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Praziquantel induces a rapid contraction of schistosomes by a specific effect on the permeability of the cell membrane. The drug further causes vacuolization and disintegration of the schistosome tegument.
After oral administration BILTRICIDE (praziquantel) is rapidly absorbed (80%), subjected to a first pass effect, metabolized and eliminated by the kidneys. Maximal serum concentration is achieved 1-3 hours after dosing. The half-life of praziquantel in serum is 0.8-1.5 hours.
The pharmacokinetics of praziquantel were studied in 40 patients with Schistosoma mansoni infections with varying degrees of hepatic dysfunction (See table 1). In patients with schistosomiasis, the pharmacokinetic parameters did not differ significantly between those with normal hepatic function (Group 1) and those with mild (Child-Pugh class A) hepatic impairment. However, in patients with moderate-to-severe hepatic dysfunction (Child-Pugh class B and C), praziquantel half-life, Cmax, and AUC increased progressively with the degree of hepatic impairment. In Child-Pugh class B, the increases in mean half-life, Cmax, and AUC relative to Group 1 were 1.58-fold, 1.76-fold, and 3.55-fold, respectively. The corresponding increases in Child-Pugh class C patients were 2.82-fold, 4.29-fold, and 15-fold for half-life, Cmax, and AUC.
Table 1: Pharmacokinetic parameters of praziquantel in four
groups of patients with varying degrees of liver function following administration
of 40 mg/kg under fasting conditions.
|Patient Group||Half-life (hr)||Tmax (hr)||Cmax (μg/mL)||AUC (μg/mL* hr)|
|Normal hepatic function (Group 1)||2.99 ± 1.28||1.48 ±0.74||0.83 ± 0.52||3.02 ±0.59|
|Child-Pugh A (Group 2)||4.66±2.77||1.37 ± 0.61||0.93± 0.58||3.87 ±2.44|
|Child-Pugh B (Group 3)||4.74 ±2.16a||2.21 ± 0.78a,b||1.47 ±0.74a,b||10.72 ±5.53a,b|
|Child-Pugh C (Group 4)||8.45 ±2.62a,b,c||3.2 ± 1.05a,b,c||3.57 ±1.30a,b,c||45.35 ± 17.50a,b,c|
|a) p < 0.05 compared to Group 1
b) p < 0.05 compared to Group 2
c) p < 0.05 compared to Group 3
Last reviewed on RxList: 9/13/2010
This monograph has been modified to include the generic and brand name in many instances.
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