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Paliperidone

Generic Name
Paliperidone
Brand Names
Invega, Invega Hafyera, Xeplion, Niapelf, Byannli (previously Paliperidone Janssen-Cilag International), Trevicta (previously Paliperidone Janssen), ERZOFRI
Drug Type
Small Molecule
Chemical Formula
C23H27FN4O3
CAS Number
144598-75-4
Unique Ingredient Identifier
838F01T721

Overview

Paliperidone is the primary active metabolite of risperidone. The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone. 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. It is available as an extended-release tablet, a once-monthly intramuscular injection, an every-three-month intramuscular injection, and a twice-yearly gluteal injection.

Background

Paliperidone is the primary active metabolite of risperidone. The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone. 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. It is available as an extended-release tablet, a once-monthly intramuscular injection, an every-three-month intramuscular injection, and a twice-yearly gluteal injection.

Indication

As an oral extended-release tablet and a once-monthly extended-release suspension for intramuscular injection, paliperidone is indicated for the treatment of adults and adolescents with schizophrenia and in the treatment of schizoaffective disorder in combination with antidepressants or mood stabilizers. Paliperidone is also available in both an every-three-month and twice-yearly extended-release suspension for intramuscular injection for the treatment of schizophrenia.

Associated Conditions

  • Schizoaffective Disorders
  • Schizophrenia

FDA Approved Products

PALIPERIDONE
Manufacturer:Inventia Healthcare Limited
Route:ORAL
Strength:3 mg in 1 1
Approved: 2019/06/25
NDC:49252-033
Paliperidone
Manufacturer:Tris Pharma Inc
Route:ORAL
Strength:6 mg in 1 1
Approved: 2022/10/07
NDC:27808-224
PALIPERIDONE
Manufacturer:Inventia Healthcare Limited
Route:ORAL
Strength:6 mg in 1 1
Approved: 2019/06/25
NDC:49252-034
INVEGA
Manufacturer:Janssen Pharmaceuticals, Inc.
Route:ORAL
Strength:9 mg in 1 1
Approved: 2023/08/23
NDC:50458-552
INVEGA TRINZA
Manufacturer:Janssen Pharmaceuticals, Inc
Route:INTRAMUSCULAR
Strength:819 mg in 2.63 mL
Approved: 2021/08/20
NDC:50458-609

Singapore Approved Products

INVEGA TRINZA PROLONGED RELEASE SUSPENSION FOR IM INJECTION 263MG/1.315ML
Manufacturer:Janssen Pharmaceutica NV, Beerse
Form:INJECTION, SUSPENSION, EXTENDED RELEASE
Strength:263mg/1.315ml
Online:Yes
Approved: 2017/03/06
Approval:SIN15187P
INVEGA Sustenna Prolonged Release Suspension for IM Injection 100mg/1.0ml
Manufacturer:Janssen Pharmaceutica N.V.,, Cilag AG
Form:INJECTION, SUSPENSION, EXTENDED RELEASE
Strength:100mg/1ml
Online:Yes
Approved: 2011/06/13
Approval:SIN13971P
Invega Extended-Release Tablet 6mg
Manufacturer:JANSSEN CILAG MANUFACTURING LLC
Form:TABLET, EXTENDED RELEASE
Strength:6mg
Online:Yes
Approved: 2007/12/07
Approval:SIN13381P
INVEGA TRINZA PROLONGED RELEASE SUSPENSION FOR IM INJECTION 175MG/0.875ML
Manufacturer:Janssen Pharmaceutica NV, Beerse
Form:INJECTION, SUSPENSION, EXTENDED RELEASE
Strength:175mg/0.875ml
Online:Yes
Approved: 2017/03/06
Approval:SIN15186P
Invega Extended-Release Tablet 3mg
Manufacturer:JANSSEN CILAG MANUFACTURING LLC
Form:TABLET, EXTENDED RELEASE
Strength:3mg
Online:Yes
Approved: 2007/12/07
Approval:SIN13380P

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