Treprostinilum
Treprostinilum Uses, Dosage, Side Effects, Food Interaction and all others data.
Treprostinilum is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension.
Pulmonary arterial hypertension (PAH) is a disease in which blood pressure is abnormally high in the arteries between the heart and lungs. PAH is characterized by symptoms of shortness of breath during physical exertion. The condition can ultimately lead to heart failure. Treprostinilum is a potent oral antiplatelet agent. The major pharmacologic actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. Other studies have shown that treprostinil causes a dose-related negative inotropic and lusitropic effect. No major effects on cardiac conduction have been observed.
| Trade Name | Treprostinilum |
| Availability | Prescription only |
| Generic | Treprostinil |
| Treprostinil Other Names | Treprostinil, Tréprostinil, Treprostinilo, Treprostinilum |
| Related Drugs | sildenafil, tadalafil, Revatio, Adempas, Opsumit, ambrisentan |
| Type | |
| Formula | C23H34O5 |
| Weight | Average: 390.5131 Monoisotopic: 390.240624198 |
| Protein binding | Human plasma protein binding is approximately 91% in in vitro concentrations ranging from 330 to 10,000 µ/L. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Treprostinilum is a prostacyclin vasodilator for the treatment of pulmonary arterial hypertension to relieve exercise associated symptoms and to prevent clinical deterioration after stopping epoprostenol.
For use as a continuous subcutaneous infusion or intravenous infusion (for those not able to tolerate a subcutaneous infusion) for the treatment of pulmonary arterial hypertension in patients with NYHA Class II-IV symptoms to diminish symptoms associated with exercise.
Treprostinilum is also used to associated treatment for these conditions: NYHA Functional Class II-IV Pulmonary arterial hypertension, NYHA Functional Class III Pulmonary arterial hypertension, WHO functional class II-III Pulmonary arterial hypertension, Symptomatic pulmonary arterial hypertension (PAH)
How Treprostinilum works
The major pharmacological actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In addition to treprostinil's direct vasodilatory effects, it also inhibits inflammatory cytokine. As a synthetic analogue of prostacyclin, it binds to the prostacyclin receptor, which subsequently induces the aforementioned downstream effects.
Toxicity
Symptoms of overdose are extensions of its dose-limiting pharmacologic effects and include flushing, headache, hypotension, nausea, vomiting, and diarrhea. Most events were self-limiting and resolved with reduction or withholding of treprostinil.
Food Interaction
- Take with food. Taking treprostinil with food increases oral absorption.
Treprostinilum Drug Interaction
Moderate: riociguat, aspirin, omega-3 polyunsaturated fatty acids, desvenlafaxineMinor: tadalafilUnknown: amphetamine / dextroamphetamine, fluticasone / salmeterol, glimepiride, zolpidem, testosterone, umeclidinium / vilanterol, pancrelipase, ethanol, ambrisentan, pregabalin, esomeprazole, budesonide / formoterol, tramadol, cyanocobalamin, cholecalciferol
Treprostinilum Disease Interaction
Major: hepatic impairmentModerate: bleeding, diverticulosis, hypotension, liver dysfunction, pulmonary infections, renal dysfunction
Volume of Distribution
- 14 L/70 kg
Elimination Route
Relatively rapid and complete after subcutaneous infusion, with an absolute bioavailability approximately 100%. In patients with mild (n=4) or moderate (n=5) hepatic insufficiency and portopulmonary hypertension following a subcutaneous dose of 10 ng per kg of body weight per min for 150 mins the AUC 0-∞ was increased 3-fold and 5-fold respectively.
Half Life
Terminal elimination half-life is approximately 2 to 4 hours. Plasma half-life is 34 and 85 minutes for intravenous and subcutaneous infusion of the drug, respectively.
Innovators Monograph
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