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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:ANI Pharmaceuticals, Inc.
Route:ORAL
Strength:1.5 mg in 1 1
Approved: 2023/06/30
NDC:43975-349
INVEGA SUSTENNA
Manufacturer:Janssen Pharmaceuticals, Inc.
Route:INTRAMUSCULAR
Strength:156 mg in 1 mL
Approved: 2022/07/31
NDC:50458-563
Paliperidone
Manufacturer:Lupin Pharmaceuticals, Inc.
Route:ORAL
Strength:3 mg in 1 1
Approved: 2023/12/29
NDC:68180-524
Paliperidone
Manufacturer:Amneal Pharmaceuticals LLC
Route:ORAL
Strength:6 mg in 1 1
Approved: 2022/11/20
NDC:65162-282
PALIPERIDONE
Manufacturer:Ascent Pharmaceuticals, Inc.
Route:ORAL
Strength:3 mg in 1 1
Approved: 2023/08/28
NDC:43602-295

Singapore Approved Products

INVEGA Sustenna Prolonged Release Suspension for IM Injection 150mg/1.5ml
Manufacturer:Janssen Pharmaceutica N.V.,, Cilag AG
Form:INJECTION, SUSPENSION, EXTENDED RELEASE
Strength:150mg/1.5ml
Online:Yes
Approved: 2011/06/13
Approval:SIN13972P
INVEGA Sustenna Prolonged Release Suspension for IM Injection 50mg/0.5 ml
Manufacturer:Janssen Pharmaceutica N.V.,, Cilag AG
Form:INJECTION, SUSPENSION, EXTENDED RELEASE
Strength:50mg/0.5ml
Online:Yes
Approved: 2011/06/13
Approval:SIN13969P

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