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Zileuton

    Brands

    DEA Class; Rx

    Common Brand Names; Zyflo Filmtab, Zyflo, Zyflo CR

    • 5-Lipoxygenase Inhibitors

    Oral 5-lipoxygenase inhibitor; limits leukotriene production
    Used for add-on asthma maintenance therapy in adult and pediatric patients 12 years and older; off-label use for exercise-induced bronchospasm (EIB) in adults
    Due to a potential for hepatotoxicity, periodic monitoring of liver function tests is required

    Indicated for asthma maintenance treatment.

    For the treatment of aspirin-induced asthma.
    For exercise-induced bronchospasm prophylaxis.

    Hypersensitivity

    Liver disease, LFT’s ≥3x ULN

    • Headache (24.6%)
    • Abdominal pain (5%)
    • ALT elevation ≥3 times ULN (1.9-5%)
    • Asthenia (3.8%)
    • Dyspepsia (8.2%)
    • Diarrhea (5%)
    • Generalized pain (7.8%)
    • Nausea (5.5%)
    • Leukopenia (1-3%)
    • Myalgia (7%)
    • Weakness (4%)
    • Sinusitis (7%)
    • Pharyngolaryngeal pain (5%)

    Not indicated for use in acute bronchospasm

    History of liver disease, heavy alcohol use

    Behavioral changes and sleep disorders reported

    Not recommended for patients <12 years due to risk of hepatotoxicity

    There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to asthma medications during pregnancy

    The drug and metabolites are excreted in rat milk; it is not known if zileuton is excreted in human milk, nor are there data on effects of drug on breastfed infant or effects on maternal milk production

    Adults

    2,400 mg/day PO.

    Geriatric

    2,400 mg/day PO.

    Adolescents

    2,400 mg/day PO.

    Children

    12 years: 2,400 mg/day PO.
    Less than 12 years: Safety and efficacy have not been established; not recommended due to toxicity risk.

    Infants

    Safety and efficacy have not been established; not recommended due to toxicity risk.

    Zileuton

    tablet

    • 600mg

    tablet, extended release

    • 600mg