R-praziquantel integrated population pharmacokinetics in preschool- and school-aged African children infected with Schistosoma mansoni and S. haematobium and Lao adults infected with Opisthorchis viverrini

2022 ◽  
Author(s):  
Falcoz Christine ◽  
Guzy Serge ◽  
Kovač Jana ◽  
Meister Isabel ◽  
Coulibaly Jean ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Population Pharmacokinetics ◽  
Opisthorchis Viverrini ◽  
African Children

scholarly journals Evaluation of the In Vivo Activity of Tribendimidine against Schistosoma mansoni, Fasciola hepatica, Clonorchis sinensis, and Opisthorchis viverrini

2006 ◽  
Vol 51 (3) ◽  
pp. 1096-1098 ◽  
Author(s):  
Jennifer Keiser ◽  
Xiao Shu-Hua ◽  
Jacques Chollet ◽  
Marcel Tanner ◽  
Jürg Utzinger
Keyword(s):  
Schistosoma Mansoni ◽  
Fasciola Hepatica ◽  
Clonorchis Sinensis ◽  
Opisthorchis Viverrini ◽  
High Doses

ABSTRACT We examined the in vivo activity of tribendimidine against selected trematodes. A single 150-mg/kg dose of tribendimidine achieved a 99.1% reduction of Clonorchis sinensis in rats. A 400-mg/kg dose of tribendimidine reduced Opisthorchis viverrini in hamsters by 95.7%. High doses of tribendimidine showed no activity against Schistosoma mansoni and Fasciola hepatica.

scholarly journals Population Pharmacokinetic Modeling of Tribendimidine Metabolites in Opisthorchis viverrini-Infected Adults

2016 ◽  
Vol 60 (10) ◽  
pp. 5695-5704 ◽  
Author(s):  
Fiona Vanobberghen ◽  
Melissa A. Penny ◽  
Urs Duthaler ◽  
Peter Odermatt ◽  
Somphou Sayasone ◽  
...  
Keyword(s):  
Population Pharmacokinetics ◽  
Drug Exposure ◽  
Structural Model ◽  
Dried Blood Spots ◽  
Volume Of Distribution ◽  
Opisthorchis Viverrini ◽  
Population Pharmacokinetic ◽  
Two Phase ◽  
Content Type ◽  
Population Pharmacokinetic Modeling

ABSTRACTThere is a pressing need for alternative treatments against the liver flukeOpisthorchis viverrini. Oral tribendimidine is a promising candidate, but its population pharmacokinetic properties are unknown. Two phase IIa trials were conducted in Laos inO. viverrini-infected adults receiving single oral doses of 25 to 600 mg tribendimidine administered as different formulations in each study (study 1 used 200-mg tablets, and study 2 used 50-mg tablets). Venous whole blood, plasma, and capillary dried blood spots were sampled frequently from 68 adults, and concentrations of the tribendimidine metabolites dADT (deacetylated amidantel) and adADT (acetylated dADT) were measured. Population pharmacokinetics were assessed by using nonlinear mixed-effects modeling. The relationship between drug exposure and cure (assessed at 21 days posttreatment) was evaluated by using univariable logistic regression. A six-transit compartment absorption model with a one-disposition compartment for each metabolite described the data well. Compared to the 50-mg formulation (study 2), the 200-mg formulation (study 1) had a 40.1% higher mean transit absorption time, a 113% higher dADT volume of distribution, and a 364% higher adADT volume of distribution. Each 10-year increase in age was associated with a 12.7% lower dADT clearance and a 21.2% lower adADT clearance. The highest cure rates (≥55%) were observed with doses of ≥100 mg. Higher dADT, but not adADT, peak concentrations and exposures were associated with cure (P= 0.004 and 0.003, respectively). For the first time, population pharmacokinetics of tribendimidine have been described. Known differences in the 200-mg versus 50-mg formulations were captured by covariate modeling. Further studies are needed to validate the structural model and confirm covariate relationships. (This study has been registered with the ISRCTN Registry under no. ISRCTN96948551.)

scholarly journals Population pharmacokinetics of artesunate and amodiaquine in African children

2009 ◽  
Vol 8 (1) ◽  
Author(s):  
Kasia Stepniewska ◽  
Walter Taylor ◽  
Sodiomon B Sirima ◽  
Esperance B Ouedraogo ◽  
Alphonse Ouedraogo ◽  
...  
Keyword(s):  
Population Pharmacokinetics ◽  
African Children
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