Hamel Dietmar, Bosco Antonio, Rinaldi Laura, Cringoli Giuseppe, Kaulfuß Karl-Heinz, Kellermann Michael, Fischer James, Wang Hailun, Kley Katrin, Mayr Sandra, Rauh Renate, Visser Martin, Wiefel Thea, Fankhauser Becky, Rehbein Steffen
Merial GmbH, Kathrinenhof Research Center, Walchenseestr. 8-12, 83101, Rohrdorf, Germany.
Department of Veterinary Medicine and Animal Production, University of Naples Federico II, Via della Veterinaria, 1, 80137, Naples, Italy.
BMC Vet Res. 2017 May 30;13(1):148. doi: 10.1186/s12917-017-1075-7.
The anthelmintic efficacy of the 0.5% w/v topical formulation of eprinomectin (EPN), EPRINEX® Pour-on (Merial) when administered at 1 mg/kg body weight was evaluated in sheep in two dose confirmation laboratory studies and one multicenter field study. In addition, the pharmacokinetics of EPN when administered at that dosage to adult sheep was determined.
In the two dose confirmation studies, which included 10 sheep each, sheep treated with topical EPN had significantly (p < 0.05) fewer of the following nematodes than the untreated sheep with overall reduction of nematode counts by >99%: adult Dictyocaulus filaria, Haemonchus contortus, Teladorsagia circumcincta(pinnata/trifurcata), Trichostrongylus axei, T. colubriformis, T. vitrinus, Cooperia curticei, Nematodirus battus, Strongyloides papillosus, Chabertia ovina and Oesophagostomum venulosum, and inhibited fourth-stage Teladorsagia larvae. A total of 196 sheep harboring naturally acquired gastrointestinal nematode infections were included in the field efficacy study at two sites each in Germany (48 Merino x Ile de France lambs, 52 adult Merino females) and in Italy (adult male and female Bagnolese, Lacaune, Lacaune x Bagnolese, Bagnolese x Sarda sheep; 48 animals per site). Animals were blocked on pre-treatment body weight and within each block, one animal was randomly assigned to the control (untreated) group and three animals were randomly assigned to be treated with topical EPN. Examination of feces 14 days after treatment demonstrated that, relative to the controls, topical EPN-treated sheep had significantly (p < 0.0001) lower strongylid egg counts. Reduction was ≥97% at each site and 98.6% across all sites. Pharmacokinetics of EPN following single treatment with topical EPN were determined in eight ~4.5 year old female Merino cross sheep based on the analysis of plasma samples which were collected from two hours to 21 days following treatment. The main pharmacokinetic parameters were: C 6.20 ± 1.71 ng/mL, AUC 48.8 ± 19.2 day*ng/mL, T 3.13 ± 2.99 days and T 6.40 ± 2.95 days. No treatment-related health problems or adverse drug events were observed in any study.
These studies demonstrated 0.5% w/v EPN administered topically at 1 mg/kg body weight to be highly efficacious against a broad range of ovine gastrointestinal nematodes and D. filaria lungworms and well tolerated by sheep of different ages, breeds, gender and physiological status.
在两项剂量确认实验室研究和一项多中心田间研究中,对绵羊使用1毫克/千克体重的0.5%(w/v)依普菌素(EPN)局部用制剂EPRINEX®浇泼剂(梅里亚公司)的驱虫效果进行了评估。此外,还测定了以该剂量对成年绵羊给药后EPN的药代动力学。
在两项各有10只绵羊的剂量确认研究中,局部使用EPN治疗的绵羊体内以下线虫数量显著少于未治疗的绵羊(p < 0.05),线虫总数减少超过99%:成年丝状网尾线虫、捻转血矛线虫、环纹泰勒虫(翼状/三叉泰勒虫)、奥氏奥斯特线虫、哥伦比亚细颈线虫、玻璃细颈线虫、柯氏古柏线虫、巴氏细颈线虫、乳头类圆线虫、绵羊夏伯特线虫和微小食道口线虫,以及抑制期第四阶段的环纹泰勒虫幼虫。田间药效研究在德国的两个地点(48只美利奴×法兰西岛羔羊、52只成年美利奴母羊)和意大利(成年巴尼奥莱斯羊、拉库内羊、拉库内×巴尼奥莱斯羊、巴尼奥莱斯×萨尔达羊的公母羊;每个地点48只动物)共纳入了196只自然感染胃肠道线虫的绵羊。动物按治疗前体重进行分组,在每个组内,将一只动物随机分配到对照组(未治疗),三只动物随机分配接受局部EPN治疗。治疗14天后粪便检查表明,相对于对照组,局部使用EPN治疗的绵羊的圆线虫卵计数显著更低(p < 0.0001)。每个地点的减少率≥97%,所有地点的总体减少率为98.6%。基于对治疗后2小时至21天采集的血浆样本的分析,在8只约4.5岁的美利奴杂交母羊中测定了局部使用EPN单次治疗后EPN的药代动力学。主要药代动力学参数为:C为6.20 ± 1.71纳克/毫升,AUC为48.8 ± 19.2天*纳克/毫升,T为3.13 ± 2.99天,T为6.40 ± 2.95天。在任何研究中均未观察到与治疗相关的健康问题或药物不良反应。
这些研究表明,以1毫克/千克体重局部给予0.5%(w/v)EPN对多种绵羊胃肠道线虫和丝状网尾线虫具有高效驱虫作用,并且不同年龄、品种、性别和生理状态的绵羊对其耐受性良好。