Index of drugs

Hypertension. Angina pectoris. Arrhythmias, especially supraventricular tachycardia. Prevention of mortality from cardiac causes and reinfarction after an acute phase of myocardial infarction. Palpitations caused by functional heart problems. Prophylaxis of migraine. Stable symptomatic heart failure (NYHA class II-IV, left ventricle ejection fraction <40%), in combination with other treatments.

1 tabl sustained release contains 23.75 mg, 47.5 mg, 95 mg or 190 mg Metoprolol succinate (corresponding to 25 mg, 50 mg, 100 mg or 200 mg metoprolol tartrate).

Selective drug β₁-adrenolityczny. It has only a slight stabilizing effect on cell membranes and has no agonistic properties. Metoprolol reduces or inhibits the stimulatory effect of catecholamines on the heart. It reduces the tachycardia induced catecholamine burst, increased minute capacity and cardiac contractility and lowers blood pressure. The blood levels and efficacy of metoprolol succinate prolonged-release tablets are more evened out over 24 hours than with traditional tablets. If necessary, patients with symptoms of obstructive pulmonary disease may be given metoprolol in combination with β-drugs₂-adrenomimetycznymi. In a clinical trial in patients with NYHA class II-IV heart failure and ejection fraction ≤ 40% who received metoprolol in combination with standard heart failure therapy, a reduction in overall mortality was demonstrated by 34%. After oral administration, the drug is completely absorbed. Due to the significant first-pass effect of the liver, the bioavailability of a single oral dose is approximately 50%. The bioavailability of prolonged-release tablets is about 20-30% lower than traditional tablets, but this has no significant clinical significance. The drug binds to plasma proteins in 5-10%. Each prolonged release metoprolol succinate tablet contains controlled release pellets coated with a polymer coating that regulates the release rate of metoprolol. The release of metoprolol takes place continuously for 20 h. Metoprolol is metabolised by oxidation in the liver (mainly by the CYP2D6 enzyme). Over 95% of the dose is excreted in the urine; about 5% of the dose is excreted unchanged. T_0,5 metoprolol is on average 3.5 h (range 1-9 h). The total clearance is about 1 l / min.

Hypersensitivity to metoprolol succinate, other β-blockers or other components of the preparation. Atrio-ventricular block IIst. or III. untreated heart failure (pulmonary edema, disturbed blood flow or hypotension) and permanent or periodic use of drugs that increase myocardial contractility (β-adrenergic agonists). Symptomatic and / or clinically significant sinus bradycardia (cardiac function <50 / min). Sick node syndrome. Cardiogenic shock. Severe disturbances of peripheral arterial circulation. Hypotension (systolic blood pressure <90 mm Hg). Metabolic acidosis. Severe bronchial asthma or chronic obstructive pulmonary disease. Untreated phaeochromocytoma (pheochromocytoma). Concomitant use of MAO inhibitors (other than MAO-B inhibitors). Metoprolol must not be given to patients suspected of acute myocardial infarction and heart rate <45 bpm / min, PQ interval> 0.24 s or systolic blood pressure <100 mm Hg. In addition, metoprolol must not be used in patients with heart failure and recurrent systolic blood pressure <100 mm Hg (a pre-treatment check-up is advisable). It is contraindicated (with the exception of the intensive care unit) simultaneous intravenous administration of Calcium antagonists such as Verapamil or diltiazem or other anti-arrhythmic drugs (such as disopyramide).

Β-blockers should be used with caution in patients with bronchial asthma (when co-administered with β-drugs₂-adrenomimetic in the form of tablets or inhalation, before the start of metoprolol treatment, the dose of β₂-adrenaline and increase it if necessary). Carefully used in patients with diabetes mellitus, atrioventricular conduction disorders, peripheral vascular disease, hyperthyroidism, allergy (adrenaline does not always give the desired therapeutic effect), psoriasis and Prinzmetal angina. When metoprolol is used in patients with pheochromocytoma, an alpha-blocker should be used before and continued with metoprolol. Before the surgery, the anesthetist should be informed that the patient is using β-blockers; their discontinuation for surgery is not recommended. To date, insufficient therapeutic experience with metoprolol has not been obtained in patients with heart failure associated with: unstable heart failure (NYHA class IV), acute myocardial infarction or unstable angina over the past 28 days, renal dysfunction, liver dysfunction, age > 80 years or <40 years with essential valve disease, hypertrophic obstructive cardiomyopathy, during or after cardiac surgery within 4 months before starting treatment. There is limited experience with the use of the preparation in children and adolescents.

Pregnant should only be used if the benefit for the mother outweighs the risk to the embryo or fetus. Β-blockers can reduce placental perfusion and cause fetal death and premature birth. Fetal intrauterine growth retardation has been observed after long-term use of metoprolol in pregnant women with mild or moderate hypertension. β-blockers may prolong labor and cause bradycardia in the fetus and newborn. There have been reports of hypoglycaemia, hypotension, increased bilirubinemia and a difficult response to tissue hypoxia in the newborn. The use of metoprolol should be discontinued 48-72 h before the planned parturition. If this is not possible - the newborn should be observed for 48-72 h after birth for symptoms and signs of blocking β-adrenergic receptors (eg cardiac and pulmonary complications). The concentration of metoprolol in milk is about three times higher than in plasma. Although at the therapeutic doses, the risk of harm to the child is small (except for people with slow metabolism), the child should be observed for signs of blocking β-adrenergic receptors.

Side effects are usually mild and transient. Very often: fatigue. Common: pain and dizziness, balance disorders (very rarely combined with fainting), bradycardia, palpitations, marked decrease in blood pressure and orthostatic hypotension (very rarely with fainting), exercise dyspnoea, nausea, abdominal pain, diarrhea, constipation. Uncommon: weight gain, depression, impaired concentration, drowsiness or sleeplessness, nightmarish dreams, paresthesia, transient worsening of heart failure, Ist vestibular block, precordial pain, cold hands and feet, bronchospasm, vomiting, rash (psoriasis-like rash and dystrophic skin changes), increased sweating, muscle cramps, edema. Rare: exacerbation of latent diabetes, nervousness, anxiety, visual disturbances, dryness or eye irritation, conjunctivitis, functional symptoms of heart problems, arrhythmias, conductive heart disorders, rhinitis, dry mouth, abnormal liver function tests, loss of hair, impotence and other sexual dysfunctions, plastic penile sclerosis (Peyrone's disease). Very rare or not known: thrombocytopenia, leukopenia, impairment or weakness of memory, confusion, hallucinations, personality changes (eg mood changes), tinnitus, impaired hearing, necrosis in patients with severe peripheral vascular disease prior to treatment, worsening of intermittent claudication or Raynaud's syndrome, taste disorders, hepatitis, hypersensitivity reactions to light, exacerbation of psoriasis, onset of psoriasis, psoriatic skin lesions.

Orally.Hypertension: in patients with mild or moderate hypertension - 47.5 mg metoprolol succinate (equivalent to 50 mg metoprolol tartrate) once daily; if necessary, the dose can be increased to 95-190 mg metoprolol succinate (equivalent to 100-200 mg metoprolol tartrate) per day or to add another antihypertensive drug to the treatment regimen.Angina pectoris: 95-190 mg metoprolol succinate (equivalent to 100-200 mg metoprolol tartrate) once daily; if necessary, other medicines used to treat atherosclerosis may be added to the treatment regimen.Heart arythmia: 95-190 mg metoprolol succinate (equivalent to 100-200 mg metoprolol tartrate) once a day.Prophylactic treatment after myocardial infarction: 190 mg metoprolol succinate (equivalent to 200 mg metoprolol tartrate) once a day.Palpitations caused by functional heart problems: 95 mg metoprolol succinate (equivalent to 100 mg metoprolol tartrate) once daily; if necessary, the dose can be increased to 190 mg metoprolol succinate (equivalent to 200 mg metoprolol tartrate).Prophylaxis of migraine: 95-190 mg metoprolol succinate (equivalent to 100-200 mg metoprolol tartrate) once a day.Stable symptomatic heart failure: in patients with stable symptomatic heart failure treated with other drugs, the dose of metoprolol succinate is determined individually. The recommended starting dose for NYHA class III-IV heart failure patients is 11.88 mg metoprolol succinate (equivalent to 12.5 mg metoprolol tartrate) once daily in the first week of treatment. The dose can be increased to 23.75 mg metoprolol succinate (equivalent to 25 mg metoprolol tartrate) once a day on week 2. The recommended starting dose for patients with NYHA class II heart failure is 23.75 mg metoprolol succinate (equivalent to 25 mg metoprolol tartrate) once daily in the first 2 weeks of treatment. After this period, it is recommended to double the dose. The dose is increased every other week to 190 mg metoprolol succinate (equivalent to 200 mg metoprolol tartrate) once daily or up to the maximum tolerated dose of the patient. In long-term therapy, the target dose should be set at 190 mg metoprolol succinate (equivalent to 200 mg metoprolol tartrate) per day or at the maximum tolerated dose of the patient. It is recommended that the attending physician should have adequate knowledge about the treatment of stable symptomatic heart failure. The patient's condition should be carefully assessed after each dose increase. If you have a lower blood pressure, it may be necessary to reduce the dose of another medicine used at the same time. Lowering blood pressure does not have to be an obstacle to long-term use of Metoprolol, but the dose should be reduced until the patient's condition stabilizes. In patients with severe hepatic impairment, a dose reduction should be considered. There is no need to change the dosage in patients with impaired renal function. In elderly patients, the dose should be increased with extreme caution.
The tablets should be swallowed whole or divided, but they should not be chewed or crushed. The tablets should be taken with liquid (at least half a glass).