Prostanoids Flashcards
1
Q
How are prostacyclin analogs delivered?
A
Continuous IV, subQ infusion, or via intermittent nebulizer
2
Q
What are the prostanoids commonly used?
A
EpoPROSTenol, trePROSTinil, iliPROST, selexipag
3
Q
MOA of prostanoids?
A
- mimcs the axns of endogenous prostacyclin –>
- promotes vasc relaxation
- suppresses growth of vasc sm m cells
- inhibits platelet aggregation
- Exerts these effects by binding to GPCR on cell membrane to generate cAMP
4
Q
Effects of prostanoids?
A
- ↓ PAR
- ↓ PAP
- ↑ exercise tolerance
- improves short-term survival
5
Q
PKs of epoprostenol?
A
- 1st approved, best studied
- very short half-life (~6 min) and must be given by continuous IV infusion w. a pump that can keep the drug cold
6
Q
Toxicities of epoprostenol?
A
- Serious: sepsis d/t chronic catheter; Life-threatenin problems if pump lines clog
- Common: NV, HA, flushing, jaw pain
7
Q
PKs of treprostinil?
A
- Initially approved for continuous subQ infusion but pain –> now often diluted 1:2 and administered w/ IV pump
- has longer half-life (~ 4 hrs) and doesn’t need to be cold
- QID inhalation form is now available
8
Q
Toxicities of treprostinil?
A
- Sepsis d/t chronic catheter
- Site pain w/ subQ infusion
- Jaw pain, nausea, diarrhea, edema
- Inhaled: cough, HA, throat irritation, w/ ↓ incidence of nausea, flushing, and dizziness
9
Q
PKs of Iloprost?
A
- administered byb inhalation 6-9 times per day
10
Q
Toxicities of iloprost?
A
- fainting d/t hypotension (esp if SBP < 85 mmHg)
- cough, HA, flushing, jaw pain
11
Q
PKs of selexipag?
A
- Administered PA, BID
- Tablets are $225 each or $350 for higher doses
12
Q
Toxicities of selexipag?
A
- HA, flushing, NVD, jaw, limb, & muscle pain, skin rash
