Expiration date: 08/2025

Composition

1 tablet contains: metoprolol tartrate 50 mg.

Excipients: cellulose microcrystalline, starch maize, sodium croscarmelose, copovidone, silicon dioxide colloidal anhydrous, magnesium stearate.

Pharmacological action

METOPROLOL is a selective beta-blocker that acts preferentially on beta 1-adrenergic receptors of the heart ("cardioselective beta-blocker") without internal sympathomimetic activity and with a poorly expressed membrane stabilizing effect. Has antianginal, hypotensive and antiarrhythmic action.

Blocking in low doses beta-1-adrenergic receptors of the heart, reduces catecholamines stimulated camp formation from ATP, reduces intracellular current of calcium ions , has a negative Chrono-, dromo-, batmo - and inotropic effect (slows the heart rate (HR), inhibits conduction and excitability, reduces myocardial contractility).

Total peripheral vascular resistance in the early use of beta-blockers (in the first 24 hours after ingestion) increases (as a result reciprocatng of increasing the activity of alpha-adrenergic receptors and elimination of stimulation of beta 1-adrenergic receptors), which, through 1-3 day returns to the source, and at long - decreases.

Gipotenzivne effect due to a decrease in cardiac output and synthesis of renin, inhibition of the renin-angiotensin system (is of great importance in patients with baseline hypersecretion of renin) and the Central nervous system, restoration of the sensitivity of baroreceptors of the aortic arch (does not enhance their activity in response to decreased blood pressure) and eventually, reduced peripheral sympathetic influences. Lowers high blood pressure (BP) at rest, during physical exertion and stress.

Hypotensive effect develops quickly (systolic blood pressure decreases after 15 minutes, maximum 2 hours) and lasts for 6 hours, the diastolic blood pressure changes slower: a steady decline is observed after several weeks of regular use.

Antianginalny effect is determined by the requirements decrease myocardial oxygen due to reduction in heart rate (lengthening of diastole and improved myocardial perfusion) and contractility, as well as decreased sensitivity of the myocardium to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise capacity.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased camp content, arterial hypertension), reduced rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of atrioventricular conduction (mainly in the antegrade and to a lesser extent, in the retrograde directions through the atrioventricular (AV) node) and on additional ways.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia, in functional diseases of the heart and hyperthyroidism slows the heart rate or may even lead to the restoration of sinus rhythm. Prevents the development of migraine. When used in high therapeutic doses, unlike nonselective beta-blockers, has a less pronounced effect on the organs containing the beta 1 -adrenergic receptors (pancreas, skeletal muscles, smooth muscles peripheral arteries of the bronchi and uterus) and on carbohydrate metabolism. When used in high doses (more 100 mg/day) exerts a blocking effect on both subtypes of beta-adrenergic receptors.

Testimony

• Arterial hypertension (as monotherapy or in combination with other antihypertensive agents), including hyperkinetic type.
  
• Tachycardia.
  
• Ischemic heart disease: myocardial infarction (secondary prevention), prevention of angina, supraventricular tachycardia, ventricular extrasystoles.
  

Contraindications

• Hypersensitivity to metoprolol or other ingredients, other beta-blockers.
  
• Heart failure in the decompensation stage.
  
• Cardiogenic shock.
  
• Syndrome of weakness of sinus node , Prinzmetal's angina.
  
• Atrioventricular block II and III degree.
  
• Sinoatrial block.
  
• Bradycardia (heart rate before treatment less than 50 beats per minute).
  
• Arterial hypotension (in case of use for secondary prevention of myocardial infarction, systolic BP less than 100 mm of mercury.St.).
  
• Metabolic acidosis.
  
• Late stage and severe violations of peripheral blood circulation.
  
• Concomitant use of MAO inhibitors.
  
• Lactation.
  
• The age 18 years (effectiveness and safety have not been established).
  
• When drug treatment is contraindicated in/to the introduction of such blockers "slow" calcium channels like verapamil and diltiazem , or other antiarrhythmic drugs (e.g. disopyramide ). The only exception is patients who are in intensive care.
  

With caution:

• Atrioventricular block I degree.
  
• Diabetes with strong fluctuations in blood sugar levels (the possibility of a severe hypoglycemic state).
  
• Fasting during religious fasting, and heavy physical activity (may cause severe hypoglycemic conditions).
  
• Pheochromocytoma.
  
• Chronic renal and/or hepatic insufficiency (in the appointment of metoprolol in these patients requires constant monitoring of the dynamics of the functional state of the liver and/or kidneys).
  
• Acute myocardial infarction (heart rate less than 45 beats/min, PQ interval 0.25 h, systolic BP less than 100 mm Hg. calendar).
  
• Symptomatic psoriasis or psoriasis in a personal or family history.
  
• Patients with impaired peripheral circulation, including Raynaud's syndrome.
  
• Those who are desensitizing therapy, or with severe allergic reactions in anamnesis.
  
• Bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis).
  
• Hyperthyroidism.
  
• Depression (including in history).
  
• Pregnancy.
  
• The old age.
  

In all these cases, the attending physician must carefully weigh the ratio of risk/benefit when prescribing the drug.

Application of pregnancy and breastfeeding

During pregnancy (especially in the first 3 months) the drug should be used only on strict conditions based on a thorough weighing of the benefit/risk, because to date there is no sufficient experience of its use during pregnancy, especially in the early stages of pregnancy.

If pregnant women took metoprolol, in connection with the possibility of a newborn bradycardia, hypotension and hyperglycaemia, treatment should be stopped for 48 to 72 hours before delivery. If this is not possible, the newborn needs to be under careful observation for 48-72 hours after birth.

The effect of metoprolol on the newborn, breast-feeding has not been studied, so women taking the drug, should stop breast-feeding.

Method of application and doses

The tablets are taken orally with a small amount of liquid, without chewing, with food or immediately after meals. Tablets can be divided. The course of treatment is not limited in time and depends on the characteristics of the disease. If necessary, discontinuation of treatment, reduce dose gradually (at least 10 days) under the supervision of a physician.

Arterial hypertension - the initial daily dose is 50-100 mg 1-2 doses (morning and evening). With insufficient therapeutic effect daily dose may be gradually increased to 100-200 mg. Maximum daily dose of 200 mg.

Angina, arrhythmia, prophylaxis of migraine attacks - 100-200 mg / day in two divided doses (morning and evening).

Secondary prevention of myocardial infarction - 200 mg per day in two divided doses (morning and evening).

Functional cardiac abnormalities, accompanied by tachycardia of 100 mg per day in two divided doses (morning and evening).

Upon reaching the therapeutic effect, reduce the dose (under medical supervision). Older patients are recommended to start treatment with 50 mg/day.

Side effects

From the Central nervous system: fatigue, weakness, headache, dizziness, slowing of mental and motor reactions, paresthesia in the extremities (in patients with "intermittent" claudication and Raynaud's syndrome), depression, anxiety, poor concentration, drowsiness, insomnia , "nightmarish" dream, confusion or short-term memory impairment, asthenic syndrome, muscle weakness.

From the sensory organs: rare - reduced vision, reduced secretion of tear fluid, dryness and soreness of the eyes, conjunctivitis, tinnitus, rhinitis.

From the side of cardiovascular system: sinus bradycardia , heartbeat, expressed lower AD, ortostatical gipotenzia (dizziness, sometimes loss of consciousness), rarely - decrease myocardial contractility, temporary aggravation of symptoms of chronic heart failure (edema, swelling of the feet and/or lower legs, shortness of breath), arrhythmia, manifestation of angiospasm (increased peripheral circulatory disorders, cold lower extremities, Raynaud's syndrome). Violation of conductivity of the myocardium, cardialgia.

From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, changes in taste, and in some cases - impaired liver.

With the skin: exacerbation of psoriasis, psoriasiform skin reactions, hyperemia of skin, exanthema, photodermatosis, increased sweating, and reversible alopecia.

The respiratory system: nasal congestion, difficulty of an exhalation (a bronchospasm at appointment in high doses, loss of selectivity and/or in predisposed patients), shortness of breath.

From the endocrine system: hypoglycemia (in patients, receiving insulin ), rarely - hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypothyroid state.

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

Effects on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia.

Allergic reactions: urticaria, pruritus, rash.

Other: back pain or joint pain, like all beta-blockers in isolated cases may cause a slight increase in body mass, reduced libido and/or potency, in a dramatic treatment - syndrome “cancel” (increasing angina attacks, increased blood pressure).

Special instructions

The monitoring of patients, receiving beta-adrenoblokatora includes regular monitoring of heart rate and blood pressure, maintenance of blood glucose in patients with diabetes mellitus (1 once in 4-5 months).

If necessary for patients with diabetes dose of insulin or gipoglikemicakih funds designated inwards to be selected individually.

Should teach the patient methods of calculating heart rate and instruct on the need of medical advice in the heart rate less than 50 beats/min.

When taking dosages above 200 mg per day decreases kardioselektivnost.

In heart failure, treatment with metoprolol begin only after reaching the stage of compensation. Perhaps the increased severity of hypersensitivity reactions (against the background of the burdened allergological anamnesis) and the lack of effect of conventional doses of epinephrine (adrenaline). May increase symptoms of human peripheral blood circulation.

The abolition of the drug are gradually, reducing the dose over 10 days. In a dramatic treatment may arise syndrome "cancel" (increasing angina attacks, increased blood pressure). Special attention to remove the drug should be given to patients with angina.

Angina selected dose of the drug should ensure the heart rate at rest within 55-60 beats/min, under load should not exceed 110 beats/min.

Patients using contact lenses should take into account that the treatment with beta-blockers may decrease the production of tear fluid.

Metoprolol may mask certain clinical signs of hyperthyroidism (eg, tachycardia ). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, because it can reinforce the symptoms.

At diabetes can mask the tachycardia, caused by hypoglycemia. Unlike nonselective beta-blockers hardly enhances insulin-induced hypoglycemia and delay recovery of the concentration of blood glucose to normal levels.

If necessary, the appointment of patients with bronchial asthma as concomitant therapy using beta 2 -agonists, in pheochromocytoma alpha-adrenergic blockers.

If necessary, surgery should alert the anesthesiologist on the therapy (the choice of for General anesthesia with minimal negative inotropic effects), withdrawal of the drug is not recommended.

Drugs, reducing stocks of catecholamines (e.g., reserpine), may enhance the action of beta-adrenoblokatorov, therefore, patients, accepting such combination drugs, should be under constant supervision of a physician to identify excessive blood pressure reduction and bradycardia.

Should conduct special monitoring of patients with depressive disorders taking metoprolol, in the case of the depression caused by the reception beta-adrenoblokatorov, it is recommended to discontinue therapy.

During treatment with metoprolol should wear appropriate clothing, as drug may cause skin Allergy to sunlight.

In elderly patients it is recommended to monitor liver function. The correction mode is required only in the case of elderly patients increasing bradycardia (less 50 beats/min), expressed lower AD (systolic BP below 100 mm Hg. century), atrioventricular blockade , bronchospasm, ventricular arrhythmias, severe violations of liver function, it is sometimes necessary to stop treatment.

Due to the lack of sufficient clinical data medication is not recommended for use in children.

During treatment should refrain from driving vehicles and activities potentially hazardous activities, require high concentration and psychomotor speed reactions, to reduce the consumption of ethanol.

Drug interactions

Not recommended simultaneous application with inhibitors of monoamine oxidase (MAO) because of significant increase gipotenzivnogo actions. The break in treatment between receiving MAO inhibitors and metoprolol should be not less than 14 days.

Simultaneous in/with the introduction of verapamil can trigger cardiac arrest. Co-administration of nifedipine leads to a significant decrease in blood pressure.

Funds for inhalation narcosis (derivatives of hydrocarbons) increase the risk of depression of myocardial function and hypotension.

Beta-agonists, theophylline, cocaine, estrogens (delay sodium), indomethacin and other nonsteroidal anti-inflammatory drugs (sodium retention and blocking prostaglandin synthesis by the kidneys) weaken hypotensive effect.

There is an increased inhibitory action on the Central nervous system - ethanol , summation cardiodepressivne effect with drugs for anesthesia, increased risk of peripheral circulatory disorders with ergot alkaloids.

When co-administered with oral hypoglycemic agents may reduce their effect with the insulin - increasing the risk of hypoglycemia, increased its intensity and elongation, masking some of the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

When combined with antihypertensive drugs, diuretics, nitroglycerin or blockers of slow calcium channels can develop sharp decline in AD (extra caution is needed when combined with prazosinem ), increased severity of the deceleration in heart rate and atrioventricular conduction oppression in the application of metoprolol with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), rezerpinom, clonidine, guanfacine, funds for General anesthesia and cardiac glycosides.

Inductors of microsomal liver enzymes (rifampicin, barbiturates) increase the metabolism of metoprolol, to reduce the concentration of metoprolol in plasma and reduction of the effect.

Inhibitors (zimetidin, oral contraceptives, phenothiazines) - increase the concentration in blood plasma.

Allergens, used for immunotherapy or allergen extracts for skin tests combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis, Radiocontrast iodine-containing substance for the on/in the introduction increases the risk of anaphylactic reactions.

Reduces the clearance of xanthine (except difillina), especially in patients with initially increased clearance of theophylline under the influence of Smoking. Reduces lidocaine clearance, increases the concentration of lidocaine in plasma. Enhance and prolong the antidepoliarizuth miorelaksantov, prolongs the anticoagulant effect of coumarins.

When used together with ethanol increases the risk reduction expressed AD.

Overdose

Symptoms: expressed severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, expressed lower AD, arrhythmia, ventricular arrythmia, bronchospasm, pass out, in acute overdose - cardiogenic shock, loss of consciousness, coma, atrioventricular block (until the development of a complete transverse blockade and heart failure), cardialgia. The first signs of overdosage appear 20 minutes to 2 hours after administration of the drug.

Treatment: gastric lavage and the appointment of absorbent material, symptomatic therapy: when expressed lower AD - the patient should be in Trendelenburg position, if excessive decline in blood pressure, bradycardia and heart failure, in/in, at intervals of 2-5 min, Bata-agonists - up to achieve the desired effect or/in 0.5-2 mg atropine sulfate . In the absence of positive effect - dopamine, dobutamine or norepinephrine (noradrenaline). As a follow-up, the appointment of 1-10 mg of glucagon, setting transvenous intracardiac electrical stimulator. If bronchospasm should be entered in/stimulants beta 1 -adrenergic receptors. In convulsions - slow in/with the introduction of diazepam. Hemodialysis is not effective.

Storage conditions

Keep at temperature not exceeding 30°C in a dry place.

Shelf life

5 years.