Metoprolol pills 50mg, 30pcs – MPEZ

Composition

1 tablet contains: Active ingredient-metoprolol tartrate 50.0 / 100.0 mg; excipients: microcrystalline cellulose 55.0 / 110.0 mg; corn starch 43.2 / 86.4 mg; croscarmellose sodium; 11.6 / 23.2 mg; copovidone 5.0/10.0 mg; colloidal silicon dioxide 1.9 / 3.8 mg; magnesium stearate 3.3/6.6 mg

Pharmacological action

Pharmacodynamicametoprolol refers to cardioselective blockers of β1-adrenergic receptors. It has a slight membrane-stabilizing effect and does not have internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects. Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the formation of cyclic adenosine monophosphate (cAMP) stimulated by catecholamines from adenosine triphosphate (ATP), reduces the intracellular flow of calcium ions, has a negative chrono -, dromo -, batmo – and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility). The total peripheral resistance at the beginning of the use of β1-blockers (in the first 24 hours after oral use) increases (as a result of a reciprocal increase in the activity of α-adrenergic receptors and elimination of stimulation of β2-adrenergic receptors), which returns to its original value after 1-3 days, and decreases with prolonged use. The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (which is of great importance in patients with initial hypersecretion of renin) and the central nervous system, restoration of sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure (BP) at rest, during physical exertion and stress. The antihypertensive effect develops quickly (systolic blood pressure decreases in 15 minutes, maximum – in 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular use. The antianginal effect is determined by a decrease in the myocardial oxygen demand resulting in a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for myocardial oxygen, especially in patients with chronic heart failure (CHF). The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation – sinus and ectopic pacemakers, and a slowdown in atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node and along additional pathways). With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and hyperthyroidism, it reduces the heart rate or can even lead to the restoration of sinus rhythm. Prevents the development of migraines. When used in medium therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on the organs containing beta-2-adrenergic receptors (pancreas, skeletal muscles and smooth muscles of peripheral arteries, bronchi and uterus), and on carbohydrate metabolism. When used in large doses (more than 100 mg / day), it has a blocking effect on both subtypes of beta-adrenergic receptors. Pharmacokineticsabsorption. When taken orally, metoprolol is almost completely absorbed (about 95%) from the gastrointestinal tract. It undergoes intensive presystemic metabolism, so the systemic bioavailability is about 35%. The maximum concentration in blood plasma is reached in 1.5-2 hours after use. Distribution. The connection with blood proteins is 10%. The volume of distribution is 5.5 l / kg. Penetrates through the blood-brain and placental barriers. It is excreted in breast milk in small amounts. Metabolism. Metoprolol is almost completely metabolized in the liver, mainly with the participation of the CYP2D6 isoenzyme. The half-life of metoprolol is from 3 to 4 hours, but for slow metabolizers it can increase to 7 to 8 hours. The metabolites o-desmethylmethoprolol and a-hydroxymethoprolol have weak beta-blocking activity. Output. It is mainly excreted by the kidneys (about 95%), about 10% is excreted unchanged. It is not excreted during hemodialysis. In patients with cirrhosis of the liver and portocaval anastomosis, bioavailability increases and clearance decreases. In patients with portocaval anastomosis, AUC (area under the concentration-time curve) it can increase by 6 times, and the clearance can decrease to 0.3 ml/min.

Indications

• Arterial hypertension (monotherapy or in combination with other antihypertensive agents);
• functional disorders of cardiac activity, accompanied by tachycardia;
• ischemic heart disease: myocardial infarction (secondary prevention – complex therapy), prevention of angina;
• arrhythmias of the heart (supraventricular tachycardia; ventricular extrasystoles);
• hyperthyroidism (complex therapy);
• prevention of migraine attacks.

Contraindications

• Hypersensitivity to metoprolol, or other components of the drug, β-blockers
• for chronic heart failure in the stage of decompensation;
• cardiogenic shock;
• the syndrome of weakness of the sinus node;
• sinoatrial block;
• atrioventricular block degree II-III (without an artificial pacemaker);
• severe bradycardia (heart rate less than 50 beats/min);
• severe forms of asthma and chronic obstructive pulmonary disease;
• metabolic acidosis;
• severe peripheral circulatory disorders;
• Prinzmetal’s angina;
• hypotension (in case of use in the secondary prevention of myocardial infarction, systolic blood pressure less than 100 mm Hg. St. )
• acute myocardial infarction (heart rate less than 45 beats/min, the interval PQ more of 0.24 seconds. or systolic blood pressure less than 100 mm Hg. St. ) patients receiving prolonged or intermittent inotropic therapy means and acting on β-adrenergic receptors,
• chronic obstructive pulmonary disease in the acute stage; pheochromocytoma (without the simultaneous use of α-blockers);
• breastfeeding;
• age to 18 years (efficacy and safety not established);
• simultaneous reception of monoamine oxidase inhibitors (MAOIS);
• simultaneous intravenous blocker of “slow” calcium channels (bmkk) type of verapamil (see section “Interaction with other medicines”).

With caution

Diabetes mellitus, metabolic acidosis, impaired liver and kidney function (creatinine clearance less than 40 ml/min), myasthenia gravis, grade I atrioventricular block, thyrotoxicosis, depression (including in the anamnesis), psoriasis, a burdened allergic history (possibly increased sensitivity to allergens, increased arterial hypertension and reduced therapeutic response to epinephrine), bronchial asthma, chronic obstructive pulmonary disease, peripheral circulatory disorders (intermittent claudication, Raynaud’s syndrome), old age.

Side effects

the incidence of side effects is classified according to the recommendations of the world health organization: very often – not less-10%; often – not less than 1% but < 10%; infrequently – no more than 0.1% but < 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely – less than 0.01%. From the blood and lymphatic system: very rarely – thrombocytopenia, leukopenia. From the immune system: rarely – anaphylactic reaction. From the endocrine system: rarely-hypo -, hyperglycemia in patients with type I diabetes mellitus, masking the symptoms of thyrotoxicosis. From the side of metabolism and nutrition: infrequently-an increase in body weight; rarely-an aggravation of the course of latent diabetes mellitus. From the central nervous system: often – fatigue, headache, dizziness; infrequently – asthenic syndrome, slowing down the speed of mental and motor reactions, paresthesia, anxiety, nervousness, cramps in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), depression, anxiety, decreased attention, drowsiness, sleep disorders, “nightmare” dreams, more frequent and/or brighter dreams, confusion, muscle weakness; very rarely – emotional lability, short-term memory impairment. From the side of the organ of vision: rarely-conjunctivitis, decreased secretion of lacrimal fluid, decreased vision. From the side of the organ of hearing and labyrinth disorders: rarely-hearing impairment and tinnitus.From the cardiovascular system: often-“palpitation sensation”, bradycardia, orthostatic hypotension (dizziness, loss of consciousness), cold of the lower extremities; infrequently – atrioventricular block of the first degree, pericardial pain; rarely – marked decrease in blood pressure, violation of atrioventricular conduction or aggravation of heart failure with peripheral edema and/or shortness of breath during exercise, increased complaints in patients suffering from peripheral vision disorders. circulatory disorders (including patients with Raynaud’s syndrome). Very rarely-in patients with angina pectoris, increased seizures are possible. Respiratory, thoracic and mediastinal disorders: often – shortness of breath in patients with a predisposition to bronchospasm; infrequently – nasal congestion, difficulty exhaling (bronchospasm when administered in high doses-loss of selectivity and/or in predisposed patients); rarely-allergic rhinitis. From the gastrointestinal tract: often – nausea, vomiting, abdominal pain, diarrhea, constipation; infrequently-dryness of the oral mucosa; rarely-impaired taste sensations. From the liver and biliary tract: rarely-increased activity of “hepatic” transaminases; very rarely-hepatitis. From the skin and subcutaneous tissues: infrequently-skin hyperemia, pruritus, increased sweating; rarely-alopecia; very rarely-photosensitization reaction, – psoriasis skin reaction. Musculoskeletal and connective tissue disorders: infrequently-muscle spasm; very rarely – arthralgia, muscle weakness. From the genitals and breast: rarely-decreased libido and potency, Peyronie’s disease. Laboratory parameters: very rarely – a decrease in cholesterol. high-density lipoproteins and increased plasma triglycerides.

Interaction

Concomitant use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect. The treatment interval between taking MAO inhibitors and metoprolol should be at least 14 days. beta-adrenostimulants, theophylline, cocaine, glucocorticoids, estrogens (sodium ion retention), Indometacin and other nonsteroidal anti-inflammatory drugs (sodium ion retention and blocking of prostaglandin synthesis by the kidneys) weaken the antihypertensive effect of metoprolol. When taken together with hypoglycemic agents for oral use, their effect may decrease; with insulin, it may increase the risk of hypoglycemia, increase its severity and duration, and mask some symptoms of hypoglycemia (tachycardia, increased sweating, increased blood pressure). When combined with antihypertensive agents, diuretics, angiotensin-converting enzyme inhibitors, nitroglycerin or slow calcium channel blockers, it can lead to a significant decrease in blood pressure (special caution is necessary when combined with prazosin); the risk of bradycardia increases when combined with mefloquine; a pronounced decrease in blood pressure and bradycardia when combined with epinephrine; a pronounced decrease in heart rate and inhibition of AV conduction up to complete blockade – when used metoprolol with verapamil, diltiazem, reserpine, methyldopa, clonidine, guanfacine and cardiac glycosides, general anesthesia agents (along with cardiodepressive and antihypertensive effects). Drugs that induce or inhibit CYP2D6 may affect the level of metoprolol in plasma. Plasma concentrations of metoprolol may increase when co-administered with other drugs that are a substrate for CYP2D6, such as antiarrhythmics, antihistamines, H2 receptor antagonists, antidepressants (selective serotonin reuptake inhibitors such as paroxetine, fluoxetine, sertraline), neuroleptics, and cyclooxygenase-2 inhibitors. Class I antiarrhythmic drugs can lead to the summation of a negative inotropic effect with the development of pronounced hemodynamic side effects in patients with impaired left ventricular function (this combination should be avoided in patients with sinus node weakness syndrome and impaired renal function). atrioventricular conduction band). Quinidine inhibits the metabolism of-metoprolol in fast metabolizers, leading to a significant increase in the concentration of metoprolol in plasma and an increase in its beta-blocking effect. Combination with amiodarone increases the risk of severe sinus bradycardia (including after a long time after the withdrawal of amiodarone, due to its long half-life). If metoprolol and clonidine are taken simultaneously, then when metoprolol is discontinued, clonidine is canceled after a few days (due to the risk of “withdrawal”syndrome). Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in metoprolol metabolism, a decrease in the concentration of metoprolol in blood plasma and a decrease in the effect. Inhibitors (cimetidine, oral contraceptives, phenothiazines) – increase the concentration of metoprolol in blood plasma. Diphenhydramine reduces the clearance of metoprolol, increasing its effect. Co-use with high doses of phenylpropanolamine can lead to a paradoxical increase in blood pressure (up to a hypertensive crisis). Allergens used for immunotherapy or allergen extracts for skin tests when combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiopaque agents for intravenous use increase the risk of anaphylactic reactions. Reduces the clearance of xanthine (except diphylline), especially with initially increased clearance of theophylline under the influence of smoking. Reduces the clearance of lidocaine, increases the concentration of lidocaine in blood plasma. Enhances and prolongs the action of antidepolarizing muscle relaxants; prolongs the anticoagulant effect of coumarins. When combined with anxiolytics and drugs with hypnotic activity, the antihypertensive effect is enhanced, with ethanol-the risk of a pronounced decrease in blood pressure increases and the depressing effect on the central nervous system increases. There is an increased risk of peripheral circulatory disorders with ergot alkaloids. When used concomitantly with aldesleukin, the risk of a pronounced and sharp decrease in blood pressure increases. With simultaneous use, the effectiveness of alprostadil decreases.

How to take, course of use and dosage

The drug Metoprolol should be taken orally, during or immediately after a meal, tablets can be divided in half (but not chewed) and washed down with liquid.

With arterial hypertension, the initial dose is 50-100 mg 1-2 times a day (morning and evening), with insufficient therapeutic effect, the daily dose can be increased to 100-200 mg or other antihypertensive agents are additionally used, the maximum daily dose is 200 mg.

For arrhythmia, for the prevention of angina attacks and migraines-100-200 mg 1-2 times a day (morning and evening).

Secondary prevention of myocardial infarction-200 mg per day, divided into 2 doses (morning and evening).

In case of functional disorders of cardiac activity, accompanied by tachycardia-100 mg per day in 2 doses (morning and evening).

With hyperthyroidism-150-200 mg per day in 3-4 doses (morning and evening). Elderly patients are recommended to start treatment with 50 mg per day. Renal failure does not require dose adjustment.

In case of hepatic insufficiency, dose adjustment may be required depending on the clinical condition. If there is a need to interrupt or discontinue treatment with Metoprolol after prolonged therapy, the dose of the drug should be gradually reduced by 2 times for at least 2 weeks.

If withdrawal symptoms occur, reduce the dose gradually. Abrupt discontinuation of the drug may cause myocardial ischemia and may lead to an exacerbation of angina or myocardial infarction, as well as increase arterial hypertension.

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, syncope, with acute overdose – cardiogenic shock, loss of consciousness, coma, atrioventricular block, (up to the development of complete transverse block and cardiac arrest), angina pectoris, hypoglycemia, hyperkalemia, convulsions, respiratory arrest. The first signs of overdose appear in 20 minutes-2 hours after taking the drug. Treatment with Metoprolol-Teva should be stopped immediately in case of overdose or a threatening decrease in heart rate and / or blood pressure. Treatment: gastric lavage and use of adsorbents; symptomatic therapy: with a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position; in case of excessive decrease in blood pressure, bradycardia and heart failure – intravenously (IV) with an interval of 2-5 minutes, beta-adrenomimetics-until the desired effect is achieved or iv 0.5-2 mg of atropine. In the absence of a positive effect – dopamine, dobutamine or norepinephrine (norepinephrine). In case of bronchospasm, intravenous beta-2-adrenomimetics should be administered. For convulsions-slow intravenous use of diazepam. Hemodialysis is ineffective.

Special instructions

Beta-blockers may increase sensitivity to allergens and the severity of anaphylactic reactions, so patients with a history of severe hypersensitivity reactions and patients undergoing desensitizing therapy are at risk of developing severe anaphylactic reactions. In severe renal impairment, deterioration of renal function has been reported in some cases with treatment with beta-blockers. In such cases, the use of Metoprolol-Teva should be accompanied by appropriate monitoring of renal function.Monitoring of patients taking beta-blockers includes regular monitoring of heart rate and blood pressure, blood glucose concentration in patients with diabetes mellitus (1 time in 4-5 months). If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed by mouth should be selected individually. The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. When taking a dose higher than 100 mg per day, cardioselectivity decreases. In patients with heart failure, treatment with Metoprolol-Teva is started only after reaching the compensation stage. Abrupt discontinuation of the drug should be avoided. Discontinuation of the drug should be carried out gradually, over 2 weeks. The dose is reduced gradually, in several doses, until the final dose is reached-25 mg once a day. If surgery is necessary, the surgeon/anesthesiologist should be advised about the therapy being performed in order to select a general anesthesia agent with minimal negative inotropic effects, but discontinuation of the drug before surgery is not recommended. Reciprocal activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg). It may increase the symptoms of peripheral arterial circulation disorders. In case of stress angina, the selected dose of the drug should provide a heart rate at rest in the range of 55-60 beats / min, with a load-no more than 110 beats / min. Patients using contact lenses should take into account that during treatment with beta-blockers, tear fluid production may decrease. Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non – selective beta-blockers, metoprolol significantly less affects insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels. If it is necessary to prescribe Metoprolol-Teva to patients with bronchial asthma, beta-2-adrenomimetics are used as concomitant therapy; in pheochromocytoma, alpha – blockers are used. Drugs that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for excessive blood pressure reduction and bradycardia. It is recommended to stop therapy if skin rashes occur due to taking beta-blockers. In elderly patients, regular monitoring of liver function is recommended. Correction of the dosage regimen is required only if an elderly patient develops increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver function disorders, and sometimes it is necessary to stop treatment. Special monitoring should be given to patients with depressive disorders taking metoprolol; in case of depression caused by taking beta-blockers, therapy should be discontinued. When taking the drug Metoprolol-Teva, you should refrain from taking alcohol. In smokers, the effectiveness of beta-blockers is lower. Effects on the ability to drive vehicles and mechanisms During treatment, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25°C. Keep out of reach of children!

Shelf

life is 5 years.

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Angina, Arrhythmia, Hypertension