Treprostinil
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| Trade names | Remodulin, Orenitram, Tyvaso |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| MedlinePlus | a600042 |
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| Routes of administration |
Subcutaneous, IV, inhalation, by mouth |
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| Pharmacokinetic data | |
| Bioavailability | ~100% |
| Metabolism | Substantially metabolized by the liver |
| Biological 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 |
| Chemical and physical data | |
| Formula | C23H34O5 |
| Molar mass | 390.52 g/mol |
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Treprostinil (marketed under the trade names Remodulin for infusion, Orenitram for oral, and Tyvaso for inhalation) is a vasodilator that is used for the treatment of pulmonary arterial hypertension. Treprostinil is a synthetic analog of prostacyclin (PGI2).
The inhaled form of treprostinil was approved by the FDA in July 2009 and is marketed as the trade name Tyvaso.
Treprostinil is indicated for the treatment of pulmonary arterial hypertension in patients with NYHA Class II-IV symptoms to diminish symptoms associated with exercise. It may be administered as a continuous subcutaneous infusion or continuous intravenous infusion; however, because of the risks associated with chronic indwelling central venous catheters, including serious blood stream infections, continuous intravenous infusion should be reserved for patients who are intolerant of the subcutaneous route, or in whom these risks are considered warranted. This medication is also available in inhaled and tablet forms.
In patients with pulmonary arterial hypertension requiring transition from epoprostenol sodium (Flolan), treprostinil is indicated to diminish the rate of clinical deterioration. The risks and benefits of each drug should be carefully considered prior to transition.
There is a report that Treprostinil has improved signs and symptoms in Malignant Atrophic Papulosis.
Common side effects:
Warnings:
The major effects of treprostinil are vasodilation of arteries in the lungs and body. Treprostinil also inhibits platelet aggregation and smooth muscle proliferation.
The pharmacokinetics of continuous subcutaneous treprostinil are linear over the dose range of 1.25 to 125 ng/kg/min (corresponding to plasma concentrations of about 15 pg/mL to 18,250 pg/m) and can be described by a two-compartment model. Dose proportionality at infusion rates greater than 125 ng/kg/min has not been studied.
Treprostinil is substantially metabolized by the liver, but the involved enzymes are not currently known. Five metabolites (HU1 through HU5) have been described thus far. Based on the results of in vitro human hepatic cytochrome P450 studies, Remodulin does not inhibit CYP-1A2, 2C9, 2C19, 2D6, 2E1, or 3A. Whether Remodulin induces these enzymes has not been studied.
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