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 treatments for heart failure.
Composition:
1 tabl sustained release contains 23.75 mg or 47.5 mg or 95 mg Metoprolol succinate, equivalent to 25 mg, 50 mg and 100 mg metoprolol tartrate.
Action:
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 the effects caused by the sudden release of catecholamines, such as tachycardia, increased 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%. T0,5 it is on average 3.5 hours (range 1-9 hours).
Contraindications:
Hypersensitivity to metoprolol succinate, other β-blockers or to any of the excipients. Atrio-ventricular block IIst. and 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 clinically significant sinus bradycardia (heart rate <50 / min). Sick node syndrome. Cardiogenic shock. Severe disturbances of peripheral arterial circulation. Hypotension (systolic blood pressure <90 mmHg). Metabolic acidosis. Severe bronchial asthma or chronic obstructive pulmonary disease. Untreated phaeochromocytoma. Concomitant use of MAO inhibitors (other than MAO-B inhibitors). Patients with suspected acute myocardial infarction and heart rate <45 beats / min, PQ interval> 0.24 s or systolic blood pressure <100 mmHg. Patients with heart failure and recurrent systolic blood pressure> 100 mmHg (pre-treatment screening is advisable). Co-administration (except ICU) of intravenous Calcium channel blockers (like Verapamil or diltiazem) or other anti-arrhythmic drugs (such as disopyramide).
Precautions:
To date, insufficient therapeutic experience has been obtained with metoprolol in patients with heart failure co-existing with: unstable heart failure (NYHA class IV), acute myocardial infarction or unstable angina over the past 28 days, renal dysfunction, hepatic impairment, age > 80 years, age <40 years, hemodynamically significant valvular diseases, obstructive hypertrophic cardiomyopathy, during or after cardiac surgery within 4 months before treatment with metoprolol succinate. Exercise caution in patients with bronchial asthma (when co-administered with β-drugs2-adrenomimetic, a dose of β should be checked prior to treatment with metoprolol2-adrenaline and increase it if necessary). Metoprolol may interfere with glycemic control in the treatment of diabetes and mask the symptoms of hypoglycaemia.During treatment with Metoprolol, disturbances of the atrioventricular conduction may increase (risk of atrioventricular block). The drug may increase the symptoms of peripheral vascular disease. Special care should be taken in patients with Prinzmetal angina. If metoprolol is prescribed to patients with pheochromocytoma, an alpha-blocker should be used before and continued with metoprolol. Treatment with metoprolol may mask the symptoms of hyperthyroidism. Before the surgery, the anesthetist should be informed that the patient is using β-blockers; their discontinuation for surgery is not recommended. The drug may increase the sensitivity to allergens and the severity of anaphylactic reactions; adrenaline does not always give the desired therapeutic effect in patients using β-blockers. Metoprolol may exacerbate or cause signs of psoriasis. There is little experience in the use of the drug in children and adolescents.
Pregnancy and lactation:
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 mother is small (except for people with slow metabolism), the child should be observed for signs of blocking β-adrenergic receptors.
Side effects:
Very common: fatigue, marked decrease in blood pressure and orthostatic hypotension (very rarely with fainting). 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 cramps, edema. Rare: exacerbation of latent diabetes, nervousness, tension, blurred vision, dryness or eye irritation, conjunctivitis, functional symptoms of heart problems, arrhythmia, abnormal heart conduction, rhinitis, dry mouth, abnormal liver function tests, prolapse hair, impotence and other sexual dysfunctions, plastic penile sclerosis (Peyronie's disease). Very rare or unknown frequency: thrombocytopenia, leukopenia, forgetfulness or weakness of memory, confusion hallucinations, personality changes (eg mood swings), tinnitus, impaired hearing, necrosis in patients with severe peripheral vascular disease prior to treatment, worsening intermittent claudication or syndrome Raynaud, taste disorders, hepatitis, hypersensitivity reactions to light, exacerbation of psoriasis, psoriasis, psoriatic lesions on the skin, joint pain, muscle weakness.
Dosage:
Orally.Hypertension: in patients with mild to moderate hypertension 47.5 mg once daily, if necessary, the dose may be increased to 95-190 mg once a day or other antihypertensive preparation 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 may be increased to 23.75 mg once daily in the second week. The recommended starting dose is NYHA class II heart failure patients are 23.75 mg once a day during the first 2 weeks of treatment, after which it is recommended to double the dose, the dose is increased every 2 weeks to the 190 mg dose once a day or to the maximum dose tolerated by the patient. In long-term therapy, the target dose should be set at 190 mg once a day or at the maximum tolerated dose level of the patient.Special groups of patients. In patients with severe hepatic impairment, a dose reduction should be considered. In elderly patients, be especially careful 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. Table. can be divided into halves along the dividing line. They can be swallowed whole or divided, they should not be chewed or crushed. Drink with water.