Dosing & Uses
Dosage Forms & Strengths
tablet
- 200mcg
- 400mcg
- 600mcg
- 800mcg
- 1000mcg
- 1200mcg
- 1400mcg
- 1600mcg
injection, lyophilized powder for reconstitution
- 1800mcg/vial
- Reconstituted concentration of each vial: 225 mcg/mL
Pulmonary Arterial Hypertension
Indicated for pulmonary arterial hypertension (PAH, WHO Group 1) to delay disease progression and reduce risk of hospitalization
Oral
- 200 mcg PO BID, initially
- Increase dose by 200 mcg BID, at weekly intervals (usually), to highest tolerated dose; not to exceed 1600 mcg BID
- If dose not tolerated, reduce to previous tolerated dose
-
PO to IV conversion
- Use in patients who are temporarily unable to take PO
- Current dose 200 mg PO BID: Administer 225 mg IV BID
- Current dose 400 mg PO BID: Administer 450 mg IV BID
- Current dose 600 mg PO BID: Administer 675 mg IV BID
- Current dose 800 mg PO BID: Administer 900 mg IV BID
- Current dose 1000 mg PO BID: Administer 1125 mg IV BID
- Current dose 1200 mg PO BID: Administer 1350 mg IV BID
- Current dose 1400 mg PO BID: Administer 1575 mg IV BID
- Current dose 1600 mg PO BID: Administer 1800 mg IV BID
Dosage Modifications
Renal impairment
- eGFR >15 mL/min/1.73 m2: No dosage adjustment required
- eGFR <15 mL/min/1.73 m2 or patients undergoing dialysis: No clinical experience
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment required
- Moderate (Child-Pugh B): Starting dose is 200 mcg qDay; increase by increments of 200 mcg/day at weekly intervals, as tolerated
- Severe (Child-Pugh C): Avoid use
Coadministration with moderate CYP2C8 inhibitors
- Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors (eg, clopidogrel, deferasirox, teriflunomide)
- Revert to selexipag BID dosing when moderated CYP2C8 inhibitor discontinued
Coadministration with CYP2C8 inducers
- Increase selexipag dose (up to 2-fold) if coadministered with rifampin
Dosage Considerations
Effectiveness was established in a long-term study in patients with PAH with WHO Functional Class II-III symptoms
Patients had idiopathic and heritable PAH (58%), PAH associated with connective-tissue disease (29%), or PAH associated with congenital heart disease with repaired shunts (10%)
Chronic Thromboembolic Pulmonary Hypertension (Orphan)
Orphan designation for chronic thromboembolic pulmonary hypertension
Orphan sponsor
- Janssen Research & Development LLC; 1820 Chapel Ave West, Suite 300; Cherry Hill, New Jersey 08002
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- gemfibrozil
gemfibrozil will increase the level or effect of selexipag by decreasing metabolism. Contraindicated. Coadministration of selexipag with strong CYP2C8 inhibitors doubled exposure to selexipag and increased exposure to the active metabolite by about 11-fold.
Serious - Use Alternative (3)
- darolutamide
darolutamide will increase the level or effect of selexipag by Other (see comment). Avoid or Use Alternate Drug. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).
- lasmiditan
lasmiditan increases levels of selexipag by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates.
- leniolisib
leniolisib will increase the level or effect of selexipag by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
Monitor Closely (67)
- abiraterone
abiraterone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- acalabrutinib
acalabrutinib increases effects of selexipag by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.
- apalutamide
apalutamide will decrease the level or effect of selexipag by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and may decrease systemic exposure of drugs that are BCRP substrates.
- cannabidiol
cannabidiol will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- capmatinib
capmatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- carbamazepine
carbamazepine will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- celecoxib
celecoxib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- clopidogrel
clopidogrel will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- cobicistat
cobicistat will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- colchicine
colchicine will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- cyclosporine
cyclosporine will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- dabrafenib
dabrafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- deferasirox
deferasirox will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- dexamethasone
dexamethasone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- dipyridamole
dipyridamole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- efavirenz
efavirenz will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- eltrombopag
eltrombopag will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- eluxadoline
eluxadoline will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- encorafenib
encorafenib will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.
- felodipine
felodipine will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- fosphenytoin
fosphenytoin will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- fostamatinib
fostamatinib will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of BCRP substrate drugs. Monitor for toxicities of BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.
- fostemsavir
fostemsavir will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits BCRP transporters. If possible, avoid coadministration or modify dose of BCRP substrate coadministered with fostemsavir.
- gefitinib
gefitinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- griseofulvin
griseofulvin will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- ifosfamide
ifosfamide will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- imatinib
imatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- irbesartan
irbesartan will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- ketoconazole
ketoconazole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- lapatinib
lapatinib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
lapatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors. - levoketoconazole
levoketoconazole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- losartan
losartan will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- mifepristone
mifepristone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- momelotinib
momelotinib increases toxicity of selexipag by plasma protein binding competition. Modify Therapy/Monitor Closely. Momelotinib (BCRP inhibitor) may increase exposure of BCRP substrates, which may increase the risk of BCRP substrate adverse reactions. Dose adjustment of other BCRP substrates may necessary.
- nilotinib
nilotinib will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- omaveloxolone
omaveloxolone will decrease the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Omaveloxolone may reduce systemic exposure of sensitive CYP2C8 substrates. Check prescribing information of substrate if dosage modification is needed.
- osimertinib
osimertinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- oteseconazole
oteseconazole will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- pantoprazole
pantoprazole will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- phenobarbital
phenobarbital will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- phenytoin
phenytoin will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- pioglitazone
pioglitazone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- ponatinib
ponatinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- primidone
primidone will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- quinine
quinine will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- rabeprazole
rabeprazole will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- regorafenib
regorafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- rifampin
rifampin will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Coadministration of selexipag with rifampin, an inducer of CYP2C8, UGT1A3, and 2B7 enzymes, decreased exposure to selexipag's active metabolite by 50%. Increase selexipag dose up to twice of the typical dose if coadministered with rifampin.
- rifapentine
rifapentine will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- rolapitant
rolapitant will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- rosiglitazone
rosiglitazone will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- safinamide
safinamide will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- secobarbital
secobarbital will decrease the level or effect of selexipag by increasing metabolism. Modify Therapy/Monitor Closely. Increase selexipag dose (up to 2-fold) if coadministered with strong CYP2C8 inducers.
- sofosbuvir/velpatasvir
sofosbuvir/velpatasvir will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- stiripentol
stiripentol will increase the level or effect of selexipag by Other (see comment). Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors. Stiripentol is also a BCRP transport inhibitor.
- sunitinib
sunitinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- tafamidis
tafamidis will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tafamidis meglumine
tafamidis meglumine will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tamoxifen
tamoxifen will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- teriflunomide
teriflunomide will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- trimethoprim
trimethoprim will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- vandetanib
vandetanib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- vemurafenib
vemurafenib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- voxilaprevir
voxilaprevir will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
Minor (2)
- lopinavir
lopinavir will increase the level or effect of selexipag by decreasing metabolism. Minor/Significance Unknown. Coadministration of selexipag with ritonavir may result in an increase in exposure to selexipag. Despite this pharmacokinetic change, this interaction is likely of little clinical significance.
- ritonavir
ritonavir will increase the level or effect of selexipag by decreasing metabolism. Minor/Significance Unknown. Coadministration of selexipag with ritonavir may result in an increase in exposure to selexipag. Despite this pharmacokinetic change, this interaction is likely of little clinical significance
Adverse Effects
>10%
Headache (65%)
Diarrhea (42%)
Jaw pain (26%)
Nausea (33%)
Vomiting (18%)
Pain in extremity (17%)
Myalgia (16%)
Flushing (12%)
Arthralgia (11%)
Rash (11%)
1-10%
Hemoglobin decreased below 10 g/dL (8.6%)
Anemia (8%)
Decreased appetite (6%)
Frequency Not Defined
TSH reduced (up to −0.3 MU/L from a baseline of 2.5 MU/L)
Vascular disorders: Symptomatic hypotension
Warnings
Contraindications
Hypersensitivity to the active substance or to any of the excipients
Concomitant use of strong CYP2C8 inhibitors (eg, gemfibrozil)
Cautions
If signs of pulmonary edema occur, consider the possibility of associated pulmonary veno-occlusive disease (PVOD); if PVOD is confirmed, discontinue selexipag
Drug interaction overview
- Contraindicated with strong CYP2C8 inhibitors; coadministration with strong CYP2C8 inhibitors may result in significant increased exposure to selexipag and its active metabolite
- Concomitant administration with an inducer of CYP2C8 and UGT 1A3 and 2B7 enzymes (rifampin) halved exposure to active metabolite; increase dose up to twice of the normal dose when coadministered with rifampin; reduce therapy dose when rifampin is stopped
- An increased selexipag dose (up to 2-fold) may be necessary if coadministered with strong CYP2C8 inducers
Pregnancy
Pregnancy
No adequate and well-controlled studies with selexipag exist in pregnant women
Animal studies
- Reproduction studies performed with selexipag showed no clinically relevant effects on embryofetal development and survival
- A slight reduction in maternal as well as in fetal body weight was observed when pregnant rats were administered selexipag during organogenesis at a dose producing an exposure ~47 times that in humans at the maximum recommended human dose
Lactation
Unknown if distributed in human breast milk
Selexipag or its metabolites were present in the milk of rats
Because many drugs are present in the human milk and because of the potential for serious adverse reactions in nursing infants, discontinue nursing or discontinue selexipag
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Selectively activates the prostacyclin receptor (ie, IP-receptor), one of 5 types of prostanoid receptors
Unlike prostacyclin analogs, selexipag is selective for the IP receptor over other prostanoid receptors (ie, EP1-4, DP, FP, TP)
Activating the IP receptor induces vasodilation and inhibits proliferation of vascular smooth muscle cells
Absorption
Peak plasma time: 1-3 hr; 3-4 hr (active metabolite)
Distribution
Protein bound: ~99% (albumin and alpha1-acid glycoprotein)
Metabolism
Undergoes enzymatic hydrolysis of the acylsulfonamide by hepatic carboxylesterase 1, to yield the active metabolite, which is ~37-fold as potent as selexipag
Elimination
Half-life: 0.8-2.5 hr; 6.2-13.5 hr (active metabolite)
Oral clearance: 35 L/hr
Excretion: 93% in feces; neither selexipag nor its metabolite were found in urine
Administration
IV Preparation
Reconstitution
- Remove vials from refrigerator and for ~30-60 min to reach room temperature (20-25ºC [68-77ºF])
- Protect vials from light at all times; ensure protective wrap around the label is covering vial
- Peel back light protective wrap on vial to inspect vial and then immediately close light protective wrap on the vial; contents should appear white-to-almost white broken cake or powder material
- Reconstitute vial contents using a polypropylene syringe with 8.6 mL of 0.9% NaCl; slowly inject stream directed toward the inside wall of vial to obtain concentration of 225 mcg/mL
- Gently invert vial and repeat until powder is completely dissolved; do NOT shake
- Inspect vial for discoloration by peeling back light protect wrap; solution is clear, colorless, and free from foreign material; discard if solution is discolored, cloudy, or contains visible particles
Dilution
- Must be diluted in glass containers only
- Withdraw 100 mL of 0.9% NaCl and transfer into an empty sterile glass container
- Calculate and withdraw required volume of reconstituted solution from vial using a single, appropriately sized polypropylene syringe; dilute into glass container containing 100 mL 0.9% NaCl to obtain desired final dose
- Mix diluted infusion solution by gentle inversion of the glass container 5 times; do NOT shake
- Always protect the diluted solution from light
- Assign a 4-hr expiration from the time of first vial puncture and wrap the glass container completely with light protective cover
- Visually inspect solution for particulate matter and discoloration prior to administration; diluted solution is clear and colorless; discard if particulate matter observed
IV Administration
Infuse over 80 minutes using an infusion set made of DEHP-free polyvinyl chloride, natural latex rubber-free, microbore tubing protected from light
Do not use a filter for administration
Once glass container is empty, continue infusion at the same rate with 0.9% NaCl to ensure that the entire dose has been administered
Oral Administration
Swallow tablet whole; do not split, crush, or chew
Tolerability may be improved when taken with food
Dose interruptions and discontinuations
- Missed dose: Take missed dose as soon as possible unless the next dose is within the next 6 hr
- Missed treatment for ≥3 days: Restart selexipag at a lower dose and then titrate to desired effect and tolerance
Storage
Tablet
- Store at 20-25ºC (68-77ºF); excursions permitted to 15-30°C (59-86°F)
- Keep out of reach of children
Unopened vials
- Refrigerate in the original carton at 2-8ºC (36-46ºF) until use to protect from light
Diluted solutions
- Store at room temperature (20-25ºC [68-77ºF]); must complete infusion within 4 hr from the first puncture of the vial stopper
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Uptravi oral - | 1,200 mcg tablet |  | |
| Uptravi oral - | 600 mcg tablet |  | |
| Uptravi oral - | 200 mcg tablet |  | |
| Uptravi oral - | 200 mcg (140)- 800 mcg (60) tablet |  | |
| Uptravi oral - | 1,400 mcg tablet |  | |
| Uptravi oral - | 1,000 mcg tablet |  | |
| Uptravi oral - | 800 mcg tablet |  | |
| Uptravi oral - | 400 mcg tablet |  | |
| Uptravi oral - | 1,600 mcg tablet |  |
Copyright © 2010 First DataBank, Inc.
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