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Bedaquiline

Anti-tuberculosis agent (diarylquinoline ATP synthase inhibitor) · Antitubercular drug

Also known as Sirturo

START
400 mg OD ×2 wk, then 200 mg 3×/week with food
TYPICAL MAX
400 mg/day (loading phase)
STOP IF
QTc >500 ms, significant arrhythmia, or hepatotoxicity
WATCH
ECG/QTc, electrolytes, LFTs at baseline and periodically
CDSCO approvedSchedule H1ATC J04AK05
Dose laddermg/d
200maintenance400loading/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo adjustment (mild–moderate)30CAUTIONLimited data — caution90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
2.5hONSET5hPEAK23.6w2.3dDURATION
ONSET
2.5h · absorption
PEAK
5h · Tmax (fed)
23.6w · t½ ~5.5 mo
DURATION
2.3d · 3×/week
EXCRETION
Mainly faecal; minimal renal
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Limited data; use within an optimised MDR-TB regimen if benefit outweighs risk.
FDA category + note
Top interactionssee all 12
  • AbarelixSevereDatabaseDDInter
  • AbirateroneSevereDatabaseDDInter
  • AdenosineSevereDatabaseDDInter
  • AlfuzosinSevereDatabaseDDInter
Available in India

1 branded formulation. Look up specific brands in the Drugs workspace.

Mechanism

Inhibits mycobacterial ATP synthase (proton pump c-subunit), depleting ATP and producing bactericidal/sterilising activity against Mycobacterium tuberculosis including drug-resistant strains.

Indications

Multidrug-resistant pulmonary tuberculosis (combination regimen)

Dosing

Adult
400 mg PO once daily for 2 weeks, then 200 mg three times weekly for 22 weeks, with food, in a combination regimen.
Pediatric
Weight-banded dosing under specialist care.
Renal adjustment
No adjustment in mild–moderate; caution in severe (limited data).
Hepatic adjustment
Caution; avoid in severe hepatic impairment.
Geriatric
Limited data; monitor ECG/LFTs.
Max dose
400 mg/day (loading); 200 mg three times weekly (maintenance)

Pharmacokinetics

Onset
Antimycobacterial effect over weeks
Peak effect
~5 h (Tmax, with food)
Duration
Long (very prolonged terminal elimination)
Half-life
Terminal ~5.5 months (tissue redistribution)
Bioavailability
Increased ~2× with food
Protein binding
>99.9%
Metabolism
Hepatic CYP3A4 (N-desmethyl active metabolite)
Excretion
Mainly faecal; minimal renal

Contraindications

  • Concomitant strong CYP3A4 inducers/inhibitors (caution)
  • Hypersensitivity
  • Caution: QT prolongation, hepatic disease

Side effects

Common
NauseaArthralgiaHeadacheQT prolongationTransaminase elevation
Serious
  • QT prolongation / arrhythmia
  • Hepatotoxicity
  • Increased mortality signal (early trial — use within optimised regimen)
  • Pancreatitis (rare)

Pregnancy & lactation

Pregnancy

Limited data; use within an optimised MDR-TB regimen if benefit outweighs risk.

Lactation

Accumulates in milk (animal data); weigh benefit/risk.

Drug interactions

Abarelix
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Abiraterone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Adenosine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfuzosin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alimemazine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amitriptyline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amoxapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apomorphine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Ask House about Bedaquiline

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Sources: Goodman & Gilman 14e, Harrison 22e, Katzung, BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20