Active substanceCarvedilolCarvedilol
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  • Dosage form: & nbsppills
    Composition:

    Each tablet of 12.5 mg contains active substance: carvedilol 12.5 mg.

    Excipients: lactose monohydrate (sugar milk) 64.0 mg, microcrystalline cellulose 15.0 mg, corn starch 2.0 mg, crospovidone 2.0 mg, povidone (polyvinylpyrrolidone) 3.5 mg, magnesium stearate 1.0 mg.

    Each 25 mg tablet contains active substance: carvedilol 25.0 mg.

    Excipients: lactose monohydrate (sugar milk) 128.0 mg, microcrystalline cellulose 30.0 mg, corn starch 4.0 mg, crospovidone 4.0 mg, povidone (polyvinylpyrrolidone) 7.0 mg, magnesium stearate 2.0 mg.

    Description:Tablets are white or white with a creamy shade of color, flat-cylindrical shape, with a facet on both sides and risk from one side.
    Pharmacotherapeutic group:Alpha- and beta-blocker
    ATX: & nbsp

    C.07.A.G.02   Carvedilol

    Pharmacodynamics:

    It blocks alpha1, beta1 and beta2-adrenergic receptors. Has vasodilating, antianginal and antiarrhythmic action. Carvedilol is a racemic mixture R(+) and S(-) stereoisomers, each of which has the same alpha-adrenoblocking and antioxidant properties.Beta-adrenoblokiruyuschee action carvedilol is non-selective and is due to levorotatory S(-) stereoisomer.

    The drug does not have its own sympathomimetic activity, it has membranes of stabilizing properties and properties.

    The vasodilating effect is mainly due to the blockade of alpha 1-adrenergic receptors. Due to vasodilation, the overall peripheral vascular resistance (OPSS) decreases.

    The combination of vasodilation and blockade of beta-adrenoreceptors leads to the following effects: in patients with arterial hypertension, a decrease in blood pressure (BP) is not accompanied by an increase in OPSS, peripheral blood flow (in contrast to beta-blockers) does not decrease. The heart rate (heart rate) decreases slightly. In patients with ischemic heart disease, it has an antianginal effect. Reduces pre- and postnagruzku on the heart. It has no pronounced effect on the lipid metabolism and the content of potassium, sodium and magnesium ions in the blood plasma.

    In patients with impaired left ventricular function and / or heart failure, the hemodynamic parameters favorably affect and improve the ejection fraction and the size of the left ventricle.It has an antioxidant effect, eliminating free oxygen radicals.

    Carvedilol lowers the mortality rate and reduces the frequency of hospitalizations, reduces symptoms and improves left ventricular function in patients with chronic heart failure of ischemic and non-ischemic origin. The effects of carvedilol are dose-dependent.

    Pharmacokinetics:

    Carvedilol is rapidly absorbed from the gastrointestinal tract. Has high lipophilicity. The maximum concentration in the blood is reached after 1-1,5 hours.

    It binds to blood plasma proteins by 95-99%. Bioavailability of the drug is 24-28%. The intake of food does not affect the bioavailability.

    Metabolized in the liver with the formation of a number of active metabolites - 60-75% The absorbed drug is metabolized at the first "passage" through the liver. Metabolites have antioxidant and adrenoblocking action.

    The half-life is 6-10 hours. The excretion occurs mainly with bile and feces.

    When the renal function is impaired, the pharmacokinetic parameters of carvedilol do not change significantly.

    In patients with impaired liver function, the systemic bioavailability of carvedilol is increased bydecrease in metabolism at the first "passage" through the liver. With serious violations of liver function carvedilol is contraindicated.

    Carvedilol penetrates the placental barrier.

    Indications:

    - Arterial hypertension (in monotherapy or in combination with other antihypertensive agents, for example, blockers of "slow" calcium channels);

    - ischemic heart disease (including in patients with unstable angina and painless myocardial ischemia);

    - chronic heart failure (as part of combination therapy).

    Contraindications:

    Hypersensitivity to carvedilol or other components of the drug, acute and chronic heart failure in the stage of decompensation, requiring intravenous injection of inotropes; clinically significant impairment of liver function; atrioventricular block II-III degree (except for patients with an artificial pacemaker, severe bradycardia (heart rate less than 50 beats per minute), sinus node weakness syndrome (including sinoauric blockade), severe arterial hypotension (systolic blood pressure (BP) less than 85 mm Hg.), cardiogenic shock, bronchospasm and bronchial asthma (history), age 18 years (efficacy and safety not established), lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the preparation contains lactose).

    Carefully:

    Chronic obstructive pulmonary disease, prinzmetal angina, thyrotoxicosis, peripheral vascular occlusive diseases, pheochromocytoma, psoriasis, renal failure, atrioventricular blockade of the 1st degree, extensive surgical interventions and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.

    Pregnancy and lactation:

    Beta-adrenoblockers reduce placental blood flow, which can lead to intra-uterine fetal death and premature birth. In addition, the fetus and newborns can develop unwanted reactions (in particular, hypoglycemia and bradycardia, complications from the heart and lungs).

    There is no sufficient experience of carvedilol in pregnant women. Carvedilol is contraindicated for use in pregnancy, except when the possible benefits of its use in the mother exceed the potential risk to the fetus.

    Data on the penetration of carvedilol into breast milk are not available, so if Carvedilol is needed during lactation, then breastfeeding should be discontinued.

    Dosing and Administration:

    Inside, squeezed with enough liquid.

    Arterial hypertension

    The initial dose is 12.5 mg once a day for the first two days of treatment. Then, 25 mg 1 once a day. It is possible to gradually increase the dose at intervals of not less than 2 weeks. If the antihypertensive effect is inadequate after 2 weeks of therapy, the dose can be increased 2-fold. The maximum recommended daily dose of the drug is 50 mg 1 time per day (possibly divided into 2 receptions).

    Ischemic heart disease, angina pectoris

    The initial dose is 12.5 mg twice a day in the first two days of treatment. Then, 25 mg 2 times a day. If the antianginal effect is inadequate after 2 weeks of therapy, the dose may be increased 2-fold. The maximum recommended daily dose of the drug is 100 mg per day, divided into 2 receptions.

    Chronic heart failure

    The dose is selected individually, under the careful supervision of the doctor.The recommended initial dose is 3.125 mg (the drug may be used carvedilol in a dose of 6.25 mg with a risk) 2 times a day for 2 weeks. With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg (1/2 tablets of 12.5 mg) twice a day, then to 12.5 mg twice a day, then to 25 mg 2 times per day. The dose should be increased to the maximum, which is well tolerated by the patient. With a body weight of less than 85 kg - the maximum dose is 25 mg 2 times a day, with a mass of more than 85 kg - 50 mg 2 times a day. If treatment is interrupted for more than 2 weeks, then its resumption begins with a dose of 3.125 mg (possibly the drug carvedilol in a dose of 6.25 mg with a risk) 2 times a day, followed by an increase in the dose.

    In patients with moderate to severe degree of renal failure, dose adjustment of Carvedilol is not required.

    Carvedilol is contraindicated in patients with clinical manifestations of liver dysfunction.

    Side effects:

    From the central nervous system: very often - dizziness, headache (usually not strong and arising at the beginning of treatment), weakness, fatigue, depression, paresthesia, sleep disorders, asthenia, mood lability.

    From the side of the cardiovascular system: often bradycardia, orthostatic hypotension, atrioventricular blockade of II-III degree, progression of heart failure (during the period of increasing doses), edema (including generalized, edema of the lower extremities, hypervolemia, fluid retention), angina, marked decrease in blood pressure, syncopal conditions (including presyncopal), rarely - violations of peripheral circulation (cold extremities, exacerbation of the syndrome of "intermittent" lameness and Raynaud's syndrome).

    From the side of the digestive tract: dryness of the oral mucosa, nausea, diarrhea or constipation, vomiting, abdominal pain.

    Laboratory indicators: increased activity of "hepatic" transaminases - alanine aminotransferase (ALT), aspartate aminotransferase (ACT) and gamma-glutamyltransferase, thrombocytopenia and leukopenia.

    On the part of the hematopoiesis system: rarely - thrombocytopenia, leukopenia.

    From the side of metabolism: weight gain, hypercholesterolemia; in patients with existing diabetes - hyperglycemia or hypoglycemia, violations of glycemic control.

    From the skin: skin reactions (skin rash, dermatitis, urticaria and skin itching), isolated cases of allergic reactions.

    From the respiratory system: often - shortness of breath and bronchospasm (in predisposed patients), rarely - nasal congestion.

    Other: visual impairment, decreased tear and eye irritation, flu-like syndrome, sneezing, rarely - urination disorder, renal failure and renal dysfunction in patients with diffuse vasculitis and / or renal dysfunction; very rarely - exacerbation of psoriasis, pain in the limbs, infrequent - a decrease in potency; rare cases of urinary incontinence in women; the presence of beta-adrenergic blocking properties does not exclude the possibility of manifestation of latent diabetes mellitus, decompensation of already existing diabetes mellitus or oppression of the contrinular system.

    Overdose:

    Symptoms: marked decrease in blood pressure, bradycardia, heart failure, cardiogenic shock, cardiac arrest; possible respiratory disorders, bronchospasm, vomiting, confusion and generalized convulsions.

    Treatment: it is necessary to monitor and correct vital signs, if necessary - in the intensive care unit.

    You can use the following activities:

    a) put the patient on his back (with raised legs);

    b) with pronounced bradycardia - atropine 0.5-2 mg intravenously;

    c) for the maintenance of cardiovascular activity - glucagon 1-10 mg intravenously in veins, then 2-5 mg per hour in the form of a long infusion;

    d) sympathomimetics (dobutamine, epinephrine (epinephrine)) in different doses, depending on body weight and response to ongoing therapy.

    If the clinical picture of an overdose is dominated by hypotension, norepinephrine (noradrenaline); he is appointed in conditions of continuous monitoring of blood circulation parameters.

    In the case of bradycardia resistant to treatment, the use of an artificial pacemaker is indicated.

    When bronhospazme enter beta-adrenomimetiki in the form of an aerosol (if ineffectiveness - intravenously) or aminophylline intravenously.

    When convulsions are intravenously slowly injected diazepam.

    Since a severe overdose with symptoms of shock may prolong the half-life of carvedilol and remove the drug from the depot,It is necessary to continue supporting therapy for a long time.

    Interaction:

    Carvedilol can potentiate the effect of other concurrently taken antihypertensive drugs or drugs that have an antihypertensive effect (nitrates).

    With the combined use of carvedilol and diltiazem, amiodarone and other antiarrhythmic agents impairment of conduction of cardiac impulses and violations of hemodynamic parameters may develop.

    With the simultaneous administration of carvedilol and digoxin the concentration of the latter increases and the time of atrioventricular conduction may increase.

    Carvedilol may potentiate the action insulin and hypoglycemic agents for oral administration, while the symptoms of hypoglycemia (especially tachycardia) can be masked, so in patients with diabetes it is recommended that the blood glucose concentration be monitored regularly.

    Inhibitors of microsomal oxidation (cimetidine) strengthen, and inducers (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilol.

    Drugs that reduce the content of catecholamines (reserpine, monoamine oxidase inhibitors), increase the risk of developing arterial hypotension and severe bradycardia.

    With simultaneous application cyclosporine the concentration of the latter increases (a correction of the daily dose of cyclosporine is recommended).

    Simultaneous appointment clonidine can potentiate antihypertensive and heart rhythm-reducing effects of carvedilol. If you plan to stop combination therapy with a drug with beta-adrenergic blocking properties and clonidine, you should first cancel the beta-blocker, and in a few days you can cancel clonidine, gradually reducing its dose.

    General anesthetics increase the negative inotropic and hypotensive effect of carvedilol.

    Special instructions:

    Therapy should be carried out for a long time and should not abruptly cease, especially in patients with coronary heart disease, since this can lead to a worsening of the course of the underlying disease. If necessary, the dose reduction should be gradual, within 1-2 weeks.

    In patients with chronic heart failure during the selection of the dose of Carvedilol, there may be an increase in symptoms of chronic heart failure or fluid retention.If such symptoms occur, it is necessary to increase the dose of diuretics and not increase the dose of Carvedilol until the hemodynamic parameters stabilize. Sometimes there is a need to reduce the dose of Carvedilol or, in rare cases, temporarily cancel the drug. Such cases do not prevent further correct selection of Carvedilol dose.

    Carvedilol is used with caution in combination with cardiac glycosides (possibly excessive retardation of atrioventricular conduction).

    Carvedilol can cause bradycardia, with a heart rate lower than 55 beats per minute. dose of the drug Carvedilol should be reduced.

    With caution appoint Carvedilol patients with diabetes, because it can mask or relieve the symptoms of hypoglycemia (especially tachycardia). In patients with chronic heart failure and diabetes mellitus, the drug Carvedilol can be accompanied by violations of glycemic control. Caution is needed when prescribing Carvedilol to patients with peripheral vascular disease (including Reyno's syndrome), since beta-blockers may increase the symptoms of arterial insufficiency.

    Like other beta-blockers Carvedilol can reduce the severity of symptoms of thyrotoxicosis.

    Care should be taken when prescribing Carvedilol to patients with anamnestic indications of severe hypersensitivity reactions or a course of desensitization, since beta-blockers can increase sensitivity to allergens and the severity of anaphylactic reactions.

    At the beginning of therapy with Carvedilol or with an increase in the dose of the drug in patients, especially the elderly, there may be an excessive decrease in blood pressure, especially during the transition from the "lying" position to the "standing" position. A dose adjustment is necessary.

    Regular ECG monitoring and BP indices are recommended with simultaneous appointment of Carvedilol and blockers of "slow" calcium channels such as verapamil and diltiazem, and also with antiarrhythmics.

    Non-selective beta-blockers can provoke the appearance of pain in patients with Prinzmetal angina, although alpha-adrenoblocking properties can prevent similar symptoms, prescribe Carvedilol in such cases should be done with caution.

    When Karvedilol was prescribed to patients with chronic heart failure and arterial hypotension (systolic blood pressure less than 100 mm Hg), coronary heart disease and diffuse vessel changes and / or kidney failure, reversible impairment of renal function was noted. The dose of Carvedilol is selected depending on the functional state of the kidneys.

    Patients with chronic obstructive pulmonary disease (including bronchospastic syndrome) who do not receive oral or inhaled beta2-adrenostimulants, carvedilol appoint only if the benefits from its use exceed the potential risk. If there is an initial predisposition to bronchospastic syndrome with carvedilol intake, as a result of increased respiratory tract resistance, dyspnea may develop. At the beginning of therapy and with an increase in the dose of Carvedilol, these patients should be carefully observed, reducing the dose of the drug when the initial signs of bronchospasm appear.

    In the case of surgical intervention with the use of general anesthesia, an anesthesiologist should be warned about the previous therapy with Carvedilol.

    During the treatment period, avoid drinking alcohol.

    Patients with pheochromocytoma before starting therapy for any beta-blocker should be prescribed alpha-blocker.

    Patients wearing contact lenses should note that the drug can cause a decrease in tearing.

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

    Given the potential side effects of Carvedilol, the drug should be given with caution to patients whose work requires a rapid psychomotor reaction, especially at the beginning of therapy.

    Form release / dosage:

    Tablets of 12.5 mg and 25 mg.

    Packaging:

    For 10, 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    By 10, 20, 30, 40, 50 or 100 tablets in cans of polymeric for medicines.

    One jar or 1, 2, 3, 4, 5 or 10 contour squares, together with instructions for use, are placed in a cardboard package (pack) of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 of the year.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001733/10
    Date of registration:05.03.2010 / 04.03.2013
    Expiration Date:Unlimited
    The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspOZONE LLC OZONE LLC Russia
    Information update date: & nbsp10.12.2017
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