Active substanceMetoprololMetoprolol
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  • Dosage form: & nbsptabscesses
    Composition:

    1 tablet contains

    active substance: metoprolol tartrate - 50 mg;

    Excipients: microcrystalline cellulose, potato starch, povidone, sodium starch glycolate, talc, magnesium stearate.

    Description:TOfungal tablets white, flat on both sides, with bevelled edges, with a dividing line on one side and engraved: "M" above the line, "50" below the line.
    Pharmacotherapeutic group:Beta1-blocker selective
    ATX: & nbsp

    C.07.A.B   Selective beta-blockers

    C.07.A.B.02   Metoprolol

    Pharmacodynamics:

    Metoprolol acts primarily on beta1-adrenoceptors of the heart. Does not have a membrane-stabilizing action and does not have an internal sympathomimetic activity.

    Has anti-angiogenic, antihypertensive and antiarrhythmic effect, reduces the automatism of the sinus node, reduces the heart rate (heart rate), slows the atrioventricular conduction, reduces myocardial contractility and excitability, cardiac output, myocardial oxygen demand. Suppresses the stimulating effect of catecholamines on the heart for physical and psychoemotional stress.

    The antihypertensive effect develops gradually and stabilizes towards the end of the second week of course treatment.

    With angina pectoris Metoprolol reduces the frequency and severity of seizures.

    Normalizes the heart rhythm with supraventricular tachycardia and atrial fibrillation. Metopropro reduces mortality and the possibility of recurrence in patients with myocardial infarction due to the limitation of the infarction zone and the risk of developing fatal arrhythmias.

    When used in moderate therapeutic doses, it has a less pronounced effect on the smooth musculature of the bronchi and peripheral arteries than non-selective beta-blockers.

    Pharmacokinetics:

    Absorption when taken orally is complete (95%). The solubility in fats is moderate.It is subjected to intensive presystemic metabolism, bioavailability is 50% at the first intake and increases to 70% with repeated application. Connection with blood plasma proteins - 10%. The time to reach the maximum concentration of metoprolol in the blood plasma is 1.5-2 hours after taking the tablets. During the course of treatment, bioavailability increases. Food intake increases bioavailability by 20-40%.

    Rapidly distributed in tissues, penetrates the blood-brain barrier, the placental barrier. It penetrates into the mother's milk (the concentration is higher than in the blood plasma). It is not removed during hemodialysis.

    Metabolized in the liver, two metabolites have beta-adrenoblocking activity. The half-life of metoprolol is 3.5 to 7 hours with oral administration. A significant accumulation of metabolites is observed in patients with a creatinine clearance of 5 ml / min, while the beta-adrenergic blocking activity of the drug does not increase.

    In the metabolism of the drug, the enzyme system P450 CYP2D6.

    Indications:

    - Arterial hypertension;

    - andshectic heart disease;

    - Mr.heart rate rhythm;

    - atthoracic prophylaxis after a previous myocardial infarction;

    - Pthe prevention of migraine attacks;

    - ghyperkinetic cardiac syndrome.

    Contraindications:

    - Hypersensitivity to the drug and other beta-blockers;

    - atrioventricular blockade of II and III degree;

    - toardiogenic shock;

    - fromInoatrial blockade;

    - atAcute bradycardia;

    - fromthe weakness of the sinus node;

    - fromprinzmetal prenas;

    - tsevere peripheral circulatory disorders;

    - aboutMyocardial infarction (heart rate less than 45 beats per minute, interval PQ more than 0.24 seconds, systolic blood pressure less than 100 mm Hg. item);

    - fromCardiac insufficiency in the stage of decompensation;

    - xheart failure IIB-III stage;

    - aHypotension (in case of use in secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg);

    - metabolic acidosis;

    - aboutsimultaneous reception with MAO inhibitors;

    - PThe period of lactation;

    - atozrast to 18 years (efficiency and safety not established).

    Carefully:

    Diabetes mellitus, obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome), myasthenia gravis, pheochromocytoma, atrioventricular blockade of I degree, thyrotoxicosis, depression (incl.in history), psoriasis, pregnancy, elderly age, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), chronic renal failure (CRF), severe liver and kidney dysfunction (with the appointment of metoprolol in this category of patients need constant monitoring for the dynamics of the functional state of the liver and / or kidneys).

    Pregnancy and lactation:

    Before using the drug, it is necessary to inform the doctor about the existing or possible pregnancy.

    During pregnancy (especially in the first 3 months) Metoprolol should be used only on strict indications after careful correlation of benefit and risk, since up to the present time there is insufficient experience of its use in pregnancy.

    If pregnant women took Metoprolol, then in connection with the possibility of the appearance of a newborn bradycardia, arterial hypotension and hyperglycemia, treatment is stopped for 48-72 hours before the onset of labor. If this is not possible, the newborn should be under especially careful supervision within 48 -72 hours after childbirth.

    Metoprolol penetrates into breast milk. Application of the drug Metoprolol during the period of feeding it is contraindicated.

    Dosing and Administration:

    Inside, with food or immediately after a meal. The tablet is swallowed without chewing, and washed down with a small amount of water.

    The dose of the drug should be individually tailored to the patient's condition.

    Treatment begins with a dose of 50 mg in 1-2 divided doses. If the therapeutic effect is insufficiently expressed, the daily dose is gradually increased to 200 mg. The maximum daily dose is 200 mg.

    Arterial hypertension

    With arterial hypertension, the average dose is 10-150 mg / day in 1-2 divided doses, if necessary 200 mg / day.

    Angina pectoris

    50 mg 2-3 times a day.

    Heart rhythm disturbances

    50 mg 2-3 times a day. If necessary, the dose can be increased to 200 mg / day.

    Secondary prevention of myocardial infarction

    200 mg / day in several doses.

    Prevention of migraine

    100-200 mg / day 2-4 hours.

    With hyperkinetic cardiac syndrome

    50 mg 1-2 times a day. When the therapeutic effect is achieved, the dose is reduced (under the supervision of the doctor).

    Elderly patients are advised to begin treatment with 50 mg / day.

    Side effects:

    From the nervous system: weakness, fatigue, dizziness, headache, slowing of the speed of mental and motor reactions, muscle cramps, a feeling of cold, paresthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome), tremors, anxiety, decreased attention, drowsiness, depression, insomnia , "nightmarish" dreams, confusion or short-term memory loss, hallucinations, asthenic syndrome, muscle weakness.

    From the sense organs: decreased secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis, decreased vision, tinnitus, hearing loss, rhinitis.

    From the side of the cardiovascular system: a marked decrease in blood pressure, a decrease in myocardial contractility, heart rhythm disturbances, aggravation of pre-existing atrioventricular conduction disorders, bradycardia, orthostatic hypotension (sometimes with loss of consciousness), symptoms of heart failure with peripheral edema (stop and / or lower leg), dyspnea, cardialgia.

    From the digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation, or diarrhea.Individual cases of violations of liver function (dark urine, icteric sclera or skin, cholestasis), changes in taste have been noted.

    From the skin: rashes on the skin (exacerbation of psoriasis), psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

    From the respiratory system: stuffy nose, shortness of breath. In predisposed patients - bronchospasm.

    From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemic conditions in diabetic patients, hypothyroid status.

    Allergic reactions: urticaria, skin itching, rash.

    Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of "liver" enzymes, hyperbilirubinemia.

    Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

    Other: pain in the back or joints, weight gain, decreased libido and / or potency, with a sharp cessation of treatment - withdrawal syndrome (increased angina attacks, increased blood pressure).
    Overdose:

    Symptoms: the clinical picture depends on the degree of intoxication and is manifested, in the main, by violations from the cardiovascular and central nervous system. Overdose can lead to a pronounced decrease HELL, bradycardia (up to cardiac arrest), heart failure and cardiogenic shock. In severe cases, difficulty in breathing, bronchospasm, vomiting, impaired consciousness, generalized seizures can be observed.

    Treatment: in cases of overdose or with a threatening drop in heart rate and / or blood pressure, metoprolol treatment is discontinued. In the context of the intensive care unit in addition to measures aimed at elimination from the body of metoprolol, careful monitoring of vital parameters and correcting them if necessary.

    If necessary, designate:

    - atropine;

    - glucagon;

    - sympathomimetics, depending on body weight and the effect obtained (dopamine, dobutamine or norepinephrine);

    - with refractory therapy of bradycardia, you can temporarily transfer the patient to electrocardiostimulation;

    - with bronchospasm appoint beta2-adrenomimetiki in the form of an aerosol (with insufficient effect also in / in) or aminophylline in / in.

    When generalized convulsive seizures are prescribed diazepam (in / in, slowly).

    Hemodialysis is ineffective.

    Interaction:

    With the simultaneous administration of metoprolol and

    - Insulin or oral hypoglycemic agents may increase or prolong their effect. In this case, the symptoms of hypoglycemia (especially, tachycardia and tremor) can be masked;

    - tricyclic antidepressants, barbiturates, phenothiazines, nitroglycerin may increase the hypotensive effect;

    - blockers of "slow" calcium channels (type nifedipine), in addition to increasing the hypotensive effect, heart failure may develop;

    - blockers of "slow" calcium channels (verapamil and diltiazem) Amkodarona or other antiarrhythmic agents may develop hypotension, bradycardia (development or exacerbation of course), heart rhythm disturbance, AV blockade, heart failure, cardiac arrest;

    - cardiac glycosides, reserpine, alpha-methyldopa, guanfacine and clonidine coins, there is a dangerous decrease in heart rate;

    - norepinephrine, epinephrine or other sympathomimetic agents (eg, contained in eye drops or antitussives) may increase blood pressure;

    - indomethacin and rifampicin may reduce the antihypertensive effect of metoprolol;

    - cimetidine may increase the effects of metoprolol;

    - Lidocaine reduces the clearance of the latter;

    - narcotic drugs intensifies the hypotensive effect. In this case, the additive, negative inotropic effect of both agents is manifested;

    - competitive muscle relaxants (eg, suxamethonium, tubocurarine), neuromuscular blockade may occur;

    - allergens used for immunotherapy, or allergen extracts for skin tests increases the risk of severe systemic allergic reactions or anaphylaxis;

    - iodine-containing radiopaque substances for iv administration increases the risk of anaphylactic reactions;

    - phenytoin with IV injection, means for inhalation anesthesia (hydrocarbon derivatives), the cardiopepressive effect increases and the probability of a decrease in blood pressure increases;

    - Non-steroidal anti-inflammatory drugs (NSAIDs) (sodium retention and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids (GCS) and estrogens (sodium retention) weakening of the hypotensive effect;

    - Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to excessive blood pressure lowering;

    - Three - and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics, the central nervous system is becoming more oppressive;

    - Unhydrogenated ergot alkaloids increases the risk of peripheral circulatory disorders;

    Metoprolol reduces the clearance of xanthines (except for diphylline) and increases their concentration in the blood plasma, especially in patients with initially higherwtheophylline clearance under the influence of smoking.

    Lengthens the effect of nondepolarizing muscle relaxants and anticoagulant effect of coumarins.

    It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive effect, a break in treatment between the intake of MAO inhibitors and Metoprolol should be at least 14 days.

    Special instructions:

    With arterial hypertension, the effect occurs after 2-5 days, a stable condition occurs after 1-2 months.

    With angina pectoris, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats / min.

    In smokers, the effectiveness of beta-blockers is lower.

    Control of patients taking beta-blockers includes monitoring heart rate and blood pressure (at the beginning of the procedure - every day, then every 2 to 4 months), blood glucose in diabetic patients (once every 4-5 months).

    If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic drugs administered orally should be selected individually.

    It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at a heart rate of less than 50 beats per minute.

    In elderly patients, it is recommended that kidney function is monitored (once every 4-5 months).

    May enhance the symptoms of peripheral arterial circulation.

    The withdrawal of the drug is carried out gradually, reduce the dose for 10 days, under the supervision of a doctor. With a sharp cessation of treatment, there may be a "cancellation" syndrome (increased angina attacks, increased blood pressure). Particular attention should be paid to patients with angina when the drug is withdrawn.

    Patients using contact lenses should take into account that against the background of drug treatment Metoprolol it is possible to reduce the production of tear fluid.

    Metoprolol may mask certain clinical manifestations of hyperthyroidism (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

    With diabetes mellitus Metoprolol can mask tachycardia caused by hypoglycemia. In contrast to nonselective beta-blockers, it does not substantially increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to an optimal level.

    In elderly patients it is recommended to regularly monitor liver function.

    Correction of the dosing regimen is required only if elderly patients develop an increasing bradycardia (less than 50 beats per minute), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction; sometimes you need to stop treatment.

    Special monitoring should be carried out on the condition of patients with depressive disorders receiving Metoprolol; In the case of development of depression caused by the use of beta-blockers, it is recommended to stop therapy.

    A few days before the anesthesia with chloroform or ether should stop taking the drug. If it is necessary to perform a surgical procedure, it is necessary to warn the anesthesia about the therapy (choice of a means for general anesthesia with minimal negative inotropic action), the drug cancellation is not recommended.

    With combined therapy with clonidine, the latter should be discontinued a few days after metoprolol withdrawal in order to avoid a hypertensive crisis.

    At a dose above 200 mg / day, cardioselectivity decreases.

    It is possible to increase the severity of the reactions of hypersensitivity (against a background of a burdened allergic anamnesis) and the absence of the effect of the administration of usual doses of epinephrine.

    In case of necessity of carrying out of surgical operation, including stomatologic, it is necessary to inform the doctor about application of a preparation Metoprolol.

    During treatment with metoprolol, appropriate clothing should be worn, since the drug may cause skin allergy to sunlight.

    If it is necessary to prescribe to patients with bronchial asthma, as a concomitant therapy, beta2-adrenostimulators, with pheochromocytoma - alpha-adrenoblockers.

    Reciprocal activation of the vagus nerve can be eliminated in \ in the administration of atropine (1-2 mg).

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

    During the treatment period, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, exclude the use of ethanol.

    Form release / dosage:Tablets, 50 mg.
    Packaging:

    For 15 or 20 tablets in a blister of PVC-aluminum foil.

    2 blisters together with instructions for use are placed in a pack of cardboard.
    Storage conditions:

    In a dry, dark place at a temperature of 15 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 of the year.

    Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N016223 / 01
    Date of registration:05.04.2010 / 15.07.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:Meda Pharma GmbH & Co. KGMeda Pharma GmbH & Co. KG Germany
    Manufacturer: & nbsp
    Representation: & nbspMEDA PHARMA LLCMEDA PHARMA LLC
    Information update date: & nbsp10.05.2018
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