Metoprolol pills 50mg, 30pcs

Composition

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), red dye (Ponceau 4R).

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.

Indications

— arterial hypertension (as monotherapy or in combination with other antihypertensive agents), including hyperkinetic type, tachycardia;

— ischemic heart disease: myocardial infarction (secondary prevention-complex therapy), prevention of angina attacks;

the heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystoles);

— hyperthyroidism (complex therapy);

prevention of migraine attacks.

Contraindications

AV block II, III degree, sinoatrial block, bradycardia (heart rate less than 50 beats / min), SSR, hypotension, chronic heart failure II-III stages, acute heart failure, cardiogenic shock, metabolic acidosis, severe peripheral circulatory disorders, hypersensitivity to metoprolol.

Side effects

From the cardiovascular system:  possible bradycardia, arterial hypotension, impaired AV conduction, the appearance of symptoms of heart failure.

From the digestive system:  at the beginning of therapy, dry mouth, nausea, vomiting, diarrhea, constipation are possible; in some cases, liver function disorders may occur.

From the central nervous system and peripheral nervous system:  at the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, a feeling of cold and paresthesia in the extremities are possible; there may be a decrease in the secretion of tear fluid, conjunctivitis, rhinitis, depression, sleep disorders, nightmares.

From the hematopoietic system:  in some cases – thrombocytopenia.

From the endocrine system:  hypoglycemic conditions in patients with diabetes mellitus.

Respiratory system disorders:  predisposed patients may develop symptoms of bronchial obstruction. Allergic reactions:  skin rash, itching.

Interaction

With the simultaneous use of metoprolol and verapamil, there is a decrease in the minute and stroke volume of the heart, pulse rate. With intravenous use of verapamil while taking metoprolol, there is a risk of cardiac arrest.

Concomitant use of metoprolol with calcium channel blockers, cardiac glycosides, reserpine, nitrates, and clonidine increases the risk of hypotension, bradycardia, and AV block. Metoprolol enhances the effect of hypoglycemic drugs. Indometacin and other NSAIDs, as well as estrogens, reduce the hypotensive effect of metoprolol.

The introduction of drugs for inhalation anesthesia against the background of metoprolol increases the risk of inhibition of myocardial function and the development of arterial hypotension.

Rifampicin reduces the concentration of metoprolol in the blood. The level of metoprolol in blood plasma increases with simultaneous use of hydralazines, oral contraceptives, ranitidine, cimetidine.

How to take, course of use and dosage

Tablets are taken orally with a small amount of liquid, without chewing, with a meal or immediately after a meal.

Tablets can be divided.

The course of treatment is not limited in time and depends on the characteristics of the course of the disease.

If it is necessary to cancel treatment, the dose is reduced gradually (at least for 10 days). under the supervision of a doctor.

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.

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).

Functional disorders of cardiac activity, accompanied by tachycardia

100 mg per day in two doses (morning and evening).

When the therapeutic effect is achieved, the dose is reduced (under the supervision of a doctor).

Elderly patients are recommended to start treatment with 50 mg / day.

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 use of adsorbents; symptomatic therapy: with a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position; in case of excessive decrease in blood pressure, bradycardia and heart failure-IV, at intervals of 2-5 minutes, bata-adrenostimulants-until the desired effect is achieved or iv 0.5-2 mg of 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.

Storage conditions

Store at a temperature not exceeding 30°C, in a dry place.

Shelf

life is 5 years.

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets