Cardiogenic and hypovolaemic shock, 2nd or 3rd degree atrioventricular block, sinoatrial block, sick sinus syndrome, symptomatic bradycardia and hypotension, untreated phaeochromocytoma, metabolic acidosis, severe peripheral arterial occlusive disease, severe Raynaud’s syndrome, severe bronchial asthma or severe COPD, acute heart failure or during episodes of heart failure decompensation requiring IV inotropic therapy.
Patient with bronchospastic disease, myasthenia gravis, Raynaud’s syndrome, diabetes mellitus, Prinzmetal’s angina, 1st degree atrioventricular block, peripheral arterial occlusive disease, psoriasis, hyperthyroidism, hypoglycaemia. Patients undergoing major surgery involving general anaesthesia. Avoid abrupt withdrawal. Renal and hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Blood and lymphatic system disorders: Agranulocytosis, thrombocytopenia. Cardiac disorders: Chest pain, bradycardia, palpitations. Eye disorders: Ocular pain, visual disturbance. Gastrointestinal disorders: Vomiting, constipation, diarrhoea, dry mouth, abdominal pain. General disorders and admin site conditions: Asthenia, fatigue. Musculoskeletal and connective tissue disorders: Gout, back pain, arthralgia. Nervous system disorders: Dizziness, headache. Respiratory, thoracic and mediastinal disorders: Dyspnoea, rhinitis, sinusitis. Skin and subcutaneous tissue disorders: Rash, eczema, pruritus. Rarely, alopecia. Vascular disorders: Syncope, cold or numb extremities, hypotension, flushing.
Symptoms: Bradycardia, hypotension, bronchospasm, and hypoglycaemia. Management: Symptomatic and supportive treatment. Administer IV atropine for bradycardia, if inadequate, isoproterenol may be given cautiously. IV fluids, vasopressors and IV glucagon should be administered for hypotension. Administer bronchodilator therapy (e.g. isoproterenol and/or aminophylline) for bronchospasm; and IV glucose for hypoglycaemia.
May potentiate atrioventricular conduction time and may increase negative inotropic effect with class I antiarrhythmic drugs (e.g. quinidine, disopyramide, propafenone). Concomitant use with calcium antagonists (e.g. verapamil, diltiazem) may lead to atrioventricular block and profound hypotension. Concomitant catecholamine-depleting drugs (e.g. reserpine, guanethidine) may produce excessive reduction of sympathetic activity. Heart failure may worsen when given with centrally acting antihypertensives (e.g. clonidine, methyldopa). Increased risk of bradycardia with digitalis glycosides. Coadministration with rifampicin increases metabolic clearance of bisoprolol. Reduced hypotensive effect with NSAIDs.
May result to false-positive aldosterone/renin ratio (ARR).
Description: Bisoprolol selectively and competitively blocks β1-adrenergic receptors but has little or no effect on β2-receptors except at high doses (≥20 mg). Onset: 1-2 hours. Pharmacokinetics: Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Absolute oral bioavailability: Approx 80-90%. Time to peak plasma concentration: 2-4 hours. Distribution: Widely distributed with highest concentrations in heart, liver, lungs, and saliva. Crosses blood-brain barrier. Volume of distribution: 3.5 L/kg. Plasma protein binding: Approx 30-35%. Metabolism: Extensively metabolised in the liver mainly via oxidation by CYP3A4 (approx 95%) and CYP2D6 enzymes. Undergoes significant first-pass metabolism (approx 10-20%). Excretion: Via urine (approx 50% as unchanged drug and 50% as inactive metabolites) and via faeces (<2%). Elimination half-life: 9-12 hours.
Store between 20-25°C. Protect from light and moisture.
C07AB07 - bisoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
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