Metoprolol-Akrikhin 50 mg tablets 30
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Active substance: metoprolol 50 mg.
Excipients: lactose, potato starch, silicon dioxide colloidal, magnesium stearate, povidone, sodium starch glycolate.
Metoprolol refers to cardioselective beta-adrenergic receptor blockers that do not have internal sympathomimetic activity and membrane-stabilizing properties. It has a hypotensive, antianginal and antiarrhythmic effect. By blocking the beta1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility).
The total peripheral resistance at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) - increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), which after 1-3 days returns to the original, and with prolonged use - decreases.
The hypotensive effect is due to a reflex decrease in cardiac output and synthesis of renin, inhibition of the activity of the renin-angiotensin-aldosterone system (of greater 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 in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure at rest, with physical exertion and stress. Hypotensive 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 intake.
The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of heart rate reduction (lengthening of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases tolerance to physical activity.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in retrograde directions) through the AV node and on additional paths.
With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart disease and hyperthyroidism, it reduces heart rate, or can even lead to the restoration of sinus rhythm.
Prevents the development of migraine. When used in medium therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, 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 beta-adrenergic receptors.
Indications for use
- arterial hypertension (as monotherapy or in combination with other antihypertensive drugs);
- ischemic heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks;
- heart rhythm disturbances (supraventricular tachycardia; ventricular extrasystole);
- hyperthyroidism (complex therapy);
- prevention of migraine attacks.
- cardiogenic shock;
- atrioventricular blockade (AV) II-III degree;
- sinoatrial (SA) blockade;
- syndrome of weakness of the sinus node;
- pronounced bradycardia;
- chronic heart failure in the stage of decompensation;
- Prinzmetal's angina;
- arterial hypotension (in the case of use in the secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg. st., heart rate less than 45 beats / min);
- lactation period;
- simultaneous reception MAO inhibitors or simultaneous intravenous administration of verapamil;
- age up to 18 years (efficacy and safety have not been established);
- lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
- hypersensitivity to metoprolol or other components of the drug, other beta-blockers;
With caution: diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), peripheral vascular obliterating diseases ("intermittent" claudication, Raynaud's syndrome), chronic hepatic and / or renal failure, myasthenia gravis, pheochromocytoma (with the simultaneous use of alpha-blockers), AV blockade of the first degree, thyrotoxicosis, depression (including a history), psoriasis, pregnancy, old age.
Use in pregnancy and lactation
During pregnancy, it is prescribed taking into account the ratio of benefits for the mother and the risk to the fetus (due to the development of bradycardia, arterial hypotension, hypoglycemia in the fetus). At the same time, careful monitoring is carried out, especially for the development of the fetus. It is necessary to monitor newborns for 48-72 hours after delivery.
The effect of metoprolol on a newborn during breastfeeding has not been studied, so women taking Metoprolol-Akrikhin should stop breastfeeding.
Use in case of impaired liver functionWith caution in chronic liver failure.
Use in renal dysfunctionWith caution in chronic renal failure.
Use in childrenContraindicated in children under 18 years of age.
Use in elderly patientsWith caution to elderly patients.
Control of patients taking beta-blockers, includes regular monitoring of heart rate and blood pressure, blood glucose in patients with diabetes. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed orally should be selected individually.
It is necessary to teach the patient the method of calculating heart rate and instruct about the need for medical advice with a heart rate of less than 50 beats / min. When taking a dose above 200 mg per day, cardioselectivity decreases.
In heart failure, treatment with metoprolol is started only after reaching the compensation stage.
It is possible to increase the severity of hypersensitivity reactions (against the background of a burdened allergic history) and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline).
May increase the symptoms of peripheral arterial circulation disorders. Cancellation of the drug is carried out gradually, reducing the dose for 10 days. In case of abrupt termination treatment may experience a syndrome of "cancellation" (increased attacks of angina pectoris, increased blood pressure).
Particular attention when canceling the drug should be paid to patients with angina pectoris. With angina pectoris, the selected dose of the drug should provide a resting heart rate of 55-60 beats / min, with a load - no more than 110 beats / min.
Patients using contact lenses should take into account that against the background of treatment with beta-blockers, it is possible to reduce the production of tear fluid. Metoprolol can mask some clinical manifestations of hyperthyroidism (for example, tachycardia). A sharp withdrawal in patients with thyrotoxicosis is contraindicated, since it can increase the symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of glucose concentration in blood to normal levels.
If it is necessary to prescribe patients with bronchial asthma, beta is used as concomitant therapy 2 -adrenomimetics; with pheochromocytoma - alpha-blockers.
If it is necessary to carry out surgical intervention, it is necessary to warn the anesthesiologist about the therapy (the choice of a means for general anesthesia with minimal negative inotropic effect), discontinuation of the drug is not recommended. Drugs that reduce the supply of catecholamines (for example, reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision for excessive lowering of blood pressure and bradycardia.
In elderly patients, it is recommended to regularly monitor liver function. Correction of the dosage regimen is required only if the patient has an elderly age increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe violations of liver function, sometimes it is necessary to stop treatment.
Patients with severe renal failure are advised to monitor kidney function.
Special monitoring of the condition of patients with depressive disorders taking metoprolol should be carried out; in the case of depression caused by taking beta-blockers, it is recommended to stop therapy.
Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Influence on the ability to drive vehicles and mechanisms
At the beginning of treatment with metoprolol, patients may experience dizziness, fatigue. In this case, they must refrain from driving vehicles and exercising. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions. In the future, the determination of the safety of the dose is carried out individually.
Symptoms: severe severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, a pronounced decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, in acute overdose - cardiogenic shock, loss of consciousness, coma, atrioventricular blockade (up to the development of complete transverse blockade and cardiac arrest), cardialgia.
The first signs of an overdose appear 20 min-2 hours after taking the drug.
Treatment: gastric lavage and taking adsorbents; symptomatic therapy: with a pronounced decrease in blood pressure - the patient should be in the Trendelenburg position; in case of excessive lowering of blood pressure, bradycardia and cardiac insufficiency - intravenously, with an interval of 2-5 minutes, beta-adrenomimetics - until the desired effect is achieved or intravenously 0.5-2 mg of atropine sulfate. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine).
As follow-up measures, it is possible to administer 1-10 mg of glucagon, the installation of a transvenous intracardiac electrostimulator. With bronchospasm, beta should be administered intravenously 2 - Adrenomimetics. Metoprolol is poorly excreted by hemodialysis.
Simultaneous 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. Simultaneous intravenous administration of verapamil can provoke cardiac arrest. Simultaneous administration of nifedipine leads to a significant decrease in blood pressure.
Tools for inhalation anesthesia (hydrocarbon derivatives) increase the risk of myocardial dysfunction and the development of arterial hypotension.
Beta-adrenomimetics, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blocking the synthesis of prostaglandin by the kidneys) weaken the hypotensive effect.
There is an increase in the depressant effect on the central nervous system - with ethanol; summation of the cardiodepressive effect - with means for anesthesia; increased risk of peripheral circulatory disorders - with ergot alkaloids.
When taken together with hypoglycemic agents for oral administration, it is possible to reduce their effect; with insulin - increased risk of hypoglycemia, increased severity and lengthening, masking of some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
When combined with antihypertensive drugs, diuretics, nitroglycerin or blockers of "slow" calcium channels may develop a sharp decrease in blood pressure (special care is necessary when combined with prazosin); an increase in the severity of heart rate reduction and inhibition of atrioventricular conduction - when using metoprolol with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, methyldopa, clonidine, guanfacine, general anesthesia and cardiac glycosides. If metoprolol and clonidine are taken simultaneously, then with the abolition of metoprolol, clonidine is canceled after a few days (due to the risk of "withdrawal" syndrome).
Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in the metabolism of metoprolol, to a decrease in its concentration in the blood plasma and a decrease in the effect. Inhibitors (cimetidine, oral contraceptives, phenothiazines) - increase the concentration of metoprolol in plasma.
Allergens used for immunotherapy or allergen extracts for skin tests when combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiopaque substances for intravenous administration increase the risk of anaphylactic reactions. Reduces the clearance of xanthine (except diphylline), especially with an initially increased clearance of theophylline under the influence of smoking. Reduces the clearance of lidocaine, increases the concentration of lidocaine in the blood plasma.
Enhances and prolongs the effect of antidepolarizing muscle relaxants; prolongs the an-ticoagulant effect of coumarins.
When combined with ethanol, the risk of a pronounced decrease in blood pressure increases.
Dosage and Administration
Tablets are taken orally during or immediately after a meal, do not chew, wash down with a small amount of liquid.
Start the daily dose is 50-100 mg in 1-2 doses (morning and evening). With insufficient therapeutic effect, the daily dose can be gradually increased to 100-200 mg and / or additional administration of other antihypertensive drugs. The maximum daily dose is 200 mg.
Angina pectoris, arrhythmias, prevention of migraine attacks
100-200 mg per day in two doses (morning and evening).
Secondary prevention of myocardial infarction
200 mg per day in two doses (morning and evening).
50 mg 2 times a day (morning and evening).
In elderly patients, with impaired renal function, as well as if necessary, hemodialysis, the dose is not changed. In case of impaired liver function, the dose of the drug should be reduced depending on the clinical condition.
From the central nervous system: increased fatigue, weakness, headache pain, slowing down the speed of mental and motor reactions; rarely - paresthesia in the limbs (in patients with "intermittent" claudication and Raynaud's syndrome), depression, anxiety, decreased attention, drowsiness, insomnia, "nightmare" dreams, confusion or short-term memory impairment, muscle weakness.
From the senses: rarely - decreased vision, decreased secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus.
From the cardiovascular system: sinus bradycardia, palpitations, lowering blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness); rarely - a decrease in myocardial contractility, a temporary aggravation of the symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), arrhythmias, angiospasm (increased peripheral circulatory disorders, cooling of the lower extremities, Raynaud's syndrome), a violation myocardial conduction.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, change in taste.
From the skin: urticaria, skin itching, rash, exacerbation of psoriasis, psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.
From the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when prescribed in high doses - loss of selectivity and / or in predisposed patients), shortness of breath.
From the endocrine system: hypoglycemia (in patients receiving insulin); rarely - hyperglycemia (in patients with insulin-dependent diabetes mellitus).
Laboratory indicators: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes, extremely rarely - hyperbilirubinemia.
Effect on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia.
Other: pain in the back or joints, like all beta-blockers in isolated cases, can cause a slight increase in body weight, a decrease in libido and / or potency.
In a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Shelf life - 4 years.
- Dosage form
- 50 mg
- Number of tablets
- INN Russian