Generic Name and Formulations:
Bosentan 62.5mg, 125mg; tabs.
Indications for TRACLEER:
Pulmonary arterial hypertension (PAH) (WHO Group I) in patients with WHO Class II–IV symptoms to improve exercise ability and decrease rate of clinical worsening.
Must register patient in the Tracleer REMS Program (see full labeling for restrictions and stipulations on use). Take in the AM and PM. <40kg: 62.5mg twice daily. >40kg: Initially 62.5mg twice daily for 4 weeks, then 125mg twice daily. Dose adjustments for developing ALT/AST elevations (confirm with another test): ALT/AST >3 and ≤5xULN: reduce daily dose to 62.5mg twice daily; if levels return to pretreatment values, continue or reintoduce treatment as appropriate. ALT/AST >5 and ≤8xULN: stop treatment and monitor at least every 2 weeks; if levels return to pretreament values, consider reintroduction. ALT/AST >8xULN: stop treatment, do not reintroduce. Concomitant ritonavir (for at least 10 days): start bosentan at 62.5mg once daily or every other day based on tolerability. Discontinue bosentan at least 36 hours before starting ritonavir.
Concomitant cyclosporine A, glyburide. Pregnancy (Cat.X).
Moderate or severe hepatic impairment or ALT/AST >3xULN at baseline: not recommended. Monitor ALT/AST levels prior to initiating therapy and then monthly; discontinue if elevations are accompanied by clinical symptoms of hepatotoxicity or increases in bilirubin ≥2xULN. Counsel patient about need for contraception; obtain (–) pregnancy test prior to initiation of drug and monthly thereafter; use 2 effective methods of contraception (see full labeling). Monitor hemoglobin and hematocrit at 1 and 3 months, then every 3 months thereafter. Monitor for significant fluid retention and pulmonary edema; discontinue if pulmonary veno-occlusive disease develops. Avoid abrupt cessation. Nursing mothers: not recommended.
See Contraindications. Potentiated by CYP2C9 (eg, fluconazole amiodarone) or strong or moderate CYP3A inhibitors (eg, ketoconazole, itraconazole, amprenavir, erythromycin, diltiazem); concomitant CYP2C9 inhibitor/moderate or strong CYP3A inhibitor combinations: not recommended. Potentiated by ritonavir. Rifampin alters bosentan levels (monitor hepatic function weekly for 4 weeks, followed by normal monitoring). Caution with tacrolimus. Antagonizes CYP2C9 or CYP3A substrates (eg, simvastatin). May interfere with hormonal contraceptives; use additional forms of contraception. May antagonize warfarin.
Endothelin receptor antagonist.
Respiratory tract infection, headache, edema, chest pain, syncope, flushing, hypotension, sinusitis, arthralgia, elevated liver enzymes, palpitations, anemia; decreased sperm counts.
Only prescribers and pharmacies registered with Tracleer REMS Program may prescribe Tracleer. Patients must be enrolled and meet all conditions of Tracleer REMS Program. To register call (866) 228-3546.
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