Classes
DEA Class; Rx
Common Brand Names; Zyflo Filmtab, Zyflo, Zyflo CR
- 5-Lipoxygenase Inhibitors
Description
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
Indications
Indicated for asthma maintenance treatment.
Contraindications
Hypersensitivity
Liver disease, LFT’s ≥3x ULN
Adverse Effects
- 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%)
Warnings
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
Pregnancy and Lactation
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
Maximum Dosage
2,400 mg/day PO.
2,400 mg/day PO.
2,400 mg/day PO.
12 years: 2,400 mg/day PO.
Less than 12 years: Safety and efficacy have not been established; not recommended due to toxicity risk.
Safety and efficacy have not been established; not recommended due to toxicity risk.
How supplied
Zileuton
tablet
- 600mg
tablet, extended release
- 600mg
