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Zileuton is a weak inhibitor of CYP1A2 [4] and thus has three clinically important drug interactions, which include increasing theophylline , and propranolol levels. It has been shown to lower theophylline clearance significantly, doubling the AUC and prolonging half-life by nearly 25%. Because of theophylline's relation to caffeine (both being a methylxanthine , and theophylline being a metabolite of caffeine), caffeine's metabolism and clearance may also be reduced, but there are no drug interaction studies between zileuton and caffeine. [5] The R -isomer of warfarin metabolism and clearance is mainly affected by zileuton, while the S -isomer is not (because of metabolism via different enzymes). This can lead to an increase in prothrombin time. [6]

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