Metoprolol

General characteristics. Structure:

Active agent: a metoprolola tartrate - 50 mg.

Excipients: silicon dioxide colloid anhydrous; MKTs; sodium carboxymethylstarch (type A); magnesium stearate.

Cover:: gipromelloza; polysorbate 80; talc; titanium E 171 dioxide in the tab. on 50 mg (in addition): dye crimson (Ponso 4R).

Description. Tablets of white color, ploskotsilindrichesky, with a facet and risky.

Pharmacological properties:

Pharmacological action - antiarrhytmic, hypotensive, anti-anginal.

Indications to use:

— arterial hypertension (as monotherapy or in a combination with other anti-hypertensive means), including hyperkinetic type, tachycardia;

— coronary heart disease: a myocardial infarction (secondary prevention - complex therapy), prevention of attacks of stenocardia;

— disturbances of a heart rhythm (supraventricular tachycardia, ventricular premature ventricular contraction);

— hyperthyroidism (complex therapy);

— prevention of attacks of migraine.

Route of administration and doses:

Inside, with food or right after food, without chewing and washing down with liquid.

Arterial hypertension: the initial daily dose makes 50–100 mg in 1–2 receptions (in the morning and in the evening). At insufficient therapeutic effect the daily dose can be gradually raised to 100–200 mg and/or other anti-hypertensive means are in addition appointed.

The maximum daily dose — 200 mg.

Stenocardia, arrhythmias, prevention of attacks of migraine: 100–200 mg a day in two steps (in the morning and in the evening).

Secondary prevention of a myocardial infarction: 200 mg a day in two steps (in the morning and in the evening).

The functional disturbances of cordial activity which are followed by tachycardia: 100 mg a day in two steps (in the morning and in the evening).

At elderly patients, at renal failures, and also in need of carrying out a hemodialysis the dose is not changed.

At abnormal liver functions the dose of drug should be lowered depending on a clinical state.

Features of use:

Control of the patients accepting beta adrenoblockers includes regular observation of ChSS and the ABP, content of glucose of blood at patients with a diabetes mellitus. If necessary, for patients with a diabetes mellitus, the dose of insulin or the hypoglycemic means appointed inside should be picked up individually.

It is necessary to train the patient in a technique of calculation of ChSS and to instruct about need of medical consultation at ChSS less than 50 beats/min. At reception of a dose higher than 200 mg/days decrease cardioselectivity.

At heart failure treatment metoprololy is begun only after achievement of a stage of compensation.

Strengthening of expressiveness of hypersensitivity reactions (against the background of the burdened allergological anamnesis) and lack of effect of introduction of usual doses of Epinephrinum (adrenaline) is possible.

Can strengthen symptoms of disturbance of peripheric arterial circulation. Drug withdrawal is carried out gradually, reducing a dose within 10 days.

At the sharp termination of treatment there can be a withdrawal (strengthening of attacks of stenocardia, increase in the ABP).

Special attention at drug withdrawal needs to be paid to patients with stenocardia. At an angina of exertion the picked-up dose of drug has to provide ChSS at rest within 55-60 beats/min, at loading - no more than 110 beats/min.

The patients using contact lenses have to consider that against the background of treatment by beta adrenoblockers reduction of products of the lacrimal liquid is possible.

Metoprolol can mask some clinical manifestations of a hyperthyroidism (for example, tachycardia). Sharp cancellation at patients with a thyrotoxicosis is contraindicated as it is capable to strengthen symptomatology.

At a diabetes mellitus can mask the tachycardia caused by a hypoglycemia. Unlike nesslektivny beta adrenoblockers practically does not strengthen the glycemia caused by insulin and recovery of concentration of glucose of blood to normal level does not detain.

In need of appointment to patients with bronchial asthma, as the accompanying therapy use beta2-adrenostimulyator; at a pheochromocytoma - alpha adrenoblockers.

In need of carrying out surgical intervention it is necessary to warn the anesthesiologist about the carried-out therapy (the choice of means for the general anesthesia with the minimum negative inotropic effect), drug withdrawal is not recommended.

The drugs reducing stocks of catecholamines (for example, Reserpinum), can strengthen effect of beta adrenoblockers therefore the patients accepting such combinations of drugs have to be under constant observation of the doctor regarding detection of an excessive lowering of arterial pressure and bradycardia. At elderly patients - it is recommended to exercise control of function of a liver regularly. Correction of the mode of dosing is required only in case of emergence in sick advanced age of the accruing bradycardia (less than 50 уд. / mines), the expressed decrease in the ABP (systolic arterial pressure is lower than 100 mm of mercury.), AV blockade, a bronchospasm, ventricular arrhythmias, heavy abnormal liver functions, sometimes it is necessary to stop treatment.

Patients with a heavy renal failure are recommended to exercise control of function of kidneys.

It is necessary to carry out special control of a condition of patients with the depressive frustration accepting метопролол; in case of development of the depression caused by reception of beta adrenoblockers it is recommended to stop therapy.

Due to the lack of enough clinical data drug is not recommended to be used at children.

Influence on ability to driving of motor transport and to control of mechanisms

In an initiation of treatment metoprololy patients can test dizziness, fatigue. In this case they have to refrain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. Further definition of safety of a dose is carried out individually.

Side effects:

Side effects depend on individual sensitivity of the patient. Usually they insignificant also disappear after drug withdrawal.

From a nervous system: increased fatigue, weakness, headache, delay of speed of mental and motor reactions; seldom - paresthesias in extremities (at patients with the alternating lameness and Reynaud's syndrome), a depression, concern, decrease in attention, drowsiness, sleeplessness, dreadful dreams, confusion of consciousness or short-term disturbance of memory, muscular weakness.

From sense bodys: seldom - decrease in sight, decrease in secretion of the lacrimal liquid, dryness and morbidity of eyes, conjunctivitis, a sonitus.

From cardiovascular system: sinus bradycardia, heartbeat, decrease in the ABP, orthostatic hypotension, dizziness, sometimes loss of consciousness); seldom - decrease in contractility of a myocardium, temporary aggravation of symptoms of chronic heart failure (hypostases, puffiness of feet and/or the lower part of shins, an asthma), arrhythmias, manifestation of a vasomotor spasm (strengthening of disturbance of peripheric circulation, a cold snap of the lower extremities, Reynaud's syndrome), disturbance of conductivity of a myocardium, a cardialgia.

From the alimentary system: nausea, vomiting, an abdominal pain, dryness in a mouth, diarrhea, a lock, an abnormal liver function, taste change.

From integuments: urticaria, skin itch, rash, exacerbation of psoriasis, psoriazopodobny skin reactions, dermahemia, dieback, photodermatosis, sweating strengthening, reversible alopecia.

From respiratory system: a nose congestion, difficulty of an exhalation (a bronchospasm at appointment in high doses - loss of selectivity and/or at predisposed patients), an asthma.

From endocrine system: a hypoglycemia (at the patients receiving insulin), it is rare: a hyperglycemia (at patients with a diabetes mellitus), a hypothyroidism.

Laboratory indicators: seldom - thrombocytopenia (unusual bleedings and hemorrhages), an agranulocytosis, a leukopenia, increase in activity of liver enzymes; extremely seldom - a hyperbilirubinemia.

Influence on a fruit: the pre-natal growth inhibition, a hypoglycemia, bradycardia is possible.

Others: the dorsodynia or joints, as well as all beta adrenoblockers in isolated cases can cause insignificant increase in body weight, decrease in a libido and/or potentiality.

Interaction with other medicines:

Simultaneous use with MAO inhibitors owing to considerable strengthening of hypotensive action is not recommended. Having rummaged in treatment between reception of MAO inhibitors and a metoprolola has to make not less than 14 days.

Simultaneous in/in administration of verapamil can provoke a cardiac standstill.

Co-administration of nifedipine leads to considerable decrease in the ABP.

Means for an inhalation anesthesia (derivatives of hydrocarbons) increase risk of oppression of function of a myocardium and development of arterial hypotension.

Beta адреностимуляторы, theophylline, cocaine, etrogena (a sodium delay), indometacin and other NPVP (a delay of sodium and blocking of synthesis of prostaglandin kidneys) weaken hypotensive effect.

Rub - and tetracyclic antidepressants, antipsychotic medicines (neuroleptics), sedative and somnolent medicines strengthen oppression of TsNS.

Strengthening of the oppressing action on TsNS - with ethanol is noted; summation of cardiodepressive effect - with narcotic means; increase in risk of disturbances of peripheric circulation - with ergot alkaloids.

At joint reception with hypoglycemic means for intake decrease in their effect is possible; with insulin - increase in risk of development of a hypoglycemia, strengthening of its expressiveness and lengthening, masking of some symptoms of a hypoglycemia (tachycardia, perspiration, increase in the ABP).

At a combination to antihypertensives, diuretics, nitroglycerine or blockers of slow calcium channels sharp decrease in the ABP can develop) extra care is necessary at a combination to Prazozinum); increase in expressiveness of an urezheniye of ChSS and oppression of AV conductivity - at use of a metoprolol with verapamil, diltiazem, antiarrhytmic means (Amiodaronum), Reserpinum, finish singing alpha methyl, a clonidine, guanfatsiny, means for the general anesthesia and cardiac glycosides.

If метопролол and the clonidine is accepted at the same time, then at cancellation of a metoprolol the clonidine is cancelled in several days (in connection with risk of emergence of a withdrawal).

Inductors of microsomal enzymes of a liver (rifampicin, barbiturates) lead to strengthening of metabolism of a metoprolol, to decrease in concentration of a metoprolol in a blood plasma and to reduction of effect.

Inhibitors (Cimetidinum, oral contraceptives, fenotiazina) increase concentration of a metoprolol in plasma.

The allergens used for an immunotherapy or extracts of allergens for skin tests at combined use with metoprololy increase risk of emergence of system allergic reactions or an anaphylaxis; iodinated radiopaque substances for in/in introductions increase risk of development of anaphylactic reactions.

Reduces clearance of xanthine (except Diphyllinum), especially with initially increased clearance of theophylline under the influence of smoking.

Reduces clearance of lidocaine, increases concentration of lidocaine in a blood plasma.

Strengthens and prolongs action of the anti-depolarizing muscle relaxants; extends anticoagulating effect of coumarins.

At combined use with ethanol the risk of the expressed decrease in the ABP increases.

Contraindications:

— cardiogenic shock;

— AV blockade of the II-III degree;

— sinuatrial (SA) blockade;

— sick sinus syndrome;

— the expressed bradycardia;

— heart failure in a decompensation stage;

— Printsmetal's stenocardia;

— arterial hypotension (in case of use at secondary prevention of a myocardial infarction - systolic the ABP less than 100 mm hg, ChSS less than 45 уд. / mines);

— a concomitant use of MAO inhibitors or simultaneous in/in administration of verapamil;

— lactation period;

— age up to 18 years (efficiency and safety are not established);

— hypersensitivity to a metoprolol or other components of drug, other beta adrenoblockers.

With care - a diabetes mellitus, a metabolic acidosis, bronchial asthma, a chronic obstructive pulmonary disease (emphysema of lungs, chronic obstructive bronchitis), obliterating diseases of peripheral vessels (the alternating lameness, Reynaud's syndrome), a chronic liver and/or renal failure, a myasthenia, a pheochromocytoma, AV blockade of the I degree, a thyrotoxicosis, a depression (including in the anamnesis), psoriasis, pregnancy, advanced age.

Overdose:

Symptoms: the expressed heavy sinus bradycardia, dizziness, nausea, vomiting, cyanosis, the expressed decrease in the ABP, arrhythmia, a ventricular ekstasistoliya, a bronchospasm, a syncope, at acute overdose - cardiogenic shock, a loss of consciousness, a coma, antrioventrikulyarny blockade (up to development of total cross block and a cardiac standstill), a cardialgia.

The first signs of overdose are shown in 20 min. - the 2nd hour after administration of drug.

Treatment: a gastric lavage and purpose of the adsorbing means; symptomatic therapy: at the expressed decrease in the ABP - the patient has to be in the provision of Trendelenburga; in case of excessive decrease in the ABP, bradycardia and heart failure - in/in, at an interval of 2-5 min., beta адреностимуляторы - before achievement of desirable effect or in/in 0.5-2 mg of Atropini sulfas.

In the absence of positive effect - a dopamine, Dobutaminum or Norepinephrinum (noradrenaline).

As the subsequent measures, perhaps, purpose of 1-10 mg of a glucagon, statement of a transvenous intrakardialny electrostimulator. At a bronchospasm it is necessary to enter into stimulators of beta2-adrenoceptors. Metoprolol is badly brought by means of a hemodialysis.

Storage conditions:

To store in in the unavailable to children, dry, protected from light place, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

10 pieces - blisters (3) - packs cardboard.

14 pieces - blisters (2) - packs cardboard.

14 pieces - blisters (4) - packs cardboard.