Metoprolol retarde Acrichine pills 100mg, 30pcs

Composition

of 1 tab. : – metoprolol 100 mg

Auxiliary substances:

lactose,

potato starch,

colloidal silicon dioxide,

magnesium stearate,

povidone,

sodium starch glycolate.

Pharmacological action

Cardioselective beta-1-adrenoblocker. It does not have a membrane-stabilizing effect and does not have an internal SMA. It has antihypertensive, antiangial and antiarrhythmic effects. Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular Ca2+ current, has a negative chrono -, dromo -, batmo-and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility).

OPSS at the beginning of the use of beta-blockers (in the first 24 hours after oral use) increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta-2-adrenergic stimulation), which returns to its original value after 1-3 days, and decreases with prolonged use. The antihypertensive effect is due to a decrease in MOK and renin synthesis, inhibition of the activity of the renin-angiotensin system (which is more important in patients with initial hypersecretion of renin) and the central nervous system, restoration of the sensitivity of 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 elevated blood pressure at rest, during physical exertion and stress. The 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 use. The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation 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 exercise tolerance. By increasing the final diastolic pressure in the LV and increasing the stretching of the ventricular muscle fibers, it can increase the need for oxygen, especially in patients with CHF.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, 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 the retrograde directions through the AV node) and along additional pathways. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and thyrotoxicosis, it reduces the heart rate or can even lead to the restoration of the sinus rhythm.

Prevents the development of migraines. Unlike non-selective beta-blockers, when administered in medium therapeutic doses, it has a less pronounced effect on organs containing beta-2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism; the severity of the atherogenic effect does not differ from that of propranolol.

When taken for many years, 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 beta-adrenergic receptors. With intravenous infusion of metoprolol tartrate for 10 minutes or more, the maximum effect develops in 20 minutes, the decrease in heart rate at doses of 5 and 10 mg is 10 and 15%, respectively.

Indications

• ischemic heart disease: myocardial infarction (secondary prevention-complex therapy), prevention of angina attacks;
• arterial hypertension (as monotherapy or in combination with other antihypertensive agents);
• cardiac arrhythmias (supraventricular tachycardia; ventricular extrasystole);
• hyperthyroidism (complex therapy);
• prevention of migraine attacks.

Contraindications

• hypersensitivity to metoprolol, or other components of the drug, other beta-blockers;
• cardiogenic shock,
• atrioventricular block (AV) II-III degree,
• sinoatrial (SA) blockade;
• the syndrome of weakness of the sinus node;
• bradycardia;
• congestive heart failure in the stage of decompensation;
• Prinzmetal’s angina;
• hypotension (in case of use in the secondary prevention of myocardial infarction, systolic blood pressure less than 100 mm Hg. art, heart rate less than 45 beats/min);
• breast-feeding (see “Pregnancy and lactation”);
• simultaneous reception of monoamine oxidase inhibitors (MAOIs) or simultaneous intravenous use of verapamil (see “Interaction with other drugs”);
• the age of 18 years (effectiveness and safety not established);
• lactose intolerance, lactase deficiency or Glucose-galactose malabsorption.

Side effects

From the cardiovascular system: sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely-decreased myocardial contractility, temporary aggravation of symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), arrhythmias, angiospasm (increased peripheral circulatory disorders, cold of the lower extremities, Raynaud’s syndrome), impaired myocardial conduction.

From the sensory organs: rarely-decreased vision, decreased secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus.

From the central nervous system: increased fatigue, weakness, headache, slowing down the speed of mental and motor reactions. Rarely – paresthesia in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), depression, anxiety, decreased attention, drowsiness, insomnia, “nightmarish” dreams, confusion or short-term memory impairment, muscle weakness.

From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, taste changes.

Skin disorders: urticaria, pruritus, rash, psoriasis exacerbation, psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

From the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when administered 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 parameters: rarely-thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of “liver” enzymes, extremely rarely-Hyperbilirubinemia.

Effects on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia.

Other: back or joint pain, like all beta-blockers, may cause a slight increase in body weight, decreased libido and/or potency in isolated cases.

Interaction

Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving metoprolol.

Iodine-containing radiopaque drugs for intravenous use increase the risk of anaphylactic reactions. Phenytoin with intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure. Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. The antihypertensive effect is weakened by NSAIDs (Na + delay and blockade of Pg synthesis by the kidneys), corticosteroids and estrogens (Na+delay).

Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone, etc. Antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest, and heart failure. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

It prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills increase CNS depression. Concomitant use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, a break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

How to take it, course of use and dosage

Tablets are taken orally during or immediately after a meal, do not chew, drink a small amount of liquid.

Arterial hypertension: The initial daily dose is 50-100 mg in 1-2 divided doses (morning and evening). If the therapeutic effect is insufficient, the daily dose can be gradually increased to 100-200 mg and / or additional use of other antihypertensive agents. 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). Hyperthyroidism:50 mg 2 times a day (morning and evening).

In elderly patients, with impaired renal function, as well as if hemodialysis is necessary, the dose is not changed. In patients with impaired liver function, the dose of Metoprolol-Acri should be reduced depending on the clinical condition.

Overdose

Symptoms:

severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, syncope, acute overdose – cardiogenic shock, loss of consciousness, coma, atrioventricular block (up to the development of complete transverse block and cardiac arrest), cardialgia. The first signs of overdose appear 20 minutes -2 hours after taking the drug.

Treatment:

gastric lavage and the appointment of absorbent material; symptomatic treatment: when pronounced reduction of blood pressure, the patient should be in the Trendelenburg position; in case of excessive reduction in blood pressure, bradycardia and heart failure in/in, at intervals of 2-5 min, beta-agonists – to achieve the desired effect or/0.5-2 mg atropine sulfate. In the absence of a positive effect – dopamine, dobutamine or norepinephrine (norepinephrine).

As a follow-up, it is possible to administer 1-10 mg of glucagon, install a transvenous intracardial pacemaker. In case of bronchospasm, intravenous beta-2-adrenomimetics should be administered. Metoprolol is poorly excreted by hemodialysis.

Special instructions

 Monitoring of patients taking beta-blockers includes monitoring of heart rate and blood pressure (at the beginning of use – daily, then 1 time in 3-4 months), blood glucose concentration in diabetic patients (1 time in 4-5 months).

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50/min, the severity of allergic reactions may increase (against the background of a burdened allergic history) and there is no effect from the introduction of conventional doses of epinephrine. In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months). It may increase the symptoms of peripheral arterial circulation disorders.

Patients with cardiac arrhythmias who have systolic blood pressure below 100 mm Hg should be administered intravenously only if special precautions are taken (there is a risk of further lowering of blood pressure). Discontinuation of the drug is carried out gradually, reducing the dose over 10 days. With arterial hypertension, the effect occurs in 2-5 days, a stable effect is noted in 1-2 months. In case of stress angina, the selected dose of the drug should provide a resting heart rate of 55-60 beats / min, with a load of no more than 110 beats / min. In “smokers”, the effectiveness of beta-blockers is lower.

In combination therapy with clonidine, the latter should be discontinued several days after metoprolol is discontinued, in order to avoid a hypertensive crisis. When the dose is higher than 200 mg/day, cardioselectivity decreases. Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.

With diabetes, 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 blood glucose concentration to normal levels. If necessary, beta-2-adrenostimulants are used as concomitant therapy for patients with bronchial asthma; alpha-adrenoblockers are used for pheochromocytoma.

If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a drug for general anesthesia with minimal negative inotropic effect), and discontinuation of the drug is not recommended. Reciprocal activation of n. vagus can be eliminated by intravenous use of atropine (1-2 mg). Drugs that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for excessive blood pressure reduction or bradycardia.

If elderly patients develop increasing bradycardia (less than 50/min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney function disorders, the dose should be reduced or treatment should be discontinued.

It is recommended to stop therapy if skin rashes appear and depression develops due to taking beta-blockers. Discontinuation of the drug is carried out gradually, reducing the dose over 10 days. If treatment is abruptly discontinued, a “withdrawal” syndrome may occur (increased angina attacks, increased blood pressure).

Special attention should be paid to patients with angina pectoris when discontinuing the drug. Patients who use contact lenses should take into account that against the background of treatment with beta-blockers, tear fluid production may decrease. During pregnancy, it is prescribed only for strict indications (due to the possible development of bradycardia, hypotension, hypoglycemia and respiratory paralysis in the newborn). Treatment should be interrupted 48-72 hours before delivery.

In cases where this is not possible, it is necessary to ensure strict monitoring of newborns within 48-72 hours after delivery. During the treatment period, care should be taken when driving vehicles and doing other activities. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Pills.

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets