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paliperidone

AntipsychoticLAI available

Brands: INVEGA, INVEGA SUSTENNA, INVEGA TRINZA, INVEGA HAFYERA

Last reviewed 2025-09-23

Reviewed by PsychMed Editorial Team.

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Quick answers

  • What is paliperidone?

    Paliperidone (brand Invega) is the active metabolite of risperidone, delivered as extended-release tablets and long-acting injectable palmitate formulations for schizophrenia and schizoaffective disorder.

  • What is INVEGA?

    INVEGA is a brand name for paliperidone (other brands: INVEGA SUSTENNA, INVEGA TRINZA, INVEGA HAFYERA).

  • What is INVEGA (paliperidone) used for?

    Label indications include: Schizophrenia; schizoaffective disorder.

  • What drug class is INVEGA (paliperidone)?

    Antipsychotic.

  • What is the mechanism of action of INVEGA (paliperidone)?

    D2 and 5‑HT2A antagonism; active metabolite of risperidone.

  • What strengths does INVEGA (paliperidone) come in?

    Paliperidone extended-release (OROS) tablets: 1.5 mg, 3 mg, 6 mg, 9 mg, 12 mg once daily without cyclic titration.

  • Is INVEGA (paliperidone) a controlled substance?

    No — it is not scheduled as a controlled substance under U.S. federal law.

  • What is INVEGA (paliperidone) dosing for schizophrenia?

    Schizophrenia (adults): start 6 mg ER once daily; adjust 3–12 mg/day. Adolescents start 3 mg once daily (max 12 mg/day).

  • How is paliperidone started as a long-acting injectable (LAI)?

    Invega Sustenna: loading 234 mg (day 1 deltoid) and 156 mg (day 8 deltoid) then 39–234 mg monthly (max 234 mg monthly).

Snapshot

  • Class: Antipsychotic
  • Common US brands: INVEGA, INVEGA SUSTENNA, INVEGA TRINZA, INVEGA HAFYERA
  • Long-acting injectable formulation available.
  • Therapeutic drug monitoring not routinely recommended.
  • Last reviewed: 2025-09-23

Label indications

Schizophrenia; schizoaffective disorder.

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Clinical Highlights

Paliperidone (brand Invega) is the active metabolite of risperidone, delivered as extended-release tablets and long-acting injectable palmitate formulations for schizophrenia and schizoaffective disorder. This profile focuses on oral ER use and palmitate LAIs (Sustenna, Trinza, Hafyera) for adherence support.

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  • Paliperidone mechanism of action centers on dopamine D2 and serotonin 5-HT2A antagonism, mirroring risperidone while adding α1/α2 and H1 blockade.
  • Steady plasma levels and LAI options make paliperidone central to relapse prevention; prolactin elevation and weight gain require monitoring.
  • The compare view and the Paliperidone evidence feed can help contextualize switching strategies and LAI conversion planning.
  • Cross-titration and adverse-effect trade-offs overlap with risperidone; the Risperidone profile is a helpful companion reference.
  • Schizophrenia (adults) (FDA 2006)
  • Schizophrenia (adolescents 12–17) (FDA 2011)
  • Schizoaffective disorder (adults) (FDA 2009)

Dosing & Formulations

Paliperidone extended-release (OROS) tablets: 1.5 mg, 3 mg, 6 mg, 9 mg, 12 mg once daily without cyclic titration. Paliperidone palmitate LAIs: Sustenna (39–234 mg monthly), Trinza (273–819 mg quarterly), Hafyera (1,092–1,560 mg every 6 months); max doses 234 mg, 819 mg, and 1,560 mg per interval.

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  • Schizophrenia (adults): start 6 mg ER once daily; adjust 3–12 mg/day. Adolescents start 3 mg once daily (max 12 mg/day).
  • Schizoaffective disorder: initiate 6 mg once daily; adjust 3–12 mg/day as monotherapy or adjunct (max 12 mg/day).
  • Renal impairment: reduce starting dose to 3 mg (CrCl 50–79) or 1.5 mg (CrCl 10–49); avoid if CrCl <10.
  • Invega Sustenna: loading 234 mg (day 1 deltoid) and 156 mg (day 8 deltoid) then 39–234 mg monthly (max 234 mg monthly).
  • The LAI Navigator summarizes PP1M → PP3M → PP6M conversions and overlap planning.

Monitoring & Risks

Boxed warning: Increased mortality in elderly patients with dementia-related psychosis (class warning). Extrapyramidal symptoms: Akathisia/parkinsonism in ~10–20% depending on dose.

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  • Hyperprolactinemia: Galactorrhea, amenorrhea, gynecomastia in 20–30%.
  • Weight gain: ≥7% gain in 5–12% of patients.
  • Tachycardia: Approximately 10% in trials.
  • Somnolence: Around 10% overall.
  • QT prolongation is modest but additive with other QT-active agents—a baseline ECG is often obtained when combining or when cardiac risk factors are present.

Drug Interactions

Strong CYP3A4 or P-gp inducers (carbamazepine, rifampin, St. John’s wort) decrease exposure—avoid or monitor closely. Strong P-gp inhibitors (clarithromycin, verapamil) may increase exposure—monitor for adverse effects.

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  • Concurrent risperidone elevates paliperidone levels; adjust doses if combined.
  • Additive CNS depression with alcohol, benzodiazepines, opioids.
  • May antagonize dopaminergic agents; paliperidone is often avoided in Parkinson’s disease when possible.

Practice Notes

Renal function strongly influences dosing; creatinine clearance is typically assessed at baseline and rechecked periodically. Counseling often covers prolactin-related symptoms and fertility concerns.

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  • Maintain routine metabolic monitoring despite moderate weight gain risk.
  • Manufacturer algorithms are typically used, and oral tolerability is commonly confirmed before LAI initiation.
  • Adherence planning is especially important when transitioning from oral to LAI regimens.
  • When switching from risperidone, dose-equivalence planning and prolactin monitoring are commonly documented; the Risperidone profile can help.
  • LAI planning can be paired with the LAI Navigator, and schizoaffective mood strategies often align with the bipolar disorder hub.

Long-acting injectable (LAI) options

  • Paliperidone palmitate (PP1M/PP3M/PP6M)
    Interval
    Monthly / q3mo / q6mo
    Oral overlap
    None after loading sequence
    Injection site
    Deltoid (initiation) or gluteal
    Notes
    • PP1M loading: Day 1 deltoid 234 mg, Day 8 deltoid 156 mg
    • PP3M/PP6M require stabilization on PP1M/PP3M first

References

  1. INVEGA ER prescribing information — DailyMed / Janssen Pharmaceuticals (2025)
  2. INVEGA SUSTENNA prescribing information — DailyMed / Janssen Pharmaceuticals (2025)
  3. INVEGA TRINZA (paliperidone palmitate) prescribing information — DailyMed / Janssen Pharmaceuticals (2025)
  4. INVEGA HAFYERA (paliperidone palmitate) prescribing information — DailyMed / Janssen Pharmaceuticals (2025)
  5. Efficacy, Safety AND Early Response OF Paliperidone Extended Release Tablets — Schizophrenia Research (2007)
  6. Paliperidone palmitate maintenance treatment in delaying time to relapse in patients with schizophrenia — Schizophrenia Research (2010)
  7. Savitz2016 Paliperidone Pp3m
Paliperidone (INVEGA, INVEGA SUSTENNA +2 more) — Summary — PsychMed