Active substanceVerapamilVerapamil
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  • Dosage form: & nbspcoated tablets
    Composition:Active substance: verapamil hydrochloride (in terms of 100% substance) - 40 mg or 80 mg;

    Excipients: lactose monohydrate 26.12 mg / 52.24 mg, potato starch 9.5 mg / 19.0 mg, talc 0.375 mg / 0.75 mg, calcium stearate 0.375 mg / 0.75 mg, povidone K 17 - 3.63 mg / 7.26 mg;

    Shell accessories: polysorbate 80 (Tween 80) 0.2 mg / 0.4 mg, titanium dioxide 0.614 mg / 1.228 mg, hypromellose hydroxypropyl methyl cellulose 1.06 mg / 2.12 mg, beeswax yellow 0.002 mg / 0.004 mg, paraffin liquid -0.12 mg / 0.24 mg, tropeoline O-0.004 mg / 0.008 mg.

    Description:

    Round tablets of biconvex form, covered with a shell of yellow color.

    Pharmacotherapeutic group:The blocker of "slow" calcium channels
    ATX: & nbsp

    C.08.D.A.01   Verapamil

    C.08.D.A   Phenylalkylamine derivatives

    Pharmacodynamics:

    Verapamil is one of the main drugs group of blockers of "slow" calcium channels. It has antiarrhythmic, anti-anginal and antihypertensive activity.

    The drug reduces the need for myocardium in oxygen by decreasing myocardial contractility and reducing the heart rate.Causes the enlargement of the coronary vessels of the heart and increases coronary blood flow; reduces the tone of the smooth muscles of peripheral arteries and the general peripheral vascular resistance.

    Verapamil significantly slows the atrioventricular conduction, depresses the automatism of the sinus node, which allows the use of the drug for the treatment of supraventricular arrhythmias.

    Verapamil is the drug of choice for the treatment of angina of vasospastic genesis (Prinzmetal angina). Has an effect with angina pectoris.

    The action of verapamil begins 1-2 hours after ingestion, the maximum effect develops in most cases after 48 hours.

    Pharmacokinetics:

    When ingested, more than 90% of the dose taken is absorbed. Bioavailability is 10-20%. The maximum concentration of the drug in the blood plasma is achieved 1-2 hours after ingestion (80-400 mg / ml). Verapamil penetrates through blood-brain and placental barriers. It is metabolized by "primary passage" through the liver. The main metabolites are norverapamil, N-dealkylnorverapamil.Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. Connection with plasma proteins, blood - 90%, Half-life with a single dose is 2.8 - 7.4 hours; when taking repeated doses - 4,5 - 12 hours. It is excreted in a small amount in unchanged form (3-4%), the rest - in the form of metabolites (70%) by the kidneys, about 25 % - with bile. The secretion of breast milk is low.

    Indications:

    - Arterial hypertension.

    - Coronary heart disease, including chronic stable angina (classic angina pectoris); unstable angina; angina due to vascular spasm (Prinzmetal angina).

    - Paroxysmal supraventricular tachycardia.

    - Atrial fibrillation / flutter, accompanied by tachyarrhythmia (with the exception of Wolff-Parkinson-White syndrome and Laun-Ganong-Levin syndrome).

    Contraindications:

    Hypersensitivity to the components of the drug, severe bradycardia (less than 50 beats per minute), chronic heart failure in the stage of decompensation, arterial hypotension (below 100/60 mm Hg, in men and 95/60 mm Hg in women), cardiogenic shock (except for caused by arrhythmia), sinoatrial block,atrioventricular blockade of II and III degree (excluding patients with an artificial pacemaker); acute myocardial infarction complicated by bradycardia, severe arterial hypotension and left ventricular failure, sinus node weakness syndrome (except for patients with an artificial pacemaker), aortic aortic stenosis, Wolff-Parkinson-White syndrome, Morgagni-Adams-Stokes syndrome, concurrent use of beta- adrenoblockers (intravenously); Laun-Ganong-Levin syndrome, simultaneous reception of colchicine, lactose intolerance, lactase deficiency, glucose-galactose malabsorption, pregnancy, lactation, age under 18 years.

    Carefully:

    With caution, the drug is indicated to patients with atrioventricular blockade of the 1st degree, marked violations of liver and kidney function, in old age, with bradycardia, hypertrophic obstructive cardiomyopathy, with diseases related to neuromuscular transmission (myasthenia gravis gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy).

    Pregnancy and lactation:

    Verapamil is contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Verapamil is taken orally during or after a meal, with a small amount of water.

    Dosage regimen and duration of treatment are set individually depending on the patient's condition, severity, the features of the course of the disease and the effectiveness of therapy.

    To prevent attacks of angina pectoris, arrhythmia and in the treatment of hypertension, the drug is prescribed in an initial dose of 40-80 mg 3-4 times a day. If necessary, increase the single dose to 120-160 mg. The maximum daily dose of the drug is 480 mg.

    With prolonged treatment, the daily dose of 480 mg should not be exceeded. In the maximum dose, the drug must be taken only in a hospital.

    In patients with severe hepatic impairment, withdrawal of verapamil from the body is slow, so it is advisable to start treatment with minimal doses. The daily dose of the drug should not exceed 120 mg.

    Side effects:

    From the cardiovascular system: AV blockade I, II, III degree, stopping the sinus node, peripheral edema, tachycardia, sinus bradycardia, heart failure, pronounced lowering of blood pressure, "tides" of blood to the skin of the face, palpitation.

    From the gastrointestinal tract: nausea, vomiting, pain and discomfort in the abdomen, intestinal obstruction, constipation, diarrhea, gingival hyperplasia, increased appetite; transient increase in "hepatic" transaminases and alkaline phosphatase in blood plasma;

    From the central nervous system: dizziness, ringing in the ears, headache, fainting, anxiety, confusion, fatigue, asthenia, somnolence, depression, extrapyramidal disorders, paresthesias, tremor. Allergic reactions: skin itching, urticaria, skin rash, multiforme exudative erythema (including Stevens-Johnson syndrome), angioedema.

    Other: weight gain, agranulocytosis, gynecomastia, hyperprolactinemia, galactorrhea, arthritis, pulmonary edema, thrombocytopenia asymptomatic, purpura, peripheral edema, alopecia, muscle weakness, myalgia, arthralgia, erectile dysfunction.

    Overdose:
    Symptoms: sinus bradycardia, atrioventricular block passing in a high degree, sometimes asystole expressed lowering blood pressure, heart failure, shock, sinus arrest, hyperglycemia, stupor and metabolic acidosis.
    Treatment for early detection - washing the stomach, taking activated charcoal, setting an artificial pacemaker; with rhythm and conduction disturbances - intravenous injection of isoprenaline, norepinephrine, atropine, 10-20 ml of 10% calcium gluconate solution, artificial pacemaker; intravenous infusion of plasma-substituting solutions. Hemodialysis is not effective.
    Interaction:

    When used simultaneously with carbamazepine in patients with persistent partial epilepsy due to inhibition of the metabolism of carbamazepine in the liver verapamil strengthens its effect (risk of side effects from the central nervous system, such as diplopia, headache, ataxia and dizziness).

    With simultaneous application verapamil inhibits the metabolism of cyclosporine in the liver, which leads to a decrease in its excretion and an increase in the concentration in the blood plasma. This is accompanied by increased immunosuppressive action.

    With simultaneous application verapamil increases the concentration of theophylline (due to lower clearance).

    With the simultaneous use of verapamil with quinidine, the concentration of quinidine in the blood plasma increases(the risk of a marked decrease in blood pressure especially in patients with hypertrophic obstructive cardiomyopathy).

    With simultaneous application verapamil increases the concentration of ethanol in blood plasma and lengthens its effect.

    Because the verapamil inhibits the isoenzyme of supSa4, which is involved in the metabolism of atorvastatin, lovastatin and simvastatin, there may be manifestations of drug interaction caused by an increase in the concentrations of statins in the blood plasma (rhabdomyolysis).

    With simultaneous application verapamil increases the concentration in the blood plasma of almotriptan, glibenclamide.

    With simultaneous application verapamil increases the concentration in blood plasma of sirolimus and tacrolimus.

    With simultaneous application verapamil increases the concentration of cardiac glycosides (requires careful monitoring and reduction of the dose of glycosides). With simultaneous application verapamil increases the concentration of metoprolol and propranolol in patients with angina.

    With simultaneous application verapamil increases the plasma concentration of colchicine (a substrate for the isoenzyme of syrPa and p-glycoprotein).

    With the simultaneous use of verapamil with doxorubicin, the concentration of doxorubicin in the blood plasma increases and its effectiveness increases.

    With the simultaneous use of verapamil with imipramine, the concentration of imipramine in the blood plasma increases (the risk of unwanted changes caused by additive inhibitory action, verapamil and imipramine on AVconductivity). Does not affect the concentration of the active metabolite, desipramine.

    Verapamil increases the concentration of prazosin and terazosin with simultaneous use (risk of development of severe arterial hypotension).

    With the simultaneous use of verapamil with buspirone or midazolam, their concentration in the blood plasma increases (the risk of side effects). Inhibitors of supSa4 (including erythromycin, human immunodeficiency virus protease inhibitors), telithromycin increase plasma concentrations of verapamil.

    Grapefruit juice increases the concentration in the blood plasma r- and s-isomer of verapamil.

    Cimetidine either does not alter, or reduces the clearance of verapamil (possibly enhancing the effects of verapamil).

    Rifampicin can significantly reduce bioavailability (up to 92%), as well as the concentration of verapamil in blood plasma, which leads to a decrease in its clinical effectiveness.

    Phenobarbital increases the clearance of verapamil 5 times.

    Sulfinpyrazone increases the clearance of verapamil by about 3 times and reduces bioavailability to 60%.

    Preparations of St. John's wort penetrate reduce the concentration r- and sisomer of verapamil in blood plasma.

    With the simultaneous use of verapamil with inhalational anesthetics, the risk of developing bradycardia, atrioventricular blockade, and heart failure is increased. The combination of verapamil with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of developing atrioventricular conduction disorders, bradycardia (verapamil and beta-blockers should be used at intervals of several hours).

    Prazosin and other alpha-blockers, as well as other antihypertensive drugs (angiotensin-converting enzyme inhibitors, vasodilators, diuretics, beta-adrenoblockers) increase the antihypertensive effect of verapamil.

    With the simultaneous use of verapamil with disopyramide and flecainide, severe arterial hypotension and collapse are possible, up to a lethal outcome.The risk of developing severe manifestations of drug interaction is associated with an increase in the negative inotropic effect. Do not administer dysopyramide and flecainide for 48 hours before or 24 hours after the use of verapamil, Verapamil increases the risk of neurotoxic effect of lithium preparations.

    Verapamil enhances the effect of peripheral muscle relaxants (may require a change in the dosage regimen).

    With the simultaneous use of verapamil with acetylsalicylic acid, cases of increased bleeding time are described.

    Special instructions:

    With an increase in blood pressure in patients with hypertrophic obstructive cardiomyopathy, alpha-adrenostimulators are prescribed (phenylephrine); Do not use isoprenaline.

    Before, the beginning of therapy for heart failure, it is necessary to achieve a state of compensation. In the treatment of cardiovascular and respiratory system monitoring, glucose concentration and blood electrolyte content, circulating blood volume and urine output are necessary.

    It is not recommended to stop the treatment suddenly "on" the drug can not be abruptly abolished,it is recommended to gradually reduce the dose until the drug is completely discontinued.

    When taking the drug, it is necessary to monitor kidney function in patients with impaired renal function.

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

    After taking verapamil, individual reactions (drowsiness, dizziness) that affect the ability to perform work requiring high concentration of attention and speed of psychomotor reactions are possible. With caution apply during work drivers of vehicles and people whose profession is associated with increased concentration of attention (reduces the reaction rate).

    Form release / dosage:

    The coated tablets are 40 mg and 80 mg.

    Packaging:

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 50 tablets in a can of polymer or a bottle of polymer.

    Each jar or bottle, 2, 4 or 5 contour packs together with the instruction for use is placed in a pack of cardboard.

    Storage conditions:

    In dry, protected from light and out of reach of children at a temperature of no higher than 25 ° C.

    Shelf life:

    3 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002664
    Date of registration:29.02.2012 / 20.02.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:AVVA RUS, OJSC AVVA RUS, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp29.01.2017
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