Verapamil tabs 80mg #30

Verapamil instruction for use

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Verapamil is a drug with antiarrhythmic, antianginal and antihypertensive effects.

Release form and composition

Verapamil is available in the following dosage forms:
    Film-coated tablets (10 pcs. In blisters, 1 or 5 blisters in a cardboard box);
    Solution for intravenous administration: colorless, transparent (in colorless glass ampoules of 2 ml, 5 ampoules in blister strip packs, 2 or 10 packs in a cardboard box).
The composition of 1 tablet includes:
    Active ingredient: verapamil hydrochloride - 40 or 80 mg;
    Auxiliary components: dibasic calcium phosphate, starch, butylhydroxyanisole, purified talc, magnesium stearate, gelatin, methylparaben, hydroxypropyl methylcellulose, titanium dioxide, indigo carmine.

Pharmacodynamics

Verapamil is a drug with antiarrhythmic, antihypertensive and antianginal effects. It is a blocker of slow calcium channels. It prevents the transmembrane entry of calcium ions (and, possibly, sodium ions) into the smooth muscle cells of the myocardium and blood vessels, as well as into the cells of the myocardial conduction system. The antiarrhythmic effect of verapamil is probably due to the blockade of the slow channels of the cardiac conduction system. The electrical activity of the sinoatrial and atrioventricular node is affected by the entry of calcium into the cells through slow channels. Verapamil inhibits calcium intake, slows down atrioventricular conduction, which leads to an increase in the effective refractory period in the AV node, depending on the heart rate. In patients with atrial flutter and / or atrial fibrillation, this effect causes a decrease in ventricular rate. Verapamil prevents the re-entry of excitation in the AV node and helps to restore the correct sinus rhythm in patients suffering from paroxysmal supraventricular tachycardia, including the Wolf-Parkinson-White syndrome.
Reception of Verapamil does not affect the conduction of the impulse along additional pathways, and also does not lead to a change in the normal action potential of the atria or the time of intraventricular conduction. In this case, the drug helps to reduce the amplitude, speed of depolarization and impulse conduction in the altered atrial fibers. Verapamil does not cause spasms of peripheral arteries, does not change the total concentration of calcium in the blood serum. The active ingredient helps to reduce afterload and myocardial contractility. The negative inotropic effect of verapamil in most patients (including those with organic lesions of the heart) is offset by a decrease in afterload. Usually, this does not decrease the cardiac index, however, with severe or moderate chronic heart failure (with a pulmonary artery wedge pressure of more than 20 mm Hg and a left ventricular ejection fraction of up to 35%) there is a possibility of acute decompensation of chronic heart failure. As a result of bolus intravenous administration, the maximum therapeutic effect of verapamil occurs after 3-5 minutes. With intravenous administration of Verapamil in a standard therapeutic dose (5-10 mg), a transient, most often asymptomatic, decrease in normal blood pressure, systemic vascular resistance, and contractility is observed. There was a slight increase in the filling pressure of the left ventricle.

Pharmacokinetics

When taken orally:
    absorption: about 90–92% of the drug is absorbed in the gastrointestinal tract. The bioavailability of the drug is low (approximately 20%), which is explained by the effect of the first pass through the liver. The content in blood plasma increases gradually. The maximum plasma concentration is 81.34 ng / ml. The average time to reach the maximum concentration is 4.75 hours. One day after taking the drug, sufficiently high therapeutic concentrations (51.6 ng / ml) are found in the blood plasma. The connection with plasma proteins is about 90%;
    distribution: when taking a single dose, the half-life is from 2.8 to 7.4 hours, and with repeated administration of the drug - from 4.5 to 12 hours. In elderly patients, the half-life increases. Verapamil crosses the blood-brain and placental barriers, is excreted in breast milk;
    metabolism: metabolized in the liver (first pass effect). 12 metabolites of the drug have been recorded, the main of which is the pharmacologically active norverapamil. Other metabolites are mostly inactive;
    excretion: approximately 70% of the taken dose of the drug is excreted in the urine, and approximately 16% or more in the feces for 5 days after oral administration of the drug. In unchanged form, 3-4% is excreted from the body.
When administered intravenously:
    distribution: verapamil is well distributed in body tissues. In healthy volunteers, the volume of distribution is 1.6 to 1.8 l / kg. About 90% binds to plasma proteins;
    metabolism: in the course of metabolic studies in vitro, it has been shown that verapamil is metabolized by isoenzymes CYP1A2, CYP3A4, CYP2C8, CYP2C18 and CYP2C9 of the cytochrome P450 family. When taken orally by healthy volunteers, verapamil was extensively metabolized in the liver to form 12 metabolites, most of which were present in trace amounts. The main metabolites include forms of O- and N-dealkylated derivatives of verapamil. Studies in dogs have shown that only norverapamil is a pharmacologically active metabolite (about 20% compared to the parent compound). Verapamil crosses the blood-brain and placental barriers, in small amounts it is excreted in breast milk;
    elimination: the curve of changes in the content of the drug in the blood has a biexponential character with a fast early phase of distribution (half-life - about 4 minutes), as well as a slower terminal phase of elimination (half-life - from 2 to 5 hours). Within 24 hours, approximately 50% of the dose of the drug is excreted by the kidneys, within 5 days - 70%. About 16% of the dose of verapamil is excreted through the intestines. In unchanged form, 3-4% of verapamil is excreted from the body. The total clearance of verapamil approximately corresponds to the hepatic blood flow - about 1 L / h / kg (range from 0.7 to 1.3 L / h / kg).
In case of impaired renal function, the pharmacokinetic parameters of the drug do not change, which was recorded during studies in two groups of patients: without impaired renal function and with renal failure in the terminal stage. Norrapamil and verapamil are not excreted by hemodialysis.
The age index can change the pharmacokinetic parameters of the drug when used in patients with arterial hypertension. In elderly patients, the half-life may be increased. The relationship between age and the antihypertensive effect of the drug has not been identified.

Indications for use

    Heart rhythm disorders, including paroxysmal supraventricular tachycardia, atrial fibrillation and flutter (tachyarrhythmic variant), supraventricular extrasystole - for treatment and prevention;
    Unstable angina (angina at rest), chronic stable angina (exertional angina), vasospastic angina (variant angina, Prinzmetal angina) - for treatment and prevention;
    Arterial hypertension - for treatment.

Contraindications

Absolute:
    Chronic heart failure stage IIB-III;
    Morgagni-Adams-Stokes syndrome;
    Sinoatrial blockade;
    Sick sinus syndrome;
    Cardiogenic shock (other than those caused by arrhythmia) (for pills);
    Severe bradycardia (for tablets);
    Wolff-Parkinson-White syndrome (for pills);
    Acute heart failure (for pills);
    Atrioventricular block II and III degree (except for patients with an artificial pacemaker) (for tablets);
    Simultaneous therapy with intravenous administration of beta-blockers;
    Age under 18;
    Hypersensitivity to drug components.
Relative (the drug should be used with caution in the presence of the following conditions / diseases):
    1st degree atrioventricular block;
    Bradycardia;
    Severe functional disorders of the kidneys and liver;
    Arterial hypotension with systolic pressure below 100 mm Hg. (for tablets);
    Chronic heart failure of I and II degrees (for tablets) and I and IIA degrees (for injection solution);
    Simultaneous reception with beta-blockers (for injection solution);
    Myocardial infarction with left ventricular failure (for injectable solution);
    Elderly age (for injection solution).

Instructions for the use of Verapamil: method and dosage

Verapamil is taken orally with a small amount of water, preferably during or after meals.
The doctor sets the dosage regimen and duration of therapy individually, depending on the patient's condition, the severity and characteristics of the course of the disease, as well as the effectiveness of the drug.
The initial adult single dose for the treatment of arterial hypertension and for the prevention of angina attacks, arrhythmias is 40-80 mg, the frequency of administration is 3-4 times a day. A single dose, if necessary, is increased to 120-160 mg (maximum - 480 mg per day).
With pronounced functional disorders of the liver, it is advisable to start therapy with the lowest doses (maximum 120 mg per day).

Side effects

    Central nervous system: headache, dizziness; in rare cases - lethargy, increased nervous excitability, increased fatigue;
    Digestive system: vomiting, nausea, constipation; in some cases - a transient increase in the activity of hepatic transaminases in the blood plasma;
    Cardiovascular system: facial flushing, AV blockade, severe bradycardia, arterial hypotension, the appearance of symptoms of heart failure (when using high doses of the drug, especially in predisposed patients);
    Allergic reactions: itching, skin rash;
    Others: peripheral edema.

Overdose

Symptoms: a pronounced decrease in blood pressure (sometimes to a level that cannot be measured), loss of consciousness, shock, escaping rhythm, atrioventricular block of I or II degree (Wenckebach periods with or without a slip rhythm are often observed), complete atrioventricular block, accompanied by complete atrioventricular dissociation, cardiac arrest, sinus node arrest, sinus bradycardia, heart failure, sinoatrial blockade, asystole.
In case of early detection (it should be borne in mind that when taken orally, the release and absorption of the drug in the intestine occurs within 2 days), gastric lavage is prescribed if no more than 12 hours have passed since the application. With reduced motility of the gastrointestinal tract (in the absence of intestinal noises), this measure can be carried out in later periods.
Treatment is symptomatic and depends on the clinical picture of the overdose.
Calcium is a specific antidote. For the treatment of an overdose, a solution of calcium gluconate 10% (10-30 ml) is administered intravenously or slowly as a drop infusion. If necessary, the procedure can be repeated.
With sinus bradycardia, atrioventricular block II and III degree, cardiac arrest, isoprenaline, atropine, orciprenaline or cardiac stimulation are indicated.
With arterial hypotension, norepinephrine (norepinephrine), dobutamine, dopamine are prescribed. Hemodialysis is ineffective.

Special instructions

During therapy, it is necessary to monitor the function of the respiratory and cardiovascular systems, the level of electrolytes and glucose in the blood, the amount of urine excreted and the volume of circulating blood.
With intravenous administration of the drug, it is possible to lengthen the PQ interval at a plasma concentration above 30 mg / ml.
It is not recommended to stop therapy suddenly.
The drug should be used with caution by vehicle drivers and people whose profession is associated with increased concentration of attention (due to a decrease in the reaction rate).

Application during pregnancy and lactation

According to the instructions, the drug is contraindicated for use during pregnancy and lactation.
There are no data on the use of the drug in pregnant women.
In the course of animal studies, no direct or indirect toxic effect on the reproductive system has been identified. Since the results of animal studies do not reliably predict the response to drug therapy in humans, Verapamil during pregnancy can be used only in cases where the potential benefit to the mother is higher than the expected risk to the child.
The drug is characterized by penetration through the placental barrier, it is also found in the blood of the umbilical vein during childbirth.
Verapamil and metabolites are excreted in breast milk. According to the limited data available, the dose of the drug that a breastfeeding infant receives with milk is quite low (from 0.1 to 1% of the amount taken by the mother of Verapamil). Since the likelihood of complications for infants cannot be ruled out, the drug during breastfeeding is allowed to be used only in cases where the potential benefit to the mother is higher than the expected risk to the child.

Pediatric use

It is forbidden to use the drug to treat patients under the age of 18 years.

With impaired renal function

In severe renal failure, the drug should be used with caution, prescribing a lower initial dose.

For violations of liver function

In case of impaired liver function and severe hepatic insufficiency, the drug should be used with caution, prescribing a lower starting dose.

Use in the elderly

In the treatment of elderly patients, a lower initial dose is recommended.

Drug interactions

With the simultaneous use of the drug with certain drugs, the following effects may occur:
    Antiarrhythmics, beta-blockers and inhalation anesthetics: increased cardiotoxic effect (the risk of developing atrioventricular block, a sharp decrease in heart rate, the development of heart failure, a sharp decrease in blood pressure increases);
    Antihypertensive drugs and diuretics: strengthening the hypotensive effect of the drug;
    Digoxin: an increase in the level of concentration of digoxin in the blood plasma (to identify the optimal dosage of the drug and prevent intoxication, its level in the blood plasma should be monitored);
    Cimetidine and ranitidine: an increase in the concentration of the drug in blood plasma;
    Theophylline, prazosin, cyclosporine: an increase in their concentration in blood plasma;
    Muscle relaxants: strengthening the muscle relaxant action;
    Rifampicin, phenobarbital: a decrease in the concentration of the drug in blood plasma and a weakening of its action;
    Acetylsalicylic acid: an increase in the likelihood of bleeding;
    Quinidine: an increase in the level of concentration of quinidine in the blood plasma, an increased risk of lowering blood pressure, in hypertrophic cardiomyopathy - the development of severe arterial hypotension;
    Carbamazepine, lithium: increased risk of neurotoxic effects.

Terms and conditions of storage

Store in a dark, dry place out of reach of children at temperatures up to 25 ° C.
The shelf life is 3 years.

Reviews

Reviews of Verapamil indicate that the drug is an effective remedy for the treatment of arrhythmias, tachycardia, arterial hypertension, stable exertional angina.
During pregnancy Verapamil is used to treat tachycardia, cardiac arrhythmias, to reduce the tone of the uterus. Reviews about the effectiveness of the drug in this period are ambiguous.
Many users note such an advantage of Verapamil as its low cost. The most common side effects are constipation, flushing, and bradycardia.

Terms of sell

You don't need a prescription to buy Verapamil.