Cited by 126Poisoning and overdose treatmentsPesticide Exposure and ToxicityParaquat toxicity studies and treatments

Acute Human Self‐Poisoning with the N ‐Phenylpyrazole Insecticide Fipronil—a GABA A ‐Gated Chloride Channel Blocker

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Mohamed, Fahim, Senarathna, Lalith, Percy, Adrian, Abeyewardene, Manel, Eaglesham, Geoffrey, Cheng, Ron, Azher, Shifa, Hittarage, Ariyasena +5 more·2004·Journal of Toxicology: Clinical Toxicology

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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Crossref · 10.1081/clt-200041784

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  • Human exposure to fipronil leads to symptoms (headache, nausea and seizures) typically associated with antagonism of GABA_A receptors in the brain.

    “Human exposure to fipronil leads to symptoms (headache, nausea and seizures) typically associated with the antagonism of GABA A receptors in the brain.”

    From The insecticide fipronil and its metabolite fipronil sulphone inhibit the rat α1β2γ2L GABA<sub>A</sub>receptor (2008) · cites this paper as Mohamed et al., 2004

    The Discussion’s “Clinical features of acute human toxicity” section reports nausea and seizures in patients with fipronil poisoning, while “Mechanism of toxicity” says fipronil inhibits GABA-gated chloride channels and binds to GABA_A receptors. The paper does not report headache among the human symptoms, so that part of the attributed symptom list is unsupported. (LLM, conf=0.87)

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Research works printed but not linked: 1

  1. [12]Abeyewardene M, Eaglesham G, Cheng R, Hodge M, O'Brian S. Analysis of fipronil insecticide and its sulphone metabolite in human plasma using LCMSMS. Conference, July 2004, Brisbane, Australia. 2004. Ref Type: Abstract

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Authors
Mohamed, F., Senarathna, L., Percy, A., Abeyewardene, M., Eaglesham, G., Cheng, R., Azher, S., Hittarage, A., Dissanayake, W., Sheriff, M. H. R., Davies, W., Buckley, N. A., & Eddleston, M.
Affiliations
  • South Asian Clinical Toxicology Research Collaboration (LK)
  • Bayer CropScience, Sophia Antipolis Research Center, Santa Antipolis, France
  • Queensland Health (AU)
  • Polonnaruwa General Hospitals, North Central Province, Sri Lanka
  • Anuradhapura General Hospitals, North Central Province, Sri Lanka
  • Bayer (United Kingdom) (GB)
  • South Asian Clinical Toxicology Research Collaboration, Department of Clinical Medicine, University of Colombo, P.O. Box 271, 25 Kynsey Road, Colombo, 08, Sri Lanka
  • University of Oxford (GB)
Venue
Journal of Toxicology: Clinical Toxicology
Published
2004-01
Volume
42
Issue
7
Pages
955-963
ISSN
0731-3810 (ISSN-L)
OpenAlex
W2044819383
Cited by
125
References
24
Citations by year
2026: 2 · 2025: 9 · 2024: 7 · 2023: 4 · 2022: 11 · 2021: 16 · 2020: 3 · 2019: 7 · 2018: 6 · 2017: 9 · 2016: 7 · 2015: 14 · 2014: 4 · 2013: 3 · 2012: 6
FWCI
2.45
Type
journal article
Language
en
Open access
Locations
  • Journal of Toxicology Clinical Toxicology (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
  • ANU Open Research (Australian National University) (submittedVersion)
Funders
  • Wellcome Trust (071669, 063560)
  • Bayer Fund
  • Bayer CropScience
Topics
  • Health Sciences › Medicine › Emergency Medicine › Poisoning and overdose treatments
  • Life Sciences › Agricultural and Biological Sciences › Plant Science › Pesticide Exposure and Toxicity
  • Health Sciences › Medicine › Surgery › Paraquat toxicity studies and treatments
Keywords
fipronil, GABA-A receptor blockade, generalized tonic-clonic seizures, status epilepticus, pharmacokinetics, diazepam, supportive care
MeSH terms
Acute Disease, Adolescent, Adult, Female, Humans, Insecticides, Male, Prospective Studies, Pyrazoles, Receptors, GABA-A, Retrospective Studies, Suicide, Suicide, Attempted, Ion Channel Gating, Occupational Exposure, Fatal Outcome, Chloride Channels

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