Composition
>
of 1 tab. contains:
Active ingredients:
metoprolol 100 mg
Auxiliary substances: Â
lactose monohydrate 180 mg,
microcrystalline cellulose 72 mg,
potato starch 12 mg,
sodium carboxymethyl starch 16 mg,
povidone 16 mg,
magnesium stearate 4 mg
Pharmacological action
 Cardioselective beta-1-adrenoblocker without internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects. Reduces the automatism of the sinus node, reduces heart rate, slows down AV conduction, reduces contractility and excitability of the myocardium, reduces the minute volume of the heart, reduces the need for oxygen in the myocardium.
Suppresses the stimulating effect of catecholamines on the heart during physical and psychoemotional stress.
Causes a hypotensive effect, which stabilizes by the end of the 2nd week of the course application. For angina pectoris, metoprolol reduces the frequency and severity of seizures. Normalizes the heart rate in supraventricular tachycardia and atrial fibrillation.
In case of myocardial infarction, it helps to limit the area of ischemia of the heart muscle and reduces the risk of fatal arrhythmias, reduces the possibility of relapses of myocardial infarction. When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.
Indications
Arterial hypertension (monotherapy or in combination with other antihypertensive agents), IHD, functional cardiac disorders accompanied by tachycardia, myocardial infarction, prevention of angina attacks, cardiac arrhythmia, hyperthyroidism (complex therapy), prevention of migraine attacks.
Contraindications
Hypersensitivity, cardiogenic shock, grade II and III AV block, sinoatrial block, chronic (decompensated) heart failure, sinus node weakness syndrome, severe sinus bradycardia (heart rate less than 60 beats / min), Prinzmetal angina, acute myocardial infarction (heart rate less than 45 beats / min, PQ interval more than 0.24 sec, systolic blood pressure less than 100 mm Hg).
Pregnancy and lactation. Simultaneous intravenous use of slow calcium channel blockers such as verapamil. Under 18 years of age. Pheochromocytoma. patients receiving long-term or intermittent therapy with inotropic agents acting on beta-adrenergic receptors.
Side effects
From the cardiovascular system: possible bradycardia, hypotension, impaired AV conduction, the appearance of symptoms of heart failure.
From the digestive system: at the beginning of therapy, dry mouth, nausea, vomiting, diarrhea, constipation are possible; in some cases, liver function disorders.
From the side of the central nervous system and peripheral nervous system: at the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, a feeling of cold and paresthesia in the extremities are possible; there may be a decrease in the secretion of tear fluid, conjunctivitis, rhinitis, depression, sleep disorders, nightmares.
From the hematopoietic system: in some cases – thrombocytopenia.
Endocrine system disorders: hypoglycemic conditions in patients with diabetes mellitus.
From the respiratory system: in predisposed patients, symptoms of bronchial obstruction may occur.
Allergic reactions: skin rash, pruritus.
Interaction
When used concomitantly with antihypertensive agents, diuretics, antiarrhythmic agents, nitrates, there is a risk of developing severe arterial hypotension, bradycardia, AV block.
When used concomitantly with barbiturates, metoprolol metabolism accelerates, which leads to a decrease in its effectiveness.
When used concomitantly with hypoglycemic agents, the effect of hypoglycemic agents may increase.
When used concomitantly with NSAIDs, the hypotensive effect of metoprolol may decrease.
When used concomitantly with opioid analgesics, the cardiodepressive effect is mutually enhanced.
When used concomitantly with peripheral muscle relaxants, it is possible to increase neuromuscular blockade.
When used concomitantly with inhaled anesthesia, the risk of myocardial function suppression and hypotension increases.
When used concomitantly with oral contraceptives, hydralazine, ranitidine, cimetidine, the concentration of metoprolol in blood plasma increases.
When used concomitantly with amiodarone, hypotension, bradycardia, ventricular fibrillation, and asystole are possible.
When used concomitantly with verapamil, Cmax in blood plasma and AUC of metoprolol increases. Reduced minute and stroke volume of the heart, pulse rate, arterial hypotension. It is possible to develop heart failure, dyspnoea and sinus node block.
With intravenous use of verapamil while taking metoprolol, there is a risk of cardiac arrest.
Simultaneous use may increase bradycardia caused by digitalis glycosides.
When used concomitantly with dextropropoxifene, the bioavailability of metoprolol increases.
When used concomitantly with diazepam, it is possible to reduce the clearance and increase the AUC of diazepam, which may lead to an increase in its effects and a decrease in the rate of psychomotor reactions.
When used concomitantly with diltiazem, the concentration of metoprolol in blood plasma increases due to inhibition of its metabolism under the influence of diltiazem. Additionally, the effect on heart activity is inhibited due to the slowing of the pulse conduction through the AV node caused by diltiazem. There is a risk of developing severe bradycardia, a significant decrease in stroke and minute volume.
When used concomitantly with lidocaine, lidocaine excretion may be impaired.
Concomitant use with mibefradil in patients with low activity of the CYP2D6 isoenzyme may increase the concentration of metoprolol in blood plasma and increase the risk of toxic effects.
When used concomitantly with norepinephrine, epinephrine, other adreno – and sympathomimetics (including in the form of eye drops or as part of antitussive agents), a slight increase in blood pressure may occur.
When used concomitantly with propafenone, the concentration of metoprolol in the blood plasma increases and a toxic effect develops. Propafenone is believed to inhibit metoprolol metabolism in the liver, reducing its clearance and increasing serum concentrations.
When used concomitantly with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop.
When used concomitantly with rifampicin, the concentration of metoprolol in blood plasma decreases.
Metoprolol may cause a slight decrease in theophylline clearance in smokers.
Fluoxetine inhibits the CYP2D6 isoenzyme, which leads to inhibition of metoprolol metabolism and its accumulation, which can increase the cardiodepressive effect and cause bradycardia. A case of lethargy is described.
Fluoxetine and mainly its metabolites are characterized by a long T1 / 2, so the probability of drug interaction persists even a few days after discontinuation of fluoxetine.
There are reports of decreased clearance of metoprolol from the body when co-administered with ciprofloxacin.
When used concomitantly with ergotamine, it is possible to increase peripheral circulatory disorders.
When used concomitantly with estrogens, the antihypertensive effect of metoprolol decreases.
When used concomitantly, metoprolol increases the concentration of ethanol in the blood and prolongs its excretion.
How to take, course of use and dosage
When taken orally, the average dose is 50-100 mg / day in 1-2 divided doses. If necessary, the daily dose is gradually increased to 200 mg.
Maximum doses: when taken orally, the daily dose is 400 mg.
Overdose
Symptoms: severe sinus bradycardia, dizziness, AV block (up to the development of complete transverse block and cardiac arrest), marked decrease in blood pressure, syncope, arrhythmia/ventricular extrasystole, acute heart failure; cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma, nausea, vomiting, cyanosis, hypoglycemia, convulsions. The first signs of overdose appear 20 minutes -2 hours after taking the drug.
Treatment: gastric lavage and use of adsorbent drugs, 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-intravenous use with an interval of 2-5 minutes of beta-adrenostimulants-until the desired effect is achieved or intravenous use of 0.5-2 mg of atropine sulfate. In the absence of a positive effect — dopamine, dobutamine or norepinephrine. As a follow – up, a transvenous intracardial electrostimulator may be installed. In case of bronchospasm, intravenous beta-adrenomimetics should be administered. For convulsions-slow intravenous use of diazepam. Hemodialysis is ineffective.
Special instructions
It is used with caution in patients with chronic obstructive airway diseases, diabetes mellitus (especially with a labile course), Raynaud’s disease and obliterating peripheral artery diseases, pheochromocytoma (should be used in combination with alpha-blockers), severe renal and hepatic dysfunction.
During 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 metoprolol treatment should be carried out gradually (at least for 10 days). under the supervision of a doctor.
Concomitant use of metoprolol with MAO inhibitors is not recommended.
In combination therapy with clonidine, the latter should be discontinued several days after metoprolol is discontinued, in order to avoid a hypertensive crisis. When used concomitantly with hypoglycemic agents, correction of their dosage regimen is required.
A few days before anesthesia, it is necessary to stop taking metoprolol or choose a drug for anesthesia with minimal negative inotropic effect.
Influence on the ability to drive motor vehicles and manage mechanisms
In patients whose activity requires increased attention, the question of using metoprolol on an outpatient basis should be decided only after evaluating the individual patient response.
Form of production
Metoprolol tablets.
Storage conditions
In a dark place, at a temperature not exceeding 25°C.
See expiration date. on the packaging.
Active ingredient
Metoprolol
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For adults as directed by your doctor
Indications
Angina, Arrhythmia, Migraine, Hypertension
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