1 tabl powl. contains 5 mg or 10 mg of Bisoprolol fumarate.
Action:
Cardioselective ß-blocker with high affinity for ß receptors1 in the heart of. It does not show intrinsic sympathomimetic activity. There is no clinically significant stabilizing effect on the cell membrane. By inhibiting ß receptors2 bisoprolol slightly increases the tone of smooth muscle (including in the bronchi). The effect of the drug is maintained for over 24 hours, which allows administration in a single daily dose. After oral administration, the maximum concentration in the blood occurs after 1-3 hours. The degree of absorption of the drug does not depend on food intake. Bisoprolol binds to 30% of plasma proteins. As a result of the first pass effect of the liver, no more than 10% of the absorbed dose of the drug is metabolised in the liver. About 50% of the dose is metabolised in the liver and excreted in the urine as metabolites, 50% is excreted in the urine in unchanged form. T0,5 is 10-12 h.
Contraindications:
Hypersensitivity to Bisoprolol, other ß-blockers or other ingredients of the preparation. acute or chronic decompensated heart failure. Cardiogenic shock. Atrio-ventricular conduction block IIst. and IIIst .. The sick sinus syndrome. Block of sinus-atrioventricular conduction. Bradycardia (pulse rate less than 50 / min before starting treatment). Hypotension below 90 mmHg. Metabolic acidosis. Bronchial obstructive disease, bronchial asthma. A severe form of obliterative peripheral artery disease or a severe form of Raynaud's syndrome. Untreated phaeochromocytoma.
Precautions:
In patients treated with bisoprolol, intravenous Calcium antagonists and antiarrhythmics should not be administered intravenously, except when used in ICU ward. In patients with a history of (also including family history of) psoriasis, bisoprolol and other β-adrenergic blockers may only be used after careful consideration of the risks and benefits of such treatment. Administration of the drug to patients with a history of hypersensitivity reactions and to patients during the course of desensitization requires consideration of benefits and risks. Particularly cautiously used in cases of: diabetes mellitus and Glucose metabolism disorders; prolonged fasting and excessive physical exertion; treatment of patients with known adrenal phaeochromocytoma (bisoprolol can be used after obtaining a pharmacological blockade of α receptors), bronchial asthma and other obstructive bronchitis diseases, peripheral circulation disorders (including disease and Raynaud's syndrome); hyperthyroidism with thyrotoxicosis, atrioventricular block of Ist, hepatic and renal failure, and in the elderly. The efficacy and safety of the medicine in children has not been determined. The drug contains lactose and should not be used in patients with inherited lactose intolerance, lactase deficiency (Lapp type), or malabsorption of glucose-galactose.
Pregnancy and lactation:
It is not recommended during pregnancy if it is not absolutely necessary. If treatment with bisoprolol was considered necessary, placental flow and fetal development should be monitored. In the event of a harmful effect on pregnancy or fetal development, alternative treatment should be considered. Newborns of mothers treated with bisoprolol should be closely supervised by a physician for approximately 72 hours after birth, due to the increased risk of bradycardia, hypotension, hypoglycaemia and respiratory distress. The use of the drug during breastfeeding is not recommended due to the lack of data on the penetration of bisoprolol in breast milk.
Side effects:
Very common: bradycardia (in patients with chronic heart failure). Common: worsening of heart failure (in patients with heart failure); dizziness and headache; nausea, vomiting, diarrhea, constipation; feeling of freezing or limb numbness, hypotension; asthenia (in patients with chronic heart failure), fatigue.Uncommon: atrioventricular conduction abnormalities, worsening of heart failure and bradycardia (in patients with hypertension or angina); bronchospasm (in patients with bronchial asthma or obstructive airways disease, muscle weakness and spasms, asthenia (in patients with hypertension or angina), depression, sleep disorders. Rare: increased triglycerides, increased liver enzymes, fainting; tearing, hearing disorders, allergic rhinitis, pruritus, flushing, rash, inflammation of the liver, disturbances of potency, nightmares, hallucinations, very rare: conjunctivitis, alopecia, psoriasis or a psoriasis-like rash.
Dosage:
Treatment should be started with small doses, gradually and slowly increasing them. Doses should be adjusted to the heart rate and treatment effectiveness. Orally. The recommended starting dose is 5 mg. Usually 10 mg once a day is used and the maximum dose is 20 mg per day. In elderly patients (over 75 years), the maximum dose is 5 mg per day. In patients with advanced renal insufficiency (creatinine clearance <20 ml / min) and in patients with severe hepatic impairment, the dose of 10 mg per day should not be exceeded. The drug should be taken in the morning on an empty stomach or during breakfast. The tablets should be swallowed without chewing and washed with a sufficient amount of liquid. The tablets are divisible.
(C)
