Acute human self-poisoning with the N-phenylpyrazole insecticide fipronil--a GABAA-gated chloride channel blocker.

Fahim Mohamed, Lalith Senarathna, Adrian Percy, Manel Abeyewardene, Geoffrey Eaglesham, Ron Cheng, Shifa Azher, Ariyasena Hittarage, Wasantha Dissanayake, M H Rezvi Sheriff, Willie Davies, Nick A Buckley, Michael Eddleston
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引用次数: 105

Abstract

Objective: Fipronil, a broad spectrum N-phenylpyrazole insecticide that inhibits GABAA-gated chloride channels, has been in use since the mid-1990s. A high affinity for insect compared to mammalian GABA receptors results in lower animal toxicity than other insecticides blocking this channel. To date, only two accidental cases of fipronil poisoning in humans have been published.

Case series: We report seven patients with fipronil self-poisoning seen prospectively in Sri Lanka together with pharmacokinetics for four patients. Non-sustained generalized tonic-clonic seizures were seen in two patients (peak measured plasma fipronil concentrations 1600 and 3744 microg/L); both were managed with diazepam without complications. A patient with a peak measured plasma concentration of 1040 microg/L was asymptomatic throughout his stay. Plasma concentration was still high at discharge 3-4 days post-ingestion when the patients were well. Retrospective review of >1000 pesticide poisoning deaths since 1995 found only one death from fipronil-based products. In contrast to the good outcome of the above cases, this patient required intubation and ventilation and had continuous fits despite therapy with barbiturates and benzodiazepines.

Conclusions: Our experience with prospectively observed patients suggests that fipronil poisoning is characterized by vomiting, agitation, and seizures, and normally has a favorable outcome. Management should concentrate on supportive care and early treatment of seizures. However, further experience is needed to determine whether increased susceptibility to fipronil or larger doses can produce status epilepticus.

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氨基丁酸门控氯通道阻滞剂n -苯吡唑类杀虫剂氟虫腈的急性人体自中毒。
目的:氟虫腈是一种广谱n -苯吡唑类杀虫剂,可抑制gabaa -门控氯通道,自20世纪90年代中期以来一直被使用。与哺乳动物GABA受体相比,其对昆虫的亲和力较高,因此与阻断该通道的其他杀虫剂相比,其对动物的毒性较低。迄今为止,只发表了两起氟虫腈人体意外中毒病例。病例系列:我们报告了斯里兰卡的7例氟虫腈自我中毒患者以及4例患者的药代动力学。2例患者出现非持续性全身性强直-阵挛性癫痫发作(测定的氟虫腈血浆浓度峰值为1600和3744微克/升);两例患者均使用安定治疗,无并发症。患者血药浓度峰值为1040微克/升,在住院期间无症状。服药后3 ~ 4 d出院时血药浓度仍高,患者健康。对1995年以来超过1000例农药中毒死亡的回顾性审查发现,只有一例死亡来自氟虫腈产品。与上述病例的良好结果相反,该患者需要插管和通气,尽管使用巴比妥类药物和苯二氮卓类药物治疗,但仍持续发作。结论:我们对前瞻性观察患者的经验表明,氟虫腈中毒以呕吐、躁动和癫痫发作为特征,通常具有良好的预后。管理应侧重于支持性护理和癫痫发作的早期治疗。然而,需要进一步的经验来确定增加对氟虫腈的易感性或大剂量是否会产生癫痫持续状态。
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