Metoprolol is a cardioselective beta 1 -blocker with hypotensive, antiarrhythmic and antianginal effects.
Release form and composition
Metoprolol dosage form - tablets: round, convex on both sides, with a risk on one of the sides, film coated:
- Pink - 14 pcs. in blisters, 2 or 4 blisters in a carton box
- White (possible yellowish tint) - 10 pcs. in blisters, 3 blisters in a carton box.
The active ingredient is metoprolol tartrate. Its content in 1 tablet depending on color:
- Pink - 50 mg;
- White - 100 mg.
Excipients: microcrystalline cellulose, magnesium stearate, anhydrous colloidal silicon dioxide, sodium carboxymethyl starch (type A).
- Tablets 50 mg: talc, polysorbate 80, titanium dioxide (E171), hypromellose, a crimson dye (Ponso 4R);
- Tablets 100 mg: talc, polysorbate 80, titanium dioxide (E171), hypromellose.
Indications for use
Metoprolol is used for the following indications:
- Cardiac arrhythmias (ventricular premature beats and supraventricular tachycardia);
- Arterial hypertension (including in combination with other antihypertensive drugs), including hyperkinetic type, tachycardia;
- Ischemic heart disease: treatment of myocardial infarction (complex therapy and secondary prevention), as well as the prevention of strokes;
- Hyperthyroidism (as part of complex therapy).
Also, the drug can be used to prevent migraine attacks.
- Age up to 18 years;
- The simultaneous use of monoamine oxidase inhibitors or intravenous verapamil;
- Hypotension (systolic blood pressure - less than 100 mm Hg, heart rate - less than 45 beats / min; in the case of Metoprolol in the secondary prevention of myocardial infarction);
- Heart failure in the decompensation stage;
- Severe bradycardia;
- Printsmetal angina;
- Sinoatrial (SA) blockade;
- AV block II-III degree;
- Sick sinus syndrome;
- Cardiogenic shock;
- Hypersensitivity to the components of the drug or other beta-blockers.
Relative (requires special care due to the risk of complications):
- Elderly age;
- Chronic liver / kidney failure;
- Obliterating diseases of peripheral vessels (Raynaud's syndrome or intermittent claudication);
- Myasthenia gravis;
- AV block I degree;
- Metabolic acidosis;
- Depression (including in the anamnesis);
- Chronic obstructive bronchitis and emphysema;
- Bronchial asthma.
Dosing and Administration
Metoprolol should be taken orally, without chewing the tablets and washing them down with liquid, during a meal or immediately after a meal.
The initial daily dose for hypertension is 50-100 mg in 1 or 2 doses (in the morning and in the evening). In case of insufficiency of the therapeutic effect, the dose is gradually increased and / or prescribed in addition to other antihypertensive agents. The maximum permissible daily dose is 200 mg.
- Functional disorders of cardiac activity, accompanied by tachycardia - 50 mg 2 times a day;
- Arrhythmias, angina pectoris, and migraine prophylaxis - 50-100 mg 2 times a day;
- Secondary prevention of myocardial infarction - 100 mg 2 times a day.
In patients with impaired liver function, the dose is reduced depending on the clinical condition.
- Nervous system: headache, weakness, slowing down of the speed of mental and motor reactions, increased fatigue; rarely, decreased attention, anxiety, muscle weakness, insomnia, drowsiness, nightmares, depression, paresthesias in the limbs (in patients with intermittent claudication and Raynaud's syndrome), transient impairment of memory or confusion;
- Sense organs: rarely - dryness and soreness of the eyes, reduced secretion of the tear fluid, conjunctivitis, reduced vision, tinnitus;
- Cardiovascular system: dizziness, lowering blood pressure, palpitations, orthostatic hypotension, sinus bradycardia, and sometimes - loss of consciousness; rarely - manifestation of angiospasm (cooling of the lower extremities, increased disturbance of peripheral circulation, Raynaud’s syndrome), temporary worsening of symptoms of chronic heart failure (edema, shortness of breath, swelling of the feet and / or lower legs), impaired conduction and reduction of myocardial contractility, cardialgia, arrhythmias;
- Digestive system: abdominal pain, nausea, dry mouth, constipation, vomiting, diarrhea, change in taste, abnormal liver function;
- Respiratory system: nasal congestion, shortness of breath, difficulty breathing out; when using the drug in high doses - bronchospasm;
- Endocrine system: hypoglycemia (in patients receiving insulin); rarely - hypothyroidism, hyperglycemia (in patients with diabetes mellitus);
- Skin: exacerbation of psoriasis, rash, psoriasis-like skin reactions, pruritus, skin flushing, sweating, exanthema, photodermatosis, urticaria, reversible alopecia;
- Laboratory indicators: rarely - increased activity of liver enzymes, agranulocytosis, thrombocytopenia (unusual bleeding and hemorrhage), leukopenia; very rarely, hyperbilirubinemia;
- Other: a slight increase in body weight, pain in the back or joints, decreased libido and / or potency; when taken during pregnancy - intrauterine growth retardation, bradycardia and hypoglycemia in the fetus.
The severity of side effects depends on the individual sensitivity of the patient. Usually they are insignificant and independently pass after drug withdrawal.
In the period of use of metoprolol, control of blood pressure (BP) and heart rate (HR) is necessary. In patients with severe renal insufficiency, in addition, renal function should be monitored, in patients with diabetes mellitus - glucose content (it may be necessary to adjust the dose of insulin or oral hypoglycemic agent).
Patients should be trained in the method of counting the heart rate and warned that in case of decrease in this indicator less than 50 beats / minute, you should consult a doctor.
In heart failure, metoprolol can be administered only after reaching the stage of compensation.
It is recommended to cancel the drug gradually, reducing the dose within 10 days, because abrupt withdrawal can lead to increased blood pressure and increased angina attacks. Particular attention when stopping treatment should be given to patients with angina and thyrotoxicosis.
In the period of use of Metoprolol in patients with a burdened allergic history, it is possible to increase the severity of hypersensitivity reactions. It is also important to keep in mind that the drug can reverse the effect of the usual doses of epinephrine (adrenaline).
Metoprolol can mask the tachycardia caused by hypoglycemia in patients with diabetes mellitus, increase the symptoms of the pathology of the peripheral arterial blood circulation, reduce the production of tear fluid (which should be taken into account for patients using contact lenses).
If it is necessary to administer the drug to patients with pheochromocytoma, alpha-blockers are used as concomitant therapy, and beta2-adrenostimulants are used with bronchial asthma.
Patients taking Metoprolol concurrently with drugs that reduce the supply of catecholamines (for example, with reserpine) should be under the careful supervision of a physician, since may increase the action of beta-blockers, excessive reduction of blood pressure and the development of bradycardia. In elderly patients, it is recommended to constantly monitor liver function. Reducing the dose for the elderly is shown in the case of a pronounced decrease in blood pressure (systolic blood pressure - below 100 mmHg), increasing bradycardia (less than 50 beats / minute), ventricular arrhythmias, AV blockade, bronchospasm, and severe liver function disorders. In some cases, it requires the abolition of metoprolol.
Patients who are to undergo surgical intervention should warn the anesthesiologist about the therapy being carried out so that he selects the agent for general anesthesia with minimal negative inotropic effect. Abolishing metoprolol is not recommended.
Special monitoring during treatment should be carried out for patients with depressive disorders. If depression develops, the drug should be withdrawn.
In pregnancy, metoprolol is prescribed only according to strict indications, after assessing the ratio of benefits and risks. The treatment is carried out under close medical supervision, especially for the development of the fetus. In addition, strict observation of the newborn within 48-72 hours after birth is necessary.
At the beginning of therapy, possible increased fatigue and dizziness. In this case, it is recommended to refrain from driving and performing work that requires high concentration of attention, speed of mental and physical reactions. The degree of further restriction is determined individually.
Monoamine oxidase inhibitors significantly enhance the hypotensive effect of beta-blockers, so this combination is contraindicated. The break between taking these drugs should be at least 14 days.
Possible interaction reactions in the case of simultaneous use of Metoprolol with other drugs:
- Verapamil intravenously: cardiac arrest;
- Nifedipine: a significant reduction in blood pressure;
- Anesthetic agents: the summation of the cardiodepressive effect;
- Means for inhalation anesthesia, which are derivatives of hydrocarbons: the risk of arterial hypotension and inhibition of myocardial function;
- Etrogens, theophylline, beta-adrenostimulyatory, cocaine, indomethacin and other nonsteroidal anti-inflammatory drugs: the weakening of the hypotensive effect;
- Tri- and tetracyclic antidepressants, sedatives, hypnotics and antipsychotics, ethanol: increased inhibitory effects on the central nervous system;
- Antidepolarizing muscle relaxants: strengthening and lengthening of their action;
- Ergot alkaloids: increased risk of peripheral circulatory disorders;
- Oral hypoglycemic agents: reduction of their effect;
- Insulin: the risk of hypoglycemia, increasing its severity and masking some of its symptoms (sweating, tachycardia, increased blood pressure);
- Inductors of liver microsomal enzymes (barbiturates, rifampicin): increased metabolism and concentration of metoprolol in the blood plasma, reducing its effectiveness;
- Inhibitors (oral contraceptives, cimetidine, phenothiazines): an increase in plasma metoprolol concentration;
- Xanthines (with the exception of difillin), lidocaine: a decrease in their clearance;
- Lidocaine: increasing its concentration in the blood plasma;
- Coumarins: prolongation of their anticoagulant effect;
- Ethanol: the risk of a pronounced decrease in blood pressure;
- Iodine-containing radiopaque substances for intravenous administration: the risk of anaphylactic reactions;
- Allergen extracts for skin tests and allergens used for immunotherapy: the risk of systemic allergic reactions or anaphylaxis;
- Diuretics, antihypertensive drugs (especially prazosin), nitroglycerin, calcium channel blockers: a sharp decrease in blood pressure;
- Diltiazem, verapamil, reserpine, clonidine, guanfacine, alpha methyldopa, antiarrhythmic drugs (amiodarone), cardiac glycosides, agents for general anesthesia: inhibition of AV conduction, increase in the severity of HR reduction;
- Clonidine: the risk of withdrawal after abrupt cessation of metoprolol intake (for this reason, clonidine should be canceled a few days after discontinuation of metoprolol).
Terms and conditions of storage
Store at a temperature of 15-25 ° C in a place protected from light and moisture, inaccessible to children.
Shelf life - 5 years.