Description
Release form
Tablets are white or grayish-white tablets, round, flat, with a risk on one side and a chamfer on both sides.
Pharmacological action
Cardioselective beta1-blocker without internal sympathomimetic activity. It has a hypotensive, antianginal and antiarrhythmic effect. Reduces the automatism of the sinus node, reduces heart rate, slows down AV-conduction, reduces contractility and excitability of the myocardium, reduces cardiac output, reduces myocardial oxygen demand.
Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.
Causes a hypotensive effect that stabilizes by the end of the 2nd week of course use. With angina pectoris, metoprolol reduces the frequency and severity of seizures.
Normalizes heart rate in supraventricular tachycardia and atrial fibrillation. With myocardial infarction, it helps to limit the area of ischemia of the heart muscle and reduces the risk of fatal arrhythmias, reduces the likelihood of recurrence 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
¦ angina pectoris
¦ stable symptomatic chronic heart failure
with impaired systolic function of the left ventricle (as
adjunctive therapy for the main treatment of chronic heart failure srdlkrd myocardial infarction
¦ heart rhythm disturbance, including supraventricular tachycardia,
decrease in ventricular contraction rate during atrial fibrillation diy and
ventricular extrasystoles
¦ functional disorders of the heart, accompanied by
tachycardia
¦ prevention of migraine attacks.
Contraindications
Hypersensitivity, cardiogenic shock, AV block II and III degree, sinoatrial block, chronic (at the stage of decompensation) heart failure, sinus node weakness syndrome, severe sinus bradycardia (heart rate less than 60 beats / min Prinz, wall angina, acute angina) myocardial infarction (heart rate less than 45 udmin, PQ interval more than 0.24 seconds, systolic blood pressure less than 100 mm RT.st).
Pregnancy, lactation. Simultaneous intravenous administration of slow calcium channel blockers such as verapamil. Age to 18 years. Pheochromocytoma. patients receiving long-term or intermittent therapy with inotropic drugs and acting on beta-adrenergic receptors.
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 the peripheral arteries, pheochromocytoma (should be used in combination with alpha-adrenergic blockers), severe impaired renal and hepatic function.
Against the background of treatment with metoprolol, a decrease in the production of tear fluid is possible, which is important for patients using contact lenses.
The completion of a long course of treatment with metoprolol should be carried out gradually (for at least 10 days) under the supervision of a physician.
Concomitant use of metoprolol with MAO inhibitors is not recommended.
In combination therapy with clonidine, administration of the latter should be discontinued several days after the cancellation 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, you must stop taking metoprolol or choose a drug for anesthesia with minimal negative inotropic effect.
Influence on the ability to drive vehicles and control mechanisms
In patients whose activities require increased attention, the use of metoprolol on an outpatient basis should be decided only after evaluating the patient’s individual response.
Dosage and administration of
When administered orally, the average dose is 50-100 mg / day. in 1-2 doses.
If necessary, the daily dose is gradually increased to 200 mg.
Maximum Dosages: when taken orally, the daily dose is 400 mg.
Side effects of
From the cardiovascular system: possible bradycardia, arterial 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, and constipation are possible in some cases – impaired liver function.
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 may decrease the secretion of lacrimal fluid, conjunctivitis, rhinitis, depression, sleep disturbances, nightmares.
From the hemopoietic system: in some cases – thrombocytopenia.
From the endocrine system: hypoglycemic conditions in patients with diabetes mellitus.
From the respiratory system: in predisposed patients, symptoms of bronchial obstruction may occur.
Allergic reactions: skin rash, itching.
Drug interaction
When used simultaneously with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of severe arterial hypotension, bradycardia, and AV block.
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, the action of hypoglycemic agents may be enhanced.
With simultaneous use with NSAIDs, a decrease in the hypotensive effect of metoprolol is possible.
When used simultaneously with opioid analgesics, the cardiac depressant effect is mutually enhanced.
With simultaneous use with peripheral muscle relaxants, increased neuromuscular blockade is possible.
With simultaneous use with 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 blood plasma increases.
With simultaneous use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.
Concomitant use with verapamil increases Cmax in blood plasma and AUC of metoprolol. Minute and stroke volume of the heart, pulse rate, arterial hypotension are reduced. Perhaps the development of heart failure, dyspnea and blockade of the sinus node.
With the on / in the introduction of verapamil while taking metoprolol, there is a risk of cardiac arrest.
With simultaneous use, intensification of bradycardia caused by digitalis glycosides is possible.
With simultaneous use with dextropropoxyphene, the bioavailability of metoprolol is increased.
With simultaneous use with diazepam, a decrease in clearance and an increase in the AUC of diazepam are possible, which can lead to an increase in its effects and a decrease in the rate of psychomotor reactions.
With simultaneous use with diltiazem, the concentration of metoprolol in blood plasma increases due to inhibition of its metabolism under the influence of diltiazem. The effect on the activity of the heart is additively suppressed in connection with the slowdown in the conduction of an impulse 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 excretion of lidocaine is possible.
With simultaneous use with mibefradil in patients with low activity of the isoenzyme CYP2D6, an increase in the concentration of metoprolol in blood plasma and an increase in the risk of toxic effects may occur.
With simultaneous use with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form of eye drops or as part of antitussive drugs), 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, guanfacin, methyldopa, Clonidine may develop severe bradycardia.
With simultaneous use with rifampicin, the concentration of metoprolol in blood plasma decreases.
Metoprolol may cause a slight decrease in theophylline clearance in smoking patients.
Fluoxetine inhibits the isoenzyme of CYP2D6, this leads to inhibition of the metabolism of metoprolol and its cumulation, which can enhance the cardiodepressive effect and cause bradycardia. A case of lethargy is described.
Fluoxetine and mainly its metabolites are characterized by prolonged T1 / 2, so the likelihood of drug interaction remains even several days after the withdrawal of fluoxetine.
There are reports of a decrease in the clearance of metoprolol from the body while using ciprofloxacin.
With concomitant use with ergotamine, increased peripheral circulation disturbances are possible.
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.
Overdose
Symptoms: severe sinus bradycardia, dizziness, AV block (up to the development of complete lateral block and cardiac arrest), marked decrease in blood pressure, fainting, arrhythmia / ventricular extrasystole, acute heart failure cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma, nausea, vomiting, cyanosis, hypoglycemia, convulsions. The first signs of an overdose appear 20 minutes to 2 hours after taking the drug.
Treatment: gastric lavage and the administration of adsorbing drugs, symptomatic therapy: with a marked decrease in blood pressure – the patient should be in the Trendelenburg position in the case of an excessive decrease in blood pressure, bradycardia and heart failure – intravenous administration with an interval of 2-5 min beta-adrenostimulants – to achieve the desired effect or in / in the introduction 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 intracardiac pacemaker is possible. With bronchospasm, intravenous beta-adrenergic agonists should be administered. With convulsions, a slow intravenous administration of diazepam. Hemodialysis is ineffective.
Storage conditions
In the dark place at a temperature of no higher than 25 ° C.
Deystvuyuschee substances
Metoprolol
Conditions of dispatch from
pharmacies Prescription
dosage form
tablets
