Metoprolol MB extended release capsules 50mg №10×3

Name:
Metoprolol MV caps. with prolonged release 50 mg in a 10×3 box
Description:
Metoprolol MV 50 mg: Hard gelatin capsules, cylindrical in shape with hemispherical ends of white color. The main active ingredient Metoprolol Release formCapsules with prolonged release. Dosage 50 mg Pharmacodynamics Metoprolol is a cardioselective lipophilic ?1-blocker that does not have its own sympathomimetic and membrane stabilizing effect. Metoprolol has antihypertensive, antianginal and antiarrhythmic effects, prevents the stimulating effect of the sympathetic nervous system on the heart and causes a rapid decrease in heart rate and cardiac output. In hypertension, metoprolol lowers blood pressure in patients standing and lying down. The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance. Long-term use of immediate-release metoprolol in hypertension leads to a statistically significant decrease in left ventricular weight and improvement in its diastolic function. Metoprolol reduces plasma renin activity, both with short-term and long-term use. This effect can be explained to some extent by downregulation of renal α1 receptors, which leads to a decrease in renin production and a corresponding decrease in angiotensin-mediated vasoconstriction. Metoprolol reduces myocardial oxygen demand by reducing the frequency and strength of heart contractions, lowering systemic blood pressure. By reducing the heart rate and, accordingly, lengthening the diastole, metoprolol in angina pectoris improves blood supply and oxygenation of ischemic areas of the myocardium. Thus, the drug reduces the frequency, duration and severity of angina attacks and asymptomatic manifestations of ischemia, and also increases the physical performance of patients. With myocardial infarction. The use of the drug in the complex therapy of myocardial infarction reduces the likelihood of a recurrent infarction. At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than those of non-selective ?-blockers. Compared with non-selective ?-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism. It does not significantly alter the cardiovascular response to hypoglycemia and does not increase the duration of hypoglycemic episodes. Pharmacokinetics Absorption and distribution Metoprolol succinate is almost completely (about 95%) absorbed in the gastrointestinal tract. After absorption, metoprolol is largely metabolized by first pass through the liver. The bioavailability of the drug is approximately 30-40%. Due to metabolism by polymorphic enzymes, the concentration of metoprolol in the blood plasma is subject to significant individual fluctuations (can vary up to 17 times). The duration of the therapeutic effect after taking the drug Metoprolol MB is more than 24 hours, while a constant release rate of the active substance is achieved for 20 hours. The elimination half-life averages 3.5 hours. The binding of metoprolol to plasma proteins is 10%. Metoprolol is widely distributed in tissues and has a large apparent volume of distribution (5.5 l/kg). Metabolism and excretion Metoprolol is metabolized in the liver by cytochrome P-450 enzymes. The three main metabolites do not have a clinically significant ?-blocking effect. Approximately 95% of the dose of the drug taken orally is excreted by the kidneys, of which about 10% is unchanged, the rest of the dose of the drug is excreted as metabolites. Indications for use Arterial hypertension. Angina pectoris. Chronic heart failure in the compensation stage in addition to standard therapy (for example, in combination with diuretics, ACE inhibitors, cardiac glycosides). Maintenance therapy after myocardial infarction for the purpose of secondary prevention. Cardiac arrhythmias, including supraventricular tachycardia , a decrease in the frequency of ventricular contraction during atrial fibrillation and ventricular extrasystoles. Functional disorders of cardiac activity, accompanied by tachycardia. The capsule should be swallowed whole with a liquid. Eating does not affect the bioavailability of the drug. When selecting a dose, it is necessary to avoid the development of bradycardia. Arterial hypertension The recommended initial dose for arterial hypertension is 50 mg once a day. If there is insufficient clinical effect, the daily dose can be gradually increased to 100 mg or 200 mg, or used in combination with another antihypertensive agent. Angina The recommended starting dose for angina is 50 mg once daily. If the clinical effect is insufficient, the daily dose can be gradually increased to 100 mg or 200 mg, or another antianginal agent can be added. Compensated chronic heart failure Patients with heart failure stabilized with other drugs (i.e. without episodes of exacerbation of heart failure during the last 6 weeks on the background of the main therapy, without changes in it for at least the last two weeks), dose metoprolol is selected individually. In NYHA class II patients, the recommended starting dose of metoprolol for the first two weeks is 25 mg once daily. In patients belonging to the functional class III-IV according to the NYHA classification, the recommended initial dose for the first two weeks is 12.5 mg once a day. In patients in NYHA functional class II, after two weeks the daily dose can be increased to 50 mg, then after two weeks to 100 mg and after another two weeks to 200 mg. In more severe heart failure (NYHA functional class III-IV), the dose of metoprolol can be increased to 25 mg once a day, then every two weeks the dose can be doubled until a maximum tolerated dose of 200 mg once a day is reached. In long-term treatment, the target dose is to achieve the maximum tolerated dose of metoprolol 200 mg once daily. In terms of dose tolerance, the condition of patients after each new dose should be carefully evaluated. With the development of hypotension and / or bradycardia, it may be necessary to lower the doses of both metoprolol and concomitant therapy. The development of hypotension at the beginning of treatment or a transient worsening of the symptoms of heart failure does not necessarily mean that the patient does not tolerate this dose during chronic treatment. Such patients – against the background of careful monitoring of kidney function – should lower the dose of the drug until their condition stabilizes. There may be cases when it becomes necessary to lower the dose or discontinue the drug. At the beginning of treatment, when using low doses, the use of other long-acting metoprolol preparations is recommended, it is possible to use immediate-release metoprolol preparations. Cardiac arrhythmias 100-200 mg Metoprolol MB once a day. Maintenance treatment after myocardial infarction The usual maintenance dose is 200 mg once daily. Functional disorders of cardiac activity, accompanied by tachycardia 100 mg Metoprolol MB once a day. If necessary, the dose can be increased to 200 mg per day. Prevention of migraine attacks 100-200 mg Metoprolol MB once a day. Special groups of patients Impaired renal function. There is no need to adjust the dose in patients with impaired renal function. Liver dysfunction. Usually, due to the low degree of binding to plasma proteins, dose adjustment of metoprolol is not required. However, in severe hepatic impairment (in patients with severe liver cirrhosis or portocaval anastomosis), a dose reduction may be required. Elderly patients. There is no need to adjust the dose in elderly patients. Children. Clinical experience with metoprolol in children is limited. Use during pregnancy and lactation Metoprolol MB 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. Like other antihypertensive agents, ?-blockers can cause side effects, for example, bradycardia in the fetus, newborns or children who are breastfed. The amount of metoprolol excreted in breast milk and the β-blocking effect in a breastfed child (when the mother takes metoprolol in therapeutic doses) are insignificant. Influence on the ability to drive vehicles or potentially dangerous mechanisms When driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions, it should be borne in mind that dizziness and fatigue may occur when using Metoprolol MV. Precautions With extreme caution, Metoprolol MB should be prescribed for bronchial asthma and chronic obstructive pulmonary disease, peripheral arterial circulation disorders, pheochromocytoma, diabetes mellitus, myasthenia gravis, atrioventricular block I degree, depression (including history), severe renal failure, severe hepatic insufficiency. It is not advisable to prescribe ?-blockers to patients who need constant treatment with inotropic agents (?-agonists). When prescribing the drug Metoprolol MB, heart rate, blood pressure, blood glucose levels in diabetic patients should be regularly monitored, and liver function should be periodically monitored in elderly patients. The patient should be taught how to calculate heart rate and instructed to consult a doctor if the heart rate drops below 50 beats per minute. In patients taking metoprolol, there may be an increase in the severity of hypersensitivity reactions and the absence of a therapeutic effect from the administration of usual doses of epinephrine. Metoprolol may exacerbate existing bradycardia. In very rare cases, pre-existing moderate atrioventricular conduction disturbances may worsen, sometimes with the development of atrioventricular block. Metoprolol may increase the symptoms of peripheral arterial circulation disorders. Appointment of the drug Metoprolol MB in patients with heart failure is possible only after reaching the stage of compensation. Although the effect of cardioselective ?-blockers on respiratory function is weaker than non-selective ?-blockers, it is recommended to limit their use to patients with chronic obstructive airway diseases. If it is necessary to prescribe metoprolol to patients with bronchial asthma, it may be necessary to simultaneously use ?2-agonists (in tablets and / or in the form of an aerosol) or change (increase) the dose of previously used ?2-agonists. In the treatment of patients with pheochromocytoma, metoprolol should be combined with ?-blockers. Selective ?1-blockers have little effect on carbohydrate metabolism, but they can mask the symptoms of hypoglycemia, therefore, if Metoprolol MB is prescribed, patients with diabetes mellitus should more often check the state of carbohydrate metabolism and, if necessary, specify the dose of insulin or oral antidiabetic agents. Metoprolol may mask tachycardia as a clinical manifestation of hyperthyroidism. Patients using contact lenses should take into account that against the background of treatment with ?-blockers, a decrease in the production of lacrimal fluid is possible. In patients with cirrhosis of the liver, the bioavailability of the drug may increase. Do not abruptly stop taking the drug. Metoprolol MB should be discontinued gradually, by stepwise dose reduction over 7-14 days. Abrupt withdrawal may increase the symptoms of angina pectoris and increase the risk of coronary disorders and the development of myocardial infarction, and in patients with thyrotoxicosis, tachycardia and arrhythmias. Patients with coronary artery disease require special attention during drug withdrawal. Before surgery and anesthesia, the anesthesiologist should be warned that the patient is taking metoprolol, but it is not recommended to stop treatment with Metoprolol MB. If treatment with Metoprolol MB must nevertheless be discontinued due to surgery, this should be done at least 48 hours before surgery, except in special cases such as thyrotoxicosis and pheochromocytoma. The use of ?-blockers before surgery can reduce arrhythmogenic effects during the intervention and prevent a decrease in coronary circulation during surgical stress, which causes a predominance of sympathetic tone. If a ?-blocker is prescribed for the above reasons, a general anesthetic with minimal negative inotropic effect should be used to reduce the risk of myocardial depression. Patients with rare hereditary disorders of fructose tolerance, malabsorption of glucose-galactose, and in the absence of sucrase-isomaltase should not take this drug. Interactions 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. The combined use of metoprolol MB with the following drugs should be avoided: Barbituric acid derivatives: barbiturates (the study was conducted with pentobarbital) increase the metabolism of metoprolol, due to the induction of enzymes. 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 ?-blocker, the joint appointment of metoprolol and propafenone does not seem appropriate. Verapamil: The combination of ?-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and ?-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function. The combination of the drug Metoprolol MB with the following drugs may require dose adjustment: 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 antiarrhythmics: Class I antiarrhythmics and ?-blockers may result in a negative inotropic effect that 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 ?-blockers. This interaction has been documented for indomethacin. Probably, the described interaction will not be observed when interacting with sulindac. Negative interactions have been noted in studies with diclofenac. 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 ?-blockers mutually enhance 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 hypertension and bradycardia have been reported in patients taking non-selective ?-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. It is assumed that this risk is much lower with the use of cardioselective ?-blockers. Phenylpropanolamine: Phenylpropanolamine (norephedrine) at 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, ?-blockers can cause reactions of paradoxical arterial hypertension 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 ?-blockade. It is believed that such an interaction is also characteristic of other ?-blockers, in the metabolism of which cytochrome P4502D6 is involved. Clonidine: Hypertensive reactions with abrupt withdrawal of clonidine may be exacerbated by the combined use of ?-blockers. When used together, in the event of clonidine withdrawal, discontinuation of ?-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 simultaneously taking metoprolol and other ?-blockers (eye drops) or monoamine oxidase inhibitors (MAOIs) should be closely monitored. Against the background of taking ?-blockers, inhalation anesthetics increase the cardiodepressive effect. Against the background of taking β-blockers, patients receiving hypoglycemic agents for oral administration 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 ?-blockers, can increase the time of atrioventricular conduction and cause bradycardia. Contraindications Hypersensitivity to metoprolol or any other component of the drug, or to other ?-blockers. Atrioventricular block II and III degree. Decompensated heart failure resistant to the usual treatment. Severe sinus bradycardia (heart rate less than 50 beats per minute). Prinzmetal’s angina. Cardiogenic shock. Severe arterial hypotension (systolic blood pressure below 100 mm Hg). Acute myocardial infarction with: heart rate less than 45 beats per minute; systolic blood pressure below 100 mm Hg, moderate and severe cardiac insufficiency); prolongation of the PQ interval for more than 0.24 seconds; severe heart failure; atrioventricular block II or III degree. Severe disorders of the peripheral arterial circulation. Severe bronchial asthma, severe chronic obstructive pulmonary disease. Poorly controlled diabetes mellitus. Metabolic acidosis. Uncompensated I pheochromocytoma. Severe peripheral vascular diseases with the threat of gangrene. Long-term or intermittent therapy with inotropic agents and acting on α-adrenergic receptors. Simultaneously with intravenous administration of calcium channel blockers such as verapamil and diltiazem or other antiarrhythmic drugs (disopyramide). Simultaneously with drugs from the group of MAO inhibitors. Psoriasis. Age up to 18 years (efficacy and safety have not been established). Composition One capsule of Metoprolol MB 50 mg contains: active substance: metoprolol succinate (pellets 60%) – 47.5 mg, which corresponds to 50 mg of metoprolol tartrate; excipients: microcrystalline cellulose spheres (60-80#), anhydrous colloidal silicon dioxide, hypromellose (HPMC E5), sucrose, ethyl cellulose N-50, stearic acid, polyethylene glycol (6000). composition of the hard gelatin capsule: gelatin, titanium dioxide (E 171). Overdose Overdose in humans has been observed in very rare cases. Symptoms: with an overdose of metoprolol, the most serious symptoms are from the cardiovascular system, however, sometimes, especially in children and adolescents, symptoms from the central nervous system and suppression of pulmonary function, bradycardia, AV blockade of I-III degree, asystole, a pronounced decrease in blood pressure may prevail , poor peripheral perfusion, heart failure, cardiogenic shock; depression of lung function, apnea, as well as increased fatigue, impaired consciousness, loss of consciousness, tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, esophageal spasm is possible, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia; effects on the kidneys; transient myasthenic syndrome; concomitant use of alcohol, antihypertensive drugs, quinidine or barbiturates may worsen the patient’s condition. The first signs of an overdose can be observed 20 minutes – 2 hours after taking the drug. Treatment: the appointment of activated charcoal, if necessary, gastric lavage. IMPORTANT! 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). If necessary, maintain airway patency (intubation) and adequate ventilation of the lungs. Replenishment of circulating blood volume and infusion of glucose. ECG control. Atropine 1.0-2.0 mg IV, if necessary, repeat the introduction (especially in the case of vagal symptoms). In the case of (suppression) depression of the myocardium, infusion administration of dobutamine or dopamine is indicated. You can also use glucagon 50-150 mcg/kg IV at intervals of 1 minute. In some cases, the addition of adrenaline to therapy may be effective. With arrhythmia and an extensive ventricular (QRS) complex, infusion solutions of sodium (chloride or bicarbonate) are administered. It is possible to install an artificial pacemaker. Cardiac arrest due to an overdose may require resuscitation for several hours. Terbutaline can be used to relieve bronchospasm (by injection or by inhalation). Symptomatic treatment is carried out. Side effects Metoprolol MB is well tolerated by patients, the side effects are mostly mild and reversible. 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), unknown (cannot be determined from the available data). Blood and lymphatic system disorders: very rarely - thrombocytopenia. Metabolic and nutritional disorders: infrequently - weight gain; very rarely - taste disturbances Disorders from the nervous system: very often - increased fatigue; often: dizziness, headache; rarely - increased nervous excitability, anxiety, impotence / sexual dysfunction; not often - paresthesia, convulsions, depression, weakening of attention, drowsiness or insomnia, nightmares; very rarely - amnesia / memory impairment, depression, hallucinations. On the part of the organ of vision: rarely - visual disturbances, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears. Disturbances from the organ of hearing and the vestibular apparatus: very rarely - ringing in the ears. Heart disorders: often - bradycardia, palpitations; infrequently - a temporary increase in symptoms of heart failure, AV blockade of the first degree; cardiogenic shock in patients with acute myocardial infarction; rarely - other cardiac conduction disorders, arrhythmias. Vascular disorders: often - orthostatic hypotension (very rarely accompanied by fainting), cold extremities; very rarely - gangrene in patients with previous severe disorders of the peripheral circulation. Respiratory, thoracic and mediastinal disorders: often - shortness of breath with physical effort; not often - bronchospasm; rarely - rhinitis. Gastrointestinal disorders: often - nausea, pain in the abdomen, diarrhea, constipation; not often - vomiting; rarely - dry mouth. Liver and biliary tract disorders: rarely - liver dysfunction; very rarely - hepatitis. Skin and subcutaneous tissue disorders: infrequently - rash (in the form of urticaria), excessive sweating; rarely - hair loss; very rarely: photosensitivity, exacerbation of psoriasis. Musculoskeletal and connective tissue disorders: very rarely - arthralgia. 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 MB extended release capsules 50mg No. 10x3