Metoprolol pills 50 mg 30 pcs
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Active ingredients
Metoprolol
Release form
Pills
Composition
Metoprolol succinate 47.66 mg, which corresponds to the content of metoprolol tartrate 50 mg; Excipients: hypromellose - 161.29 mg, ludipress LCE (lactose monohydrate - 94.7-98.3%, povidone - 3-4%) - 87.42 mg, colloidal silica - 1.5 mg , magnesium stearate - 1.5 mg.; The composition of the shell: the finished mixture "Opadry II" is green (polyvinyl alcohol - 6 mg, talc - 2.22 mg, macrogol - 3.03 mg, titanium dioxide - 2.925 mg, dye quinoline yellow (aluminum varnish) - 0.268 mg, iron dye black oxide - 0.015 mg, indigo carmine dye (aluminum varnish) - 0.542 mg) - 15 mg.
Pharmacological effect
Cardioselective beta1-adrenoblocker. It has no membrane stabilizing effect and does not possess intrinsic sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects. By blocking β1-adrenoreceptors of the heart in low doses, it reduces catecholamine-stimulated formation of cAMP from ATP, decreases the intracellular current of calcium ions, and has a negative chrono-dromo-, batmo- and inotropic effect (reduces heart rate, suppresses conductivity and excitability, reduces myocardial contractility). OPS at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in β-adrenoreceptor activity and the removal of β2-adrenoreceptor stimulation), after 1-3 days it returns to baseline, and with prolonged administration decreases. the effect is due to a decrease in the minute volume of blood flow and renin synthesis, inhibition of the activity of the RAAS (is more important in patients with initial renin hypersecretion) and the central nervous system, the restoration of the sensitivity of the baroreceptor s aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces increased blood pressure at rest, with physical exertion and stress. The antihypertensive effect lasts for more than 24 hours; the antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening diastole and an improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation.Reduces the number and severity of angina attacks and increases exercise tolerance. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles can increase the oxygen demand, especially in patients with chronic heart failure. The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction ( mainly in the antegrade and to a lesser extent in the retrograde directions through the AV node) and along additional routes. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and thyrotoxicosis, the heart rate decreases or it can even lead to the restoration of sinus rhythm; migraine.; In contrast to non-selective beta-adrenergic blockers, when administered in moderate therapeutic doses, it has a less pronounced effect on organs containing β2 -adrenoreceptors (pancreas naya gland, skeletal muscle, smooth muscle of peripheral arteries, bronchi and uterus) and carbohydrate metabolism; the severity of atherogenic action does not differ from that of propranolol. With many years of admission reduces the concentration of cholesterol in the blood. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of β-adrenoreceptors.
Pharmacokinetics
Absorption; Absorption Absorption complete (95%). Fat solubility is moderate. Subjected to intensive presystemic metabolism, bioavailability - 50% at the first dose and increases to 70% when reapplied. The time to reach Cmax in the blood plasma is 6-12 hours after taking the drug. During the course of treatment, bioavailability increases. Eating increases bioavailability by 20-40%; Distribution; Plasma protein binding - 10%. It is rapidly distributed in the tissues, penetrates the BBB, placental barrier. Penetrates into breast milk.; Metabolism; Metabolized in the liver; 2 metabolites have beta-adreno-blocking activity. CYP2D6 isoenzyme is involved in the metabolism of the drug; elimination; T1 / 2 - from 3.5 to 7 hours when taken orally.It is not removed during hemodialysis.; Pharmacokinetics in special clinical situations; Significant accumulation of metabolites is observed in patients with CC 5 ml / min, while the beta-adrenoceptor blocking activity of the drug does not increase.; Bioavailability increases with cirrhosis of the liver, while reducing its overall clearance.
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); - CHD: prevention of attacks of stable angina pectoris, reduction of mortality and the frequency of recurrent myocardial infarction after the acute phase of myocardial infarction; - cardiac arrhythmias, including supraventricular tachycardia, a decrease in the frequency of ventricular contractions during atrial fibrillation and ventricular extrasystoles; - functional disorders of cardiac activity, accompanied by tachycardia; - prevention of migraine attacks.
Contraindications
- cardiogenic shock; - AV blockade II-III degree; - sinoatrial block; - SSSU; - severe bradycardia (heart rate less than 50 beats / min); - acute heart failure or chronic heart failure in the stage of decompensation; - arterial hypotension (systolic blood pressure less than 100 mm Hg); - acute myocardial infarction (heart rate less than 45 beats / min, PQ interval more than 0.24 s, systolic blood pressure less than 100 mm Hg); - severe bronchial asthma; - severe violations of peripheral circulation; - simultaneous administration of MAO inhibitors or simultaneous intravenous administration of verapamil; - pheochromocytoma (without simultaneous administration of alpha-blockers); - age up to 18 years (efficacy and safety have not been established); - lactation period; - Lactase deficiency, lactose intolerance, glucose / galactose malabsorption syndrome; - hypersensitivity to metoprolol and other beta-blockers. With caution, you should prescribe the drug for diabetes mellitus, AV blockade of I degree, Prinzmetal angina, metabolic acidosis, bronchial asthma, COPD, severe renal and / or hepatic insufficiency, myasthenia, fechochromocytoid lesions, myochenia, fechochromocytosis, COPD, severe renal and / or hepatic insufficiency, myasthenia, fechochromocytosis, bronchial asthma, COPD, renal and / or hepatic failure. (while taking alpha-blockers), thyrotoxicosis, depression (including history), psoriasis, peripheral circulatory disorders (intermittent claudication, Raynaud's syndrome), pregnancy, and the patient I am elderly.
Use during pregnancy and lactation
During pregnancy, the drug Metoprolol Retard-Akrikhin should be used only according to 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 h after delivery. The use of the drug Metoprolol retard-Akrihin is contraindicated during lactation. If necessary, the use of the drug during lactation breastfeeding should be stopped.
Dosage and administration
The drug Metoprolol Retard-Akrihin is taken orally 1 time per day. Tablets are recommended to be taken in the morning, without chewing, washing down with water. Metoprolol retard-Akrikhin can be taken regardless of the meal.; To prevent bradycardia, the dose is adjusted individually and increased gradually. In case of arterial hypertension and angina, the initial dose is 50 mg 1 time / day, with insufficient therapeutic effect, the daily dose can be increased to 100 - 200 mg / day. In hypertension with an ineffectiveness of the drug in a dose of 100-200 mg / day, you can add another antihypertensive agent. In NYHA class II functional class according to the NYHA classification (without exacerbations of the last 6 weeks and without a change in the complex therapy in the last 2 weeks), the recommended Initial dose - 25 mg 1 time / day. After 2 weeks, the daily dose can be increased to 50 mg, then after 2 weeks - up to 100 mg, after another 2 weeks - up to 200 mg; In NYHA classification III-IV functional class, the recommended initial dose is the first 2 weeks 12.5 mg 1 time / day. It is possible to 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 under observation, since in some patients, the symptoms of heart failure may worsen. After 1-2 weeks, the dose may be increased to 25 mg 1 time / day. Then after 2 weeks, the dose can be increased to 50 mg 1 time / day. Patients who tolerate the drug wellYou can double the dose every 2 weeks to reach the maximum dose of 200 mg 1 time / day; With the secondary prevention of myocardial infarction and heart rhythm disorders, the initial dose is 100 mg 1 time / day; For functional disorders of the heart, accompanied by tachycardia, 50 mg / day, if necessary, the dose can be increased up to 200 mg / day. For the prevention of migraine attacks, 100-200 mg should be administered 1 time / day. For elderly patients, patients with renal insufficiency or patients on hemodialysis, corrections These doses are not required. Liver dysfunction affects the elimination of metoprolol, therefore, dose adjustment may be required depending on the clinical condition.
Side effects
Frequency of side effects: very often (> 1/10), often (> 1/100 and less than 1/10), infrequently (> 1/1000 and less than 1/100), rarely (> 1/10 000 and less than 1 / 1000), very rarely (less than 1/10 000, including individual messages); From the side of the cardiovascular system: often - bradycardia, orthostatic hypotension (including with fainting), cooling of the lower extremities, feeling of palpitations; infrequently - a temporary increase in the symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV-blockade of the first degree; rarely - myocardial conduction disorders, arrhythmia; very rarely - gangrene (in patients with impaired peripheral circulation); On the part of the central nervous system: very often - increased fatigue, reduced speed of mental and motor responses; often - dizziness, headache; infrequently - paresthesias, convulsions, depression, loss of concentration, drowsiness, insomnia, nightmares; rarely - asthenia, tremor, increased nervous irritability, anxiety; very rarely - amnesia / memory impairment, depression, hallucinations, myasthenia. From the senses: rarely - visual impairment, dryness and / or eye irritation, conjunctivitis; very rarely - ringing in the ears, a violation of 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. On the laboratory side: very rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased liver enzymes, hyperbilirubinemia.; Endocrine system: often - hypoglycemia (in patients with type 1 diabetes mellitus) rarely - hyperglycemia (in patients with type 2 diabetes mellitus), hypothyroid condition.; 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), excessive reduction of blood pressure, impaired peripheral circulation, increased symptoms of heart failure, cardiogenic shock, respiratory depression, apnea, cyanosis, increased fatigue, dizziness, loss of consciousness , coma, tremor, convulsions, excessive sweating, paresthesia, bronchospasm, nausea, vomiting, esophagism, hypoglycemia or hyperglycemia, hyperkalemia, transient myasthenia may develop. The first signs of overdose appear after 20 min-2 h after taking the drug.; Treatment: if the drug has been taken recently - gastric lavage and taking of absorbing agents; in violation of AV-conduction and / or bradycardia - in / in the introduction of 1-2 mg of atropine, epinephrine (adrenaline) or staging a temporary pacemaker; with a decrease in blood pressure of the patient should be transferred to the Trendelenburg position. If there are no signs of pulmonary edema - in / in plasma-substituting solutions, with the ineffectiveness - the introduction of epinephrine, dopamine, dobutamine; in acute heart failure - cardiac glycosides, diuretics; with convulsions - in / in diazepam; with bronchospasm - inhalation or parenteral beta2-adrenomimetiki.
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 the CYP2D6 isoenzyme.Drugs that inhibit or induce CYP2D6 activity can affect plasma concentration of metoprolol. Sn (derivatives of barbituric acid, rifampicin) reduce the concentration of metoprolol in the blood plasma.; Simultaneous administration of metoprolol with cardiac glycosides, clonidine, slow calcium blockers nadel (verapamil, diltiazem), amiodarone, class I antiarrhythmic drugs, general anesthesia, methyldopa, guanfacin can lead to a decrease in blood pressure and severe bradycardia. and the development of arterial hypotension. Simultaneous IV injection of verapamil may provoke cardiac arrest.; NSAIDs and beta-adrenomimetics weaken the antihypertensive effect of beta-adrenoblokato s;. Ergot alkaloids while the use of metoprolol increase the risk of peripheral circulatory disorders;. When co-administered metoprolol with oral hypoglycemic drugs may reduce the effect; with insulin - increased risk of hypoglycemia, lengthening and increasing its severity, masking some of the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure) .; Metoprolol reduces the clearance of xanthines (except diafillin), especially in patients with initially increased clearance of theophylline under the influence of smoking .; Metoprolol reduces lidocaine clearance, increases the concentration of lidocaine in plasma.; Metoprolol strengthens and prolongs the action of non-depolarizing muscle relaxants; prolongs the anticoagulant effect of coumarins. With simultaneous administration of epinephrine (adrenaline) with beta-blockers, it is possible to increase blood pressure and bradycardia.; Phenylpropanolamine (norephedrine) with simultaneous use with metoprolol may increase diastolic blood pressure.; samples when combined with metoprolol increase the risk of systemic allergic reactions oranaphylaxis.; Iodine-containing radiopaque agents for iv administration when combined with metoprolol increase the risk of anaphylactic reactions.; When metoprolol is used together with ethanol, the risk of pronounced decrease in blood pressure increases.
special instructions
Monitoring patients taking beta-blockers includes regular monitoring of heart rate and blood pressure. Patients should be trained in the method of counting heart rate and instructed on the need for medical consultation with a heart rate less than 50 bpm; Increased severity of allergic reactions is possible (against the background of burdened allergological anamnesis) and lack of effect from the administration of usual doses of epinephrine (adrenaline) .; In elderly patients It is recommended that kidney function be monitored (once every 4-5 months). Taking Metoprolol Retard-Akrikhin can intensify the symptoms of impaired peripheral arterial circulation. Ia selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats / min.; In smoking patients, the effectiveness of beta-adrenergic blockers is lower.; Metoprolol retard-Akrikhin may mask some clinical manifestations thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated because it can increase symptoms. In diabetes mellitus, taking Metoprolol Retard-Akrikhin can mask tachycardia caused by hypoglycemia. with pheochromocytoma - alpha-adrenergic blockers. If surgery is necessary, an anesthesiologist should be warned about taking the drug Metoprolol Retard-Akrikhin (you need to choose a remedy for general anesthesia with minimal negative inotropic effect), it is not recommended to remove the drug.; eliminate intravenous injection of atropine (1-2 mg); in case of increasing bradycardia (less than 50 beats / min), hypotension (systolic blood pressure below 100 mm Hg), AV blockade s, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction, reduce the dose or discontinue treatment; It is recommended to stop therapy when skin rashes appear and the development of depression caused by beta-adrenergic blockers.; With the abrupt cancellation of clonidine, the blood pressure may rise sharply receiving beta-blockers.In the case of clonidine withdrawal, discontinuation of beta-blockers should be started a few days before clonidine is canceled. Preparations that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, therefore patients taking such combinations of drugs should be under constant medical observation to detect excessive reduction of blood pressure or bradycardia. With a sudden cessation of treatment, withdrawal syndrome may occur (increased angina attacks, increased blood pressure). Particular attention in case of drug withdrawal should be given to patients with angina, chronic heart failure, after myocardial infarction. Cancellation of the drug Metoprolol Retard-Akrikhin is carried out gradually, reducing the dose for 10 days.; Patients using contact lenses should take into account that during treatment with beta-adrenergic blockers, the production of tear fluid can be reduced.; Influence on the ability to drive vehicles and control mechanisms; During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed. ktsy.