Analogs of "Verapamila": a list of drugs, reviews. "Verapamil": indications, instructions for use

The date: 04.11.2019

Composition and form of release

in contour cellular pack 10, 15 or 25 pcs.; in a pack of cardboard 1, 2, 3, 4, 5 and 10 pcs.; or in PE banks at 30, 50 or 100 pcs.; In a pack of cardboard 1 bank.

Characteristic

Verapamil is one of the main preparations of the BKK group.

pharmachologic effect

pharmachologic effect - antihypertensive, anti-infanal, antiarrhythmic.

Pharmacodynamics

The drug reduces the need of myocardium in oxygen by reducing the reduction of myocardium and reduce heart rate. It causes the expansion of the coronary blood vessels and increases the coronary blood flow; Reduces the tone of smooth muscles of peripheral arteries and an OPS.

Verapamil significantly slows the AV conduction, inhibits the automatism of the sinus node, which allows the drug to treat reductant-central arrhythmias.

Verapamil is a drug selection for the treatment of angina of vasospadic genes (printelaty angina). It has an effect for the angina of the voltage, as well as in the treatment of angina with sufficient rhythm disorders.

Pharmacokinetics

When taking inside, more than 90% of the adopted dose is absorbed. Subjected to metabolism at the "first passage" through the liver. Binding with proteins 90%. T 1/2 when taking a single dose - 2.8-7.4 h; When receiving repeated doses - 4.5-12 hours. It is removed mainly by the kidneys and 9-16% - through the intestine. The main metabolite is novelverpamina, which has less pronounced hypotensive activity than unchanged verapamil.

Indications of the drug Verapamil

treatment and prevention of heart rate disorders: paroxysmal superstricular tachycardia, fluttering and flickering atrial (tachyarhythmic variant), religorary extrasistol;

treatment and prevention of angina: chronic stable angina (stainless angina), unstable angina (stenocardia of rest), vasospadic angina (angina printelastyle, variant angina);

treatment of arterial hypertension.

Contraindications

increased sensitivity to the components of the drug;

pronounced bradycardia;

chronic heart failure of the IIB-III stage;

cardiogenic shock (with the exception of arrhythmia caused);

synoyatrial blockade;

AV blockade II and III degree (excluding patients with an artificial rhythm driver);

sine node weakness syndrome;

wolf Parkinson-White syndrome;

morgali-Adams - Stokes syndrome;

acute heart failure;

the simultaneous use of beta-adrenobloclars in / in;

children's age up to 18 years.

Application in pregnancy and breastfeeding

The use of verapamila during pregnancy is possible only when the expected benefit for the mother exceeds the potential risk to the fetus.

If it is necessary to use the drug during breastfeeding period, it should be borne in mind that verapamil is distinguished with breast milk, so breastfeeding must be stopped.

Side effects

When applying verapamil is possible:

From the side of the cardiovascular system: Redness of the face, pronounced bradycardia, AV blockade, arterial hypotension, the appearance of symptoms of heart failure when using the drug in high doses, especially in predisposed patients.

From the gearbox: nausea, vomiting, constipation; In some cases, the transient increase in the activity of hepatic transaminases in the blood plasma;

From the CNS: Dizziness, headache, in rare cases - increased nervous excitability, inhibition, increased fatigue.

Allergic reactions: Skin rash, itching.

Others: Development of peripheral edema.

Interaction

With the simultaneous use of verapamila:

with antiarrhythmic drugs, beta-adrenoblockers and inhalation anesthetics there is an amplification of a cardiodepressive effect (increasing the risk of AV blockade, a sharp decline in heart rate, the development of heart failure, sharp drops of blood pressure);

with antihypertensive means and diuretics - it is possible to strengthen the hypotensive effect of verapamil;

with digoxin - it is possible to increase the concentration of digoxin in the blood plasma due to the deterioration of its kidney removal (therefore it is necessary to monitor the level of digoxin in the blood plasma in order to detect its optimal dosage and prevent intoxication);

with cimetidine and ranitidine - the concentration of verapamil in the blood plasma increases;

with rifampicin, phenobarbital - it is possible to reduce the concentration in the blood plasma, the weakening of verapamila;

with theophylline, prazosin, cyclosporin - it is possible to increase the concentration of these substances in the blood plasma;

with minelaxanta - it is possible to strengthen the minelaxing action;

with acetylsalicylic acid - the likelihood of bleeding is intensified;

with quinidine - the concentration of chinidine in the blood plasma increases, the threat of decrease in blood pressure is increasing, and in patients with hypertrophic cardiomyopathy, there is a pronounced arterial hypotension;

with carbamazepine and lithium - the risk of neurotoxic effects is increasing.

Method of application and dose

Inside During or after eating, drinking a small amount of water.

The dosing mode and the duration of treatment are established individually depending on the state of the patient, the degree of severity, the characteristics of the course of the disease and the effectiveness of therapy.

For the prevention of attacks of angina, arrhythmia and in the treatment of arterial hypertension, the drug is prescribed by adults in the initial dose of 40-80 mg 3-4 times a day. If necessary, increase the one-time dose to 120-160 mg.

Maximum daily dose - 480 mg.

In patients with pronounced violations of the liver function, the removal of verapamil from the body slowly, so treatment is advisable to start with minimal doses. The daily dose of the drug should not exceed 120 mg.

Overdose

Symptoms: Large doses (taking up to 6 g of the drug) can cause deep depression of consciousness, arterial hypotension, sinus bradycardia, moving in AV blockade, sometimes asistol.

Treatment: In the occurrence of arterial hypotension and / or complete AV blockade - in / in the introduction of fluid, dopamine (dopamine), calcium gluconate, isoproterenol or norepinephrine. Treatment is symptomatic and depends on the clinical picture of an overdose. Hemodialysis is not effective.

special instructions

With caution, it is necessary to prescribe a drug with an AV degree blockade, chronic heart failure I and II degree, arterial hypotension (garden<100 мм рт. ст. ), брадикардией, выраженными нарушениями функции печени.

In the treatment, control of the function of cardiovascular and respiratory systems, blood levels and blood levels in the blood, BCC and the amount of urine allocated is necessary.

Conditions for the storage of the drug Verapamil

In a dry place, at a temperature not higher than 25 ° C.

Keep out of the reach of children.

The shelf life of the drug Verapamil

3 years.

Do not apply after the expiration date indicated on the package.

Medical Instructions

Synonyms of nosological groups

Rubric ICB-10	Synonyms for diseases of the ICD-10
I10 essential (primary) hypertension	Arterial hypertension
	Arterial hypertension


	Arterial hypertension
	Sudden increase in hell

	Hypertensive state
	Hypertensive crisis
	Hypertension
	Hypertension arterial
	Hypertenia malignant
	Essential hypertension
	Hypertonic disease
	Hypertensive crisis
	Hypertensive crisis
	Hypertension
	Malignant hypertension
	Malignant hypertension
	Isolated systolic hypertension
	Crisis hypertensive

	Primary arterial hypertension

	Essential arterial hypertension
	Essential arterial hypertension
	Essential hypertension
	Essential hypertension
I15 Secondary hypertension	Arterial hypertension
	Arterial hypertension
	Arterial hypertension of critical flow
	Arterial hypertension complicated by diabetes
	Arterial hypertension
	Vasorenal hypertension
	Sudden increase in hell
	Hypertensive circulatory disorder
	Hypertensive state
	Hypertensive crisis
	Hypertension
	Hypertension arterial
	Hypertenia malignant
	Hypertension is symptomatic
	Hypertensive crisis
	Hypertensive crisis
	Hypertension
	Malignant hypertension
	Malignant hypertension
	Crisis hypertensive
	Exacerbation of hypertension
	Renal hypertension
	Renovascular arterial hypertension
	Renovascular hypertension
	Symptomatic arterial hypertension
	Transient arterial hypertension
I20 angina [breast toad]	Gebereden's disease
	Angina pectoris
	Stenokard attack
	Recurrent angina
	Spontaneous angina
	Stable angina
	Stencardia X Syndrome
	Angina
	Angina (attack)
	Threw stress
	Road angina
	Handicardia progressive
	Stenicard mixed
	Spontaneous angina
	Stenzard stable
	Chronic stable angina
I20.0 Unstable angina	Gebereden's disease
	Unstable angina
	Angina unstable
I20.1 angina with documented spasm	Gebereden's disease
	Vazospadic angina
	Vazospadic angina printelala
	Variant angina
	Cardiospasm
	Coronarpasm
	Coronaropastic angina printela
	Printametal anginaland
	Spasm of coronary arteries
	Spasm of coronary vessels
	Night coronaropastic
	Stenria Prinzmetala
I20.8 Other walls of angina	Spontaneous angina
	Stable angina stress
	Stable angina rest
	Stencardia X Syndrome
	Handicardia progressive
	Spontaneous angina
I25 chronic ischemic heart disease	Ischemic heart disease against the background of hypercholesterolemia
	Ischemic heart disease chronic
	Myocardial Ischemia during arteriosclerosis
	Myocardial ischemia recurrent
	Coronary heart disease
	Stable IBS
	Expressive transluminal angioplasty
I25.2 transferred in the past myocardial infarction	Cardial syndrome
	Mocked myocardial infarction
	Post-infarction cardiosclerosis
	Postinfarction period
	Rehabilitation after myocardial infarction
	Recognition of the operated vessel
	State after myocardial infarction
	Status after transferred myocardial infarction
	Stenrope Postinfarc
I42.1 obstructive hypertrophic cardiomyopathy	Asymmetric hypertrophy of the interventricular partition
	Hypertrophic cardiomyopathy
	Hypertrophic obstructive cardiomyopathy
	Myocardial hypertrophy with obstruction
	Cardiomyopathy hypertrophic obstructive
	Obtaining restrictive cardiomyopathy
I47.1 Supported Tachycardia	Supported paroxysmal tachycardia
	Supported Tahiaritmia
	Supported Tachycardia
	Neckwarce disorders rhythm
	Supported paroxysmal tachycardia
	Neckwarce Tahiaritimia
	Supported tachycardia
	Neurogenic sinus tachycardia
	Orthodrome tachycardia
	Paraxismal asshortonian tachycardia
	Paroxysm Supported Tachycardia
	Paroxysm for religorakkova tachycardia with WPW syndrome
	Paroxism atrial tachycardia
	Paroxysmal Supported Tahiaritmia
	Paroxysmal asshortaric tachycardia
	Polytonian atrial tachycardia
	Atrial arrhythmia
	Atrial True Tachycardia
	Atrial tachycardia
	Atrial tachycardia with av blockade
	Reperfusion arrhythmia
	Reflex Berchold Yarisha
	Recurient Sustainable Neckwarce Paroxysmal Tachycardia
	Symptomatic ventricular tachycardia
	Wolf Parkinson-White Syndrome
	Sinus tachycardia
	Supported paroxysmal tachycardia


	Supported extrasystole
	Supported arrhythmias
	Tachycardia from AV connection
	Tachycardia Neznaudocycova
	Tachycardia orthodromic
	Tachycardia sinusovaya
	Uzl Tachycardia
	Chaotic Polytonian Atrial Tachycardia
I47.2 Ventricular tachycardia	Stomatricular arrhythmia
	Stomatricular paroxysmal tachycardia
	Stomatricular Tahiaritmia
	Stomatricular Tachycardia
	Paroxysmal bidirectional spine-shaped ventricular tachycardia
	Paroxysmal ventricular tachycardia
	Torsade de Pointees (Torsade de Pointes)
	Pyruette tachycardia with myocardial infarction
	Symptomatic ventricular tachycardia
	Tachycardia Zastochekova
	Threatening Life Stomach Arrhythmia
	Stable ventricular tachycardia
	Stable monomorphic ventricular tachycardia
I48 Fibrillation and atrial flirt	Refrigeration of frequent rhythm of ventricles when flickering or fluttering atrial
	Flickering atrial
	Supported arrhythmia
	Paroxism of the flicker and fluttering atrial
	Paroxism flickering atservation
	Paroxysmal shape of the flicker and fluttering atrial
	Paroxysmal flickering and atrial flutter
	Paroxysmal flicker atrial
	Permanent shape of flickering tachyarhythmia
	Atrial extrasystole
	Atrial extrasystoles
	Tahiarhythmic atrial flicker
	Tahisistolic atrial flicker
	Atrial tremble
	Threatening Life Fibrillation Golders Heart
	Atrial fibrillation
	Chronic flickering atrial
I49.1 Premature depolarization atrial	Arrhydramya Neznastroykova
	Supported arrhythmia
	Supported extrasystole
	Supported arrhythmias
	Supported extrasystoles
	Extrasystolism Supported
	Presense extrasistoly
I49.4 Other and unspecified premature depolarization	Extraceistral arrhythmia
	Extrasystole
	Extrasystolia uncomfortable
I49.9 heart rhythm violation	AV reciprocal tachycardia
	AV-nodal reciprocal tachycardia
	Antidrome reciprocal tachycardia
	Arrhythmia
	Arrhythmia
	Heart arythmy
	Arrhythmia due to hypokalemia
	Ventricular arrhythmia
	Ventricular Tahiaritmia
	High frequency reduction of ventricles
	Clear tachiisistolic arrhythmia
	Violation of heart rhythm
	Disturbance of heart rhythm
	Disturbance of cardiac rhythm
	Paroxysmal superstitreal arrhythmia
	Paroxysmal suprolenricular arrhythmia
	Paroxysmal suprolenricular tachycardia
	Paroxysmal violation of rhythm
	Paroxysmal atrial and ventricular rhythm
	Premordial pathological ripple
	Cardiac arrhythmias
	Supported Tahiaritmia
	Supported Tachycardia
	Supported arrhythmias
	Tahiaritmia
	Extraceistral arrhythmia
R07.2 Heart pain	Pain syndrome with myocardial infarction
	Pain in cardiological patients
	Cardialgy
	Cardialiag on the background of myocardial dormriconal dystrophy
	Cardial syndrome
	Cardionerement
	Myocardial ischemic pain
	Neurosis of the heart
	Pericardial pain
	Pseudo-sundenokard
	Functional cardialgy

Pharmacological action - antianginal, hypotensive, antiarrhythmic.
Blocks calcium channels (acts from the inside of the cell membrane) and lowers the transmembrane calcium current. Interaction with the channel is determined by the degree of depolarization of the membrane: the open calcium channels of the depolarized membrane more effectively blocks. A lesser extent affects the closed channels of the polarized membrane, preventing them with activation. Slightly affects sodium channels and alpha adrenoreceptors. Reduces the reduction, the driver's frequency of the rhythm of the sinus node and the speed in the AV node, synoyatrile and AV conductivity, relaxes smooth muscles (more from the arterioles than veins), causes peripheral vasodilation, lowers the OPS, reduces post capacity. Increases myocardial perfusion, reduces the imbalance between the need and supply of the heart with oxygen, contributes to the regression of the left ventricular hypertrophy, lowers blood pressure. Prevents development and eliminates spasm of coronary arteries at variant angina. In patients with uncomplicated hypertrophic cardiomyopathy improves blood outflow from ventricles. Reduces the frequency and severity of the headaches of vascular genesis. Inhibits neuromuscular transmission in the pseudogiperrophic Mopathy of Duzhenna and lengthens the recovery period after the application of this image. In vitro blocks the P170 enzyme and partially eliminates the resistance of cancer cells to chemotherapeutic means.
After receiving the inside, more than 90% of the dose is absorbed, bioavailability is 20-35% due to metabolism with the "first passage" through the liver (increases with long-term reception in large doses). TMAC is 1-2 h (tablets), 5-7 h (tablets of prolonged action) and 7-9 h (prolonged capsules). Binds with plasma proteins by 90%. Metabolized in the liver with the formation of noverapamila, which has 20% of the hypotensive activity of verapamila, and 11 other metabolites (are defined in trace quantities). T1 / 2 When ingestion of a single dose - 2.8-7.4 hours, with repeated doses - 4.5-12 hours (due to the saturation of enzyme liver systems). When in / in administration of T1 / 2, two-phase: Early - about 4 minutes, finite - 2-5 when taking the beginning of action, it is noted after 1-2 under conditions in / in administration an antiarrhythmic action is developing for 1-5 min (usually less than 2 Min), hemodynamic effects - for 3-5 minutes. The duration of action is 8-10 hours (pills) or 24 hours (capsules and tablets of prolonged action). When in / in administration, an antiarrhythmic action lasts about 2 hours, hemodynamic - 10-20 minutes. The main kidneys is excreted and feces (about 16%). It penetrates into breast milk, passes through the placenta and is determined in the blood of the umbilical vein in childbirth. Fast / in Introduction causes a hypotension from a mother leading to a distress of the fetus. With a long reception, the clearance decreases and bioavailability increases. Against the background of severe liver function, the plasma clearance decreases by 70% and T1 / 2 increases to 14-16.
According to the results obtained in 2-year experiments on rats when administered in doses, 12 times larger than the MARDCH, and in the Bacterial test of the Eix (5 of the studied strains, the dose - 3 mg per cup, with or without metabolic activation) does not have carcinogenic and mutagenic activity. In experiments on rats in doses, 6 times larger than the dose, recommended for a person, slows down the growth of the fetus and increases the frequency of the intrauterine death of the fruit.

Verapamil is a drug that has hypotensive ( reduces pressure in vessels), antiarrhythmic ( prevents the appearance of various heart rhythm disorders) and antianginal action ( reduces symptoms of ischemic heart disease). This medication refers to a group of calcium channels of slow channels that affect the operation of the cardiovascular system. It is worth noting that Verapamil influences the heart muscle to a greater extent ( myocardia) than on the vessels.

Verapamil is a white crystalline powder, which is well soluble in water. This drug is pretty quickly and almost completely dissolved in the digestive tract. The maximum impact on the body verapamil has for the first 2 - 4 hours after oral administration ( inside).

Types of medicine, commercial names of analogs, output

Due to the fact that verapamil is well absorbed when taking inside, it is most often prescribed in a tablet form. Verapamil is also produced as a solution for intravenous administration.

It is worth mentioning that Verapamil is produced under other names - Veratrid, Voroorad, Isopin, Caveryl, Leoptin, Finoptin, etc.

Firms manufacturers Verapamila

Manufacturing firm	Commercial name of the drug	The country	Form release	Dosage
*Aveksima*	*Verapamil*	*Russia*	Sheath-covered tablets.	It is selected individually. Medication should be taken in 30 - 40 minutes before meals. Adults and adolescents over 15 years old are prescribed at 0.04 - 0.08 grams ( 40 - 80 milligrams) Three times a day. If necessary, the doctor may increase the dose to 0.12 - 0.16 grams ( 120 - 160 milligrams). The daily dosage should not exceed 240 - 480 milligrams. For children from six to fourteen years, the daily dose is 80 - 360 milligrams, and children under six years are incorporated to 40 - 60 milligrams. Multiplicity of reception of tablets ( children from six to fourteen years) is 3 - 4 times a day.
*North Star*	*Verapamil*	*Russia*
*Chemical Pharmaceutical Combine Akrichin*	*Verapamil*	*Russia*
*Alkaloid*	*Verapamil*	*Macedonia*
*Obolenskaya*	*Verapamil*	*Russia*
*Unipharm.*	*Verapamil-Sofarma*	*Bulgaria*	Tablets covered with film shell ( film coating is less than 10% of the mass of the entire tablet).
*Valentine Pharmaceutical*	*Verapamil*	*Russia*
*Serena Pharma.*	*Verapamil*	*India*
*Alkaloid*	*Verapamil*	*Macedonia*	Tablets, long ( prolonged) actions.	It should be taken before or after taking food, while drinking a tablet with a small amount of water ( 50 - 100 milliliters). As a rule, a daily dose is used from 240 to 360 milligrams. This dosage can be increased to 480 milligrams ( treatment should be held in the hospital). Multiplicity of reception is 2 - 3 times a day. It should be noted that the initial dose for patients with impaired kidney and liver function should not exceed 120 milligrams.
*Esk*	*Verapamil Eskaya*	*Russia*	Solution for intravenous administration.	Enter slowly, at least 2 - 3 minutes. Under the introduction, it should be constantly checking the heart rate and blood pressure. Adults are introduced 5 - 10 milligms ( one-time dosage). In the absence of the necessary effect, the introduction in the same dosage should be repeated. The maximum daily dosage for adults should not exceed 480 milligrams. The initial dose for people with impaired kidney and liver function should not exceed 120 milligrams. A single dose for children up to one year is 0.75 - 2 milligrams, from one to five years to 2 - 3 milligrams, from six to fourteen years - 2.5 - 3.5 milligram.
*Biosynthesis*	*Verapamil*	*Russia*	Solution for intravenous administration.

Mechanism of therapeutic action of medication

Verapamil is a blocker of slow calcium channels of L-type ( it is calcium antagonist), which are located in the heart muscle, as well as in the vessels. In the heart of calcium channels are located in a synoyatrial and atrioventricular node, as well as in Purkinier fibers ( these structures are part of the conductive heart system and maintain its normal contractile function.). Increased calcium ion penetration rate from the intercellular space in the cells of the conductive heart system leads to a violation of the rhythm. These changes inevitably lead to excessive increase in oxygen consumption by the heart muscle, which is further manifested by a decrease in blood tissue bloodiffs ( ischemia) and oxygen starvation ( hypoxia). Verapamil reduces myocardial needs ( heart muscle) in oxygen that consumes more than 10% of all inhaled oxygen, and is also able to eliminate the imbalance between the supply and consumption of oxygen in cardiomyocytes ( myocardial cells). Along with the above mechanisms in cardiomyocytes, there is an increase in the concentration of potassium ions, which is necessary for normal heart rhythm.

Calcium ion penetration in the vascular wall cell leads to the reflex expansion of the coronary arteries of the heart ( food vessels), and also expands peripheral arterial vessels ( arteries and arterioles). There is also a decrease in the total peripheral resistance of the vessels ( hypotensive action).

It should be noted that verapamil is well absorbed in the body, but due to essential individual differences, this medication can have an effect at different times ( from 1 to 4 hours). Verapamil when entering liver cells is actively metabolized ( subjected to enzymatic cleavage). In the future, hitting the blood, it binds to plasma proteins ( 90% ). The necessary constant concentration of medication in the blood is achieved, as a rule, on the fourth day after re-use of the drug. Verapamil is displayed through bile ( 25% ), with urine ( 70% ), as well as unchanged ( 4 – 5 % ). The period of extraction of verapamil significantly increases in people with various impaired liver function.

With intravenous administration, an antiarrhythmic effect is already achieved in the first 5 minutes and lasts about two hours ( verapamil is an antiarrhythmic drug IV group). Hypotensive action ( lowering blood pressure) It is observed after 3 - 6 minutes and lasts no more than 25 minutes. In most cases, Verapamil is well tolerated.

Indications for use

Verapamil is prescribed for prophylaxis, as well as for the treatment of different heart rate disorders, with ischemic heart disease ( violation of the blood supply of myocardium against the background of the damage of coronary vessels), as well as in some other diseases of the heart.

Application Verapamila

Indication to application	Mechanism of action	Dosage
*Prevention and treatment of ischemic heart disease ( IBS)*
Chronic stable angina *(the emergence of painful sensations for sternum caused by the same type of physical exertion)*	Reduces the output of calcium ions in coronary vessels and thereby bows spasm. Increases the concentration of potassium ions in myocardial cells, which also helps to reduce the reduction of the heart muscle and reduce pain. Reduces the total peripheral resistance of the vessels, which leads to a decrease in pressure in the arteries.	The dosage should be selected individually. When used inside ( parenteral) The drug must be taken in half an hour before meals. One-time dosage for adolescents up to 15 years and for adults is 40 - 80 milligrams. Medication should be taken up to three times a day. Sometimes a one-time dosage can be increased to 120 - 160 milligrams. For children under six years old are prescribed by 40 - 60 milligram, and from six to fourteen years to 80 - 360 milligrams per day. Children and teens up to 14 years old take the drug up to four times a day.
Unstable angina *(breast pain can occur both with any physical activity and on the background of full rest)*
Vazospadic angina *(spasm of vessels feeding the heart, which occurs at rest)*
Prevention and treatment of some heart rhythm disorders
Paroxysmal asshortaric tachycardia *(sharp and parked heartbeat)*	Reduces the excitability of ectopic foci ( these foci have their own excitability and may disrupt the normal rhythm of the heart.). Normalizes and largely reduces heart rhythm.	Most often used intravenously. During inkjet administration, it is necessary to monitor the indicators of the electrocardiogram, arterial pressure during 2 to 3 minutes, and calculate the pulse. A single dosage for adults is 5 - 10 milligrams. If during the first 5 - 10 minutes does not observe the desired effect, it is necessary to re-enter a medicine in the same dosage. The multiplicity of administration should be selected by the attending physician. Children up to one year are prescribed 0.75 - 2 milligrams. Children from one to five years at 2 - 3 milligrams. Children from six to fourteen years at 2.5 - 3.5 mg.
Supported extrasystole *(the appearance of extraordinary incomplete cuts of the heart against the background of increasing the excitability of ectopic foci)*
Chronic form of flickering and atrial flutter *(frequent and ordered reduction of the atria of the heart)*		Apply both intravenously and inside.
Prevention and treatment of hypertensive states
Hypertension *(increased blood pressure over 140/90 mm RT. Art.)*	Importantly affects the arterial vessels of the middle and small caliber and blocks the release of calcium in them, which leads to their reflex expansion. Also expands coronary artery.	Most often used intravenously ( to achieve a faster effect).
Hypertensive crisis *(excessive increase in pressure that can lead to the defeat of various organs and systems)*
Other heart disease
Hypertrophic cardiomyopathy *(thickening of the muscular layer of the left, and sometimes the right ventricle of the heart)*	It helps to reduce the reduction of the heart muscle due to the reduction of excitability in the conductive system of the heart. Reduces calcium exit rate in heart vessels, as well as in peripheral arteries.	It can be used inward or in the form of intravenous injections.

How to apply medication?

Depending on the pathology, verapamil can assign in tablet form, as well as as intravenous injections.

Verapamil tablets are most often prescribed for the prevention or treatment of ischemic heart disease. Take tablets should be before meal ( for 30 - 40 minutes), while drinking them with a small amount of liquid ( 50 - 100 milliliters). Dosage should be selected individually taking into account the type and severity of pathology. A single dosage for adults and adolescents over 15 years old is, on average, 40 - 80 milligrams. Tablets are accepted twice or three times a day. In rare cases, a one-time dose can be increased to 120 - 160 milligrams ( only after consulting a doctor). Verapamil tablets can also be prescribed to children. For children under six years, one-time dose is 15 - 20 milligrams, and for children from six to fourteen years - 20 - 80 milligrams ( 3 - 4 times a day).

In some cases, the doctor may appoint a reception of a long or prolonged verapamil. Most often it is prescribed to reduce pressure ( with hypertension), as well as for the prevention of attacks of angina and supertoday tachycardia. The daily dose of verapamil prolonged action is 240 - 360 milligrams. Medication should be taken in the morning during or immediately after meals. Also, the tablet should be made with a small amount of fluid ( 50 - 100 milligrams). It should be noted that people with a violation of the hepatic function, as well as for the elderly, one-time dose should be reduced.

For the treatment and prevention of different heart rate disorders ( supported extrasystole, paroxysmal superstricular tachycardia, chronic form of flickering and atrial flutter), as well as with hypertensive crisis, verapamil is used intravenously. Verapamil is introduced for at least 2 - 3 minutes under constant control of heart rate and blood pressure. Adults are openly introduced 5 or 10 milligrams of the medication, and in the absence of the effect they repeat in the same dose. Children up to one year, 0.75 - 2 milligram, from one to five years at 2 - 3 milligrams, from six to fourteen years to 2.5 - 3.5 milligram verapamil. People of old age, as well as patients with impaired liver and kidney function, one-time and daily dose must be reduced ( less than 120 milligrams per day).

Possible side effects

The impact of verapamil on the cardiovascular system may in some cases lead to serious consequences. That is why intravenous introduction of this medication should be carried out only in the hospital ( under the direct supervision of the doctor). Verapamil can also lead to the appearance of drug allergies.

Verapamil is able to cause the following side effects:

violations from the cardiovascular system;
allergic manifestations;
disorders on the part of the central and peripheral nervous system;
disorders from the digestive tract;

Cardiovascular disorders

The reception of verapamil sometimes will burn to lead to significant violations of the rhythm of cardiac activity. It is worth noting that these violations most often occur with the intravenous use of the medication.

The following side effects from the cardiovascular system are distinguished:

hypotension;
angina;
atrioventricular blockade of the heart;
asistolia.

Bradycardiarepresents a pronounced reduction in heart rate ( less than 50 shots per minute). Bradycardia arises due to a decrease in the conductivity of the synoatrial node, which normally generates 60 to 90 heart cuts. Subjectively bradycardia may not cause any sensations, but most often this state is manifested by such symptoms as dizziness, severe weakness, cold sweat, as well as pre-perspective and fainting condition, which is caused by a decrease in oxygen intake to brain tissues ( hypoxia brain).

Hypotensionit is characterized by a decrease in blood pressure ( below 90/60 mm Hg. Art.). Reducing the excitability of the entire conductive heart system inevitably leads to a decrease in the pump function, which is performed by the heart muscle. Due to lowering the blood pressure of the fabric and the organs experience oxygen starvation, which can largely violate their activities.

Heart failureit is a state in which the contractile function of the heart is significantly violated. In the future, at the level of the whole organism, blood flows. If there is deficiency of the left ventricle of the heart, it leads to the appearance of shortness of breath, hemoptia and cyanosis ( skin and mucosa acquire a shiny shade). In case of failure of the right ventricle of the heart, shortness of breath is observed, hepatomegaly ( increase in the size of the liver), Edema extremities. Rapidly evolving ( acute) Heart failure can lead to such complications as a cardiac asthma ( sinwing attack against the background of violation of the contractual activity of the heart), cardiogenic shock ( shock condition caused by a significant decrease in the contractile function of the left ventricle) or pulmonary swelling. It is worth noting that acute heart failure can directly threaten the life of a person and even lead to a fatal outcome.

Angina(angina pectoris) It is pain syndrome, which, as a rule, occurs after intensive physical exertion. Also angina can appear against the background of psycho-emotional stress or after meals. Stenzardi may manifest itself not only with pain in the chest, but also a sense of discomfort for the sternum. Pain, as a rule, can spread ( irradiate) In the left hand, between the blades, in the neck or lower jaw. The duration of pain during angina does not exceed 15 minutes. It is worth noting that angina region can lead to myocardial infarction against the background of the damage to the coronary arteries of the heart.

Atrioventricular blockade of the heartit is one of the types of the blockade of the heart, in which there is a violation of the pulse from the atria of the heart to the ventricles. An atrioventricular blockade most often leads to a violation of the heart rhythm. It is worth noting that there are three degrees of the blockade of an atrioventricular node. Incorrect intravenous administration of verapamil can cause an atrioventricular blockade of 3 degree for which the reduction in heart rate is characterized to 20 and below. Full atrioventricular blockade ( lack of electrical impulses to ventricles) leads to a complete stopping of cardiac activity and a fatal outcome.

Asistoliait is a complete cessation of cardiac activity. The ashistolia of the ventricles is the cause of the heart stop at about 3 - 5% of cases.

Allergic manifestations

Drug allergies can occur almost on any medicinal product. As a rule, the drug allergies is manifested by the occurrence of skin rashes and itching.

When receiving verapamil, the following allergic manifestations may be observed:

stevens - Johnson syndrome.

Hivesit is characterized by the appearance of itching blisters on the skin ( skin rash). This form of an allergic reaction occurs due to the release of a large number of histamine ( allergic reaction mediator), which is involved in increasing the permeability of the vascular wall of the capillaries ( small vessels), which leads to the emergence of edema of surrounding tissues. Skin rash is most often symmetrical and reminds blistering with a nettle burn. After the discontinuation of the medication, the skin rash completely disappears.

Stevens Syndrome - Johnson, or malignant exudative erythema, is a rather serious allergic reaction. This syndrome is manifested by the appearance on the skin and mucous membranes of the eyes, the oral cavity, pharynx, the genital organs of pinkish-red bubbles ( papula) who may have a different size ( from a few millimeters to several centimeters). Most often the skin of the forearm, brushes, stops, shins and faces are affected. After opening data, the papules on the mucous membranes and the skin remains strongly painful bleeding areas. It should be noted that this type of skin rash is accompanied by a strong itch. Also, Stevens - Johnson syndrome is often accompanied by fever, headache, as well as pains in the joints.

Violations by the central and peripheral nervous system

The reduction in heart rate frequency inevitably leads to oxygen starvation of the brain. Nerve cells ( neurons) Very sensitive to the lack of oxygen, which is necessary for their normal functioning. With a decrease in the pumping function of the heart, arterial blood does not sufficiently feed the nerve tissues of the brain, which can lead to various disorders and pathological conditions.
bloodfaction, soreness, as well as edema gum. Hyperplasia occurs due to the violation of the calcium yield from the tissues of the gum, which further leads to a circulation disorder. Ultimately, the decane functional tissue is replaced on the connecting tissue ( collagen).

Constipationit occurs most often with long-term reception of verapamila. As a rule, constipation has an atony character for which the decrease in the tone of the intestine muscles is characteristic. The cessation of reception of verapamil in the absolute majority of cases normalizes the work of the intestine.

Increased hepatic samplesit arises due to the fact that verapamil is metabolized in the liver. The disintegration products of this drug are able to violate the normal functioning of hepatic cells ( hepatocytes). As a result, various enzymes fall from hepatocytes to the blood ( alaninaotransferase, Aspartataminotransferase, alkaline phosphatase), which normally should not penetrate the bloodstream.

Approximate cost of medication

Verapamil and its analogues can be found in almost any city of the Russian Federation. Depending on the form of release, the price of this medication may differ slightly.

The average cost of Verapamila

Town	The average cost of medication
Town	Pills	Tablets of prolonged action	Solution for intravenous administration
*Moscow*	21 rubles	142 rubles	23 rubles
*Kazan*	20 rubles	140 rubles	21 rubles
*Krasnoyarsk*	20 rubles	138 rubles	20 rubles
*Samara*	19 rubles	137 rubles	20 rubles
*Tyumen.*	22 rubles	142 rubles	24 rubles
*Chelyabinsk*	24 rubles	145 rubles	26 rubles

Verapamil

Latin name

Verapamil.

Chemical name

alfa-methylamino] propyl] -3,4-dimethoxy- alpha- (1-methyl ethyl) benzelacetonitrile (and in the form of hydrochloride)

Gross formula

C 27 H 38 N 2 O 4

Pharmacological group

Calcium channel blockers

Nonological Classification (ICD-10)

CAS code

53-53-9

Characteristic

Phenylalkylamine derivative. Verapamila hydrochloride - white crystalline powder. Soluble in water, chloroform, methanol.

Pharmacology

Pharmacological action - antichangal, hypotensive, antiarrhythmic.

Blocks calcium channels (acts from the inside of the cell membrane) and lowers the transmembrane calcium current. Interaction with the channel is determined by the degree of depolarization of the membrane: the open calcium channels of the depolarized membrane more effectively blocks. A lesser extent affects the closed channels of the polarized membrane, preventing them with activation. Slightly affects sodium channels and alpha adrenoreceptors. Reduces the reduction, the driver's frequency of the rhythm of the sinus node and the speed in the AV node, synoyatrile and AV conductivity, relaxes smooth muscles (more from the arterioles than veins), causes peripheral vasodilation, lowers the OPS, reduces post capacity. Increases myocardial perfusion, reduces the imbalance between the need and supply of the heart with oxygen, contributes to the regression of the left ventricular hypertrophy, lowers blood pressure. Prevents development and eliminates spasm of coronary arteries at variant angina. In patients with uncomplicated hypertrophic cardiomyopathy improves blood outflow from ventricles. Reduces the frequency and severity of the headaches of vascular genesis. Inhibits neuromuscular transmission in the pseudogiperrophic Mopathy of Duzhenna and lengthens the recovery period after the application of this image. In vitro blocks the P170 enzyme and partially eliminates the resistance of cancer cells to chemotherapeutic means.

After receiving the inside, more than 90% of the dose is absorbed, bioavailability is 20-35% due to metabolism with the "first passage" through the liver (increases with long-term reception in large doses). The achievement time with MAs is 1-2 h (tablets), 5-7 hours (tablets of prolonged action) and 7-9 h (prolonged action capsules). Binds with plasma proteins by 90%. Metabolized in the liver with the formation of noverapamila, which has 20% of the hypotensive activity of verapamila, and 11 other metabolites (are defined in trace quantities). T 1/2 When taking an inside of a single dose - 2.8-7.4 hours, during repeated doses - 4.5-12 hours (due to the saturation of enzyme liver systems). When in / in the introduction of T 1/2, two-phase: Early - about 4 minutes, the final - 2-5 hours. When taking into account, the beginning of action is marked after 1-2 hours. Under conditions in / in administration, antiarrhythmic action is developing within 1-5 Min (usually less than 2 min), hemodynamic effects - for 3-5 minutes. The duration of action is 8-10 hours (pills) or 24 hours (capsules and tablets of prolonged action). When in / in administration, an antiarrhythmic action lasts about 2 hours, hemodynamic - 10-20 minutes. The main kidneys is excreted and feces (about 16%). It penetrates into breast milk, passes through the placenta and is determined in the blood of the umbilical vein in childbirth. Fast / in Introduction causes a hypotension from a mother leading to a distress of the fetus. With a long reception, the clearance decreases and bioavailability increases. Against the background of severe liver function, the plasma clearance decreases by 70% and T 1/2 increases to 14-16 hours.

According to the results obtained in 2-year experiments on rats when administered in doses, 12 times larger than the MARDCH, and in the Bacterial test of the Eix (5 of the studied strains, the dose - 3 mg per cup, with or without metabolic activation) does not have carcinogenic and mutagenic activity. In experiments on rats in doses, 6 times larger than the dose, recommended for a person, slows down the growth of the fetus and increases the frequency of the intrauterine death of the fruit.

Application

Paroxysmal superstricular tachycardia (except WPW-syndrome), sinus tachycardia, atrial extrasystole, flickering and fluttering atrial, angina (including printelastal, voltage, post-infarction), arterial hypertension, hypertensive crisis, idiopathic hypertrophic stenosis, hypertrophic cardiomyopathy.

Contraindications

Hypersensitivity, pronounced hypotension (garden less than 90 mm Hg. Art.), Cardiogenic shock, AV blockade of II and III degree, myocardial infarction (acute or recently transferred and complicated bradycardia, hypotension, left bonded deficiency), severe bradycardia (less than 50 ° C. / min), chronic heart failure stage III, fluttering and fibrillation of atrial and WPW-syndrome or Louun-Ganong-Levin syndrome (except patients with a pacemaker), a sine node weak syndrome (if the electrocardiomator is not implanted), the synodatrial blockade, Morganya syndrome - Adams - Stokes, digitalistic intoxication, heavy stenosis of the mouth of aorta, pregnancy, breastfeeding.

Restrictions on application

AV Degree Blocade, chronic heart failure I and II stages, light or moderate hypotension, expressed myopathy (Duzhenne syndrome), renal and / or liver failure, ventricular tachycardia with a wide QRS complex (for I / in maintenance).

Application in pregnancy and breastfeeding

The use of verapamila during pregnancy is possible only when the expected benefit for the mother exceeds the potential risk to the fetus.

At the time of treatment, breastfeeding should be stopped (verapamil is allocated with breast milk).

Side effects

From the side of the cardiovascular system and blood (blood formation, hemostasis): arterial hypotension, bradycardia (sinus), AV blockade, the appearance of heart failure symptoms (when used in high doses).

From the side of the nervous system and the senses: headache, dizziness, nervousness, inhibition, drowsiness, weakness, fatigue, paresthesia.

From the head of the gastrointestinal bodies: nausea, dyspeptic phenomena, constipation; Rarely - gumper hyperplasia, increasing the activity of hepatic transaminases, SFF.

Allergic reactions: skin rash, urticaria, skin itching; Rarely - angioedema edema, Stevens - Johnson syndrome.

Others: hyperemia of the skin of the face, bronchospasm (with / in administration), peripheral edema, very rarely gynecomastia, increasing prolactin secretion (individual cases).

Interaction

Increases the level in the plasma of digoxin, cyclosporine, theophylline, carbamazepine, reduces lithium. Weakens the antibacterial activity of rifampicin, the deprimating effect of the phenobarbital, reduces the clearance of metoprolol and propranolol, enhances the action of the muscle relaxants. Rifampicin, sulfinpyrazone, phenobarbital, calcium salts, vitamin D - weaken action. Hypotensive effect enhance antihypertensive preparations (diuretics, vasodilators), tricyclic and tetracyclic antidepressants and neuroleptics: anti-indant - nitrates. Beta-adrenobloclars, class antiarrhythmics, cardiac glycosides, inhalation anesthetics, radiocontrase substances potentiate (mutually) inhibit influence on the synoatic node automatism, AV conductivity and myocardial reductions. With the simultaneous use of verapamil with acetylsalicylic acid - strengthening of existing bleeding. Cimetidine increases the content of verapamil in the plasma.

Overdose

Symptoms: arterial hypotension, bradycardia, AV blockade, cardiogenic shock, coma, asistolia.

Treatment: Calcium gluconate (10-20 ml of 10% V / c) is used as a specific antidote; In bradycardia and AV blockade, atropine, isoprenaline or orcproenaline are introduced; under hypotension - plasma-substituting solutions, dopamine, norepinephrine; With the manifestation of signs of heart failure - Dobutamine.

Method of application and dose

Inside. The dosing mode and the duration of treatment are established individually depending on the state of the patient, the degree of severity, the characteristics of the course of the disease and the effectiveness of therapy. For the prevention of angina attacks, arrhythmias and in the treatment of arterial hypertension prescribed adults in the initial dose of 40-80 mg 3-4 times a day. If necessary, increase the one-time dose to 120-160 mg. Maximum daily dose - 480 mg. In patients with pronounced liver disorders, the removal of verapamil is slowed down, so treatment is advisable to start with minimal doses; The daily dose should not exceed 120 mg.

V / in slowly: an adult initial dose of 5-10 mg (for at least 2 minutes) under the control of blood pressure, heart rate and an ECG, with an insufficient effect, repeated administration is possible after 30 minutes at a dose of 10 mg. Children up to 1 year at a dose of 0.1-0.2 μg / kg (usually one-time dose is 0.75-2 mg), for at least 2 minutes, for children 1-15 years in a dose of 0.1-0.3 mg / kg for at least 2 minutes (usually one-time dose is no more than 2-5 mg). With a hypertensive crisis - 5-10 mg V / in slowly.

Precautions

Caution is prescribed to patients with hypertrophic cardiomyopathy, complicated by the obstruction of the left ventricle, the high pressure of the jam in the pulmonary capillaries, the paroxysmal night shortness of breath or ortope, disruption of the function of the sinus-atrial node. When prescribing to patients with a pronounced violation of the liver function and neuromuscular transmission (Durane Moopathy), constant medical control is needed and perhaps a reduction in the dose. With caution to apply during operation to drivers of vehicles and people whose profession is associated with an increased concentration of attention (the reaction rate is reduced), it is recommended to exclude alcohol intake.

special instructions

An injection form is incompatible with albumin, injection forms of amphotericin B, hydralazine, sulfamethoxazole, trimethopril and can fall into a pH solution above 6.0.

Year of the last adjustment

2008

Interactions with other active substances

Akarbossa *	Against the background of verapamil, the effect of acarbosa is weakened; When combined purpose, constant control of blood glucose concentration is necessary.
Atenolol * + Chlortalidon *	Against the background of verapamil, chrono-, foreign and drromotropic effects are enhanced.
Atrakuria Beales *
Acebutolol *	Acebutolol increases (mutually) hypotensive effect and the likelihood of violations of automatic, conductivity, and myocardial reductions, enhances the negative effect on heart rate (severe bradycardia), AV conductivity (up to full blockade) and / or heartfelt reduction.
Acetylsalicylic acid	Against the background of verapamil, hypocoagulation activity increases and existing bleeding increases.
Bumetanide *	Bometanide can enhance (mutually) hypotensive effect.
Valsartan *	Valsartan enhances (mutually) hypotensive effect.
VECURIONIY Bromide *	Against the background of verapamila, a minelaxation is enhanced and prolonged.
Galotan *	Gatalus enhances the oppression of the functions of the CSS (anticipation of hypotension and the inhibition of AV conductivity).
Hydralazine *	Hydralazine enhances (mutually) hypotensive effect.
Hydrochlorothiazide * + Captive *	The combination of hydrochlorothiazide + captopril enhances (mutually) hypotensive effect.
Digitoxin *	Digitoxine enhances (mutually) bradycardia and the inhibition of conductivity in the AV node. Against the background of verapamil can decline almost a third clearance.
Digoxin*	Against the background of verapamil due to a decrease in clearance and / or V SS, the concentration of digoxin in the blood and the risk of toxicity increases.
Dizeciramide *	Dizeciramide increases the risk of ventricular arrhythmia, reduces the minute volume of the heart; It should not be prescribed 48 hours before or within 24 hours after verapamila (deaths are described).
Diltialand *	Diltiazem enhances (mutually) effects.
Doxorubicin *	According to experimental data, on the background of verapamil, the initial peak of concentration in the heart increases with an increase in the frequency and severity of degenerative changes of myocardium, accompanied by shorter of survival terms.
Indomethacin *	Indomethacin weakens the hypotensive effect due to the inhibiting GHG in the kidneys, deterioration of blood circulation in them with sodium delay and water.
Isradipine *	Isradipine enhances (mutually) effects.
Kandesartan * Cyiletyl	Candesartan cyractyl enhances (mutually) hypotensive effect.
Carbamazepine *	Against the background of verapamil, the concentration of carbamazepine may increase, which leads to the development of a number of side effects (diplopia, headache, ataxia or dizziness).
Clonidine *	Clonidine enhances (mutually) hypotensive effect.
Telealcyferol *	Decalciferol weakens the hypotensive effect of verapamil.
Lithium Carbonate	With a combined appointment, it is possible to rise in the level of lithium in tissues and enhancing its neurotoxic effects.
Lozartan *	Lozartan enhances (mutually) hypotensive effect.
Methipranolol *	Methipranolol enhances (mutually) hypotensive effect and increases the likelihood of violations of automatism, conductivity and myocardial reductions, increases negative effect on heart rate (severe bradycardia), AV conductivity (up to full blockade) and / or heartfelt reduction.
Metoprolol *	Metoprolol enhances (mutually) hypotensive effect. Against the background of verapamil decreases the clearance of metoprolol.
Mibeffrad *	Mibifradil strengthens (mutually) effects.
Nadolol *	Enhances (Mutually) hypotensive effect and increases the likelihood of violations of automatic, conductivity, and myocardial reductions, the negative impact on heart rate (severe bradycardia), AV conductivity (up to the full blockade) and / or heartfill.
Sodium nitroprusside	Sodium Nitroprusside strengthens (mutually) hypotensive effect.
Nicotine	Nicotine, accelerating biotransformation, reduces the concentration of verapamil in the blood and reduces the severity of anti-inanimal, hypotensive and antiarrhythmic effects.
Octreotide *	Octreotide changes the effect; When sharing may require a dose correction of verapamil.
Perindopril *	Perindopril enhances (mutually) hypotensive effect.
Prazozin *	Prazosi H enhances (mutually) hypotensive effect.
Pramipeksol *	Against the background of verapamil competing for the transport system secreting in the channels of cations, the clearance is reduced (by about 20%).
Propranolol *	Propranolol enhances (mutually) effect and can increase the negative effect on heart rate, AV conductivity and / or heartfill, causing severe bradycardium, AV blockade (up to full). Against the background of verapamil decreases clearance.

Formula: C27H38N2O4, chemical name: alpha-methylamino] propyl] -3,4-dimethoxy-alpha (1-methyl ethyl) benzecenetonitrile (and in the form of hydrochloride).
Pharmacological group: Organotropic agents / Cardiovascular agents / Selective blockers of calcium channels 1 of the class / derivative of diphenylallilamin.
Pharmachologic effect: Antiarrhythmic, hypotensive, antianginal.

Pharmacological properties

Verapamil has a blocking effect on calcium channels (acting from the inside of the cell membrane) and reduces the governmental calcium current. The degree of interaction with the channel is determined by the membrane depolarization level: the most effectively verapamil blocks open channels of the depolarized membrane. Less effect on closed channels with a polarized membrane, preventing them with activation. Almost acts on alpha-adrenoreceptors, and sodium channels. Verapamil reduces the reduction, the speed of the rhythm driver in the AV, the frequency of the rhythm driver in the sinus node, AV and the synoatrile conductivity, the total peripheral resistance of the vessels, a post-load, causes peripheral vasodilation, relaxes smooth muscles (mainly in the arteriols, in the veins less). Increases myocardial perfusion, reduces the difference between the supply and demand of the heart in oxygen, contributes to the opposite development of left ventricular hypertrophy, reduces blood pressure. Removes spasms of coronary arteries during angina and warns their development. In patients with uncomplicated hypertrophic cardiomyopathy makes better blood outflow from ventricles. Reduces severity and frequency and headaches of vascular origin. Verapamil slows the neuromuscular transmission during the pseudo-booster the dunes myopathy and makes more recovery period after the use of the eyewear. Blocks the P170 in vitro enzyme and partially eliminates the immunity of cancer cells to chemotherapeutic drugs. After consuming verapamil inside, more than 90% of the drug dose is absorbed, but bioavailability is only 20-35% due to metabolism in the liver at the first passage, bioavailability increases with long use in large doses. The maximum concentration is achieved after 1 to 2 hours for tablets, after 5 - 7 hours for prolonged tablets, after 7 to 9 hours for prolonged capsules. By 90% binds to plasma proteins. In the liver, Verapamil is metabolized with the formation of novelverpamina, which has 20% hypotensive verapamil activity, and other metabolites (which are determined in small quantities). The half-life when using a single dose inside is 2.8-7.4 hours, with repeated receptions - 4.5-12 hours (due to saturation of hepatic enzyme systems). When administered intravenously, half-life has two phases: early - about 4 minutes, finite - 2-5 hours. When used inside the beginning of the appearance of effects is marked after 1-2 hours. Under the conditions of administration, intravenously antiarrhythmic effect develops for 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 prolonged pills and capsules. When administered intravenously, the antiarrhythmic effect lasts about 2 hours, hemodynamic - 10-20 minutes. Announced by the main images by 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. Fast administration intravenously causes a hypotension from a mother, which leads to a disasterness of the fetus.
With long use, the clearance is reduced and bioavailability increases. With severe liver disorders, the plasma clearance decreases by 70% and half-life increases to 14-16 hours. According to the results that were obtained in 2-year experiments on rats when using doses, which are 12 times higher than the MARDCH, and in the Bacterial tests of EMS, verapamil does not have mutagenic and carcinogenic activity. In experiments on rats in doses, which are 6 times higher than the doses, which are recommended for a person, verapamil slows down the growth of the fetus and increases the frequency of the intrauterine death of the fruit.

Indications

Supported paroxysmal tachycardia (with the exception of WPW-syndrome), atrial extrasystolia, sinus tachycardia, fluttering and flickering atrial, angina (including stress angina, princetale, post-infarction), arterial hypertension, hypertrophic idiopathic stenosis, hypertensive crisis, hypertrophic cardiomyopathy.

The method of use of verapamil and dose

The use of verapamil inside. The duration of treatment and dosing regimen are established individually and depend on the state of the patient, the features of the flow and the severity of the disease, the effectiveness of treatment. For the prevention of arrhythmias, angina 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 reception frequency is reduced), to eat with a small amount of water. If necessary, a one-time dose can be increased to 120-160 mg. The maximum daily dose is 480 mg. In patients with severe liver disorders, the removal of verapamil slowed down, so the therapy is better to start with minimal doses; The daily dose should be no more than 120 mg. Use of verapamil intravenously. To introduce slowly: the initial dose for adults is 5-10 mg (to introduce at least 2 minutes) under the control of the ECG, the pulse rate, blood pressure, in case of insufficient effectiveness it is possible to repeat the introduction after half an hour at a dose of 10 mg. Children up to 1 year for at least 2 minutes 0.1-0.2 μg / kg (usually a single dose 0.75-2 mg), children 1-15 years old for at least 2 minutes 0.1-0.3 mg / kg (usually one-time dose is no more than 2-5 mg). With a hypertensive crisis, intravenously slowly 5-10 mg.
When you pass the next reception of Verapamil to do this when remember, the next reception is made after the set time from last use.
Carefully use in patients with hypertrophic cardiomyopathy, which is complicated by high swing pressure in pulmonary capillaries, obstruction of the left ventricle, ortopnoe or paroxysmal night shortness, disruption of the sinus-atrial node. When used in patients with a pronounced disorder of neuromuscular transmission (Duzhenna myopathy) and the liver operation, constant control of the doctor is necessary and, possibly, a decrease in the dose of the drug. With caution, use drivers while working and people whose professions are associated with a high concentration of attention (since Verapamil decreases the reaction rate). During therapy, verapamil is recommended to eliminate alcohol intake. The injection form of verapamil may fall into a solution in a solution with a pH of more than 6.0.

Contraindications for use

Hypersensitivity, cardiogenic shock, pronounced hypotension (systolic blood pressure is less than 90 mm Hg. Art.), AV blockade 3 and 2 degrees, pronounced bradycardia (pulse frequency less than 50 UD / min), myocardial infarction (recently transferred or acute and complicated bradycardia , hypotension, left ventricular deficiency), chronic heart failure 3 stage, fibrillation and fluttering atrial and Launa-Ganong-Levin syndrome (except patients with a pacemaker) or WPW syndrome, a sine node weak syndrome (if there is no electrocardiotimulator), Morganya syndrome - Adams - Stokes, synoyatrial blockade, digitalistic intoxication, pregnancy, heavy stenosis of the mouth of aorta, breastfeeding.

Restrictions on the use of verapamil

AV blockade 1 degree, light or moderate hypotension, chronic heart failure 2 and 1 stages, myopathy expressed (Durane syndrome), hepatic and / or renal failure, for introducing intravenous ventricular tachycardia with a wide QRS complex.

Application in pregnancy and breastfeeding

The use of verapamil during pregnancy and breastfeeding is contraindicated.

Side effects Verapamila

Digestive system: Nausea, dispersion phenomena, constipation, rarely - increase the activity of alkaline phosphatase and hepatic transaminases, gum hyperplasia;
nervous system: Headache, nervousness, dizziness, inhibition, weakness, drowsiness, paresthesia, fatigue; Allergic reactions: skin rash and itching, urticaria, rarely - Stevens - Johnson syndrome, angioedema edema;
circulation system: sinus bradycardia, arterial hypotension, AV blockade, at high doses - the appearance of heart failure symptoms;
others: Bronchospasm (when administered intravenously), peripheral swelling, hyperemia of the skin of the face, very rarely gynecomastia, increasing the secretion of prolactin (in some cases).

The interaction of verapamil with other substances

It increases the concentration in the plasma of digoxin, theophylline, cyclosporine, carbamazepine, reduces lithium preparations. Reduces the antibacterial activity of rifampicin, the depring effects of phenobarbital, lowers the clearance of propranolol and metoprolol, increases the effects of the muscle relaxants. Rifampicin, phenobarbital, sulfintizon, vitamin D, calcium salts - reduce the effect of verapamila. Hypotensive property increase antihypertensive products (vasodilators, diuretics), tetracyclic and tricyclic antidepressants, neuroleptics; Antianginal effect increase nitrates. Beta-adrenoblays, cardiac glycosides, class IA antiarrimics, X-ray-contrast substances, inhaled anesthetics mutually potentiate the inhibitory effect on AV conductivity, the automatism of the synoatrial assembly and the reduction of myocardium. With the joint use of verapamil with acetylsalicylic acid, existing bleeding is enhanced. Cimetidine increases the level of verapamil in plasma.

Overdose

In the overdose of verapamil, arterial hypotension, AV blockade, bradycardia, coma, cardiogenic shock, asistolia arise. The introduction of calcium gluconate is needed (10-20 ml of a 10% intravenous solution) as a specific antidote; At AV blockade and bradycardia, atropine, orciprenaline or isoprenaline are introduced; under hypotension - dopamine, plasma-substituting solutions, norepinephrine; With the manifestation of signs of heart failure - Dobutamine.