Metoprolol tablets 100mg №10×3

NameMetoprolol tablets 100mg in a 10×3 box. The main active ingredient is metoprolol. Release form Tablets. Dosage 100 mg Pharmacodynamics Metoprolol is a beta-blocker. It has no intrinsic sympathomimetic activity. Increased blood pressure decreases both in the standing position and in the supine position. Does not cause orthostatic hypotension and does not affect the electrolyte composition of the blood. It has antianginal, antihypertensive and antiarrhythmic effects. Reduces the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress, leads to a decrease in heart rate, myocardial contractility, cardiac output. In the first days of use, the drug increases OPSS, which normalizes or even decreases with prolonged use. Reduces myocardial oxygen demand (due to a decrease in heart rate and a decrease in myocardial contractility), reduces the number and severity of angina attacks and increases exercise tolerance. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia, functional heart disease and hyperthyroidism, it slows down the heart rate and can lead to the restoration of sinus rhythm. The antiarrhythmic effect is due to a decrease in the rate of spontaneous excitation of the sinus and ectopic pacemaker and a slowdown in AV conduction. Prevents the development of headache of vascular origin. To a lesser extent than non-selective beta-blockers, it affects the release of insulin and carbohydrate metabolism, masks the symptoms of hypoglycemia in patients with diabetes mellitus, increases blood triglycerides, reduces the content of free fatty acids and high density lipoproteins. Pharmacokinetics Absorption and distribution After oral administration, metoprolol is almost completely (approximately 95%) absorbed from the gastrointestinal tract. The maximum plasma concentration is reached after 1.5-2 hours. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with multiple doses. Simultaneous food intake can increase the bioavailability of metoprolol by 30-40%. Plasma protein binding – 10%. Penetrates through the BBB and the placental barrier, excreted in breast milk. Metoprolol is widely distributed in tissues and has a large volume of distribution (5.6 l/kg). Metabolism and excretion Metoprolol is extensively biotransformed in the liver to form inactive metabolites. The plasma half-life is 1 to 9 hours (mean 3.5 hours). The total clearance of the drug is about 1 l / min. It is excreted mainly by the kidneys (95%), about 5% – unchanged, the rest – in the form of metabolites. Separate groups of patients Significant differences in the pharmacokinetics of metoprolol in elderly patients have not been identified. In case of impaired renal function, the excretion of metabolites decreases and the excretion of unchanged metoprolol practically does not change. In severe renal failure (GFR 5 ml / min), there is a significant accumulation of metabolites, but the degree of beta-adrenergic blockade does not increase. Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and/or after a porto-caval shunt, bioavailability may increase and overall clearance may decrease. After porto-caval shunting, the total clearance of the drug is approximately 0.3 l / min, and the area under the concentration-time curve increases by about 6 times compared with healthy individuals. Indications for use Arterial hypertension. Angina pectoris. Stable symptomatic chronic heart failure with impaired systolic function of the left ventricle (as adjuvant therapy to the main treatment of chronic heart failure). Reducing mortality and the frequency of re-infarction after the acute phase of myocardial infarction. , reduction in the frequency of ventricular contraction during atrial fibrillation and ventricular extrasystoles. Functional disorders of cardiac activity, accompanied by tachycardia. Prevention of migraine attacks. As an adjuvant for hyperthyroidism. Tablets are taken orally during or after meals, without chewing and drinking plenty of drinking water. During the dose selection period, heart rate should be monitored to prevent bradycardia. The duration of the course of therapy is set by the doctor individually and depends on the characteristics of the course of the disease. If, after prolonged use of the drug, discontinuation of treatment is required, then this should be done gradually and slowly, since a sudden withdrawal of the drug can lead to a sharp increase in blood pressure. Arterial hypertension. With moderate to moderate arterial hypertension, the initial dose is 25-50 mg twice a day (morning and evening). If necessary, the daily dose can be gradually increased to 200 mg (100 mg in the morning and evening) or another antihypertensive agent can be added. Angina. The initial dose is 25-50 mg two to three times a day. Depending on the effect, this dose can be gradually increased to 200 mg per day in two doses or another antianginal drug can be added. Secondary prevention of myocardial infarction. The usual dose is 50-100 mg twice a day (morning and evening). Arrhythmias. The initial dose is 25-50 mg two to three times a day. If necessary, the daily dose can be gradually increased to 200 mg or another antiarrhythmic agent can be added. Hyperthyroidism. The dose should be set individually. Recommendations for use: at the beginning of treatment, 50 mg 3-4 times a day; the dose can be increased to 100 mg 3-4 times a day if the heart rate is higher than 75 beats / minute after 3-4 days of treatment with the initial dose of the drug. In hyperthyroidism, the biotransformation of metoprolol is increased, so it may be necessary to use a higher dose of the drug. The drug is usually used during the period of withdrawal of another drug. Functional disorders of the heart, accompanied by tachycardia. The usual dose is 50 mg twice a day (morning and evening); if necessary, a single dose can be increased to 100 mg, while maintaining the same regimen. Prevention of migraine attacks. The usual dose is 50 mg twice a day (morning and evening); if necessary, it can be increased to 100 mg per day. Special groups of patients Impaired renal function. Changing the dosage of the drug in case of impaired renal function is not required. Liver dysfunction. In patients suffering from liver disease, metoprolol is prescribed in the same doses as in patients whose liver function is not impaired. However, in case of significant impairment of liver function (for example, after bypass surgery), it may be necessary to reduce the dose of metoprolol. Elderly patients. Dose adjustment is not required. Children. Clinical experience with metoprolol in children is limited. Use during pregnancy and lactation Metoprolol should not be administered during pregnancy and during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or child. Pregnancy Beta-adrenergic drugs can impair placental perfusion and cause fetal death and preterm labor. Fetal growth retardation has been observed after long-term use of metoprolol in pregnant women with mild to moderately elevated blood pressure. Beta-adrenolytic drugs can prolong labor and cause bradycardia in the fetus and newborn. There are also reports of the appearance of hypoglycemia, hypotension, increased bilirubinemia, as well as a difficult reaction to tissue hypoxemia in the newborn. Treatment with the drug must be interrupted 48-72 hours before the planned date of delivery. When this is not possible, the newborn should be monitored for 48-72 hours after birth for subjective and objective symptoms of beta-adrenergic receptor blocking (eg, cardiac and pulmonary complications). Breast-feeding The concentration of metoprolol in milk is approximately three times greater than in blood plasma. Despite the fact that after the use of the drug in therapeutic doses, the risk of harmful effects on an infant is small (except for people with a slow metabolism), an infant who is breastfed should be monitored for signs of blocking beta-adrenergic receptors. Influence on the ability to drive vehicles or potentially dangerous mechanisms Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention. During treatment with metoprolol, dizziness and increased fatigue may occur, so patients should evaluate their reaction to the drug before driving a car or servicing mechanical devices in motion. The symptoms described may be exacerbated by the simultaneous use of alcohol or after changing medications. Precautions In the event of an increase in bradycardia, the dose of the drug must be reduced or the drug discontinued, gradually reducing the dose. Beta-adrenolytic drugs should be used with caution in patients with asthma. If a patient with asthma takes a beta2-adrenomimetic drug (in the form of tablets or inhalations), in this case, when starting treatment with metoprolol, the dose of beta2-adrenergic agonist should be monitored and increased if necessary. Metoprolol may impair glycemic control in the treatment of diabetes mellitus and mask signs of hypoglycemia. In patients with non-insulin-dependent diabetes mellitus, plasma glucose levels should be monitored. Atrioventricular conduction disturbances may occasionally be exacerbated during treatment with metoprolol (possibility of atrioventricular block). Metoprolol can exacerbate peripheral arterial disease such as intermittent claudication. In Prinzmetal’s angina, beta-blockers may increase the number and duration of attacks. In patients with psoriasis while taking metoprolol, an exacerbation of the disease is possible. Beta-adrenergic drugs may exacerbate the symptoms of psoriasis or cause it to reappear. In the case when metoprolol is prescribed for patients with tumors emanating from chromaffin tissue (pheochromocytoma), it is necessary to first apply the alpha-adrenolytic drug and continue its use simultaneously with metoprolol. Treatment with metoprolol may mask signs of hyperthyroidism. When conducting general anesthesia while taking beta-blockers, the risk of arterial hypotension increases. If surgical intervention is necessary, the anesthesiologist should be warned about the therapy being carried out in order to select an anesthetic agent with a minimal negative inotropic effect, however, discontinuation of the drug before surgery in patients with coronary artery disease is not recommended. Before conducting a radiological study with iodine-containing contrast agents, treatment with metoprolol should be stopped in advance. In cases where the use of metoprolol is absolutely necessary and cannot be canceled, it is necessary to prescribe appropriate treatment. High doses of metoprolol should be avoided immediately without prior titration in patients undergoing non-cardiac surgery, as in patients with cardiovascular risk factors this has been associated with bradycardia, arterial hypotension and stroke, including death. As well as other beta-adrenolytic drugs, metoprolol can increase both sensitivity to allergens and exacerbate anaphylactic reactions. Adrenaline does not always give the desired therapeutic result in patients treated with beta-adrenergic drugs. Patients with severely impaired renal function, with serious acute conditions accompanied by metabolic acidosis, and patients receiving combined treatment with digitalis preparations should be given special attention. For the elderly, the drug is prescribed with caution in low doses and under constant medical supervision with regular monitoring of renal function. Patients using contact lenses should take into account that against the background of treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible. Metoprolol contains lactose monohydrate. It should not be given to patients with rare hereditary problems of galactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome. Interaction with other drugs Metoprolol is a CYP2D6 substrate, and therefore, drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) may affect the plasma concentration of metoprolol tartrate. The co-administration of Metoprolol with the following medicinal products should be avoided Barbituric acid derivatives. Barbiturates increase the metabolism of metoprolol due to enzyme induction. Propafenone. When propafenone was administered to four patients treated with metoprolol, there was an increase in the plasma concentration of metoprolol by 2-5 times, while two patients had side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. Probably, the interaction is due to inhibition by propafenone, like quinidine, of the metabolism of metoprolol through the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a beta-blocker, the co-administration of metoprolol and propafenone does not seem appropriate. Verapamil. The combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function. The combination of Metoprolol with the following drugs may require dose adjustment of Amiodarone. The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia. Given the extremely long half-life of amiodarone (50 days), the potential for interactions long after amiodarone withdrawal should be taken into account. Class I antiarrhythmic drugs. Class I antiarrhythmics and beta-blockers can lead to a cumulative negative inotropic effect, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with sick sinus syndrome and impaired AV conduction. The interaction is described on the example of disopyramide. Non-steroidal anti-inflammatory drugs (NSAIDs). NSAIDs weaken the antihypertensive effect of beta-blockers. Research has focused mainly on indomethacin. This action will not occur when interacting with sulindac. In studies with diclofenac, no such interaction was found. Diphenhydramine. Diphenhydramine reduces the clearance of metoprolol to ?-hydroxymetoprolol by 2.5 times. At the same time, there is an increase in the action of metoprolol. Diltiazem: Diltiazem and beta-blockers mutually reinforce the inhibitory effect on AV conduction and sinus node function. When metoprolol was combined with diltiazem, there were cases of severe bradycardia. epinephrine. 10 cases of severe arterial hypertension and bradycardia have been reported in patients taking non-selective beta-blockers (including pindolol and propranolol) and receiving epinephrine. The interaction was also noted in the group of healthy volunteers. It is assumed that similar reactions can be observed when using epinephrine in conjunction with local anesthetics in case of accidental entry into the vascular bed. This risk is expected to be much lower with cardioselective beta-blockers. Phenylpropanolamine. Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, beta-blockers may cause paradoxical hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported while taking phenylpropanolamine. Quinidine. Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation, causing mainly a significant increase in the plasma concentration of metoprolol and an increase in beta-blockade. It is believed that a similar interaction is also characteristic of other beta-blockers, in the metabolism of which cytochrome P4502D6 is involved. Clonidine. Hypertensive reactions with abrupt withdrawal of clonidine may be aggravated by the combined use of beta-blockers. When used together, if clonidine is discontinued, discontinuation of beta-blockers should begin a few days before clonidine is discontinued. Rifampicin. Rifampicin may increase the metabolism of metoprolol, decreasing the plasma concentration of metoprolol. Patients concomitantly taking metoprolol and other beta-blockers (eye drops) or monoamine oxidase inhibitors should be closely monitored. Against the background of taking beta-blockers, inhalation anesthetics increase the cardiodepressive effect. Against the background of taking beta-blockers, patients receiving oral hypoglycemic agents may require dose adjustment of the latter. The plasma concentration of metoprolol may increase when taking cimetidine or hydralazine. Cardiac glycosides, when used together with beta-blockers, can increase the time of atrioventricular conduction and cause bradycardia. Metoprolol may cause a decrease in the withdrawal of other drugs (eg, lidocaine). Contraindications Hypersensitivity to metoprolol tartrate, other beta-adrenergic drugs or any other excipients. Blockade of the atrioventricular node of the second or third degree. Heart failure in the stage of decompensation (pulmonary edema, circulatory disorders or hypotension) and continuous or intermittent use of drugs that increase myocardial contractility (agonists of beta-adrenergic receptors). Symptomatic and clinical sinus bradycardia (heart rate <50/min). Sick sinus syndrome. Cardiogenic shock. Prinzmetal's angina. Severe disorders of the peripheral arterial circulation. Hypotension (systolic pressure <90 mm Hg). metabolic acidosis. Severe bronchial asthma or chronic obstructive pulmonary disease. Simultaneous use of monoamine oxidase inhibitors (with the exception of MAO-B inhibitors). Severe peripheral vascular disease with gangrene threat. Age up to 18 years (efficacy and safety not established). Metoprolol should not be administered to patients with suspected acute myocardial infarction and heart rate less than 45 beats/min, PQ interval>0.24 seconds, or systolic pressure <100 mm. rt. Art. Metoprolol should not be used in patients with heart failure and recurrent systolic blood pressure less than 100 mm. rt. Art. (examination before treatment is indicated). Contraindicated (with the exception of the intensive care unit) the simultaneous administration of intravenous drugs that block calcium channels, such as verapamil or diltiazem, or other antiarrhythmic drugs (such as disopyramide). Composition Each tablet contains: active substance: metoprolol tartrate - 100 mg; excipients: anhydrous colloidal silicon dioxide, microcrystalline cellulose, sodium starch glycolate (type A), talc, magnesium stearate, lactose monohydrate. Overdose Symptoms: hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase with the simultaneous use of alcohol, antihypertensive drugs, quinidine and barbiturates. The first symptoms of an overdose appear 20 minutes - 2 hours after taking the drug. Treatment: Intensive care and monitoring of the patient's vital functions (circulation and respiration, kidneys, glycemia, serum electrolytes) is necessary. If the drug was taken not too long ago, gastric lavage is mandatory, if lavage is not possible and the patient is conscious, vomiting can be induced (in the presence of medical personnel), followed by the introduction of activated charcoal and an osmotic laxative. Atropine (0.25–0.5 mg IV for adults, 10–20 mcg/kg for children) should be given before gastric lavage (due to the risk of vagus nerve stimulation). In severe hypotension, bradycardia and the threat of heart failure, beta1-agonists (dobutamine) should be administered intravenously at intervals of 2 to 5 minutes or by infusion until the desired effect is achieved. In the absence of selective beta1-agonists, intravenously administer atropine or dopamine. In the absence of the desired effect, it is possible to use other adrenomimetics (isoprenaline or norepinephrine). The introduction of glucagon in doses of 1-10 mg is useful in achieving reversibility of the effects of blockade of beta receptors. With severe bradycardia that is resistant to pharmacotherapy, implantation of a pacemaker may be required. Bronchospasm can be relieved by intravenous administration of a beta2-agonist (eg, salbutamol or terbutaline). These antidotes can be used in doses higher than therapeutic. Hemodialysis is ineffective. Side effect The frequency of adverse reactions indicated below was determined using the following note: very often (> 1/10), often (> 1/100 – < 1/10), infrequently (> 1/1.000 – < 1/100), rarely (> 1/10.000 – < 1/1.000), very rare (< 1/10.000), not known (cannot be determined from the available data). Blood and lymphatic system disorders: very rarely - thrombocytopenia, leukopenia. Endocrine system disorders: rarely - exacerbation of latent diabetes mellitus. Metabolic and nutritional disorders: infrequently - weight gain. Mental disorders: infrequently - depression, weakening of concentration, drowsiness or insomnia, nightmares; rarely - nervousness, tension; very rarely - forgetfulness or memory loss, confusion, hallucinations, personality changes (for example, mood changes). Nervous system disorders: often - dizziness, headaches; infrequently - paresthesia. On the part of the organ of vision: rarely - visual disturbances, dry or irritated eyes, conjunctivitis. Disturbances from the organ of hearing and the vestibular apparatus: often - balance disorders (along with loss of consciousness); very rarely - tinnitus, hearing impairment. Heart disorders: often - bradycardia, tachycardia; infrequently - transient exacerbation of symptoms of heart failure, blockade of the atrioventricular node of the 1st degree, pain behind the sternum, cardiogenic shock in patients with acute myocardial infarction; rarely - functional signs of cardiac dysfunction, heart rhythm disturbances, cardiac conduction disturbances. Vascular disorders: often - a pronounced decrease in blood pressure and orthostatic hypotension, very rarely with loss of consciousness; infrequently - cold palms and feet; very rarely - necrosis in patients with severe peripheral vascular disease that occurs before treatment, capillary blood flow disorders or Raynaud's syndrome. Respiratory, thoracic and mediastinal disorders: often - shortness of breath; infrequently - bronchospasm; rarely - catarrhal phenomena. Gastrointestinal disorders: often - nausea, abdominal pain, diarrhea, constipation; infrequently - vomiting; rarely - dry mouth; very rarely - taste disorders. On the part of the liver and biliary tract: rarely - violations of liver tests; very rarely - hepatitis. Skin and subcutaneous tissue disorders: infrequently - rash (lichen-like urticaria and dystrophic skin changes), excessive sweating; rarely - hair loss; very rarely - reactions associated with increased sensitivity to light, exacerbation of scaly lichen, the appearance of scaly lichen, lichen-like changes on the skin. Musculoskeletal and connective tissue disorders: infrequently - muscle cramps; very rarely - joint pain, muscle weakness. Renal and urinary tract disorders: rarely - impotence and other sexual disorders, plastic induration of the penis (Peyronie's disease). General disorders and disorders at the injection site: very often - increased fatigue; infrequently - swelling. Storage conditions In a place protected from moisture and light at a temperature not exceeding 25? Keep out of the reach of children. Buy Metoprolol tablets 100mg No. 10x3 Price for Metoprolol tablets 100mg No. 10x3