Metoprolol-Acrichine pills 50mg, 30pcs

Composition

1 tablet contains:

Active ingredients:

metoprolol tartrate 50 mg.

Auxiliary substances:

colloidal anhydrous silicon dioxide,

microcrystalline cellulose,

sodium carboxymethyl starch (type A),

magnesium stearate.

Shell composition:

hypromellose,

polysorbate 80,

talc,

titanium dioxide (E 171).

Pharmacological action

Metoprolol is a cardioselective beta-adrenergic receptor blocker with no intrinsic sympathomimetic activity or membrane-stabilizing properties. It has antihypertensive, antianginal and antiarrhythmic effects.

By blocking the beta-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular Ca2+ current, and has a negative chrono -, dromo -, batmo -, and inotropic effect (reduces heart rate, inhibits conduction and excitability, and reduces myocardial contractility).

Total peripheral resistance 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 the activity of alpha-adrenergic receptors and elimination of beta-adrenergic stimulation), which returns to the initial value after 1-3 days, and decreases with prolonged use.

The acute antihypertensive effect is due to a decrease in cardiac output, a stable antihypertensive effect develops within 2-3 weeks and is due to a decrease in renin synthesis and plasma renin accumulation, inhibition of the renin-angiotensive system activity (of great importance in patients with initial renin hypersecretion) and the central nervous system, restoration of the sensitivity of aortic arch baroreceptors (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 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. Blood pressure decreases after 15 minutes, maximum-after 2 hours and continues for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular intake.

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 hyperthyroidism, it reduces the heart rate, or even can lead to the restoration of sinus rhythm. Prevents the development of migraines.

When used in medium therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on the organs containing beta-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.

PHARMACOKINETICS

Metoprolol is rapidly and almost completely (95%) absorbed in the gastrointestinal tract. Cmax in blood plasma is reached 1-2 hours after oral use. T1 / 2 averages 3.5 hours (ranging from 1 hour to 9 hours).

Bioavailability is 50% at the first dose and increases to 70% with repeated use. Food intake increases bioavailability by 20-40%. The bioavailability of metoprolol increases in cirrhosis of the liver. Binding to plasma proteins is on average 10%.

The drug penetrates through the blood-brain and placental barriers. It is excreted in breast milk in small amounts.

It is metabolized in the liver. The metabolites have no pharmacological activity. About 5% of the drug is excreted unchanged by the kidneys. Treatment of patients with reduced renal function does not require dose adjustment. Impaired liver function slows down the metabolism of the drug, and in cases of insufficient liver function, the dose of the drug should be reduced. It is not removed during hemodialysis.

Indications

• hypertension, arterial hypertension I and II degree (can monotherapy in severe cases in combination with diuretics and other antihypertensive drugs);
• angina, prevention of angina attacks;
• the rhythm of the heart (supraventricular tachycardia, paroxysmal supraventricular tachycardia, extrasystoles);
• acute myocardial infarction and secondary prevention after myocardial infarction;
• cardiac hyperkinetic syndrome, essential cardiovascular hyperkinesis, functional disorders of cardiac activity, accompanied by palpitations;
• idiopathic dilated cardiomyopathy;
• mitral valve prolapse;
• to reduce morbidity and risk of death in the cardiovascular diseases and coronary heart disease (including sudden death);
• prevention of migraine attacks;
• thyrotoxicosis (complex therapy);
• treatment of akathisia induced by neuroleptics.

Use during pregnancy and lactation

Metoprolol is contraindicated during pregnancy, lactation, and children.

Contraindications

• atrioventricular block II and III degree;
• sinoauricular blockade;
• sinus bradycardia (heart rate less than 60 per minute);
• the syndrome of weakness of the sinus node;
• hypotension (SBP less than 100 mm Hg. St. )
• congestive heart failure stage II and III, uncompensated heart failure;
• acute heart failure;
• cardiogenic shock (metoprolol should not be administered to patients with suspected acute myocardial infarction);
• metabolic acidosis;
• susceptibility to bronchospasm (bronchial asthma, bronchial overreaction);
• labile form of diabetes mellitus, hypoglycemia;
• severe peripheral circulatory disorders;
• simultaneous reception of MAO inhibitors;
• individual intolerance (including a history of hypersensitivity) metoprolol.

Restrictions to use:  Severe allergic history, bronchial asthma, emphysema, non-allergic bronchitis, hyperthyroidism, psoriasis, pheochromocytoma, liver and/or kidney function disorders, myasthenia gravis, depression, general anesthesia, pregnancy, breast-feeding, elderly and children.

Side effects

Nervous system disorders:  increased fatigue, weakness, headache, slowing of 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, nightmares, confusion or short-term memory impairment, muscle weakness.

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

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, cardialgia.

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

From the side of the skin:  urticaria, pruritus, rash, psoriasis exacerbation, psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

Respiratory system disorders:  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 diabetes mellitus), hypothyroidism.

Laboratory parameters:  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 services:  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.

Interaction

Concomitant use with monoamine oxidase (MAO) inhibitors is not recommended due to a significant increase in the hypotensive effect. The treatment interval between taking MAO inhibitors and metoprolol should be at least 14 days.

Simultaneous intravenous use of verapamil may cause cardiac arrest. Simultaneous use of nifedipine leads to a significant decrease in blood pressure.

Inhaled anaesthetic agents (hydrocarbon derivatives) increase the risk of myocardial function depression and hypotension.

Beta-adrenostimulants, theophylline, cocaine, estrogens (sodium retention), Indometacin and other nonsteroidal anti-inflammatory drugs (sodium retention and blocking prostaglandin synthesis by the kidneys) weaken the hypotensive effect.

There is an increase in the depressive effect on the central nervous system – with ethanol ; summation of the cardiodepressive effect – with anesthesia; an increase in the risk of peripheral circulatory disorders – with ergot alkaloids.

When taken together with oral hypoglycemic agents, their effect may decrease; with insulin, it may increase the risk of hypoglycemia, increase its severity and lengthening, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

When combined with antihypertensive agents, diuretics, nitroglycerin or slow calcium channel blockers, a sharp decrease in blood pressure may develop (special caution is necessary when combined with prazosin); an increase in the severity of heart rate reduction and atrioventricular conduction depression when using metoprolol with verapamil, diltiazem, antiarrhythmic agents (amiodarone), reserpine, clonidine, guanfacine, general anesthesia and cardiac glycosides.

Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in metoprolol metabolism, a decrease in the concentration of metoprolol in blood plasma and a decrease in the effect.

Inhibitors (cimetidine, oral contraceptives, phenothiazines) – increase the concentration in blood 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 use increase the risk of anaphylactic reactions.

Reduces the clearance of xanthine (except diphylline), especially in patients with initially increased clearance of theophylline under the influence of smoking. Reduces the clearance of lidocaine, increases the concentration of lidocaine in blood plasma. Enhances and prolongs the action of antidepolarizing muscle relaxants; prolongs the anticoagulant effect of coumarins.

When combined with ethanol, the risk of a pronounced decrease in blood pressure increases.

How to take, course of use and dosage

Inside, with food or immediately after a meal, without chewing and washing down with 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 other antihypertensive agents are additionally prescribed.

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 divided doses (morning and evening).

Functional disorders of cardiac activity accompanied by tachycardia: 100 mg per day in two divided doses (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 the drug 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 in 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 must be in the Trendelenburg position; in case of excessive decline in blood pressure, bradycardia and heart failure in/in, at intervals of 2-5 min, the bat-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 prescribe 1-10 mg of glucagon, setting up a transvenous intracardial electrostimulator. In case of bronchospasm, intravenous beta-1-adrenergic stimulants should be administered. For convulsions-slow intravenous use of diazepam. Hemodialysis is not effective.

Special instructions

Monitoring of patients taking beta-blockers includes regular monitoring of heart rate and blood pressure, blood glucose in patients with diabetes mellitus (1 time in 4-5 months).

If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed by mouth should be selected individually.

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 beats/min.

When taking a dose higher than 200 mg per day, cardioselectivity decreases.

In heart failure, treatment with metoprolol begins 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 (epinephrine). It may increase the symptoms of peripheral arterial circulation disorders.

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.

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 of no more than 110 beats / min.

Patients who use contact lenses should take into account that against the background of treatment with beta-blockers, tear fluid production may decrease.

Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase 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 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 general anesthesia agent with minimal negative inotropic effect), and discontinuing the drug is not recommended.

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 lowering of blood pressure and bradycardia.

Special monitoring should be carried out for patients with depressive disorders taking metoprolol; in case of depression caused by taking beta-blockers, it is recommended to stop therapy.

During treatment with metoprolol, appropriate clothing should be worn, as the drug may cause skin allergies to sunlight.

In elderly patients, monitoring of liver function is recommended. Correction of the dosage regimen is required only if elderly patients develop increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver function disorders, and sometimes it is necessary to stop treatment.

Due to the lack of sufficient clinical data, the drug is not recommended for use in children.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, and to exclude the use of ethanol.

Form of production

Pills.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Angina, Hypertension, Myocardial Infarction, Migraine, Arrhythmia