Prostacyclin
Chemical
A prostaglandin produced by pulmonary endothelium with powerful VD & anti-platelet aggregation effects
Use
Pulmonary VD
Presentation
Injection powder for solution
MoA
- Prostacyclin bunds to prostacyclin receptor
- Activates AC
- ↑cAMP
- ↓MLKC activity & ↓Ca2+ availability
- VD → Also → potent inhibition platelet aggregation & smooth m. proliferation
- Pulsatile flow & local shear stress are important stimuli for endogenous prostacyclin release
cAMP
- Inhibits platelet aggregation
- Counteracts ↑Ca2+ from thromboxane A2 binding that would lead to platelet activation & coagulation
PD
CVS
- Direct pulmonary & systemic VD
- ↓afterL = ↑CO
- Reflex ↑HR
- Inhibition of platelet aggregation
PK
A
N/A
D
357mL/kg
M
Spout degradation & enzyme metabolism; 2 metabolites have activity, additional metabolites formed don’t
E
Urinary excretion
t ½ 6 mins
Adverse Effects
- Bleeding
- Headache
- Flushing
- Nausea
- ↓BP
- Worsens V/Q mismatch