Metoprolol-Akrikhin
Metoprolol-Akrikhin: 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-Akrikhin
ATX code: C07AB02
Active ingredient: Metoprolol (Metoprolol)
Producer: JSC "AKRIKHIN KhFK" (Russia)
Description and photo update: 09.10.2019
Prices in pharmacies: from 35 rubles.
Buy
Metoprolol-Akrikhin is a cardioselective β-adrenergic receptor blocker.
Release form and composition
Dosage form - tablets: flat-cylindrical, white with a yellowish or grayish tinge, with a bevel (in a cardboard box there are 3 contour cell packs containing 10 tablets each, and instructions for use of Metoprolol-Akrikhin).
Composition of 1 tablet:
- active substance: metoprolol tartrate - 50 mg (in terms of 100% substance);
- auxiliary components: magnesium stearate, sodium carboxymethyl starch, povidone, potato starch, colloidal silicon dioxide, lactose monohydrate.
Pharmacological properties
Pharmacodynamics
Metoprolol-Akrikhin is a cardioselective β-adrenergic receptor blocker, which does not possess membrane stabilizing properties and intrinsic sympathomimetic activity. The actions of the substance include antiarrhythmic, antianginal and hypotensive.
By blocking β1-adrenergic receptors in the heart in low doses, the drug causes:
- lowering the catecholamine-stimulated formation of cyclic adenosine monophosphate from adenosine triphosphate;
- decrease in the intracellular current of calcium ions;
- a decrease in heart rate, a decrease in myocardial contractility, inhibition of excitability and conduction (has a negative chrono-, dromo-, batmo- and inotropic effect).
At the beginning of therapy with β-blockers, in the first 24 hours after their oral administration, due to the reciprocal increase in the activity of α-adrenergic receptors and the elimination of stimulation of β2-adrenergic receptors, the total peripheral resistance increases. After 1–3 days, it returns to the initial one, and in cases of prolonged treatment it decreases.
Reflex decrease in renin synthesis and cardiac output, inhibition of the activity of the central nervous and renin-angiotensin-aldosterone system (of particular importance in the case of initial hypersecretion of renin), restoration of the sensitivity of the aortic arch baroreceptors (their activity does not increase in response to a decrease in blood pressure) and, as a consequence, decrease in peripheral sympathetic influences, cause the hypotensive effect of metoprolol. Metoprolol-Akrikhin lowers high blood pressure at rest, during physical exertion and stress.
The antihypertensive effect of the drug develops rapidly and lasts for 6 hours. Systolic blood pressure decreases after 15–120 minutes (maximum), diastolic changes more slowly and decreases steadily over several weeks of regular use of the drug.
A decrease in myocardial sensitivity to the effects of sympathetic innervation, a decrease in myocardial oxygen demand due to a decrease in contractility and heart rate (improvement of myocardial perfusion and prolongation of diastole) determine the antianginal effect of metoprolol.
The use of Metoprolol-Akrikhin reduces the severity and number of angina attacks, increases exercise tolerance.
Deceleration of atrioventricular conduction (mostly in the antegrade direction, to a lesser extent in the retrograde direction) through the atrioventricular node and along additional pathways, a decrease in the rate of spontaneous excitation of ectopic and sinus pacemakers, as well as elimination of arrhythmogenic factors (arterial hypertension, increased content of cyclic adenosine activity of the sympathetic nervous system, tachycardia) determine the antiarrhythmic effect of the drug.
Metoprolol-Akrikhin, with atrial fibrillation, supraventricular tachycardia, sinus tachycardia against the background of functional cardiac pathologies and hyperthyroidism, slows down the heart rate and can even serve to restore sinus rhythm.
Taking the drug prevents the occurrence of migraines.
In contrast to non-selective β-blockers, the use of the drug in moderate therapeutic doses affects carbohydrate metabolism and organs containing β2-adrenergic receptors (smooth muscles of the uterus, bronchi and peripheral arteries, skeletal muscles, pancreas) less pronounced.
The use of the substance in large doses (more than 0.1 g per day) has a blocking effect on both subtypes of β-adrenergic receptors.
Pharmacokinetics
When taken orally, metoprolol is completely absorbed (95%), and its maximum concentration in the blood plasma is observed after 1-2 hours. The average half-life of the drug is 3.5 hours (varies from 1 to 9 hours).
The substance undergoes intensive first-pass metabolism. Its bioavailability at the first intake is 50%, and with repeated use it increases to 70%. Bioavailability increases with food intake (by 20-40%) and against the background of liver cirrhosis.
The connection of metoprolol with blood plasma proteins is 10%. It crosses the placental / blood-brain barrier, as well as into breast milk (in small quantities). The metabolism of the drug is carried out in the liver with the participation of the isoenzyme CYP2D6, with the formation of 2 metabolites with β-adrenergic blocking activity. Approximately 5% of the substance is excreted unchanged by the kidneys.
No dosage adjustment is required for patients with reduced renal function.
In case of impaired liver function, the metabolism of the drug slows down. Its dose is reduced in the presence of liver failure.
Metoprolol-Akrikhin is not removed during hemodialysis.
Indications for use
- arterial hypertension (as monotherapy or in combination with other antihypertensive drugs);
- coronary heart disease - angina pectoris (for the prevention of seizures), myocardial infarction (for secondary prevention, as part of complex therapy);
- heart rhythm disturbances (ventricular premature beats, supraventricular tachycardia);
- hyperthyroidism (as part of complex treatment);
- migraine (for the prevention of attacks).
Contraindications
Absolute:
- chronic heart failure in the stage of decompensation;
- atrioventricular block II and III degree;
- severe bradycardia;
- sick sinus syndrome;
- Prinzmetal's angina;
- cardiogenic shock;
- sinoatrial blockade;
- arterial hypotension (when prescribing a drug for secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg, heart rate less than 45 beats per minute);
- glucose-galactose malabsorption, lactase deficiency or lactose intolerance;
- combination therapy with monoamine oxidase inhibitors, combined intravenous administration of verapamil;
- period of breastfeeding;
- age under 18;
- individual intolerance to the components of the drug and other β-blockers.
Relative (Metoprolol-Akrikhin is prescribed under medical supervision):
- chronic renal and / or hepatic failure;
- metabolic acidosis;
- chronic obstructive pulmonary disease (chronic obstructive bronchitis, pulmonary emphysema);
- bronchial asthma;
- diabetes;
- myasthenia gravis;
- obliterating diseases of peripheral vessels (Raynaud's syndrome, intermittent claudication);
- pheochromocytoma (with combined treatment with α-blockers);
- thyrotoxicosis;
- atrioventricular block I degree;
- depression, including a history;
- psoriasis;
- pregnancy;
- elderly age.
Metoprolol-Akrikhin, instructions for use: method and dosage
Metoprolol-Akrikhin tablets are taken orally, simultaneously with food or immediately after taking it, not chewed and washed down with a liquid (a small amount).
Recommended dosage regimen:
- arterial hypertension: initial dose - 1-2 tablets per day in 1 or 2 doses (in the morning and evening). If the therapeutic effect is insufficient, the dose can be gradually increased to 2–4 tablets per day and / or other antihypertensive drugs may be additionally prescribed. The maximum dose is 4 tablets per day;
- migraine (prevention of seizures), arrhythmia, angina pectoris: 2 to 4 tablets per day, divided into 2 doses (in the morning and evening);
- myocardial infarction (for secondary prevention): 4 tablets per day, divided into 2 doses (in the morning and evening);
- hyperthyroidism: 1 tablet 2 times a day (in the morning and evening).
Correction of the dosage regimen during hemodialysis, against the background of impaired renal function and for elderly patients is not carried out.
In cases of liver dysfunction, the dose of Metoprolol-Akrikhin, depending on the patient's clinical condition, is reduced.
Side effects
Possible side reactions of Metoprolol-Akrikhin [> 10% - very often; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <(0.01%, including isolated messages) - very rare]:
- central nervous system: slowing down of the speed of motor and mental reactions, headache, weakness, increased fatigue; rarely - muscle weakness, paresthesia in the limbs (with intermittent claudication and Raynaud's syndrome), short-term memory impairment or confusion, nightmares, insomnia, drowsiness, decreased attention, anxiety, depression;
- sense organs: rarely - tinnitus, conjunctivitis, soreness and dryness of the eyes, decreased secretion of lacrimal fluid, decreased vision;
- cardiovascular system: orthostatic hypotension (dizziness, sometimes loss of consciousness), decreased blood pressure, palpitations, sinus bradycardia; rarely - impaired myocardial conduction, manifestation of angiospasm (Raynaud's syndrome, coldness of the lower extremities, increased disturbance of peripheral circulation), arrhythmia, temporary worsening of manifestations of chronic heart failure (shortness of breath, edema, swelling of the lower legs and / or feet), decreased myocardial contractility;
- digestive system: change in taste, constipation, diarrhea, dry mouth, abdominal pain, nausea, vomiting;
- skin: reversible alopecia, increased sweating, photodermatosis, exanthema, skin flushing, psoriasis-like skin reactions, exacerbation of psoriasis, urticaria, skin rash, itching;
- respiratory system: shortness of breath, difficulty in exhaling (bronchospasm when administered in high doses - loss of selectivity and / or in predisposed patients), nasal congestion;
- endocrine system: hypoglycemia (in patients receiving insulin); rarely - hyperglycemia (with insulin-dependent diabetes mellitus);
- laboratory parameters: rarely - an increase in the activity of liver enzymes, leukopenia, agranulocytosis, thrombocytopenia (unusual bleeding and hemorrhage); extremely rare - hyperbilirubinemia;
- effect on the fetus: bradycardia, hypoglycemia, intrauterine growth retardation;
- others: back or joint pain; in isolated cases, taking metoprolol, like other β-blockers, can lead to slight weight gain, decreased potency and / or libido.
Overdose
The main symptoms of an overdose of Metoprolol-Akrikhin: nausea, vomiting, fainting, dizziness, bronchospasm, ventricular premature beats, arrhythmia, marked decrease in blood pressure, cyanosis, severe sinus bradycardia. In cases of acute overdose, cardialgia, atrioventricular blockade (up to the development of complete transverse blockade and cardiac arrest), loss of consciousness, cardiogenic shock and coma are possible. The first manifestations of metoprolol intoxication are noted after a period of 20 to 120 minutes after taking it.
Therapy: the appointment of adsorbent drugs, gastric lavage, symptomatic treatment. If the patient has a marked decrease in blood pressure, he needs to take the Trendelenburg position.
With an excessive decrease in blood pressure, bradycardia and heart failure, β-adrenergic agonists are injected intravenously at intervals of 2-5 minutes until the desired effect is achieved, or from 0.5 to 2 mg of atropine sulfate. If there is no positive effect, norepinephrine (norepinephrine), dobutamine, or dopamine are prescribed.
As a follow-up, it is allowed to install a transvenous intracardiac pacemaker, administer 1–10 mg of glucagon. With the development of bronchospasm, the patient is injected intravenously with β2-adrenergic agonists.
Through hemodialysis, the drug is removed poorly.
special instructions
Monitoring patients receiving β-blocker therapy includes regular monitoring of blood pressure, heart rate, glucose concentration in patients with diabetes mellitus. On an individual basis, if necessary, with diabetes mellitus, a dose of insulin or hypoglycemic drugs for oral administration is selected.
The patient should be trained in the method of calculating the heart rate and instructed to seek medical advice if the indicator is less than 50 beats per minute. Doses in excess of 4 tablets per day reduce cardioselectivity. In cases of heart failure, Metoprolol-Akrikhin is started only after the compensation stage has been reached.
The likelihood of increased severity of hypersensitivity reactions (with a burdened history) and the lack of effect from the introduction of epinephrine (adrenaline) in usual doses should be taken into account.
Metoprolol-Akrikhin may enhance the manifestations inherent in impaired peripheral arterial circulation.
Cancellation of the drug should be carried out gradually, reducing the dose over 10 days. Abrupt cessation of therapy can lead to the development of a withdrawal syndrome (increase in blood pressure, increased angina attacks). Particular attention should be paid to patients with angina pectoris during the period of discontinuation of metoprolol.
In cases of exertional angina, the prescribed dose of Metoprolol-Akrikhin should provide a heart rate at rest in the range from 55 to 60 beats per minute, and with loads - no more than 110 beats per minute.
When using contact lenses, it is important to keep in mind that taking beta-blockers can reduce the production of tear fluid.
The drug may mask some of the clinical symptoms of hyperthyroidism (eg, tachycardia). Abrupt withdrawal of treatment is contraindicated in patients with thyrotoxicosis, as it can aggravate the symptoms.
Against the background of diabetes mellitus, Metoprolol-Akrikhin can mask tachycardia caused by hypoglycemia. In comparison with nonselective β-blockers, the drug practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal values.
If Metoprolol-Akrikhin is necessary for pheochromocytoma, α-adrenergic blockers are used as concomitant therapy, and β2-adrenomimetics are used for bronchial asthma.
If an operation is necessary, the anesthesiologist should be informed in advance about the therapy with metoprolol, so that he can select a means for general anesthesia with a minimal negative inotropic effect. Cancellation of the drug in such cases is not recommended.
Strengthening the action of β-blockers is possible with the combined use of drugs that reduce the reserves of catecholamines (for example, reserpine). In this regard, for patients receiving such a combination, constant medical supervision should be established in order to detect bradycardia and an excessive decrease in blood pressure.
In elderly patients, it is recommended to regularly monitor liver function. If there is ventricular arrhythmia, atrioventricular block, increasing bradycardia (less than 50 beats per minute), bronchospasm, a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg) or severe liver dysfunction, the dosage regimen is adjusted. In some cases, it may be necessary to cancel therapy.
In severe renal failure, it is important to monitor renal function.
The condition of patients with depressive disorders receiving Metoprolol-Akrikhin should be monitored. With the development of depression caused by the use of β-blockers, therapy is discontinued.
Influence on the ability to drive vehicles and complex mechanisms
The initiation of drug therapy may be accompanied by the development of fatigue and dizziness. In such cases, patients should refrain from driving vehicles and conducting potentially hazardous activities, the performance of which requires the speed of psychomotor reactions and increased concentration of attention. In the future, the safety of the dose of Metoprolol-Akrikhin is determined on an individual basis.
Application during pregnancy and lactation
Metoprolol-Akrikhin during pregnancy is prescribed with caution in cases where the potential benefit of therapy for the mother is higher than the estimated risks of hypoglycemia, arterial hypotension or bradycardia in the fetus. In this case, careful medical supervision should be carried out, especially for the development of the fetus. Close monitoring of the newborn is also required for the period from 48 to 72 hours after delivery.
Since the effect of metoprolol on a breastfed newborn has not been studied, breastfeeding should be discontinued while using it.
Pediatric use
Metoprolol-Akrikhin is not prescribed for children and adolescents under 18 years old, since the safety and effectiveness of its use in patients of this age group have not been established.
With impaired renal function
In chronic renal failure, Metoprolol-Akrikhin is prescribed with caution.
For violations of liver function
The use of the drug in patients with chronic hepatic insufficiency requires medical supervision.
Use in the elderly
Elderly patients need to be careful with drug therapy.
Drug interactions
Possible interactions of Metoprolol-Akrikhin with other substances / drugs:
- monoamine oxidase inhibitors: its hypotensive effect can be significantly enhanced. The use of the combination is not recommended; a break of 14 days (at least) should be observed between taking the drugs;
- verapamil for intravenous administration: cardiac arrest is possible;
- nifedipine: significant reduction in blood pressure;
- drugs for inhalation anesthesia (hydrocarbon derivatives): an increase in the likelihood of suppression of myocardial function and the occurrence of arterial hypotension;
- estrogens, cocaine, theophylline, β-adrenomimetics (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (blocking the synthesis of prostaglandin by the kidneys, sodium retention): weakening its hypotensive effect;
- ethanol: increased inhibitory effect on the central nervous system, increased risk of a pronounced decrease in blood pressure;
- drugs for anesthesia: summation of the cardiodepressant effect;
- ergot alkaloids: increased risk of peripheral circulatory disorders;
- hypoglycemic agents for oral administration: their therapeutic effect may decrease;
- insulin: increasing the risk of hypoglycemia, increasing its severity and lengthening, masking some manifestations of pathology (increased blood pressure, sweating, tachycardia);
- blockers of slow calcium channels, nitroglycerin, diuretics, antihypertensive drugs: a sharp decrease in blood pressure is possible. Particular care should be taken when using a combination with prazosin;
- cardiac glycosides, agents for general anesthesia, guanfacine, clonidine, methyldopa, reserpine, amiodarone (antiarrhythmics), diltiazem, verapamil: increasing the severity of a decrease in heart rate, inhibition of atrioventricular conduction;
- clonidine: Withdrawal may develop. In this regard, upon termination of metoprolol therapy, clonidine treatment is canceled after several days;
- inducers of liver microsomal enzymes (barbiturates, rifampicin): increased metabolism, decreased plasma concentration and decreased therapeutic effect;
- inhibitors (phenothiazines, oral contraceptives, cimetidine): an increase in its concentration in blood plasma;
- allergens prescribed for immunotherapy, allergen extracts for skin tests: increased likelihood of developing systemic allergic reactions or anaphylaxis;
- iodine-containing X-ray contrast agents for intravenous administration: increased risk of anaphylactic reactions;
- xanthines (except diphylline): decrease in the clearance of metoprolol, especially in cases of an initial increase in the clearance of theophylline under the influence of smoking;
- lidocaine: a decrease in the clearance of metoprolol and an increase in its concentration in blood plasma;
- antidepolarizing muscle relaxants: prolongation and enhancement of their action;
- coumarins: lengthening their anticoagulant effect.
Analogs
The analogues of Metoprolol-Akrikhin are Serdol, Metoprolol-Teva, Corvitol 50, Egilok Retard, Metocard, Betalok ZOK, Metoprolol Zentiva, Metokor Adipharm, Betalok, Metoprolol.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Metoprolol-Akrikhin
According to reviews, Metoprolol-Akrikhin is a safe, affordable and effective drug used in the treatment of migraines and tachycardia. In some cases, with prolonged therapy, the drug is addictive - after its cancellation, shortness of breath appears and the heart rate increases.
Price for Metoprolol-Akrikhin in pharmacies
The approximate price for Metoprolol-Akrikhin, 50 mg tablets, in a package of 30 tablets, is 58 rubles.
Metoprolol-Akrikhin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Metoprolol-Akrikhin 50 mg tablets 30 pcs. 35 RUB Buy |
|
Metoprolol-Akrikhin tablets 50mg 30 pcs. RUB 61 Buy |
|
Metoprolol-Akrikhin 50 mg tablets 60 pcs. RUB 76 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!
