Metoprolol
Metoprolol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Metoprolol
ATX code: C07AB02
Active substance: metoprolol
Manufacturer: Ozone (Russia), Moscow Endocrine Plant (Russia), Hemopharm (Serbia), Adipharm (Bulgaria), Biochemist (Russia), Marbiopharm (Russia), Zentiva (Slovakia), Organika (Russia), Ratiopharm (Germany)
Description and photo update: 2019-07-08
Prices in pharmacies: from 18 rubles.
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Metoprolol is a selective beta 1 -adrenergic blocker.
Release form and composition
Dosage forms:
- Tablets: white with a gray tint or white, with a chamfer on both sides and a dividing line on one side, have a round flat shape, 100 mg each (10 or 30 pcs. In a blister strip, in a cardboard box from 1 to 10 packs; 10, 20, 30, 40, 50, 60, 70, 80, 90 or 100 pcs. in polymer containers, in a cardboard box 1 container; 10 pcs. in blisters, in a cardboard box 3 or 5 blisters), 50 mg (in blister packs: 10 pcs., In a cardboard bundle 1, 2, 3, 5 or 10 packages, 15 or 20 pcs., In a cardboard bundle 2 packages, 30 pcs., In a cardboard bundle 1 or 2 packages; in polymeric containers of 20, 30, 40 or 50 pcs., In a cardboard box 1 container), 25 mg each (in blisters: 10 pcs., In a cardboard box 1 package, 30 pcs., In cardboard box 1 or 2 packages; in polymer containers of 20,40 or 50 pcs., 1 container in a carton box);
- Film-coated tablets: round, biconvex, with a dividing line on one side, can be pinkish or from white to yellowish-white, 50 mg each (14 pieces in blisters, in a cardboard box 2 or 4 blisters), 100 mg each (10 pcs. in blisters, in a cardboard box 3 blisters).
The active ingredient is metoprolol tartrate:
- 1 tablet - 25 mg, 50 mg or 100 mg;
- 1 film-coated tablet - 50 mg (pink) or 100 mg.
Auxiliary components:
- Tablets: microcrystalline cellulose, lactose monohydrate, potato starch, povidone, sodium carboxymethyl starch, magnesium stearate;
- Film-coated tablets: sodium carboxymethyl starch (type A), microcrystalline cellulose, anhydrous colloidal silicon dioxide, magnesium stearate.
Additionally, the shell contains: polysorbate 80, hypromellose, titanium dioxide (E171), talc; the pink shell contains a crimson dye (Ponso 4R).
Pharmacological properties
Pharmacodynamics
Metoprolol is a cardioselective beta1-blocker. It has antiarrhythmic, antianginal, antihypertensive and insignificant membrane stabilizing effect.
By blocking beta1-adrenergic receptors of the heart, catecholamine-stimulated formation of cAMP (cyclic adenosine monophosphate) from ATP (adenosine triphosphate) decreases, intracellular calcium flow decreases, heart rate decreases, myocardial contractility decreases, excitability and conductivity are inhibited.
In the first 24 hours after taking beta-blockers, the total peripheral vascular resistance increases, after 1–3 days it returns to its original value, and with prolonged use of the drug it decreases.
The antihypertensive effect of metoprolol is due to the following effects:
- decrease in minute blood volume;
- decreased renin synthesis;
- inhibition of the activity of the renin-angiotensin-aldosterone system;
- suppression of the activity of the central nervous system;
- restoration of the sensitivity of the aortic arch baroreceptors;
- decrease in peripheral sympathetic influences.
The drug reduces high blood pressure during stress, physical exertion and at rest. The antihypertensive effect of metoprolol develops rather quickly: it takes from 15 minutes to 2 hours to decrease systolic blood pressure (the effect lasts for 6 hours); for a stable decrease in diastolic blood pressure, regular intake of the drug is required for several weeks.
The antianginal effect of metoprolol is determined by a decrease in the oxygen demand of the heart muscle due to a decrease in contractility and heart rate, as well as a decrease in the sensitivity of the myocardium to the influence of sympathetic innervation. Metoprolol reduces the number and severity of angina attacks and increases exercise tolerance. In some patients, especially those suffering from chronic heart failure, an increase in myocardial oxygen demand is possible due to an increase in the end-diastolic pressure in the left ventricle and a stronger stretching of the muscle fibers of the ventricles.
The antiarrhythmic effect of metoprolol is due to the following effects:
- elimination of arrhythmogenic factors (arterial hypertension, tachycardia, increased cAMP content, increased activity of the sympathetic part of the nervous system);
- slowing down the atrioventricular conduction;
- a decrease in the rate of spontaneous excitation of ectopic and sinus pacemakers.
The drug slows down the heart rate and can restore the rhythm in patients with atrial fibrillation, supraventricular and sinus tachycardia with thyrotoxicosis and functional heart diseases.
Metoprolol helps prevent the development of migraine attacks.
It differs from nonselective beta-blockers in that when used in medium therapeutic doses, it has less effect on carbohydrate metabolism and organs containing beta2-adrenergic receptors (smooth muscles of the bronchi, peripheral arteries and uterus, skeletal muscles, pancreas). When taking high doses of the drug (more than 100 mg per day), beta1 and beta2 adrenergic receptors are blocked.
Pharmacokinetics
Metoprolol is 95% absorbed in the gastrointestinal tract. Moderately soluble in fats. When taken for the first time, the bioavailability is 50%, with repeated use, it increases to 70%. The drug is 10% bound to plasma proteins. The maximum concentration is reached in 1.5–2 hours. With the course of treatment with metoprolol, its bioavailability increases. Simultaneous intake with food increases bioavailability by 20-40%.
Metoprolol quickly penetrates into all tissues, as well as through the blood-brain and placental barriers. Excreted in breast milk (concentration in breast milk exceeds the concentration in plasma).
The metabolism of the drug occurs in the liver with the participation of the CYP2D6 isoenzyme. Two metabolites have a beta-blocking effect. The half-life for oral administration is 3.5-7 hours. It is not removed during hemodialysis.
With a creatinine clearance of 5 ml / min, a significant accumulation of metabolites is observed, but the activity of the drug does not increase.
In hepatic failure, the bioavailability of metoprolol increases, and its total clearance decreases.
Indications for use
- Ischemic heart disease: myocardial infarction (as part of the complex therapy of secondary prevention), prevention of angina attacks;
- Monotherapy or as part of a combination treatment (with other antihypertensive drugs) of arterial hypertension, including hyperkinetic type, tachycardia;
- Hyperthyroidism (as part of complex therapy);
- Heart rhythm disorders, including ventricular premature beats, supraventricular tachycardia;
- Prevention of migraine attacks.
Contraindications
- Cardiogenic shock;
- Sinoatrial (SA) block;
- Atrioventricular (AV) block II-III degree;
- Severe bradycardia;
- Sick sinus syndrome;
- Prinzmetal's angina;
- Heart failure in the stage of decompensation;
- Arterial hypotension (for secondary prevention of myocardial infarction - with systolic blood pressure (BP) below 100 mm Hg and a heart rate (HR) less than 45 beats per minute);
- Concomitant therapy with monoamine oxidase (MAO) inhibitors or verapamil;
- Age under 18;
- Breastfeeding period;
- Hypersensitivity to drug components or other beta-blockers.
It is recommended to prescribe metoprolol with caution to patients with AV blockade of the 1st degree, metabolic acidosis, diabetes mellitus, chronic obstructive pulmonary disease (chronic obstructive bronchitis, pulmonary emphysema), bronchial asthma, obliterating peripheral vascular diseases (Raynaud's syndrome, intermittent claudication), myasthenia gravis, chronic renal and / or hepatic failure, pheochromocytoma, thyrotoxicosis, psoriasis, depression (including history), in old age and during pregnancy.
Instructions for the use of Metoprolol: method and dosage
The tablets are taken whole by mouth, during or immediately after a meal, with plenty of liquid.
The dosage regimen is prescribed by the doctor based on clinical indications.
Recommended daily dosage:
- Secondary prevention of myocardial infarction: 200 mg in 2 divided doses (morning and evening);
- Arterial hypertension: initial dose of 50-100 mg in 1 or 2 divided doses. To achieve a therapeutic effect, a gradual increase in the dose to 100-200 mg and / or the simultaneous administration of other antihypertensive drugs is shown. The daily dose should not exceed 200 mg;
- Tachycardia against the background of functional disorders of cardiac activity: 100 mg in 2 divided doses;
- Angina pectoris, arrhythmias, prevention of migraine attacks: 100-200 mg in 2 divided doses.
No dose adjustment is required for impaired renal function, the need for hemodialysis, and treatment of elderly patients.
Appointment of Metoprolol to patients with functional liver disorders should be made in accordance with their clinical condition.
Side effects
- Cardiovascular system: palpitations, sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, loss of consciousness); rarely - a decrease in myocardial contractility, arrhythmias, a temporary increase in the symptoms of chronic heart failure (shortness of breath, edema, including the feet and / or lower legs), manifestation of angiospasm (coldness of the lower extremities, increased disturbance of peripheral circulation, Raynaud's syndrome), cardialgia, violation myocardial conductivity;
- Nervous system: weakness, increased fatigue, slowing down of the speed of psychomotor reactions, headache; rarely - anxiety, muscle weakness, paresthesias in the limbs (against the background of intermittent claudication and Raynaud's syndrome), drowsiness, depression, insomnia, decreased attention, confusion, nightmares, short-term memory impairment;
- Digestive system: dry mouth, nausea, vomiting, change in taste, abdominal pain, diarrhea or constipation, liver function disorder;
- Sense organs: rarely - tinnitus, decreased secretion of lacrimal fluid, decreased vision, conjunctivitis, dryness and soreness of the eyes;
- Skin: itching, rash, urticaria, increased sweating, exacerbation of psoriasis, psoriasis-like reactions, exanthema, hyperemia, photodermatosis, reversible alopecia;
- Endocrine system: hypoglycemia (with insulin-dependent diabetes mellitus); rarely - hypothyroidism, hyperglycemia (with diabetes mellitus);
- Respiratory system: nasal congestion, shortness of breath, difficulty breathing out (bronchospasm at high doses);
- Laboratory indicators: rarely - agranulocytosis, thrombocytopenia (unusual hemorrhages and bleeding), leukopenia, increased activity of hepatic transaminases; very rarely - hyperbilirubinemia;
- Effect on the fetus: possible intrauterine bradycardia, growth retardation, hypoglycemia;
- Others: back or joint pain; in isolated cases - a slight increase in body weight, decreased potency and libido.
The likelihood and degree of manifestation of side effects depend on the individual sensitivity of the patient, as a rule, they are insignificant and transient.
Overdose
In case of an overdose, the following symptoms occur: dizziness, cyanosis, vomiting, nausea, bronchospasm, severe severe sinus bradycardia, arrhythmia, fainting, marked decrease in blood pressure, ventricular premature beats. In acute overdose, atrioventricular block, cardiogenic shock, cardialgia, coma, loss of consciousness may occur.
The first signs of an overdose appear after 20 minutes - 2 hours after taking the drug.
The patient should be gastric lavage and prescribe adsorbing agents. Symptomatic therapy is performed: with a decrease in blood pressure, the patient is placed in a supine position with a slightly raised pelvis and legs; with an excessive decrease in blood pressure, heart failure and bradycardia, beta-adrenostimulants are administered intravenously at intervals of 2–5 minutes (until the desired effect is achieved) or atropine sulfate intravenously at a dose of 0.5–2 mg.
If there is no positive effect, dopamine, norepinephrine, or dobutamine are given.
In the future, it is possible to prescribe glucagon at a dose of 1–10 mg and an electrostimulator. In the case of bronchospasm, beta2-adrenergic receptor stimulants are administered intravenously. Hemodialysis is ineffective.
special instructions
Treatment with beta-blockers must be accompanied by regular monitoring of heart rate and blood pressure, in patients with diabetes mellitus - the level of glucose in the blood (the dose of hypoglycemic agents or insulin is selected individually).
When prescribing the drug, the patient should be taught the method of self-calculating the heart rate and instructed to immediately consult a doctor if the heart rate is below 50 beats per minute.
The cardioselectivity of Metoprolol at a dose of more than 200 mg per day decreases.
The use of the drug in the treatment of heart failure should be started only at the stage of compensation.
In patients with a burdened allergic history, an increase in the severity and lack of effect from usual doses of epinephrine (adrenaline) in hypersensitivity reactions is possible.
The drug can increase the symptoms of peripheral arterial circulation pathology.
Cancellation of the drug should be carried out by gradually reducing the dose over 10 days. Abrupt cessation of treatment can cause a withdrawal syndrome in the patient (increased blood pressure, increased angina attacks).
The individual dose of the drug for angina pectoris should provide the patient with a heart rate at rest of 55-60 beats per minute, with a load - no higher than 110.
When using contact lenses, it is necessary to take into account the decrease in the production of tear fluid while taking beta-blockers.
The drug can mask tachycardia and other symptoms of hyperthyroidism.
In patients with diabetes mellitus, Metoprolol may mask tachycardia caused by hypoglycemia. With insulin-induced glycemia, the drug has practically no effect on the process of restoring the blood glucose concentration to normal levels.
In bronchial asthma, the use of the drug is indicated with the simultaneous administration of beta 2 -adrenostimulants, with pheochromocytoma - alpha-blockers.
Before carrying out a surgical operation, it is necessary to inform the anesthesiologist about taking Metoprolol so that general anesthesia is carried out with minimal negative inotropic effect without discontinuing the drug.
It should be borne in mind that with the simultaneous use of reserpine and other drugs that reduce the reserves of catecholamines and enhance the effect of beta-blockers, an excessive decrease in blood pressure and the development of bradycardia are possible.
In elderly patients, it is necessary to control liver function, and with a strong decrease in blood pressure, AV blockade, the appearance of bronchospasm, ventricular arrhythmias, increasing bradycardia, severe liver dysfunction, dose adjustment or drug withdrawal is required.
With severe renal failure, regular monitoring of renal function is required.
It is necessary to monitor the condition of patients with depressive disorders; if signs of depression develop, treatment should be discontinued.
At the beginning of the use of the drug, patients should be careful or refuse to drive vehicles and mechanisms, since during this period they may experience fatigue and dizziness. During treatment, the safety of the dose is determined individually.
Application during pregnancy and lactation
For pregnant women, the drug is prescribed only according to strict indications, taking into account the benefit / risk ratio, since under the influence of Metoprolol, the development of bradycardia, hypoglycemia and arterial hypotension in the fetus is possible. Requires close monitoring of the development of the fetus, as well as newborns in the first 48-72 hours after delivery.
If necessary, use the drug during breastfeeding, breastfeeding should be discontinued.
Pediatric use
According to the instructions, Metoprolol is contraindicated in children and adolescents under 18 years of age, since its effectiveness and safety when used in childhood have not been established.
With impaired renal function
The drug is used with caution in patients with chronic renal failure.
For violations of liver function
The drug is used with caution in patients with chronic hepatic failure.
Use in the elderly
The drug is prescribed with caution to the elderly.
Drug interactions
It is impossible to prescribe Metoprolol simultaneously with MAO inhibitors due to an increase in the hypotensive effect, it is necessary to observe a break between taking drugs for at least 14 days.
Intravenous (IV) administration of verapamil while taking metoprolol can cause cardiac arrest.
With simultaneous use with Metoprolol:
- Nifedipine, ethanol - significantly reduce blood pressure;
- Derivatives of hydrocarbons for inhalation anesthesia - increase the likelihood of developing arterial hypotension against the background of suppression of myocardial function;
- Theophylline, beta-adrenostimulants, cocaine, estrogens, indomethacin and other non-steroidal anti-inflammatory drugs - weaken the hypotensive effect;
- Antipsychotics, tetra- and tricyclic antidepressants, hypnotics and sedatives and ethanol - increase the depression of the nervous system;
- Ergot alkaloids - increase the risk of peripheral circulation disorders;
- Antihypertensive drugs, diuretics, slow calcium channel blockers or nitroglycerin - potentiate a sharp decrease in blood pressure (especially prazosin);
- Diltiazem, verapamil, antiarrhythmics (amiodarone), methyldopa, reserpine, clonidine, general anesthetics, guanfacine, cardiac glycosides - lead to a strong decrease in heart rate and inhibition of AV conduction;
- Rifampicin, barbiturates (inducers of liver microsomal enzymes) - accelerate the metabolism of metoprolol, reducing its concentration in blood plasma and reducing the clinical effect;
- Oral hypoglycemic agents and insulin - reduce their effectiveness, the risk of hypoglycemia increases;
- Oral contraceptives, cimetidine, phenothiazines (inhibitors) - increase the concentration of metoprolol in blood plasma.
Metoprolol reduces the clearance of xanthine (except for diphylline), especially in patients with increased clearance of theophylline against the background of smoking, increases the concentration of lidocaine in the blood plasma, prolongs the anticoagulant effect of coumarins, prolongs and enhances the effect of antidepolarizing muscle relaxants.
Combination with allergen extracts used for skin tests and allergens for immunotherapy increases the likelihood of developing systemic allergic reactions (including anaphylaxis). When taken simultaneously with radiopaque iodine-containing agents for intravenous administration, the risk of anaphylactic reactions increases.
With the simultaneous use of metoprolol and clonidine, if it is necessary to stop treatment, clonidine should be canceled only a few days after metoprolol.
Analogs
Metoprolol analogs are: Betalok, Metocard, Metoprolol Retard-Akrihin, Metoprolol-Acri, Metoprolol-Ratiopharm, Metoprolol-OBL, Metoprolol Organic, Metoprolol Zentiva, Anepro, Vasokardin, Corvitol, Metoblok, Metokzil, Metoprol.
Terms and conditions of storage
Keep out of the reach of children.
Store in a dry, dark place at a temperature of 15-25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Metoprolol
On Internet resources, you can find numerous reviews about Metoprolol. In most cases, patients respond positively to the drug, noting its availability and high efficiency in various cardiovascular pathologies. Metoprolol helps with attacks of angina pectoris, high blood pressure, tachycardia, severe headaches and migraines.
Some patients complain of side effects (weakness, shortness of breath), addiction to the drug and the presence of a large number of contraindications, which requires a particularly careful approach when prescribing Metoprolol.
Quite rarely, there are reviews that say that the drug was not effective or less effective than similar drugs.
Price for Metoprolol in pharmacies
The drug is produced by various pharmaceutical companies, despite this, the price of Metoprolol varies slightly:
- tablets 25 mg (60 pcs. in a package) - from 35 rubles;
- tablets 50 mg (30 pcs. in a package) - from 20 rubles;
- tablets 50 mg (50 pcs. in a package) - from 29 rubles;
- tablets 100 mg (30 pcs. in a package) - from 25 rubles;
- tablets 100 mg (50 pcs. in a package) - from 77 rubles.
Metoprolol: prices in online pharmacies
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Drug name Price Pharmacy |
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Metoprolol 50 mg tablets 30 pcs. RUB 18 Buy |
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Metoprolol retard-Akrikhin 25 mg film-coated prolonged-release tablets 30 pcs. 113 RUB Buy |
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Metoprolol 100 mg film-coated tablets with prolonged release 30 pcs. 299 r Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
