INVEGA TRINZA PROLONGED RELEASE SUSPENSION FOR IM INJECTION 350MG/1.75ML

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.

Active Ingredient / Synonyms

9-Hydroxyrisperidone | Paliperidone | Ro-76477 | Paliperidone |

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.

Pharmacodynamics

Paliperidone is an atypical antipsychotic developed by Janssen Pharmaceutica. Chemically, paliperidone is primary active metabolite of the older antipsychotic risperidone (paliperidone is 9-hydroxyrisperidone). While its specific mechanism of action is unknown, it is believed paliperidone and risperidone act via similar, if not the same, pathways.

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:

One week following administration of a single oral dose of 1 mg immediate-release 14C-paliperidone to 5 healthy volunteers, 59% (range 51% – 67%) of the dose was excreted unchanged into urine, 32% (26% – 41%) of the dose was recovered as metabolites, and 6% – 12% of the dose was not recovered.

Half-life

The terminal elimination half-life of paliperidone is approximately 23 hours.

Clearance

Not Available

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.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

INVEGA TRINZA PROLONGED RELEASE SUSPENSION FOR IM INJECTION 350MG/1.75ML was registered with Health Science Authority of Singapore by JOHNSON & JOHNSON PTE LTD. It is marketed with the registration number of SIN15188P with effective from 2017-03-06.

This product contains 350mg/0.875ml of Paliperidone in the form of INJECTION, SUSPENSION, EXTENDED-RELEASE.

The medicine was manufactured by Janssen Pharmaceutica NV in BELGIUM

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N05AX13

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