Paliperidone

Drugbox
IUPAC_name = 3- [2- [4-(6-fluorobenzo [d] isoxazol-3-yl)-1-piperidyl] ethyl] -7-
hydroxy-4-methyl-1,5-diazabicyclo [4.4.0] deca-3,5-dien-2-one



width = 250
CAS_number= 144598-75-4
ATC_prefix=N05
ATC_suffix=AX13
ATC_supplemental=
PubChem=115237
DrugBank=DB01267
C = 23 | H = 27 | F = 1 | N = 4 | O = 3
molecular_weight = 426.484 g/mol
bioavailability= 28%
metabolism =
elimination_half-life=23 hours
excretion =
pregnancy_category = C
legal_status = Rx-only
routes_of_administration=oral- extended release

Paliperidone (sold as INVEGA) is an atypical antipsychotic 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. Chemically, paliperidone is primary active metabolite of the older atypical antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone, i.e. risperidone with an extra hydroxyl group). It is indicated in the treatment of schizophrenia, as well as manic and mixed episodes occurring in conjunction with Bipolar I Disorder, and depression.

Pharmacology

While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not identical, pathways; therapeutic effect may be due to a combination of D2 and 5-HT2A receptor antagonism. Paliperidone also has antagonist effect at α1 and α2 adrenergic receptors and at H1 histamine receptors. [cite web|url=http://www.prescribingreference.com/products/showProducts/which/Invega|title=Prescribing Reference: New Product Releases - INVEGA|accessdate=2008-05-25]

Paliperidone (as Invega) was approved by the FDA for the treatment of schizophrenia on December 20, 2006. This agent will initially be marketed for the treatment of schizophrenia and then for bipolar mania. Clinical trials of paliperidone for the treatment of schizoaffective disorder are also planned. It may also be used off-label for other conditions. The drug significantly reduces side-effects present in other anti-psychotic drugs formerly used to treat both schizophrenia as well as bipolar disorderFact|date=August 2008. Like risperidone, its possible use in autism and Asperger's syndrome may be studied.

ee also

* Risperidone
* OROS

References

External links

* [http://www.invega.com INVEGA Web site]


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