Metocard, tablets 50 mg, 30 pcs.

Methocard – antiarrhythmic, hypotensive, antianginal.

Selectively blocks beta₁-adrenoreceptors, inhibits the action of endogenous catecholamines, inhibits the activity of the renin-angiotensin system.

Decreases minute volume and heart function. Inhibits central sympathetic impulses. It has no membrane stabilizing effect and has no intrinsic sympathomimetic activity.

Pharmacokinetics

It is rapidly and almost completely absorbed from the gastrointestinal tract. C_max and T_max with Metocard 100 mg or Metocard retard administration 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%. Metabolized in the liver, T_1/2 – 3.5 h. It is excreted mainly by the kidneys (95%). Passes through the placenta.

Indications

Migraine, Angina, Hypertension (high blood pressure), Tinnitus, Arrhythmia, Swelling, Headache, Tachycardia, Cardialgia (heart pain)

Arterial hypertension, IBS, heart failure

Active ingredient

Metoprolol

Composition

1 tablet contains:

metoprolol tartrate 50 mg.

Auxiliary substances:

lactose,

povidone,

talc,

Magnesium stearate,

Microcrystalline cellulose,

Rice starch.

How to take, the dosage

The drug is taken orally at the same time as a meal or immediately after a meal. The tablets may be divided in half, but not chewed, and washed down with liquids.

The dose is determined individually depending on tolerance and therapeutic effectiveness. The maximum dose is 400 mg/day.

In case of arterial hypertension, the initial dose is 50-100 mg/day in 1-2 doses. If necessary, the daily dose is gradually increased to 100-200 mg. In the absence of a satisfactory therapeutic effect, Metocard may be prescribed in combination with other antihypertensive agents. The maximum daily dose is 200 mg.

In angina pectoris, arrhythmia, prevention of migraine attacks, 100-200 mg/day in 2 doses (morning and evening).

In secondary prevention of myocardial infarction, a dose of 200 mg/day in 2 doses (morning and evening) is prescribed.

In functional disorders of cardiac activity accompanied with tachycardia the drug is prescribed in a dose of 100 mg/day in 2 doses (morning and evening).

In elderly patients with impaired renal function and when hemodialysis is necessary, there is no need to adjust the dose of the drug.

In patients with impaired hepatic function, the dose of the drug should be reduced depending on the clinical condition.

Interaction

The concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. A break of at least 14 days should be taken between MAO inhibitors and metoprolol.

Concomitant intravenous administration of verapamil may provoke cardiac arrest. Simultaneous administration of nifedipine leads to a significant decrease in BP.

The concomitant use of Metocardium with agents for inhaled general anesthesia (hydrocarbon derivatives) increases the risk of myocardial depression and arterial hypotension; Beta-adrenergic stimulants, theophylline, cocaine, estrogens (sodium retention), indomethacin and other NSAIDs (sodium retention and blocking of prostaglandin synthesis by the kidneys) weaken the hypotensive effect.

There is marked an increase of CNS depressant action when concomitant use with ethanol; summation of the cardiodepressant effect – with agents for general anesthesia; increase of risk of peripheral circulation disorders – with ergot alkaloids.

When co-administered with oral hypoglycemic agents, it is possible to decrease their effect; with insulin – increasing the risk of hypoglycemia, increasing its intensity and duration, masking of some symptoms of hypoglycemia (tachycardia, sweating, increased BP).

When combined with antihypertensive agents, diuretics, nitroglycerin or slow calcium channel blockers, a sharp decrease in BP may develop (special caution is required when combined with prazosin).

When using Metocard with verapamil, diltiazem, antiarrhythmic agents (amiodarone), reserpine, alpha-methyldopa, clonidine, guanfacine, agents for general anesthesia and cardiac glycosides, an increase in HR depression and inhibition of AV conduction is observed.

If metoprolol and clonidine are taken concomitantly, then clonidine must be withdrawn after several days if metoprolol is withdrawn (due to the risk of withdrawal).

Hepatic microsomal enzyme inducers (rifampicin, barbiturates) lead to increased metabolism of metoprolol and decreased plasma concentrations of metoprolol and reduced effect. Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) – increase the plasma concentration of metoprolol.

Allergens used for immunotherapy or allergen extracts for skin tests when combined with metoprololol increase the risk of systemic allergic reactions or anaphylaxis; iodine containing x-ray contrast agents for IV administration increase the risk of anaphylactic reactions.

Methoprolol concomitant use decreases clearance of xanthine (except diphylline), especially with initially increased clearance of theophylline due to smoking; decreases lidocaine clearance, increases plasma lidocaine concentrations.

Methocard, when used concomitantly, increases and prolongs the effect of antidepolarizing muscle relaxants, prolongs the anticoagulant effect of coumarins.

In co-administration of Metocard with ethanol the risk of a pronounced decrease in BP increases.

The tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), sedatives and hypnotics when combined with metoprolol increase CNS depression.

Special Instructions

Control of patients taking Metocard includes regular monitoring of HR and BP, blood glucose content in diabetic patients. If necessary, the dose of insulin or oral hypoglycemic drugs for diabetic patients should be adjusted individually.

The patient should be instructed on how to calculate heart rate and instructed to consult a physician if the heart rate is less than 50 bpm. Dose above 200 mg/day decreases cardiac selectivity.

In heart failure, treatment with metoprolol is not started until the compensation stage is reached.

The severity of hypersensitivity reactions may increase (against a background of a history of severe allergic reactions) and the lack of effect of the usual doses of epinephrine (adrenaline).

The symptoms of peripheral arterial circulation disorders may worsen with the use of Metocard.

Stop the drug gradually, reducing the dose over 10 days.

When the drug is stopped abruptly, withdrawal syndrome (increased angina pectoris, increased BP) may occur. Special attention should be paid to patients with angina pectoris when withdrawing the drug.

In angina patients with tension angina, the selected dose of the drug should provide an HR at rest within 55-60 beats/min, and not more than 110 beats/min on exertion.

Patients who wear contact lenses should be aware that treatment with beta-adrenoblockers may decrease lacrimal fluid production.

Methoprolol may mask some clinical manifestations of hyperthyroidism (e.g., tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it may exacerbate the symptoms.

In diabetic patients, Methocard may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenoblockers, it does not practically increase insulin-induced hypoglycemia and does not delay the recovery of blood glucose concentration to normal levels.

If patients with bronchial asthma need to be prescribed as a concomitant therapy, stimulators of ? 2 -adrenoreceptors; in pheochromocytoma, alpha-adrenoblockers.

If it is necessary to perform surgical intervention, the anesthesiologist must be warned about the therapy (choice of general anesthetic agent with minimal negative inotropic effect), cancellation of the drug is not recommended.

Catecholamine-lowering agents (e.g., reserpine) can potentiate the effects of beta-adrenoblockers, so patients taking these combinations of agents should be under constant medical monitoring for excessive BP reduction and bradycardia.

In elderly patients, regular monitoring of liver function is recommended. The dosing regimen should be adjusted only in elderly patients with increasing bradycardia (less than 50 bpm), marked BP decrease (systolic BP below 100 mmHg), AV blockade, bronchospasm, ventricular arrhythmias, severe hepatic impairment, sometimes therapy must be discontinued.

Patients with severe renal impairment should have their renal function monitored.

Patients with depressive disorders taking metoprolol should be monitored particularly; if depression develops as a result of taking beta-adrenoblockers, discontinuing therapy is recommended.

The drug should be used with caution in severe hepatic dysfunction.

The drug should be used with caution in severe renal dysfunction.

The safety and effectiveness of the drug in children and adolescents under 18 years of age has not been established.

In the beginning of treatment with metoprolol, patients may experience dizziness and fatigue. In this case they should refrain from driving motor transport and engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions. In the future, this question should be decided after assessing the patient’s individual response to the therapy.

Contraindications

• pulse less than 50 beats per min
• severe heart failure
• bronchial asthmasevere hepatic and/or renal dysfunction
• high sensitivity to Methocard.

.

Side effects

Nervous system and sensory organs: headache, dizziness, nightmares, insomnia, depression, short-term amnesia, disorientation, paresthesia; visual disturbances, dry eyes, tinnitus.

Cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia, palpitations, hypotension, AV conduction disorders, circulatory failure, thrombocytopenia, agranulocytosis.

Respiratory system: bronchospasm, choking.

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

Allergic reactions: itching, rash, psoriatic skin changes.

Others: Peyronie’s disease, myalgia, alopecia.

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked BP decrease, arrhythmia, ventricular extasystole, bronchospasm, syncope, in acute overdose – cardiogenic shock, loss of consciousness, coma, AV-blockade (up to development of complete transverse block and cardiac arrest), cardialgia. The first signs of overdose occur 20 minutes to 2 hours after taking the drug.
Treatment: gastric lavage, prescription of adsorptive agents, symptomatic therapy: if BP is significantly decreased, the patient should be in Trendelenburg position; in case of excessive pressure drop, bradycardia and heart failure – intravenous injection (at 2-5 min intervals) of beta-adrenergic stimulators – until the desired effect is achieved, or intravenous injection of 0.5-2 mg of atropine sulfate. If there is no positive effect, administer dopamine, dobutamine or norepinephrine (norepinephrine). As a follow-up, it is possible to prescribe 1-10 mg of glucagon, placement of transvenous intracardiac pacing. In case of bronchospasm, intravenous a2 -adrenoreceptor stimulators should be administered.

Metoprolol is poorly excreted by hemodialysis.

Similarities

Metoprolol, Betaloc Zoc, Egilok, Metoprolol-Teva