Cardioselective drug β1-adrenolytic, deprived of intrinsic sympathomimetic activity and stabilizing properties of cell membranes. The mechanism of hypotensive action is not explained, it is known that bisoprolol significantly reduces renin activity in plasma. In patients with ischemic heart disease blocking β receptors1-adrenergic relieves heart rate, reduces ejection volume and myocardial oxygen demand. Bioavailability is 90%. Plasma proteins are approximately 30% bound. It is metabolized in the liver and excreted in the urine, including 50% in the form of metabolites. T0,5 is 10-12 h, the effect is maintained for 24 h after a single administration.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. acute heart failure or during incidents of decompensation of heart failure requiring intravenous inotropic medication. Cardiogenic shock. Atrio-ventricular block IIst. or IIIst. (without a pacemaker). Sick node syndrome. Sinus-vestibular block. Symptomatic bradycardia. Symptomatic hypotension. Severe bronchial asthma or severe chronic obstructive pulmonary disease. Severe cases of obliterative peripheral arterial disease or severe cases of Raynaud's syndrome. Untreated phaeochromocytoma. Metabolic acidosis.
Precautions:
Do not use bisoprolol in children and adolescents under 12 years of age due to lack of clinical experience in this age group. Do not interrupt the treatment with bisoprolol unless it is clearly indicated, especially in patients with ischemic heart disease, due to the possibility of temporary worsening of cardiac function. Bisoprolol should be used with extreme caution in patients with: hypertension or angina pectoris and concomitant heart failure; in patients with diabetes with significant fluctuations in blood Glucose (the medicine may mask the symptoms of hypoglycaemia); in people using a strict diet; during desensitization treatment (the possibility of increasing the sensitivity to allergens and the severity of anaphylactic reactions, the use of epinephrine may not always bring the expected therapeutic effects); in first degree atrioventricular block; in Prinzmetal's stuffing box; in obliterative disease of the peripheral arteries (symptoms may increase, especially at the beginning of treatment). In patients with a history of psoriasis or psoriasis, bisoprolol should only be used after careful consideration of the benefits and risks. The medicine may mask the symptoms of thyrotoxicosis. In patients with pheochromocytoma, the drug should be used only after administration of α-blockers. In patients undergoing general anesthesia, the blocking of β-blockers decreases the occurrence of arrhythmia and myocardial ischemia during the introduction of anesthesia, intubation and after the procedure. It is now recommended to continue the use of β-blockers during the intraoperative period. If it is necessary to stop the use of β-blockers prior to surgery, this should be done gradually and completed 48 hours before the planned anesthesia. In the case of bronchial asthma or other obstructive pulmonary diseases, concomitant use of bronchodilators is recommended. Patients with asthma may occasionally experience an increase in resistance in the airways, so it may be necessary to increase the dose of2-adrenomimetyków. Due to the lactose content, the preparation should not be used in patients with rare inherited disorders associated with galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose - galactose.
Pregnancy and lactation:
Bisoprolol may have a detrimental effect on pregnancy and / or the development of the fetus or newborn baby.Β-blockers reduce placental flow, which may cause fetal growth retardation, fetal death, miscarriage or premature birth. In the fetus and newborn, bisoprolol may cause, among others, hypoglycaemia and bradycardia. If beta blocker therapy is necessary, selective β-medication should be used1-adrenolitycznym. The drug should not be used during pregnancy unless clearly necessary. If treatment with bisoprolol was considered necessary, the uterine-placental flow and fetal development should be monitored. The newborn should be under strict control. Symptoms of hypoglycaemia and bradycardia usually occur within 3 days after birth. Breastfeeding during administration of bisoprolol is not recommended.
Side effects:
Very common: bradycardia (in patients with chronic heart failure). Common: dizziness, headache, gastrointestinal disturbances (nausea, vomiting, diarrhea, constipation), feeling cold or numb in the limbs, hypotension (especially in patients with heart failure), weakness (in patients with chronic heart failure), fatigue. Uncommon: atrioventricular conduction disorder, worsening myocardial insufficiency and bradycardia and asthenia (in patients with arterial hypertension or angina), bronchospasm in patients with bronchial asthma or history indicating obstructive pulmonary disease, muscle weakness, muscle spasms, depression sleep disorders. Rare: increased triglycerides, increased liver enzymes (ALAT, AST), fainting; decreased tear secretion, impaired hearing, allergic rhinitis, hypersensitivity reactions (itching, sudden redness, rash), hepatitis, potency disorders, nightmares, hallucinations. Very rare: conjunctivitis; alopecia, call or exacerbation of psoriasis or psoriasis-like rash. Unsolicited symptoms such as dizziness, headache, fatigue occur mainly at the beginning of treatment. They are usually mild and usually disappear within 1-2 weeks.
Dosage:
Oral: it is recommended to start treatment with the lowest possible dose; initially 5 mg a day; the usual therapeutic dose is 10 mg once a day; the maximum daily dose is 20 mg. In patients with mild to moderate hepatic or renal impairment, dose modification is not usually necessary. In patients with severe renal impairment (creatinine clearance <20 ml / min) and in patients with severe hepatic impairment, the daily dose should not exceed 10 mg. It is not necessary to change the dose in elderly patients, but it is recommended to start with the lowest possible dose. The tablets should be taken in the morning, you can during the meal with liquid.