Comparative Pharmacology
Head-to-head clinical analysis: ZYFLO versus ZYFLO CR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ZYFLO versus ZYFLO CR.
ZYFLO vs ZYFLO CR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Zyflo (zileuton) is a specific inhibitor of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. This reduces the synthesis of leukotrienes (LTA4, LTB4, LTC4, LTD4, LTE4), which are potent bronchoconstrictors and pro-inflammatory mediators.
Zileuton is a selective inhibitor of 5-lipoxygenase (5-LO), thereby inhibiting leukotriene biosynthesis, including leukotrienes LTB4, LTC4, LTD4, and LTE4, which are bronchoconstrictors and pro-inflammatory mediators.
600 mg orally four times daily.
Adults: 600 mg orally twice daily (total daily dose 1200 mg).
None Documented
None Documented
Terminal half-life is approximately 2.5 hours in healthy adults; clinical context: requires dosing 4 times daily due to short half-life.
Terminal elimination half-life is approximately 5.5 hours in healthy adults; may be prolonged in patients with hepatic impairment.
Renal (approximately 0.5% unchanged); biliary/fecal (approximately 75% as metabolites); the remainder is metabolized and eliminated via other routes.
Primarily hepatic metabolism; approximately 10% excreted unchanged in urine, 80% as metabolites in feces via biliary elimination.
Category C
Category C
Leukotriene Inhibitor
Leukotriene Inhibitor