Metocard, pills 100mg, 30pcs

Composition

1 tablet contains metoprolol tartrate 100 mg

Pharmacological action

Metocardium – antiarrhythmic, hypotensive, antianginal.

Selectively blocks beta_-1-adrenergic receptors, interferes with the action of endogenous catecholamines, and inhibits the activity of the renin-angiotensin system.

Pharmacodynamics

Reduces minute volume and heart rate. Inhibits central sympathetic impulses. It does not have a membrane-stabilizing effect and does not have internal sympathomimetic activity.

Pharmacokinetics

It is rapidly and almost completely absorbed from the gastrointestinal tract. cmax and T_max when taking Metocard 100 mg or Metocard retard are 99.4±33 ng/mg and 1.58±0.55 h, or 152.9±72.8 ng/ml and 2.75±0.87 h. Protein binding is 11-12%. It is metabolized in the liver, T_1/2 — 3.5 hours. It is mainly excreted by the kidneys (95%). Passes through the placenta.

Indications

Arterial hypertension, CHD, heart failure

Contraindications

• pulse less than 50 beats per minute
• severe heart failure
• bronchial asthma
• severe liver and/or kidney function disorders
• hypersensitivity to Metocard.

Side effects

From the nervous system and sensory organs: headache, dizziness, nightmares, insomnia, depression, short-term amnesia, disorientation, paresthesia; visual impairment, dry eyes, tinnitus.

From the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia, palpitation, hypotension, violation of AV conduction, circulatory insufficiency, thrombocytopenia, agranulocytosis.

Respiratory system disorders: bronchospasm, suffocation.

Gastrointestinal disorders: dry mouth, heartburn, flatulence, stomach pain, vomiting, constipation/diarrhea.

Allergic reactions: itching, rash, psoriatic skin changes.

Others: Peyronie’s disease, myalgia, alopecia.

Interaction

Concomitant use of Metocardia with 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.

Concomitant use of nifedipine leads to a significant reduction in blood pressure.

Inhaled general anaesthetics (hydrocarbon derivatives) increase the risk of myocardial suppression and hypotension.

Beta-adrenostimulants, theophylline, cocaine, etrogens (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 general anesthesia; an increase in the risk of peripheral circulatory disorders — with ergot alkaloids.

When Metocardia is co-administered with hypoglycemic agents for oral use, their effect may decrease; with insulin — it may increase the risk of hypoglycemia, increase its severity and lengthening, and mask some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

When Metocardia is 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 a decrease in heart rate and suppression of atrioventricular conduction — when using metoprolol with verapamil, diltiazem, antiarrhythmic agents (amiodarone), reserpine, alpha-methyldopa, clonidine, guanfacine, general anaesthetics, and cardiac glycosides.

If metoprolol and clonidine are taken simultaneously, then when metoprolol is discontinued, 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 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 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 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. Tri-and tetracyclic antidepressants, antipsychotic drugs( neuroleptics), sedative and hypnotic drugs increase CNS depression.

How to take, course of use and dosage

Metocard is taken orally, without chewing, with a small amount of liquid.

Arterial hypertension-50 mg 2 times a day; if necessary, after a week the dose is increased to 200 mg / day (2 tablets of 100 mg). In the absence of a positive therapeutic result, the drug may be used in combination with other antihypertensive or diuretic agents.

Angina pectoris — 50-100 mg 2-3 times a day, if necessary, it is possible to increase the dose to 400 mg / day.

In case of cardiac arrhythmias – 50 mg 2-3 times a day.

Caution should be exercised when treating elderly patients (no dose adjustment is generally required).

The maximum dose is 400 mg / day.

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular ecstasystole, 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 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, with an interval of 2-5 minutes, beta-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-2-adrenergic stimulants should be administered. Metoprolol is poorly excreted by hemodialysis.

Special instructions

Monitoring of patients taking beta-blockers includes regular monitoring of their heart rate (HR) and blood pressure, as well as blood glucose levels in patients with diabetes mellitus. 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.

In case of stress angina, the selected dose of the drug should provide a heart rate at rest in the range of 55-60 beats / min, with a load-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 hyperthyroidism (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 it is necessary to prescribe to patients with bronchial asthma, beta-2-adrenostimulants are used as concomitant therapy; with pheochromocytoma, alpha — adrenoblockers are used.

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.

In elderly patients, regular monitoring of liver function is recommended. Correction of the dosage regimen is required only if an elderly patient develops 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. Monitoring of renal function is recommended for patients with severe renal insufficiency. 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.

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

Impact on the ability to drive vehicles and complex equipment

At the beginning of treatment with metoprolol, patients may experience dizziness and fatigue. In this case, they should refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions. In the future, the dose safety is determined individually.

Form of production

Tablets

Storage conditions

In a dark place, 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

Migraine, Angina, Arrhythmia, Hypertension