Pulm HTN Drugs

Question 1

epoprostenol

Answer 1

• mimics the actions of endogenous prostacyclins, by activating G-PCRs to generate cAMP
• lowers pulmonary artery resistance, decreased pressure
• must be given continuous IV infusion d/t short t1/2
• risk of sepsis, n/v, flushing

Question 2

treprostinil

Answer 2

• mimics the actions of endogenous prostacyclins, by activating G-PCRs to generate cAMP
• lowers pulmonary artery resistance, decreased pressure
• longer t1/2
• risk of sepsis, site pain w/ subQ, jaw pain, cough

Question 3

iloprost

Answer 3

• mimics the actions of endogenous prostacyclins, by activating G-PCRs to generate cAMP
• lowers pulmonary artery resistance, decreased pressure
• administered by inhalation 6-9x/day
• risk of fainting, cough, headache, flushing

Question 4

selexipag

Answer 4

• mimics the actions of endogenous prostacyclins, by activating G-PCRs to generate cAMP
• lowers pulmonary artery resistance, decreased pressure
• administered orally BID
• risk of headache, flushing, jaw pain

Question 5

sildenafil

Answer 5

• selectively blocks PDE type V to prevent the breakdown of cGMP
• causes smooth muscle relaxation, improves exercise tolerance, and slows symptom progression in PAH
• administered orally with t1/2 of 4hr
• risk of headache, flushing, priapism, visual disturbances, hypotension

Question 6

tadalafil

Answer 6

• selectively blocks PDE type V to prevent the breakdown of cGMP
• causes smooth muscle relaxation, improves exercise tolerance, and slows symptom progression in PAH
• administered orally with longer t1/2
• risk of headache, flushing, priapism, visual disturbances, hypotension

Question 7

bosentan

Answer 7

• nonspecifically blocks ETa and ETb endothelin receptors
• improves exercise tolerance and slows symptom progression in PAH
• administered orally
• risk of hepatotoxicity, teratogenesis
• increases metabolism of warfarin and oral contraceptives (must use 2 forms of birth control!!)

Question 8

ambrisentan

Answer 8

• selectively blocks ETa endothelin receptor
• improves exercise tolerance and slows symptom progression in PAH
• administered orally
• risk of teratogenesis, peripheral edema, anemia, and reduced sperm
• does not accelerate metabolism of warfarin or oral contraceptives, but pt must still use 2 forms of birth control!!

Question 9

macicentan

Answer 9

• nonspecifically blocks ETa and ETb endothelin receptors
• improves exercise tolerance and slows symptom progression in PAH
• administered orally once daily because of long t1/2 (18h)
• risk teratogenesis
• increases metabolism of warfarin and oral contraceptives (must use 2 forms of birth control!!)

Question 10

riociguat

Answer 10

• stabilizes guanylate cyclase and NO binding, leading to increased cGMP and increased vasodilation
• improves exercise tolerance and slows symptom progression in PAH
• administered orally and has t1/2 of 12 hrs
• risk of hypotension, fetal harm, headache, dizziness