Product Information
Registration Status: ActiveINVEGA SUSTENNA PROLONGED RELEASE SUSPENSION FOR IM INJECTION 150MG/1.5ML is approved to be sold in Singapore with effective from 2011-06-13. It is marketed by JOHNSON & JOHNSON PTE LTD, with the registration number of SIN13972P.
This product contains Paliperidone 150mg/1.5ml in the form of INJECTION, SUSPENSION, EXTENDED-RELEASE. It is approved for INTRAMUSCULAR use.
This product is manufactured by Janssen Pharmaceutica N.V. in SWITZERLAND, and in BELGIUM.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Paliperidone is the primary active metabolite of the older antipsychotic risperidone. While its specific mechanism of action is unknown, it is believed that paliperidone and risperidone act via similar if not the same pathways. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006.
Indication
For the treatment of schizophrenia.
Mechanism of Action
Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone, as with other drugs having efficacy in schizophrenia, is unknown, but it has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism.
Pharmacokinetics
- Absorption
- The absolute oral bioavailability of paliperidone following paliperidone administration is 28%.
- Distribution
- * 487 L
- Metabolism
- Although in vitro studies suggested a role for CYP2D6 and CYP3A4 in the metabolism of paliperidone, in vivo results indicate that these isozymes play a limited role in the overall elimination of paliperidone. Four primary metabolic pathways have been identified in vivo, none of which could be shown to account for more than 10% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Paliperidone does not undergo extensive metabolism and a significant portion of its metabolism occurs in the kidneys.
- Elimination
Toxicity
The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis.
Active Ingredient/Synonyms
9-Hydroxyrisperidone | Paliperidone | Ro-76477 | Paliperidone |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.