Metoprolol tablets p / o prolonged action 100mg, No. 30

• Arterial hypertension,

• prevention of angina attacks,

• heart rhythm disturbances (supraventricular tachycardia, extrasystole),

• secondary prevention after myocardial infarction,

• hyperkinetic cardiac syndrome (including hyperthyroidism, NCD).

• Prevention of migraine attacks.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

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.

Sustained-release tablets, film-coated white or almost white, round, biconvex; in cross section, the core is white or almost white.

1 tab.

Active ingredient: metoprolol tartrate - 25 mg, which corresponds to the content of metoprolol succinate - 23.83 mg

Excipients: hypromellose - 48 mg, pregelatinized corn starch - 42.97 mg, ethyl cellulose - 32 mg, glycerol dibehenate (glyceryl behenate) - 8 mg, povidone K30 - 2 mg, colloidal silicon dioxide - 1.6 mg, magnesium stearate - 1.6 mg.

Film casing No. 1: aqueous dispersion of ethyl cellulose for film coating, containing ethyl cellulose -18.8%, ammonia solution - 28% (4.4%), medium-chain triglycerides (4%), oleic acid (2.2%), calculated on dry matter - 6.4 mg ...

Film casing No. 2: (hypromellose - 2.88 mg, talc - 0.96 mg, titanium dioxide - 0.528 mg, macrogol 4000 - 0.432 mg) or (dry mixture for film coating containing (hypromellose - 60%, talc - 20%, titanium dioxide - 11%, macrogol 4000 - 9%)) - 4.8 mg.

• Hypersensitivity to metoprolol or other beta-blockers;

• AV block II and III degree (without pacemaker);

• heart failure in the stage of decompensation;

• patients receiving long-term or intermittent therapy with inotropic agents and agents acting on ?-adrenergic receptors;

• clinically significant sinus bradycardia;

• SSSU;

• cardiogenic shock;

• severe peripheral circulatory disorders, incl. with the threat of gangrene;

• arterial hypotension (systolic blood pressure less than 100 mm Hg. Art.);

• patients with acute myocardial infarction (heart rate less than 45 beats / min, PQ interval duration more than 0.24 sec or systolic blood pressure less than 100 mm Hg);

• for the treatment of supraventricular tachycardia with systolic blood pressure less than 110 mm Hg;

• intravenous administration of calcium channel blockers such as verapamil and diltiazem;

• simultaneous administration of MAO inhibitors;

• severe forms of bronchial asthma and COPD;

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

• breastfeeding period;

• children under 18 years of age.

Carefully

AV block I degree; Prinzmetal's angina; COPD and mild bronchial asthma; diabetes; severe renal failure.

Clinical and pharmacological group: Beta1-blocker

Pharmaco-therapeutic group: Selective beta1-blocker

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.

Pharmacokinetics

After oral administration, metoprolol is rapidly and almost completely absorbed from the gastrointestinal tract, Cmax of the active substance in the blood plasma is reached after 1-2 hours. After absorption, metoprolol is largely subjected to the effect of the 'first pass' through the liver. Plasma protein binding is low, about 5-10%. Vd is 5.6 l / kg. It is quickly distributed in tissues, penetrates the BBB, the placental barrier. Excreted in breast milk. Metoprolol undergoes oxidative metabolism in the liver (mainly with the participation of the isoenzyme CYP2D6) with the formation of 3 main metabolites, none of which has a clinically significant beta-adrenergic blocking effect. T1 / 2 of metoprolol from plasma is 3-4 hours and does not change during the course of treatment. More than 95% of the dose taken is excreted by the kidneys, about 5% of the dose taken is excreted by the kidneys unchanged.

Indications

• Arterial hypertension,

• prevention of angina attacks,

• heart rhythm disturbances (supraventricular tachycardia, extrasystole),

• secondary prevention after myocardial infarction,

• hyperkinetic cardiac syndrome (including hyperthyroidism, NCD).

• Prevention of migraine attacks.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

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.

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 of 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, decreased libido and / or potency, with abrupt cessation of treatment - 'withdrawal' syndrome (increased angina attacks, increased blood pressure).

Laboratory findings: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, hyperbilirubinemia.

Contraindications for use

• Hypersensitivity to metoprolol or other beta-blockers;

• AV block II and III degree (without pacemaker);

• heart failure in the stage of decompensation;

• patients receiving long-term or intermittent therapy with inotropic agents and agents acting on ?-adrenergic receptors;

• clinically significant sinus bradycardia;

• SSSU;

• cardiogenic shock;

• severe peripheral circulatory disorders, incl. with the threat of gangrene;

• arterial hypotension (systolic blood pressure less than 100 mm Hg. Art.);

• patients with acute myocardial infarction (heart rate less than 45 beats / min, PQ interval duration more than 0.24 sec or systolic blood pressure less than 100 mm Hg);

• for the treatment of supraventricular tachycardia with systolic blood pressure less than 110 mm Hg;

• intravenous administration of calcium channel blockers such as verapamil and diltiazem;

• simultaneous administration of MAO inhibitors;

• severe forms of bronchial asthma and COPD;

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

• breastfeeding period;

• children under 18 years of age.

Carefully

AV block I degree; Prinzmetal's angina; COPD and mild bronchial asthma; diabetes; severe renal failure.

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 monitoring of the condition of the newborn for 48-72 hours.

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 peripheral arterial diseases, 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.

ѕри в/в введении верапамила на фоне приема метопролола существует угроза остановки сердца.

ѕри одновременном применении возможно усиление брадикардии, вызванной гликозидами наперст¤нки.

ѕри одновременном применении с декстропропоксифеном повышаетс¤ биодоступность метопролола.

ѕри одновременном применении с диазепамом возможно снижение клиренса и увеличение јUC диазепама, что может привести к усилению его эффектов и уменьшению скорости психомоторных реакций.

ѕри одновременном применении с дилтиаземом повышаетс¤ концентраци¤ метопролола в плазме крови вследствие ингибировани¤ его метаболизма под вли¤нием дилтиазема. јддитивно угнетаетс¤ вли¤ние на де¤тельность сердца в св¤зи с замедлением проведени¤ импульса через AV-узел, вызываемым дилтиаземом. ¬озникает риск развити¤ выраженной брадикардии, значительного уменьшени¤ ударного и минутного объема.

ѕри одновременном применении с лидокаином возможно нарушение выведени¤ лидокаина.

ѕри одновременном применении с мибефрадилом у пациентов с низкой активностью изофермента CYP2D6 возможно повышение концентрации метопролола в плазме крови и увеличение риска развити¤ токсических эффектов.

ѕри одновременном применении с норэпинефрином, эпинефрином, другими адрено- и симпатомиметиками (в т.ч. в форме глазных капель или в составе противокашлевых средств) возможно некоторое повышение ј?.

ѕри одновременном применении с пропафеноном повышаетс¤ концентраци¤ метопролола в плазме крови и развиваетс¤ токсическое действие. ѕолагают, что пропафенон ингибирует метаболизм метопролола в печени, уменьша¤ его клиренс и повыша¤ сывороточные концентрации.

ѕри одновременном применении с резерпином, гуанфацином, метилдопой, клонидином возможно развитие выраженной брадикардии.

ѕри одновременном применении с рифампицином уменьшаетс¤ концентраци¤ метопролола в плазме крови.

ћетопролол может вызвать небольшое уменьшение клиренса теофиллина у кур¤щих пациентов.

‘луоксетин ингибирует изофермент CYP2D6, это приводит к угнетению метаболизма метопролола и его кумул¤ции, что может усиливать кардиодепрессивное действие и вызывать брадикардию. ќписан случай развити¤ летаргии.

‘луоксетин и главным образом его метаболиты характеризуютс¤ длительным T1/2, поэтому веро¤тность лекарственного взаимодействи¤ сохран¤етс¤ даже через несколько дней после отмены флуоксетина.

»меютс¤ сообщени¤ об уменьшении клиренса метопролола из организма при одновременном применении с ципрофлоксацином.

ѕри одновременном применении с эрготамином возможно усиление нарушений периферического кровообращени¤.

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 prolongs its elimination.

Storage conditions:

Store in a dark place at a temperature not exceeding 25 ? C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Vacation conditions

On prescription

Manufacturer

Joint Stock Company 'VERTEX' (JSC 'VERTEX'), St. Petersburg, Road to Kamenka, 62, lit. A, Russia

Marketing Authorization Holder / Organization Receiving Consumer Claims:

JSC 'VERTEX'