Overview
Bisoprolol is a cardioselective beta-1 adrenergic receptor blocker used primarily for hypertension, chronic heart failure, and angina pectoris. It reduces heart rate, myocardial contractility, and blood pressure through selective beta-1 blockade with minimal effect on beta-2 receptors at therapeutic doses.
Mechanism of Action
Competitively blocks beta-1 adrenergic receptors in cardiac tissue, reducing sympathetic stimulation. This decreases heart rate, myocardial contractility, and renin release, leading to reduced blood pressure and myocardial oxygen demand.
Indications
- Hypertension
- Chronic stable heart failure (NYHA Class II-III) with reduced ejection fraction
- Angina pectoris
Dosage
Hypertension: Initial 5 mg once daily, may increase to 10 mg once daily. Heart failure: Start with 1.25 mg once daily, titrate gradually to target dose of 10 mg once daily. Angina: 5-10 mg once daily. Take with or without food.
Contraindications
- Cardiogenic shock
- Sick sinus syndrome
- Second or third degree AV block (without pacemaker)
- Severe bradycardia
- Severe bronchial asthma or COPD
- Uncompensated heart failure
- Hypersensitivity to bisoprolol
Side Effects
- Bradycardia
- Fatigue
- Dizziness
- Headache
- Cold extremities
- Dyspnea
- Nausea
- Diarrhea
- Sleep disturbances
- Depression
- Bronchospasm (rare at therapeutic doses)
Interactions
- Calcium channel blockers (verapamil, diltiazem) - increased risk of bradycardia
- Other antihypertensives - additive hypotensive effects
- Insulin/oral hypoglycemics - masked hypoglycemia symptoms
- NSAIDs - reduced antihypertensive effect
- Clonidine - rebound hypertension if withdrawn concurrently
- Digoxin - increased risk of bradycardia