TABLE 3

Effect of ethanol and treatment with specific MCT1 inhibitor (AZD-3965) on toxicokinetics after GHB oral administration.

ParameterGHB (n = 4)GHB + ethanol (n = 4)GHB + ethanol + AZD (n = 4)
AUC (mg·min/ml)230 ± 30167 ± 7139 ± 18*
CL/F (ml/min per kg)6.60 ± 0.869.01 ± 0.4110.9 ± 1.60*
CLR (ml/min per kg)1.67 ± 0.551.68 ± 0.392.72 ± 0.43#
CLNR/F (ml/min per kg)4.92 ± 1.107.33 ± 0.748.24 ± 1.68*
Vss/F (ml)584 ± 161394 ± 60814 ± 227#
Urinary recovery (%)25.8 ± 9.8718.8 ± 4.9325.2 ± 5.4
Cmax906 ± 111906 ± 112489 ± 167#
Tmax330 ± 60121 ± 0211 ± 114*
t1/2 (min)40.4 ± 22.463.2 ± 14.374.1 ± 13.0*
  • AZD-3965 was administered at a dose of 5 mg/kg 60 minutes after GHB (1500 mg/kg p.o.). Ethanol was administered at a dose of 2 g/kg i.v. 5 minutes before GHB. Data are presented as means ± S.D. AZD, AZD-3965; Tmax, time of maximal concentration; t1/2, terminal half-life.

  • *Significantly different from GHB alone (P < 0.05); #Significantly different from GHB + ethanol (P < 0.05).