Área Farmacología, Facultad de Veterinaria, Universidad de la República, Montevideo, Uruguay.
BMC Vet Res. 2013 Feb 11;9:27. doi: 10.1186/1746-6148-9-27.
Several oral ivermectin (IVM) formulations for use in sheep are available in the pharmaceutical veterinary market in different countries. All of them are indicated at the same dose rate to treat the gastrointestinal nematodes. However, there is a lack of information on the relative systemic exposure (plasma bioavailability) and clinical efficacy among oral formulations routinely used in sheep. The main goal of the work reported here was to perform a pharmaco-parasitological assessment of three different IVM oral formulations in lambs infected with multiple resistant gastrointestinal nematodes. The comparative drug systemic exposure (IVM plasma concentrations) and nematodicidal efficacies (clinical efficacy) in lambs were determined for a reference (RF) and two different test (T1, T2) IVM oral formulations. One hundred and fifty six (n= 156) healthy Corriedale lambs, naturally infected with multiple resistant gastrointestinal nematodes were allocated into four experimental groups (n=39). Animals in each group received treatment (200 μg/kg) with either the RF, one of the test IVM formulations or were kept as untreated control. Blood samples were collected over 15 days post-treatment (n=8). The IVM plasma concentrations were measured by high performance liquid chromatography with fluorescence detection. The faecal nematode egg count reduction test (FECRT) (n=39) and evaluation of the clinical efficacy were performed at day 14 post-treatment (n=6), where a predominance of IVM highly resistant nematodes was observed.
Neither the overall kinetic behaviour nor the IVM systemic exposure differed among all the tested oral formulations. Equivalent efficacy results were obtained for the different preparations, with an evident therapeutic failure to control Haemonchus spp. and Teladorsagia circumcincta, which correlates with a high degree of nematode resistance to IVM.
在不同国家的兽医制药市场上,有几种可用于绵羊的口服伊维菌素(IVM)制剂。它们都以相同的剂量率用于治疗胃肠道线虫。然而,关于绵羊常规使用的口服制剂的相对全身暴露(血浆生物利用度)和临床疗效的信息却很少。这里报告的工作的主要目标是对感染多重耐药胃肠道线虫的羔羊进行三种不同 IVM 口服制剂的药代寄生虫学评估。通过比较药物全身暴露(IVM 血浆浓度)和驱虫功效(临床疗效),确定了参考(RF)和两种不同的试验(T1、T2)IVM 口服制剂在羔羊中的效果。156 只(n=156)健康的科里代尔羔羊,自然感染了多重耐药的胃肠道线虫,被分配到四个实验组(n=39)。每组动物接受 200μg/kg 的 RF、一种试验 IVM 制剂或作为未处理的对照组进行治疗。在治疗后 15 天内采集血样(n=8)。通过高效液相色谱法荧光检测测量 IVM 血浆浓度。在治疗后第 14 天进行粪便线虫卵计数减少试验(FECRT)(n=39)和临床疗效评估(n=6),此时观察到 IVM 高度耐药线虫占优势。
所有测试的口服制剂在整体动力学行为和 IVM 全身暴露方面均无差异。不同制剂的疗效结果相当,控制 Haemonchus spp.和 Teladorsagia circumcincta 的疗效明显失败,这与 IVM 对线虫的高度耐药性有关。