Elanco Animal Health, Mattenstrasse 24a, 4058, Basel, Switzerland.
Elanco Animal Health, 2500 Innovation Way, Greenfield, IN, 46140, USA.
Parasit Vectors. 2017 Nov 1;10(1):529. doi: 10.1186/s13071-017-2466-0.
Lotilaner (Credelio™, Elanco), a novel isoxazoline, is a systemic insecticide and acaricide that is rapidly absorbed following oral administration to dogs and has a half-life of 30 days. As part of a development program, studies were undertaken to investigate lotilaner's initial and sustained efficacy and speed of kill against fleas.
Four studies were conducted to evaluate the onset of lotilaner's speed of flea knockdown at the time of treatment, and to determine the sustained speed of flea kill (SOK) up to 35 days post-treatment. Each study assessed one or two specific time points (4, 6, 8 and 12 h) post-treatment and following weekly re-infestations. In each study, dogs were randomised to a lotilaner or an untreated group based on pre-administration flea counts, and before treatment were infested with adult Ctenocephalides felis. Dogs randomised to a lotilaner group received a single treatment on Day 0, at the minimum recommended dose rate of 20 mg/kg, 30 (± 5) minutes after being fed. Efficacy was calculated using geometric, and arithmetic mean flea counts in treated versus untreated groups.
On Day 0, lotilaner efficacy was 89.9% at 4 h, 99.2% at 6 h, 99.9% at 8 h, and 100% at 12 h post-treatment. At each weekly assessment, lotilaner efficacy at 4 h remained at > 97%, at 8 h remained at > 99%, and at 12 h remained at 100% through Day 35. Across all studies, there were no treatment-related adverse events.
Lotilaner's rapid flea knockdown immediately following treatment and sustained SOK through 35 days post-treatment offers a new solution for helping to eliminate the health risks that accompany flea infestations on dogs. The consistency of the rapid, sustained flea SOK demonstrated in these studies generates confidence that monthly use of lotilaner in dogs can be valuable in disrupting the flea life cycle in a contaminated environment, and that newly acquired fleas will die quickly, thereby reducing the discomfort of flea bites. The sustained lotilaner SOK also provides confidence that there will be no "end-of-dose" resurgence in flea burdens with the potential accompanying consequence of flares in flea-bite hypersensitivity.
利替拉纳（Credelio，礼蓝）是一种新型异噁唑啉类药物，为一种全身性杀虫剂和杀螨剂，犬经口给药后迅速吸收，半衰期为 30 天。作为开发计划的一部分，开展了多项研究，以评估利替拉纳对跳蚤的初期和持续疗效以及杀灭速度。
开展了四项研究以评估利替拉纳在治疗时的跳蚤击倒速度的起始情况，并确定治疗后 35 天内的持续跳蚤杀灭速度（SOK）。每项研究均评估了治疗后 4、6、8 和 12 小时以及每周重新感染时的一个或两个特定时间点。在每项研究中，根据治疗前的跳蚤计数，基于给药前的跳蚤计数，将犬随机分配到利替拉纳组或未处理组，并且在治疗前用成年猫栉首蚤进行感染。随机分配到利替拉纳组的犬于第 0 天按最低推荐剂量 20mg/kg 单次给药，在进食后 30（±5）分钟。使用处理组与未处理组的几何和算术平均跳蚤计数来计算疗效。
在第 0 天，4 小时时利替拉纳的疗效为 89.9%，6 小时时为 99.2%，8 小时时为 99.9%，12 小时时为 100%。在每周评估时，4 小时时的疗效仍保持在＞97%，8 小时时保持在＞99%，12 小时时保持在 100%，直至第 35 天。在所有研究中，均未观察到与治疗相关的不良事件。
利替拉纳在治疗后立即迅速杀灭跳蚤，并且在治疗后 35 天内持续保持 SOK，为消除狗身上跳蚤感染带来的健康风险提供了新的解决方案。这些研究中一致显示出的快速、持续的跳蚤 SOK 使我们有信心，每月使用利替拉纳治疗狗可以在受污染的环境中破坏跳蚤的生命周期，并且新感染的跳蚤将迅速死亡，从而减少跳蚤叮咬带来的不适。持续的利替拉纳 SOK 还使我们有信心，不会出现跳蚤负担的“剂量结束”反弹，并且不会随之出现跳蚤叮咬超敏反应的加剧。
