Egilok pills 100 mg 60 pcs
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Active ingredients
Metoprolol
Release form
Pills
Composition
Metoprolol tartrate 100 mg. Supplementary substances: microcrystalline cellulose, sodium carboxymethyl starch, silicon dioxide, colloidal anhydrous, povidone, magnesium stearate.
Pharmacological effect
Cardioselective beta1-blocker without internal sympathomimetic activity. It has a hypotensive, antianginal and antiarrhythmic effect. It lowers the automatism of the sinus node, reduces heart rate, slows AV conductivity, reduces contractility and myocardial excitability, reduces cardiac output, reduces myocardial need for oxygen. Suppresses the stimulating effect of catecholamines on the heart during physical and psychoemotional stress. It causes a hypotensive effect, which stabilizes by the end of the 2nd week of course application. With exertional angina, metoprolol reduces the frequency and severity of seizures. Normalizes heart rhythm in supraventricular tachycardia and atrial fibrillation. When myocardial infarction contributes to the limitation of the ischemic zone of the heart muscle and reduces the risk of fatal arrhythmias, reduces the likelihood of recurrence of myocardial infarction. When used in moderate therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.
Pharmacokinetics
After oral administration, metoprolol is rapidly and almost completely absorbed from the gastrointestinal tract, the Cmax of the active substance in the blood plasma is reached in 1-2 hours. After absorption, metoprolol is largely exposed to the effect of first passage through the liver. Intensively metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system with the formation of nektivnyh metabolites. T1 / 2 of plasma metoprolol is 3-4 h and does not change during the course of treatment. More than 95% of the dose taken is excreted by the kidneys, of which only 3% is unchanged.
Indications
Arterial hypertension, prevention of strokes, heart rhythm disturbances (supraventricular tachycardia, extrasystole), secondary prophylaxis after myocardial infarction, hyperkinetic cardiac syndrome (including hyperthyroidism, NDC). Prevention of migraine attacks.
Contraindications
AV block II and III degree, sinoatrial block, bradycardia (HR less than 50 beats / min), SSSU, arterial hypotension, chronic heart failure IIB-III stage, acute heart failure, cardiogenic shock, metabolic acidosis, marked disorders of peripheral circulation hypersensitivity to metoprolol.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Use during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus. Metoprolol penetrates the placental barrier. In connection with the possible development of bradycardia in the newborn, arterial hypotension, hypoglycemia and respiratory arrest, metoprolol must be canceled 48-72 hours before the planned period of delivery. After delivery, it is necessary to ensure strict monitoring of the condition of the newborn for 48-72 hours. Metoprolol is excreted in small quantities with breast milk. Use during lactation is not recommended.
Dosage and administration
When ingested, the average dose is 100 mg / day in 1-2 doses. If necessary, the daily dose is gradually increased to 200 mg. With the / in the introduction of a single dose of 2-5 mg; in the absence of the effect, repeated administration is possible after 5 minutes. Maximum doses: when taken orally, the daily dose is 400 mg, with intravenous administration, a single dose is 15-20 mg.
Side effects
Since the cardiovascular system: possible bradycardia, arterial hypotension,AV conduction disorders, symptoms of heart failure. From the digestive system: dry mouth, nausea, vomiting, diarrhea, constipation are possible at the beginning of therapy; in some cases, liver dysfunction. From the central nervous system and peripheral nervous system: weakness, fatigue, dizziness, headache, muscle cramps, feeling of cold and paresthesia in the limbs are possible at the beginning of therapy; reduction of secretion of the tear fluid, conjunctivitis, rhinitis, depression, sleep disorders, nightmares are possible. From the hematopoietic system: in some cases - thrombocytopenia. From the endocrine system: hypoglycemic states in patients with diabetes. From the respiratory system: from susceptible patients possible symptoms of bronchial obstruction. Allergic reactions: skin rash, itching.
Interaction with other drugs
With simultaneous use with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of severe arterial hypotension, bradycardia, AV blockade. Metoprolol metabolism accelerates with simultaneous use with barbiturates, which reduces its effectiveness. With simultaneous use with hypoglycemic agents, it is possible enhancing the action of hypoglycemic agents. When used simultaneously with NSAIDs, the hypotensive action of metoprolol may be reduced. When used simultaneously with opioid analgesics, the cardiodepressive effect is mutually enhanced. If used simultaneously with peripheral muscle relaxants, neuromuscular blockade may be increased. If used simultaneously with inhalation anesthesia, the risk of inhibition of myocardial function and the development of arterial hypotension is increased. , ranitidine, cimetidine increases the concentration of metoprolol in the blood plasma. At the same time enii with amiodarone may be hypotension, bradycardia, ventricular fibrillation, asistoliya.Pri simultaneous use of verapamil increases Cmax and AUC in the blood plasma of metoprolol. Minute and stroke volume of the heart, pulse rate, arterial hypotension are reduced.Heart failure, dyspnea, and sinus node blockage may develop. With intravenous administration of verapamil while taking metoprolol, there is a threat of cardiac arrest. With simultaneous use, bradycardia caused by glycosides of digitalis may be increased. With simultaneous use with dextropropoxyfen, the bioavailability of metoprolol may increase. diazepam may decrease clearance and increase AUC of diazepam, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions iy.Pri simultaneous application with diltiazem increased concentration of metoprolol in the blood plasma due to 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 impulse conduction through the AV node caused by diltiazem. There is a risk of severe bradycardia, a significant decrease in stroke and minute volume. If used simultaneously with lidocaine, impaired lidocaine may be impaired. Concurrent use with mibefradil in patients with low CYP2D6 isoenzyme may increase plasma concentrations of metoprolol and increase the risk of toxic effects. simultaneous use with norepinephrine, epinephrine, other adreno-and sympathomimetics (including in the form of eye drops or as part of anti-cough O funds) may be some increase in AD.Pri simultaneous use of propafenone increased metoprolol plasma concentration and develops a toxic effect. It is believed that propafenone inhibits the metabolism of metoprolol in the liver, reducing its clearance and increasing serum concentrations. When used concurrently with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop. When used concurrently with rifampicin, the concentration of metoprolol in the blood plasma decreases. decrease in theophylline clearance in smoking patients. Fluoxetine inhibits CYP2D6 isoenzyme, this leads to inhibition of metabolism of metoprolol and its accumulation, It may enhance the cardiodepressive effect and cause bradycardia.A case of development of lethargy is described. Fluoxetine and mainly its metabolites are characterized by prolonged T1 / 2, so the likelihood of drug interaction persists even several days after discontinuing fluoxetine. There are reports of a decrease in clearance of metoprolol from the body while using it with ciprofloxacin. enhancement of peripheral circulatory disorders. When used simultaneously with estrogens, the antihypertensive effect of metoprolo is reduced a.Pri simultaneous application metoprolol increases blood ethanol concentration and lengthens its excretion.
special instructions
It is used with caution in patients with chronic obstructive respiratory diseases, diabetes (especially when labile), Raynaud's disease and obliterating diseases of peripheral arteries, pheochromocytoma (should be used in conjunction with alpha-adrenergic blockers), marked impaired renal function and liver. treatment of metoprolol may reduce the production of tear fluid, which is important for patients who use contact lenses. Completion of a long course of treatment oprololom should be gradually (at least for 10 days) under observation to the simultaneous vracha.Ne metoprolol MAO.Pri inhibitors combination therapy with clonidine intake latter should stop after a few days after discontinuation of metoprolol to prevent hypertensive crisis. With simultaneous use with hypoglycemic agents, correction of their dosing regimen is required. For several days before performing anesthesia, it is necessary to stop taking metoprolol or find a remedy for anesthesia with minimal negative inotropic effects. Influence on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of metoprolol on an outpatient basis should be resolved only after evaluating the individual response of the patient.