USMLE

Endothelin Receptor Antagonists (Bosentan)

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Respiratory Pharm
  1. Ipratropium vs Tiotropium
  2. 1st Generation Antihistamines
  3. 2nd-Generation Antihistamines
  4. Albuterol vs Salmeterol
  5. Fluticasone & Budesonide
  6. Montelukast & Zafirlukast
  7. Zileuton
  8. Omalizumab
  9. Cromolyn & Nedocromil
  10. Guaifenesin
  11. Endothelin Receptor Antagonists (Bosentan)
  12. Prostaglandin Analogs (Epoprostenol, Iloprost)
  13. Theophylline

Summary

Bosentan is an endothelin receptor antagonist which works to inhibit vasoconstriction. The resulting effect is vasodilation, especially in the pulmonary vessels.  This makes the drug useful for treating pulmonary hypertension. The most notable side effect of bosentan is hepatotoxicity.

Key Points

  • Bosentan
    • Mechanism
      • Endothelin Receptor Antagonist
        • Endothelin is an endogenous vasoconstrictor
        • Stimulates vasodilation → Decreased PVR
    • Clinical Use
      • Pulmonary Hypertension
        • probably most important fact here
    • Adverse Effects
      • Hepatoxicity
        • LFTs should be monitored