Index of drugs

Hypertension. Angina pectoris. Arrhythmias, especially supraventricular tachycardia. Prevention of sudden cardiac death and reinfarction in patients after an acute phase of infarction. Paroxysmatic arrhythmias in the course of functional heart disorders. Prophylaxis of migraine. Stable, symptomatic heart failure (NYHA class II-IV, with left ventricle ejection fraction <40%), in combination with other treatments.

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

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, increased minute capacity and cardiac contractility, and also lowers blood pressure. Metoprolol is completely absorbed after oral administration. Due to the significant first-pass effect of the liver, the bioavailability of a single oral dose is about 50%. Bioavailability of tablets sustained release is about 20-30% lower than traditional tablets, but this is not clinically significant, as the AUC values ​​remain the same. In about 5-10%, it binds to plasma proteins. Each tablet of metoprolol succinate on the front release contains a large number of controlled release pellets that propagate in the gastrointestinal tract, releasing metoprolol continuously for 20 h. Metoprolol is mainly, but not exclusively, metabolised by CYP2D6 into inactive metabolites. Due to the polymorphism of the CYP2D6 gene, the metabolic rate varies individually with those with slow metabolism (around 7-8%) showing higher plasma concentrations and slower rates of excretion compared to those with rapid metabolism. Over 95% of the oral dose is excreted in the urine. Approx. 5% of the dose is excreted unchanged, in individual cases up to 30%. T_0,5 metoprolol is on average 3.5 h (range 1-9 h).

Hypersensitivity to Metoprolol, 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 cardiac 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).

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-adrenomimetic and increase it if necessary; metoprolol in the form of tabl. about release works on β receptors₂ to a lesser extent than traditional forms of the selective β-blocker tablets). Metoprolol may impair glycemic control in the treatment of diabetes and mask the symptoms of hypoglycaemia (this risk is lower when metoprolol is used in the form of retardation table than in the case of traditional forms and significantly lower than in the case of non-selective β-blockers).During treatment with metoprolol, disturbances of the atrioventricular conduction may increase (risk of atrioventricular block). Due to the antihypertensive effect, metoprolol may exacerbate the symptoms of peripheral vascular disease. If metoprolol is prescribed to patients with a 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 anesthesiologist should be informed that the patient accepts β-blockers (their discontinuation is not recommended during the operation). 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. In patients with Prinzmetal's angina, selective β-blockers should be used with caution. There are insufficient data on the use of metoprolol in patients with heart failure coexisting with the factors listed below: unstable heart failure (NYHA class IV); acute myocardial infarction or unstable angina over the previous 28 days; kidney problems; liver dysfunction; age> 80 years; age <40 years; hemodynamically significant valve disease; hypertrophic obstructive cardiomyopathy; during or after cardiac surgery within the last 4 months before treatment with metoprolol succinate. Abrupt discontinuation of the β-blocker may exacerbate heart failure and increase the risk of myocardial infarction and sudden death. The drug should not be withdrawn suddenly. The drug should be discontinued gradually over a period of at least 2 weeks, reducing the dose until the lowest dose corresponding to half the tablet at the end. release with the lowest potency, i.e. 11.875 mg of metoprolol succinate (corresponding to 12.5 mg of metoprolol tartrate). This final dose should be used for at least 4 days before the end of treatment. If you have any withdrawal symptoms, the dose should be reduced even more slowly. It is not recommended for use in children and adolescents due to limited clinical experience.

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 it 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.

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, anxiety, 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 frequency unknown: thrombocytopenia, leukopenia, forgetfulness or weakness of memory, confusion hallucinations, personality changes (e.g.mood changes), tinnitus, impaired hearing, necrosis in patients with severe peripheral vascular disease prior to treatment, worsening intermittent claudication or Raynaud's syndrome, taste disorders, hepatitis, hypersensitivity reactions to light, exacerbation of psoriasis, onset of psoriasis, psoriasis-like changes on the skin, joint pain, muscle weakness.

Orally. Adults.Hypertension: in patients with mild to moderate hypertension 47.5 mg once daily. If necessary, the dose can be increased to 95-190 mg per day or to add another antihypertensive drug to the treatment regimen.Angina pectoris: 95-190 mg once a day. If necessary, other preparations used in the treatment of coronary heart disease may be included in the treatment schedule.Heart arythmia: 95-190 mg once a day.Prevention of myocardial infarction190 mg once a day.Paroxysmatic arrhythmias in the course of functional heart disorders: 95 mg once a day. If necessary, the dose can be increased up to 190 mg.Prophylaxis of migraine: 95-190 mg once a day.Stable symptomatic heart failure. In patients with stable symptomatic heart failure, treated with other medicines, the dose of metoprolol succinate is determined 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 for patients with NYHA class II heart failure is 23.75 mg once daily in the first 2 weeks of treatment. After the first two weeks, it is recommended to double the dose. The dose should be increased every other week to 190 mg once a day or up 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. 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. In the event of a drop in blood pressure, it may be necessary to reduce the dose of another medicine used at the same time. The reduction in blood pressure does not have to be an obstacle to the long-term use of metoprolol, but a lower dose should be administered until the patient's condition has stabilized.Special groups of patients. No dose adjustment is necessary for patients with impaired renal function. In patients with severe hepatic impairment, eg in patients with portal vein anastomosis with a superior vena cava, a dose reduction may be necessary. There is insufficient data on patients> 80 years of age, so special care should be taken when increasing the dose.
The tablets should be taken once a day in the morning. The tablets should be swallowed whole or divided, they should not be chewed or crushed. Drink with water (at least half a glass). The tablet can be divided into equal halves.