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]
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| Trade names | Remodulin, Orenitram, Tyvaso, others |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Subcutaneous, intravenous, inhalation, by mouth |
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| Bioavailability | ~100% |
| Metabolism | Substantially metabolized by the liver |
| Elimination half-life | 4 hours |
| Excretion | Urine (79% of administered dose is excreted as 4% unchanged drug and 64% as identified metabolites); feces (13%) |
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| ECHA InfoCard | 100.236.149 |
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| Formula | C23H34O5 |
| Molar mass | 390.520 g·mol−1 |
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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.
