Points of comparisonZafirlukast (Accolate)Zileuton (Zyflo)
Mechanism of actionBlocks the cysteinyl leukotrienes LTD4 and LTE4 at the CsyLT1 receptorSelectively and reversibly inhibits the 5-lipoxygenase pathway
Adverse effectsGenerally well toleratedGenerally well tolerated
Side effects include headache, infection, nausea, diarrheaSide effects include dyspepsia, headache, infections, asthma exacerbations
Elevated liver transaminase levels (usually transient; however, liver function tests should be performed monthly for the first three months of therapy and then every two to three months for the first year of treatment)
Drug interactionsInteracts with drugs metabolized by cytochrome P450 enzymes 3A4 (e.g., phenytoin [Dilantin], carbamazepine [Tegretol]) and 2C9 (e.g., cisapride [Propulsid], astemizole [Hismanal], dihydropyridine calcium channel blockers)May interact with drugs metabolized by cytochrome P450 enzymes 1A2, 3A4 and 2C9
Reported interactions with theophylline, warfarin and propranolol (Inderal)
Increases the effect of warfarin (Coumadin)
Plasma level decreased by erythromycin and theophylline
Plasma level raised by aspirin
ContraindicationsBreast feedingActive liver disease
Breast feeding
PrecautionsShould be used with caution in elderly patients and patients with hepatic disease
Use in pregnancyCategory BNot recommended
Dosage20 mg twice daily, taken one hour before or two hours after meals600 mg orally, taken four times daily with or without food
Cost*$56$83