Objective: This article overviews the recommended dosing strategies for the treatment of schizophrenia patients using the recently FDA-approved once-monthly long-acting injectable atypical antipsychotic, paliperidone palmitate.
Methods: Using pharmacokinetic (PK), efficacy and safety data from clinical trials and a comprehensive population PK simulation model, dosing recommendations for paliperidone palmitate have been generated.
Results: The recommended initiation regimen is 150 mg eq. paliperidone palmitate (234 mg) on Day 1 followed by 100 mg eq. paliperidone palmitate (156 mg) on Day 8, each administered into the deltoid muscle, using a 1-inch 23 gauge (G) needle in those <90 kg and a 1.5-inch 22 G needle in those > or =90 kg. No oral supplementation is required. Monthly maintenance doses of paliperidone palmitate range from 25-150 mg eq. (39-234 mg; recommended dose of 75 mg eq. [117 mg]) injected into the deltoid (using weight-adjusted needle) or gluteal (using 1.5 inch 22 G needle) muscle. The Day 8 dose may be administered +/-2 days and monthly doses +/-7 days, without a clinically significant impact on plasma concentrations. In patients with mild renal impairment (creatinine clearance [CrCL]: 50-80 mL/min), dosage should be adjusted. No dose adjustment is required in patients with mild or moderate hepatic impairment; no data currently exist regarding severe hepatic impairment. Elderly patients with normal renal function should receive the same dosage as younger adult patients with normal renal function. In the event of an age-related decline in CrCL, dosage should be adjusted accordingly. Paliperidone palmitate treatment can be initiated the day after discontinuing previous oral antipsychotic treatment. Paliperidone palmitate should be initiated at the next scheduled injection, and monthly thereafter, in patients switching from other long-acting injectable antipsychotics, including long-acting risperidone.
Conclusions: These data provide practical guidance to clinicians on how to use paliperidone palmitate in adult patients with schizophrenia.