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Paliperidone palmitate LAI

INVEGA SUSTENNA

What it isLong-acting D2 and 5-HT2A antagonist; maintenance treatment of schizophrenia and schizoaffective disorder.

Why this oneIts deltoid loading regimen on days 1 and 8 means no oral overlap at all; it is the only LAI labeled for schizoaffective disorder.

What limits itPaliperidone is renally cleared, so dosing falls with kidney impairment, and prolactin elevation is the class-typical liability.

FDA label

BOXED WARNING Increased mortality in elderly patients with dementia-related psychosis treated with antipsychotic drugs.
FDA dosingPopulationStartTargetMax
Schizophreniaadults234 mg deltoid Day 1, 156 mg deltoid Day 8117 mg monthly (39–234 mg)234 mg monthly
Schizoaffective disorder (monotherapy or adjunct)adults234 mg deltoid Day 1, 156 mg deltoid Day 878–234 mg monthly234 mg monthly

Titration Maintenance dose adjustments may be made monthly.

Renal Mild (CrCl 50–<80): 156 mg Day 1, 117 mg Day 8, then 78 mg monthly (max 156 mg monthly). Moderate–severe (CrCl <50): not recommended.

Hepatic No adjustment for mild–moderate; not studied in severe.

Prolonged-release; full effect of a dose change may not be evident for several months.

Instructions

Cautions

Adverse reactions

Pregnancy No established drug-associated risk of major birth defects; third-trimester exposure risks extrapyramidal and/or withdrawal symptoms in neonates.

Lactation Paliperidone present in breast milk; monitor infant for sedation, failure to thrive, jitteriness, and extrapyramidal symptoms.

⚠ BOXED WARNING

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: Paliperidone palmitate LAI ballicule

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

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