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Bisoprolol

Cardioselective beta-1 adrenergic receptor antagonist (beta-blocker) · Antihypertensive, Antiarrhythmic, Antianginal, Heart Failure Treatment, Thyrotoxicosis Management

Also known as Bisoprolol fumarate

START
Check HR (>60 bpm), BP, auscultate for wheeze. Baseline ECG. In HFrEF: start at 1.25mg and titrate slowly (every 2 weeks) while monitoring for fluid overload.
TYPICAL MAX
20mg/day (HTN); 10mg/day (HFrEF). Loss of cardioselectivity at doses >20mg.
STOP IF
HR <50 bpm, SBP <90 mmHg, new wheeze/bronchospasm, acute heart failure decompensation, second-degree AV block, syncope.
WATCH
HFrEF: may worsen symptoms initially—ensure stable fluid status before starting and during titration. Diabetics: may mask hypoglycemia. Do not stop abruptly—rebound angina/arrhythmia risk. COPD: preferred beta-blocker if indication exists (cardioselective).
CDSCO approvedSchedule HATC C07AB07
Dose laddermg/d
1.25HFrEF start2.5titrate5titrate10titrate20Max HTN
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo adjustment20REDUCEMax 10mg/day90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
2hONSET3hPEAK11h1dDURATION
ONSET
2h · Onset 1-2 hours
PEAK
3h · Tmax 2-4 hours
11h · t½ ~10-12 hours
DURATION
1d · 24 hours (QD)
EXCRETION
Renal and fecal (~50% each)
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Crosses placenta; may cause fetal bradycardia, hypoglycemia, and growth restriction. Use lowest effective dose. Monitor newborn for 48-72h after delivery (bradycardia, hypoglycemia).
FDA category + note
Top interactionssee all 12
  • LidocaineSevereTextbook-citedKDT 7e · p950
  • AdrenalineSevereTextbookKDT 7e · p133
  • AmilorideSevereTextbookKDT 7e
  • SofosbuvirSevereTextbookHarrison 22e · unknown
Available in India

108 branded formulations and 3 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Mechanism

Selective competitive antagonism of beta-1 adrenergic receptors in cardiac muscle, reducing heart rate, myocardial contractility, and cardiac output. At higher doses (>20mg), loses cardioselectivity and blocks beta-2 receptors.

Indications

HypertensionChronic heart failure with reduced ejection fraction (HFrEF)Chronic stable anginaSupraventricular tachyarrhythmias (rate control)Post-myocardial infarction secondary prevention

Dosing

Adult
Hypertension/angina: 5mg PO daily initially, may increase to 10mg daily; max 20mg daily. HFrEF: 1.25mg PO daily initially, double every 2 weeks to 2.5mg, 3.75mg, 5mg, 7.5mg, target 10mg daily (CIBIS-II target).
Pediatric
Not established in children.
Renal adjustment
No adjustment needed for mild-moderate impairment. Severe (CrCl <20): max 10mg/day.
Hepatic adjustment
No adjustment for mild-moderate. Severe: use caution.
Geriatric
Start 2.5mg daily; slower titration; monitor for bradycardia and hypotension.
Max dose
20mg/day (hypertension); 10mg/day (HFrEF)

Pharmacokinetics

Onset
1-2 hours
Peak effect
Tmax 2-4 hours; antihypertensive effect over 1-2 weeks
Duration
24 hours (QD dosing)
Half-life
~10-12 hours
Bioavailability
~88% (first-pass metabolism ~10-15%)
Protein binding
~30%
Metabolism
Hepatic via CYP3A4 (~50%) and CYP2D6 (~50%); metabolites inactive
Excretion
~50% renal (unchanged + metabolites); ~50% fecal

Contraindications

  • Severe bradycardia (<60 bpm)
  • Second or third-degree AV block
  • Sick sinus syndrome
  • Cardiogenic shock
  • Severe asthma or COPD (relative—less risk than non-selective beta-blockers)
  • Severe peripheral arterial disease
  • Hypersensitivity to bisoprolol

Side effects

Common
FatigueBradycardiaHypotensionDizzinessHeadacheCold extremitiesGastrointestinal upsetSleep disturbances
Serious
  • Severe bradycardia / heart block
  • Heart failure decompensation
  • Bronchospasm (less common than non-selective BBs)
  • Masking of hypoglycemia
  • Peripheral vascular insufficiency
  • Depression
  • Sexual dysfunction

Pregnancy & lactation

Pregnancy

Crosses placenta; may cause fetal bradycardia, hypoglycemia, and growth restriction. Use lowest effective dose. Monitor newborn for 48-72h after delivery (bradycardia, hypoglycemia).

Lactation

Excreted in breast milk in low concentrations (~3% of maternal dose); infant exposure minimal. Generally considered compatible with breastfeeding. Monitor infant for bradycardia.

Drug interactions

Lidocaine
Severe
Textbook-cited

Enhanced bradycardia and hypotension.

Avoid concurrent use

Source: KDT 7e · p950

Adrenaline
Severe
Textbook

Marked rise in BP.

Adrenaline should not be given to patients receiving β blockers.

Source: KDT 7e · p133

Amiloride
Severe
Textbook

Hyperkalaemia more likely.

Source: KDT 7e

Sofosbuvir
Severe
Textbook

Severe bradycardia.

Extreme caution advised if amiodarone is co-administered with sofosbuvir and a beta blocker.

Source: Harrison 22e · unknown

Aminophylline
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clonidine
Severe
Database

Beta-blocker masks clonidine withdrawal rebound hypertension; abrupt discontinuation of either can cause hypertensive crisis.

Withdraw bisoprolol first over 1-2 weeks, then taper clonidine.

Source: Kimi deep-research + Cla

Diltiazem
Severe
Database

Increased propensity for AV block, severe bradycardia, and decreased left ventricular function.

Avoid concurrent administration. The concurrent administration of diltiazem with a beta blocker is contraindicated.

Source: DDInter

Disopyramide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Dolasetron
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Dyphylline
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Related guidelines

Ask House about Bisoprolol

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19