Generic Name and Formulations:
Selexipag 200mcg, 400mcg, 600mcg, 800mcg, 1000mcg, 1200mcg, 1400mcg, 1600mcg; tabs.
Indications for UPTRAVI:
Pulmonary arterial hypertension (PAH) (WHO Group 1) in patients with WHO functional Class II–III symptoms, to delay disease progression and reduce the risk of hospitalization for PAH.
Swallow whole; may take with food to improve tolerability. Initially 200mcg twice daily; increase by 200mcg increments twice daily at weekly intervals to highest tolerated dose up to 1600mcg twice daily; reduce to previous dose if not tolerated. Moderate hepatic impairment (Child-Pugh class B): initially 200mcg once daily; increase in 200mcg increments once daily at weekly intervals as tolerated.
Concomitant strong CYP2C8 inhibitors (eg, gemfibrozil).
Discontinue if pulmonary veno-occlusive disease confirmed. Severe hepatic impairment (Child-Pugh class C): avoid. Pregnancy. Nursing mothers: not recommended.
Prostacyclin receptor agonist.
See Contraindications. May be potentiated by concomitant moderate CYP2C8 inhibitors (eg, teriflunomide, deferasirox); consider less frequent or reduced dosing. May be antagonized by concomitant CYP2C8 and UGT 1A3 or 2B7 inducers (eg, rifampin); increase up to twice the dose.
Headache, diarrhea, nausea, jaw pain, vomiting, pain in extremity, myalgia, flushing, arthralgia, rash, anemia, decreased appetite.
Tabs 200mcg—60, 140; 400mcg, 600mcg, 800mcg, 1000mcg, 1200mcg, 1400mcg, 1600mcg—60; Titration pack—1 (140 x 200mcg tabs) + (60 x 800mcg tabs)