Pulmonary Hypertension Drugs

  1. What determines whether a patient can be on calcium channel blockers to treat pulmonary hypertension?
    If he/she responds to acute vasoreactive test
  2. What is vasoreactive testing?
    Helps identify patients that may benefit from CCB
  3. Name 3 CCB agents:
    • Nifedipine
    • Amlodipine
    • Diltiazem
  4. What is the mechanism of action for calcium channel blocker?
    decrease influx of Ca2+ L type
  5. What is the therapeutic indication for CCB?
    Pulmonary hypertension in vasoreactive patients
  6. What is the route of administration for CCB?
    Oral
  7. What are adverse effects for CCB
    • Hypotension
    • Peripheral edema
  8. What is a contraindication for CCB?
    Significant right heart failure
  9. What are treatment options when patient does not respond to vasoreactive test?
    • Endothelin receptor antagonist
    • PDE 5 inhibitor
    • Prostacyclin analog
  10. What is ET-1 recetpr?
    A potent vasoconstrictor
  11. Is bosentan a selecteive blocker of ET-1 receptors?
    No, nonselevtive
  12. Which receptor is Ambrisentan selective for?
    ETa
  13. True/False: Endothelin-1 can bind onto ETb on endothelial cell and would lead to release of NO and resulting in vascular smooth muscle cell relaxation
    True
  14. What is the effect of Endothelin-1 binding to ETa and ETb receptors on smooth muscle cell?
    Smooth muscle cell contraction
  15. What is the effect of endothelin-1 binding to ETb receptor on endothelial cell?
    Ultimately lead to smooth muscle cell relaxation
  16. Which ET-1 receptor antagonist is most efficacious and safe?
    Macitentan
  17. What is the therapeutic use for ET-1 receptor antagonist?
    Pulmonary hypertension
  18. What is the route of administration for ET-1 receptor antagonist?
    Oral
  19. What other cellular component might ET-1 receptor antagonist have an effect on?
    Induce CYP3A4 and CYP2CP- could metabolize other drugs sooner
  20. What are adverse effects of ET-1 receptor antagonist
    • Peripheral edema
    • Hepatotoxicity
  21. What is a required test that patients on ET-1 receptor antagonists must do on a monthly basis?
    Liver function test
  22. What is a contraindication for ET-1 receptor antagonist?
    Pregnancy
  23. What are 2 agents of PDE5 inhibitor?
    • Sildenafil
    • Tadalafil
  24. What is the biochemical effect of PDE5 inhibitor use?
    Would degrade PDE 5 (PDE 5 degrades cGMP; cGMP allows for smooth muscle relaxation), which would ultimately lead to smooth muscle cell relaxation
  25. What is the route of administration for Sildenafil?
    • Powder for suspension
    • Oral
    • Iv
  26. What are adverse effects for Sildenafil?
    • Flushing
    • Headache
  27. What is a contraindication for Sildenafil?
    Nitrate use – otherwise could lead to hypotension
  28. What is the mechanism of action for riociguat?
    Stimulate soluble guanylate cyclase
  29. What is the route of administration of riociguat?
    Oral
  30. What are adverse effects of riociguat?
    • Embryo-fetal toxicity
    • Hypotension
    • Bleeding
  31. What are contraindications for riociguat?
    • Pregnancy
    • Nitrates
    • PDE inhibitors
  32. What is the mechanism of action for prostacyclin analogs?
    Bind prostacyclin receptor  enhance adenyl cyclase  decrease intracellular Ca2+ -> vascular relaxation
  33. What are 3 agents of prostacyclin analogs?
    • Epoprostenol
    • Iloprost
    • Treprostinil
  34. What is the route of administration for epoproostenol?
    IV
  35. What is the route of administration for trepostinil?
    IV, SQ, inhalation, oral
  36. What is the route of administration for iloprost?
    Inhalation
  37. What are adverse effects for IV prostacyclin analogs?
    • Flushing
    • Headache
    • Diarrhea
    • Infusion site pain (esp trepostinil)
  38. What are adverse effects for inhaled prostacyclin analogs?
    • Flushing
    • Jaw pain
  39. What are some IV prostacyclin analogs?
    • Epoprostenol
    • Trepostinil
  40. What are inhaled prostacyclin analog?
    • Iloprost
    • trepostinil
  41. What is an oral prostacyclin analog?
    Trepostinil
  42. What is a SQ prostacyclin analog?
    Trepostinil
Author
lykthrnn
ID
345359
Card Set
Pulmonary Hypertension Drugs
Description
Pulmonary Midterm
Updated