TABLE 1

Pharmacokinetic parameters of talinolol in Mdr1a(−/−) and wild-type rats after intravenous (1 mg/kg) and oral (5 mg/kg) administration of talinolol

ParametersIntravenousOral
WTMdr1a(−/−)WTMdr1a(−/−)
AUC/dose, μM · h/mg/kg0.3 ± 0.060.4 ± 0.050.02 ± 0.0020.09 ± 0.02*
t1/2, h0.7 ± 0.21.0 ± 0.2
Cl, ml · min−1 · kg−1153 ± 18119 ± 15
Vdss, l/kg4.8 ± 0.56.5 ± 1.3
Cmax, μM0.06 ± 0.010.21 ± 0.07
Tmax, h2.0 ± 0.001.7 ± 0.3
F, %723
  • WT, wild-type; Cl, clearance; Vdss, volume of distribution at steady state; Cmax, maximum concentration; Tmax, time to reach maximum concentration; F, bioavailability.

  • * Significantly different from wild-type animals (P < 0.05).