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

    1 tablet contains;

    Active substance: Verapamil hydrochloride is 80 mg.

    Auxiliary substances of the core: Lactose monohydrate (sugar milk) - 30 mg, potato starch - 43.6 mg, calcium stearate - 1.6 mg, talc - 4.8 mg,

    Shell accessories: polysorbate-80 - 0.76 mg, titanium dioxide 0.36 mg, methyl cellulose MC-15 2.512 mg, beeswax 0.162 mg, vaseline oil 0.2 mg, tropelin-O dye, or quinoline yellow E- 104 0.006 mg.

    Description:

    Round, biconvex tablets, covered with a film coat from light yellow to yellow. On the cross section, the nucleus is white or almost white in color.

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

    C.08.D.A.01   Verapamil

    C.08.D.A   Phenylalkylamine derivatives

    Pharmacodynamics:

    The blocker of "slow" calcium channels (inhibits the transmembrane transport of calcium ions to the contractile fibers of smooth muscle cells of the myocardium and coronary vessels). Has antianginal, antiarrhythmic, antihypertensive and antihypertensive effect.The antianginal effect is associated with both direct action on the myocardium at the level of cellular metabolic processes, and with an indirect effect on the cardiac muscle due to decreased afterload.

    Blocking the flow of calcium ions to the contractile fibers of the smooth muscle cells of the coronary arteries, increases myocardial perfusion, even in post-stenotic areas, and eliminates, stops coronary spasm.

    The hypotensive effect of verapamil is due to a decrease in the overall resistance of peripheral vessels without a compensatory increase in the heart rate (heart rate). Verapamil does not affect normal blood pressure (BP).

    Verapamil has a pronounced antiarrhythmic effect, especially with supraventricular arrhythmia, delays the impulse in the atrioventricular (AV) node, as a result of which the sinus rhythm is restored and / or the frequency of ventricular contractions is normalized depending on the type of arrhythmia. Verapamil does not affect or slightly reduces the heart rate.

    The beginning of the action when taken orally - after 1-2 hours, the maximum effect develops in 30-90 minutes, the duration of action is 8-10 hours.
    Pharmacokinetics:

    When ingestion is rapidly absorbed in the small intestine, absorption - 90-92%, bioavailability after a single intake - 24-35 % due to intensive metabolism during primary passage through the liver and increases by 1.5-2 times with prolonged use. With prolonged use in increasing doses bioavailability may increase. Time to reach the maximum concentration (TCam) for oral administration - 1-2 hours. The maximum concentration is 80-400 ng / ml. Connection with plasma proteins

    - 90%. Penetrates through the blood-brain barrier, placental barrier and into breast milk (in low concentrations).

    Rapidly metabolized in the liver by N-dealkylation and O-demethylation, with the formation of several metabolites (12 have been identified in humans). Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. The main pharmacologically active metabolite is noraverapamil (20% of the hypotensive activity of verapamil). In the metabolism of verapamil, isozymes participate CYP3A4, CYP3A5 and CYP3A7.

    Half-life with oral administration - 3-7 hours with a single admission, 4-12 hours - with prolonged use (in connection withsaturation of the enzyme systems of the liver and increased plasma concentrations, the elimination half-life almost doubles). With hepatic insufficiency increases bioavailability and increases the half-life. Output 70% of the kidneys (3-5% unchanged), 16-25 % - through the intestines. It is not excreted by hemodialysis.

    Indications:

    - Treatment and prevention of cardiac arrhythmias: paroxysmal supraventricular tachycardia; flutter and atrial fibrillation (tachyarrhythmic variant); supraventricular extrasystole;

    - Treatment and prevention: chronic stable angina (angina of tension); unstable angina; vasospastic angina (Prinzmetal angina, variant angina);

    - Treatment of arterial hypertension.

    Contraindications:

    • hypersensitivity to verapamil and other components of the drug;
    • cardiogenic shock;
    • acute myocardial infarction with complications (bradycardia, severe arterial hypotension, left ventricular failure);
    • atrioventricular blockade of II and III degree except for patients with an artificial pacemaker;
    • syndrome of weakness of the sinus node with the exception of patients with an artificial pacemaker;
    • lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
    • Atrial fibrillation / flutter with additional routes (Wolff-Parkinson-White-Laun-Ganong-Levin syndrome);
    • simultaneous application with colchicine;
    • age to 18 years.

    Carefully:

    Atrioventricular block of the 1st degree, chronic heart failure, arterial hypotension, bradycardia, hypertrophic obstructive cardiomyopathy, marked violations of the liver or kidney function, delay of neuromuscular transmission (myasthenia gravis gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy), elderly age.

    Pregnancy and lactation:

    Data on the clinical use of the drug Verapamil-LekT in pregnancy is not enough, so the drug should not be used during pregnancy. When using the drug Verapamil-LekT during lactation, it is necessary to stop breastfeeding.

    Dosing and Administration:

    Verapamil-lekT is taken orally during or after a meal, with a small amount of water.Tablets are taken whole, not rassasyvaya and not chewing, they can not be divided, divided into parts.

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

    The average dose for all recommended indications for use varies from 240 to 480 mg per day. The initial dose is 40-80 mg (it is possible to take verapamil in a dosage form of 40 mg).

    With prolonged use, the maximum daily dose of 480 mg should not be exceeded. In the maximum daily dose the drug must be taken only in a hospital. The duration of therapy is determined by the doctor.

    In patients with impaired hepatic function, excretion of verapamil from the body is slow, so it is advisable to start with a dose of 40 mg 2-3 times a day. The daily dose of the drug should not exceed 120 mg.

    Side effects:

    From the immune system: hypersensitivity reactions.

    From the central nervous system: headache, dizziness, fainting, anxiety, retardation, paresthesia, tremor, fatigue, asthenia, drowsiness, depression,extrapyramidal disorders (ataxia, "masklike" face, "shuffling" gait, stiffness of hands or feet, trembling of hands and fingers, difficulty swallowing).

    From the organ of hearing: tinnitus.

    From the cardiovascular system: atrioventricular block I, II, III degree, stopping the sinus node, peripheral edema, tachycardia, sinus bradycardia, heart failure, marked decrease in blood pressure, "tides" of blood to the skin of the face, a feeling of palpitations.

    From the digestive system: nausea, vomiting, constipation, intestinal obstruction, gingival hyperplasia, pain or discomfort in the abdomen.

    From the skin: angioedema, Stevens-Johnson syndrome, maculopapular rash, hives, purpura, pruritus, erythema multiforme, alopecia.

    From the musculoskeletal system: muscle weakness, myalgia, arthralgia.

    From the reproductive system and the mammary glands: erectile dysfunction, galactorrhea, gynecomastia.

    From the laboratory indicators: increased activity "hepatic" transaminases, hyperprolactinemia.

    Overdose:

    Symptoms: marked decrease in blood pressure, sinus bradycardia passing into AV blockade of a high degree, stopping the sinus node, hyperglycemia, stupor and metabolic acidosis. Reported lethal cases as a result of an overdose.

    Treatment: should be symptomatic and supportive therapy, including gastric lavage, reception of activated charcoal, parenteral administration of calcium preparations and beta-adrenomimetics. Verapamil is not excreted by hemodialysis.

    Interaction:

    Increases the area under the concentration-time curve (AUC) carbamazepine in patients with persistent partial epilepsy (risk of side effects such as diplopia, headache, ataxia and dizziness). Raises the AUC, the equilibrium concentration (Css) and the maximum concentration (Cmah) cyclosporine.

    Increases the concentration of theophylline (due to decreased clearance), ethanol (and lengthens its effect), the concentration of quinidine (the risk of a pronounced decrease in blood pressure, especially in patients with IHSS).

    It may increase the concentration of atorvastatin and lovastatin when used concomitantly.

    Increases significantly AUC and Cmah simvastatin.

    Raises the AUC and Cmalmotriptan, glibenclamide.

    Increases the concentration of sirolimus and tacrolimus.

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

    Raises the AUC and Cmmetoprolol and propranolol in patients with

    Increases the plasma concentration of colchicine (substrate for isoenzyme CYP3A and P glycoprotein).

    When ingestion significantly increases AUC and Cmah doxorubicin; IV injection of verapamil in patients with progressive neoplasms does not affect the pharmacokinetics of doxorubicin.

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

    Increases Cmof prazosin and terazosin and AUC terazosin.

    Significantly increases AUC and Cmbuspirone and midazolam.

    Inhibitors CYP3A4 (incl. erythromycin, HIV protease inhibitors), telithromycin increase plasma concentrations of verapamil. Grapefruit juice increases AUC and Cmah verapamil.

    Cimetidine either does not alter, or reduces the clearance of verapamil.

    Rifampicin can significantly reduce bioavailability (up to 92%), and AUC and Cmah verapamil.

    Rifampicin and sulfinpyrazone may reduce the antihypertensive effect of verapamil.

    Phenobarbital increases the clearance of verapamil 5 times.

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

    Drug preparations of St. John's wort reduce AUC verapamil and, respectively, CmOh.

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

    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 antihypertensives (angiotensin-converting enzyme inhibitors, vasodilators, diuretics, beta-blockers) increase the hypotensive effect.

    Dysopyramide and flecainide should not be administered within 48 hours before 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 drugs.

    Strengthens the action of peripheral muscle relaxants (may require a change in the dosage regimen).

    With simultaneous use with acetylsalicylic acid, there was a slightly greater increase in bleeding time than with acetylsalicylic acid alone.

    Patients receiving verapamil, treatment with HMG-CoA reductase inhibitors should begin with the lowest possible doses, which later on with the continuation of the drug therapy taking into account the concentration of cholesterol in the serum.

    Special instructions:

    The drug Verapamil-Lect can not be abruptly abolished, it is recommended to gradually reduce the dose until the drug is completely discontinued.

    In the treatment it is necessary to monitor the functions of the cardiovascular system, the respiratory system, the concentration of glucose and the content of electrolytes in the blood, the volume of circulating blood and diuresis.

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

    Care must be taken when driving vehicles and working with mechanisms that require increased concentration.

    Form release / dosage:

    Tablets, film-coated, 80 mg.

    Packaging:

    10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil printed and lacquered.

    For 50 or 100 tablets in cans of orange glass or cans of polymer type BP. 5 contour mesh packages or each jar along with the instruction for use is placed in a pack of cardboard box.

    Storage conditions:

    Store in a 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 expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001634
    Date of registration:09.04.2012
    Expiration Date:09.04.2017
    The owner of the registration certificate:Tyumen Chemical - Pharmaceutical Plant, OJSC Tyumen Chemical - Pharmaceutical Plant, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp29.01.2017
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