Metocardium
Metocard: 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: Metocard
ATX code: C07AB02
Active ingredient: metoprolol (metoprolol)
Manufacturer: Polfarma S. A. (Poland)
Description and photo update: 28.11.2018
Prices in pharmacies: from 50 rubles.
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Metocardium is a selective beta 1 -adrenergic blocker.
Release form and composition
The drug is produced in the form of tablets: round, biconvex, white, with a dividing line (10 pcs. In blisters, in a cardboard box 3 blisters and instructions for using Metocard).
Composition of 1 tablet:
- active substance: metoprolol tartrate - 50 or 100 mg;
- auxiliary components: microcrystalline cellulose, talc, rice starch, povidone, lactose, magnesium stearate.
Pharmacological properties
Pharmacodynamics
The active substance of Metocard - metoprolol tartrate, is a cardioselective beta 1 -adrenoceptor blocker, which has hypotensive, antiarrhythmic and antianginal effects. Does not possess membrane stabilizing and internal sympathomimetic activity.
In low doses, metoprolol blocks β 1 -adrenoreceptors of the heart, as a result of which it reduces the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP) stimulated by catecholamines, reduces the intracellular Ca 2+ current, and also has a negative batmo-, ino-, dromo- and chronotropic effect (reduces myocardial contractility, inhibits excitability and conduction, slows down the heart rate).
The total peripheral vascular resistance in the first day after taking Metocard increases, after 1–3 days it returns to the initial one, with prolonged use of a beta-blocker - decreases.
The acute hypotensive effect of Metocard is due to a decrease in cardiac output.
A stable antihypertensive effect develops within 2–3 weeks and is due to the following effects: a decrease in renin synthesis, accumulation of plasma renin, inhibition of the activity of the central nervous system and the renin-angiotensin system (which is especially important for patients with initial hypersecretion of renin), restoration of the sensitivity of the aortic arch baroreceptors (there is no increase in their activity due to a decrease in blood pressure), a decrease in peripheral sympathetic influences. Metocardium reduces high blood pressure (BP) at rest, during exercise and under stress.
A decrease in blood pressure is noted on average after 15 minutes (maximum - after 2 hours) and continues for 6 hours. Diastolic blood pressure decreases more slowly: a stable decrease occurs after several weeks of regular intake of the drug.
The antianginal action of Metocardium is manifested by a decrease in myocardial sensitivity to the effects of sympathetic innervation, as well as myocardial oxygen demand due to a decrease in contractility and heart rate (prolongation of diastole and improvement of myocardial perfusion). Metocardium increases exercise tolerance, reduces the severity and number of angina attacks.
The antiarrhythmic effect of metoprolol is due to its ability to eliminate arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), reduce the rate of spontaneous excitation of sinus and ectopic pacemakers, slow down conduction along additional pathways and atrioventricular node, conduction (through the AV node) predominantly in the antegrade direction, to a lesser extent in the retrograde direction).
Metocardium slows down the heart rate (HR) and even leads to the restoration of sinus rhythm in atrial fibrillation, supraventricular tachycardia, sinus tachycardia in functional heart disease and hyperthyroidism. Metoprolol also prevents the development of migraines.
Unlike non-selective beta-blockers, selective, when used in moderate therapeutic doses, have a less pronounced effect on carbohydrate metabolism and on organs in which β 2 -adrenergic receptors are present, such as skeletal muscles, pancreas, smooth muscles of the uterus, bronchi and peripheral arteries … When used in high doses (more than 100 mg per day), metoprolol has a blocking effect on both subtypes of β-adrenergic receptors.
Pharmacokinetics
Once in the gastrointestinal tract, metoprolol is absorbed quickly and almost completely (95%).
The maximum plasma concentration is reached after 1–2 hours.
Bioavailability at the first dose is 50%, with repeated use it increases to 70%. This indicator increases with simultaneous use with food (by 20-40%), as well as with cirrhosis of the liver.
Plasma protein binding is approximately 10%.
Metoprolol crosses the placental and blood-brain barriers. In small amounts, the substance is excreted in breast milk.
The drug is metabolized in the liver with the formation of metabolites that do not have pharmacological activity.
The half-life is 1-9 hours (average 3.5 hours). About 5% of the drug is excreted unchanged by the kidneys. It is not removed during hemodialysis.
The metabolism of the drug slows down with impaired liver function.
Indications for use
- arterial hypertension, including hyperkinetic type (in the form of a single drug or in combination with other antihypertensive drugs);
- ischemic heart disease: myocardial infarction (complex therapy for secondary prevention), prevention of angina attacks;
- heart rhythm disorders: ventricular premature beats and supraventricular tachycardia;
- prevention of migraine attacks;
- hyperthyroidism (complex therapy).
Contraindications
Absolute:
- arterial hypotension (when Metocard is prescribed for secondary prevention of myocardial infarction: systolic blood pressure - <100 mm Hg, heart rate - <45 beats / min);
- chronic heart failure in the phase of decompensation;
- sinoatrial blockade;
- cardiogenic shock;
- Prinzmetal's angina;
- severe bradycardia;
- atrioventricular block II or III degree;
- sick sinus syndrome;
- age up to 18 years;
- lactation period (breastfeeding);
- the simultaneous use of verapamil (intravenously) and monoamine oxidase inhibitors;
- hypersensitivity to any component of the drug or other beta-blockers.
Relative (special care is required when using Metocard):
- atrioventricular block I degree;
- obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome);
- bronchial asthma;
- metabolic acidosis;
- thyrotoxicosis;
- diabetes;
- chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis);
- pheochromocytoma;
- myasthenia gravis;
- chronic hepatic and / or renal failure;
- psoriasis;
- depression (current or history);
- pregnancy;
- elderly age.
Metocard, instructions for use: method and dosage
Metocard tablets are taken orally with a sufficient amount of water, during or immediately after a meal. If necessary, the tablets can be divided into 2 parts, but must not be chewed.
Recommended dosage regimens:
- arterial hypertension: 50-100 mg per day in 1 or 2 doses. In the future, if the effect is insufficient, the daily dose is gradually increased to 100 mg, maximum up to 200 mg. If in this case there is no satisfactory therapeutic effect, Metocard is prescribed in combination with other antihypertensive drugs;
- arrhythmia, angina pectoris, prevention of migraine attacks: 50-100 mg 2 times a day (morning and evening);
- secondary prevention of myocardial infarction: 100 mg 2 times a day (morning and evening);
- functional disorders of cardiac activity with tachycardia: 50 mg 2 times a day (morning and evening).
Side effects
- on the part of the cardiovascular system: lowering blood pressure, palpitations, dizziness, orthostatic hypotension, sinus bradycardia; sometimes - loss of consciousness; rarely - arrhythmias, myocardial conduction disturbances, temporary worsening of symptoms of chronic heart failure (shortness of breath, swelling of the feet and / or lower legs, edema), manifestation of angiospasm (Raynaud's syndrome, coldness of the lower extremities, increased peripheral circulation disorders), decreased myocardial contractility;
- from the central and peripheral nervous system: slowing down of the speed of mental and motor reactions, weakness, increased fatigue, headache; rarely - insomnia / drowsiness, nightmares, decreased attention, anxiety, confusion or short-term memory impairment, depression, muscle weakness, paresthesia in the limbs (in patients with intermittent claudication and Raynaud's syndrome);
- from the digestive system: dry mouth, abdominal pain, change in taste, diarrhea / constipation, nausea, vomiting, increased activity of liver enzymes, liver dysfunction; extremely rare - hyperbilirubinemia;
- from the hematopoietic system: rarely - leukopenia, agranulocytosis, thrombocytopenia (unusual bleeding and hemorrhage);
- on the part of the respiratory system: shortness of breath, difficulty in exhaling (when prescribed in high doses - bronchospasm), nasal congestion;
- from the endocrine system: hypothyroidism; in patients with non-insulin dependent diabetes mellitus - hyperglycemia;
- on the part of the sensory organs: rarely - dryness and soreness of the eyes, decreased secretion of tear fluid, decreased vision, conjunctivitis, tinnitus;
- dermatological reactions: increased sweating, rash, pruritus, photodermatosis, skin flushing, exanthema, urticaria, psoriasis-like skin reactions, exacerbation of psoriasis, reversible alopecia;
- others: joint / back pain; in isolated cases - a slight increase in body weight, decreased libido and / or potency;
- effect on the fetus: bradycardia, hypoglycemia, intrauterine growth retardation is possible.
The types and severity of side effects depend on the individual characteristics of the patient. Basically, they are of a minor nature and disappear after the abolition of Metocardium.
Overdose
Symptoms: dizziness, fainting, nausea, vomiting, marked decrease in blood pressure, ventricular premature beats, arrhythmias, severe sinus bradycardia, bronchospasm, cyanosis; in acute overdose - loss of consciousness, cardialgia, cardiogenic shock, AV blockade (up to the development of complete transverse blockade and cardiac arrest), coma. The first signs of an overdose appear 20–120 minutes after taking an excessive dose of Metocard.
First aid includes gastric lavage and absorption of adsorbents. Further treatment is symptomatic. With a pronounced decrease in blood pressure, the patient should be placed in the Trendelenburg position (lying on his back at an angle of 45 ° with the pelvis raised in relation to the head). With a significant decrease in blood pressure, heart failure and bradycardia, beta-adrenostimulants or atropine sulfate are administered intravenously with an interval of 2-5 minutes. If there is no benefit, dopamine, dobutamine, or norepinephrine (norepinephrine) are given. In the future, if necessary, appoint 1-10 mg of glucagon, put a transvenous intracardiac pacemaker. In case of development of bronchospasm, stimulants of β 2 -adrenoreceptors are administered intravenously.
With the help of hemodialysis, metoprolol is poorly excreted.
special instructions
Patients receiving Metocard require regular monitoring of blood pressure and heart rate. Patients with diabetes mellitus need to monitor blood glucose levels, if necessary, the dose of insulin / oral hypoglycemic drugs should be adjusted.
Patients with severe renal impairment should be monitored for renal function, elderly patients for liver function. Elderly patients need a dose adjustment of Metocard in case of a decrease in systolic blood pressure (<100 mm Hg), an increase in bradycardia (<50 beats / min), the development of AV blockade, ventricular arrhythmias, bronchospasm, severe liver dysfunction. In some cases, treatment must be interrupted.
The physician should teach each patient how to calculate heart rate and explain the importance of seeking medical attention if the frequency is less than 50 beats per minute.
Patients with a history of depressive disorders should be under special supervision. If depression develops while taking a beta-blocker, therapy is discontinued.
Treatment of heart failure can only be started after the compensation stage has been reached.
In case of exertional angina, the dose of Metocardium is selected so that it provides a resting heart rate of 55–60 beats / min, with a load - no more than 110 beats / min.
When prescribing a surgical operation, the patient should warn the anesthesiologist about taking metoprolol, since this affects the choice of a means for general anesthesia (with a minimal negative inotropic effect). It is not recommended to cancel antihypertensive therapy.
Metocardium can cause increased hypersensitivity reactions (against the background of a burdened allergic history) and the lack of effect from the introduction of standard doses of adrenaline (epinephrine).
Patients who use contact lenses should take into account that beta-blockers can reduce the production of tear fluid.
Metoprolol may exacerbate symptoms of peripheral arterial circulation disorder.
Some clinical signs of hyperthyroidism (eg, tachycardia) may be masked during therapy. It is contraindicated to abruptly cancel Metocard, since after stopping it, symptoms may increase.
Metoprolol can mask tachycardia caused by hypoglycemia in patients with diabetes mellitus. Unlike non-selective beta-blockers, selective ones practically do not increase insulin-induced hypoglycemia, and also do not delay the restoration of glucose levels to normal values.
When Metocard is prescribed to patients with pheochromocytoma, alpha-blockers are used as concomitant therapy, and β 2 -adrenoreceptor stimulants are used with bronchial asthma.
Drugs that reduce the supply of catecholamines (for example, reserpine) can increase the action of Metocard, which is fraught with an excessive decrease in blood pressure and the development of bradycardia. In this regard, patients should be under close medical supervision.
It is necessary to cancel Metocard gradually, reducing the dose within 10 days, otherwise the development of a withdrawal syndrome is possible (manifested by an increase in blood pressure and an increase in angina attacks). Patients with angina pectoris require special supervision.
Influence on the ability to drive vehicles and complex mechanisms
At the initial stage of therapy, dizziness and increased fatigue are possible. In this case, it is recommended to refrain from any activities that require increased attention and speed of reactions. The degree of further restrictions is determined individually.
Application during pregnancy and lactation
For pregnant women, Metocard can only be prescribed by a doctor after a careful assessment of the balance of benefits and risks, since metoprolol penetrates the placental barrier and can cause arterial hypotension, bradycardia, and hypoglycemia in a newborn. In this regard, if it is necessary to use the drug during gestation, constant monitoring of the condition of the fetus is required for the entire duration of therapy, as well as in the first 48–72 hours after childbirth.
The drug passes into breast milk, its effect on the newborn has not been studied, therefore it is recommended to stop breastfeeding if metoprolol treatment is necessary during lactation.
Pediatric use
Metocard is prohibited for use under the age of 18.
With impaired renal function
Preparations containing metoprolol should be used with caution in patients diagnosed with impaired renal function. No dose adjustment is required.
For violations of liver function
Preparations containing metoprolol should be prescribed with caution to patients diagnosed with liver dysfunction. The doctor determines the dose individually, depending on the clinical condition of the patient.
Use in the elderly
With caution, Metocard tablets are used in old age. It is not necessary to adjust the dose of the drug.
Drug interactions
- monoamine oxidase inhibitors: the hypotensive effect is significantly enhanced (the interval between medications should be at least 14 days);
- verapamil (intravenous): possible cardiac arrest;
- nifedipine: blood pressure is significantly reduced;
- means for inhalation general anesthesia (hydrocarbon derivatives): the risk of developing arterial hypotension and suppression of myocardial function increases;
- antihypertensive drugs, blockers of slow calcium channels, nitroglycerin, diuretics: a sharp decrease in blood pressure is possible (special care should be taken with the simultaneous use of prazosin);
- inducers of microsomal liver enzymes (rifampicin, barbiturates): the metabolism of metoprolol increases, its plasma concentration decreases and, as a consequence, the effect decreases;
- inhibitors of microsomal liver enzymes (phenothiazines, cimetidine, oral contraceptives): the plasma concentration of metoprolol increases;
- xanthines (except diphylline): their clearance decreases, especially in patients with initially increased theophylline clearance due to smoking;
- lidocaine: its clearance decreases, blood concentration increases;
- hypnotics and sedatives, antipsychotics (antipsychotics), tri- and tetracyclic antidepressants: the inhibitory effect on the central nervous system is enhanced;
- oral hypoglycemic agents: it is possible to reduce the severity of their action;
- insulin: the risk of developing hypoglycemia increases, its severity and duration increase, some symptoms of hypoglycemia (sweating, tachycardia, high blood pressure) may be masked;
- beta-adrenostimulants, indomethacin and other non-steroidal anti-inflammatory drugs, estrogens, theophylline, cocaine: the hypotensive effect of metoprolol is weakened;
- antidepolarizing muscle relaxants: their effect is enhanced and prolonged;
- coumarins: their effect is lengthened;
- means for general anesthesia: the cardiodepressant effect is summed up;
- ergot alkaloids: increased risk of peripheral circulatory disorders;
- ethanol: the inhibitory effect on the central nervous system increases, the risk of a pronounced decrease in blood pressure increases;
- allergens used for immunotherapy and allergen extracts for skin tests: increases the likelihood of developing systemic allergic reactions or anaphylaxis;
- iodine-containing X-ray contrast agents used intravenously: the risk of anaphylactic reactions increases;
- cardiac glycosides, agents for general anesthesia, antiarrhythmics (amiodarone), alpha-methyldopa, verapamil, clonidine, diltiazem, guanfacine, reserpine: the severity of a decrease in heart rate increases, atrioventricular conduction is inhibited (when used simultaneously with metoprolol, clonidine continues to take the first for several days; simultaneous withdrawal is contraindicated due to the likelihood of withdrawal).
Analogs
Metocard analogues are: Aritel, Aritel Cor, Atenolol, Atenolol Nycomed, Betak, Betacard, Betaxolol, Betalok, Betalok ZOK, Bivotenz, Bidop, Binelol, Biprol, Bisogamma, Bisoprolol, Vero-Atenolol, Lokoron, Cororon, Nebivolol, Nebilet, Nebilong, Tirez, Egilok, Estecor, etc.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C in a place protected from light and moisture, out of reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Metocard
Metocard is a drug widely used to treat arterial hypertension and various cardiac pathologies. However, it does not always help as monotherapy, therefore it is often prescribed in combination with other antihypertensive drugs.
Patients sometimes complain about the development of side effects. Doctors, however, emphasize that the described adverse reactions are often manifestations of the underlying disease.
Nevertheless, most of the reviews about Metocardium are positive: patients note that the drug quickly and well reduces high blood pressure.
Price for Metocard in pharmacies
Approximate prices for Metocard are: 30 tablets of 50 mg - 59-70 rubles, 30 tablets of 100 mg - 61-85 rubles.
Metocard: prices in online pharmacies
Drug name Price Pharmacy |
Metocard 100 mg tablets 30 pcs. RUB 50 Buy |
Metocard 50 mg tablets 30 pcs. RUB 59 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!