Bisoprolol

Generic Name

Bisoprolol fumarate

Brand Names

Concor

Zebeta (in some regions)

Emcor

Generic formulations widely available globally

Drug Class

Beta-1 selective adrenergic receptor blocker (Cardioselective beta-blocker)

Antihypertensive agent

Antianginal agent

Mechanism of Action

Bisoprolol selectively blocks beta-1 adrenergic receptors in the heart, reducing the effects of adrenaline and noradrenaline

This leads to decreased heart rate, myocardial contractility, and cardiac output

It also reduces renin secretion from the kidneys, contributing to a drop in blood pressure

Because of its cardioselectivity, it has less effect on beta-2 receptors found in bronchial and vascular smooth muscle, making it safer than non-selective beta-blockers in patients with mild asthma or COPD

Its effects are dose-dependent; cardioselectivity may decrease at higher doses

Indications

Approved Uses

Hypertension (high blood pressure)

Chronic stable angina pectoris

Chronic heart failure (stable, with reduced ejection fraction, usually in combination with ACE inhibitors, diuretics, and aldosterone antagonists)

Off-label/Clinical Practice Uses

Atrial fibrillation (rate control)

Supraventricular tachycardia

Migraine prophylaxis (rarely)

Anxiety-related tachycardia

Prevention of myocardial infarction recurrence

Post-myocardial infarction beta-blocker therapy

Management of hyperthyroidism symptoms

Dosing and Administration

Hypertension/Angina (Adults)

Initial dose: 5 mg once daily

May be increased to 10 mg once daily

Maximum dose: 20 mg once daily

Chronic Heart Failure (Adults)

Start at 1.25 mg once daily

Titrate slowly every 1–2 weeks if tolerated:

Next doses: 2.5 mg → 3.75 mg → 5 mg → 7.5 mg → 10 mg

Target maintenance dose: 10 mg once daily

Renal Impairment

For severe renal dysfunction (creatinine clearance <40 mL/min), maximum dose should not exceed 10 mg/day

Dose adjustment or close monitoring may be required

Hepatic Impairment

Use cautiously in moderate to severe hepatic impairment

No routine dose adjustment, but start at lower end of dosing range and monitor

Elderly

No specific dosage adjustment, but initiate therapy at the lower dose range

Monitor for bradycardia, hypotension, and fatigue

Pediatric Use

Safety and efficacy not established in children

Not recommended unless under specialist advice

Contraindications

Hypersensitivity to bisoprolol or any component

Severe bradycardia

Second- or third-degree AV block without pacemaker

Sick sinus syndrome

Cardiogenic shock

Acute decompensated heart failure

Severe peripheral arterial disease with critical limb ischemia

Severe asthma or bronchospasm

Precautions

Avoid abrupt discontinuation—gradually taper to avoid rebound tachycardia, hypertension, or angina exacerbation

Use caution in patients with mild/moderate bronchospastic disease

May mask signs of hypoglycemia in diabetic patients (e.g. tachycardia)

May mask signs of hyperthyroidism

May worsen symptoms in patients with peripheral vascular disease or Raynaud's phenomenon

Monitor patients with history of depression

Avoid in untreated pheochromocytoma unless alpha-blockade established

Adverse Effects

Common

Bradycardia

Fatigue

Dizziness

Hypotension

Headache

Cold extremities

Nausea

Diarrhea or constipation

Sleep disturbances or vivid dreams

Less Common

Depression

Impotence or reduced libido

Shortness of breath in predisposed patients

Weight gain (in heart failure patients)

Atrioventricular block (dose-dependent)

Rare but Serious

Exacerbation of heart failure

Bronchospasm (in asthma or COPD)

Severe bradycardia or hypotension

Masked hypoglycemia in diabetic patients

Liver enzyme elevations

Hypersensitivity reactions (rash, pruritus)

Pregnancy and Lactation

Pregnancy

Category C (may vary by country)

Bisoprolol crosses the placenta and may cause fetal bradycardia, hypoglycemia, or growth restriction

Use only when clearly indicated and benefits outweigh risks

Close fetal monitoring recommended if used

Lactation

Excreted in small amounts in breast milk

Use with caution in breastfeeding mothers

Monitor infant for bradycardia and hypoglycemia

Use in Special Populations

Heart Failure Patients

Initiate at very low doses

Titrate slowly over weeks with close monitoring

Use only in stable CHF

Renal and Hepatic Impairment

Dose reduction may be required

Monitor closely for accumulation effects

Elderly Patients

Greater sensitivity to bradycardia and hypotension

Start low and monitor regularly

Diabetic Patients

May mask adrenergic symptoms of hypoglycemia

Use with regular glucose monitoring

Drug Interactions

Calcium Channel Blockers (e.g. verapamil, diltiazem)

Additive effects on AV conduction and myocardial depression

Avoid combination or monitor ECG closely

Clonidine

Risk of rebound hypertension if either drug is withdrawn abruptly

Discontinue beta-blocker several days before stopping clonidine

Antiarrhythmics (e.g. amiodarone, digoxin)

Increased risk of bradycardia and AV block

Monitor ECG and heart rate

NSAIDs

May reduce antihypertensive efficacy of bisoprolol

Monitor blood pressure

Insulin and oral hypoglycemics

May mask hypoglycemia symptoms

Monitor glucose closely

Anesthesia agents

May enhance myocardial depression and hypotension

Inform anesthetist of beta-blocker use

Monitoring Parameters

Heart rate (avoid HR <50 bpm)

Blood pressure

Signs of worsening heart failure

Electrocardiogram in high-risk patients

Serum glucose (in diabetics)

Renal and liver function in prolonged use

Patient Counseling Points

Take the medication at the same time each day

Do not stop taking bisoprolol abruptly

Inform provider of fatigue, dizziness, fainting, or breathing difficulty

Check your pulse; report very slow heartbeat

May take a few weeks for full effect

Rise slowly to avoid lightheadedness

Avoid alcohol and excessive heat exposure

Inform dentist/surgeon of bisoprolol use

If diabetic, monitor glucose more frequently

Report cold hands/feet, mood changes, or new shortness of breath

Storage

Store at room temperature

Protect from moisture and heat

Keep in original container with tight cap