Salman Muhammad, Abbas Rao Zahid, Mehmood Khalid, Hussain Riaz, Shah Sehar, Faheem Mehwish, Zaheer Tean, Abbas Asghar, Morales Bernardo, Aneva Ina, Martínez José L
Department of Parasitology, University of Agriculture Faisalabad, Faisalabad 38000, Pakistan.
Department of Clinical Medicine and Surgery, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
Pharmaceuticals (Basel). 2022 Mar 9;15(3):332. doi: 10.3390/ph15030332.
Macrocyclic lactones, particularly the avermectins, have completely revolutionized the approaches aimed at control of parasites. These avermectins are the most widely used anti-parasitic drugs in veterinary field with sales exceeding one billion US dollars annually. However, before clinical usage, their safety evaluation in the animals is a major critical factor that must be considered. Many studies have reported the negative effects of avermectins like ivermectin, abamectin, doramectin, and eprinomectin on the host animals. These harmful effects arise from avermectins targeting GABA and glutamate-gated chloride channels present both in the parasites and the host animals. In this review, various modes of avermectins action along with the negative effects on the host like nephrotoxicity, hepatotoxicity, neurotoxicity, reproductive toxicity, and endocrine disruption were discussed in detail. Furthermore, other important issues like ecotoxicity, drug resistance, and drug residues in milk associated with avermectins usage were also discussed, which need special attention.
大环内酯类药物,尤其是阿维菌素,彻底改变了寄生虫控制方法。这些阿维菌素是兽医领域使用最广泛的抗寄生虫药物,年销售额超过十亿美元。然而,在临床使用之前,对动物进行安全性评估是必须考虑的一个主要关键因素。许多研究报告了伊维菌素、阿维菌素、多拉菌素和埃普利诺菌素等阿维菌素对宿主动物的负面影响。这些有害影响源于阿维菌素作用于寄生虫和宿主动物中都存在的γ-氨基丁酸(GABA)和谷氨酸门控氯离子通道。在本综述中,详细讨论了阿维菌素的各种作用方式以及对宿主的负面影响,如肾毒性、肝毒性、神经毒性、生殖毒性和内分泌干扰。此外,还讨论了与阿维菌素使用相关的其他重要问题,如生态毒性、耐药性和牛奶中的药物残留,这些问题需要特别关注。