Bisoprolol

Indications
 Oral
Hypertension
Adult: 2.5-10 mg daily as a single dose. Max: 20 mg daily.
CrCl (ml/min)Dosage Recommendation
<40Initial dose should be 2.5 mg daily.
<20Max: 10 mg daily.
Hepatic impairment: Severe impairment: Initially, 2.5 mg daily. Max: 10 mg daily.
Oral
Angina pectoris
Adult: 2.5-10 mg daily as a single dose. Max: 20 mg daily.
CrCl (ml/min)Dosage Recommendation
<40Initial dose should be 2.5 mg daily.
<20Max: 10 mg daily.
Hepatic impairment: Severe impairment: Initially, 2.5 mg daily. Max: 10 mg daily.
Oral
Heart failure
Adult: Initially, 1.25 mg once daily doubled after 1 wk if tolerated, then increased gradually at 1-4-wk intervals. Max: 10 mg daily.
Renal impairment: Dosage reduction may be necessary.
Hepatic impairment: Dosage reduction may be necessary.

Special Populations: Management of HTN and angina pectoris in severe renal impairment (CrCl <20 mL/min) and severe hepatic impairment: Max dose: 10 mg daily.
Contraindications
 Low cardiac output and uncompensated cardiac failure; sinus bradycardia, 1st ° heart block, cardiogenic shock, bronchospasm; severe haemorrhage. Pregnancy.
Warnings / Precautions
 Bronchospastic disease, hyperthyroidism, peripheral vascular disease, undergoing anaesthesia. Monitor blood glucose regularly. May mask symptoms of hypoglycaemia. Elderly. Gradual withdrawal is advised. Lactation.
Adverse Reactions
 Giddiness, headache, fatigue, bradycardia. Nausea, vomiting, diarrhoea or constipation, stomach discomfort, mild ocular stinging, photophobia, keratitis, decreased sexual ability. GI disturbances, dyspnoea, cold extremities, insomnia, hallucination, drowsiness and mood alterations.
Potentially Fatal: AV block, bradycardia. Rare but may occur in patients with preexisting cardiac disease. Includes severe bronchospasm, hypoglycaemia, hypotension, orthostatic hypotension, bradyarrhythmias. 'Rebound phenomenon' leading to unstable angina or MI on sudden withdrawal.
Overdose Reactions
 Symptoms include bradycardia, hypotension, congestive heart failure, bronchospasm, and hypoglycemia. Treatment include stopping the drug and instituting supportive and symptomatic measures.
Drug Interactions
 Decreased effect with aluminum and calcium salts, barbiturates, cholestyramine, NSAIDs, ampicillin, rifampicin. May mask tachycardia from hypoglycaemia induced by insulin and oral hypoglycaemics. Effects of other antihypertensives may be intensified.
Potentially Fatal: May increase the effects of drugs which slow AV conduction, α-blockers and α-adrenergic stimulants. Enhances the action of anaesthetic agents, clonidine, calcium antagonists, digitalis, hypoglycaemic agents and NSAIDs.
See Below for More bisoprolol Drug Interactions
Lab Interactions
 Increased cholesterol, thyroxine, glucose and triglycerides levels.
Mechanism of Actions
 Bisoprolol selectively and competitively blocks β-1 receptors but has little or no effect on β-2 receptors except at high doses.
Absorption: Absorbed completely from the GI tract (oral); peak plasma concentrations after 2-4 hr.
Distribution: Protein-binding: 30%.
Metabolism: In the liver.
Excretion: Excreted in urine. 10-12 hr (elimination half-life).
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store below 25°C.
ATC Classification
 C07AB07 - bisoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
Storage
 Oral: Store below 25°C.
Available As
  • Bisoprolol 10 mg
  • Bisoprolol 2.5 mg
  • Bisoprolol Fumarate 2.5 mg
  • Bisoprolol 5 mg
  • Bisoprolol Fumarate 5 mg

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