Uses
Synthetic analog of Prostacyclin (P839060). Antihypertensive. Treprostinil, marketed under the trade name Remodulin is a medication used to treat pulmonary arterial hypertension (PAH).
Definition
ChEBI: Treprostinil is a carboxylic acid and a carbotricyclic compound. It has a role as a platelet aggregation inhibitor, a vasodilator agent, an antihypertensive agent, a cardiovascular drug, a vitamin K antagonist and a human blood serum metabolite.
Pharmacokinetics
Treprostinil is
rapidly absorbed from the subcutaneous site of infusion, with an almost 100% bioavailability and a mean half-life of 85
minutes (34 minutes for the IV infusion). The IV solution must be diluted with normal saline or sterile water before
starting the infusion. Unlike epoprostenol, treprostinil is stable at room temperature for up to 5 years, with vasodilation
action lasting from 4 to 6 hours, compared with the short, 2- to 3-minute action for epoprostenol. Because of its long
life in the body, it can be administered under the skin with a microinfusion subcutaneous infusion pump rather than into
the bloodstream and, thus, without hospitalization, as contrasted with the central IV infusion of epoprostenol.
Clinical Use
Treprostinil is a synthetic, stable form of prostacyclin for the treatment for advanced pulmonary
hypertension with NYHA class III or IV symptoms as well as for late-stage peripheral vascular disease (PVD). Its sodium
salt injectable form is administered either as a continuous subcutaneous infusion directly into the skin or, if the
subcutaneous infusion is not tolerated, as a continuous IV infusion without an implanted catheter.
Side effects
Side effects include jaw pain, headaches, nausea, diarrhea, flushing, and localized pain at the delivery site under the
skin. This pain has been reported as slight to severe irritation. Patients using the drug seem to ex-perience
improvement in their condition, including decreased fatigue, decreased shortness of breath, and decreased pulmonary
artery pressures, as well as overall improvement in quality of life.
