Release form of Metoprolol
Metoprolol is available in tablet form for systemic treatment. The main substance is metoprolol tartrate, which can be contained in the amount of 25 mg, 50 mg or 100 mg in one tablet. Auxiliary components:
- magnesium stearate;
- silica;
- sodium carboxymethyl starch;
- microcrystalline cellulose.
The drug belongs to the cardioselective beta-blockers.
Metoprolol tablets: what for?
The main directions of action of Metoprolol include:
- antianginal;
- antiarrhythmic;
- hypotensive.
Taking the drug stabilizes blood pressure if it has been elevated as a result of stress or after physical exertion. In addition, due to the antianginal effect, excessive heart rate and myocardial demand for oxygen molecules are reduced.
As a result of a course of taking Metoprolol, the body's ability to tolerate physical activity increases, the risk of developing angina pectoris decreases, making attacks less frequent than before treatment. The medicine helps restore sinus rhythm, normalize heart rate, and prevent the development of migraines.
At small therapeutic doses, Metoprolol does not have a systemic effect on other organs, as well as on carbohydrate metabolism, unlike its analogues. Taking the drug for several years reduces the level of cholesterol in the blood.
Metoprolol-Teva
Monitoring of patients taking beta-blockers includes monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), blood glucose concentration in patients with diabetes (once every 4-5 months). The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50/min.
It is possible that the severity of allergic reactions may increase (against the background of a burdened allergic history) and there will be no effect from the administration of usual doses of epinephrine.
In elderly patients, it is recommended to monitor kidney function (once every 4-5 months). May increase symptoms of peripheral arterial circulation disorders. Patients with cardiac arrhythmias whose systolic blood pressure is below 100 mm Hg should be given IV only if special precautions are taken (there is a risk of a further decrease in blood pressure). The drug is discontinued gradually, reducing the dose over 10 days.
In case of arterial hypertension, the effect occurs after 2-5 days, a stable effect is observed after 1-2 months.
For exertional angina, the selected dose of the drug should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min. In smokers, the effectiveness of beta-blockers is lower.
In combination therapy with clonidine, the latter should be discontinued several days after metoprolol is discontinued in order to avoid a hypertensive crisis. At a dose above 200 mg/day, cardioselectivity decreases.
Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels.
If necessary, beta2-agonists are used as concomitant therapy for patients with bronchial asthma; for pheochromocytoma - alpha-blockers.
If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not recommended.
Reciprocal activation of the n.vagus can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.
If elderly patients develop increasing bradycardia (less than 50/min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction, it is necessary to reduce the dose or stop treatment . It is recommended to discontinue therapy if skin rashes appear and depression develops caused by taking beta-blockers.
The drug is discontinued gradually, reducing the dose over 10 days. If treatment is abruptly stopped, withdrawal syndrome may occur (increased angina attacks, increased blood pressure). When discontinuing the drug, special attention should be paid to patients with angina pectoris.
Patients who use contact lenses should take into account that during treatment with beta-blockers, the production of tear fluid may decrease.
During pregnancy, it is prescribed only for strict indications (due to the possible development of bradycardia, hypotension, hypoglycemia and respiratory paralysis in the newborn). Treatment must be interrupted 48-72 hours before delivery. In cases where this is not possible, it is necessary to ensure strict monitoring of newborns for 48-72 hours after delivery.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Metoprolol: instructions for use
Depending on the disease, a specific dose of the active substance is prescribed. For angina pectoris, take 50 mg three times a day. Tachyarrhythmia, Thyrotoxicosis, and hyperkinetic cardiac syndrome are treated with a single or double dose of the drug at a dosage of 50 mg.
To prevent migraines, take 25 mg of the drug every 4 hours during the day, but not more than 200 mg/day.
In case of myocardial infarction, a single dose is determined by the attending physician, who objectively assessed the patient’s condition. Important indications that influence the dose size are the pulse rate, the height of the heart muscle peaks on the ECG, as well as the level of blood pressure at the time of admission to the medical facility.
People aged 60+ are generally not recommended to start treatment with a dose exceeding 50 mg per day.
Metoprolol overdose
When taking any medication, you must follow the recommended dosage. Excessive use of Metoprolol leads to the following side effects:
- dizziness;
- a sharp decrease in blood pressure;
- arrhythmia;
- ventricular extrasystole;
- cardiogenic shock.
In addition, an overdose can lead to fainting, cardiac arrest or coma.
The fact that the patient took the medicine in a dose exceeding the norm can be guessed after 20 minutes by the symptoms. To save the patient, it is necessary to perform gastric lavage and give enterosorbent. If the patient's blood pressure drops below a critical level, dopamine and norepinephrine are used. An electrical stimulator can be installed using the transvenous method. If convulsions occur, diazepam is administered as a bolus. In case of severe bronchospasm caused by an overdose of Metoprolol, long- or short-acting beta-2 adrenergic agonists are used.
Metoprolol-Teva tablets 50 mg 30 pcs. in Moscow
Pharmacological action: Metoprolol is a cardioselective β1-adrenergic receptor blocker.
It has a slight membrane-stabilizing effect and does not have internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects.
By blocking β1-adrenergic receptors 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-, bathmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility). The total peripheral resistance at the beginning of the use of β 1-adrenergic blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of α-adrenergic receptors and the elimination of stimulation of β 2-adrenergic receptors), which after 1-3 days returns to the original one, and when Long-term use decreases.
The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (of great importance in patients with initial hypersecretion of renin) and the central nervous system, restoration of the sensitivity of the baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease blood pressure) and, ultimately, a decrease in peripheral sympathetic influences. Reduces high blood pressure (BP) at rest, during physical exertion and stress.
The antihypertensive effect develops quickly (systolic blood pressure decreases after 15 minutes, maximum after 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular use.
The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance. By increasing end-diastolic pressure in the left ventricle and increasing the stretch of ventricular muscle fibers, it can increase myocardial 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 content, arterial hypertension), a decrease in the rate of spontaneous excitation - sinus and ectopic pacemakers and a slowdown of atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node and along additional pathways).
With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and hyperthyroidism, it reduces the heart rate or can even lead to the restoration of sinus rhythm. Prevents the development of migraine.
When used in average therapeutic doses, in contrast to non-selective β-blockers, it has a less pronounced effect on organs containing β 2-adrenergic receptors (pancreas, skeletal muscles and smooth muscles of peripheral arteries, bronchi and uterus), and on carbohydrate metabolism. When used in large doses (more than 100 mg/day), it has a blocking effect on both subtypes of β-adrenergic receptors.
Pharmacokinetics:
Suction.
When taken orally, metoprolol is almost completely absorbed (about 95%) from the gastrointestinal tract. It undergoes intensive first-pass metabolism, so systemic bioavailability is about 35%. The maximum concentration in blood plasma is achieved 1.5-2 hours after administration.
Distribution.
The connection with blood proteins is 10%. Volume of distribution - 5.5 l/kg. Penetrates through the blood-brain and placental barriers. Excreted into breast milk in small quantities.
Metabolism.
Metoprolol is almost completely metabolized in the liver, mainly with the participation of the CYP2D6 isoenzyme. The half-life of metoprolol is 3 to 4 hours, but in slow metabolizers it can increase to 7 to 8 hours. Metabolites o-desmethylmetoprolol and a-hydroxymetoprolol have weak β-adrenergic blocking activity.
Excretion.
It is excreted primarily by the kidneys (about 95%), about 10% is excreted unchanged. Not excreted during hemodialysis.
In patients with liver cirrhosis and portocaval anastomosis, bioavailability increases and clearance decreases. In patients with portocaval anastomosis, the AUC (area under the concentration-time curve) may increase 6-fold, and clearance may decrease to 0.3 ml/min.
Side effects of Metoprolol
Taking Metoprolol in rare cases can cause a number of side effects:
- increased fatigue;
- drowsiness;
- decreased concentration;
- sleep disorders.
Less common are negative effects on the organ of vision: dry tear duct, dry eye syndrome and pain.
From the digestive tract - taste disturbance and decreased liver function. In addition, skin reactions in the form of photodermatosis also occur. If the patient has a manifestation of psoriasis on the skin, the affected area may increase or enter an acute stage. In some patients, the intensity of sweating increases.
From the respiratory system - nasal congestion, bronchospasm or shortness of breath appears.
Metoprolol-Teva tablet 50 mg x30
Trade name: Metoprolol-Ratiopharm International name: Metoprolol
Release forms: tablets 50, 100 mg (blisters)
Composition: metoprolol tartrate 50/100 mg
Pharmacological group: selective beta1-adrenergic blocker
Pharmacological group according to ATK: C07AB02 (Metoprolol)
Pharmacological action: antianginal, antiarrhythmic, selective beta-adrenergic blocking, hypotensive,
Indications: IHD, exertional angina, unstable angina, myocardial infarction (acute phase, as well as secondary prevention). Arterial hypertension, hypertensive crisis. CHF (compensated) in combination with diuretics, ACE inhibitors and cardiac glycosides. Rhythm disturbances (including during general anesthesia) - sinus tachycardia, ventricular and supraventricular arrhythmias (including supraventricular tachycardia, atrial fibrillation, atrial flutter, atrial tachycardia, tachyarrhythmias caused by digitalis, catecholamines, ventricular extrasystole, arrhythmias on background of mitral valve prolapse), congenital long QT syndrome. Thyrotoxicosis (complex therapy), withdrawal syndrome, migraine (prevention), tremor (essential, senile), anxiety (auxiliary treatment), akathisia against the background of antipsychotics.
Dosage regimen: Orally, with food or immediately after a meal, the tablets can be divided in half, but not chewed and washed down with liquid; for long-acting dosage forms - swallow whole, do not crush, do not break (except for metoprolol succinate and tartrate), do not chew. For arterial hypertension, the average dose is 100-150 mg/day in 1-2 doses, if necessary - 200 mg/day. For angina pectoris - 50 mg 2-3 times a day. For hyperkinetic cardiac syndrome (including thyrotoxicosis) - 50 mg 1-2 times a day. For tachyarrhythmia - 50 mg 2-3 times a day, if necessary - 200-300 mg/day. Secondary prevention of myocardial infarction - 200 mg/day. Prevention of migraine - 100-200 mg/day in 2-4 doses. To relieve paroxysmal supraventricular tachycardia, it is administered parenterally in a hospital setting. Administer slowly, a dose of 2-5 mg (1-2 mg/min). If there is no effect, the administration can be repeated after 5 minutes. Increasing the dose above 15 mg usually does not lead to greater severity of action. After stopping the attack of arrhythmia, patients are transferred to oral administration at a dose of 50 mg 4 times a day, with the first dose taken 15 minutes after stopping the IV administration. In the acute stage of myocardial infarction, immediately after hospitalization of the patient (with constant monitoring of hemodynamics: ECG, heart rate, AV conduction, blood pressure), a bolus of 5 mg should be administered intravenously, the administration should be repeated every 2 minutes until a total dose of 15 mg is reached. If well tolerated, after 15 minutes - orally, 25-50 mg every 6 hours, for 2 days. Patients who do not tolerate the full IV dose should be started on oral administration, starting with a half dose. Maintenance therapy continues at doses of 200 mg/day (in 2 doses) for 3 months to 3 years. Elderly patients are recommended to start treatment with 50 mg/day. Renal failure does not require dose adjustment. In case of liver failure, it is advisable to prescribe other beta-blockers that are not metabolized in the liver.
Contraindications: Hypersensitivity, cardiogenic shock, AV block II-III stage, SA block, SSSU, sinus bradycardia (heart rate less than 50/min), acute HF or decompensated CHF, Prinzmetal's angina, arterial hypotension, acute myocardial infarction (PQ more than 0.24 s or systolic blood pressure less than 100 mm Hg), lactation period, simultaneous use of MAO inhibitors or simultaneous intravenous administration of verapamil.
Side effects: From the nervous system: increased fatigue, weakness, headache, slower speed of mental and motor reactions. Rarely: paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremor, convulsions, depression, anxiety, decreased attention, drowsiness, insomnia, nightmares, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis . From the senses: rarely - decreased vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis, tinnitus, decreased hearing. From the cardiovascular system: sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely - decreased myocardial contractility, development (worsening) of CHF (edema, swelling of the feet and/or lower legs, shortness of breath), heart rhythm disturbances, manifestation of vasospasm (increased peripheral circulatory disorders, coldness of the lower extremities, Raynaud's syndrome), myocardial conduction disturbances, cardialgia. Very rarely - worsening of pre-existing AV conduction disorders. From the digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea, in some cases - impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), changes in taste. From the skin: skin rashes (exacerbation of psoriasis), psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia. From the respiratory system: nasal congestion, bronchospasm when prescribed in high doses (loss of selectivity and/or in predisposed patients), shortness of breath. From the endocrine system: hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state. Allergic reactions: urticaria, skin itching, rash. Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes, hyperbilirubinemia. Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. Other: pain in the back or joints, weight gain, decreased libido and/or potency, with abrupt cessation of treatment - “smokers” syndrome; the effectiveness of beta-blockers is lower. In combination therapy with clonidine, the latter should be discontinued several days after metoprolol is discontinued in order to avoid a hypertensive crisis. At a dose above 200 mg/day, cardioselectivity decreases. Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels. If necessary, beta2-adrenergic stimulants are used as concomitant therapy for patients with bronchial asthma, and alpha-blockers for pheochromocytoma. If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not recommended. Reciprocal activation of the n.vagus can be eliminated by intravenous administration of atropine (1-2 mg). Drugs that reduce catecholamine reserves (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia. If elderly patients develop increasing bradycardia (less than 50/min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction, it is necessary to reduce the dose or stop treatment . It is recommended to discontinue therapy if skin rashes appear and depression develops caused by taking beta-blockers. The drug is discontinued gradually, reducing the dose over 10 days. With abrupt cessation of treatment, intermittent claudication syndrome, Raynaud's syndrome), pregnancy, childhood (efficacy and safety have not been determined), and old age may occur.
Interactions: Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving metoprolol. Iodine-containing radiopaque drugs for intravenous administration increase the risk of developing anaphylactic reactions. Phenytoin with intravenous administration, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure. Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. The hypotensive effect is weakened by NSAIDs (Na+ retention and blockade of Pg synthesis by the kidneys), corticosteroids and estrogens (Na+ retention). Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and HF. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure. Prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase CNS depression. Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect; the break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Dispensed from pharmacies: Available with prescription
Drug registration number: P No. 011845/01
Date of registration (re-registration) of the drug: 02/03/2006
