Updated: 4/29/2019

Pulmonary Hypertension Drugs

Review Topic
  • 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.
  • 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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