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bedaquiline (Rx)Brand and Other Names:Sirturo

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 100mg
more...

Multidrug Resistant Pulmonary Tuberculosis

Diarylquinoline antimycobacterial indicated as part of combination therapy in adults (≥18 years) with pulmonary multidrug resistant tuberculosis (MDR-TB)

Weeks 1-2: 400 mg PO qDay for 2 weeks, THEN

Weeks 3-24: 200 mg 3 times/week for 22 weeks

Take with a multidrug regimen consisting of at least 4 other drugs that the MDR-TB is likely susceptible for the entire 24 week duration

CDC provisional guidelines

  • May be used off-label on a case-by-case basis in children, HIV-infected persons, pregnant women, persons with extrapulmonary MDR TB, and patients with comorbid conditions on concomitant medications when an effective treatment regimen cannot otherwise be provided
  • May be used on a case-by-case basis for durations longer than 24 weeks when an effective treatment regimen cannot be provided otherwise
  • Reference: MMWR Recommendations and Reports. October 25, 2013/62(rr9);1-12

Dosing Considerations

Reserve for use when an effective treatment regimen cannot otherwise be provided

Not indicated to treat latent, extrapulmonary, or drug-sensitive tuberculosis

Use in combination with at least 4 other drugs to which the patient's MDR-TB isolate is likely to be susceptible

Treatment of nontuberculous mycobacteria infections have not been established

Administration

Take with food

Swallow whole with water

Missed dose

  • During first 2 weeks of treatment: Do not make up the missed dose but continue the usual dosing schedule
  • From week 3 onwards: If a 200 mg dose is missed, patients should take the missed dose as soon as possible, and then resume the 3 times/week regimen

Dosage Forms & Strengths

tablet

  • 100mg
more...

Multidrug Resistant Pulmonary Tuberculosis (Off-label)

<18 years: Safety and efficacy not established

Diarylquinoline antimycobacterial indicated as part of combination therapy in adults (≥18 years) with pulmonary multidrug resistant tuberculosis (MDR-TB)

CDC provisional guidelines suggest off-label use in children on a case-by-case basis

Weeks 1-2: 400 mg PO qDay for 2 weeks, THEN

Weeks 3-24: 200 mg 3 times/week for 22 weeks

Take with a multidrug regimen consisting of at least 4 other drugs that the MDR-TB is likely susceptible for the entire 24 week duration

Dosing Considerations

Reserve for use when an effective treatment regimen cannot otherwise be provided

Not indicated to treat latent, extrapulmonary, or drug-sensitive tuberculosis;

CDC provisional guidelines suggest off-label uses on a case-by-case basis in children, HIV-infected persons, pregnant women, persons with extrapulmonary MDR TB, and patients with comorbid conditions on concomitant medications when an effective treatment regimen cannot otherwise be provided

Use in combination with at least 4 other drugs to which the patient's MDR-TB isolate is likely to be susceptible

Treatment of nontuberculous mycobacteria infections have not been established

Administration

Take with food

Swallow whole with water

Missed dose

  • During first 2 weeks of treatment: Do not make up the missed dose but continue the usual dosing schedule
  • From week 3 onwards: If a 200 mg dose is missed, patients should take the missed dose as soon as possible, and then resume the 3 times/week regimen
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Interactions

Interaction Checker

bedaquiline 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%

            Nausea (38%)

            Arthralgia (32.9%)

            Headache (27.8%)

            1-10%

            Transaminases increased (8.9%)

            Blood amylase increased (2.5%)

            Frequency Not Defined

            QT prolongation

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            Warnings

            Black Box Warnings

            An increased risk of death was seen in the bedaquiline treatment group (9/79, 11.4%) compared to the placebo treatment group (2/81, 2.5%) in 1 clinical trial

            Only use when an effective treatment regimen cannot otherwise be provided

            QT prolongation can occur; coadministration with drugs that prolong the QT interval may cause additive QT prolongation

            Contraindications

            None

            Cautions

            Increased risk of death in bedaquiline treatment group (see Black Box Warnings) Metabolized by CYP3A4; avoid strong CYP3A4 inducers (eg, rifampin, rifapentine, rifabutin) that may reduce bedaquiline’s effect

            Coadministration with CYP3A4 inhibitors may increase systemic exposure and result in adverse effects; avoid coadministration with strong CYP3A4 inhibitors for more than 14 consecutive days, unless the benefit of treatment outweighs the risk

            Use bedaquiline with caution when co-administered with lopinavir/ritonavir and only if the benefit outweighs the risk

            There are no clinical data on the combined use of antiretroviral agents and bedaquiline in HIV/MDR-TB coinfected patients and only limited clinical data on the use of SIRTURO in HIV/MDR-TB coinfected patients not receiving antiretroviral therapy

            Administered by directly observed therapy (DOT)

            Hepatotoxicity

            • Hepatic-related adverse effects increased when bedaquiline added to multidrug regimen; avoid alcohol and other hepatotoxic drugs
            • Monitor symptoms (such as fatigue, anorexia, nausea, jaundice, dark urine, liver tenderness and hepatomegaly) and laboratory tests (ALT, AST, alkaline phosphatase, and bilirubin) at baseline, monthly while on treatment, and as needed; test for viral hepatitis and discontinue other hepatotoxic medications if evidence of new or worsening liver dysfunction occurs
            • Monitor ALT, AST, Alkaline phosphatase, and bilirubin at baseline, and monthly while on treatment
            • Discontinue if
              • aminotransferase increases are accompanied by total bilirubin elevation >2x ULN
              • aminotransferase elevations >8x ULN
              • aminotransferase elevations persist beyond 2 weeks

            QT prolongation

            • Also see Black Box Warnings
            • Prolongs QT interval; obtain ECG before initiating treatment and at least 2, 12, and 24 weeks after starting treatment
            • Obtain baseline serum levels for potassium, calcium, and magnesium and correct if abnormal; follow-up electrolyte monitoring if QT prolongation detected
            • Increased risk for QT prolongation with:
            • -coadministration with QT prolonging drugs (eg, fluoroquinolones, macrolides, clofazimine)
            • -history of Torsade de Pointes
            • -history of congenital long QT syndrome
            • -history of hypothyroidism and bradyarrhythmias
            • -history of uncompensated heart failure
            • -serum calcium, magnesium, or potassium levels below the lower limits of normal
            • Discontinue bedaquiline and other QT prolonging drugs if the following develops:
            • -clinically significant ventricular arrhythmia
            • -QTcF interval >500 ms
            • Monitor ECG to confirm QT interval returned to baseline
            • If syncope occurs, obtain ECG
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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: Unknown whether distributed in human breast milk Pharmacology

            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

            Diarylquinoline; inhibits mycobacterial adenosine 5'-triphosphate (ATP) synthase, an enzyme essential for the generation of energy in Mycobacterium tuberculosis

            Absorption

            Bioavailability: Increased 2-fold when taken with standard meal compared with fasted conditions

            Peak Plasma Concentration: 5 hr

            Distribution

            Protein Bound: >99.9%

            Vd: 164 L

            Metabolism

            Metabolized primarily by CYP3A4 to form N-monodesmethyl metabolite (M2) which is 4- to 6-times less active

            Elimination

            Half-life: 5.5 months (mean terminal half-life of bedaquiline and the M2 metabolite)

            Renal clearance: <0.001%

            Excretion: Mainly in feces

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            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.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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