Trade names Invega MedlinePlus a607005 Molar mass 426.484 g/mol | AHFS/Drugs.com Monograph CAS ID 144598-75-4 | |
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License data EU EMA: InvegaUS FDA: Paliperidone Pregnancycategory AU: B3US: C (Risk not ruled out) Routes ofadministration Oral (OROS tablets), IM depot injection | ||
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 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.
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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.
Pharmacology
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 α2 adrenergic 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.
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. 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.
Adverse effect incidences
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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.