Paliperidone

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Paliperidone
Paliperidone.svg
Systematic (IUPAC) name
(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
Clinical data
Trade names Invega
AHFS/Drugs.com monograph
MedlinePlus a607005
Licence data EMA:Link, US FDA:link
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Legal status
Routes of
administration		 Oral (OROS tablets), IM depot injection
Pharmacokinetic data
Bioavailability 28% (oral)
Biological half-life 23 hours (oral)
Identifiers
CAS Number 144598-75-4 YesY
ATC code N05AX13 (WHO)
PubChem CID: 115237
DrugBank DB01267 YesY
ChemSpider 7978307 YesY
UNII 838F01T721 YesY
KEGG D05339 YesY
ChEBI CHEBI:82978 N
ChEMBL CHEMBL1621 N
Chemical data
Formula C23H27FN4O3
Molecular mass 426.484 g/mol
  • 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 YesY
  • Key:PMXMIIMHBWHSKN-LJQANCHMSA-N YesY
 NYesY (what is this?)  (verify)

Paliperidone (trade name Invega), also known as 9-hydroxyrisperidone, is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class of medications. It is developed by Janssen Pharmaceutica. Invega is an extended release formulation of paliperidone that uses the OROS extended release system to allow for once-daily dosing.

Paliperidone palmitate (trade name Invega Sustenna, named Xeplion in Europe and other countries) is a long-acting injectable formulation of paliperidone palmitoyl ester indicated for once-monthly injection after an initial titration period. Paliperidone is used to treat mania and at lower doses as maintenance for bipolar disorder. It is also used for schizophrenia and schizoaffective disorder.

On May 18, 2015 a new formulation of paliperidone palmitate was approved by the FDA under the brand name Invega Trinza.[1] It is a 3-month extended-release injectable suspension suitable for schizophrenic patients after they have been adequately treated with Invega Sustenna for at least four months.[2]

Pharmacology

Paliperidone is the primary active metabolite of the older antipsychotic risperidone.[3] While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not identical, pathways.

Paliperidone has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors.[4] It does not bind to muscarinic acetylcholine receptors. In addition, it binds with dopamine and serotonin receptors.

Paliperidone has less affinity for D4 receptors than risperidone.[5][6]

Paliperidone (as Invega) was approved by the Food and Drug Administration (FDA) for the treatment of schizophrenia in 2006. It is marketed for the treatment of schizophrenia and schizoaffective disorder. Paliperidone was approved by the FDA for the treatment of schizoaffective disorder in 2009. It may also be used off-label for other conditions. Recently, the long-acting injectable form of paliperidone, marketed as Invega Sustenna in U.S. and Xeplion in Europe, was approved by the FDA on July 31, 2009. It was approved in Europe in 2011 for schizophrenia.[7] In Europe the monthly (every 28 days) injection comes in 50 mg, 75 mg, 100 mg, and 150 mg of paliperidone without the 25 mg injection that is available in the U.S. A dose of 75 mg for a month in an injection is the equivalent of 6 mg per day of paliperidone oral. 6 mg of paliperidone oral (Invega) is equivalent to 2 to 3 mg of risperidone.[8]

Effects

Comparison of paliperidone palmitate to risperidone long-acting injection for schizophrenia[9]
Measured outcome Findings in words Findings in numbers Quality of evidence
Recurrence of psychotic symptoms No more likely to have a recurrence of psychotic symptoms with paliperidone palmitate RR 1.23 CI 0.98 to 1.53 Moderate
Lack of efficacy People are 35% more likely to experience lack of efficacy with paliperidone palmitate RR 1.35 CI 1.06 to 1.71
Use of anticholinergic medications 30% less likely to use anticholinergic medications with paliperidone palmitate RR 0.67 CI 0.55 to 0.82

Adverse effects

Adverse effect incidences

Sources:[10][11][12][13]

Very Common (>10% incidence)
  • Headache
  • Tachycardia
  • Somnolence (causes less sedation than most atypical antipsychotics[14])
  • Insomnia
  • Hyperprolactinaemia (seems to cause comparable prolactin elevation to its parent drug, risperidone[14])
Common (1–10% incidence)

Deaths

In April 2014, it was reported that 21 Japanese people who had received shots of the long-acting injectable paliperidone to date had died.[15][16][17][18][19][20][21]

References

  1. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ http://pdsp.med.unc.edu/pdsp.php?knowID=&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=2327&testLigand=&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query[full citation needed]
  6. ↑ http://pdsp.med.unc.edu/pdsp.php?knowID=&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=2328&testLigand=&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query[full citation needed]
  7. ↑ https://www.www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/002105/human_med_001424.jsp&mid=WC0b01ac058001d124&murl=menus/medicines/medicines.jsp&jsenabled=true[full citation needed]
  8. ↑ https://www.invegasustenna.com/invegasustenna/index.html[full citation needed]
  9. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  10. ↑ Truven Health Analytics, Inc. DrugPoint® System (Internet) [cited 2013 Sep 30]. Greenwood Village, CO: Thomsen Healthcare; 2013.
  11. ↑ INVEGA® PRODUCT INFORMATION [Internet]. Janssen Pharmaceuticals; 2013 [cited 2013 Sep 30]. Available from: https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2013-PI-01421-1
  12. ↑ Joint Formulary Committee. British National Formulary (BNF) 65. Pharmaceutical Pr; 2013.
  13. ↑ paliperidone (Rx) - Invega, Invega Sustenna [Internet]. Medscape Reference. [cited 2013 Sep 30]. Available from: http://reference.medscape.com/drug/invega-sustenna-paliperidone-342992#4
  14. ↑ 14.0 14.1 14.2 14.3 Lua error in package.lua at line 80: module 'strict' not found.
  15. ↑ 21 users of schizophrenia drug dead | The Japan Times
  16. ↑ Schizophrénie: controverse autour d'un médicament au Japon | Médecine
  17. ↑ 20 minutes - Un médicament anti-schizophrénie tue - Monde
  18. ↑ Deaths reported after Xeplion injections - Life & Style - NZ Herald News
  19. ↑ 17 deaths reported after schizophrenia drug injections | Japan Today: Japan News and Discussion
  20. ↑ 21 Dead in Japan From New Johnson & Johnson Antipsychotic | Mad In America
  21. ↑ Schizophrenia drug blamed for 17 deaths | Sky News Australia

External links

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