Treprostinil

Pregnancy
categoryRoutes of
administrationSubcutaneous, intravenous, inhalation, by mouthATC codeLegal statusLegal status Pharmacokinetic dataBioavailability~100%MetabolismSubstantially metabolized by the liverElimination half-life4 hoursExcretionUrine (79% of administered dose is excreted as 4% unchanged drug and 64% as identified metabolites); feces (13%)IdentifiersCAS NumberPubChem CIDIUPHAR/BPSDrugBankChemSpiderUNIIKEGGChEBIChEMBLECHA InfoCard100.236.149 Chemical and physical dataFormulaC₂₃H₃₄O₅Molar mass390.520 g·mol^−1 NY (what is this?)  (verify)

Treprostinil, sold under the brand names Remodulin for infusion, Orenitram for oral, and Tyvaso for inhalation, is a vasodilator that is used for the treatment of pulmonary arterial hypertension.^[6]

Treprostinil was approved for use in the United States in May 2002.^[7]

Medical uses

Treprostinil is indicated for the treatment of pulmonary arterial hypertension in people with NYHA Class II-IV symptoms to diminish symptoms associated with exercise.^[1]

Adverse effects

• Since treprostinil is a vasodilator, its antihypertensive effect may be compounded by other medications that affect the blood pressure, including calcium channel blockers, diuretics, and other vasodilating agents.^[8]
• Because of treprostinil's inhibiting effect on platelet aggregation, there is an increased risk of bleeding, especially among patients who are also taking anticoagulants.^[8]
• It is not known whether treprostinil is excreted in breast milk. Caution is advised when administering this medication to nursing women.
• Caution is advised when administering treprostinil to patients who have impaired kidney or liver function.^[8]

Common side effects depending on route of administration:

• 85% of patients report pain or other reaction at the infusion site.^[8]

Administration

For infusion

Treprostinil may be administered as a continuous subcutaneous infusion or continuous intravenous infusion.^[1]

Inhaled form

The inhaled form of treprostinil was approved by the FDA in July 2009, and is sold under the brand name Tyvaso.^[3][4]

Oral form

The oral form of treprostinil was approved by the FDA in December 2013, and is sold under the brand name Orenitram.^[2]

History

During the 1960s a UK research team, headed by Professor John Vane began to explore the role of prostaglandins in anaphylaxis and respiratory diseases. Working with a team from the Royal College of Surgeons, Vane discovered that aspirin and other oral anti-inflammatory drugs worked by inhibiting the synthesis of prostaglandins. This finding opened the door to a broader understanding of the role of prostaglandins in the body.

Vane and a team from the Wellcome Foundation had identified a lipid mediator they called “PG-X,” which inhibited platelet aggregation. PG-X, which later would become known as prostacyclin, was 30 times more potent than any other known anti-aggregatory agent.^{[citation needed]}

By 1976, Vane and fellow researcher Salvador Moncada published the first paper on prostacyclin, in the scientific journal Nature.^[9]

Treprostinil (Remodulin) was approved for use in the United States in May 2002,^[1][7] and again in July 2018.^[10] Tyvaso, the inhaled form of treprostinil, was approved for use in the United States in July 2009.^[11] Orenitram was approved in December 2013.^[12]

Treprostinil (Trepulmix) was approved for use in the European Union in April 2020.^[5]

Research

Treprostinil therapy may be effective in treating Degos disease.^[13]

References

Further reading

• Narine L, Hague LK, Walker JH, Vicente C, Schilz R, Desjardins O, et al. (December 2005). "Cost-minimization analysis of treprostinil vs. epoprostenol as an alternate to oral therapy non-responders for the treatment of pulmonary arterial hypertension". Current Medical Research and Opinion. 21 (12): 2007–2016. doi:10.1185/030079905X75104. PMID 16368052. S2CID 13162585.{{cite journal}}: CS1 maint: overridden setting (link)