From the FDA Drug Label
The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for paliperidone and any potential adverse effects on the breastfed child from paliperidone or from the mother's underlying condition Limited data from published literature report the presence of paliperidone in human breast milk In a study in which juvenile rats were treated with oral paliperidone from days 24 to 73 of age, a reversible impairment of performance in a test of learning and memory was seen, in females only, with a no-effect dose of 0. 63 mg/kg/day, which produced plasma levels (AUC) of paliperidone similar to those in adolescents at MRHD of 12 mg/day.
The FDA drug label does not answer the question about paliperidone levels.
From the Research
Paliperidone levels should be monitored regularly in patients receiving this antipsychotic medication, with therapeutic plasma concentrations typically ranging from 20-60 ng/mL. For patients starting paliperidone, baseline levels should be obtained after reaching steady state (approximately 4-5 days for oral formulations or after the second injection for long-acting injectable forms) 1. Follow-up monitoring is recommended every 3-6 months during stable treatment and whenever there are concerns about efficacy, adherence, or side effects. Dose adjustments may be necessary based on clinical response and measured levels, with particular attention needed in patients with renal impairment, as paliperidone is primarily excreted unchanged by the kidneys.
Key Considerations
- Levels above the therapeutic range may increase the risk of side effects like extrapyramidal symptoms, QT prolongation, and metabolic disturbances, while subtherapeutic levels may result in inadequate symptom control 2.
- When interpreting results, it's essential to consider the timing of the blood draw relative to medication administration, with trough levels (taken just before the next scheduled dose) providing the most consistent and useful information for clinical decision-making 3.
- The recommended initiation regimen for paliperidone palmitate is 150 mg eq. paliperidone palmitate on day 1, followed by 100 mg eq. paliperidone palmitate on day 8, with monthly maintenance doses ranging from 25-150 mg eq. 1, 4.
- In patients with mild renal impairment, dosage should be adjusted, and no dose adjustment is required in patients with mild or moderate hepatic impairment 1, 5.
Monitoring and Dose Adjustment
- Regular monitoring of paliperidone levels is crucial to ensure therapeutic efficacy and minimize the risk of adverse effects.
- Dose adjustments should be made based on clinical response and measured levels, taking into account factors such as renal impairment and hepatic function.
- The most recent and highest quality study 5 provides guidance on switching from paliperidone palmitate 1 monthly to 3 monthly formulation in schizophrenia, recommending a 3.5-fold multiple of the last PP1M dose for the first injection of PP3M.