Bisoprolol


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Angina pectoris; Hypertension Initial: 5 mg once daily adjusted according to response. Usual dose: 10 mg once daily. Max: 20 mg/day. Chronic heart failure Initial: 1.25 mg once daily. May be doubled after 1 week then increased gradually at 1-4 week intervals. Max: 10 mg/day.
Dosage Details
Oral
Angina pectoris, Hypertension
Adult: Initially, 5 mg once daily adjusted according to response. Usual dose: 10 mg once daily. Max: 20 mg daily.

Oral
Chronic heart failure
Adult: Initially, 1.25 mg once daily. May be doubled after 1 week if tolerated, then gradually increase at 1-4 week intervals. Max: 10 mg once daily.
Special Patient Group
Patients with bronchospastic disease: Initially, 2.5 mg once daily.
Renal Impairment
Angina pectoris, Hypertension:
CrCl Dosage
<40 Initially, 2.5 mg once daily. Max: 10 mg daily.
Hepatic Impairment
Angina pectoris, Hypertension: Severe: Initially, 2.5 mg once daily. Max: 10 mg daily.
Administration
May be taken with or without food.
Contraindications
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.
Special Precautions
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.
Adverse Reactions
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.
MonitoringParameters
Monitor ECG, heart rate and blood pressure.
Overdosage
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.
Drug Interactions
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.
Lab Interference
May result to false-positive aldosterone/renin ratio (ARR).
Action
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.
Chemical Structure

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Storage
Store between 20-25°C. Protect from light and moisture.
MIMS Class
ATC Classification
C07AB07 - bisoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
Disclaimer: This information is independently developed by MIMS based on Bisoprolol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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