Metoprolol retard-Akrikhin 50 mg long-acting tablets 30

$22.80
Size chart
Women's clothing size
SizeXSSML
Euro 32/34 36 38 40
USA 0/2 4 6 8
Bust(in) 31-32 33 34 36
Bust(cm) 80.5-82.5 84.5 87 92
Waist(in) 24-25 26 27 29
Waist(cm) 62.5-64.5 66.5 69 74
Hips(in) 34-35 36 37 39
Hips(cm) 87.5-89.5 91.5 94 99
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Description
Country
Russia
Active ingredient
Metoprolol
Dosage
50 mg
Composition

Active substance: metoprolol succinate 47.66 mg, which corresponds to the content of metoprolol tartrate 50 mg.

Excipients: hypromellose - 161.29 mg, ludipress LCE (lactose monohydrate - 94.7-98.3%, povidone - 3-4%) - 87.42 mg, silicon dioxide colloidal - 1.5 mg, magnesium stearate - 1.5 mg.

Composition of the shell: ready-made mixture "Opadrai II" green color (polyvinyl alcohol - 6 mg, talc - 2.22 mg, macrogol - 3.03 mg, titanium dioxide - 2.925 mg, quinoline yellow dye (aluminum varnish) - 0.268 mg, iron oxide black dye - 0.015 mg, indigo carmine dye (aluminum varnish) - 0.542 mg) - 15 mg.

Pharmacological properties

Cardioselective beta1-blocker. Does not membrane-stabilizing action and does not have internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects.

Blocking in low doses β1-adrenergic receptors of the heart, 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). OPSS 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 α-adrenergic receptors and the elimination of stimulation of β2-adrenergic receptors), after 1-3 days it returns to the original one, and with prolonged administration it decreases.

Antihypertensive effect is due to a decrease in the minute volume of blood flow and renin synthesis, inhibition of THE activity of RAAS (of greater importance in patients with initial hypersecretion renin) and the central nervous system, restoring 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. The antihypertensive effect lasts more than 24 hours.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (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 the tolerance of physical activity. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure.

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 the 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 along additional pathways.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart disease and thyrotoxicosis, it reduces heart rate or can even lead to the restoration of sinus rhythm.

Prevents the development of migraine.

Unlike non-selective beta-blockers, when administered in medium therapeutic doses, it has a less pronounced effect on organs containing β2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism; the severity of the atherogenic action does not differ from the action propranolol. With long-term intake, it reduces the concentration of cholesterol in the blood. When used in large doses (more than 100 mg / day), it has a blocking effect on both subtypes of β-adrenergic receptors.

Indications for use
  • arterial hypertension;
  • chronic heart failure of II-IV functional class according to the NYHA classification in the stage of compensation (as part of complex therapy);
  • IHD: prevention of attacks of stable angina pectoris, reduction of mortality and frequency of repeated myocardial infarction after the acute phase of myocardial infarction;
  • heart rhythm disturbances, including supraventricular tachycardia, a decrease in the frequency of ventricular contraction during atrial fibrillation and ventricular extrasystoles;
  • functional disorders of cardiac activity, accompanied by tachycardia;
  • prevention of migraine attacks.
Contraindications
  • cardiogenic shock;
  • AV blockade of the II-III degree;
  • sinoatrial blockade;
  • CCSU;
  • pronounced bradycardia (heart rate <50 beats / min);
  • acute heart failure or chronic heart failure in the stage of decompensation;
  • arterial hypotension (systolic blood pressure <100 mm Hg);
  • acute myocardial infarction (heart rate <45 beats / min, PQ interval more than 0.24 s, systolic blood pressure <100 mm Hg);
  • severe bronchial asthma;
  • severe disorders of peripheral circulation;
  • simultaneous administration of MAO inhibitors or simultaneous intravenous administration of verapamil;
  • pheochromocytoma (without simultaneous administration of alpha-blockers);
  • age up to 18 years (efficacy and safety have not been established);
  • lactation period;
  • lactase deficiency, lactose intolerance, glucose/galactose malabsorption syndrome;
  • hypersensitivity to metoprolol and other beta-blockers.

With caution, the drug should be prescribed for diabetes mellitus, AV blockade of the I degree, Prinzmetal's angina, metabolic acidosis, bronchial asthma, COPD, severe renal and / or hepatic insufficiency, myasthenia gravis, pheochromocytoma (while taking alpha-blockers), thyrotoxicosis, depression (including a history), psoriasis, peripheral circulatory disorders (intermittent claudication, Raynaud's syndrome), pregnancy, as well as elderly patients.

Use in pregnancy and lactation

During pregnancy, the drug Metoprolol retard-Akrikhin should be used only for strict indications, when the expected benefit to the mother exceeds the potential risk for fetus / child (due to the possible development of bradycardia in a newborn, a decrease in blood pressure, hypoglycemia and respiratory paralysis). At the same time, careful monitoring is carried out, especially for the development of the fetus. Treatment is stopped 48-72 hours before the onset of childbirth. If this is not possible, then the newborn should be under particularly close observation for 48-72 hours after childbirth.

The use of the drug Metoprolol retard-Akrikhin is contraindicated during lactation. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Use in case of impaired liver function

Impaired liver function affects the excretion of metoprolol, so dose adjustment may be required depending on the clinical condition.

Use in renal dysfunction

Patients with renal insufficiency or patients on hemodialysis do not need dose adjustment.

Application in children

Contraindicated in children and adolescents under 18 years of age.

Use in elderly patients

Elderly patients do not need dose adjustment.

In elderly patients, it is recommended to monitor kidney function (1 time in 4-5 months).

Special instructions

Control of patients taking beta-blockers includes regular monitoring of heart rate and blood pressure. 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.

It is possible to increase the severity of allergic reactions (against the background of a burdened allergic history) and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline).

In elderly patients, it is recommended to monitor kidney function (1 time in 4-5 months).

Taking the drug Metoprolol retard-Akrikhin may increase the symptoms of peripheral disorders arterial circulation.

With angina pectoris, the selected dose of the drug should provide a resting heart rate in the range of 55-60 beats / min, with a load - no more than 110 beats / min.

In smoking patients, the effectiveness of beta-blockers is lower.

Metoprolol retard-Akrikhin can mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since it can increase the symptoms.

In diabetes mellitus, taking the drug Metoprolol retard-Akrikhin can mask tachycardia caused by hypoglycemia.

If necessary, the appointment of patients with bronchial asthma as concomitant therapy is used beta 2 -adrenomimetics; with pheochromocytoma - alpha-blockers.

If it is necessary to carry out surgical intervention, it is necessary to warn the anesthesiologist about taking the drug Metoprolol retard-Akrikhin (it is necessary to choose a remedy for general anesthesia with minimal negative inotropic effect), discontinuation of the drug is not recommended.

Reciprocal activation of the vagus nerve can be eliminated intravenously by administering atropine (1-2 mg).

In case of increasing bradycardia (less than 50 beats / min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe impairment of liver and kidney function, it is necessary to reduce the dose or stop treatment.

It is recommended to stop therapy with the appearance of skin rashes and the development of depression caused by taking beta-blockers.

With a sharp withdrawal of clonidine, blood pressure can rise sharply, while taking beta-blockers. In case of withdrawal of clonidine, discontinuation of beta-blockers should be started a few days before the withdrawal of clonidine.

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 reduction in blood pressure or bradycardia.

With a sharp cessation of treatment, withdrawal syndrome may occur (increased attacks of angina pectoris, increased blood pressure). Particular attention when canceling the drug should be paid to patients with angina pectoris, chronic heart failure, after myocardial infarction. The abolition of the drug Metoprolol retard-Akrikhin is carried out gradually, reducing the dose for 10 days.

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.

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: severe bradycardia, AV-blockade (up to the development of a complete transverse blockade and cardiac arrest), excessive decrease in blood pressure, impaired peripheral circulation, increased symptoms of heart failure, cardiogenic shock, respiratory depression, apnea, cyanosis, increased fatigue, dizziness, loss of consciousness, coma, tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, possibly the development of esophagospasm, hypoglycemia or hyperglycemia, hyperkalemia, transient myasthenia gravis. The first signs of an overdose appear 20 minutes-2 hours after taking the drug.

Treatment: if the drug is taken recently - gastric lavage and taking adsorbents; in case of violation of AV-conduction and / or bradycardia - intravenous administration of 1-2 mg of atropine, epinephrine (adrenaline) or staging a temporary pacemaker; with a decrease in blood pressure, the patient should be transferred to the Trendelenburg position. If there are no signs of pulmonary edema - intravenous plasma-substituting solutions, with ineffectiveness - the introduction of epinephrine, dopamine, dobutamine; in acute heart failure - cardiac glycosides, diuretics; with convulsions - intravenous diazepam; with bronchospasm - inhaled or parenterally beta 2 - Adrenomimetics.

Drug Interactions

Agents that reduce the reserves of catecholamines (for example, reserpine, MAO inhibitors) when used simultaneously with metoprolol can enhance the hypotensive effect or cause pronounced bradycardia. The break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days.

Metoprolol is a substrate of the isoenzyme CYP2D6. Drugs that inhibit or induce the activity of CYP2D6 can affect the plasma concentration of metoprolol.

CYP2D6 inhibitors (some antidepressants and neuroleptics, quinidine, terbinafine, celecoxib, propafenone, diphenhydramine, hydroxychlorin, cimetidine) increase the concentration of metoprolol in the blood plasma.

Inducers CYP2D6 (derivatives of barbituric acid, rifampicin) reduce the concentration of metoprolol in the blood plasma.

Simultaneous administration of metoprolol with cardiac glycosides, clonidine, slow calcium channel blockers (verapamil, diltiazem), amiodarone, class I antiarrhythmic drugs, general anesthesia, methyldopa, guanfacine can lead to a decrease in blood pressure and severe bradycardia.

Means for inhalation anesthesia (hydrocarbon derivatives) with simultaneous use with metoprolol increase the risk of myocardial dysfunction and the development of arterial hypotension.

Simultaneous intravenous administration of verapamil can provoke cardiac arrest.

NSAIDs and beta-adrenomimetics weaken antihypertensive effect of beta-blockers.

Ergot alkaloids with simultaneous use with metoprolol increase the risk of peripheral circulatory disorders.

When metoprolol is taken together with oral hypoglycemic drugs, it is possible to reduce their effect; with insulin - increased risk of hypoglycemia, prolongation and intensification of its severity, masking of some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

Metoprolol reduces the clearance of xanthins (except diaphylline), especially in patients with initially increased clearance of theophylline under the influence of smoking.

Metoprolol reduces the clearance of lidocaine, increases the concentration of lidocaine in plasma.

Metoprolol enhances and prolongs the action of non-depolarizing muscle relaxants; prolongs the anticoagulant effect of coumarins.

With the simultaneous administration of epinephrine (adrenaline) with beta-blockers, it is possible to increase blood pressure and Aetiology.

Phenylpropanolamine (norephedrine) with simultaneous use with metoprolol can increase diastolic blood pressure.

Allergens used for immunotherapy or allergen extracts for skin tests when combined with methoprolol increase the risk of systemic allergic reactions or anaphylaxis.

Iodine-containing radiopaque agents for intravenous administration when combined with metoprolol increase the risk of anaphylactic reactions.

With the combined use of metoprolol with ethanol, the risk of a pronounced decrease in blood pressure increases.

Dosage and Administration

The drug Metoprolol retard-Akrikhin is taken orally 1 time / day. Tablets are recommended to be taken in the morning, without chewing, washed down with water. Metoprolol retard-Akrikhin can be taken regardless of food intake.

In order to prevent bradycardia, the dose is selected individually and increase gradually.

With arterial hypertension and angina pectoris, the initial dose is 50 mg 1 time / day, with insufficient therapeutic effect, the daily dose can be increased to 100-200 mg / day. With arterial hypertension with the ineffectiveness of the drug at a dose of 100-200 mg / day, another antihypertensive agent can be added.

In chronic heart failure of the II functional class according to the NYHA classification (without exacerbations of the last 6 weeks and without changes in complex therapy within the last 2 weeks), the recommended initial dose is 25 mg 1 time / day. After 2 weeks, the daily dose can be increased to 50 mg, then after 2 weeks - up to 100 mg, after another 2 weeks - up to 200 mg.

In chronic heart failure iii-IV functional class according to the NYHA classification, the recommended initial dose is the first 2 weeks 12.5 mg 1 time / day. It is possible to use metoprolol in another dosage form, for example, tablets of 25 mg with a risk. In the period of increasing the dose, the patient should be under observation, because in some patients the symptoms of heart failure may worsen.

After 1-2 weeks, the dose can be increased to 25 mg 1 time / day. Then, after 2 weeks, the dose can be increased to 50 mg 1 time / day. Patients who tolerate the drug well can double the dose every 2 weeks until the maximum dose of 200 mg is reached 1 time / day.

With secondary prevention of myocardial infarction and heart rhythm disturbances, the initial dose is 100 mg 1 time / day.

With functional disorders of cardiac activity, accompanied by tachycardia, 50 mg / day is prescribed, if necessary, the dose can be increased to 200 mg / day.

For the prevention of migraine attacks, 100-200 mg 1 time / day is prescribed.

Elderly patients, patients with renal insufficiency or patients on hemodialysis, dose adjustment is not required.

Impaired liver function affects the excretion of metoprolol, so dose adjustment may be required depending on the clinical condition.

Side effects

Frequency of side effects: very common (>1/10), often (>1/100 and <1/10), infrequent (>1/1000 and <1/100), rare (>1/10,000 and <1/1000), very rare (<1/10,000, including individual messages).

From the cardiovascular system: often - bradycardia, orthostatic hypotension (including fainting), cooling of the lower extremities, a feeling of palpitations; infrequently - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV-blockade of the I degree; rarely - myocardial conduction disorders, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders).

From the side of the central nervous system: very often - increased fatigue, a decrease in the speed of mental and motor reactions; often - dizziness, headache; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; rarely - asthenia, tremor, increased nervous excitability, anxiety; very rarely - amnesia / memory impairment, depression, hallucinations, myasthenia gravis.

From the senses: rarely - visual impairment, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, a violation of taste sensations.

From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function, hepatitis.

From the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis, psoriasis-like skin reactions.

From the respiratory system: often - shortness of breath; infrequently - bronchospasm in patients with bronchial asthma; rarely - rhinitis.

On the part of laboratory indicators: very rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of hepatic enzymes, hyperbilirubinemia.

From the endocrine system: often - hypoglycemia (in patients with type 1 diabetes mellitus), rarely - hyperglycemia (in patients with type 2 diabetes mellitus), hypothyroid condition.

Other: infrequently - an increase in body weight; rarely - impotence / sexual dysfunction; very rarely - arthralgia, thrombocytopenia.

Storage conditions

The drug should be stored in a dry, protected from light, out of the reach of children at a temperature not exceeding 25 ° C.

Shelf life - 2 years.

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Product Details

Data sheet

Brand
Akrikhin
service_future
otc_04
Dosage form
long-acting tablets
Dosage
50 mg
INN
Metoprolol
Number of tablets
30
INN Russian
Метопролол
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