Metoprolol succinate. Tablets release, with (25 mg, 50 mg, 100 mg).
Selective beta-blocker without internal sympathomimetic activity. Due to the peculiarities of the dosage form, a constant concentration of metoprolol in the blood plasma is maintained, and a stable clinical effect is achieved within 24 hours. The preparation is characterized by better beta-selectivity in comparison with traditional metoprolol.
Reduces the risk of side effects (bradycardia, weakness). To a lesser extent affects the smooth muscles of the bronchi, the allocation of insulin, carbohydrate metabolism and the activity of the CCC.
The use of arterial hypertension leads to a decrease in blood pressure of more than 24 hours. At the beginning of treatment, there is an increase in OPSS, with prolonged use of OPSS decreases.
Bioavailability is 30-40%. The release rate depends on the acidity of the medium. The connection with proteins is 5-10%. T 1/2 – 3.5 hours Biotransformation – in the liver by oxidation. It is excreted in the urine in the form of metabolites, unchanged in about 5%.
Arterial hypertension, angina, heart rhythm disturbances (supraventricular tachycardia, extrasystole), secondary prophylaxis after MI, CHF (as an auxiliary therapy), prevention of migraine attacks.
When choosing therapy, bradycardia should be avoided. The drug is taken after a meal. Tablets should be swallowed with a liquid. Tablets can be divided in half, but you can not chew or crumble. With arterial hypertension, the initial dose of 50-100 mg 1p / day. With angina, the daily dose is 50-100 mg 1 p / day.
With the maintenance treatment of MI, the drug is prescribed at 200 mg 1 p / day. The minimum duration of treatment 3 months. With supraventricular tachycardia and extrasystole, the drug is prescribed for 100-100 mg 1 p / day.
With CHF, the dose is selected individually, the initial dose of the first 2 weeks is 12.5 mg 1 p / day, then the dose increases to 25 mg 1 p / day, after 2 weeks – up to 50 mg 1 p / day, with good tolerability dose may be increased up to 200 mg 1 p / day. For prevention of migraine attacks, the drug is used in a daily dose of 100-200 mg 1 p / day.
At the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, a feeling of cold and paresthesia in the limbs are possible.
There may also be bradycardia, hypotension, disturbances in AV conduction, the appearance of symptoms of HF, a decrease in the secretion of tear fluid, conjunctivitis, rhinitis, depression, sleep disturbances, nightmares, dry mouth, hypoglycemic conditions in patients with diabetes, vomiting, diarrhea, constipation. Patients who are predisposed may develop symptoms of bronchial obstruction. Individual cases of violations of liver function, thrombocytopenia were noted.
– AV blockade of II and III degrees,
– sinus-atrial blockade,
– arterial hypotension,
– chronic heart failure in decompensation stage,
– cardiogenic shock,
– suspicion of acute myocardial infarction at heart rate less than 45 beats / min,
– violation peripheral circulation,
– intravenous administration of calcium channel blockers (with simultaneous iv administration of verapamil should be borne in mind the threat of cardiac arrest),
– age to 18 years,
– hypersensitivity to metoprolol.
Arterial hypotension, AV blockade, bradycardia up to the cardiac arrest, CH, cardiogenic shock, respiratory failure, bronchospasm, vomiting, impaired consciousness, seizures of generalized convulsions, nausea, vomiting, hypoglycemia.
Gastric lavage, atropine 0.5-2 mg IV, rapidly, sympathomimetics – dopamine, dobutamine, epinephrine. Resuscitative measures.
Interaction with other drugs
Antiarrhythmic agents of the first class are the sum of the negative inotropic action. The content of metoprolol in the blood plasma increases with simultaneous administration of antacids, diphenhydramine, hydralazines, oral contraceptives, ranitidine and, apparently, cimetidine. Taking rifampicin reduces the concentration of metoprolol in the blood plasma.