Medically reviewed by Drugs.com. Last updated on Aug 17, 2020.
(se LEX i pag)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Uptravi: 200 mcg, 400 mcg, 600 mcg, 800 mcg, 1000 mcg, 1200 mcg, 1400 mcg, 1600 mcg
Tablet Therapy Pack, Oral:
Uptravi: 200 mcg (140s) and 800 mcg (60s) (200 ea)
Brand Names: U.S.
- Prostacyclin IP Receptor Agonist
Selexipag is a selective prostacyclin IP receptor agonist. Prostacyclin is produced in the endothelial cells and induces vasodilation; also inhibits platelet aggregation. Patients with pulmonary arterial hypertension appear to have a dysregulation in the prostacyclin metabolic pathways (Galie 2013).
Rapid (Kaufmann 2015)
Metabolism: Hepatic via CYP3A4, CYP2C8, UGT1A3 and UGT2B7; hydrolyzed by carboxylesterase1 to the active metabolite, ACT-333679, which is a major contributor to the activity (Kaufmann 2015); the active metabolite is then glucuronidated.
Feces (~93%); urine (12%; as inactive metabolites)
Time to Peak
Selexipag: 1 to 3 hours; Active metabolite: 3 to 4 hours; Delayed with food
Terminal: Selexipag: 0.8 to 2.5 hours; Active metabolite: 6.2 to 13.5 hours
~99%; to albumin and alpha-1 acid glycoprotein
Special Populations: Renal Function Impairment
A 40% to 70% increase in exposure to selexipag and its active metabolite was observed in severe renal impairment (estimated glomerular filtration rate ≥15 to <30 mL/minute/1.73 m2).
Special Populations: Hepatic Function Impairment
In mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment, exposure was 2- and 4-fold that seen in healthy subjects. Exposure to the active metabolite was doubled in moderate hepatic impairment.
Use: Labeled Indications
Pulmonary arterial hypertension: Treatment of pulmonary arterial hypertension (PAH) (WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH.
Concomitant use with strong CYP2C8 inhibitors (eg, gemfibrozil).
Canadian labeling: Additional contraindication (not in US labeling): Hypersensitivity to selexipag or any component of the formulation
Pulmonary arterial hypertension:
Note: A clinician with expertise in pulmonary arterial hypertension should be consulted for all management decisions (ACCP [Klinger 2019]).
Oral: Initial: 200 mcg twice daily; increase by 200 mcg twice daily, usually at weekly intervals, to the highest tolerated dose; maximum dose: 1,600 mcg twice daily. If a dose is not tolerated, reduce dose to previously tolerated dose.
Missed dose: If dose is missed, take dose as soon as possible unless the next dose is within the next 6 hours. If ≥3 days of treatment are missed, restart at a lower dose and then retitrate.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Refer to adult dosing.
Oral: Administer with or without food; tolerability may be improved when taken with food. Swallow tablets whole; do not split, crush, or chew.
Store at 20ºC to 25ºC (68ºF to 77ºF); excursions permitted to 15°C and 30°C (59°F and 86°F).
CYP2C8 Inhibitors (Moderate): May increase serum concentrations of the active metabolite(s) of Selexipag. Management: Reduce the selexipag dose to once daily when combined with moderate CYP2C8 inhibitors. Revert back to twice daily selexipag dosing upon stopping the moderate CYP2C8 inhibitor. Consider therapy modification
CYP2C8 Inhibitors (Strong): May increase serum concentrations of the active metabolite(s) of Selexipag. CYP2C8 Inhibitors (Strong) may increase the serum concentration of Selexipag. Avoid combination
Lumacaftor and Ivacaftor: May decrease the serum concentration of CYP2C8 Substrates (High Risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may increase the serum concentration of CYP2C8 Substrates (High Risk with Inhibitors or Inducers). Monitor therapy
RifAMPin: May decrease serum concentrations of the active metabolite(s) of Selexipag. Management: Increase the selexipag dose (up to 2-fold) when combined with rifampin. Monitor for decreased selexipag efficacy. Consider therapy modification
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Cardiovascular: Flushing (12%)
Central nervous system: Headache (65%)
Dermatologic: Skin rash (11%)
Gastrointestinal: Diarrhea (42%), nausea (33%), vomiting (18%)
Neuromuscular & skeletal: Jaw pain (26%), limb pain (17%), myalgia (16%), arthralgia (11%)
1% to 10%:
Endocrine & metabolic: Hyperthyroidism (1%)
Gastrointestinal: Decreased appetite (6%)
Hematologic & oncologic: Decreased hemoglobin (below 10 g/dL: 9%), anemia (8%)
<1%, postmarketing, and/or case reports: Symptomatic hypotension
Concerns related to adverse effects:
• Pulmonary edema: If signs/symptoms of pulmonary edema occur, consider the possibility of associated pulmonary veno-occlusive disease (PVOD). If PVOD is confirmed, discontinue treatment.
• Hepatic impairment: Use with caution in patients with moderate hepatic impairment (dosage modification is recommended); avoid use in patients with severe hepatic impairment (has not been studied).
Liver function tests. Monitor for signs of pulmonary edema and for improvements in pulmonary function, exercise tolerance, and quality of life.
Adverse events have not been observed in animal reproduction studies. Women with pulmonary arterial hypertension (PAH) are encouraged to avoid pregnancy (McLaughlin 2009).
What is this drug used for?
• It is used to treat high blood pressure in the lungs.
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Jaw pain
• Muscle pain
• Joint pain
• Painful extremities
• Lack of appetite
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
• Trouble breathing
• Severe loss of strength and energy
• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
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Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
More about selexipag
- Side Effects
- During Pregnancy
- Dosage Information
- Drug Interactions
- En Español
- 22 Reviews
- Drug class: agents for pulmonary hypertension
Other brands: Uptravi