Bosentan

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Administration

  • Type: Endothelin receptor antagonists
  • Dosage Forms:
  • Routes of Administration: Oral
  • Common Trade Names: Tracleer

Adult Dosing

  • 62.5-125mg PO BID

Pediatric Dosing

Safety/efficacy not established

Special Populations

  • Pregnancy Rating: X
  • Lactation risk: Infant risk cannot be ruled out
  • Renal dosing:
  • Hepatic dosing: avoid in moderate-severe disease

Contraindications

  • Allergy to class/drug
  • Concomitant administration with cyclosporine A or glyburide
  • Pregnancy or potential pregnancy

Adverse Reactions

Serious

  • Anemia
  • Cirrhosis, liver failure
  • Oligozoospermia
  • Edema, fluid retention

Common

  • Anemia
  • Respiratory tract infection

Pharmacology

  • Half-life: 5h
  • Metabolism: Hepatic: via CYP3A4 and CYP2C9
  • Excretion: Biliary, renal

Mechanism of Action

  • Dual endothelin receptor antagonist, inhibits vasoconstriction --> vasodilation

Comments

See Also

References

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