Epoprostenol is a vasodilator and platelet aggregation inhibitor used for the management of primary pulmonary hypertension and pulmonary hypertension in patients with heart failure. A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation.
- Mechanism
- Curator reviewed
Prostaglandins are present in most body tissues and fluids and mediate many biological functions. Epoprostenol (PGI2) is a member of the family of prostaglandins that is derived from arachidonic acid. The major pharmacological actions of epoprostenol is ultimately inhibition of platelet aggregation. Prostacycline (PGI2) from endothelial cells activate G protein-coupled receptors on platelets and endothelial cells. This activation causes adenylate cyclase to produce cyclic AMP which inhibits further platelet activation and activates protein kinase A. Cyclic AMP also prevents coagulation by preventing an increase in intracellular calcium from thromboxane A2 binding. PKA then continues the cascade by phosphorylating and inhibiting myosin light-chain kinase which leads to smooth muscle relaxation and vasodilation. Notably, PGI2 and TXA2 work as physiological antagonists.
- Primary indication
- For the long-term intravenous treatment of primary pulmonary hypertension and pulmonary hypertension associated with the scleroderma spectrum of disease in NYHA Class III and Class IV patients who do not respond adequately to conventional therapy.Curator reviewed · 2 structured indications
- Formula / weight
- C20H32O5 · 352.4651 g/mol (avg)
- First approval
- Canada, 2001 · United States, 1995
- Also known as
- Prostacyclin · Prostaglandin I2 · Prostaglandin X · Vasocyclin
- Code names
- ACT-385781A · U-53,217
- Brand names
Resolves to
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Which drugs share a target with Epoprostenol, and which of those have an active Phase 3 trial?
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