Paliperidone palmitate

Paliperidone

Clinical data
Trade names	Invega
AHFS/Drugs.com	Monograph
MedlinePlus	a607005
License data	EU EMA: Invega US FDA: Paliperidone
Pregnancy category	AU: B3 US: C (Risk not ruled out)
Routes of administration	Oral (OROS tablets), IM depot injection
ATC code	N05AX13 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	28% (oral)
Biological half-life	23 hours (oral)
Identifiers
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
CAS Number	144598-75-4 Y
PubChem CID	115237
DrugBank	DB01267 Y
ChemSpider	7978307 Y
UNII	838F01T721
KEGG	D05339 Y
ChEBI	CHEBI:82978 N
ChEMBL	CHEMBL1621 N
ECHA InfoCard	100.117.604
Chemical and physical data
Formula	C23H27FN4O3
Molar mass	426.484 g/mol
3D model (Jmol)	Interactive image
SMILES O=C/1N5/C(=N\C(=C\1CCN4CCC(c3noc2cc(F)ccc23)CC4)C)[C@H](O)CCC5
InChI 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 Y Key:PMXMIIMHBWHSKN-LJQANCHMSA-N Y
NY (what is this?)

Paliperidone (trade name Invega), also known as 9-hydroxyrisperidone, is a dopamine antagonist and 5-HT_2A antagonist of the atypical antipsychotic class of medications. It is marketed 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-every 28 days injection after an initial titration period. Paliperidone is used to treat mania and at lower doses as maintenance for bipolar disorder. It is also indicated in the US by the FDA 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. A similar 3 -monthly injection of prolonged release suspension was approved in 2016 by the European Medicines Agency originally under the brand name Paliperidone Janssen, later renamed to Trevicta.

Paliperidone is the primary active metabolite of the older antipsychotic risperidone. 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 α₂adrenergic receptors and at H₁ histamine receptors. It does not bind to muscarinic acetylcholine receptors. In addition, it blocks dopamine and serotonin receptors.

Paliperidone has less affinity for D4 receptors than risperidone.