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. Late stages of peripheral arterial occlusive disease or severe forms of Raynaud's syndrome. Untreated phaeochromocytoma. Metabolic acidosis. Co-administration of floctafenine and sultopride.
Precautions:
The drug should not be used in the treatment of chronic heart failure (due to the inability to gradually increase the dose with this preparation). Due to the lack of use experience, it is not recommended for use in children and adolescents below 12 years of age. Bisoprolol should be used with extreme caution in patients with: hypertension or angina pectoris and concomitant heart failure; with bronchial asthma or other chronic obstructive pulmonary diseases (you should be given concomitant bronchodilators at the same time, it may be necessary to increase the dose of2agonists); with diabetes with large fluctuations in blood Glucose (the risk of masking the symptoms of hypoglycaemia), with hyperthyroidism (the ability to mask the symptoms of hyperthyroidism), 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 adrenaline may not always bring the expected therapeutic effects); in first degree atrioventricular block; in Prinzmetal's stuffing box; in disorders of peripheral circulation (the symptoms may increase, especially at the beginning of treatment); in patients with pheochromocytoma (the drug should be used only after administration of alpha-blocker drugs); in patients with a history of psoriasis or psoriasis only after careful consideration of the benefits and risks. 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. 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. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency 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 medicine 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:
Common: fatigue, exhaustion, dizziness, headaches (especially at the beginning of treatment, they are generally mild and often disappear within 1-2 weeks), feelings of cold or numbness in the limbs, Raynaud's syndrome, exacerbation of existing claudication, disorder gastrointestinal (nausea, vomiting, diarrhea, abdominal pain and constipation). Uncommon: sleep disturbances, depression, bradycardia, atrioventricular conduction disorders (releasing atrioventricular conduction or exacerbation of the existing atrio-ventricular block), worsening of concomitant heart failure, orthostatic hypotension, bronchospasm in patients with bronchial asthma or obstructive pulmonary disease interview, weakness and muscle spasms, joint pain, asthenia. Rare: allergic rhinitis, emergence of antinuclear antibodies with atypical clinical features similar to lupus, resolving after stopping treatment, increased triglycerides, hypoglycaemia, nightmares, hallucinations, syncope, decreased tear secretion, impaired hearing, hepatitis, hypersensitivity reactions (pruritus, redness of the face, rash), potency disorders, increased liver enzymes (ALAT, AST). Very rare: conjunctivitis, alopecia, induction or worsening of psoriasis or psoriasis-like rash.
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 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.