Chemistry:Paliperidone palmitate

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Short description: Chemical compound
Paliperidone palmitate
Paliperidone palmitate.svg
Clinical data
Trade namesInvega Hayfera, Invega Sustenna, Invega Trinza, others
Other namesPP; PP1M; PP3M; PP6M; JNS-010; RO-92670; RO92670
MedlinePlusa607005
License data
Routes of
administration		Intramuscular
Drug classAtypical antipsychotic
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC39H57FN4O4
Molar mass664.907 g·mol−1
3D model (JSmol)

Paliperidone palmitate (PP), sold under the brand name Invega Sustenna among others, is an atypical antipsychotic which is used in the treatment of schizophrenia and schizoaffective disorder.[1][6][7] It is an antipsychotic ester – specifically the palmitate ester of paliperidone – and acts as a long-lasting form of paliperidone.[7] Paliperidone palmitate is formulated as an aqueous suspension, has a strong smell similar to alcohol, and is administered by intramuscular injection into deltoid or gluteal muscle once every 1, 3, or 6 months depending on the formulation.[7][8][6] A formulation for injection once every 6 months is also pending regulatory approval as of September 2021.[6][9]

With the once-monthly formulation of paliperidone palmitate, the time to peak is 13 days and the elimination half-life is 25 to 49 days, and with the 3-month formulation, the time to peak is 30 to 33 days and the half-life is 84 to 95 days via deltoid muscle and 118 to 139 days gluteally.[10] The peak-to-trough ratio of paliperidone palmitate at steady state ranges from 1.56 to 1.70 with the 1- and 3-month formulations.[10] The 3-month formulation of paliperidone palmitate has larger crystal sizes than the 1-month formulation and this allows for its longer duration.[11] No pharmacokinetic data for the 6-month formulation has been released as of January 2021.[11]


References

  1. ↑ 1.0 1.1 "Invega Sustenna- paliperidone palmitate injection". 31 January 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1af14e42-951d-414d-8564-5d5fce138554. 
  2. ↑ "Invega Trinza- paliperidone palmitate injection, suspension, extended release". 31 January 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c39e65d7-fa44-4e4c-8b12-a654d3ed0eae. 
  3. ↑ "Invega Hafyera- paliperidone palmitate injection, suspension, extended release". https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6cd61892-d2cb-434d-83ed-5c1b2c4e7a0b. 
  4. ↑ "Byannli EPAR". 28 April 2020. https://www.ema.europa.eu/en/medicines/human/EPAR/byannli-previously-paliperidone-janssen-cilag-international. 
  5. ↑ "Byannli Product information". https://ec.europa.eu/health/documents/community-register/html/h1453.htm. 
  6. ↑ 6.0 6.1 6.2 "Paliperidone palmitate - Johnson & Johnson - AdisInsight". https://adisinsight.springer.com/drugs/800040526. 
  7. ↑ 7.0 7.1 7.2 "A review of paliperidone palmitate". Expert Rev Neurother 12 (12): 1383–97. December 2012. doi:10.1586/ern.12.137. PMID 23237346. 
  8. ↑ "Paliperidone 3-Month Injection for Treatment of Schizophrenia: A Narrative Review". Front Psychiatry 12: 699748. 2021. doi:10.3389/fpsyt.2021.699748. PMID 34621193. 
  9. ↑ Peitl, Vjekoslav; Vlahović, Darko (1 June 2021). "Paliperidone Palmitate 6-month (PP6M)". Archives of Psychiatry Research 57 (2): 229–232. doi:10.20471/dec.2021.57.02.13. ISSN 2671-1079. 
  10. ↑ 10.0 10.1 "Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview". CNS Drugs 35 (1): 39–59. January 2021. doi:10.1007/s40263-020-00779-5. PMID 33507525. 
  11. ↑ 11.0 11.1 "Therapeutic Drug Monitoring of Long-Acting Injectable Antipsychotic Drugs". Ther Drug Monit 43 (1): 79–102. February 2021. doi:10.1097/FTD.0000000000000830. PMID 33196621. 

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