Description
Latin name
METOPROLOL
Release form
Pink film-coated tablets, round, biconvex, with a notch on one side.
Pharmacological action
Cardioselective beta1-blocker without internal sympathomimetic activity. It has a hypotensive, antianginal and antiarrhythmic effect. Reduces the automatism of the sinus node, reduces heart rate, slows down AV-conduction, reduces contractility and excitability of the myocardium, reduces cardiac output, reduces myocardial oxygen demand. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.
Causes a hypotensive effect that stabilizes by the end of the 2nd week of course use. With angina pectoris, metoprolol reduces the frequency and severity of seizures. Normalizes heart rate with supraventricular tachycardia and atrial fibrillation. With myocardial infarction, it helps to limit the area of ischemia of the heart muscle and reduces the risk of fatal arrhythmias, reduces the likelihood of recurrence of myocardial infarction. When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.
Indications
– arterial hypertension (as monotherapy or in combination with other antihypertensive agents), including hyperkinetic type, tachycardia
– coronary heart disease: myocardial infarction (secondary prevention-complex therapy), prevention of angina pectoris – angina pectoris heart (supraventricular tachycardia, ventricular extrasystole)
– hyperthyroidism (complex therapy)
– prevention of migraine attacks.
Contraindications
– cardiogenic shock
– AV block II ² III degree
– sinoatrial (SA) blockade
– severe sinus node syndrome
– severe bradycardia
– cardiac stenosis in cardiac arrhythmia, cardiac sarditis if used in the secondary prevention of myocardial infarction – systolic blood pressure less than 100 mm Hg, heart rate less than 45 beats / min)
– simultaneous administration of MAO inhibitors or simultaneous iv administration of verapamil
– lactation period
– age grows up to 18 years (efficiency and safety are not established)
– hypersensitivity to metoprolol or other components of the drug, other beta-blockers.
Precautions – diabetes mellitus, metabolic acidosis,
Use during pregnancy and lactation
During pregnancy, it is prescribed according to strict indications taking into account the benefit / risk ratio (due to the development of the fetus bradycardia, arterial hypotension, hypoglycemia). At the same time, careful monitoring is carried out, especially for the development of the fetus. It is necessary to strictly monitor newborns within 48-72 hours after delivery.
The effect of metoprolol on a newborn, while breastfeeding has not been studied, therefore, women taking metoprolol should stop breast-feeding.
Special instructions
Monitoring patients with beta-blockers includes regular monitoring of heart rate and blood pressure, blood glucose in patients with diabetes. If necessary for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed orally should be selected individually.
The patient should be trained in the method of calculating heart rate and instructed on the need for medical advice for heart rate less than 50 beats / min. When taking doses above 200 mg / day, cardioselectivity decreases.
In heart failure, treatment with metoprolol begins only after the compensation stage has been reached.
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 administration of usual doses of epinephrine (adrenaline).
May aggravate symptoms of peripheral arterial circulatory disorders. Drug withdrawal is carried out gradually, reducing the dose within 10 days.
With a sharp cessation of treatment, withdrawal syndrome (increased angina attacks, increased blood pressure) may occur.
Particular attention when discontinuing the drug must be given to patients with angina pectoris. With angina pectoris, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load of not more than 110 beats / min.
Patients using contact lenses should take into account that tear fluid production may be reduced during treatment with beta-blockers.
Metoprolol may mask some clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can enhance symptoms.
With diabetes, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced glycemia and does not delay the restoration of blood glucose concentrations to normal levels.
If necessary, the appointment of patients with bronchial asthma, beta2-adrenostimulants with pheochromocytoma – alpha-adrenergic blockers are used as concomitant therapy.
If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy (the choice of a means for general anesthesia with minimal negative inotropic effect), drug withdrawal is not recommended.
Drugs that reduce catecholamine stores (e.g., reserpine) can enhance the effects of beta-blockers, so patients taking these combinations of drugs, should be under the constant supervision of a doctor to detect an excessive decrease in blood pressure and bradycardia. In elderly patients, it is recommended to regularly monitor liver function. Correction of the dosing regimen is required only in the case of an elderly patient with increasing bradycardia (less than 50 beats / min), a marked decrease in blood pressure (systolic blood pressure below 100 mmHg), AV blockade, bronchospasm, ventricular arrhythmias, and severe disorders liver function, sometimes it is necessary to stop treatment.
Patients with severe renal impairment are advised to monitor renal function.
Special monitoring of the condition of patients with depressive disorders taking metoprolol should be carried out in the event of development of depression caused by beta-blockers, discontinuation of therapy is recommended.
Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Effect on the ability to drive vehicles and control mechanisms
At the beginning of treatment with metoprolol, patients may experience dizziness, 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 determination of dose safety is carried out individually.
Composition
1 tab. metoprolol tartrate 50 mg
Excipients: anhydrous colloidal silicon dioxide, microcrystalline cellulose, sodium carboxymethyl starch (type A), magnesium stearate.
Shell composition: hypromellose, polysorbate 80, talc, titanium dioxide (E171), crimson dye (Ponceau 4R).
Dosage and administration of
Tablets are taken orally with food or immediately after eating, without chewing and drinking with liquid.
Arterial hypertension
The initial daily dose is 50-100 mg in 1-2 doses (morning and evening). With insufficient therapeutic effect, the daily dose can be gradually increased to 100-200 mg and / or the additional appointment of other antihypertensive agents. The maximum daily dose of 200 mg.
Angina pectoris, arrhythmias, prevention of migraine attacks – 100-200 mg / day in 2 divided doses (morning and evening).
Secondary prevention of myocardial infarction – 200 mg / day, 2 doses (morning and evening).
Functional disturbances of cardiac activity, accompanied by tachycardia -100 mg / day in 2 divided doses (morning and evening).
In elderly patients, with impaired renal function, as well as with the need for hemodialysis, the dose is not changed.
In case of impaired liver function, the dose should be reduced depending on the clinical condition.
Side effects
Side effects depend on the individual sensitivity of the patient. Usually they are insignificant and disappear after discontinuation of the drug.
From the nervous system: fatigue, weakness, headache, slowing down the rate 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.
On the part of the sensory organs: rarely – decreased vision, decreased secretion of lacrimal fluid, dry and sore 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 worsening of symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath ), arrhythmias, manifestation of angiospasm (increased impairment of peripheral circulation, cooling of the lower extremities, Raynaud’s syndrome), impaired myocardial conduction, cardialgia.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, impaired liver function, taste change.
From the skin: urticaria, pruritus, rash, exacerbation of psoriasis, psoriasis-like skin reactions, hyperemia of the skin, exanthema, photodermatosis, increased sweating, reversible alopecia.
From the respiratory system: nasal congestion, difficulty breathing out (bronchospasm when prescribed 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 indicators: rarely – thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes is extremely rare – hyperbilirubinemia.
Influence on the fetus: intrauterine growth retardation, hypoglycemia, and bradycardia are possible.
Other: pain in the back or joints, like all beta-blockers, in rare cases can cause a slight increase in body weight, decreased libido and / or potency.
Drug Interactions
Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. A break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days.
The simultaneous iv administration of verapamil can cause cardiac arrest.
Concomitant administration of nifedipine leads to a significant decrease in blood pressure.
Inhalation anesthetics (derivatives of hydrocarbons) increase the risk of inhibition of myocardial function and the development of arterial hypotension.
Beta-adrenostimulants, theophylline, cocaine, etrogens (sodium retention), indomethacin and other NSAIDs (sodium retention and kidney blocking of prostaglandin synthesis) weaken the hypotensive effect.
Three and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), sedative and hypnotic drugs increase central nervous system depression.
There is an increase in the inhibitory effect on the central nervous system – with ethanol, the summation of the cardiodepressive effect – with anesthetics, an increased risk of peripheral circulation disorders – with ergot alkaloids.
When taken together with hypoglycemic agents for oral administration, it is possible to reduce their effect with insulin – increasing the risk of hypoglycemia, increasing its severity and lengthening, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
When combined with antihypertensive drugs, diuretics, a sharp decrease in blood pressure may develop with nitroglycerin or with slow calcium channel blockers) special care is needed when combined with prazosin) increased severity of heart rate reduction and inhibition of AV conductivity – with metoprolol with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, alpha-methyl dopa , clonidine, guanfacine, general anesthetics and cardiac glycosides.
If metoprolol and clonidine are taken at the same time, then when metoprolol is canceled, clonidine is canceled after a few days (due to the risk of withdrawal syndrome).
Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to increased metabolism of metoprolol, to a decrease in the concentration of metoprolol in blood plasma and a decrease in the effect.
Inhibitors (cimetidine, oral contraceptives, phenothiazines) increase the concentration of metoprolol in plasma.
Allergens used for immunotherapy or allergen extracts for skin tests when used together with metoprolol increase the risk of systemic allergic reactions or anaphylaxis iodine-containing radiopaque substances for iv administration increase the risk of anaphylactic reactions.
Reduces xanthine clearance (except for diphillin), especially with an initially increased clearance of theophylline under the influence of smoking.
Reduces the clearance of lidocaine, increases the concentration of lidocaine in blood plasma.
Strengthens and prolongs the action of antidepolarizing muscle relaxants, lengthens the anticoagulant effect of coumarins.
When combined with ethanol, the risk of a marked decrease in blood pressure increases.
Overdose
Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, pronounced decrease in blood pressure, arrhythmia, ventricular ecstasy, bronchospasm, fainting, with acute overdose – cardiogenic shock, loss of consciousness, coma, anthrioventricular blockade (up to the development of complete transverse blockade and cardiac arrest), cardialgia.
The first signs of an overdose appear 20 minutes – 2 hours after taking the drug.
Treatment: gastric lavage and the appointment of adsorbing agents symptomatic therapy: with a pronounced decrease in BP, the patient should be in Trendelenburg in case of excessive decrease in BP, bradycardia and heart failure – in / in, with an interval of 2-5 min, beta-adrenal. until the desired effect is achieved or in / in 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 administer 1-10 mg of glucagon, staging a transvenous intracardiac pacemaker. At bronchospasm it is necessary to enter in / in stimulators of beta2-adrenoreceptors. Metoprolol is poorly excreted by hemodialysis.
Storage Conditions
Keep out of reach of children, in a dry, dark place at 15 ° C to 25 ° C.
shelf life
5 years
Active ingredient
Metoprolol
Terms and conditions
prescription
Dosage form
tablets
Possible product names
Metoprolol tablets 50 mg 50 pcs.
