Metoprolol ratiopharm pills 50mg N30
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Description
Metoprolol ratiopharm pills are a beta-blocker that affects the heart’s beta-adrenoreceptors and improves blood flow through the arteries of the heart muscle.
Active ingredients
Metoprolol
Release form
Pills
Composition
Metoprolol Tartrate 50 mg
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 accepted dose 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.
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 within 48-72 hours. Metoprolol is excreted in small quantities with breast milk. Use during lactation is not recommended.
Dosage and administration
Tablets are taken internally with a small amount of liquid, without chewing, with food or immediately after a meal. Tablets can be divided. The course of treatment is not limited in time and depends on the characteristics of the course of the disease. If it is necessary to cancel treatment, the dose is reduced gradually (minimum for 10 days) under the supervision of a physician. Arterial hypertension: the initial daily dose is 50-100 mg in 1-2 doses (in the morning and in the evening). With insufficient therapeutic effect, the daily dose can be gradually increased to 100-200 mg. The maximum daily dose of 200 mg.Stenocardia, arrhythmias, prevention of migraine attacks: 100-200 mg per day in two doses (in the morning and in the evening). Secondary prevention of myocardial infarction: 200 mg per day in two doses (in the morning and evening). Functional disorders of the heart activities accompanied by tachycardia: 100 mg per day in two doses (morning and evening). When a therapeutic effect is achieved, the dose is reduced (under the supervision of a physician). Older patients are advised to begin treatment with 50 mg / day. How to divide a pill. "Metoprolol ratiopharm" - pills can be easily divided into 2 or 4 parts. To divide the tablet, it is necessary to put a non-hard surface (for example, a plate) with a cross-shaped incision up.If you push one finger into the center of the cross-cut incision, the tablet can easily be divided into 4 parts (25 mg each). Two fingers on the edge of the tablet, the tablet is easy to split into 2 parts (50 mg each).
Side effects
Since the cardiovascular system: possible bradycardia, arterial hypotension, violations of AV-conduction, the appearance of symptoms of heart failure. On the part of the digestive system: at the beginning of therapy, dry mouth, nausea, vomiting, diarrhea, constipation; in some cases - abnormal liver function. On the part of the central nervous system and peripheral nervous system: at the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, feeling of cold and paresthesia in the limbs; reduction of secretion of tear fluid, conjunctivitis, rhinitis, depression, sleep disturbances, nightmarish dreams are possible. From the hematopoietic system: in some cases - thrombocytopenia. On the part of the endocrine system: hypoglycemic states in patients with diabetes mellitus. On the part of the respiratory system: symptoms of bronchial obstruction are possible in predisposed patients. Allergic reactions: skin rash, itching.
Overdose
Symptoms: severe severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked reduction in blood pressure, arrhythmia, ventricular extrasystoles, bronchospasm, syncope, in acute overdose - cardiogenic shock, loss of consciousness, coma, atrio-ventricular mode, loss of heart failure, a heart block, a bowel strains, a heart block, an amyloventricular block, a heart block, a heart failure, a heart block, a heart block, a heart block, a heart block, an amyloventricular syndrome, a heart failure, an obstructive chest syndrome, a heart failure, a heart failure, a heart failure, a coma cardiac arrest), cardialgia. The first signs of overdose appear after 20 minutes - 2 hours after taking the drug. Treatment: gastric lavage and the appointment of absorbent funds; symptomatic therapy: with a marked reduction in blood pressure - the patient should be in the Trendelenburg position; in case of excessive reduction of blood pressure, bradycardia and heart failure - in / in, with an interval of 2-5 minutes, bata-adrenostimulyatory - to achieve the desired effect or in / in 0.5-2 mg of atropine sulfate. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine). As a follow-up, perhaps, the appointment of 1-10 mg of glucagon, staging transvenous intracardial electrostimulator.When bronchospasm should be introduced into / in stimulators beta 1 -adrenoreceptors. For convulsions, slow i.v. administration of diazepam. Hemodialysis is not effective.
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. With simultaneous use with barbiturates, metabolism of metoprolol is accelerated, which leads to a decrease in its effectiveness. With simultaneous use with hypoglycemic agents may increase 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 cardiodepressive effect is mutually enhanced. With simultaneous use with peripheral muscle relaxants may increase neuromuscular blockade. With simultaneous use with agents for inhalation anesthesia increases the risk of inhibition of myocardial function and the development of arterial hypotension. With simultaneous use with oral contraceptives, hydralazine, ranitidine, cimetidine increases the concentration of metoprolol in the blood plasma. With simultaneous use with amiodarone arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible. With simultaneous use with verapamil Cmax increases in 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 in patients receiving metoprolol there is a threat of cardiac arrest. With simultaneous use may increase bradycardia caused by digitalis glycosides. When used simultaneously with dextropropoxyphene, the bioavailability of metoprolol is increased. With simultaneous use with diazepam may decrease clearance and increase the AUC of diazepam, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions. With simultaneous use with diltiazem, the concentration of metoprolol in the blood plasma increases 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. With simultaneous use with lidocaine, a violation of lidocaine may be possible. With simultaneous use with mibefradil in patients with low CYP2D6 isoenzyme, it is possible to increase the concentration of metoprolol in the blood plasma and increase the risk of toxic effects. With simultaneous use with norepinephrine, epinephrine, other adreno-and sympathomimetics (including in the form of eye drops or as part of antitussives), some 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, reducing its clearance and increasing serum concentrations. With simultaneous use with reserpine, guanfacine, methyldopa, clonidine, the development of severe bradycardia is possible. With simultaneous use of rifampicin decreases the concentration of metoprolol in the blood plasma. Metoprolol may cause a slight decrease in theophylline clearance in smoking patients. Fluoxetine inhibits the CYP2D6 isoenzyme, which leads to inhibition of metabolism of metoprolol and its accumulation, which can enhance the cardiodepressive effect and cause bradycardia. The case of the development of lethargy is described. Fluoxetine and mainly its metabolites are characterized by a long T1 / 2, so the likelihood of drug interaction persists even a few days after discontinuing fluoxetine. There are reports of a decrease in the clearance of metoprolol from the body while using it with ciprofloxacin. With simultaneous use with ergotamine may increase peripheral circulatory disorders. With simultaneous use with estrogen decreases the antihypertensive effect of metoprolol. With simultaneous use of metoprolol increases the concentration of ethanol in the blood and prolongs its excretion.
special instructions
It is used with caution in patients with chronic obstructive airway diseases, diabetes mellitus (especially when labile), Raynaud's disease and obliterating diseases of the peripheral arteries, pheochromocytoma (should be used in conjunction with alpha-blockers), marked impaired renal function and liver.With metoprolol treatment, a reduction in the production of tear fluid is possible, which is important for patients using contact lenses. The completion of a prolonged course of treatment with metoprolol should be carried out gradually (for at least 10 days) under the supervision of a physician. The simultaneous use of metoprolol with MAO inhibitors is not recommended. In combination therapy with clonidine, the latter should be stopped several days after the cancellation of metoprolol, in order to avoid a hypertensive crisis. At simultaneous use with hypoglycemic agents correction of their dosing regimen is required. A few days before undergoing anesthesia, it is necessary to stop taking metoprolol or to choose a remedy for anesthesia with minimal negative inotropic effects. Impact on the ability to drive vehicles and control mechanisms In patients whose activities require increased attention, the question of the use of metoprolol on an outpatient basis should be addressed only after evaluating the patient's individual response.