Index of drugs

Hypertension. Angina pectoris. Arrhythmias, especially supraventricular tachycardia. Prophylaxis of death from cardiac causes and re-myocardial infarction 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 methods of treatment of heart failure.

1 tabl sustained release contains 23.75 mg, 47.5 mg or 95 mg Metoprolol succinate, equivalent to 25 mg, 50 mg or 100 mg metoprolol tartrate.

Selective drug β₁-adrenolityczny. It has a slight stabilizing effect on cell membranes and has no agonistic properties. It reduces or inhibits the stimulating effects of catecholamines (released especially under the influence of physical or mental stress) on the heart. It reduces tachycardia, minute capacity and cardiac contractility, and further reduces blood pressure. Metoprolol is completely absorbed after oral administration. Has a significant first-pass effect through the liver; the oral bioavailability of a single oral dose is 50%. Each prolonged-release metoprolol succinate tablet contains a large number of controlled release pellets that propagate in the gastrointestinal tract, releasing metoprolol continuously for 20 h. Metoprolol is metabolised by oxidation in the liver, mainly via CYP2D6 to inactive metabolites. Due to the polymorphism of the CYP2D6 gene, the rate of drug metabolism varies individually. Over 95% of the oral dose is excreted in the urine. Approx. 5% of the dose in unchanged form, in individual cases up to 30%. T_0,5 it is on average 3.5 hours (range 1-9 hours).

Hypersensitivity to metoprolol succinate, other β-blockers or other components of the drug. Atrio-ventricular block IIst. or III. untreated heart failure (pulmonary edema, blood stasis or hypotension) and permanent or periodic use of drugs that increase myocardial contractility (β-adrenergic agonists). Symptomatic and clinically significant sinus bradycardia (heart rate <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. 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 is contraindicated in patients with heart failure and recurrent systolic blood pressure <100 mm Hg (pre-treatment screening is advisable). Contraindicated (with the exception of the intensive care unit) is the simultaneous intravenous administration of Calcium channel blockers 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. If an asthmatic patient is using β₂-adrenomimetic (in the form of tablets or inhalants), then starting treatment with metoprolol should be checked dose β₂-adrenomimetic and increase it if necessary. Metoprolol in the form of tablets about release works on β receptors₂-adrenergic weaker than selective β-drugs₁-adrenolytic in the form of traditional tablets. Metoprolol may reduce the effectiveness of antidiabetic treatment and mask the symptoms of hypoglycaemia. The risk is lower when using metoprolol in the form of tablets by the release than in the case of selective β drugs₁-adrenolytic in the form of traditional tablets and significantly smaller than in the case of non-selective β-blockers. In the case where metoprolol is prescribed to patients with pheochromocytoma, the α-adrenolytic agent must be used in advance and continued to be administered simultaneously with metoprolol. Treatment with metoprolol may mask the symptoms of hyperthyroidism. Before the surgery, the anesthesiologist should be informed that the patient is taking β-blockers. Their discontinuation is not recommended. Selective β drugs₁-adrenolytic should be used with caution in patients with Prinzmetal angina.To date, no sufficient therapeutic experience has been obtained regarding the use of metoprolol in patients with heart failure co-existing with the following factors: unstable heart failure (NYHA class IV), acute myocardial infarction or unstable angina over the past 28 days, renal dysfunction, liver dysfunction , age> 80 years, age <40 years, hemodynamically significant valvular disease, narrowing hypertrophic cardiomyopathy, during or after cardiac surgery within 4 months before treatment with metoprolol succinate. There is little experience in the use of metoprolol in children and adolescents.

Due to the lack of tests, the drug can be administered during pregnancy only if the benefit for the mother outweighs the risk to the embryo or fetus. Β-blockers reduce placental perfusion and may cause fetal death and premature birth. The intrauterine fetal development was delayed after long-term use of metoprolol in pregnant women with mild and moderate hypertension. Β-blockers can prolong labor and cause bradycardia in the fetus and newborn. There are also reports of hypoglycaemia, hypotension, hyperbilirubinemia and a reduced response to 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 the blocking of β-adrenergic receptors (eg cardiac and pulmonary complications). The concentration of metoprolol in milk is about three times higher than in the mother's plasma, although its total amount in milk is small. Although, at therapeutic doses, the risk of side effects is low (except for people with slow metabolism), the breast-fed infant should be observed for signs of beta-adrenergic blocking.

Very common: significant decrease in blood pressure, orthostatic hypotension (very rarely with fainting), fatigue. Common: pain and dizziness, bradycardia, balance disorders (very rarely combined with fainting), palpitations, cold hands and feet, exercise dyspnoea, nausea, abdominal pain, diarrhea, constipation. Uncommon: weight gain, depression, decreased concentration, drowsiness, nightmares, paresthesia, transient worsening of heart failure, Ist block, precordial pain, bronchospasm, vomiting, rash (psoriasis-like urticaria) and dystrophic skin changes), increased sweating, muscle spasms, swelling. 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 , hair loss, impotence and other sexual dysfunctions, plastic penile sclerosis (Peyronie's disease). Very rare: thrombocytopenia, leukopenia, forgetfulness 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, severity of intermittent claudication or Raynaud's syndrome, taste disorders, hepatitis, hypersensitivity reactions to light, exacerbation of psoriasis, psoriasis, psoriasis-like skin changes, arthralgia, muscle weakness. Metoprolol can increase both the sensitivity to allergens and the severity of anaphylactic reactions. Β-blockers may exacerbate the symptoms of psoriasis or cause it to occur. Sudden discontinuation of β-blockers may exacerbate heart failure and increase the risk of myocardial infarction and sudden death.

Orally.Hypertension: in patients with mild to moderate hypertension 47.5 mg once daily, if necessary, the dose can be increased to 95-190 mg daily or add another antihypertensive drug to the treatment regimen.Angina pectoris: 95-190 mg once a day, if necessary, other medicines used to treat coronary artery disease may be added to the treatment schedule.Heart arythmia: 95-190 mg once a day.Prophylactic treatment after myocardial infarction190 mg once a day.Heart palpitations caused by functional cardiac disorders: 95 mg once a day, if necessary, the dose may be increased to 190 mg.Migraine prophylaxis: 95-190 mg once a day.Stable symptomatic heart failure: individually. The recommended starting dose for patients with NYHA class III-IV heart failure is 11.88 mg once daily in the first week of treatment, the dose can be increased to 23.75 mg daily in the second week. The recommended starting dose in patients with class II NYHA heart failure is 23.75 mg once daily in the first 2 weeks of treatment, after which it is recommended to double the dose, the dose is increased every other week to 190 mg per day or up to the maximum dose tolerated by the patient . In long-term therapy, the target dose should be set at 190 mg daily or at the maximum tolerated dose level of the patient. If a drop in blood pressure occurs, it may be necessary to reduce the dose of another concomitant medicine. The drop in blood pressure does not have to be an obstacle to the long-term use of Metoprolol, however, the dose should be reduced until the patient has stabilized.
Special groups of patients. In patients with severe hepatic impairment, for example, in patients with portal vein anastomosis with a superior vena cava, a dose reduction may be necessary. In patients> 80 years, special care should be taken when increasing the dose. There is no need to change the dosage in patients with impaired renal function.
The tablets should be taken once a day in the morning. The tablets can be divided into halves along the dividing line. They can be swallowed whole or divided, they should not be chewed or crushed. Drink at least 1/2 glass of water.