User:Mr. Ibrahem/Asenapine

From Wikipedia, the free encyclopedia
Mr. Ibrahem/Asenapine
Skeletal formula of asenapine
Ball-and-stick model of the asenapine molecule
Clinical data
Trade namesSaphris, Sycrest, Secuado, others
Other namesAsenapine maleate, ORG-5222
AHFS/Drugs.comMonograph
MedlinePlusa610015
License data
Pregnancy
category
  • AU: C
Routes of
administration		Under the tongue
Drug classAtypical antipsychotic
Legal status
Legal status
Pharmacokinetic data
Bioavailability35% (sublingual), <2% (by mouth)[3][4][1][5]
Protein binding95%[3][4][1][5]
Metabolismhepatic (glucurinodation by UGT1A4 and oxidative metabolism by CYP1A2)[3][4][1][5]
Elimination half-life24 hours[3][4][1][5]
ExcretionKidney (50%), Faecal (40%; ~5–16% as unchanged drug in faeces)[3][4][1][5]
Identifiers
  • (3aRS,12bRS)-rel-5-Chloro-2,3,3a,12b-tetrahydro-
    2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole
Chemical and physical data
FormulaC17H16ClNO
Molar mass285.77 g·mol−1
3D model (JSmol)
  • Clc4cc2c(Oc1c(cccc1)[C@@H]3CN(C[C@@H]23)C)cc4
  • InChI=1S/C17H16ClNO/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19/h2-8,14-15H,9-10H2,1H3/t14-,15-/m0/s1 checkY
  • Key:VSWBSWWIRNCQIJ-GJZGRUSLSA-N checkY

  • as salt: InChI=1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,15-;/m1./s1
  • Key:GMDCDXMAFMEDAG-CHHFXETESA-N
 ☒NcheckY (what is this?)  (verify)

Asenapine, sold under the brand name Saphris among others, is an atypical antipsychotic used to treat schizophrenia and mania in bipolar disorder.[6][2] Use in older people with dementia related psychosis may increase the risk of death.[6] It is used under the tongue.[7]

Common side effects include sleepiness, dizziness, weight gain, movement disorders, and numbness within the mouth.[6] Other side effects may include stroke, neuroleptic malignant syndrome, tardive dyskinesia, diabetes, low white blood cells, seizures, and QT prolongation.[6] How it works is not clear, but is believed to involve blocking serotonin and dopamine receptors.[2]

Asenapine was approved for medical use in the United States in 2009 and Europe in 2010.[6][2] The first generic versions were approved in 2020.[8] In the United Kingdom it costs the NHS about £100 per month as of 2021.[9] This amount in the United States is about 200 USD.[10]

References[edit]

  1. ^ a b c d e f "Sycrest 5mg sublingual tablets - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 23 September 2020. Retrieved 9 September 2020.
  2. ^ a b c d e "Sycrest EPAR". European Medicines Agency (EMA). Archived from the original on 15 August 2020. Retrieved 9 September 2020.
  3. ^ a b c d e "Product Information Saphris (asenapine maleate)" (PDF). TGA eBusiness Services. Merck Sharp & Dohme (Australia) Pty Limited. 14 January 2013. Archived from the original on 2 April 2019. Retrieved 23 October 2013.
  4. ^ a b c d e "Saphris (asenapine maleate) tablet". DailyMed. Organon Pharmaceuticals. March 2013. Archived from the original on 3 December 2013. Retrieved 23 October 2013.
  5. ^ a b c d e "Product information Sycrest – EMEA/H/C/001177 –II/0012" (PDF). European Medicines Agency. N.V. Organon. 21 February 2013. Archived (PDF) from the original on 28 July 2017. Retrieved 23 October 2013.
  6. ^ a b c d e f g "DailyMed - SAPHRIS- asenapine maleate tablet". dailymed.nlm.nih.gov. Archived from the original on 13 November 2021. Retrieved 16 January 2022.
  7. ^ "Asenapine". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Archived from the original on 16 January 2022. Retrieved 16 January 2022.
  8. ^ Research, Center for Drug Evaluation and (23 February 2021). "2020 First Generic Drug Approvals". FDA. Archived from the original on 26 September 2021. Retrieved 16 January 2022.
  9. ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 376. ISBN 978-0857114105.
  10. ^ "Asenapine Prices, Coupons & Savings Tips". GoodRx. Archived from the original on 23 October 2016. Retrieved 16 January 2022.
Retrieved from "https://en.wikipedia.org/w/index.php?title=User:Mr._Ibrahem/Asenapine&oldid=1102296507"