the general vascular resistance. This ensures a drop in blood pressure. Acting on the atrioventricular node and restoring sinus rhythm, Verapamil has an antiarrhythmic effect. The drug inhibits platelet adhesion and is not addictive. Intensive metabolism, the concentration of the maximum level in the blood plasma after 1-2 hours, excretion from the body is rapid.

Indications for use

According to the instructions, the drug Verapamil can be prescribed in the following cases:

angina pectoris;
arterial hypertension;
tachycardia: sinus, atrial, supraventricular;
hypertensive crisis;
primary hypertension;
supraventricular extrasystole;
vasospastic angina pectoris;
hypertrophic cardiomyopathy;
coronary heart disease;
flutter and atrial fibrillation;
paroxysmal supraventricular tachycardia;
stable exertional angina;
atrial fibrillation.

Instructions for the use of Verapamil

There can be no uniform guidelines for the use of the drug, therefore the most common options will be considered below. Verapamil - the instructions for the use of which are always detailed in the annotation should be prescribed to you by the doctor. The form of the prescribed drug, the dosage and the scheme of use depends on the age of the patient, his diagnosis, what drugs he will take additionally.

Pills

The drug of this form is consumed with food or a few minutes after, washed down with a small amount of pure non-carbonated water. Dosage options and duration of treatment with Verapamil:

Adults and adolescents weighing more than 50 kg, 40-80 mg 3-4 times a day with the same interval. The dose may be increased, but should not exceed 480 mg.
A child under 6 years of age with a heart rhythm disorder 80-120 mg of Verapamil, divided into 3 doses.
Children 6-14 years old 80-360 mg for 2 doses.
Long-acting verapamil is prescribed only by the attending physician. The frequency of reception is reduced.

In ampoules

Rules for the use of Verapamil indicated by the instructions:

The drug is administered intravenously through a dropper, slowly, especially if the patient is elderly. 2 ml of the drug is diluted with 100 ml of 0.9% sodium chloride solution.
To stop heart rhythm disturbances, it is recommended to apply 2-4 ml of Verapamil (1-2 ampoules). Injection through the vein is jet.
Treatment of children under one year old is carried out in exceptional cases for health reasons. The dosage is calculated individually, taking into account weight, age, and other characteristics.
Children 1-5 years old are injected with 0.8-1.2 ml of Verapamil intravenously.
At the age of 6-14 years, 1-2 ml of the drug is prescribed.

During pregnancy

According to the instructions, the use of Verapamil by girls in an "interesting position" is advisable when:

the risk of premature birth (in combination with other drugs);
ischemic heart disease;
placental insufficiency;
treatment and prevention of arrhythmias;
nephropathy of pregnant women;
hypertension (including crisis);
different types of angina pectoris;
idiopathic hypertrophic subaortic stenosis;
hypertrophic cardiomyopathy;
blocking the side effects of drugs that increase the heart rate (for example, Ginipral).

Pregnancy dosage:

40-80 mg 3-4 times a day. Better not to increase the dose.
Maximum 120-160 mg at a time.

Peculiarities:

Reception in the first trimester only on strict indications.
It is advisable to start drinking Verapamil from 20-24 weeks of pregnancy.
Discontinue use 1-2 months before delivery.

Side effects

When Verapamil is taken in the body, atypical reactions can be observed, especially if an overdose is allowed. The occurrence of such side effects is possible when using:

Cardiovascular system and blood. Arterial hypotension, symptoms of heart failure, sinus bradycardia, tachycardia. Rare side effects: angina pectoris, heart attack, arrhythmia.
Digestive system. Nausea, diarrhea, constipation, bleeding and soreness of the gums, increased appetite.
Nervous system. Dizziness, difficulty swallowing, headache, tremor of fingers, fainting, limited mobility, anxiety, shuffling gait, lethargy, ataxia, fatigue, mask-like face, asthenia, depression, drowsiness.
Allergic reactions. Exudative erythema, itching and skin rash, hyperemia.
Other. Weight gain, pulmonary edema, agranulocytosis, vision loss, gynecomastia, arthritis, hyperprolactinemia, arthritis, galactorrhea.

Contraindications

The use of Verapamil is prohibited when:

severe arterial hypotension;
hypersensitivity to substances in the composition;
AV blockade of 2-3 degrees;
lactation period;
cardiogenic shock;
severe aortic stenosis;
myocardial infarction;
sick sinus syndrome;
digitalis intoxication;
sinoatrial blockade;
flutter and atrial fibrillation;
severe bradycardia;
SSSU;
severe LV dysfunction.

kidney failure;
pregnancy;
chronic heart failure;
abnormal liver function;
ventricular tachycardia;
AV blockade of 1 degree;
moderate to mild hypotension;
severe myopathy.

Interaction

If the doctor has prescribed Verapamil for you - the instructions for the correct use of which are very detailed, be sure to tell him what other drugs you are taking. He can change his action in one direction or another when interacting with:

Prazorin;
Ketoconazole and Itraconazole;
Aspirin;
Atenol;
Timolol;
Metoprol;
Anaprilin;
Nadolol;
Carbamazepine;
Cimetidine;
Clarithromycin;
Cyclosporine;
Digoxin;
Disopravmid;
Indinavir;
Viracept;
Ritonavir;
Quinidine;
drugs against increased blood pressure;
diuretics;
Erythromycin;
Flecainide;
cardiac glycosides;
Nefazodone;
Phenobarbital;
Theophylline;
Pioglitazone;
Telithromycin;
Rifampicin.

Analogs

Preparations that contain the same main component, or have a similar effect on the body:

Verogalid;
Veratard;
Finoptin;
Verapabene;
Isoptin;
Atsupamil;
Lecoptin;
Veramil;
Lecoptin;
Gallopamil;
Nimodipine;
Nifedipine;
Ryodipin;
Amlodipine;
Nicardipine;
Flamon;
Kaveril;
Falicard;
Veracard.

Price

The cost of Verapamil depends on the form of release, manufacturer, packaging. The drug can be ordered in the catalog of an ordinary pharmacy or bought in an online store, according to reviews, quite inexpensively. You can find approximate prices for it in the table:

Video: Medicine Verapamil

Attention! The information presented in the article is for informational purposes only. The materials of the article do not call for self-treatment. Only a qualified doctor can diagnose and give recommendations for treatment, based on the individual characteristics of a particular patient.

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Formula: C27H38N2O4, chemical name: alpha-methylamino] propyl] -3,4-dimethoxy-alpha- (1-methylethyl) benzeneacetonitrile (and as hydrochloride).
Pharmacological group: organotropic agents / cardiovascular agents / class 1 selective calcium channel blockers / diphenylalkylamine derivative.
Pharmachologic effect: antiarrhythmic, hypotensive, antianginal.

Pharmacological properties

Verapamil has a blocking effect on calcium channels (acts on the inner side of the cell membrane) and reduces the transmembrane calcium current. The degree of interaction with the channel is determined by the level of membrane depolarization: verapamil most effectively blocks the open channels of the depolarized membrane. Less affects the closed channels with a polarized membrane, preventing their activation. It has little effect on both alpha-adrenergic receptors and sodium channels. Verapamil reduces contractility, conduction velocity in the AV node, pacemaker frequency in the sinus node, AV and sinoatrial conduction, total peripheral vascular resistance, afterload, causes peripheral vasodilation, relaxes smooth muscles (mainly in arterioles, less in veins). Increases myocardial perfusion, reduces the difference between the supply and the heart's need for oxygen, promotes the reverse development of left ventricular hypertrophy, and lowers blood pressure. Removes spasms of the coronary arteries with angina pectoris and prevents their development. In patients with uncomplicated hypertrophic cardiomyopathy, it improves the outflow of blood from the ventricles. Reduces the severity and frequency of vascular headaches. Verapamil inhibits neuromuscular transmission in Duchenne pseudohypertrophic myopathy and prolongs the recovery period after using vecuronium. Blocks the P170 enzyme in vitro and partially eliminates the resistance of cancer cells to chemotherapeutic drugs. After the use of verapamil, more than 90% of the drug dose is absorbed inside, but the bioavailability is only 20–35% due to metabolism in the liver during the first passage, bioavailability increases with prolonged use in large doses. The maximum concentration is reached after 1 - 2 hours for tablets, after 5 - 7 hours for prolonged-release tablets, after 7 - 9 hours for extended-release capsules. It binds to plasma proteins by 90%. In the liver, verapamil is metabolized to form norverapamil, which has 20% of the hypotensive activity of verapamil, and other metabolites (which are determined in small amounts). The half-life when using a single dose inside is 2.8-7.4 hours, with repeated doses - 4.5-12 hours (due to saturation of the hepatic enzyme systems). When administered intravenously, the elimination half-life has two phases: early - about 4 minutes, final - 2-5 hours. When used internally, the onset of the effects is noted after 1-2 hours. Under conditions of intravenous administration, the antiarrhythmic effect develops within 1-5 minutes (usually less than 2 minutes), hemodynamic effects in 3-5 minutes. The duration of the effects is 8-10 hours for tablets or 24 hours for extended-release tablets and capsules. When administered intravenously, the antiarrhythmic effect lasts about 2 hours, the hemodynamic effect lasts 10–20 minutes. It is excreted mainly by the kidneys, about 16% with feces.
Verapamil passes into breast milk and through the placenta, is determined in childbirth in the blood of the umbilical vein. Rapid intravenous administration induces maternal hypotension, which leads to fetal distress.
With prolonged use, clearance decreases and bioavailability increases. In severe liver dysfunctions, plasma clearance is reduced by 70% and the elimination half-life is increased to 14-16 hours. According to the results that were obtained in 2-year experiments on rats using doses that are 12 times higher than the MRDC, and in the Ames bacterial tests, verapamil does not have mutagenic and carcinogenic activity. In experiments on rats at doses that are 6 times higher than those recommended for humans, verapamil inhibits fetal growth and increases the frequency of intrauterine fetal death.

Indications

Supraventricular paroxysmal tachycardia (with the exception of WPW syndrome), atrial premature beats, sinus tachycardia, atrial flutter and atrial fibrillation, angina pectoris (including exertional angina, Prinzmetal, postinfarction), arterial hypertension, hypertrophic cardiac arrest and diopathic stenocardia, hypertrophic crisis and diopathic stenocardia

Dosing and administration of verapamil

Using verapamil inside. The duration of treatment and the dosage regimen are set individually and depend on the patient's condition, characteristics of the course and severity of the disease, and the effectiveness of treatment. For the prevention of arrhythmia, angina pectoris and for the treatment of arterial hypertension, adults are prescribed an initial dose of 40–80 mg 3-4 times a day (for prolonged forms, the frequency of administration is reduced), washed down with a small amount of water before meals. If necessary, a single dose can be increased to 120–160 mg. The maximum daily dose is 480 mg. In patients with severe liver dysfunctions, the elimination of verapamil is slow, so it is better to start therapy with minimal doses; the daily dose should be no more than 120 mg. The use of verapamil intravenously. To be administered slowly: the initial dose for adults is 5-10 mg (to be administered for at least 2 minutes) under the control of an ECG, pulse rate, blood pressure; if the effectiveness is insufficient, it is possible to repeat the administration in half an hour at a dose of 10 mg. Children under 1 year old for at least 2 minutes 0.1-0.2 μg / kg (usually a single dose of 0.75-2 mg), children 1-15 years old for at least 2 minutes 0.1-0.3 mg / kg (usually a single dose of no more than 2–5 mg). In hypertensive crisis intravenously slowly 5-10 mg.
If you skip the next dose of verapamil, do it, when you remember, make the next dose after the set time from the last use.
Use with caution in patients with hypertrophic cardiomyopathy, which is complicated by high wedge pressure in the pulmonary capillaries, left ventricular obstruction, orthopnea or paroxysmal nocturnal dyspnea, sinus-atrial node dysfunction. When used in patients with severe disorders of neuromuscular transmission (Duchenne myopathy) and liver function, constant monitoring by a doctor and, possibly, a decrease in the dose of the drug is necessary. Use with caution for drivers during work and for people whose professions are associated with a high concentration of attention (since verapamil decreases the reaction rate). During therapy with verapamil, it is recommended to exclude alcohol intake. The injectable form of verapamil can precipitate in solution with a pH greater than 6.0.

Contraindications for use

Hypersensitivity, cardiogenic shock, severe hypotension (systolic blood pressure less than 90 mm Hg), AV block 3 and 2 degrees, severe bradycardia (pulse rate less than 50 beats / min), myocardial infarction (recent or acute and complicated by bradycardia , hypotension, left ventricular failure), chronic heart failure stage 3, atrial fibrillation and flutter and Laun-Ganong-Levin syndrome (except for patients with a pacemaker) or WPW syndrome, sick sinus syndrome (if there is no pacemaker), Morgagni-Adams syndrome - Stokes, sinoatrial block, digitalis intoxication, pregnancy, severe aortic stenosis, breastfeeding.

Restrictions on the use of verapamil

AV block of 1 degree, mild or moderate hypotension, chronic heart failure of 2 and 1 stages, severe myopathy (Duchenne syndrome), hepatic and / or renal failure, for intravenous administration of ventricular tachycardia with a wide QRS complex.

Application during pregnancy and lactation

The use of verapamil during pregnancy and lactation is contraindicated.

Side effects of verapamil

Digestive system: nausea, dyspepsia, constipation, rarely - increased activity of alkaline phosphatase and hepatic transaminases, gingival hyperplasia;
nervous system: headache, nervousness, dizziness, lethargy, weakness, drowsiness, paresthesia, fatigue; allergic reactions: skin rash and itching, urticaria, rarely - Stevens-Johnson syndrome, angioedema;
circulatory system: sinus bradycardia, arterial hypotension, AV block, at high doses - the appearance of symptoms of heart failure;
others: bronchospasm (when administered intravenously), peripheral edema, hyperemia of the facial skin, very rarely - gynecomastia, increased secretion of prolactin (in some cases).

Interaction of verapamil with other substances

Increases plasma concentration of digoxin, theophylline, cyclosporine, carbamazepine, reduces - lithium preparations. Reduces the antibacterial activity of rifampicin, deprimatory effects of phenobarbital, reduces the clearance of propranolol and metoprolol, increases the effects of muscle relaxants. Rifampicin, phenobarbital, sulfinpyrazone, vitamin D, calcium salts - reduce the effect of verapamil. The antihypertensive property is increased by antihypertensive agents (vasodilators, diuretics), tetracyclic and tricyclic antidepressants, antipsychotics; antianginal effect is increased by nitrates. Beta-blockers, cardiac glycosides, class IA antiarrhythmics, radiopaque contrast agents, inhalation anesthetics mutually potentiate the inhibitory effect on AV conduction, automatism of the sinoatrial node and myocardial contractility. When verapamil is used together with acetylsalicylic acid, existing bleeding increases. Cimetidine increases plasma levels of verapamil.

Overdose

In case of an overdose of verapamil, arterial hypotension, AV blockade, bradycardia, coma, cardiogenic shock, asystole occur. It is necessary to administer calcium gluconate (10–20 ml of a 10% solution intravenously) as a specific antidote; with AV blockade and bradycardia, atropine, orciprenaline or isoprenaline are administered; with hypotension - dopamine, plasma-substituting solutions, norepinephrine; with the manifestation of signs of heart failure - dobutamine.

VERAPAMIL Verapamil

Active substance

›› Verapamil *

Latin name

›› C08DA01 Verapamil

Pharmacological group: Calcium channel blockers

Nosological classification (ICD-10)

›› I10-I15 Diseases characterized by high blood pressure
›› I20 Angina [angina pectoris]
›› I25 Chronic ischemic heart disease
›› I25.2 Past myocardial infarction
›› I47.2 Ventricular tachycardia
›› I49.4 Other and unspecified premature depolarization
›› R07.2 Pain in the region of the heart

Composition and form of release

1 tablet contains verapamil hydrochloride 40 or 80 mg; in vials of 30 or 50 pcs. respectively, in a cardboard box 1 bottle.
1 ampoule with 2 ml of solution for injection - 5 mg; in a blister 5 pcs., in a cardboard box 2 blisters.
1 retard tablet - 240 mg; in vials of 20 pcs., in a cardboard box 1 bottle.

pharmachologic effect

pharmachologic effect- hypotensive, antianginal, antiarrhythmic... Blocks calcium channels.

Indications

Arterial hypertension, ischemic heart disease, angina pectoris, paroxysmal tachycardia, extrasystole, postinfarction period.

Contraindications

Wolff-Parkinson-White syndrome, cardiogenic shock, hypotension, AV block, congestive heart failure.

Side effects

Dizziness, nausea, headache, hyperemia, hypotension, AV block, bradycardia, constipation.

Method of administration and dosage

Inside, adults - 80-160 mg (pills) 3 times a day 30 minutes before meals or in the morning, on an empty stomach - 1 tab. Retard (the dose is selected individually), additionally (if necessary) - 1 / 2-1 tab. .retard (in the evening). The maximum daily dose is 480 mg.
Children under 14 years old - 40 mg (pills) 2-3 times a day, infants and young children - 20 mg (pills) 2-3 times a day.
IV slowly, adults - 5-10 mg, maintenance dose - IV drip (previously dissolved in 100-150 ml of isotonic sodium chloride solution) at a rate of 5-10 mg / h (no more than 100 mg / day). Children: newborns - 0.75-1 mg, up to 1 year old - 0.75-2 mg, 1-5 years old - 2-3 mg, 6-14 years old - 2.5-5 mg.

Shelf life

Storage conditions

List B. In the dark place at a temperature of 15-25 ° C.

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VERAPAMIL (Verapamilum) *. 5 - [(3,4-Dimethoxyphenethyl) methylamino] -2- (3,4-dimethoxyphenyl) -2-isopropylvaleronitrile hydrochloride. Synonyms: Verpamil, Isoptin, Falicard, Phenoptin, Calan, Cardilax, Dilacoran, Falicard, Finoptin, Ikacor, Iproveratril, Isopine, Isoptin, Manidon, Vasolan, Vepamil, Verapamilhydrochlorid, Verapamil, etc. a complicated version of the phenylalkylamine molecule (see. Sensit). The drug has antiadrenergic activity. Previously, it was believed that its therapeutic effect is due to the weakening of sympathetic impulses entering the blood vessels, heart and other organs. Currently, it is classified as an antagonist of calcium ions, and it is one of the main drugs in this group. Verapamil causes expansion of the coronary vessels of the heart and increases coronary blood flow; lowers the heart's need for oxygen. In ischemic processes in the myocardium, the drug helps to reduce the disproportion between the need for and the supply of oxygen to the heart, both by increasing the blood supply and by better utilization and more economical consumption of the delivered oxygen. The drug reduces myocardial contractility, but due to the expansion of peripheral vessels and a decrease in vascular resistance, cardiac output does not change significantly. The drug inhibits platelet aggregation. Verapamil affects the cardiac conduction system, inhibits sinoatrial and atrioventricular conduction. Has antiarrhythmic effect; refers to antiarrhythmic drugs of group IV (see. Antiarrhythmic drugs). In addition, it has some natriuretic and diuretic effects by reducing tubular reabsorption. In the mechanism of the antianginal action of verapamil, along with antagonism towards calcium ions, an increase in the content of potassium ions in myocardial cells also plays a role. Verapamil is well absorbed when taken orally. The peak concentration in blood plasma is detected after 1 to 3 hours. However, there are significant individual differences in the pharmacokinetics of the drug. The half-life varies from 2.5 to 7.5 hours after a single dose and from 4.5 to 12 hours after repeated administration. A constant therapeutic concentration in the blood is usually achieved after 4 days from the start of repeated ingestion. The drug is extensively metabolized in the liver. In case of impaired liver function, the time of drug release is significantly lengthened. About 5% of the drug is released unchanged. Verapamil is used internally and in the form of injections. Inside take in chronic coronary artery disease to prevent attacks of angina pectoris, especially in combination with atrial extrasystole and a tendency to tachycardia. As an antiarrhythmic agent, it is prescribed mainly for atrial arrhythmias: with supraventricular tachycardia, extrasystoles. With ventricular arrhythmias, including with ventricular premature beats; the drug is ineffective. It is also recommended for arterial hypertension, but nifedipine is more effective as an antihypertensive agent for severe hypertension (see). Intravenously used for acute attacks of angina pectoris, attacks of supraventricular paroxysmal tachycardia and hypertensive crises. Inside take 30 minutes before meals. Doses, especially taking into account possible fluctuations in pharmacokinetics, are selected individually. In milder forms of angina pectoris, 0.04-0.08 g (40-80 mg) is prescribed 3-4 times a day. If necessary, increase the single dose to 0.12 - 0.16 g (120 - 160 mg). The usual daily dose is 0.24 - 0.48 g (240 - 480 mg). Supportive therapy (in smaller, individually selected doses) is carried out for a long time. It is noted that tolerance does not develop with the use of verapamil (in contrast to organic nitrates and nifedipine). On the contrary, the anti-ischemic effect increases with regular use of verapamil. Intravenously, to stop the paroxysm of supraventricular tachycardia, slowly inject 2-4 ml of a 0.25% solution (5-10 mg) for adults. Repeatedly for maintenance therapy, it is administered once a day by drip at a rate of 0.005 mg / kg per minute, not earlier than 30 minutes after the jet injection. A solution of verapamil is prepared by diluting 2 ml of a 0.25% solution of the drug (1 ampoule) in 100 - 150 ml of isotonic sodium chloride solution or 5% glucose solution. Children are prescribed the drug in smaller doses: up to 4 years of age, they are usually given by mouth 0.02 g (20 mg) 2 - 3 times a day; up to 14 years old - 0.04 (40 mg) 2 - 3 times a day. Intravenously administered at the age of 1 to 5 years at 0.002 - 0.003 g (2 - 3 mg), from 6 to 14 years - at 0.025 - 0.05 g (2.5 - 5 mg). Verapamil is generally well tolerated. However, nausea, vomiting, dizziness, increased fatigue, the development of peripheral edema, allergic reactions are possible, relatively often (especially with prolonged use) constipation of an atonic nature occurs. Large doses can cause arterial hypotension, atrioventricular block. Contraindications: cardiac shock, severe hypotension, acute myocardial infarction with atrioventricular block; the first 3 months of pregnancy and the period of breastfeeding. Caution should be exercised with the simultaneous use of verapamil and β-blockers (due to the possible summation of the effect on the conductivity and contractility of the heart). Verapamil is administered intravenously under the control of hemodynamic parameters. Form of release of tablets of 0.04 g (40 mg); 0.08 g (80 mg) and 0.12 g (120 mg) in a package of 30 and 100 pieces; 0.25% solution in ampoules of 2 ml (5 mg) in a package of 5 ampoules; prolonged-release tablets of 0.2 g (200 mg) and 0.24 g (240 mg). Storage: List B. In the dark place.

Dictionary of Medicines. 2005 .

Synonyms:

See what "VERAPAMIL" is in other dictionaries:

IUPAC chemical compound? Gross formula? ATX classification ... Wikipedia

Noun., Number of synonyms: 15 azupamil (1) antiarrhythmic (5) veramil (1) ... Synonym dictionary

verapamil- a drug that normalizes the heart rate, lowers blood pressure and improves blood supply to the heart muscle. It is used for arterial hypertension, angina pectoris, arrhythmias. It is a cheap analogue of IZOPTIN and FINOPTIN ... Analogues of expensive drugs

- (isopropyl hydrochloride [(N methyl N homoveratryl) aminopropyl] 3,4 dimethoxyphenyl acetonitrile; isoptin; finoptin), mol. m. 491.1; colorless crystals; t. pl. 146 ... Chemical encyclopedia

VERAPAMIL- (verapamil) calcium antagonist; is used to treat hypertension, angina pectoris and arrhythmias. Assigned internally; possible side effects: constipation, nausea and hypotension. Trade names: Cordilox, Securon, Univer ... Explanatory Dictionary of Medicine- n., number of synonyms: 1 verapamil (15) ASIS Synonym Dictionary. V.N. Trishin. 2013 ... Synonym dictionary

Calcium antagonist; is used to treat hypertension, angina pectoris and arrhythmias. Assigned internally; possible side effects: constipation, nausea and hypotension. Trade names: Cordilox, Securon, Univer.