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Drugs, Supplies and Delivery
Bisoprolol
Bisoprolol is a cardioselective beta-1 adrenergic receptor blocker widely used to manage hypertension, chronic heart failure, and angina. Known for its high selectivity and once-daily dosing, bisoprolol is a cornerstone in cardiovascular therapy. This article synthesizes evidence from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to outline its pharmacology, clinical applications, and safety profile.
Bisoprolol selectively inhibits beta-1 adrenergic receptors in the heart, leading to:
- Reduced Heart Rate and Contractility: Lowers cardiac output by decreasing sympathetic stimulation.
- Suppressed Renin Release: Inhibits renin-angiotensin-aldosterone system (RAAS) activation, reducing blood volume.
- Vasodilation: Indirectly improves endothelial function over time (Lippincott Textbook of Pharmacology).
Its high beta-1 selectivity minimizes effects on beta-2 receptors (e.g., bronchoconstriction), making it safer for patients with mild respiratory conditions compared to non-selective beta-blockers (Lange Basic & Clinical Pharmacology).
- Hypertension:
- First-line or adjunctive therapy, particularly in patients with comorbid angina or arrhythmias.
- Chronic Heart Failure with Reduced Ejection Fraction (HFrEF):
- Improves survival and reduces hospitalization (e.g., CIBIS-II trial) (BNF).
- Chronic Stable Angina: Reduces myocardial oxygen demand.
- Off-Label: Post-myocardial infarction (MI) management.
- Hypertension:
- Adults: 5–10 mg once daily, increased to 20 mg daily if needed.
- Elderly: Start at 2.5 mg daily to minimize adverse effects.
- Heart Failure:
- Initial dose 1.25 mg once daily, titrated weekly to 10 mg daily as tolerated.
- Renal/Hepatic Impairment:
- Renal (eGFR <20 mL/min): Max 10 mg daily.
- Hepatic Cirrhosis: Avoid in severe impairment (BNF).
- Bradycardia, fatigue, dizziness, cold extremities.
- Sleep disturbances, depression.
Serious (Rare):
- Heart Failure Exacerbation: Avoid in decompensated heart failure.
- Bronchospasm: Rare but possible in severe asthma/COPD.
- Hypoglycemia Masking: Blunts tachycardia, a key hypoglycemia symptom in diabetics (Lippincott Textbook of Pharmacology).
- Contraindications:
- Severe bradycardia, second-/third-degree heart block, cardiogenic shock.
- Acute asthma, severe peripheral arterial disease.
- Monitoring:
- Heart rate, blood pressure, and signs of worsening heart failure.
- Renal/hepatic function in long-term use.
- Pregnancy/Lactation:
- Pregnancy: Category C (risk of fetal growth restriction); use only if benefits outweigh risks.
- Lactation: Excreted in breast milk; monitor infant for bradycardia (BNF).
- Calcium Channel Blockers (e.g., verapamil): Additive bradycardia/AV block.
- CYP3A4 Inhibitors (e.g., fluoxetine): Increase bisoprolol levels (reduce dose).
- Insulin/Sulfonylureas: Masks hypoglycemia symptoms (e.g., tremor, palpitations).
- NSAIDs (e.g., ibuprofen): Reduce antihypertensive efficacy (Lange Basic & Clinical Pharmacology).
- Generic: Bisoprolol fumarate.
- Brand Names: Cardicor® (UK), Zebeta® (US), Concor® (EU).
- Combination Products: Bisoprolol/hydrochlorothiazide (e.g., Lodoz®).
