Metoprolol, tablets 100 mg 30 pcs

A cardioselective beta1-adrenoblocker without intrinsic sympathomimetic activity. It has hypotensive, antianginal and antiarrhythmic effects. It reduces automatism of the sinus node, decreases heart rate, slows AV conduction, reduces myocardial contractility and excitability, decreases cardiac output, and decreases myocardial oxygen demand.

Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.

Causes a hypotensive effect, which stabilizes by the end of the 2nd week of course use. In tension angina metoprolol reduces the frequency and severity of attacks. It normalizes the heart rhythm in supraventricular tachycardia and atrial fibrillation.

In myocardial infarction helps to limit the zone of ischemia of the heart muscle and reduces the risk of fatal arrhythmias, reduces the possibility of recurrent myocardial infarction. When used in medium therapeutic doses, it has less pronounced effect on the smooth muscle of the bronchi and peripheral arteries than non-selective beta-adrenoblockers.

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Indications

Arterial hypertension (monotherapy or in combination with other antihypertensive agents), CHD, functional heart disorders accompanied by tachycardia, myocardial infarction, prevention of angina attacks, heart rhythm disorders, hyperthyroidism (complex therapy), prevention of migraine attacks.

Active ingredient

Composition

1 tablet contains:

The active ingredients:

metoprolol100 mg

Excipients:

Lactose monohydrate 180 mg,

Microcrystalline cellulose 72 mg,

Potato starch 12 mg,

sodium carboxymethyl starch 16 mg,

povidone 16 mg,

magnesium stearate 4 mg.

How to take, the dosage

When administered orally, the average dose is 50-100 mg/day in 1-2 doses. If necessary, the daily dose is gradually increased to 200 mg.

Maximum doses: When taken orally, the daily dose is 400 mg.

Interaction

In concomitant use with antihypertensive agents, diuretics, antiarrhythmic agents, nitrates, there is a risk of significant arterial hypotension, bradycardia, AV-blockade.

Concomitant use with barbiturates accelerates metabolism of metoprolol, which leads to a decrease in its effectiveness.

Concomitant use with hypoglycemic agents may increase the effect of hypoglycemic agents.

Concomitant use with NSAIDs may decrease the hypotensive effect of metoprolol.

Concomitant use with opioid analgesics mutually enhances the cardiodepressant effect.

Concomitant use with peripheral myorelaxants may increase neuromuscular blockade.

Concomitant use with agents for inhalation anesthesia increases the risk of inhibition of myocardial function and development of arterial hypotension.

Concomitant use with oral contraceptives, hydralazine, ranitidine, cimetidine increases the plasma concentration of metoprolol.

In concomitant use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation and asystole may occur.

Concomitant use with verapamil increases plasma Cmax and AUC of metoprolol. Cardiac minute and stroke volume, pulse rate, and arterial hypotension decrease. Heart failure, dyspnea and sinus node block may develop.

Intravenous administration of verapamil with metoprolol may cause cardiac arrest.

Concomitant use may increase bradycardia caused by foxglove glycosides.

Concomitant use with dextropropoxyphene increases the bioavailability of metoprolol.

Concomitant use with diazepam may decrease the clearance and increase the AUC of diazepam, which may increase its effects and decrease the rate of psychomotor reactions.

Concomitant use with diltiazem increases plasma concentrations of metoprolol due to inhibition of its metabolism by diltiazem. The effect on cardiac activity is additively inhibited due to delayed pulse conduction through the AV node caused by diltiazem. There is a risk of development of marked bradycardia, significant decrease of stroke and minute volume.

Concomitant use with lidocaine may impair lidocaine excretion.

Concomitant use with mibefradil in patients with low CYP2D6 isoenzyme activity may increase plasma concentrations of metoprolol and increase the risk of toxic effects.

Concomitant use with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form of eye drops or as part of anti-cough medicine) may slightly increase BP.

Concomitant use with propafenone increases plasma concentrations of metoprolol and develops toxic effects. Propafenone is thought to inhibit metabolism of metoprolol in the liver, decreasing its clearance and increasing serum concentrations.

Concomitant use with reserpine, guanfacine, methyldopa, clonidine may result in marked bradycardia.

Concomitant use with rifampicin decreases plasma concentrations of metoprolol.

Metoprolol may cause a slight decrease in theophylline clearance in smoking patients.

Fluoxetine inhibits CYP2D6 isoenzyme, this leads to inhibition of metabolism of metoprolol and its cumulation, which may increase the cardiodepressant effect and cause bradycardia. A case of lethargy has been described.

Fluoxetine and mainly its metabolites have a long T1/2, so the possibility of drug interaction persists even several days after withdrawal of fluoxetine.

There have been reports of decreased clearance of metoprolol from the body when used concomitantly with ciprofloxacin.

Concomitant use with ergotamine may increase peripheral circulatory disorders.

Concomitant use with estrogens decreases the antihypertensive effect of metoprolol.

Concomitant use of metoprolol increases the blood concentration of ethanol and prolongs its excretion.

Special Instructions

With caution, use in patients with chronic obstructive airway diseases, diabetes mellitus (especially with a labile course), Raynaud’s disease and peripheral artery obliterating diseases, pheochromocytoma (should be used in combination with alpha-adrenoblockers), marked renal and liver function disorders.

Treatment with metoprolol may decrease tear fluid production, which is important for patients who wear contact lenses.

Continuation of long-term treatment with metoprolol should be gradual (at least 10 days) under medical supervision.

The concomitant use of metoprolol with MAO inhibitors is not recommended.

In combined therapy with clonidine, the latter should be discontinued several days after withdrawal of metoprolol to avoid a hypertensive crisis. If used concomitantly with hypoglycemic agents, their dosing regimen should be corrected.

A few days before anesthesia, metoprolol should be discontinued or anesthesia agent with minimal negative inotropic effects should be selected.

Impact on driving and operating ability

In patients whose activities require increased attention, outpatient use of metoprolol should only be considered after evaluating the patient’s individual response.

Contraindications

Hypersensitivity, cardiogenic shock, grade II and III AV block, sinoatrial block, chronic (decompensation stage) heart failure, sinus node weakness syndrome, marked sinus bradycardia (heart rate less than 60 beats per minute)./min), Prinzmetal’s angina, acute myocardial infarction (heart rate less than 45 beats per minute, PQ interval greater than 0.24 sec, systolic BP less than 100 mm PT.st).

Pregnancy, lactation. Concomitant intravenous administration of “slow” calcium channel blockers such as verapamil. Age before 18 years. Pheochromocytoma. patients receiving long-term or intermittent therapy with inotropic agents acting on beta-adrenoceptors.

Side effects

Cardiovascular system disorders: bradycardia, arterial hypotension, AV conduction disorders, occurrence of symptoms of heart failure are possible.

Digestive system disorders: at the beginning of therapy dry mouth, nausea, vomiting, diarrhea, constipation; liver function disorders in single cases.

CNS and peripheral nervous system disorders: weakness, fatigue, dizziness, headache, muscle cramps, cold sensation and paresthesia in extremities may occur; decreased tear fluid secretion, conjunctivitis, rhinitis, depression, sleep disorders, nightmares may occur.

Hematopoietic system: in some cases – thrombocytopenia.

Endocrine system disorders: hypoglycemic states in patients with diabetes.

Respiratory system: in predisposed patients there may be symptoms of bronchial obstruction.

Allergic reactions: skin rash, itching.

Overdose

Symptoms: pronounced sinus bradycardia, dizziness, AV-blockade (up to development of complete transverse blockade and cardiac arrest), marked BP decrease, fainting, arrhythmia/ventricular extrasystole, acute heart failure; cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma, nausea, vomiting, cyanosis, hypoglycemia, seizures. The first signs of overdose occur 20 minutes to 2 hours after taking the drug.

Treatment: gastric lavage and administration of adsorptive drugs, symptomatic therapy: if BP significantly decreased – the patient should be in Trendelenburg position; in case of excessive BP decrease, bradycardia and heart failure – intravenous infusion of beta-adrenostimulants with 2-5 min intervals – until the desired effect is achieved, or intravenous injection of 0.5-2 mg of atropine sulfate. If there is no positive effect – dopamine, dobutamine or norepinephrine. A transvenous intracardiac pacemaker may be used as a follow-up. In bronchospasm, IV beta-adrenomimetics should be administered. Slow IV diazepam should be administered in case of seizures. Hemodialysis is ineffective.

Similarities