TRACLEER Rx

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TRACLEER

Pulmonary hypertension
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Generic Name and Formulations:

Bosentan 62.5mg, 125mg; tabs.

Select therapeutic use:

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.

Adult:

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.

Children:

Not established.

Contraindications:

Concomitant cyclosporine A, glyburide. Pregnancy (Cat.X).

Warnings/Precautions:

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.

Interactions:

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.

Pharmacological Class:

Endothelin receptor antagonist.

Adverse Reactions:

Respiratory tract infection, headache, edema, chest pain, syncope, flushing, hypotension, sinusitis, arthralgia, elevated liver enzymes, palpitations, anemia; decreased sperm counts.

Note:

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.

REMS:

YES

How Supplied:

Tabs—30, 60

TRACLEER 62.5mg tablets (Qty:60)

appx. price $9959.00