异噁唑啉类动物驱虫药的研究及应用

doi:10.11843/j.issn.0366-6964.2025.01.012

摘要/Abstract

摘要：

异噁唑啉类药物具有多种功效。近年来，因其对各种类型体外寄生虫的疗效好、安全性高，被广泛应用于抗宠物体外寄生虫。异噁唑啉类药物选择性地抑制无脊椎动物的谷氨酸和γ-氨基丁酸门控氯离子通道，使其神经系统紊乱而瘫痪死亡。本文从结构特点、作用机制、药代动力学、药效学和临床驱虫应用等方面综述了异噁唑啉类驱虫药近年来的研究，分析了兽医领域中不同药物的应用情况及潜在毒性，展望异噁唑啉类动物驱虫药的未来发展情况。

关键词: 异噁唑啉, 体外寄生虫, 安全性, 兽医

Abstract:

Isoxazoline drugs have a variety of biological effects. In recent years, they have been widely used in pet to combat ectoparasites due to their excellent effectiveness and high safety against various types of ectoparasites. Isoxazoline drugs selectively inhibits glutamate and gamma-aminobutyrate gated chloride ion channels in invertebrates, resulting in nervous system dysfunction, paralysis and death. This review focuses on the structural characteristics, mechanism of action, pharmacokinetics, pharmacodynamics and clinical anthelmintic application of isoxazoline anthelmintic drugs in recent years. The application and potential toxicity of different drugs in veterinary medicine are analyzed, and presents the future prospect of isoxazoline anthelmintics in animals.

Key words: isoxazoline, ectoparasite, safety, veterinary

中图分类号:

S859.795

王达锋, 马叶涵, 陈春, 龚佳豪, 四朗玉珍, 张军忍, 郭大伟. 异噁唑啉类动物驱虫药的研究及应用[J]. 畜牧兽医学报, 2025, 56(1): 126-135.

WANG Dafeng, MA Yehan, CHEN Chun, GONG Jiahao, SILANG Yuzhen, ZHANG Junren, GUO Dawei. Research and Application of Isoxazoline Anthelmintic Drugs in Animals[J]. Acta Veterinaria et Zootechnica Sinica, 2025, 56(1): 126-135.

图/表 5

图 1

表 1

图 2

表 2

异噁唑啉类动物驱虫药参数汇总"

主药名称 Main drug names	商品名 Product names	剂型 Dosage form	针对病原 The targeted pathogens	靶动物 Target animals	药代动力学参数 The pharmacokinetic parameters
氟雷拉纳 Fluralaner	BRAVECTO^® (贝卫多)、BRAVECTO^® PLUS、BRAVECTO^® 1-MONTH、Exzolt	咀嚼片、滴剂、溶液、复方滴剂	猫蚤、厩螫蝇、铜绿蝇、埃及伊蚊、微小牛蜱、黑脚硬蜱、美洲犬蜱、血红扇头蜱、长角血蜱、美洲钝眼蜱、蓖子硬蜱、牛虱、家禽红螨、北方禽螨、蠕形螨、疥螨、耳螨	犬、猫、蛋鸡、黑熊、鲑鱼、裸眼袋熊等	生物利用度：≈ 25% 达峰时间(T_max)：1 d(内服)；6~25 d(滴剂) 消除半衰期(T_1/2)：12~19 d 达峰浓度(C_max)：0.7~3.4 μg·mL^-1 表观分布容积(V_d)：3.1 L·kg^-1(犬)； 3.5 L·kg^-1(猫) 清除率(Cl)：5.8 mL·(h·kg)^-1(犬)； 9.6 mL·(h·kg)^-1(猫)
阿福拉纳 Afoxolaner	NexGard^® (尼可信)、NexGard Spectra^® (超可信)、NexGard ^® COMBO、NexGard^® PLUS	咀嚼片、复方滴剂	跳蚤、黑脚硬蜱、长角血蜱、美洲犬蜱、美洲钝眼蜱、血红扇头蜱、蓖子硬蜱、牛虱、莱姆病螺旋体(间接)、蠕形螨、疥螨、耳螨、蛇虱	犬、猫、宠物蛇、蟒蛇、猪等	生物利用度：73.9% 达峰时间(T_max)：2~6 h 消除半衰期(T_1/2)：≈16 d 达峰浓度(C_max)：1.7 μg·mL^-1 表观分布容积(V_d)：2.68 L·kg^-1(犬) 清除率(Cl)：4.95 mL·(h·kg)^-1
乐替拉纳 Lotilaner	Credelio^TM (可立奥)、Credelio^TM PLUS、Credelio^TM CAT、Xdemvy^TM	咀嚼片、滴眼液、复方片剂	跳蚤、美洲钝眼蜱、美洲犬蜱、血红扇头蜱、黑脚硬蜱、蓖子硬蜱、牛虱、蠕形螨	犬、猫等	生物利用度：拌料给药可达81%(犬)；100%(猫) 达峰时间(T_max)：2~4 h 消除半衰期(T_1/2)：≈30 d 达峰浓度(C_max)：4.0 μg·mL^-1 表观分布容积(V_d)：6.45 L·kg^-1(犬)； 5.37 L·kg^-1(猫) 清除率(Cl)：7.5 mL·(h·kg)^-1(犬)； 5.4 mL·(h·kg)^-1(猫)
沙罗拉纳 Sarolaner	Simparica^®、Revolution^® PLUS、Simparica TRIO^®	咀嚼片、复方片剂、复方滴剂	跳蚤、美洲钝眼蜱、斑点钝眼蜱、美洲犬蜱、黑脚硬蜱、海湾蜱、蓖子硬蜱、耳螨、牛虱、蠕形螨、疥螨、	犬、猫等	生物利用度：>85% 达峰时间(T_max)：＜24 h 消除半衰期(T_1/2)：11~12 d 达峰浓度(C_max)：1.1 μg·mL^-1 表观分布容积(V_d)：2.81 L·kg^-1(犬) 清除率(Cl)：7.2 mL·(h·kg)^-1(犬)

表 2

图 3

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异噁唑啉环(▲) Isoxazoline ring	药物名称 Drug name	Ar¹	Ar²	专利公开号 The publication number of the patent	专利申请日 The date of the patent application
	氟雷拉纳 Fluralaner			WO2005085216	2005-03-04
	阿福拉纳 Afoxolaner			WO2009002809A2	2008-06-20
	乐替拉纳 Lotilaner			WO2010070068A2	2009-12-17
	沙罗拉纳 Sarolaner			WO2012120399A1	2012-02-23

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