Albendazole (ABZ) is one of the most important benzimidazole compounds possessing high activity against the lancet fluke, Dicrocoelium dendriticum. ABZ sulphoxide (ABZ.SO) is the main molecule present in the bloodstream of an ABZ-treated host. The aim of this study was to characterise the pattern of ex vivo uptake of ABZ and ABZ.SO by lancet flukes and the export of both anthelmintics from these parasites. Transport of these anthelmintics in both living and dead flukes was compared. The adult flukes were collected from mouflons (Ovis musimon) which had been infected naturally. Results showed that more lipophilic ABZ was imported to a higher extent than ABZ.SO, and that significantly higher concentrations of ABZ were detected within living flukes as compared to dead ones. The same pattern was revealed in the study of ABZ and ABZ.SO export from the flukes' bodies. In addition to passive diffusion, active ABZ uptake and active efflux of ABZ and ABZ.SO in D. dendriticum could be assumed. 相似文献
Three on-farm studies were conducted in Nicaragua during three consecutive years (1999–2001) to assess the impact of natural helminth infections on growth performance of free-range chickens aged 3–4 months. On all participating farms, half of the chickens were treated regularly with anthelmintics (Trifén avícola – a combined formulation of piperazine, phenothiazine and dichlorophen – or albendazole) to express the growth potential of non-infected birds, whereas the other half served as non-treated controls. In 1999, treated chickens had a 39% higher weight gain compared to the control group 6 weeks after the first treatment on 15 farms. In 2000 and 2001, treated chickens had similar weight gain as the control group 10 weeks after the first treatment on 7 farms and 12 farms, respectively. The main reason for the very-different weight gain figures seems to be the weather conditions. In 1999, the study site experienced a rainy season with precipitation far above average, whereas in 2000 and 2001 the rainy seasons had precipitations far below average. Based on these findings, routine use of anthelmintics in the study area would only be recommended in wet years when production losses due to helminth infections seem to be pronounced.
In 2001, the study set-up included an assessment of the effect of protein supplementation (soybean) on growth on six farms. Supplemented chickens (treated and non-treated with anthelmintics) had 17% higher weight gain than non-supplemented. Protein supplementation affected neither worm burdens nor faecal egg counts for any of the studied helminths.
The post-mortem examinations showed that Trifén reduced burdens of Ascaridia galli, Heterakis gallinarum, and cestodes (efficacies of 100, 100 and 67%, respectively). Albendazole reduced burdens of H. gallinarum (efficacy of 100%). Efficacies against other helminths were difficult to assess due to low worm burdens. Chickens treated with albendazole had lower Ascaridia and Heterakis faecal egg counts than non-treated chickens. 相似文献
The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO(2) (0.3%), albendazole 2-aminosulfone (ABZ-SO(2)NH(2)) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). 相似文献
The pharmacokinetics of albendazole were studied in sheep and goats following single and divided doseadministration at nematocidal and flukicidal dose rates. The disposition curves of the metabolites indicated increased uptake of the drug both in sheep and goats at divided dose schedules compared to single dose administration (P<0.05). The increased bioavailability of benzimidazole anthelmintics in divided dose schedules could improve their efficacy and help in extending their lives. 相似文献