What is Invega (paliperidone) used for?

Invega (Paliperidone) Uses and Indications

Invega (paliperidone) is primarily indicated for the treatment of schizophrenia in adults and adolescents (ages 12-17), and for the treatment of schizoaffective disorder in adults as both monotherapy and as an adjunct to mood stabilizers and/or antidepressants. 1

Primary FDA-Approved Indications

• Treatment of schizophrenia in adults, with efficacy established in three 6-week trials and one maintenance trial 1
• Treatment of schizophrenia in adolescents (ages 12-17), with efficacy established in one 6-week trial 1
• Treatment of schizoaffective disorder in adults as monotherapy and as an adjunct to mood stabilizers and/or antidepressants, with efficacy established in two 6-week trials 1, 2

Mechanism of Action

• Paliperidone is the active metabolite of risperidone and works primarily through antagonism of dopamine D2 and serotonin 5-HT2A receptors 2
• Available in extended-release (ER) oral formulation that provides stable plasma drug concentrations over a 24-hour period 3
• Also available in long-acting injectable formulations, including a 6-month formulation (Invega Hafyera) 4

Clinical Efficacy in Schizophrenia

• Paliperidone ER 3-12 mg/day significantly improves Positive and Negative Syndrome Scale (PANSS) total scores compared to placebo in patients with acute schizophrenia 3
• Improvement in symptoms can be observed as early as 4 days after treatment initiation in some trials 3
• Effective against both positive and negative symptoms of schizophrenia 3
• In prevention of symptom recurrence, paliperidone ER recipients had significantly longer time to recurrence than placebo recipients 3
• When compared with quetiapine, paliperidone ER was associated with significantly greater improvements in PANSS total scores at 2 weeks and 6 weeks 3

Clinical Efficacy in Schizoaffective Disorder

• Paliperidone is the first agent specifically approved for the treatment of schizoaffective disorder 2
• Efficacy demonstrated in two 6-week, randomized, double-blind, placebo-controlled trials 2
• In flexible-dose trials (3-12 mg/day), paliperidone showed significantly greater improvement in PANSS total scores compared to placebo 2
• In fixed-dose trials, the higher dose range (9-12 mg/day) showed significant improvement over placebo 2

Role in Treatment Algorithms

• Paliperidone can be used as a second-line treatment for schizophrenia when patients do not respond to a D2 partial agonist (like aripiprazole) 5
• In treatment algorithms, paliperidone is considered among the options (along with amisulpride, risperidone, or olanzapine) when switching from a first antipsychotic that was ineffective 5
• Long-acting injectable paliperidone has been associated with a 49% reduction in the risk for psychiatric rehospitalization, making it more effective than oral antipsychotic monotherapy 5

Dosing Considerations

• The recommended starting dose of paliperidone ER in adults is 6 mg/day with no initial dose titration required 6
• Higher doses (up to the maximum recommended dose of 12 mg/day) may provide additional benefit but also increase the risk of adverse reactions 6
• Paliperidone ER may be preferred over risperidone when liver disease, drug-drug interactions, or other alterations in metabolism make appropriate dosing of risperidone difficult to determine 6

Safety and Tolerability

• Most commonly reported adverse events include headache, tremor, dizziness, insomnia, nausea, akathisia, dyspepsia, hypertonia, somnolence, and sedation 2
• Has little effect on plasma glucose, lipid, or insulin levels, but increases plasma prolactin levels over both short and longer-term treatment periods 3
• Clinically significant weight gain can occur in approximately 15% of patients during longer-term treatment 3
• Extrapyramidal symptoms occur in about 25% of patients treated with higher doses (9-12 mg/day) 3

Special Considerations

• When transitioning from long-acting injectable paliperidone to oral formulations, maintaining the same active compound is preferred to minimize risk of relapse 7
• Abrupt discontinuation of long-acting injectable paliperidone without establishing therapeutic levels of oral medication first should be avoided 7
• Close monitoring for signs of psychotic relapse during and after any medication transition is essential 7

Paliperidone's unique pharmacokinetic profile, with renal excretion as the major route of elimination and minimal hepatic metabolism, makes it a useful option for patients with liver disease or those taking medications that might interact with other antipsychotics 6.