Pulmonary HTN Pharm

Question 1

Epoprostenol

Answer 1

a. MOA - mimics prostacyclin –> vascular relaxation, surpasses growth of vascular sm, inhibits platelet aggregation
b. Clinical use - PAH
c. PK - short t1/2 (6 min); given by continuous IV
d. AE - sepsis, N/V, jaw pain, HA, flushing

Question 2

Treprostinil

Answer 2

a. MOA - mimics prostacyclin –> vascular relaxation, surpasses growth of vascular sm, inhibits platelet aggregation
b. Clinical use - PAH
c. PK - subQ (pain!), mainly IV (t1/2 4 hours), no fridge, inhalation form available qid
d. AE - sepsis, N, jaw pain, diarrhea, edema

Question 3

Why is sepsis a risk in certain prostanoids? which ones?

Answer 3

a. chronic catheritization

b. epoporstenol, treprostinil

Question 4

Iloprost

Answer 4

a. MOA - mimics prostacyclin –> vascular relaxation, surpasses growth of vascular sm, inhibits platelet aggregation
b. Clinical use - PAH
c. PK - inhalation 6-9 times per day
d. AE - fainting, cough, HA, flushing, jaw pain

Question 5

Selexipag

Answer 5

a. MOA - mimics prostacyclin –> vascular relaxation, surpasses growth of vascular sm, inhibits platelet aggregation
b. Clinical use - PAH
c. PK - orally, BID
d. AE - HA, flushing, diarrhea, N/V, jaw/limb/muscle pain, skin rash

Question 6

Bosentan

Answer 6

a. MOA - nonspecifically blocks Eta and ETb endothelia Rs
b. Clinical use - PAH
c. PK - oral
d. AE - hepatotoxicity, teratogenesis, anemia, reduced sperm production,
e. Drug interactions - accelerates metabolism of warfarin, oral contraceptives

Question 7

Ambrisentan

Answer 7

a. MOA - specifically blocks Eta Rs
b. Clinical use - PAH
c. PK - oral
d. AE - teratogenesis, anemia, reduced sperm production,

Question 8

Macitentan

Answer 8

a. MOA - nonselective agent

b. 18 hr half life

Question 9

Sildenafil

Answer 9

a. MOA - PDE 5 inhibitor
b. Clinical use - PAH
c. PK - oral
d. AE - HA, flushing, dyspepsia; visual disturbances, mild hypotension, priapism

*tadalafil works the same, but with a longer t1/2

Question 10

Riociguat

Answer 10

a. MOA - sensitizes sGC to endogenous NO by stabilizing NO-sGC binding; also directly stimulates sGC; also increased generation of cGMP
b. Clinical Use - PAH
c. PK - oral
d. AE - hypotension, HA, dizziness, dyspepsia; fetal harm

Question 11

What weight loss pills can cause PAH?

Answer 11

fenfluramine and phentermine