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Table 1 Plasma pharmacokinetic parameters (mean ± SD) for triclabendazole sulphoxide (TCBZ.SO) and triclabendazole sulphone (TCBZ.SO2) obtained after the intraruminal (i.r.) administration of triclabendazole (TCBZ, 10 mg/kg, i.r.) alone or co-administered with ivermectin (IVM, 0.2 mg/kg, s.c.) and methimazole (MTZ, 1.5 mg/kg, i.m.) to Fasciola hepatica-infected sheep.

From: Unchanged triclabendazole kinetics after co-administration with ivermectin and methimazole: failure of its therapeutic activity against triclabendazole-resistant liver flukes

PHARMACOKINETIC PARAMETERS

TCBZ.SO

TCBZ.SO2

 

TCBZ alone

Combined treatment

TCBZ alone

Combined treatment

Cmax (μg/ml)

14.0 ± 0.85

15.6 ± 1.46

13.5 ± 1.68

12.3 ± 1.28

Tmax (h)

22.5 ± 7.55

24.0 ± 4.90

39.0 ± 6.00

42.0 ± 6.93

AUC0-t(μg.h/ml)

653.9 ± 140.6

650.7 ± 122.8

868.2 ± 217.6

893.7 ± 114.1

AUC0-∞ (μg.h/ml)

661.5 ± 148.5

657.1 ± 119.4

917.9 ± 270.6

945.6 ± 129.3

T1/2el (h)

17.5 ± 8.45

18.4 ± 5.82

26.8 ± 10.9

30.4 ± 9.30

MRT (h)

38.8 ± 10.5

39.1 ± 5.03

61.3 ± 17.2

67.6 ± 9.71

T1/2for (h)

6.85 ± 2.18

8.26 ± 1.22

12.3 ± 2.90

13.5 ± 1.93

  1. Cmax: peak plasma concentration; Tmax: time to the Cmax; AUC 0-t : Area under the plasma concentration vs. time curve from 0 to the detection time; AUC 0-∞ (μg.h/ml): Area under the plasma concentration vs. time curve extrapolated to infinity; T1/2el: elimination half-life; MRT: mean residence time (obtained by non-compartmental analysis of the data); T1/2for: formation half life.