Several formulations of macrocyclic lactones (abamectin, ivermectin, moxidectin), including ivermectin combined with pyrantel (tetrahydropyrimidine) and ivermectin combined with praziquantel (pyrazinoisoquinolin derivative), were tested regarding their efficacy to control gastrointestinal nematodes of horses on a stud farm in southern Brazil. In addition, we tested a pharmaceutically produced generic paste containing ivermectin 4%. Similar formulations of avermectins had different efficacies measured by reduction of EPG. Levels of efficacy of the tested drugs varied against Strongylus edentatus, S. equinus and S. vulgaris. The generic paste (ivermectin 4%) was less effective than the conventional drugs.
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http://dx.doi.org/10.1016/j.parint.2012.05.001 | DOI Listing |
Vet Parasitol
January 2025
Laboratory of Veterinary Clinical Parasitology, Federal University of Paraná, UFPR, R: dos Funcionários, 1540, Curitiba, PR CEP: 81530-000, Brazil. Electronic address:
Haemonchus contortus is a gastrointestinal parasite that affects ruminants (cattle, sheep, etc.), having a significant welfare impact worldwide. The rise of anthelmintic resistance poses a growing challenge to adequate control, compromising the success of treatments.
View Article and Find Full Text PDFMed Vet Entomol
January 2025
Mahidol Oxford Tropical Medicine Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Mass ivermectin (IVM) treatment of livestock (MITL) is under consideration as a malaria control tool as IVM-treated livestock are lethal to blood-feeding Anopheles mosquitoes. MITL is routinely used as a prophylaxis in livestock to reduce the burden and transmission of helminth infections. Recently, there has been a shift in the veterinary IVM market in Southeast Asia wherein nearly all standard IVM formulations are now co-formulated with clorsulon (CLO).
View Article and Find Full Text PDFCells
January 2025
Nuclear Signaling Laboratory, Monash Biomedicine Discovery Institute, Department of Biochemistry and Molecular Biology, Monash University, Clayton, VIC 3800, Australia.
Signal-dependent transport into and out of the nucleus mediated by members of the importin (IMP) superfamily is crucial for eukaryotic function, with inhibitors targeting IMPα being of key interest as anti-infectious agents, including against the apicomplexan species and , causative agents of malaria and toxoplasmosis, respectively. We recently showed that the FDA-approved macrocyclic lactone ivermectin, as well as several other different small molecule inhibitors, can specifically bind to and inhibit and IMPα functions, as well as limit parasite growth. Here we focus on the FDA-approved antiparasitic moxidectin, a structural analogue of ivermectin, for its IMPα-targeting and anti-apicomplexan properties for the first time.
View Article and Find Full Text PDFJ Org Chem
January 2025
Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
There has been a long search for a simple preparation of new cyclic analogues of ionophore antibiotics. We report a simple and general synthesis of three new cyclic derivatives of polyether ionophore, monensin A (MON). The application of the Huisgen 1,3-dipolar cycloaddition of azides and terminal alkynes to macrocyclization results in a concise, synthetic route to monensin lacton or lactam in only 4 steps.
View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
December 2024
Bristol Veterinary School, University of Bristol, Bristol, BS40 5DU, UK.
Cyathostomins are the most abundant equid endoparasites globally. There are approximately fifty cyathostomin species and, whilst they occupy distinct niches within the large intestine, they are generally considered to share similar characteristics in terms of pathogenicity and response to drug treatment. There are three classes of anthelmintic licensed in the UK to treat cyathostomins (benzimidazoles, tetrahydropyrimidines and macrocyclic lactones) and cases of resistance have been documented for all classes.
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