艾弗梅克丁代谢物的药理动力学及其对抗Anopheles stephensi蚊子的活性
Charlotte Kern1,2, Pie Müller3,4, Carlos Chaccour5,6,7
1Division of Clinical Pharmacology & Toxicology, Department of Internal Medicine, University Hospital Bern, Bern, Switzerland.
Malaria journal
|June 24, 2023
概括
甲素代谢物M1和M2对Anopheles stephensi蚊子有毒,这可能解释了在疟疾载体控制工作中观察到的长期"后甲素效应".
科学领域:
- 药理学 药理学是指药理学的学科.
- 载体生物学 载体生物学
- 药用化学 医学化学
背景情况:
- 伊弗梅克是一种用于寄生虫感染的杀虫剂.
- 它通过减少蚊子的存活率,显示出作为疟疾载体控制剂的潜力.
- 一个"ivermectin后效应"表明长时间的蚊子毒性超出可检测的药物水平.
研究的目的:
- 为了研究ivermectin代谢物的药理动力学特性.
- 为了确定ivermectin代谢物是否有助于杀蚊活性.
- 评估代谢产物的作用在"ivermectin后效应".
主要方法:
- 艾弗梅克丁是使用人类细胞染色体P450酶 (CYP3A4 / 5) 代谢的.
- 在人类志愿者中净化了9种代谢物,并评估了它们的药理动力学.
- 代谢物被测试出对Anopheles stephensi蚊子的毒性.
主要成果:
- CYP3A4主要形成的代谢物M1-M8; CYP3A5形成的代谢物M9.
- 代谢物M1 (脱甲基-H2B1a) 和M2 (基-H2B1a) 对An.高度有毒. 斯蒂芬斯. 斯蒂芬斯. 斯蒂芬斯.
- 代谢物M4 (脱甲基,氧-H2B1a) 在3天内将蚊子的存活率降低到35%.
- 代谢物M1和M4的半衰期比ivermectin的半衰期长.
结论:
- 甲胺代谢物M1和M2具有显著的杀蚊活性.
- 这些代谢物很可能是观察到的"ivermectin后效应"的原因.
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