zileuton (Rx)

Brand and Other Names:Zyflo Filmtab, Zyflo, more...Zyflo CR
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 600mg

tablet, extended release

  • 600mg
more...

Asthma

Extended release: 1200 mg PO twice daily, within 1 hour after morning and evening meals

Conventional: 600 mg PO four times daily

Monitor: LFTs

Contraindicated in hepatic dysfunction

Dosage Forms & Strengths

tablet

  • 600mg

tablet, extended release

  • 600mg
more...

Asthma

<12 years

  • Safety and efficacy not established
  • The FDA has not required pediatric studies in patients <12 years old due to the risk of hepatotoxicity; not recommeded for children younger than 12 years

>12 years

  • Extended Release: 1200 mg PO twice daily, within 1 hour after morning and evening meals
  • Conventional: 600 mg PO four times daily
  • Monitor: LFTs
  • Contraindicated in hepatic dysfunction
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Interactions

Interaction Checker

and zileuton

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (24.6%)

            1-10%

            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%)

            < 1%

            Hepatitis

            Behavioral changes

            Jaundice

            Liver failure

            Suicidality

            Suicide

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            Warnings

            Contraindications

            Hypersensitivity

            Liver disease, LFT's ≥3x ULN

            Cautions

            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

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            Pregnancy & Lactation

            Pregnancy Category: C

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Inhibitor of 5-lipoxygenase, which inhibits formation of LTB4, LTC4, LTD4, & LTE4

            Inhibition of leukotriene formation reduces eosinophil and neutrophil migration, neutrophil and monocyte aggregation, capillary permeability, and smooth muscle contraction

            Pharmacokinetics

            Half-Life: 2.5 hr

            Onset: 2-5 hr

            Peak Plasma Time: 1.7 hr

            Protein Bound: 93%

            Vd: 1.2 L/kg

            Metabolites: O-glucuronide conjugate & N-dehydroxylated metabolite

            Clearance: 7 mL/min/kg

            Excretion: Urine (95%); feces (2%)

            Enzymes inhibited: hepatic CYP1A2, CYP3A4, and CYP2C9

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            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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