Tafenoquine is an 8-aminoquinoline anti-malarial drug recently approved as a single-dose (300 mg) therapy for Plasmodium vivax relapse prevention, when co-administered with 3-days of chloroquine or other blood schizonticide. Tafenoquine 200 mg weekly after a loading dose is also approved as travellers’ prophylaxis. The development of tafenoquine has been conducted over many years, using various dosing regimens in diverse populations. This review brings together all the preclinical and clinical data concerning tafenoquine central nervous system safety. Data were assembled from published sources. The risk of neuropsychiatric adverse events (NPAEs) with single-dose tafenoquine (300 mg) in combination with chloroquine to achieve P. vivax relapse prevention is particularly examined. There was no evidence of neurotoxicity with tafenoquine in preclinical animal models. In clinical studies in P. vivax relapse prevention, nervous system adverse events, mainly headache and dizziness, occurred in 11.4% (36/317) of patients with tafenoquine (300 mg)/chloroquine versus 10.2% (19/187) with placebo/chloroquine; and in 15.5% (75/483) of patients with tafenoquine/chloroquine versus 13.3% (35/264) with primaquine (15 mg/day for 14 days)/chloroquine. Psychiatric adverse events, mainly insomnia, occurred in 3.8% (12/317) of patients with tafenoquine/chloroquine versus 2.7% (5/187) with placebo/chloroquine; and in 2.9% (14/483) of patients with tafenoquine/chloroquine versus 3.4% (9/264) for primaquine/chloroquine. There were no serious or severe NPAEs observed with tafenoquine (300 mg)/chloroquine in these studies. The risk:benefit of single-dose tafenoquine/chloroquine in P. vivax relapse prevention is favourable in the presence of malaria, with a low risk of NPAEs, similar to that seen with chloroquine alone or primaquine/chloroquine.

中文翻译：

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tafenoquine在间日疟原虫复发预防中的神经和精神安全性：综述

Tafenoquine是一种8-氨基喹啉抗疟疾药物，最近与3天的氯喹或其他血型抗裂血药合用时，被批准用于预防间日疟原虫复发的单剂量（300毫克）疗法。负荷剂量后每周200 mg的苯酚喹啉也被批准为旅行者的预防措施。使用不同人群的各种给药方案，已经开展了多年的tafenoquine开发。这篇综述汇集了有关tafenoquine中枢神经系统安全性的所有临床前和临床数据。数据来自公开来源。特别检查了单剂量塔夫诺喹（300 mg）与氯喹联用可预防间日疟原虫复发的神经精神疾病不良事件（NPAEs）的风险。在临床前的动物模型中，没有证据显示他芬喹具有神经毒性。在预防间日疟原虫复发的临床研究中，使用tafenoquine（300 mg）/氯喹的患者中有11.4％（36/317）发生神经系统不良事件，主要是头痛和头晕，而使用安慰剂/安慰剂/复发者发生了10.2％（19/187）。氯喹 tafenoquine / chloroquine的患者占15.5％（75/483），而primaquine（15 mg / day，持续14天）/ chloroquine的患者占13.3％（35/264）。服用tafenoquine / chloroquine的患者发生精神疾病的不良事件主要为失眠，发生率为3.8％（12/317），而使用安慰剂/氯喹的患者发生的不良反应为2.7％（5/187）；tafenoquine / chloroquine的患者占2.9％（14/483），primaquinquin / chloroquine的患者占3.4％（9/264）。在这些研究中，未观察到铁氟喹（300 mg）/氯喹存在严重或严重的NPAE。风险：