Metoprolol retard Akrikhin film-coated pills 50mg N30
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Description
Tablets Metoprolol retard - Akrikhin is a cardio-selective beta1-blocker. It has no membrane stabilizing effect and does not possess intrinsic sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects. By blocking beta1-adrenoreceptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, has a negative chrono, dromo, batmo and inotropic effect (decreases heart rate) ), inhibits conductivity and excitability, reduces myocardial contractility). General peripheral vascular resistance (OPSS) at the beginning of beta-blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the removal of beta2-adrenoreceptor stimulation), which after 1-3 days returns to its original, and with prolonged appointment decreases. The antihypertensive effect is due to a decrease in the minute volume of blood flow and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (is more important in patients with initial renin hypersecretion) and the central nervous system, restoration of the sensitivity of baroreceptors of the aortic arch (their activity does not increase in response to reduction blood pressure (BP) and, as a result, decrease in peripheral sympathetic effects. the hypertensive effect lasts for more than 24 hours.The antianginal effect is determined by a decrease in myocardial oxygen demand due to a decrease in heart rate (lengthening diastole and improved myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. due to an increase in the end diastolic pressure in the left ventricle and an increase in the stretching of the muscle fibers of the ventricles oxygen demand, 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, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of atrioventricular (AV) conduction (mainly in antegrade and to a lesser extent in retrograde through the AV node) and along additional paths. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional heart disease and thyrotoxicosis, the heart rate slows down or may even lead to the restoration of sinus rhythm. Prevents migraine development. Unlike non-selective beta-adrenergic blockers, when administered in moderate therapeutic doses, the organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries, bronchi and uterus) and carbohydrate metabolism are less pronounced. from the action of propranolol. With many years of admission reduces the concentration of cholesterol in the blood. When used in high doses (more than 100 mg / day), it has a blocking effect on both beta adrenoreceptor subtypes.
Active ingredients
Metoprolol
Release form
Pills
Composition
Active ingredient: metoprolol succinate - 47.66 mg. Excipients: hypromellose, ludepress LCE (lactose monohydrate 94.7-98.3%, povidone 3-4%), colloidal silicon dioxide, magnesium stearate. The composition of the shell: ready-mixed "Opadry II" green (polyvinyl alcohol, talc, macrogol, titanium dioxide, quinoline yellow dye (aluminum varnish), iron dye black oxide, dye indigo carmine (aluminum varnish)).
Indications
Arterial hypertension, chronic heart failure of the II-IV functional class according to the NYHA classification in the compensation stage (as part of complex therapy), coronary heart disease (prevention of attacks of stable angina, reduction of mortality and recurrence of myocardial infarction after the acute phase of myocardial infarction), cardiac arrhythmias , including supraventricular tachycardia, reduction in the rate of ventricular contraction during atrial fibrillation and ventricular extrasystoles, functional disorders of cardiac activity flax, accompanied by tachycardia, prevention of migraine attacks.
Precautionary measures
Before use, consult with your doctor.
Use during pregnancy and lactation
During pregnancy, the drug Metoprolol Retard-Akrikhin should be used only under strict indications when the expected benefit to the mother outweighs the potential risk to the fetus / child (due to the possible development of bradycardia in the newborn, lowering blood pressure, hypoglycemia and respiratory paralysis). At the same time carry out careful monitoring especially for the development of the fetus. Treatment is stopped 48-72 hours before the onset of labor. If this is not possible, the newborn should be under especially careful observation for 48-72 hours after birth. The use of the drug Metoprolol Retard-Akrikhin is contraindicated during lactation, in case of need the use of the drug during lactation, breastfeeding should be stopped.
Dosage and administration
Metoprolol retard-Akrikhin is intended for oral administration 1 time per day, it is recommended to be taken in the morning, without chewing, drinking water. Metoprolol retard-Akrikhin can be taken regardless of the meal. In order to prevent bradycardia, the dose is selected individually and increased gradually. With hypertension and angina, the initial dose of 50 mg 1 time per day, with insufficient therapeutic effect, the daily dose can be increased to 100-200 mg per day. With hypertension with the ineffectiveness of the drug at a dose of 100-200 mg per day, you can add another antihypertensive agent. In chronic heart failure II functional class according to the NYHA classification (without exacerbations of the last 6 weeks and without a change in the complex therapy during the last 2 weeks), the recommended initial dose is 25 mg once a day. After two weeks, the daily dose can be increased to 50 mg, then after two weeks to 100 mg, in another two weeks to 200 mg. In chronic heart failure III-IV functional class according to the NYHA classification, the recommended initial dose for the first 2 weeks is 12.5 mg of the drug once a day. You can use metoprolol in another dosage form, for example, 25 mg pills with a risk. During the period of increasing the dose, the patient should be supervised, since in some patients the symptoms of heart failure may worsen. After 1-2 weeks, the dose may be increased to 25 mg once daily.Then after 2 weeks, the dose may be increased to 50 mg once a day. Patients who tolerate the drug well can double the dose every 2 weeks until reaching the maximum dose of 200 mg of the drug once a day. Secondary prevention of myocardial infarction and cardiac arrhythmias - the initial dose of 100 mg 1 time per day. With functional disorders of cardiac activity, accompanied by tachycardia - 50 mg per day, if necessary, the dose can be increased to 200 mg per day. Prevention of migraine attacks: 100-200 mg 1 time per day. Elderly patients with renal failure or patients on hemodialysis, dose adjustment is not required. Impaired liver function affects the elimination of metoprolol, therefore, dose adjustment may be required depending on the clinical condition.
Side effects
Frequency of side effects: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less than 1/10000, including individual messages. Since the cardiovascular system: often - bradycardia, orthostatic hypotension (including with fainting), cooling of the lower extremities, feeling of heartbeat, rarely - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV block I degree rarely - myocardial conduction disorders, arrhythmia, very rarely - gangrene (in patients with peripheral circulatory disorders). On the part of the central nervous system: very often - increased fatigue, reduced speed of mental and motor reactions, often - dizziness, headache, rarely - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, “nightmarish” dreams, rarely - asthenia , tremor, increased nervous irritability, anxiety, very rarely - amnesia / impaired memory, depression, hallucinations, myasthenia. On the part of the senses: rarely - impaired vision, dry and / or irritated eyes, conjunctivitis, very rarely - tinnitus, impaired taste. On the part of the digestive system: often - nausea, abdominal pain, constipation or diarrhea, infrequently - vomiting, rarely - dryness of the oral mucosa, abnormal liver function, hepatitis.On the part of the skin: infrequently - urticaria, increased sweating, rarely - alopecia, very rarely - photosensitization, exacerbation of the course of psoriasis, psoriasis-like skin reactions. On the part of the respiratory system: often - shortness of breath, infrequently - bronchospasm in patients with bronchial asthma, rarely - rhinitis. Laboratory indicators: very rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of “liver” enzymes, hyperbilirubinemia. On the part of the endocrine system: often - hypoglycemia (in patients with diabetes mellitus type I), rarely - hyperglycemia (in patients with diabetes mellitus type II), a hypothyroid state. Other: infrequently - weight gain, rarely - impotence sexual dysfunction, very rarely - arthralgia, thrombocytopenia.
Overdose
Symptoms: severe bradycardia, AV blockade (up to the development of complete transverse blockade and cardiac arrest), marked reduction of blood pressure, impaired peripheral circulation, increased symptoms of heart failure, cardiogenic shock, respiratory depression, apnea, cyanosis, fatigue, dizziness, loss of consciousness, coma, tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, esophagism, hypoglycemia or hyperglycemia, hyperkalemia, transient myasthenia may develop. The first signs of overdose appear after 20 minutes - 2 hours after taking the drug. Treatment: If the drug is taken recently - gastric lavage and taking absorbent means, in violation of atrioventricular conductivity and / or bradycardia - intravenous administration of 1-2 mg of atropine, epinephrine (adrenaline) or setting a temporary pacemaker, while lowering blood pressure - the patient should be in the Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasma-substituting solutions, with ineffectiveness - administration of epinephrine, dopamine, dobutamine, with acute heart failure - cardiac glycosides, diuretics, with convulsions - intravenous diazepam, with bronchospasm - inhalation or parenteral beta-2 adrenomimetica.
Interaction with other drugs
Catecholamine depleting agents (for example, reserpine, MAO inhibitors) when used concomitantly with metoprolol may enhance the hypotensive effect or cause pronounced bradycardia. A break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days. Metoprolol is a substrate of CYP2D6 isoenzyme.Drugs that inhibit or induce the activity of the CYP2D6 isoenzyme can affect the plasma concentration of metoprolol. Inhibitors of the isoenzyme CYP2D6: some antidepressants and antipsychotics, quinidine, terbinafine, celecoxib, propafenone, difehydramine, hydroxychlorin, cimetidine - increase the concentration of metoprolol in the blood plasma. Inductors of CYP2D6 isoenzyme: barbituric acid derivatives, rifampicin - reduce the concentration of metoprolol in the blood plasma. Simultaneous use with cardiac glycosides, clonidine, blockers of “slow” calcium channels (verapamil, diltiazem), amiodarone, class I antiarrhythmic drugs, general anesthesia drugs, methyldopa, guanfacine can lead to a decrease in blood pressure and marked bradycardia. Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of inhibition of myocardial function and the development of arterial hypotension. Simultaneous intravenous administration of verapamil can trigger cardiac arrest. Non-steroidal anti-inflammatory drugs (NSAIDs) and beta-adrenomimetics weaken the antihypertensive effect of beta-blockers. Ergot alkaloids increase the risk of peripheral circulatory disorders. When taken together with oral hypoglycemic drugs, their effect may be reduced, with insulin - an increased risk of hypoglycemia, lengthening and enhancement of its severity, masking some of the symptoms of hypoglycemia (tachycardia, sweating, high blood pressure). Reduces clearance of xanthines (except diafillin), especially in patients with initially increased clearance of theophylline under the influence of smoking. Reduces clearance of lidocaine, increases the concentration of lidocaine in plasma. Strengthens and prolongs the action of non-depolarizing muscle relaxants, prolongs the anticoagulant effect of coumarins. At the same time taking epinephrine (adrenaline) with beta-blockers may increase blood pressure and bradycardia. Phenylpropanolamine (norephedrine) may increase diastolic blood pressure. Allergens used for immunotherapy, or allergy extracts for skin tests when combined with metoprolol, increase the risk of systemic allergic reactions or anaphylaxis, iodine-containing contrast agents for intravenous administration increase the risk of anaphylactic reactions. When combined with ethanol increases the risk of a pronounced decrease in blood pressure.