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Paliperidone

INVEGA

What it isD2 and 5-HT2A antagonist and active risperidone metabolite; schizophrenia and schizoaffective disorder.

Why it mattersIts long-acting injections offer the longest maintenance intervals available in psychiatry.

What it changesRenal clearance requires dose adjustment in CKD. Prolactin elevation, EPS, and QT prolongation can end treatment.

FDA-approved for

FDA label

BOXED WARNING Increased mortality in elderly patients with dementia-related psychosis; not approved for dementia-related psychosis.
FDA dosingPopulationStartTargetMax
SchizophreniaAdults6 mg QD3–12 mg QD12 mg QD
SchizophreniaAdolescents 12–17 yr3 mg QD3–12 mg QD (wt-dependent)6 mg (<51 kg) / 12 mg (≥51 kg) QD
Schizoaffective disorderAdults6 mg QD3–12 mg QD12 mg QD

Titration >5 days between increases (>4 days for schizoaffective); 3 mg/day increments

Renal Mild (CrCl 50–<80): start 3 mg QD, max 6 mg QD. Moderate–severe (CrCl 10–<50): 3 mg QOD or 1.5 mg QD, max 3 mg QD. CrCl <10: not recommended.

Hepatic Mild–moderate (Child-Pugh A/B): no adjustment. Severe: not studied.

Instructions

Cautions

Adverse reactions

Pregnancy Third-trimester exposure risks neonatal EPS/withdrawal symptoms; no clearly established increased malformation risk.

Lactation Present in human milk; monitor infant for sedation, failure to thrive, jitteriness, EPS.

⚠ BOXED WARNING

Cost, est. cash$5–$150/month

Generic entry2015

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability2 / 4
Sedation liability2 / 4
QT / Torsades2 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.

Mechanism of action: Paliperidone ballicule

Paliperidone ballicule: receptor binding, kinetics and half-life diagram

Open Paliperidone in the interactive console ↗

Memory aids: mascots and interaction avatars

Paliperidone INVEGA mascot mnemonic cartoon
“Pale lips In Vegas”
Spooky mascot → antipsychotic
Variation of risperidone Frankenstein mascot → paliperidone is active metabolite
Paliperidone Box: minimal PK interactions avatar
Box: minimal PK interactions

Open Paliperidone in the interactive console ↗