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Dual Endothelin Receptor Antagonist (ERA) Pregnancy: Contraindicated (Pregnancy Prevention Programme)

Bosentan

Brand names: Tracleer

Adult dose

Dose: 62.5 mg BD for 4 weeks, then 125 mg BD
Route: Oral
Frequency: Twice daily
Max: 125 mg BD
For PAH and digital ulcers in systemic sclerosis. Monthly LFT monitoring mandatory — risk of hepatotoxicity. Teratogenic — mandatory PPP.

Paediatric dose

Route: Oral
Frequency: BD
Max: Paediatric dosing by weight: 10–20 kg: 31.25 mg BD; >20–40 kg: 62.5 mg BD; >40 kg: 125 mg BD
Paediatric dispersible tablet (Volibris paediatric) available for PAH. Specialist initiation.

Dose adjustments

Renal

No dose adjustment required

Hepatic

Contraindicated in moderate-severe hepatic impairment. Hepatotoxicity risk — monitor LFTs monthly.

Clinical pearls

  • Bosentan is a potent inducer of CYP2C9 and CYP3A4 — multiple drug interactions
  • Monthly LFT monitoring is mandatory; stop if ALT >8× ULN
  • Pregnancy prevention programme (PPP) mandatory — pregnancy test monthly
  • First ERA approved for PAH; also used for digital ulcer prevention in SSc (RAPIDS trials)

Contraindications

  • Pregnancy (mandatory PPP)
  • Moderate-severe hepatic impairment
  • Concomitant ciclosporin
  • Concomitant glibenclamide

Side effects

  • Hepatotoxicity (10% — dose-dependent, usually reversible)
  • Anaemia (haemoglobin decrease)
  • Fluid retention/oedema
  • Flushing
  • Headache
  • Elevated transaminases

Interactions

  • Ciclosporin — 50-fold increase in bosentan levels (contraindicated)
  • Glibenclamide — increased hepatotoxicity risk (contraindicated)
  • Hormonal contraceptives — reduced efficacy (use barrier method)
  • Warfarin — reduced INR; monitor carefully
  • Sildenafil — reduced sildenafil levels

Monitoring

  • LFTs monthly
  • Haemoglobin (3 and 6 months, then 6-monthly)
  • Blood pressure
  • Pregnancy testing monthly for WOCBP

Reference: BNFc; RAPIDS-2 Trial (Matucci-Cerinic et al, Ann Rheum Dis 2008); BNF; NICE TA233. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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