Active substanceVerapamilVerapamil
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  • Dosage form: & nbspfilm coated tablets
    Composition:

    One tablet contains:

    of the active substance: verapamil hydrochloride (in terms of 100% substance) - 40 mg

    Excipients: core - lactose (sugar milk), calcium stearate, potato starch, talc, polysorbate (Tween-80), povidone (polyvinylpyrrolidone low molecular weight); shell - Opadrai II (series 85) (polyvinyl alcohol, partially hydrolyzed, talc, macrogol (polyethylene glycol 3350), titanium dioxide, iron oxide dye, aluminum lacquer based on yellow quinoline, aluminum varnish based on yellow sunset, aluminum lacquer based on indigo carmine ).

    Description:Tablets covered with a film coating of yellow color, round biconvex.
    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). It has an effect in angina pectoris as well as in the treatment of angina with supraventricular rhythm disorders.

    Pharmacokinetics:

    When ingested, more than 90% of the dose taken is absorbed.

    Bioavailability - 10-20%. The maximum concentration (Stach) of the drug in blood plasma is achieved 1-2 hours after oral administration (80-400 ng / ml). Verapamil penetrates through blood-brain and placental barriers. It is metabolized by the "first pass" through the liver. The main metabolites are norverapamil, N-dialkylverapamil and N-dealkylnorveralamyl. Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. Connection with blood plasma proteins

    - 90%. The half-life for 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%) kidneys, about 25% - with bile. The secretion of breast milk is low.

    Indications:

    1. Treatment and prevention of violations heart rate:

    • paroxysmal supraventricular tachycardia;
    • flutter and atrial fibrillation (tachyarrhythmic variant);
    • supraventricular extrasystole;

    2. Treatment and prevention

    • chronic stable angina (stress angina); unstable angina;
    • vasospastic angina (Prinzmetal angina, variant angina);

    3. Treatment of arterial hypertension.

    Contraindications:

    Hypersensitivity to verapamil and other components of the drug, pronounced bradycardia, chronic heart failure II B - III stage, severe arterial hypotension, cardiogenic shock (with the exception of caused by arrhythmia),sinoauric blockade, atrioventricular blockade of stage II and III (excluding patients with an artificial pacemaker), acute myocardial infarction, sinus node weakness syndrome, aortic aortic stenosis, Wolff-Parkinson-White syndrome, Morgagni-Adams-Stokes syndrome, severe left ventricular dysfunction, flutter and atrial fibrillation and WPW - Syndrome or Laun-Ganong-Levin syndrome (except for patients with a pacemaker), acute heart failure, simultaneous use of beta-blockers (intravenously), pregnancy, lactation, age under 18 years (efficacy and safety not established), simultaneous reception of colchicine.

    Carefully:

    With caution it is necessary to appoint patients with atrioventricular blockade of I degree, chronic heart failure I-II stage, expressed violations of the liver and / or kidney function, arterial hypotension, bradycardia, in old age, with delayed neuromuscular transmission.

    Dosing and Administration:

    Verapamil is taken orally during or after a meal, with a small amount of water. Dosing regimen and duration of treatment are set individually independence 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 to adults at 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.

    In patients with severe hepatic impairment, excretion of verapamil from the body is slowed, so it is advisable to start treatment with minimal doses.

    The daily dose of the drug should not exceed 120 mg for patients with severe hepatic insufficiency.

    Side effects:

    When using Verapamil, the following are possible:

    - from the cardiovascular system: possible reddening of the face, pronounced bradycardia, atrioventricular blockade, marked decrease in arterial pressure, the appearance of symptoms of heart failure when using the drug in high doses, especially in predisposed patients, tachycardia; rarely - angina pectoris up to the development of myocardial infarction (especially in patients with severe obstructive lesions of the coronary arteries), arrhythmia (including fibrillation and flutter of the ventricles);

    - from the gastrointestinal tract: nausea, vomiting, constipation, rarely - diarrhea; in some cases - a transient increase in the activity of "liver" transaminases and alkaline phosphatase in the blood plasma;

    - from the central nervous system: dizziness, headache, fainting, anxiety, asthenia, drowsiness, depression, extrapyramidal disorders (ataxia, masky face, shuffling gait, stiffness of hands or feet, trembling of hands and fingers, difficulty swallowing), in rare cases - increased nervous excitability, inhibition , fatigue;

    - allergic reactions: skin rash, itching, hyperemia of the skin of the face, multiforme exudative erythema (including Stevens-Johnson syndrome);

    - Other: gynecomastia, hyperprolactinemia, gingival hyperplasia, weight gain, very rarely - agranulocytosis, galactorrhea, arthritis, transient loss of vision, pulmonary edema, thrombocytopenia, asymptomatic, peripheral edema.

    Overdose:

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

    Treatment: with early detection - gastric lavage, Activated carbon; 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:

    With the simultaneous use of verapamil with:

    - enhances AUC (area under the concentration-time curve) of carbamazepine in patients with stable partial epilepsy (risk of side effects such as diplopia, headache, ataxia and dizziness).

    - enhances AUC, Css (ground clearance) and Cmax (the maximum concentration of the drug) of cyclosporine.

    - enhances AUC and Cmax glibenclamide.

    - increases the concentration of sirolimus and tacrolimus.

    - significantly increases AUC and Cmax buspirone and midazolam.

    - increases the concentration of theophylline (due to lower clearance), ethanol (and lengthens its effect), the concentration of quinidine (the risk of pronounced reduction in blood pressure).

    - can increase the concentration of atorvastatin and lovastatin.

    - increases significantly AUC and Cmax simvastatin.

    - enhances AUC and Cmax almotriptan.

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

    - enhances AUC and Cmax metoprolol and propranolol in patients with angina pectoris.

    - increases the plasma concentration of colchicine (a substrate for CYP3A and p-glycoprotein).

    - when taken orally significantly increases AUC and Cmax doxorubicin.

    - slightly increases AUC imipramine; does not affect the concentration of the active metabolite, desipramine.

    - increases Cmax prazosin and terazosin and AUC terazosin.

    - inhibitors CYP3A (including erythromycin, ritonavir and other antiviral HIV drugs), telithromycin increase plasma concentrations of verapamil.

    - grapefruit juice increases AUC and Cmax R- and S- isomer of verapamil.

    - cimetidine increases the bioavailability of verapamil by almost 40-50% (due to a decrease in hepatic metabolism), so it may be necessary to reduce the dose of the latter.

    - rifampicin can significantly reduce bioavailability (up to 92%), and AUC and Cmax verapamil.

    - Phenobarbital increases the clearance of verapamil 5 times.

    - sulfinpyrazone increases the clearance of verapamil by about 3 times and reduces bioavailability (60%).

    - preparations of St. John's wort penetrate lower AUC R- and S- isomer of verapamil and Cmax.

    - while simultaneous use with inhalation anesthetics increases the risk of bradycardia, atrioventricular blockade, heart failure.

    - a combination with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of developing atrioventricular conduction disorders, bradycardia (the administration of verapamil and beta-blockers should be performed at intervals of several hours)

    - prazosin and other alpha-blockers, as well as other antihypertensive drugs (ATP inhibitors, vasodilators, diuretics, beta-adrenoblockers) increase the hypotensive effect.

    - disopyramide and flecainide should not be administered within 48 hours or 24 hours after the use of verapamil (summation of a negative inotropic effect, up to a lethal outcome).

    - increases the risk of neurotoxic effect of lithium preparations.

    - enhances the action of peripheral muscle relaxants (a change may be required mode of dosing).

    - while simultaneous use with acetylsalicylic acid (ASA), there was a slightly greater increase in bleeding time than with ASA alone.

    - carbamazepine and lithium increases the risk of neurotoxic effects.

    Special instructions:

    To increase blood pressure in patients with hypertrophic cardiomyopathy, alpha-adrenergic stimulants (phenylephrine); Do not use isoprenaline. Before starting therapy for heart failure, it is necessary to achieve a compensated state.

    In the treatment it is necessary to monitor the function of the cardiovascular and respiratory systems, the content of glucose and blood electrolytes, the volume of circulating blood and the amount of urine released.

    It is not recommended to stop treatment suddenly.

    Form release / dosage:Tablets, film-coated, 40 mg
    Packaging:

    10 tablets per contour cell pack.

    For 50 tablets in a jar of light-protective glass or a can of polymer, or a polymer bottle.

    Each jar or bottle, 1, 2 or 5 contour squares together with the instruction for use is placed in a pack of cardboard.

    Storage conditions:

    List B. In a dry, the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the date shown on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-010487/08
    Date of registration:24.12.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp29.01.2017
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