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
  1. VD → Also → potent inhibition platelet aggregation & smooth m. proliferation
  • Pulsatile flow & local shear stress are important stimuli for endogenous prostacyclin release

cAMP

  1. 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