bosentan (Rx)Brand and Other Names:Tracleer

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 62.5mg
  • 125mg
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Pulmonary Arterial Hypertension (PAH)

Indicated to improve exercise ability and decrease worsening of PAH; effectiveness shown in NYHA II-IV, idiopathic or heritable PAH, connective tissue diseases that result in PAH, and PAH associated with congenital heart disease with left-to-right shunts

<40 kg: Maintain dose at 62.5 mg PO twice daily with or without food

>40 kg: 62.5 mg PO twice daily for 4 weeks and then increased to maintenance dosage 125 mg PO twice daily

Discontinuation of treatment: Consider a reduction in dosage to 62.5 mg PO twice daily for 3-7 days

Dosage modifications

ALT/AST levels

  • >3 and <5 x ULN: Confirm test; if confirmed, reduce dose to 62.5 mg twice daily or interrupt treatment and monitor liver tests q2wk; if levels return to pretreatment values, continue or reintroduce treatment at starting dose
  • >5 and <8 x ULN: Confirm test; if confirmed, stop treatment and monitor liver tests at least q2wk; if levels return to pretreatment values, consider reintroduction of the treatment at reduced dose
  • >8 x ULN: Stop treatment; reintroduction should not be considered

Liver impairment

  • Mild: No dose adjustment required
  • Moderate or severe: Avoid use

Coadministration with strong CYP3A4 inhibitor (ie, cobicistat or ritonavir)

  • Have been receiving elvitegravir/cobicistat/emtricitabine/tenofovir or ritonavir for at least 10 days: Start bosentan at 62.5 mg qDay or every other day based upon individual tolerability
  • Have been receiving bosentan: Discontinue bosentan at least 36 hr prior to initiation of elvitegravir/cobicistat/emtricitabine/tenofovir or ritonavir; after at least 10 days, resume bosentan at 62.5 mg qDay or every other day based upon individual tolerability

Idiopathic Pulmonary Fibrosis (Orphan)

Orphan indication sponsor

  • Actelion Pharmaceuticals Ltd; Gewerbestrasse 16, CH-4123; Switzerland

Systemic Sclerosis (Orphan)

Reduction of the number (treatment) of new digital ulcers in patients with systemic sclerosis

Orphan indication sponsor

  • Actelion Pharmaceuticals Ltd; Gewerbestrasse 16, CH-4123; Switzerland

Administration

Healthcare professionals who prescribe therapy must enroll in the Tracleer REMS Program and must comply with the required monitoring to minimize the risks associated with therapy

Not recommended

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Interactions

Interaction Checker

bosentan and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Hgb decreased; >1 g/dL (57%)

            Inhibition of spermatogenesis (25%)

            Headache (16-22%)

            Nasopharyngitis (11%)

            Transaminses increased (12%)

            Respiratory tract infection (22%)

            Increased transaminases (12%)

            1-10%

            Edema, lower limb (5-8%)

            Flushing (7-9%)

            Hypotension (7%)

            Hepatic abnormalities (4%)

            Palpitations (4%)

            Anemia (3%)

            Dyspepsia (4%)

            Edema, general (4%)

            Fatigue (2%)

            Pruritus (4%)

            <1%

            Hyperbilirubinemia

            Vasculitis

            Jaundice

            Leukopenia

            Thrombocytopenia

            Leukocytoplastic

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            Warnings

            Black Box Warnings

            Hepatotoxicity

            • 3-fold ULN elevation of ALT and AST in ~11% of patients observed
            • Measure serum aminotransferase levels (and bilirubin if aminotransferase levels elevated) at baseline & then monthly
            • Rare cases of unexplained hepatic cirrhosis reported after prolonged therapy (>12 mth) Avoid in patients with elevated aminotransferase levels (>3 x ULN) at baseline because monitoring liver injury may be more difficult
            • Discontinue drug if liver aminotransferase elevations accompanied by clinical symptoms of liver injury (eg, nausea, vomiting, fever, abdominal pain, jaundice, unusual lethargy or fatigue) or increases in bilirubin >2 x ULN

            Pregnancy Contraindication

            • Likely to produce serious birth defects if used by pregnant women; this effect has been seen consistently when administered to animals
            • Negative pregnancy test result required before initiating & prevention of pregnancy required thereafter by the use of at least 2 reliable methods of contraception (unless tubal sterilization or Copper T 380A IUD or LNg 20 IUD inserted, in which case no other contraception required)
            • Obtain monthly pregnancy tests

            Restricted Distribution Program

            • Because of risks of liver injury and birth defects, available only through restricted distribution program called the Tracleer Access Program (TAP) by calling 1-866-228-3546; only prescribers and pharmacies registered with the program may prescribe and distribute bosentan
            • May be dispensed only to patients enrolled in and meet all conditions of TAP

            Contraindications

            Hypersensitivity

            Pregnancy

            Concomitant cyclosporine or glyburide use

            Cautions

            Avoid use with moderate-to-severe hepatic impairment

            Monitor LFTs; avoid use if ALT or AST >3 x ULN or bilirubin >2 x ULN (see Black Box Warnings and Dosage Modifications)

            Peripheral edema, veno-occlusive disease (discontinue if suspected), decreased sperm count, or decreased Hgb/Hct may occur

            Breastfeeding NOT recommended

            May interact with many medications

            Product requires special handling and disposal

            Reduces efficacy of hormonal contraceptives

            Avoid pregnancy; use 2 forms of birth control (hormonal contraceptives alone may not be effective)

            Increased risk of worsening HF related to fluid retention and death in HF patients.

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            Pregnancy & Lactation

            Pregnancy Category: X

            Lactation: Not known if excreted in breast milk; not recommended

            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.

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            Pharmacology

            Mechanism of Action

            Competitive antagonist of endothelin-1; blocks endothelin receptors on vascular endothelium and smooth muscle resulting in inhibition of vasoconstriction

            Absorption

            Bioavailability: 50%

            Peak plasma time: 3-5hr

            Duration: 24 hr

            Distribution

            Protein Bound: >98% (primarily to albumin)

            Vd: 18L

            Metabolism

            Metabolized by hepatic CYP2C9 and CYP3A4

            Metabolites: Ro 48-5033 (active metabolite), Ro 47-8634 (inactive metabolite)

            Enzymes induced: CYP2C9, CYP3A4

            Elimination

            Half-Life: 5-8 hr

            Excretion: Feces (predominantly); urine (minimal)

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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