Metoperolol retard Akrichin instructions for use. Metoprolol Akrichin Instructions for use

Instructions for use

Active substances

Form release

Pills

Structure

Metoprolol Succinate 23.83 mg, which corresponds to the content of metoprolol Tartrate 25 mg; Auxiliary substances: Hyprocell slide - 155.96 mg, Ludipress LCER (monohydrate lactose - 94.7-98.3%, Pisidone - 3-4%) - 117.21 mg, silicon colloidal dioxide - 1.5 mg , magnesium stearate - 1.5 mg. The composition of the shell: the finished mixture of "Oddray II" of orange color (polyvinyl alcohol - 6 mg, talc - 2.22 mg, macrogol - 3.03 mg, titanium dioxide - 3.36 mg, red oxide dye - 0.009 mg, Iron dye oxide yellow - 0.378 mg, iron dye black - 0.003 mg) - 15 mg.

Pharmacological effect

Cardooselective beta1 adrenoblocator. It does not have a membrane-stabilizing effect and does not have internal sympathomimetic activity. It has antihypertensive, anti-infanal and antiarrhythmic effect.; Blocking in low doses of β1-adrenoreceptors of the heart, reduces the formation of CATCHOLAMINS, the formation of CAMF from ATF, reduces intracellular current of calcium ions, has a negative chrono-, dromo-, butmol, and inotropic action (CHS cuts, inhibits conductivity and excitability, reduces myocardial reductions). OPS at the beginning of the use of beta adrenobloclars (in the first 24 hours after oral reception) Increases (as a result of reciprocal increase in the activity of the ADRENORTERSPORTORS and eliminating the stimulation of β2-adrenoreceptors), after 1-3 days it returns to the original, and during long-term purpose decreases .; antihypertensive effect is due to a reduction in the minute volume of blood flow and the synthesis of Renin, the oppression of the activity of Rase (has More important in patients with initial hypersection of renin) and CNS, the restoration of the sensitivity of the borerotors of the arc of the aorta (there is no amplification of their activity in response to the decrease in blood pressure) and as a result, a decrease in peripheral sympathetic influences. Reduces increased blood pressure at rest, with physical stress and stress. Antihypertensive effect lasts more than 24 hours; the anti-infanal effect is determined by the decrease in the need of myocardial in oxygen as a result of the decrease in heart rate (lengthening of diastole and improved myocardial perfusion) and a reduction, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of seizures of angina and increases portability exercise. Due to the increase in the final diastolic pressure in the left ventricle and an increase in the tension of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure.; Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, high activity of sympathetic. nervous system, enlarged CAMF content, arterial hypertension), reducing the speed of spontaneous excitation of sine and ectopic rhythm drivers and a deduction of AV-conduct (mainly in the antegrade and to a lesser extent in retrograde directions through AV-node) and for additional ways.; for supritericular tachycardia, atrial flications, sinus tachycardia with functional diseases Hearts and thyrotoxicosis regenerates heart disease or can even lead to restoration of sinus rhythm.; warns the development of migraine.; unlike non-selective beta-adrenoblockers in the appointment in the average therapeutic doses Less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles peripheral arteries, bronchi and uterus) and for carbohydrate exchange; The severity of atherogenic action does not differ from the action of propranolol. With many years of reception, it reduces the concentration of cholesterol in the blood. When applied in large doses (more than 100 mg / day), it has a blocking effect on both subtype of β-adrenoreceptors.

Pharmacokinetics

Suction; absorption when taking inside full (95%). Solubility in fats moderate. It is subjected to intense preyed metabolism, bio-sauna - 50% at the first reception and increases to 70% during re-use. The time of reaching Cmax in the blood plasma is 6-12 hours after receiving the drug. During the course treatment, bioavailability increases. Eating increases bioavailability by 20-40%.; Distribution; binding to plasma proteins - 10%. Quickly distributed in the tissues, penetrates the BC, a placental barrier. Penetrates into breast milk .; metabolism; metabolized in the liver, 2 metabolites have beta-adrenoblocating activity. In the metabolism of the drug, the CYP2D6 isoenzyme takes part.; Elimination; T1 / 2 - from 3.5 to 7 hours when taking inside. It is not removed during hemodialysis.; Pharmacokinetics in special clinical cases; a significant accumulation of metabolites is observed in patients with QC 5 ml / min, while the beta-adrenoblocking activity of the drug does not increase .; bioavailability increases in the cirrhosis of the liver, while its overall clearance is reduced.

Indications

Arterial hypertension; - chronic heart failure of the II-IV functional class according to the NYHA classification in the compensation stage (as part of complex therapy); - IBS: Prevention of attacks stable angina, reduced mortality and frequency of myocardial repeated heart attack after the acute phase of myocardial infarction; - Disturbances of the heart rhythm, including supertoday tachycardia, reducing the frequency of ventricles during atrial fibrillation and ventricular extrasystoles; - functional violations of cardiac activity, accompanied by tachycardia; - Prevention of migraine attacks.

Contraindications

Cardiogenic shock; - AV blockade of II-III heat; - synoyatrial blockade; - SCC; - pronounced bradycardia (heart rate less than 50 hp / min); - acute heart failure or chronic heart failure in the decompensation stage; - arterial hypotension (systolic blood pressure less than 100 mm Hg); - acute infarction myocardium (heart rate less than 45 UD / min, the interval PQ is more than 0.24 ° C, systolic blood pressure is less than 100 mm Hg); - severe bronchial asthma; - severe disorders of peripheral blood circulation; - simultaneous reception of Mao inhibitors or simultaneous V / in the introduction of verapamil; - Feochromocytoma (without simultaneous reception of alpha adrenoblockers); - age up to 18 years old (efficiency and security are not established); - lactation period; - lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome; - increased sensitivity to metoprolol and other beta adrenoblockers.; With caution, the drug should be prescribed when sugar diabetes, AV blockade I heat, angina printela, metabolic acidosis, bronchial asthma, COPD, renal and / or liver failure Heavy degree, Miasthenia, Feochromocytoma (with simultaneous adre-adrenoblochetors), thyrotoxicosis, depression (incl. In history), psoriasis, peripheral circulatory disorders (interspersed chromoty, Reino syndrome), pregnancy, and elderly patients.

Application in pregnancy and breastfeeding

During pregnancy, the drug Metoprolol Restard-Akrichin should be applied only by strict indications when the expected benefit for the mother exceeds the potential risk to the fetus / child (due to possible development Newborn bradycardia, reduction of blood pressure, hypoglycemia and respiratory paralysis). At the same time, careful observation is carried out especially for the development of the fetus. Treatment is stopped in 48-72 hours before the occurrence of childbirth. If this is not possible, the newborn must be under a particularly thorough observation within 48-72 hours after childbirth.; The use of the drug metoprolol Retard-acryoin is contraindicated during lactation. If necessary, the use of the drug during the lactation breast-feeding Need to stop.

Method of application and dose

The drug metoprolol retard-acryer is taken inside 1 time / day. Tablets are recommended to take in the morning, not chewing, drinking water. Metoprolol Readend-Akrichin can be taken regardless of meals.; In order to prevent bradycardia, the dose is selected individually and increase gradually.; In arterial hypertension and angina, the initial dose - 50 mg 1 time / day, with insufficient therapeutic effect The daily dose can be increased to 100-200 mg / day. With arterial hypertension in the ineffectiveness of the drug at a dose of 100-200 mg / day, another hypotensive agent can be added.; With chronic heart failure of the II functional class according to NYHA classification (without exacerbation of the last 6 weeks and unchanged in comprehensive therapy for the last 2 weeks) Recommended Initial dose - 25 mg 1 time / day. After 2 weeks, the daily dose can be increased to 50 mg, then in 2 weeks - up to 100 mg, after another 2 weeks - up to 200 mg.; With chronic heart failure of the III-IV functional class on the NYHA classification, the recommended initial dose - the first 2 weeks 12.5 mg 1 time / day. It is possible to use metoprolol in another dosage formFor example, 25 mg tablets with risk. During the period of increasing the dose, the patient must be under observation, because In some patients, symptoms of heart failure may worsen.; After 1-2 weeks, the dose can be increased to 25 mg 1 time / day. Then after 2 weeks, the dose can be increased to 50 mg 1 time / day. Patients who are well transferred to the drug can double dose every 2 weeks before reaching a maximum dose of 200 mg 1 time / day.; When secondary prophylaxis Myocardial infarction and heart rate disorders The initial dose is 100 mg 1 time / day; with functional violations of cardiac activity, accompanied by tachycardia, are prescribed 50 mg / day, if necessary, a dose can be increased to 200 mg / day; for the prevention of migraine attacks are prescribed. 100-200 mg 1 time / day; elderly patients, patients with renal failure or patients on hemodialysis, dose correction is not required.; Violations of the liver function affect the removal of metoprolol, therefore, a dose correction may be required depending on the clinical state.

Side effects

Frequency side Effects: Very often (\u003e 1/10), often (\u003e 1/100 and less than 1/10), infrequently (\u003e 1/1000 and less than 1/100), rarely (\u003e 1/10,000 and less than 1/1000), Very rare (less than 1/10,000, including individual messages).; from the side of cardio-vascular system: often - bradycardia, ortostatic hypotension (including fainting), cooling lower extremities, feeling of heartbeat; Infrequently - temporary strengthening of heart failure symptoms, cardiogenic shock in patients with myocardial infarction, AV degree AV blockade; rarely - the conductivity violations of myocardium, arrhythmia; Very rarely - gangrene (in patients with peripheral circulatory disorders).; from the CNS: Very often - increased fatigue, reducing the rate of mental and motor reactions; Often - dizziness, headache; infrequently - paresthesia, convulsions, depression, decline in the concentration of attention, drowsiness, insomnia, nightmarish dreams; rarely - asthenia, tremor, increased nervous excitability, anxiety; Very rarely - amnesia / violation of memory, depression, hallucinations, myasthenia.; on the part of the senses: rarely - impairment of vision, dryness and / or eye irritation, conjunctivitis; Very rarely - ringing in the ears, violation of taste sensations.; on the part digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently vomiting; Rarely - dry oral mucosa, violation of the liver function, hepatitis.; from the side skin Pokrov: infrequent - urticaria, strengthening of sweating; rarely alopecia; Very rarely - photosensibilization, aggravation of the flow of psoriasis, psoriazo-like skin reactions.; From the side of the respiratory system: often - shortness of breath; infrequently - bronchospasm in patients with bronchial asthma; Rarely rhinitis.; on the part of laboratory indicators: very rarely thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of hepatic enzymes, hyperbilirubinemia.; from endocrine system: often - hypoglycemia (in patients with type 1 diabetes mellitus), rarely hyperglycemia (in patients with type 2 diabetes mellitus), hypothyroid condition.; Other: infrequently - an increase in body weight; rarely - impotence / sexual dysfunction; Very rarely - arthralgia, thrombocytopenia.

Overdose

Symptoms: pronounced bradycardia, AV blockade (up to the development of the full transverse blockade and stopping heart), excessive decrease in blood pressure, impaired peripheral blood circulation, strengthening symptoms of heart failure, cardiogenic shock, inhibition of breathing, apnea, cyanosis, increased fatigue, dizziness, loss of consciousness , coma, tremor, convulsions, increased sweating, paresthesias, bronchospasm, nausea, vomiting, it is possible to develop esophagospasm, hypoglycemia or hyperglycemia, hypercalemia, transient miastic. The first signs of overdose are manifested in 20 minutes after taking the drug.; Treatment: if the drug is adopted recently - washing the stomach and reception of adsorbing agents; in violation of AV conductivity and / or bradycardia - in / in the introduction of 1-2 mg of atropine, epinephrine (adrenaline) or the setting of the temporary pacemaker; When declining the patient's blood pressure should be transferred to the Trendelenburg position. If there are no signs of pulmonary edema - in / in plasma-substituting solutions, with ineffectiveness - the introduction of epinephrine, dopamine, dobutamine; with acute heart failure - heart glycosides, diuretics; for convulsions - in / in diazepam; With bronchospasm - inhalation or parenterally beta2-adrenomimetics.

Interaction with other drugs

Means that reduce the stocks of catecholamines (for example, reserpine, Mao inhibitors) while simultaneously use with metoprolol can enhance the hypotensive effect or cause pronounced bradycardia. A break in the treatment between the intake of inhibitors of Mao and Metoprolol should be at least 14 days .; Metoprolol is the substrate of the CYP2D6 isoenzyme. Medicinal productswhich inhibit or induce the activity of CYP2D6, can affect the plasma concentration of metoprolol.; CYP2D6 inhibitors (some antidepressants and neuroleptics, quinidine, terbinefin, celecoxib, conpaphenone, diphenhydramine, hydroxychlorine, cimetidine) increase the concentration of metoprolol in blood plasma.; Inductors CYP2D6 (derivatives Barbituric acid, rifampicin) reduce the concentration of metoprolol in blood plasma.; simultaneous method of metoprolol with cardiac glycosides, clonidine, poly-calcium channel blockers (verapamil, diltiazem), amiodarone, antiarrhythmic means I class, a means for general anesthesia, methyldop, Guangfatin can lead to a decrease in blood pressure and pronounced bradycardia.; Funds for inhalation Narcosis (hydrocarbon derivatives), while simultaneously use with metoprolol, increase the risk of oppression of the myocardial function and the development of arterial hypotension.; Simultaneous in / in the introduction of verapamil can trigger the heart stop.; NSAIDs and beta adrenemeters weaken the antihypertensive effect of beta-adrenobloclars.; Arkaloids Metoprolol raises the risk of peripheral circulatory disorders.; With a joint method of metoprolol with oral hypoglycemic drugs, it is possible to reduce their effect; With insulin - raising the risk of development of hypoglycemia, lengthening and enhancing its severity, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).; Metoprolol reduces xanthin clearance (except diaphiline), especially in patients with initially increased theophylline clearance under the influence of smoking.; Metoprolol reduces lidocaine clearance increases the concentration of lidocaine in plasma.; Metoprolol enhances and prolongs the effect of non-compolant minelaxants; Extlifies the anticoagulant effect of kumarins.; With simultaneous administration of epinephrine (adrenaline) with beta-adrenoblockers, it is possible to increase blood pressure and bradycardia.; Phenylpropanolamine (Norefedrine) with a simultaneous use with metoprolol can increase diastolic blood pressure .; Allergens used for immunotherapy, or allergen extracts for immunotherapy samples When sharing with metoprolol, the risk of systemic allergic reactions or anaphylaxis;; iodine-containing radiopatrical agents for in / in administration with joint use with metoprolol, increase the risk of developing anaphylactic reactions.; With the joint use of metoprolol with ethanol, the risk of a pronounced reduction of blood pressure increases

special instructions

Control of patients receiving beta-adrenoblays include regular observation of heart rate and blood pressure. The patient should be trained by the CSS counting methodology and to instruct the need for medical advice at the heart rate of less than 50 ° C. / min.; It is possible to strengthen the severity of allergic reactions (against the background of an exempted allergological history) and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline); in elderly patients It is recommended that the kidney function is monitored (1 time in 4-5 months).; Reception of the drug Metoprolol Retard-acryoine can increase the symptoms of the impaired peripheral blood circulation.; With a stainlessness of the voltage, a selected dose of the drug should provide heart rate at rest within 55-60 Д. / Min, with a load - no more than 110 ° C. / min.; in smokers patients, the effectiveness of beta-adrenoblastors is lower .; Metoprolol Retard-Akrichin can mask some clinical manifestations thyrotoxicosis (for example, tachycardia). The sharp cancellation of the drug in patients with thyrotoxicosis is contraindicated, since it is capable of strengthening symptoms.; With diabetes mellitus, metoprolol retard-acryene drug can mask tachycardia caused by hypoglycemia.; If necessary, beta2-adrenomimetics are used as concomitant therapy to patients with bronchial asthma; at feochromocytoma - alpha-adrenoblays.; if necessary surgical intervention It is necessary to prevent the anesthesiologist's doctor about taking the drug Metoprolol Restard-Akrichin (a choice of means for general anesthesia with a minimum negative inotropic effect is required), the abolition of the drug is not recommended.; Reciprocal activation wandering nerve It can be eliminated in / in the administration of atropine (1-2 mg).; in case of increasing bradycardia (less than 50 UD / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias , severe disorders of the liver and kidney function need to be reduced by a dose or discontinue treatment .; It is recommended to stop therapy when the skin rashes and the development of depression caused by the reception of beta-adrenobloclochetors.; With a sharp cancellation of clonidine, it can dramatically increase the blood pressure, while receiving beta-adrenoblockers. In case of cancellation of clonidine, the termination of the reception of beta-adrenobloclockers should be started a few days before the cancellation of the clonidine.; Preparations that reduce the stocks of catecholamines (for example, reserpine) can enhance the effect of beta-adrenobloclars, so patients taking such combinations of drugs should be under constant medical supervision for the detection of excessive decrease in blood pressure or bradycardia.; With a sharp discontinuation of treatment, cancellation syndrome may occur (increase in angina attacks, increased blood pressure). Special attention in the abolition of the drug must be given to patients with angina, chronic heart failure, after the myocardial infarction suffered. The abolition of the drug metoprolol Retard-Akrichin is gradually carried out, reducing the dose for 10 days.; Patients who use contact lenses, I must take into account that against the background of the treatment of beta-adrenoblockers it is possible to reduce the products of the tear fluid.; Effect on the ability to drive vehicles and management of mechanisms; during the treatment period, caution must be taken when driving vehicles and occupation of other potentially hazardous species Activities requiring increased concentration of attention and speed of psychomotor reactions.

Beta 1 -adrenoblocator

Active substance

Release form, composition and packaging

Auxiliary substances: HalpRellos - 155.96 mg, Ludipress LCER (monohydrate lactose - 94.7-98.3%, - 3-4%) - 117.21 mg, silicon colloidal dioxide - 1.5 mg, magnesium stearate - 1.5 mg.

The composition of the shell: The finished mixture of "Odrai II" of orange color (polyvinyl alcohol - 6 mg, talc - 2.22 mg, macrogol - 3.03 mg, titanium dioxide - 3.36 mg, iron oxide dye - 0.009 mg, glaze dye yellow - 0.378 mg, oxide dye oxide Black - 0.003 mg) - 15 mg.

Tablets of prolonged action covered with film shell from light green to green, round, double bobbling; On a break - white with a grayish or creamy color shade.

Auxiliary substances: Hyprocellis - 161.29 mg, LUDIPRESS LCER (monohydrate lactose - 94.7-98.3%, povidone - 3-4%) - 87.42 mg, silicon colloidal dioxide - 1.5 mg, magnesium stearate - 1.5 mg.

The composition of the shell: The finished mixture of "Oddray II" is green (polyvinyl alcohol - 6 mg, talc - 2.22 mg, macrogol - 3.03 mg, titanium dioxide - 2.925 mg, chinoline yellow dye (aluminum varnish) - 0.268 mg, iron ocheside black - 0.015 mg, Dye (aluminum varnish) - 0.542 mg) - 15 mg.

10 pieces. - Packaging cell contour (3) - packs cardboard.

Tablets of prolonged action covered with film shell yellowish brown, round, double-screw; On a break - white with a grayish or creamy color shade.

Auxiliary substances: Hyprocellis - 184.84 mg, Ludipress LCER (monohydrate lactose - 94.7-98.3%, Pisidone - 3-4%) - 412.84 mg, silicon colloidal dioxide - 3.5 mg, magnesium stearate - 3.5 mg.

The composition of the shell: The finished mixture of "Oddray II" of orange color (polyvinyl alcohol - 14 mg, talc - 5.18 mg, macrogol - 7.07 mg, titanium dioxide - 7.84 mg, iron oxide dye - 0.021 mg, iron oxide dye yellow - 0.882 mg, glaze dye oxide Black - 0.007 mg) - 35 mg.

30 pcs. - Polypropylene banks (1) - packs cardboard.
30 pcs. - Plastic bottles (1) - packs cardboard.

pharmachologic effect

Cardooselective beta 1 -adrenoblocator. It does not have a membrane-stabilizing effect and does not have internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effect.

Blocking in low doses of β 1 -adrenororeceptors of the heart, reduces the formation of CATCHOLAMINS, the formation of CAMF from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo, butmol and inthropic effect (CSS regenerates, inhibits conductivity and excitability, reduces myocardial reductions) . OPS at the beginning of use (in the first 24 hours after oral administration) increases (as a result of reciprocal increase in the activity of α-adrenoreceptors and eliminating the stimulation of β 2 -adrenoreceptors), after 1-3 days it returns to the original, and during long-term purpose decreases.

The antihypertensive effect is due to a decrease in the minute volume of blood flow and synthesis of renin, the oppression of the activity of RAAS (it is greater in patients with the initial hyperception of renin) and the central nervous system, the restoration of the sensitivity of the aortic arc baroreceptors (there is no amplification of their activity in response to decreased blood pressure) and as a result, a decrease in peripherals Sympathetic influences. Reduces increased blood pressure at rest, with physical stress and stress. Antihypertensive effect lasts more than 24 hours.

The antiagonal effect is determined by a decrease in the need of myocardium in oxygen as a result of a decrease in heart rate (lengthening of diastole and improved myocardial perfusion) and a reduction, as well as a decrease in the sensitivity of myocardium to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases the tolerability of physical exertion. Due to the increase in the final diastolic pressure in the left ventricle and increasing the stretching of muscle ventricular fibers can increase the need for oxygen, especially in patients with chronic heart failure.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, the increased activity of the sympathetic nervous system, an increased content of CAMF, arterial hypertension), a decrease in the speed of spontaneous excitation of sine and ectopic rhythm drivers and a deduction of AV (mainly in antegradine and to a lesser extent in retrograde directions through AV - SELL) and for extra ways.

In case of sucanementaric tachycardia, the flickering of atrial, sinus tachycardia with functional diseases of the heart and thyrotoxicosis is reducing the heart rate or may even lead to the restoration of sine rhythm.

Warns the development of migraine.

In contrast to non-selective beta-adrenobloclockers, at average therapeutic doses, there is a less pronounced effect on organs containing β 2 - adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and for carbohydrate exchange; The severity of atherogenic action does not differ from the action of propranolol. With many years of reception, it reduces the concentration of cholesterol in the blood. When applied in large doses (more than 100 mg / day), it has a blocking effect on both subtype of β-adrenoreceptors.

Pharmacokinetics

Suction

Absorption when receiving inside full (95%). Solubility in fats moderate. It is subjected to intense preyed metabolism, bio-sauna - 50% at the first reception and increases to 70% during re-use. The time of reaching C Max in the blood is 6-12 hours after receiving the drug. During the course treatment, bioavailability increases. Eating increases bioavailability by 20-40%.

Distribution

Binding with plasma proteins - 10%. Quickly distributed in the tissues, penetrates the BC, a placental barrier. Penetrates breast milk.

Metabolism

Metabolized in the liver, 2 metabolite possess beta-adrenoblocking activity. The CYP2D6 isoenzyme takes part in the drug metabolism.

Election

T 1/2 - from 3.5 to 7 hours when taking inside. Not removed during hemodialysis.

Pharmacokinetics in special clinical cases

Significant accumulation of metabolites is observed in patients with QC 5 ml / min, while the beta-adrenoblocking activity of the drug does not increase.

Bioavailability increases during cirrhosis, while its overall clearance is reduced.

Indications

• arterial hypertension;
• chronic heart failure of the II-IV functional class according to NYHA classification under compensation (as part of complex therapy);
• IHD: Prevention of stable angina attacks, decreased mortality and frequency of myocardial repeated heart attack after the acute phase of myocardial infarction;
• disturbance of the heart rhythm, including superspostricular tachycardia, reduction of the frequency of ventricular reduction in atrial fibrillation and ventricular extrasystoles;
• functional impaired cardiac activity accompanied by tachycardia;
• prevention of migraine attacks.

Contraindications

• cardiogenic shock;
• AV blockade of II-III heat;
• synoyatrial blockade;
• SCS;
• pronounced bradycardia (heart rate<50 уд./мин);
• acute heart failure or chronic heart failure in the decompensation stage;
• arterial hypotension (systolic blood pressure<100 мм рт.ст.);
• acute myocardial infarction (heart rate<45 уд/мин, интервал PQ более 0.24 с, систолическое АД <100 мм рт.ст.);
• severe bronchial asthma;
• severe impairment of peripheral blood circulation;
• simultaneous reception of Mao inhibitors or simultaneous V / in the introduction of verapamil;
• feochromocytoma (without simultaneous reception of alpha adrenoblockers);
• age up to 18 years (efficiency and safety are not established);
• lactation period;
• lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome;
• increased sensitivity to metoprolol and other beta adrenoblockers.

Carefullya drug should be prescribed under diabetes, AV blockade I of the heater, angina printelasta, metabolic acidosis, bronchial asthma, COPL, renal and / or hepatic insufficiency of severe, myasthenia, pheochromocytoma (with simultaneous adre-adrenobloclain), thyrotoxicosis, depression (in T.ch. in history), psoriasis, peripheral circulatory disorders (interspersed chromoty, Reino syndrome), pregnancy, and elderly patients.

Dosage

The drug metoprolol retard-acryer is taken inside 1 time / day. Tablets are recommended to take in the morning, not chewing, drinking water. Metoprolol Retard-Akrichin can be taken regardless of meals.

In order to prevent bradycardia, the dose is selected individually and increase gradually.

For arterial hypertension and anginathe initial dose is 50 mg 1 time / day, with an insufficient therapeutic effect, the daily dose can be increased to 100-200 mg / day. In arterial hypertension in the ineffectiveness of the drug at a dose of 100-200 mg / day, another hypotensive means can be added.

For Chronic Heart Failure II Functional Classification of NYHA(Without exacerbations the last 6 weeks and unchanged in complex therapy during the last 2 weeks) recommended initial dose - 25 mg 1 time / day. After 2 weeks, the daily dose can be increased to 50 mg, then after 2 weeks - up to 100 mg, after another 2 weeks - up to 200 mg.

For Chronic heart failure of the III-IV functional class according to NYHA classificationrecommended initial dose - the first 2 weeks 12.5 mg 1 time / day. It is possible to use metoprolol in another dosage form, for example, 25 mg tablets with a risk. During the period of increasing the dose, the patient must be under observation, because In some patients, symptoms of heart failure may worse.

After 1-2 weeks, the dose can be increased to 25 mg 1 time / day. Then after 2 weeks, the dose can be increased to 50 mg 1 time / day. Patients who are well transferred to the drug can double dose every 2 weeks before reaching the maximum dose of 200 mg 1 time / day.

For Secondary prevention of myocardial infarction and heart rate disordersthe initial dose is 100 mg 1 time / day.

For Functional violations of cardiac activity accompanied by tachycardia,assign 50 mg / day, if necessary, a dose can be increased to 200 mg / day.

For Preventing migraine attacks Assign 100-200 mg 1 time / day.

Elderly patients, patients with renal failure or patients on hemodialysis, Dose correction is not required.

Violations of the liver function Influenced by the removal of metoprolol, therefore, a dose correction may be required depending on the clinical state.

Side effects

Side Effect Frequency: Very often (\u003e 1/10), often (\u003e 1/100 and<1/10), нечасто (>1/1000 I.<1/100), редко (>1/10 000 I.<1/1000), очень редко (<1/10 000, включая отдельные сообщения).

From the side of the cardiovascular system:often - bradycardia, orthostatic hypotension (including fainting), cooling lower extremities, feeling of heartbeat; infrequently increased strengthening of heart failure symptoms, cardiogenic shock in patients with myocardial infarction, AV degree AV blockade; rarely - the conductivity violations of myocardium, arrhythmia; Very rarely - gangrene (in patients with peripheral circulatory disorders).

From the CNS:very often - increased fatigue, reducing the rate of mental and motor reactions; Often - dizziness, headache; infrequently - paresthesia, convulsions, depression, decline in the concentration of attention, drowsiness, insomnia, nightmarish dreams; rarely - asthenia, tremor, increased nervous excitability, anxiety; Very rarely - amnesia / violation of memory, depression, hallucinations, myasthenia.

From the senses:rarely - violation of vision, dryness and / or eye irritation, conjunctivitis; Very rarely - ringing in the ears, violation of taste sensations.

From the digestive system:often - nausea, abdominal pain, constipation or diarrhea; infrequently vomiting; Rarely - dry oral mucosa, violation of the liver function, hepatitis.

From the side of the skin:infrequently - urticaria, strengthening of sweating; rarely alopecia; Very rarely - photosensibilization, exacerbation of the flow of psoriasis, psoriazo-like skin reactions.

From the respiratory system:often - shortness of breath; infrequently - bronchospasm in patients with bronchial asthma; Rarely rhinitis.

From the laboratory indicators:very rarely thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increasing the activity of hepatic enzymes, hyperbilirubinemia.

From the endocrine system:often - hypoglycemia (in patients with type 1 diabetes mellitus), rarely hyperglycemia (in patients with type 2 diabetes mellitus), hypothyroid state.

Others:infrequently - an increase in body weight; rarely - impotence / sexual dysfunction; Very rarely - arthralgia, thrombocytopenia.

Overdose

Symptoms:pronounced bradycardia, AV blockade (up to the development of the full transverse blockade and stopping heart), excessive decrease in blood pressure, impaired peripheral blood circulation, strengthening of symptoms of heart failure, cardiogenic shock, respiratory depression, apnea, cyanosis, increased fatigue, dizziness, loss of consciousness, coma , tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, the development of esophagospasm, hypoglycemia or hyperglycemia, hypercalemia, transient miastic. The first signs of overdose are manifested in 20 minutes after taking the drug.

Treatment:if the drug adopted recently - washing the stomach and reception of adsorbing agents; in violation of AV conductivity and / or bradycardia - in / in the introduction of 1-2 mg of atropine, epinephrine (adrenaline) or the setting of the temporary pacemaker; When declining the patient's blood pressure should be transferred to the Trendelenburg position. If there are no signs of pulmonary edema - in / in, with ineffectiveness - the introduction of epinephrine, dopamine, dobutamine; with acute heart failure - heart glycosides, diuretics; for convulsions - in / in diazepam; With bronchospasm - inhalation or parenterally beta 2 -adrenomimetics.

Medicinal interaction

Means that reduce the stocks of catecholamines (for example, reserpine, Mao inhibitors) while simultaneously use with metoprolol can enhance the hypotensive effect or cause pronounced bradycardia. A break in the treatment between the intake of Inhibitors of Mao and Metoprolol should be at least 14 days.

Metoprolol is the substrate of the CYP2D6 isoenzyme. Drugs that inhibit or induce the activity of CYP2D6 can affect the plasma concentration of metoprolol.

CYP2D6 inhibitors (some antidepressants and neuroleptics, quinidine, terbinefin, celecoxib, conpaphenone, diphenhydramine, hydroxy chlorin, cimetidine) increase the concentration of metoprolol in the blood plasma.

CYP2D6 inductors (barbituric acid derivatives, rifampicin) reduce the concentration of metoprolol in blood plasma.

The simultaneous intake of metoprolol with heart glycosides, clonidine, block plactors of slow calcium channels (verapamil, diltiazem), amiodarone, antiarrhythmic media I, with means for general anesthesia, methyldop, guangafatin can lead to a decrease in blood pressure and pronounced bradycardia.

The means for inhalation anesthesia (hydrocarbon derivatives) while simultaneously use with metoprolol increase the risk of oppression of the function of myocardium and the development of arterial hypotension.

Simultaneous in / in the introduction of verapamil can provoke a heart stop.

NSAIDs and beta adrenomimetics weaken the antihypertensive effect of beta-adrenobloclars.

The alkaloids of the ardines with simultaneous use with metoprolol increase the risk of peripheral circulatory disorders.

With a joint method of metoprolol with oral hypoglycemic drugs, it is possible to reduce their effect; With insulin - increasing the risk of development of hypoglycemia, lengthening and strengthening its severity, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

Metoprolol reduces xanthin clearance (except diaphiline), especially in patients with initially elevated theophylline clearance under the influence of smoking.

Metoprolol reduces lidocaine clearance, increases the concentration of lidocaine in plasma.

Metoprolol enhances and prolongs the effect of non-polarizing minelaxants; Extlifies the anticoagulant effect of kumarins.

With simultaneous admission of epinephrine (adrenaline) with beta-adrenoblockers, it is possible to increase hell and bradycardia.

Phenylpropanolamine (Norefedrin) while simultaneously use with metoprolol can increase diastolic blood pressure.

Allergens used for immunotherapy, or extracts of allergens for skin samples during co-use with metoprolol increase the risk of systemic allergic reactions or anaphylaxis.

With the joint use of metoprolol with ethanol, the risk of a pronounced decline in blood pressure increases.

special instructions

Control of patients receiving beta-adrenoblays include regular observation of heart rate and blood pressure. The patient should be trained by the procedure for calculating the heart rate and instruct about the need for medical advice at the heart rate of less than 50 ° C. / min.

It is possible to strengthen the severity of allergic reactions (against the background of a burdened allergological history) and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline).

Reception of the drug Metoprolol Restard-Akrichin can strengthen the symptoms of the impaired peripheral blood circulation.

With the walls of the voltage, the selected dose of the drug should provide heart rate at rest in the range of 55-60 ° C. / min, with a load - no more than 110 ° C. / min.

In smoking patients, the effectiveness of beta-adrenoblastors below.

Metoprolol Restard-Akrichin can mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). The sharp abolition of the drug in patients with thyrotoxicosis is contraindicated because it is capable of strengthening symptoms.

In diabetes mellitus, the drug metoprolol retard-acryoine can mask tachycardia caused by hypoglycemia.

If you need to appoint patients with bronchial asthma, beta 2 -adrenomimetics are used as concomitant therapy; With feochromocytoma - alpha-adrenoblocators.

If necessary, a surgical intervention must be warned by a anesthesiologist's doctor about taking the drug Metoprolol Restard-Akrichin (the choice of means for general anesthesia with a minimal negative inotropic effect) is not recommended for the abolition of the drug.

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

In the case of increasing bradycardia (less than 50 UD / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe disorders of the liver and kidney function, it is necessary to reduce the dose or discontinue treatment.

With a sharp cancellation of clonidine, he can dramatically increase the blood pressure, while at the same time receiving beta-adrenobloclars. In case of cancellation of clonidine, the termination of the reception of beta-adrenoblastors should be started a few days before the cancellation of the clonidine.

Preparations that reduce the reserves of catecholamines (for example, reserpine) can enhance the effect of beta-adrenobloclockers, therefore patients taking such combinations of drugs should be under constant medical supervision to identify excessive decrease in blood pressure or bradycardia.

With a sharp discontinuation of treatment, cancellation syndrome may occur (enhancing angina attacks, an increase in blood pressure). Special attention in the abolition of the drug must be given to patients with angina, chronic heart failure, after the myocardial infarction suffered. The abolition of the drug metoprolol Retard-Akrichin is gradually carried out, reducing the dose within 10 days.

Patients enjoying contact lenses should take into account that against the background of the treatment of beta-adrenoblockers, it is possible to reduce the products of the tear fluid.

Impact on the ability to driving vehicles and control mechanisms

During the period of treatment, care must be taken when driving vehicles and occupation by other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Pregnancy and lactation

When pregnancy, the drug Metoprolol Restard-Akrichin should be applied only by strict indications when the expected benefit for the mother exceeds the potential risk to the fetus / child (due to the possible development of newborn bradycardia, reduction of blood pressure, hypoglycemia and respiratory paralysis). At the same time, careful observation is carried out especially for the development of the fetus. Treatment is stopped in 48-72 hours before the occurrence of childbirth. If this is not possible, the newborn must be under particularly thorough observation within 48-72 hours after childbirth.

Application in old age

Patients of elderly dose correction is not required.

Conditions of vacation from pharmacies

The drug is released by the prescription.

Terms and Storage Terms

The drug should be stored in a dry, light-protected, inaccessible for children at a temperature not higher than 25 ° C. Shelf life - 2 years.

During treatment, it is possible to change the results of tests during laboratory studies (increase of urea level, transamamine, phosphatase, LDH).

Precautions

In patients with chronic heart failure, it is possible to deteriorate the contractile ability of myocardium, which causes the need to apply heart glycosides and / or diuretics with careful monitoring of hemodynamic status. In the event of an increasing bradycardia or AV blockade, it is necessary to reduce the dose or in / in entering atropine. Against the background of sugar diabetes and hyperfunction of the thyroid gland, metoprolol can mask tachycardia caused by hypoglycemia or thyrotoxicosis. In patients with diabetes, the dose correction of antidiabetic drugs and thorough control of the level of glycemia is needed. During the treatment of surgical intervention, a anesthetic agent with the smallest negative inotropic effect should become a means of choice. Perhaps the more pronounced development of the reaction of hypersensitivity and the absence of the therapeutic effect of conventional doses of adrenaline on the background of an exempted allergological history. With the termination of the simultaneous treatment with clonidine, the metoprolol is canceled gradually, a few days before the cancellation of the clonidine, due to the danger of the development of severe hypertensive crisis. In patients with feochromocyte, use is possible only with alpha-adreenolithics. The metoprolol reception is stopped in 2-3 days before delivery (the risk of bradycardia, hypotension and hypoglycemia in a newborn), in exceptional cases, newborns after delivery should be under medical control within 48-72 hours. It should be refracted from use in pediatric practice, since the safety and efficiency of its use in children is not defined. When canceling treatment, reduce the dose must be gradually within 10-14 days. Patients with IBS should be under the careful observation of the doctor during this period. With caution to apply during operation to drivers of vehicles and people whose profession is associated with increased concentration of attention.

Application Metoprolol Retard Akrichin during pregnancy and feeding

Perhaps if the expected effect of therapy exceeds the potential risk to the fetus. At the time of treatment, breastfeeding should be stopped.

Overdose

Symptoms: arterial hypotension, sharp heart failure, bradycardia, heart stop, AV blockade, cardiogenic shock, bronchospasm, respiratory impairment and consciousness / coma, nausea, vomiting, generalized cramps, cyanosis (manifest after 20 minutes - 2 hours after reception).

Treatment: stomach wash, symptomatic therapy: administration of atropine sulfate (V / in fast 0.5-2 mg) - in bradycardia and violation of AV conduction; glucagon (1-10 mg V / B, then in / in drip 2-2.5 mg / h) and dobutamine - in the event of a decrease in myocardial reduction; adreminimetics (noraderenalin, adrenaline, etc.) - with arterial hypotension; diazepam (in / in slow) - to eliminate seizures; Inhalation of beta adrenomimetics or in / in inkjet administration of Euphillin to relieve bronchospast reactions; Cardiosulation.

Interaction

The hypotension potentiate sympatholytolitis, nifedipine, nitroglycerin, diuretics, hydralazine and other hypotensive drugs. Antiarrhythmic and anesthesia rates increase the risk of developing bradycardia, arrhythmias, hypotension. Preparations of vintage potentiate the deceleration of AV conductivity. Simultaneous in / in the introduction of verapamil and diltiazem can provoke a stop of the heart. Beta adreminimetics, aminoophyllin, cocaine, estrogens, indomethacin and other NSAIDs weaken antihypertensive effect. Enhances and prolong the effect of antide -olarizing muscle relaxants. The combination with alcohol leads to a mutual strengthening of the oppressive effect on the CNS. Allergens increase the risk of severe systemic allergic reactions or anaphylaxis. Changes the effectiveness of insulin and oral antidiabetic agents and increases the risk of hypoglycemia. Oral contraceptives, cimetidine, ranitidine, phenothiazines - increase the level of metoprolol in the blood, rifampicin - reduces. Lower Lidocaine clearance, beta2-adrenomimetics efficiency (a dose increase in the latter). Incompatible with Inhibitors of Mao Type A.

Side effects metoprolol retard Akrichin

From the side of the nervous system and senses: at least 10% - weakness; 1-9.9% - dizziness and headache; 0.1-0.9% - Reducing attention concentration, drowsiness / insomnia, nightmares, depression, muscle cramps, paresthesia; 0.01-0.09% - nervousness, anxiety, weakening of libido, visual impairment, xerofthalmia, conjunctivitis; Less than 0.01% - lethargy, increased fatigue, anxiety, confusion of consciousness, amnesia / short-term loss of memory, hallucinations, noise in ears, violation of taste sensations.

From the cardiovascular system and blood (hematoporation, hemostasis): 1-9.9% - bradycardia, heartbeat, hypotension, cooling limbs; 0.1-0.9% - heart failure, AV blockade, edema syndrome, chest pain; 0.01-0.09% is a decrease in the reduction of myocardium, arrhythmia, less than 0.01% - gangrene (in patients with severe peripheral circulation); Violation of the conductivity of myocardium, syncope, thrombocytopenia, leukopenia, agranulocytosis.

From the head of the gastrointestinal bodies: 1-9.9% - nausea, abdominal pain, diarrhea or constipation; 0.1-0.9% - vomiting; 0.01-0.09% - dryness in the oral cavity, liver function disorders; Meteorism, dyspepsia, heartburn, hepatitis.

From the respiratory system: shortness of breath (1-9.9%), bronchospasm (0.1-0.9%), vasomotor rhinitis (0.01-0.09%), dneap.

From the side of the skin: 0.1-0.9% - rash, dystrophic skin changes; 0.01-0.09% - reversible alopecia; less than 0.01% - photosensibilization, exacerbation of psoriasis; Itching, erythema, urticaria, hyperhydrosis.

Others: Reducing body weight (0.1-0.9%), arthritium, arthritis, Malgy, muscle weakness, Peyroni disease.

Restrictions on application

Sugar diabetes, hypoglycemia, burded allergic history, metabolic acidosis, bronchial asthma, emphysema, non-allergic bronchitis, hyperthyroidism, psoriasis, feuhromocytoma, violation of the liver function and / or kidney, myasthenia, depression, carrying out general anesthesia, elderly and children's age.

Metoprolol retard Akrichin Contraindication

Hypersensitivity, AV blockade II and III degree, synoatrial blockade, acute or chronic (in the decompensation stage) heart failure, sine node weak syndrome, expressed sinus bradycardia (heart rate less than 60 q / min), cardiogenic shock, arterial hypotension (garden less 100 mm Hg. Art.), Pronounced disorders of peripheral blood circulation, pregnancy, breastfeeding.

Indications for the application of metoprolol retard Akrichin

Arterial hypertension of moderate and moderate gravity (monotherapy or in combination with other hypotensive drugs), IBS, hyperkinetic cardiac syndrome, heart rate impaired (sinus tachycardia, ventricular and sufficientar-centuric arrhythmia, including paroxysmal tachycardia, sucanementaricular tachycardia, extrasistol, fluttering and flickering atrial, atrial Tachycardia), hypertrophic cardiomyopathy, mitral valve prolapse, myocardial infarction (prevention and treatment), migraine (prevention), thyrotoxicosis (complex therapy); Treatment of acatus caused by neuroleptics.

pharmachologic effect

Pharmacological action - antianginal, hypotensive, antiarrhythmic. Blocks predominantly beta1-adrenoreceptors of the heart, does not have internal sympathomimetic and membrane-stabilizing activity. Reduces the heart rate and the garden, slows down the heart rate, weakens the stimulating effect of catecholamines on myocardials during exercise and mental overvoltage, prevents reflex orthostatic tachycardia. The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, the inhibition of the activity of the renin-angiotensin system and the central nervous system, the restoration of the sensitivity of baroreceptors and, as a result, a decrease in peripheral sympathetic influences. The hypotensive effect develops quickly (the garden decreases after 15 minutes, the maximum - after 2 hours) and continues for 6 hours; When taking the subcinate metoprolol - the clinical effect of the blockade of beta1-adrenoreceptors is preserved 24 hours. Dad varies slower: a stable decrease is observed after several weeks of regular reception. The antianginal effect is a consequence of the reduction of the frequency and force of heart rate, the energy costs and the needs of myocardium in oxygen. Reduces the frequency and severity of IBS seizures, the mortality rate in patients with diagnosed myocardial infarction increases the portability of the loads. Metoprollane succinate reduces the risk of death (including sudden death), the occurrence of repeated heart attack (including patients with diabetes mellitus) and improves the quality of life of patients with acute myocardial infarction and idiopathic dilatation cardiomyopathy. An antiarrhythmic effect manifests itself in the elimination of arrhythmogenic sympathetic effects on the conductive heart system, slowing the sinus rhythm and the speed of excitation of excitation via AV node, braking of automatism and lengthening the refractory period. It has a moderate negative inotropic effect. Cardooselectivity is preserved when using daily doses, not exceeding 200 mg. Due to the election action on beta1-adrenoreceptors, the risk of bronchospasm is theoretically reduced (in patients with bronchial asthma less decreases the life function of the lungs), hypoglycemia and narrowing peripheral vessels.

In experiments on dogs (up to 105 mg / kg / day, for 1 year), rats (up to 800 mg / kg / day, for 2 years) and mice (up to 750 mg / kg / day, for 21 months) Signs of carcinogenicity were not found, but histological changes in the type of hyperplasia of hepatic cells and induction by macrophages of the pulmonary fabric are revealed. With the introduction of albino mice in doses up to 750 mg / kg / day for 21 months, increased the frequency of the development of benign adenomes in the females, but when re-conducting experience, an increase in the incidence of any tumors was not noted. The results of the test of dominant lethal mutations in mice, studies of chromosome of somatic cells, dough on the anomalies of the nuclei of somatic cells in interfase, etc. indicated the absence of mutagenic properties. In rats received doses, 55.5 times higher than the maximum daily dose for a person (450 mg) did not affect fertility, increased the parameters of the postpact death and reduced the survival rate of newborn animals (there was no signs of teratogenicity).

Metoprolol Tartrate quickly and almost completely (95%) is absorbed when taking inside, subjected to intense preyed metabolism. Bioavailability is about 50% at the first reception and increases to 70% when re-use. About 12% binds to albumin plasma blood. It is quickly distributed in the tissues, penetrates through the GEB (the level in the CNS is 78% of the plasma concentration), the placental barrier, breast milk (concentration exceeds plasma). Distribution volume - 5.5 l / kg. Cmax is achieved after 1-2 hours after taking, the blood level varies significantly. T1 / 2 - from 3 to 7 hours. Biotransformed in the liver, with the formation of two active metabolites. It is removed mainly by the kidneys in the form of metabolites, CL - 1 l / min. When taking inside, less than 5% is excreted with urine unchanged, with in / in infusion - about 10%. If the kidney function is violated, bioavailability does not change, but the rate of excretion of metabolites can decrease. In patients with cirrhosis of the liver, metabolism and general clearance slows down (no dosing mode correction is required). Not removed during hemodialysis. When in / in the infusion of the metoprolol of the tartrate for 10 minutes and the more maximum action is developing after 20 minutes, the demolition of the heart rhythm with doses of 5 and 10 mg is 10 and 15%, respectively. After taking inside in the same doses of Cmax metoprolol, the succinate is 1/4-1 / 2 cmax metoprolol of the tartrate, but is more durable. Bioavailability in doses of 50-400 mg (1 time per day) by 23% less from such after the reception of a similar dose of tartrate. Pharmacokinetic parameters do not depend on the age of patients.

Characteristic

Metoprolol Tartrate: White, almost odorless crystalline powder, well-soluble in water, methylene chloride, chloroform and alcohol, weakly soluble in acetone, insoluble on the air.

Metoprolol Sukcinate: White crystalline powder, easily soluble in water, soluble in methanol, moderately soluble in ethanol, weakly soluble in dichloromethane and 2-propanol, practically insoluble in ethyl acetate, acetone, diethyl ether and heptane.

Chemical name metoprolol retard Akrichin

(±) -1--3 - [(1-methyl ethyl) amino] -2-propanol (in the form of a tartrate or succinate)

Metoprolol Reptard is appointed by medical experts to reduce blood pressure and eliminate symptoms of ischemic disease. The drug allows you to normalize the heart rate, with prolonged use for several years, reduces cholesterol levels. As a result, it is possible to stabilize blood pressure indicators, reduce the risk of developing myocardial infarction, atherosclerotic changes in vessels and the development of ischemia.

Release form, composition and packaging

Cardooselective Beta-adrenoreceptor blocker is produced in tablet form. The unit of medication contains 25, 50 or 100 mg of metoprolol succinate. Tablets visually distinguished by brown-yellow color and round shape.

Ingredients are additionally used:

• povidone;
• milk sugar;
• hypimloose;
• colloid dehydrated silicon dioxide;
• magnesium stearate.

The surface of the tablets is covered with an outer film sheath consisting of macrogol, talc, titanium dioxide and polyvinyl alcohol. The yellow-brown tablets give the presence of a red, black and yellow dye based on iron oxide. In contour cellular packages, contains 10 units of the drug.

pharmachologic effect

The medication allows you to stabilize heart rate rhythms, has a hypotensive and antiagonal effect. Pharmacological properties are based on the suppression of the activity of beta adrenoreceptors of the heart. As a result, the conductivity of nerve impulses in myocardium occurs, the excitability and the frequency of heart abbreviations (heart rate) decreases.

The total peripheral resistance after one-time intake is increased during the first day, after which it returns to the initial values \u200b\u200bwithin 24-72 hours. With long-term method of metoprolol, it gradually decreases.

The antianginal effect is due to a decrease in the need of cardiomyocytes in oxygen. This occurs as a result of a decrease in heart rate and myocardial susceptibility to impulses of the sympathetic nervous system. There is an increase in myocardium resistance to physical exertion, the degree of severity and the frequency of angina attacks are reduced.

The pressure is reduced against the background of drug therapy due to a reduction in the minute volume of blood and reinforcing renin production. The hypotensive effect is preserved for 24 hours and is not weakened from stressful conditions, physical activity.

Unlike non-selective beta1 adrenoblockers, metoprolol does not have a strong influence on carbohydrate exchange and does not suppress the effect of beta2-adrenoreceptors. With regular reception for 1-5 years, a decrease in the plasma concentration of cholesterol may be observed.

The medicine is 95% absorbed in the microvascular of the small intestine, from where it falls into the arterial bed. At the first passage through the liver cells, bioavailability decreases to 50%, while metoprolol is intensive transformation with the formation of 2 active metabolites. When receiving a re-dose, bioavailability rises to 70%. Succinate metoprolol reaches maximum values \u200b\u200bin blood serum for 6-12 hours. Parallel meal increases bioavailability by 25-40%.

There is a low degree of binding with plasma proteins - 10%. The half-life lasts from 3.5 to 7 hours. The drug is excreted through the kidneys.

Indications for the use of metoprolol retard

In clinical practice, the drug is applied to:

• reduction of high blood pressure (blood pressure);
• stabilization of cardiac rhythm on the background of ventricular extrasystole, suprazdroke tachycardia, atrial fibrillation;
• eliminating ischemic heart disease and as a prevention of aggravation of stable angina, reducing the likelihood of death or re-infarction of the heart muscle;
• treatment of heart failure chronic form;
• elimination of disorders of the functional activity of the heart.

The medicine is used as a preventive measure in the fight against migraine.

Method of Dosing Metoprolol Retard

The medicine must be taken 1 time per day. It is recommended to take tablets in the morning. To reduce the risk of bradycardia, the dosage for each patient is selected on an individual basis. With an insufficient therapeutic effect, one-time dose gradually increases.

Side effect

Contraindications for the use of metoprolol retard

It is strictly forbidden to prescribe a drug to people with the following diseases:

• atrioventricular blockade of the II-III degree and synoatrial blockade;
• heart rate below 50 shots per minute;
• cardiogenic shock;
• acute heart muscle heart attack;
• severe bronchial asthma;
• acute heart failure;
• hereditary form of hypolactasy, lactase deficiency, glucose-galactose malabsorption syndrome;
• feochromocytoma;
• severe peripheral circulation disorders;
• increased susceptibility to metoprolol and subsidiary components.

special instructions

Careful control of blood pressure and heart rate monitoring during drug therapy is needed. The patient should inform the attending physician about the reduction of heart rhythm below 50 ice / min or the appearance of adverse reactions from the CNS. Therapeutic effect is reduced during smoking.

In predisposed patients's allergy, there is an absence of an organism's reaction to the standard dosage of epinephrine and the appearance of anaphylactic reactions. Before conducting an operational intervention, you must inform the duty anesthesiologist about the method of metoprolol.

The drug is able to disguise the clinical picture of thyrotoxicosis. Patients with this pathological process strictly prohibited a sharp cessation of therapy, because it is possible to strengthen the symptomatic picture of thyrotoxicosis.

In some cases, with a sharp cancellation of therapy, the abolition syndrome is possible, characterized by an increase in blood pressure, in the amplification of angina. Clean the reception with a gradual reduction in dosage for 7-10 days.

Patients who use contact lenses is important to take into account that the production of tear fluid is reduced during the treatment of beta-adrenoblockers.

Application in pregnancy and breastfeeding

The medicine is accepted under strict medical control only in cases where the benefits for the organism of the mother above the expected appearance of anomalies in the fetus in the process of embryonic development. During pregnancy, careful observation of the embryo is necessary. Medicinal therapy is stopped 1-3 days before the intended start of generic activity. The newborn must be under the control of a specialist within 24-72 hours after birth.

In the period of therapy, Metoprolol must cancel breastfeeding.

Application in children

The drug is prohibited for the use of children under 18.

Application with violations of the kidney function

Dose adjustment is not required.

Overdose

When abusing the drug, the appearance is possible:

• severe bradycardia;
• severe drop in blood pressure;
• peripheral circulation disorders;
• dynake;
• atrioventricular conduction disorders;
• tremor and violations of shallow motility;
• muscle cramps;
• oppression of consciousness;
• bronchospasm;
• cardiogenic shock, coma;
• blockages and stops of the heart;
• losses of glycemic control.

The first overdose symptoms begin to manifest themselves 20-120 minutes after taking a high dosage. If the patient accepted the drug for 4 last hours, it is necessary to wash the cavity of the stomach, cause vomiting and give an adsorbing agent. With pronounced bradycardia, an intravenous administration of adrenaline or an atropine dose of 1-2 mg is necessary. When decreasing blood pressure, it is necessary to translate the patient into a horizontal position and lift the legs. In case of acute heart failure, cardiac diuretics are required.

Medicinal interaction

The reserpine and monooxidase blockers with a parallel reception with metoprolol are capable of reduced the level of catecholamines, due to which an antihypertensive action is possible. Care must be taken, because such a combination of medicines can lead to severe bradycardia. To reduce the risk of the appearance of a side effect, the interval between the receptions should be 2 weeks.

The inhibitory activity of CYP2D6 isoenzyme: psychotic preparations, neuroleptics, cimetidine, terbinafin, increase the serum level of metoprolol in the blood. At the same time, the decrease in the concentration is observed when using rifampicin and barbiturates.

Preparations for inhalation anesthesia increase the likelihood of the development of hypotension. They can cause the oppression of the contractile ability of myocardium.

If during the drug therapy by Metoprolol Retard introduce intravenously verapamil, a heart stop may occur. Beta adreminimetics and nonsteroidal anti-inflammatory agents suppress the hypotensive effect.

Metoprolol is able to reduce the therapeutic effect of hypoglycemic drugs, so people with diabetes must be consulted with the attending physician about the correction of the dosage of glycemic drugs. Insulin therapy is prohibited - metoprolol increases the likelihood of the development of hypoglycemia and diabetic coma.

Contrast substances containing iodine for radiography during intravenous administration increase the likelihood of anaphylactic shock. During the period of therapy, Metoprolol Retard cannot be taken alcohol - ethanol causes a sharp drop in blood pressure. Sukcinate increases the concentration of lidocaine in plasma.

Terms and Storage Terms

The medicine can be stored for 2 years at a temperature mode to + 20 ° C. It is recommended to contain tablets in a place isolated from sun exposure.

The difference between metoprolol from metoprolol retard

The peculiarity of TTARD-Akrichin metoprolol tablets is a prolonged action that is preserved within 24 hours. In contrast, the classic metoprolol contains a salt tartrate salt that has a quick therapeutic effect for 30 minutes for a short time.

Instructions for use

Metoprolol Restard-Akrichin Instructions for use

Dosage form

Tablets covered with film shell, round, double-screwed. Tablets with dosages 100 mg of yellowish brownish color.

Structure

active substance: metoprolol Succinate in terms of 100% equivalent to 100 mg metoprolol Tartrate Auxiliary substances: Halgimelloose, LUDIPRESS LACI [monohydrate lactose, silicon colloidal dioxide dioxide; Magnesium Stearat

Pharmacodynamics

Cardooselective beta1 adrenoblocator. It does not have a membrane-stabilizing effect and does not have internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effect.

Blocked in low doses of beta1-adrenoreceptors of the heart, reduces the formation of cyclic adenosine monophosphate (CAMP) from adenosine-micron phosphate (ATP) stimulated by catecholamines, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, butmary and inthropic effect (heart rate reducing (heart rate ), inhibits conductivity and excitability, reduces the reduction of myocardium).

Overall peripheral vascular resistance (OPS) at the beginning of the use of beta-adrenobloclars (in the first 24 hours after oral administration) increases (as a result of reciprocal increase in the activity of alpha-adrenoreceptors and eliminating beta stimulation? Adrenoreceptors), which in 1-3 days returns to the original, And with long-term assignment decreases.

The antihypertensive effect is due to a decrease in the minute volume of blood flow and the synthesis of renin, the inhibition of the activity of the renin-angiotensin-aldosterone system (it is greater in patients with the initial hypersection of the renin) and the central nervous system, the restoration of the sensitivity of the aortic arc barorestors (there is no amplification of their activity in response to reduction Arterial pressure (AD) and as a result, a decrease in peripheral sympathetic effects. Reduces increased blood pressure at rest, with physical voltage and stress. Antihypertensive effect lasts more than 24 hours.

The antiagonal effect is determined by a decrease in the need of myocardium in oxygen as a result of a decrease in heart rate (lengthening of diastole and improved myocardial perfusion) and a reduction, as well as a decrease in the sensitivity of myocardium to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases the tolerability of physical exertion. Due to the increase in finite diastolic pressure in the left ventricle and an increase in the stretching of muscle fibers of the ventricles can increase the need for oxygen, especially in patients with chronic heart failure (CXN).

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, the increased activity of the sympathetic nervous system, an increased content of CAMF, arterial hypertension), a decrease in the speed of spontaneous excitation of sine and ectopic rhythm drivers and a slowdown in antegrantricular (AV) conduct (mainly in antegradine and to a lesser extent in retrograde directions Through AV node) and for additional ways.

In case of sucanementaric tachycardia, the flickering of atrial, sinus tachycardia with functional diseases of the heart and thyrotoxicosis is reducing the heart rate or may even lead to the restoration of sine rhythm.

Warns the development of migraine.

In contrast to non-selective beta-adrenobloclockers, a less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) has a less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletal muscles. The severity of atherogenic action does not differ from the action of propranolol. With many years of reception, it reduces the concentration of cholesterol in the blood. When applied in large doses (more than 100 mg / day), it has a blocking effect on both subtype of beta-adrenoreceptors.

Pharmacokinetics

Absorption when receiving inside full (95%). The maximum concentration in the blood plasma is achieved 1-2 hours after intake. The half-life on average is 3.5 hours (ranging from 1 to 9 h). It is subjected to intense pretest metabolism, bioavailability is 50% at the first reception and increases to 70% when re-use. Eating increases bioavailability by 20-40%. The bioavailability of metoprolol increases with cirrhosis of the liver. Communication with blood plasma proteins - 10%. Penetrates the hematorencephalic and placental barriers. Penetrates breast milk in minor quantities. Metabolized in the liver, 2 metabolite possess beta-adrenoblocking activity. The CYP2D6 isoenzyme takes part in the drug metabolism. About 5% is displayed unchanged by the kidneys. Treatment of patients with reduced kidney function does not require a dose correction of the drug. The violation of the liver function slows down the metabolism of the drug, and in cases of insufficiency of the liver function of the dose of the drug must be reduced. Not removed during hemodialysis.

Side effects

The frequency of side effects: very often - more than 1/10, often more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less than 1/10000, including individual messages.

From the side of the cardiovascular system: often - bradycardia, orthostatic hypotension (including fainting), cooling lower limbs, feeling of heartbeat; infrequent increase in heart failure symptoms, cardiogenic shock in patients with myocardial infarction, AV degree blockade; rarely - the conductivity violations of myocardium, arrhythmia; Very rarely - gangrene (in patients with peripheral circulatory disorders).

On the part of the central nervous system: very often increased fatigue, reducing the rate of mental and motor reactions; Often - dizziness, headache; Infrequently - paresthesia, convulsions, depression, decline in the concentration of attention, drowsiness, insomnia, "nightmarish" dreams; rarely - asthenia, tremor, increased nervous excitability, anxiety; Very rarely - amnesia / violation of memory, depression, hallucinations, myasthenia.

From the sides of the senses: rarely - impairment of vision, dryness and / or eye irritation, conjunctivitis; Very rarely - ringing in the ears, violation of taste sensations.

From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently vomiting; Rarely - dry oral mucosa, violation of the liver function, hepatitis.

From the side of the skin: infrequent - urticaria, strengthening of sweating; rarely alopecia; Very rarely - photosensibilization, exacerbation of the flow of psoriasis, psoriazo-like skin reactions.

From the respiratory system: often - shortness of breath; infrequently - bronchospasm in patients with bronchial asthma; Rarely rhinitis.

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

From the endocrine system: often - hypoglycemia (in patients with type I diabetes), rarely hyperglycemia (in patients with type II diabetes), hypothyroid state.

Others: infrequently - an increase in body weight; rarely - impotence / sexual dysfunction; Very rarely - arthralgia, thrombocytopenia.

Features of sale

prescription

Special conditions

When the stainlessness of the voltage, the selected dose of the drug should provide heart rate at rest in the range of 55-60 UD / min, with a load - not more than 110 ° C / min.

"Smokers" has the effectiveness of beta adrenoblocators below.

Metoprolol Retard can mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). The sharp abolition of the drug in patients with thyrotoxicosis is contraindicated because it is capable of strengthening symptoms.

In diabetes, it may disguise tachycardia caused by hypoglycemia.

If you need to appoint patients with bronchial asthma, beta2-adrenomimetics are used as concomitant therapy; With feochromocytoma - alpha-adrenoblocators.

If you need to carry out surgical intervention, you need to warn a doctor-anesthesiologist about the reception of the drug (the choice of means for general anesthesia with a minimal negative inotropic effect) is not recommended for the abolition of the drug.

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

In the event of an increasing bradycardia (less than 50 ration / min), arterial hypotension (systolic blood pressure below 100 mm Hg. Art.), AV blockades, bronchospasm, ventricular arrhythmias, severe disorders of the liver and kidney function, it is necessary to reduce the dose or discontinue treatment.

Metoprolol can enhance the symptoms of the peripheral circulatory disorders.

With a sharp cancellation of clonidine, can dramatically increase hell, while taking beta? Adrenoblockers. In case of cancellation of clonidine, the termination of the reception of beta-adrenoblastors should be started a few days before the cancellation of the clonidine.

Preparations that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-adrenobloclars, so patients taking such combinations of drugs should be under constant medical supervision to identify excessive decline in Hell or Bradycardia.

With a sharp discontinuation of treatment, the "Cancellation" syndrome may occur (increase in angina attacks, increased blood pressure). Special attention to the abolition of the drug must be given to patients with angina, HSN, after the myocardial infarction suffered. Cancellation of the drug is carried out gradually, reducing the dose within 10 days.

Patients using contact lenses should take into account that against the background of treatment with beta-adrenoblockers it is possible to reduce the products of the tear fluid.

During the period of treatment, care must be taken when driving vehicles and occupation by other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: pronounced bradycardia, AV blockade (up to the development of a full transverse blockade and a heart stop), a pronounced decrease in blood pressure, impaired peripheral blood circulation, strengthening of symptoms of heart failure, cardiogenic shock, respiratory depression, apnea, cyanosis, increased fatigue, dizziness, loss of consciousness, Coma, tremor, convulsions, raising sweating, paresthesia, bronchospasm, nausea, vomiting, it is possible to develop esophagospasm, hypoglycemia or hyperglycemia, hypercalemia, transient miastic. The first signs of overdose are manifested in 20 minutes after taking the drug.

Treatment:

If the drug adopted recently - washing the stomach and reception of adsorbing agents; with impaired atrioventricular conductivity and / or bradycardia - in / in the introduction of 1-2 mg of atropine, epinephrine (adrenaline) or the setting of a temporary pacemaker; With a decrease in blood pressure - the patient must be in the Trendelenburg position. If there are no signs of pulmonary edema - in / in plasma-substituting solutions, with ineffectiveness - the introduction of epinephrine, dopamine, dobutamine; with acute heart failure - heart glycosides, diuretics; for convulsions - in / in diazepam; With bronchospasm - inhalation or parenterally beta2-adrenomimetics.

Indications

Arterial hypertension (as monotherapy or in combination with other antihypertensive means);

Ischemic heart disease: Myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks;

Heart Rhythm Disorders (Support Tachycardia; ventricular extrasystole);

Hyperthyroidism (complex therapy);

Prevention of migraine attacks.

Contraindications

Increased sensitivity to metoprolol and other beta-adrenoblockers, cardiogenic shock, AV blockade of II-III degree, synoyatrial blockade, sinus-node weak syndrome, pronounced bradycardia (Heat less than 50 UD / min), acute heart failure or CHF in decompensation stage, arterial hypotension (systolic adherent less than 100 mm Hg. Art.), acute myocardial infarction (CSS less than 45 ° C / min, PQ interval more than 0.24 C, systolic blood pressure less than 100 mm Hg. Art.), Lactation period, simultaneous reception of monoaminoxidase inhibitors ( Mao) or simultaneous in / in the introduction of verapamil, feochromocytoma (without simultaneous reception of alpha-adrenobloclars), age up to 18 years (efficiency and safety are not established), lactase deficiency, lactose intolerance, glucose-galactose malabsorption, heavy bronchial asthma, severe peripheral disorders blood circulation.

Carefully

Diabetes, an atrioventricular blockade of I degree, angina printelastyle, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease, renal and / or severe hepatic insufficiency, myasthenia, feuhromocytoma (with simultaneous adre-adrenoblocators), thyrotoxicosis, depression (including . In history), psoriasis, peripheral circulatory disorders ("intersecting" chromoty, Reino syndrome), pregnancy, elderly age.

Application during pregnancy and lactation period

During pregnancy, the drug Metozok® should be applied only on strict indications when the expected benefit for the mother exceeds the potential risk to the fetus / child (due to the possible development of newborn bradycardia, reduction in blood pressure, hypoglycemia and respiratory paralysis). At the same time, careful observation is carried out especially for the development of the fetus. Treatment is stopped in 48-72 hours before the occurrence of childbirth. If this is not possible, the newborn must be under particularly thorough observation within 48-72 hours after childbirth.

The use of the drug Metozok® is contraindicated during lactation, if necessary, the use of the drug during lactation, breastfeeding must be stopped.

Medicinal interaction

Means that reduce the stocks of catecholamines (for example, reserpine, Mao inhibitors) while simultaneously use with metoprolol can enhance the hypotensive effect or cause pronounced bradycardia. A break in the treatment between the intake of Inhibitors of Mao and Metoprolol should be at least 14 days.

Metoprolol is the substrate of the CYP2D6 isoenzyme. Drugs that inhibit or induce the activity of the CYP2D6 isoenzyme can affect the plasma concentration of metoprolol.

Inhibitors of CYP2D6 isoenzyme: Some antidepressants and neuroleptics, quinidine, terbinefin, celecoxib, conpaphenon, diphydramine, hydroxychlorine, cimetidine - increase the concentration of metoprolol in blood plasma.

CYP2D6 isoenzyme inductors: barbituric acid derivatives, rifampicin - reduce the concentration of metoprolol in blood plasma.

Simultaneous reception with heart glycosides, clonidine, "slow" calcium channels (verapamil, diltiazem), amiodarone, antiarrhythmic agents I class, means for general anesthesia, methyldop, Guangafatin can lead to a decrease in blood pressure and pronounced bradycardia.

Funds for inhalation anesthesia (hydrocarbon derivatives) increase the risk of oppression of the function of myocardium and the development of arterial hypotension.

Simultaneous in / in the introduction of verapamil can provoke a heart stop.

Nonteroidal anti-inflammatory drugs (NSAIDs) and beta adrethrenimetics weaken the antihypertensive effect of beta-adrenobloclars.

The alkaloids of the ardines increase the risk of peripheral circulatory disorders.

With joint admission with oral hypoglycemic drugs, it is possible to reduce their effect; With insulin - an increase in the risk of development of hypoglycemia, lengthening and strengthening its severity, masking some symptoms of hypoglycemia (tachycardia, sweating, an increase in blood pressure).

Reduces xanthin clearance (except diaphiline), especially in patients with initially elevated theophylline clearance under the influence of smoking. Reduces lidocaine clearance increases the concentration of lidocaine in plasma.

Reinforces and prolong the effect of non-compolarizing muscle relaxants; Extlifies the anticoagulant effect of kumarins.

With simultaneous reception of epinephrine (adrenaline) with beta-adrenoblockers, it is possible to increase hell and bradycardia.

Phenylpropanolamine (Norefedrin) can increase diastolic blood pressure.

Allergens used for immunotherapy, or extracts of allergens for skin samples with co-use with metoprolol, increase the risk of systemic allergic reactions or anaphylaxis; Iodine-containing radiocontrase funds for B / in administration increase the risk of developing anaphylactic reactions.

When used with ethanol, the risk of pronounced decrease in blood pressure increases.

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