Paliperidone

Paliperidone
Clinical data
Trade namesInvega, Xeplion, Trevicta, others
Other names9-hydroxyrisperidone; PP; PP1M; PP3M; PP6M; JNS-010; RO-92670; RO92670
AHFS/Drugs.comMonograph
MedlinePlusa607005
License data
Pregnancy
category
  • AU: B3
Routes of
administration
By mouth, intramuscular
Drug classAtypical antipsychotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability28% (oral)
Elimination half-life23 hours (by mouth)
Excretion1% unchanged in urine 18% unchanged in feces
Identifiers
  • (RS)-3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.117.604 Edit this at Wikidata
Chemical and physical data
FormulaC23H27FN4O3
Molar mass426.492 g·mol−1
3D model (JSmol)
  • O=C/1N5/C(=N\C(=C\1CCN4CCC(c3noc2cc(F)ccc23)CC4)C)[C@H](O)CCC5
  • InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3/t19-/m1/s1 checkY
  • Key:PMXMIIMHBWHSKN-LJQANCHMSA-N checkY

  • as palmitate: InChI=1S/C39H57FN4O4/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-18-36(45)47-34-17-16-24-44-38(34)41-29(2)32(39(44)46)23-27-43-25-21-30(22-26-43)37-33-20-19-31(40)28-35(33)48-42-37/h19-20,28,30,34H,3-18,21-27H2,1-2H3
  • Key:VOMKSBFLAZZBOW-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

Paliperidone, sold under the brand name Invega among others, is an atypical antipsychotic.[14] It is mainly used to treat schizophrenia and schizoaffective disorder.[14] It is marketed by Janssen Pharmaceuticals.[4]

The most frequent side effects include headache, insomnia (difficulty sleeping), sleepiness, parkinsonism (effects similar to Parkinson's disease such as shaking, muscle stiffness and slow movement), dystonia (involuntary muscle contractions), tremor (shaking), dizziness, akathisia (restlessness), agitation, anxiety, depression, increased weight, nausea, vomiting, constipation, dyspepsia (heartburn), diarrhea, dry mouth, tiredness, toothache, muscle and bone pain, back pain, asthenia (weakness), tachycardia (increased heart rate), high blood pressure, prolonged QT interval (an alteration of the electrical activity of the heart), upper respiratory tract infection (nose and throat infections) and cough.[8]

Paliperidone was approved by the US Food and Drug Administration (FDA) for the treatment of schizophrenia in December 2006,[4] and in the European Union in June 2007.[8] Paliperidone palmitate is a long-acting injectable formulation of paliperidone palmitoyl ester.[14][15] It is on the World Health Organization's List of Essential Medicines.[16] Paliperidone is available as a generic medication.[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 October 22, 2023.
  2. ^ Anvisa (March 31, 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 April 4, 2023). Archived from the original on August 3, 2023. Retrieved August 16, 2023.
  3. ^ "Product monograph brand safety updates". Health Canada. July 7, 2016. Archived from the original on March 29, 2024. Retrieved April 3, 2024.
  4. ^ a b c "Invega- paliperidone tablet, extended release". DailyMed. Archived from the original on January 24, 2016. Retrieved August 19, 2020.
  5. ^ Cite error: The named reference Invega Hafyera FDA label was invoked but never defined (see the help page).
  6. ^ Cite error: The named reference Invega Sustenna FDA label was invoked but never defined (see the help page).
  7. ^ Cite error: The named reference Invega Trinza FDA label was invoked but never defined (see the help page).
  8. ^ a b c "Invega EPAR". European Medicines Agency. June 25, 2007. Archived from the original on January 9, 2021. Retrieved February 1, 2024. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  9. ^ "Byannli EPAR". European Medicines Agency. April 28, 2020. Archived from the original on March 5, 2023. Retrieved March 4, 2023.
  10. ^ "Byannli Product information". Union Register of medicinal products. Archived from the original on March 5, 2023. Retrieved March 3, 2023.
  11. ^ "Trevicta EPAR". European Medicines Agency. December 5, 2014. Archived from the original on February 1, 2024. Retrieved February 1, 2024.
  12. ^ "Xeplion EPAR". European Medicines Agency. March 4, 2011. Archived from the original on February 17, 2024. Retrieved February 1, 2024.
  13. ^ a b "Niapelf EPAR". European Medicines Agency (EMA). March 21, 2024. Archived from the original on February 17, 2024. Retrieved April 5, 2024.
  14. ^ a b c Chue P, Chue J (December 2012). "A review of paliperidone palmitate". Expert Review of Neurotherapeutics. 12 (12): 1383–1397. doi:10.1586/ern.12.137. PMID 23237346. S2CID 36437470.
  15. ^ Edinoff AN, Doppalapudi PK, Orellana C, Ochoa C, Patti S, Ghaffar Y, et al. (2021). "Paliperidone 3-Month Injection for Treatment of Schizophrenia: A Narrative Review". Frontiers in Psychiatry. 12: 699748. doi:10.3389/fpsyt.2021.699748. PMC 8490677. PMID 34621193.
  16. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.

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