Updated: 1/1/2022

Pulmonary Hypertension Drugs

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  • Snapshot
    • A 67-year-old man presents to the clinic with complaints of dyspnea and fatigue for 1 month. He reports that it is difficult to breathe when he walks for 5 minutes (compared to 30 minutes 2 months ago). His past medical history is significant for mitral stenosis secondary to rheumatic fever. A physical examination shows a loud P2 heart sound on auscultation.
  • Overview
    • Treatment of pulmonary hypertension (PH) usually begins with primary therapy that is directed at the underlying cause of PH
    • Treatment/medications directed at PH itself are detailed below
  • Endothelin Receptor Antagonists
    • Mechanism of action
      • competitively antagonizes endothelin-1 receptors, which are potent vasoconstrictors and smooth muscle mitogens
      • decreases pulmonary vascular resistance
      • examples
        • bosentan and macitentan
    • Clinical use
      • pulmonary hypertension
    • Adverse effects
      • hepatic toxicity
        • monitor LFTs while on medication
      • peripheral edema
      • teratogenic
  • Phosphodiesterase Type 5 (PDE5) Inhibitors
    • Mechanism of action
      • inhibits PDE5 which increases cyclic GMP, prolonging the vasodilatory effect of nitric oxide
      • examples
        • sildenafil and tadalafil
    • Clinical use
      • pulmonary hypertension
      • erectile dysfunction
    • Adverse effects
      • severe hypotension
      • headache
  • Prostacyclin Pathway Agonists
    • Mechanism of action
      • PGI2 (prostacyclin) agonist with direct vasodilatory effects on the pulmonary and systemic arterial vascular beds
      • inhibition of platelet aggregation
      • examples
        • epoprostenol, iloprost, treprostinil, and selexipag
    • Clinical use
      • pulmonary hypertension
    • Adverse effects
      • flushing
      • jaw pain
      • hypotension
      • pulmonary edema

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