Pharmacokinetic investigation of albendazole and praziquantel in Thai children infected withGiardia intestinalis

Abstract

The pharmacokinetics of albendazole/albendazole sulphoxide and praziquantel were investigated in Thai children with Giardia infection. Twenty school-age children were randomly allocated to receive either a single oral dose of albendazole (400 mg/child) or the same dose of albendazole given concurrently with a single oral dose of praziquantel (20 mg/kg). The concentrations of albendazole/albendazole sulphoxide and praziquantel in plasma samples, collected at intervals in the first 24 h post-treatment, were then quantified using HPLC with ultra-violet detection. No significant pharmacokinetic interaction between the albendazole and praziquantel was demonstrated. For albendazole sulphoxide, the active metabolite of albendazole, there was marked inter-individual variation in the maximum plasma concentration and the 'area under the curve'. The pharmacokinetics of albendazole sulphoxide were similar whether albendazole was given alone or in combination with praziquantel.

A Review of Pharmacokinetic Drug–Drug Interactions with the Anthelmintic Medications Albendazole and Mebendazole

“…After duplicate articles were removed, titles and abstracts of articles were reviewed by two authors, producing 35 articles , of which 17 were included in the review [9][10][11][12][13][14][15][16][17][18][19][20][21][22][23][24][25]. Eighteen articles were excluded for the following reasons: eight articles used animals [26][27][28][29][30][31][32][33]; two articles contained only in vitro data [34,35]; two articles did not contain any pharmacokinetic data of either albendazole or mebendazole [36,37]; two articles only contained data on drug-food interactions [38,39]; and four articles did not contain data on any drug interactions with either albendazole or mebendazole [40][41][42][43].…”

“…The changes in pharmacokinetic parameters of C max and AUC for both albendazole and praziquantel may improve therapeutic efficacy; however, these elevations may also represent an increased risk of adverse drug effects. This combination has also been studied by Pengsaa et al [18], for safety purposes, in a prospective, randomized trial enrolling 20 Thai children infected with Giardia intestinalis. Unlike the findings by Lima et al [18], the combination of albendazole and praziquantel used in this trial was found to have no statistically significant changes in the pharmacokinetic parameters of either drug.…”

“…This combination has also been studied by Pengsaa et al [18], for safety purposes, in a prospective, randomized trial enrolling 20 Thai children infected with Giardia intestinalis. Unlike the findings by Lima et al [18], the combination of albendazole and praziquantel used in this trial was found to have no statistically significant changes in the pharmacokinetic parameters of either drug. However, of interest, the authors of this trial found that no adverse effects of either drug were noted in any of the 20 children investigated [17].…”

Simultaneous determination of albendazole metabolites, praziquantel and its metabolite in plasma by high-performance liquid chromatography–electrospray mass spectrometry

“…Due to this extensive metabolism, plasma concentrations of ABZ are usually low and pharmacokinetic studies are developed using ASOX and ASON concentrations [11][12][13][14][15]. PZQ is metabolized to several hydroxylated metabolites [16][17][18], mainly trans-4-hydroxypraziquantel (TRANS), an active metabolite [19].…”

Simultaneous determination of albendazole and praziquantel in rat plasma by HPLC-UV

“…Albendazole [ABZ] is an inactive moiety but it readily gets metabolized to an active metabolite Albendazole sulfoxide [ABZSO] then this ABZSO is then further metabolized to an inactive metabolite Albendazole sulfone [ABZSO2] [10]. As ABZ is metabolized extensively, therefore, the plasma concentration of ABZ is also very low as a result the pharmacokinetic studies were been done using Albendazole sulfoxide [ABZSO] as an active metabolite and Albendazole sulfone [ABZSO2] as an inactive metabolite [11][12][13][14][15]. Metabolism of Praziquantel [PRQ] occurs giving a number of hydroxylated metabolites [16][17][18], among which the active metabolite is mainly trans-4-hydroxypraziquantel [TRANS], an active metabolite [19].…”