Drugs for Pulmonary Hypertension and DVT/PE (Wolff) Flashcards
What are the 5 drug classes used to treat Pulmonary Hypertension? (P/EA/PI/GCS/C)
prostanoids, endothelin antagonists, PDE 5 inhibitors, Guanylate cyclase sensitizers, CCBs
What are the 4 Prostanoids used for Pulmonary Hypertension? (E/T/I/S)
epoprostenol
treprostinil
iloprost
selexipag
What are the 3 Endothelin antagonists used for Pulmonary Hypertension? (B/A/M)
bosentan
ambrisentan
macicentan
What are the 2 PDE 5 inhibitors (S/T) and what is the 1 guanylate cyclase sensitizer (R) used for Pulmonary Hypertension?
PDE 5 –> sildenafil and tadalafil
GCS –> riociguat
What is a known genetic mutation that is linked to PAH and what are two drugs that can cause PAH? (Fen/Phen)
Genetics: BMPR2 (bone morphogenic protein receptor 2)
- seen in < 25% of idiopathic PAH
Drugs: fenfluramine/phentermine
- weight loss pills
What is the difference between these WHO FC for PAH:
Class 1
Class 2
Class 3
Class 4
- pulmonary HTN without resulting limitation of physical activity
- pulmonary HTN with SLIGHT limitation of physical activity; ordinary activity causes symptoms
- pulmonary HTN with MARKED limitation of physical activity; less than ordinary activity causes symptoms; still comfortable at rest
- pulmonary HTN with INABILITY to carry out physical activity without symptoms; manifest signs of RIGHT HEART FAILURE
What is the Vasopressor Test and what are positive findings?
- recommended that Group 1 PAH undergo vasopressor testing; administration of short-acting vasodilators
(+) = PAP dec. > 10 mmHg, MPAP < 40 mmHg, or CO is unchanged or increased
- see more response from idiopathic, familial, or anorexigen-induced PAH
50% of these patients benefit from treatment with CALCIUM CHANNEL BLOCKERS - nifedipine, diltiazem, amlodipine
Epoprostenol
What is its MOA, what is it used for, how is it administered, and what is its major serious adverse effect?
MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH
- administered as continuous IV due to 6 minute half-life; used with pump that can keep the drug COLD
AE: sepsis due to chronic catheter
Treprostinil
What is its MOA, what is it used for, how is it administered, and what is its major adverse effect?
MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH
- administered with pump IV in dilution 1:2 and DOESN’T require refrigeration; has 4 hour half-life
- used to be SubQ but was too painful
AE: sepsis due to chronic catheter
Iloprost
What is its MOA, what is it used for, how is it administered, and what is its major adverse effect?
MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH
- administered by INHALATION 6-9x day
AE: fainting due to hypotension (especially if SBP < 85 mmHg)
Selexipag
What is its MOA, what is it used for, and how is it administered?
Who benefits from this medication?
MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH
- administered ORALLY twice daily, but is EXPENSIVE
kids with PAH and/or their caregivers often refuse central line for IV, so this is a good alternative
Bosentan
What is its MOA, what is it used for, how is it administered, and what are its two serious adverse effects?
What are two drug interactions this drug has?
MOA: nonspecific ETa and ETb endothelin receptor blocker used for PAH
- administered ORALLY
AE: hepatotoxicity and teratogenesis
DI: accelerates metabolism of WARFARIN and ORAL CONTRACEPTIVES
- all patients MUST use 2 forms of birth control
Ambrisentan
What is its MOA, what is it used for, how is it administered, what is its serious adverse effect?
What are its drug interactions?
MOA: selective ETa receptor blocker used for PAH
- administered ORALLY
AE: teratogenesis (does NOT DAMAGE LIVER)
DI: does NOT accelerate Warfarin or oral contraceptive metabolism, but pts should STILL USE 2 forms of contraception
Macicentan
What is it and what is its half-life?
- non-selective Endothelin Antagonist
- half-life of 18 hrs allows for one/day dosing
Sildenafil
What is its MOA, what is it used for, how is it administered, and what are its 3 most common complications (H/F/D)?
What is Tadalafil?
MOA: selectively blocks phosphodiesterase Type 5, an enzyme that breaks down cGMP, and is used to treat PAH
- administered ORALLY with a 4 hr half-life
AE: headache, flushing, dyspepsia
- mild hypotension when used alone
- inc. hypotension with alpha-blockers/nitrates
Tadalafil = LONGER half-life than Sildenafil