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This study comprehensively evaluated the in vitro and in vivo anthelmintic efficacy and pharmacokinetics of four benzimidazole compounds: febantel (FB), fenbendazole (FBZ), albendazole (ABZ), and mebendazole (MBZ) against the gill fluke Microcotyle sebastis in cultured black rockfish (Sebastes schlegelii). In vitro tests with isolated adult parasites demonstrated that ABZ exhibited the highest efficacy, followed by FBZ, while MBZ showed minimal activity and FB remained largely inactive at lower concentrations. At the highest concentration tested (200 mg/L), FB showed only weak, nonspecific activity. In in vivo experiments, ABZ was the most effective drug when orally administered at 50 mg/kg for three consecutive days, while FB demonstrated greater efficacy than FBZ, and MBZ exhibited the lowest efficacy under the tested conditions. Pharmacokinetic analysis revealed marked variation among the drugs, with FB achieving the highest active metabolite levels at 100 mg/kg. ABZ, at 50 mg/kg, achieved comparable systemic exposure to FBZ at 100 mg/kg through its active metabolite albendazole sulfoxide (ABZSO). These findings highlight ABZ as the most efficacious compound, with FB showing promise through metabolic conversion to FBZ, and MBZ demonstrating limited efficacy due to poor absorption and rapid inactivation. Overall, this study provides an integrated evaluation of both efficacy and pharmacokinetics, indicating that ABZ and FB are effective candidates for managing M. sebastis infections in aquaculture.
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http://dx.doi.org/10.1016/j.vetpar.2025.110573 | DOI Listing |
Vet Parasitol
August 2025
Department of Aquatic Life Medicine, Kunsan National University, Gunsan 54150, Republic of Korea. Electronic address:
This study comprehensively evaluated the in vitro and in vivo anthelmintic efficacy and pharmacokinetics of four benzimidazole compounds: febantel (FB), fenbendazole (FBZ), albendazole (ABZ), and mebendazole (MBZ) against the gill fluke Microcotyle sebastis in cultured black rockfish (Sebastes schlegelii). In vitro tests with isolated adult parasites demonstrated that ABZ exhibited the highest efficacy, followed by FBZ, while MBZ showed minimal activity and FB remained largely inactive at lower concentrations. At the highest concentration tested (200 mg/L), FB showed only weak, nonspecific activity.
View Article and Find Full Text PDFJ Genet Eng Biotechnol
March 2025
Department of Tropical Medicine, Faculty of Medicine, Khon Kaen University, Khon Kaen 40002, Thailand; WHO Collaborating Center for Research and Control of Opisthorchiasis (Southeast Asian Liver Fluke Disease), Tropical Disease Research Center, Khon Kaen University, Khon Kaen 40002, Thailand. Electr
Background: Benzimidazole resistance is an emerging challenge among parasitic helminths. It is caused by single nucleotide polymorphisms (SNPs) in specific loci in helminths' β-tubulin genes. Field studies and laboratory investigations reported resistance-associated SNPs in 4 codon locations with 7 allelic variations among hookworms.
View Article and Find Full Text PDFSci Total Environ
January 2024
Univ. Grenoble Alpes, CNRS, INRAE, IRD, Grenoble INP, IGE, Grenoble, France.
Various pharmaceuticals are essential for livestock farming, but some are highly toxic to aquatic life if they reach surface water bodies. Mediterranean Climate is characterized by dry summers followed by intense autumn storms. We studied the effect of these climatic conditions on the risk of pharmaceutical residues transfer to streams at the catchment-scale.
View Article and Find Full Text PDFACS Omega
January 2022
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Horus University-Egypt, New Damietta 34518, Egypt.
Cancer is a leading cause of death worldwide and its incidence is unfortunately anticipated to rise in the next years. On the other hand, vascular endothelial growth factor receptor 2 (VEGFR-2) is highly expressed in tumor-associated endothelial cells, where it affects tumor-promoting angiogenesis. Therefore, VEGFR-2 is considered one of the most promising therapeutic targets for cancer treatment.
View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
December 2019
Faculty of Veterinary Medicine, University of Calgary, Calgary, Alberta, T2N 4N1, Canada. Electronic address:
We have undertaken a detailed analysis of the biotransformation of five of the most therapeutically important benzimidazole anthelmintics - albendazole (ABZ), mebendazole (MBZ), thiabendazole (TBZ), oxfendazole (OxBZ) and fenbendazole (FBZ) - in Caenorhabditis elegans and the ruminant parasite Haemonchus contortus. Drug metabolites were detected by LC-MS/MS analysis in supernatants of C. elegans cultures with a hexose conjugate, most likely glucose, dominating for all five drugs.
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