Tirilazad Ketoconazole

Fleishaker JC, Pearson PG, Wienkers LC, et al. Biotransformation of tirilazad in humans 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability. J Pharmacol Exp Ther 1996 277 991-998. 

Phenobarbital and phenytoin reduce the serum levels of tirilazad mesilate whereas ketoconazole increases them. Finasteride inhibits the metabolism of tirilazad to its active metabolite. No pharmacokinetic interaction appears to occur between cimetidine or nimodipine and tirilazad. 

Tirilazad mesilate, 10 mg/kg orally or 2 mg/kg intravenously, was given to 12 healthy men and women, either alone or on day 4 of a 7-day regimen of ketoconazole 200 mg daily. The ketoconazole more than doubled the absolute bioavailability of the oral tirilazad mesilate (from 8.7% to 20.9%), apparently because its metabolism by the cytochrome P450 isoen-... 

---