Metoprolol tablets 100mg, No. 60

• Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);

• functional disorders of cardiac activity, accompanied by tachycardia;

• IHD: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks;

• heart rhythm disturbances (supraventricular tachycardia; ventricular premature beats);

• hyperthyroidism (complex therapy);

• prevention of migraine attacks.

When taken orally, the average dose is 100 mg / day in 1-2 doses. If necessary, the daily dose is gradually increased to 200 mg. With the on / in the introduction, a single dose - 2-5 mg; in the absence of effect, repeated administration is possible after 5 minutes.

Maximum doses: for oral administration, the daily dose is 400 mg, for intravenous administration, a single dose is 15-20 mg.

Tablets are white or almost white, round, flat-cylindrical, with a risk and with a chamfer, slight marbling is allowed.

1 tab.

metoprolol tartrate 100 mg

Excipients: lactose monohydrate - 186.8 mg, potato starch - 52.8 mg, povidone K25 - 13.2 mg, magnesium stearate - 3.6 mg, colloidal silicon dioxide - 3.6 mg.

• Cardiogenic shock;

• AV block II-III degree (without an artificial pacemaker);

• sinoatrial blockade;

• sick sinus syndrome;

• severe bradycardia (heart rate less than 50 beats / min);

• chronic heart failure in the stage of decompensation;

• Prinzmetal's angina;

• acute myocardial infarction (heart rate less than 45 beats / min, PQ interval more than 0.25 sec, systolic blood pressure less than 100 mm Hg);

• lactation period;

• simultaneous administration of MAO inhibitors; simultaneous intravenous administration of slow calcium channel blockers such as verapamil, diltiazem;

• age 18 years (efficacy and safety have not been established);

• pheochromocytoma (without the simultaneous use of alpha-blockers);

• severe peripheral circulatory disorders;

• severe forms of bronchial asthma and chronic obstructive pulmonary disease;

• hypersensitivity to metoprolol or other components of the drug, other beta-blockers.

pharmachologic effect

Cardioselective beta1-blocker without intrinsic sympathomimetic activity. It has hypotensive, antianginal and antiarrhythmic effects. Reduces the automatism of the sinus node, reduces heart rate, slows down AV conduction, reduces myocardial contractility and excitability, decreases cardiac output, and reduces myocardial oxygen demand. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress. It causes a hypotensive effect, which stabilizes by the end of the 2nd week of course use. With exertional angina, metoprolol reduces the frequency and severity of attacks. Normalizes heart rate with supraventricular tachycardia and atrial fibrillation. In case of myocardial infarction, it helps to limit the zone of ischemia of the heart muscle and reduces the risk of developing fatal arrhythmias,reduces the possibility of recurrence of myocardial infarction. Prevents the development of migraines. When used in moderate therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing ?2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism. When taken for many years, it reduces the concentration of cholesterol in the blood. When used in high doses (more than 100 mg / day), it has a blocking effect on both subtypes of ?-adrenergic receptors.smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism. When taken for many years, it reduces the concentration of cholesterol in the blood. When used in high doses (more than 100 mg / day), it has a blocking effect on both subtypes of ?-adrenergic receptors.smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism. When taken for many years, it reduces the concentration of cholesterol in the blood. When used in high doses (more than 100 mg / day), it has a blocking effect on both subtypes of ?-adrenergic receptors.

Side effect

From the side of the cardiovascular system: often - sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness), postural disorders (very rarely accompanied by fainting); rarely - a decrease in myocardial contractility, the development (aggravation) of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), heart rhythm disturbances, myocardial conduction disturbances, cardialgia, manifestation of angiospasm (increased peripheral circulatory disorders, coldness of the lower extremities, Raynaud's syndrome); very rarely - aggravation of pre-existing AV conduction disorders, gangrene in patients with previous severe peripheral circulatory disorders. From the nervous system: very often - increased fatigue, often - weakness, headache,slowing down the speed of mental and motor reactions; rarely - paresthesia, convulsions, tremors, convulsions, depression, anxiety, decreased attention, drowsiness, insomnia, nightmares, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, impotence / sexual dysfunction, Peyronie's disease; very rarely - amnesia / memory impairment, depression, hallucinations. From the respiratory system: often - nasal congestion; infrequently - bronchospasm when administered in high doses (loss of selectivity in predisposed patients), shortness of breath; rarely - rhinitis. From the digestive system: often - nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea; rarely - dryness of the oral mucosa; very rarely - a change in taste. From the liver and biliary tract:rarely - impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), increased activity of hepatic transaminases. From the side of the organ of vision: rarely - decreased vision, decreased secretion of lacrimal fluid, dryness and soreness of the eyes, conjunctivitis. On the part of the organ of hearing and labyrinthine disorders: rarely - tinnitus, hearing loss. From the endocrine system: rarely - hyperglycemia (in patients with non-insulin dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism. Skin and subcutaneous tissue disorders: infrequently - skin rashes (exacerbation of psoriasis), psoriasis-like skin reactions, skin flushing, exanthema, photodermatosis, increased sweating, reversible alopecia. Allergic reactions: infrequently - urticaria. General reactions: rarely - back or joint pain, weight gain,a decrease in libido and / or potency, with a sharp cessation of treatment - a 'withdrawal' syndrome (increased angina attacks, increased blood pressure). Laboratory findings: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, hyperbilirubinemia.

Application during pregnancy and lactation

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. Metoprolol crosses the placental barrier. In connection with the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory arrest in a newborn, metoprolol should be canceled 48-72 hours before the planned delivery date. After delivery, it is necessary to ensure strict control over the condition of the newborn for 48-72 hours. It is excreted in breast milk. Use during breastfeeding is contraindicated.

Application for violations of liver function

Use with caution in patients with severely impaired liver function.

Application for impaired renal function

Use with caution in patients with severe renal impairment.

Application in children

Contraindicated for use in children and adolescents under the age of 18 years.

Use in elderly patients

In elderly patients, it is recommended to start treatment with a dose of 50 mg / day, because a sharp decrease in blood pressure or increasing bradycardia may be more pronounced.

special instructions

Use with caution in patients with chronic obstructive respiratory diseases, diabetes mellitus (especially with labile course), Raynaud's disease and obliterating diseases of peripheral arteries, pheochromocytoma (should be used in combination with alpha-blockers), severe renal and liver dysfunction. Against the background of treatment with metoprolol, it is possible to reduce the production of tear fluid, which is important for patients using contact lenses. Completion of a long course of treatment with metoprolol should be carried out gradually (at least within 10 days) under the supervision of a physician. The simultaneous use of metoprolol with MAO inhibitors is not recommended. When combined therapy with clonidine, the latter should be discontinued a few days after discontinuation of metoprolol,in order to avoid a hypertensive crisis. With simultaneous use with hypoglycemic agents, correction of their dosage regimen is required. A few days before anesthesia, it is necessary to stop taking metoprolol or choose an anesthesia drug with a minimal negative inotropic effect.

Influence on the ability to drive vehicles and mechanisms

In patients whose activities require increased attention, the question of using metoprolol on an outpatient basis should be resolved only after assessing the patient's individual response.

Drug interactions

With simultaneous use with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of severe arterial hypotension, bradycardia, AV blockade. With simultaneous use with barbiturates, the metabolism of metoprolol is accelerated, which leads to a decrease in its effectiveness. With simultaneous use with hypoglycemic agents, it is possible to enhance the action of hypoglycemic agents. With simultaneous use with NSAIDs, it is possible to reduce the hypotensive effect of metoprolol. With simultaneous use with opioid analgesics, the cardiodepressant effect is mutually enhanced. With simultaneous use with peripheral muscle relaxants, neuromuscular blockade may increase.With simultaneous use with agents for inhalation anesthesia, the risk of inhibition of myocardial function and the development of arterial hypotension increases. With simultaneous use with oral contraceptives, hydralazine, ranitidine, cimetidine, the concentration of metoprolol in the blood plasma increases. With simultaneous use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible. With simultaneous use with verapamil, the Cmax in the blood plasma and the AUC of metoprolol increase. The minute and stroke volume of the heart, pulse rate, arterial hypotension decrease. Perhaps the development of heart failure, dyspnea and sinus blockade. With intravenous administration of verapamil while taking metoprolol, there is a threat of cardiac arrest. With simultaneous use, it is possible to increase bradycardia,caused by digitalis glycosides. With simultaneous use with dextropropoxyphene, the bioavailability of metoprolol increases. With simultaneous use with diazepam, a decrease in clearance and an increase in AUC of diazepam are possible, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions. With simultaneous use with diltiazem, the concentration of metoprolol in the blood plasma increases due to the inhibition of its metabolism under the influence of diltiazem. The effect on the activity of the heart is additively inhibited due to the slowing down of the impulse conduction through the AV node caused by diltiazem. There is a risk of developing severe bradycardia, a significant decrease in stroke and minute volume. With simultaneous use with lidocaine, a violation of the elimination of lidocaine is possible.With simultaneous use with mibefradil in patients with low activity of the isoenzyme CYP2D6, it is possible to increase the concentration of metoprolol in the blood plasma and increase the risk of toxic effects. With simultaneous use with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form of eye drops or as part of antitussives), a slight increase in blood pressure is possible. With simultaneous use with propafenone, the concentration of metoprolol in the blood plasma increases and a toxic effect develops. It is believed that propafenone inhibits the metabolism of metoprolol in the liver, decreasing its clearance and increasing serum concentrations. With simultaneous use with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop.With simultaneous use with rifampicin, the concentration of metoprolol in the blood plasma decreases. Metoprolol may cause a slight decrease in theophylline clearance in patients who smoke. Fluoxetine inhibits the CYP2D6 isoenzyme, this leads to inhibition of the metabolism of metoprolol and its cumulation, which can enhance the cardiodepressant effect and cause bradycardia. A case of lethargy development is described. Fluoxetine and mainly its metabolites are characterized by a prolonged T1 / 2, so the likelihood of drug interactions persists even several days after discontinuation of fluoxetine. There are reports of a decrease in the clearance of metoprolol from the body when used simultaneously with ciprofloxacin. With simultaneous use with ergotamine, it is possible to increase peripheral circulatory disorders.With simultaneous use with estrogens, the antihypertensive effect of metoprolol decreases. With the simultaneous use of metoprolol increases the concentration of ethanol in the blood and lengthens its excretion.