Pharmacodynamics
Albendazole, a benzimidazole, has a broad spectrum repellent effect. Nematodes are sensitive to it, and it also has a strong effect on tapeworm fluke (but requires a larger dose), but is not effective against schistosoma. The main mechanism of action is binding with the nematode microtubulin. Albendazole binds to β-tubulin and prevents it from polymerizing with α-tubulin to form microtubules. Microtubules are the basic structural unit of many organelles and are necessary for cell reproduction processes such as mitosis, protein assembly and energy metabolism. The affinity of Albendar to nematode microtubulin is significantly higher than that of mammalian microtubulin, so it has little toxicity to mammals. This product not only has a strong effect on adult insects, but also has a strong effect on immature insects and larvae, and has a killing effect on eggs.
Pharmacokinetics
Albendazole is a benzimidazole that is well absorbed internally. Cattle can absorb 50% of the administered dose from the gastrointestinal tract and recover 47% of the internal dose of drug metabolites from the urine within 9 days. After internal administration in sheep, because it is quickly metabolized to albendazole sulphoxide (the main active metabolite of deworming), the protodrug cannot be detected in blood or can only be detected for a short time. At 20 hours after administration, metabolites albendazole sulfoxide and albendazole sulfoxide reached plasma drug peak concentrations. The elimination half-lives of sulfoxide metabolites in cattle, sheep, pigs and chickens were 20.5, 7.7-9.0, 5.9 and 4.3 hours, and the elimination half-lives of sulfoxide metabolites were 11.6, 11.8, 9.2 and 2.5 hours, respectively. In addition to sulfoxide and sulfone, there are hydroxylation, hydrolysis and binding products, which are excreted through bile
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