Perampanel

Perampanel
Skeletal formula of perampanel
Ball-and-stick model of the perampanel molecule
Clinical data
Trade namesFycompa
Other namesE2007
AHFS/Drugs.comMonograph
MedlinePlusa614006
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth
Drug classAnticonvulsant
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability116%[9]
Protein binding95–96%
MetabolismLiver, mostly via CYP3A4 and/or CYP3A5
Elimination half-life105 hours, 295 hours (moderate hepatic impairment)
Excretion70% faeces, 30% urine
Identifiers
  • 5'-(2-cyanophenyl)-1'-phenyl-2,3'-bipyridinyl-6'(1H)-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.219.846 Edit this at Wikidata
Chemical and physical data
FormulaC23H15N3O
Molar mass349.393 g·mol−1
3D model (JSmol)
  • N#Cc2ccccc2-c1cc(-c4ncccc4)cn(c1=O)-c3ccccc3
  • InChI=1S/C23H15N3O/c24-15-17-8-4-5-11-20(17)21-14-18(22-12-6-7-13-25-22) 16-26(23(21)27)19-9-2-1-3-10-19/h1-14,16H ☒N
  • Key:PRMWGUBFXWROHD-UHFFFAOYSA-N ☒N

  • as hydrate: InChI=1S/4C23H15N3O.3H2O/c4*24-15-17-8-4-5-11-20(17)21-14-18(22-12-6-7-13-25-22)16-26(23(21)27)19-9-2-1-3-10-19;;;/h4*1-14,16H;3*1H2
  • Key:PDWMJDKMSASBNE-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

Perampanel, sold under the brand name Fycompa, is an anti-epileptic medication developed by Eisai Co. that is used in addition to other drugs to treat partial seizures and generalized tonic-clonic seizures for people older than twelve years.[8] It was first approved in 2012, and as of 2016, its optimal role in the treatment of epilepsy relative to other drugs was not clear.[10] It was the first antiepileptic drug in the class of selective non-competitive antagonist of AMPA receptors.[11]

The drug label has a black box warning that the drug may cause serious psychiatric and behavioral changes; it may cause homicidal or suicidal thoughts.[8] Other side effects have included dizziness, somnolence, vertigo, aggression, anger, loss of coordination, blurred vision, irritability, and slurred speech.[8] Perampanel reduced the effectiveness of levonorgestrel oral contraceptives by about 40%.[8] Women who may get pregnant should not take it as studies in animals show it may harm a fetus.[12] Perampanel is liable to be abused; very high doses produced euphoria responses similar to ketamine.[8] It is designated as a Schedule III controlled substance by the Drug Enforcement Administration.[8]

As of August 2016 perampanel had been studied and development discontinued in migraine, multiple sclerosis, neuropathic pain, and Parkinson's disease.[13]

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  2. ^ "AusPAR: Perampanel hemisesquihydrate". Therapeutic Goods Administration (TGA). 10 May 2021. Retrieved 12 June 2021.
  3. ^ "TGA eBS - Product and Consumer Medicine Information Licence".
  4. ^ "Fycompa". NPS MedicineWise. 15 July 2021. Retrieved 19 February 2022.
  5. ^ "Prescription medicines: registration of new chemical entities in Australia, 2014". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  6. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  7. ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  8. ^ a b c d e f g "Fycompa- perampanel tablet Fycompa- perampanel suspension". DailyMed. Retrieved 12 June 2021.
  9. ^ Yang X, Wu TC, Yuxin MA, Lee JY, Bhattaram VA, Mehta MU. "U.S. FDA Clinical Pharmacology Review. Fycompa (perampanel)" (PDF): 25. {{cite journal}}: Cite journal requires |journal= (help)
  10. ^ Besag FM, Patsalos PN (2016). "Clinical efficacy of perampanel for partial-onset and primary generalized tonic-clonic seizures". Neuropsychiatric Disease and Treatment. 12: 1215–20. doi:10.2147/NDT.S83842. PMC 4876101. PMID 27274257. S2CID 14176469.
  11. ^ Chong DJ, Lerman AM (April 2016). "Practice Update: Review of Anticonvulsant Therapy". Current Neurology and Neuroscience Reports. 16 (4): 39. doi:10.1007/s11910-016-0640-y. PMID 26984292. S2CID 9090302.
  12. ^ EMA Summary of Product Characteristics Archived 20 September 2018 at the Wayback Machine. "Index pagel". 17 September 2018. Archived from the original on 20 June 2018. Retrieved 21 August 2012.
  13. ^ "Perampanel". AdisInsight. Retrieved 29 August 2016.