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泰法诺喹和伯氨喹与早期的 8-氨基喹啉类药物不同,不会出现与中枢神经系统病变相关的临床神经体征。

Tafenoquine and primaquine do not exhibit clinical neurologic signs associated with central nervous system lesions in the same manner as earlier 8-aminoquinolines.

机构信息

Fast-Track Drugs & Biologics, North Potomac, MD, 20878, USA.

Clinical Network Services Pty Ltd, 88/4 Jephson Road, Toowong, 4066, Queensland, Australia.

出版信息

Malar J. 2018 Nov 6;17(1):407. doi: 10.1186/s12936-018-2555-3.

Abstract

BACKGROUND

Tafenoquine was recently approved for Plasmodium vivax radical cure (KRINTAFEL™) and malaria prevention (ARAKODA™).

METHODS

A review of the non-clinical and clinical literature was conducted to assess whether tafenoquine (and primaquine) exhibit the same neurologic lesions and associated clinical signs as earlier 8-aminoquinolines, as has been alleged in recent opinion pieces.

RESULTS

Plasmocid, pamaquine and pentaquine damage specific neuro-anatomical structures in Rhesus monkeys and humans leading to corresponding deficits in neurologic function. Neurologic therapeutic indices for these 3 drugs calculated based on monkey data were well correlated with human data. Despite 60 years of use, there is no evidence that primaquine exhibits similar neurotoxicity in humans.

DISCUSSION/CONCLUSIONS: Extrapolation of data from Rhesus monkeys to humans, and the available clinical data, suggest that tafenoquine also does not exhibit pamaquine, pentaquine or plasmocid-like clinical neurologic signs in humans.

摘要

背景

他非诺喹啉最近被批准用于根治间日疟原虫(KRINTAFEL™)和预防疟疾(ARAKODA™)。

方法

对非临床和临床文献进行了回顾,以评估他非诺喹啉(和伯氨喹啉)是否与早期的 8-氨基喹啉一样,引起相同的神经病变和相关的临床体征,正如最近的一些观点文章所声称的那样。

结果

疟立康、扑疟喹啉和戊奎宁会损害恒河猴和人类特定的神经解剖结构,导致相应的神经功能缺陷。基于猴子数据计算的这 3 种药物的神经治疗指数与人类数据相关性良好。尽管使用了 60 年,但没有证据表明伯氨喹啉在人类中表现出类似的神经毒性。

讨论/结论:从恒河猴到人类的数据推断,以及现有的临床数据表明,他非诺喹啉在人类中也没有表现出与扑疟喹啉、戊奎宁或疟立康类似的临床神经体征。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/218b/6219089/a0fefc245326/12936_2018_2555_Fig1_HTML.jpg

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