Tirilazad mesilate

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QH11IO2 53064-79-2) see Cefditoien pivoxil 21-iodo-16a-methylpregna-l,4,9(ll)-triene-3,20-dione (C22H27IO2 111668-07-6) see Tirilazad mesilate... 

CH4O3S 75-75-2) see Alatrofloxacin mesilate Alendronate sodium Dolasetron mesilate Glaziovine Nelfinavir mesylate Tirilazad mesilate Trovafloxacin mesilate... 

C4HCI3N2 3764-01-0) see Minoxidil Tirilazad mesilate l-tricyclo[3.3.1.1 ]dec-l-ylethanone oxime... 

C6II I()2 53064-79-2) see Cefditoren pivoxil 21 -iodo-16(x-methy Ipregna-1,4,9( 11 )-trienc-3,20-dionc (C22H27I02 111668-07-6) sec Tirilazad mesilate... 

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. 

A study in 16 healthy men found that cimetidine 300 mg every 6 hours for 4 days had no effect on the pharmacokinetics of a single 2-mg/kg dose of tirilazad mesilate, given by infusion over 10 minutes on day 2, nor on U-89678, its active metabolite. No special precautions would seem necessary if cimetidine is given with tirilazad mesilate. 

In a study, 8 healthy men were given finasteride 5 mg daily for 10 days, with tirilazad mesilate 10 mg/kg orally or 2 mg/kg intravenously on day 7. Finasteride increased the AIJCs of intravenous and oral tirilazad by 21% and 29%, respectively. Oral finasteride reduced the AUCs of the active metabolite (U-89678) by 92% when tirilazad was given intravenously and by 75% when tirilazad was given orally. Although the metabolism of tirilazad to U-89678 was inhibited there was only a moderate effect on the overall clearance of tirilazad and the interaction was considered unlikely to be of clinical significance. ... 

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-... 

In a single-dose study in 12 healthy men, there was no pharmaeokinetie or pharmacodynamie interaetion between intravenous tirilazad mesilate 2 mg/kg and oral nimodipine 60 mg. No speeial preeautions would seem necessary if nimodipine is given with tirilazad mesilate... 

The pharmacokinetics of tirilazad mesilate (1.5 mg/kg as 10 minute intravenous infusions every 6 hours for 29 doses) were studied in 15 healthy subjects before and after they took phenobarbital 100 mg daily for 8 days. The phenobarbital increased the clearance of the tirilazad by 25% in the male subjects and 29% in the female, and the AUC of the active metabolite of tirilazad (U-89678) was reduced by 51% in the males and 69% in the females. The reason is thought to be that the phenobarbital acts as an enzyme inducer, which increases the metabolism of the tirilazad. The clinical importance of these reductions awaits assessment, but be alert for evidence of reduced effects if both drugs are given. It is doubtful if the full enzyme-inducing effects of the phenobarbital would have been reached in this study after only one week, so anticipate a greater effect if it is given for a longer period. 

After taking phenytoin 200 mg every 8 hours for 11 doses then 100 mg every 8 hours for 5 doses, the AUCg.g of tirilazad mesilate was reduced by 35% in 12 healthy subjects. The AUC of the active metabolite, U-89678, was reduced by 87%. Another report by the same group of workers found that phenytoin every 8 hours for 7 days (9 doses of200 mg followed by 13 doses of 100 mg) reduced the clearance of tirilazad by 92% and of U-89678 by 93%. In another report the authors noted that phenytoin increased the metabolism of tirilazad and its metabolite in men and women to similar extents. The clinical importance of these reductions is still to be assessed, but be alert for any evidence of reduced tirilazad effects if both drugs are given. 

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