Table 1

Mean (±S.D.) pharmacokinetic parameters for tirilazad mesylate (TM) after administration of 2.0 mg/kg tirilazad mesylate i.v. and 10 mg/kg of tirilazad mesylate p.o. in the presence and absence of 5 mg finasteride coadministration

ParametersTreatment
10 mg/kg TM p.o. + finasteride10 mg/kg TM p.o.2.0 mg/kg TM i.v. + finasteride2.0 mg/kg TM i.v.
AUC0–∞ (ng hr/ml)243518875324ab 4413
(1113)(1036)(1550)(847)
Cinf (ng/ml)1-c 38234363245699
(79.2)(85.4)(1490)(1583)
CL (L/hr)1-d 309ae 39925.9ab 30.0
(119)(146)(7.82)(5.37)
F0.0910.083
(0.029)(0.029)
λz (hr−1)0.01380.01220.01320.0119
(0.0084)(0.0037)(0.0023)(0.0025)
t½ (hr)61.662.553.760.4
(24.0)(22.0)(8.84)(12.7)
Tmax (hr)1.251.38
(0.707)(0.744)
Vss (L)638778
(193)(244)

  • 1-a P < .05.

  • 1-b Comparison of i.v. treatments.

  • ↵1-c Cinf for i.v. doses, Cmax for oral doses.

  • ↵1-d Systemic clearance for i.v. doses, CLPO for oral doses.

  • 1-e Comparison of oral treatments.