Chemistry:Imepitoin

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Imepitoin (INN), sold under the brand name Pexion, is an anticonvulsant which is used in veterinary medicine in Europe to treat epilepsy in dogs.[1][2][3][4] It was approved in the United States for veterinary use in December 2018.[5] The drug also has anxiolytic effects.[1][2] It was originally developed to treat epilepsy in humans, but clinical trials were terminated upon findings of unfavorable metabolic differences in smokers and non-smokers.[1][2]

Imepitoin acts as a low-affinity (4,350–5,140 nM; relative to Ki = 6.8 nM for diazepam and Ki = 1.7 nM for clonazepam) partial agonist of the benzodiazepine site of the GABAA receptor (up to 12–21% of the maximal potentiation of diazepam, a full agonist of this site).[1] It is the first partial agonist to be approved for the treatment of epilepsy.[1] The drug also dose-dependently blocks voltage-gated calcium channels.[3] It is not a benzodiazepine; instead, it is an imidazolone, and bears some structural similarities to hydantoin anticonvulsants like ethotoin and phenytoin.[1]

See also

  • Separation anxiety in dogs § Benzodiazepine treatment

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "The pharmacology of imepitoin: the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy". CNS Drugs 28 (1): 29–43. 2014. doi:10.1007/s40263-013-0129-z. PMID 24357084. 
  2. ↑ 2.0 2.1 2.2 "Antiseizure Medications". Seizures in Dogs and Cats. Wiley. 29 April 2015. pp. 209–. ISBN 978-1-118-68970-7. https://books.google.com/books?id=BoXgCAAAQBAJ&pg=PA209. 
  3. ↑ 3.0 3.1 "Seizures and Narcolepsy". Practical Guide to Canine and Feline Neurology. Wiley. 8 September 2015. pp. 259. ISBN 978-1-119-06204-2. https://books.google.com/books?id=JSWJCgAAQBAJ&pg=PT259. 
  4. ↑ "Imepitoin". drugs.com. https://www.drugs.com/international/imepitoin.html. 
  5. ↑ "Original New Animal Drug Application". https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downloadFoi/5907. 



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