Summary

• Always check the needle hub for signs of damage or leakage after attaching the needle to the syringe using a gentle twisting motion. A cracked needle hub can result in leakage of the medication and incomplete administration of the dose.¹
• During administration of INVEGA SUSTENNA, slowly inject the entire contents intramuscularly (IM) into the selected deltoid or gluteal muscle of the patient. Do not administer by any other route.^1,2
• INVEGA SUSTENNA is a suspension, and the syringe is not calibrated. Therefore, administration of INVEGA SUSTENNA should be in a single injection. Do not administer the dose in divided injections.^1,2
• No systematically collected clinical data is available on administering 2 separate injections of INVEGA SUSTENNA.
• Pharmacokinetic (PK) modeling simulations have been conducted to predict plasma concentrations when giving INVEGA SUSTENNA 234 mg in 2 divided doses.³

DOSAGE STRENGTH INFORMATION

Doses of paliperidone palmitate extended-release injectable suspension may be expressed in milligram equivalents of paliperidone (active moiety) or milligrams of paliperidone palmitate. Dosage information in this response has been converted to mg of paliperidone palmitate to reflect the commercially available dosage strengths in the United States. The conversion factor from mg eq to mg is 1.56.

• INVEGA SUSTENNA doses expressed as 39, 78, 117, 156, and 234 mg of paliperidone palmitate are equal to 25, 50, 75, 100, and 150 mg eq of paliperidone, respectively.

ADMINISTRATION OF INVEGA SUSTENNA 234 MG AS SIMULTANEOUS 156 MG AND 78 MG INJECTION

No systematically collected data is available on using INVEGA SUSTENNA 156 mg and 78 mg in place of an INVEGA SUSTENNA 234 mg injection. Table: Expected Change in Median Peak and Trough Paliperidone Plasma Concentrations After Conversion from INVEGA SUSTENNA 234 mg to 156 mg + 78 mg, depicts the expected change in median peak and trough plasma concentrations via PK simulation for the first 3 cycles after conversion from 1 INVEGA SUSTENNA 234 mg to separate INVEGA SUSTENNA 156 mg and 78 mg simultaneous injections.³ These simulated increases in plasma paliperidone concentrations are less than the intrasubject variability seen in clinical trials.

The PK simulation below depicts the expected paliperidone plasma concentration for simulated subjects receiving INVEGA SUSTENNA 234 mg at steady-state, including after conversion to simultaneous INVEGA SUSTENNA 156 mg and 78 mg injections. In Figure: 90% Prediction Interval for Conversion from INVEGA SUSTENNA 234 mg to 156 mg + 78 mg Injections, all simulated subjects received INVEGA SUSTENNA 234 mg at 12, 8, and 4 weeks before time zero. The red line depicts the median expected paliperidone plasma concentration in subjects who continued to receive the 234 mg dose every 4 weeks. The black line depicts the median expected paliperidone plasma concentration in subjects who received separate injections of INVEGA SUSTENNA 156 mg and 78 mg at week 0, week 4, and week 8. The shaded region depicts the 90% prediction interval of paliperidone plasma concentrations for the 2 dosing regimens. It is expected that 90% of subjects will fall within this range.

ADMINISTRATION OF INVEGA SUSTENNA 234 MG AS 2 SIMULTANEOUS 117 MG INJECTIONS

No systematically collected data is available on administering 2 simultaneous injections of INVEGA SUSTENNA 117 mg. Table: Expected Change in Median Peak and Trough Paliperidone Plasma Concentrations After Conversion from INVEGA SUSTENNA 234 mg to 117 mg + 117 mg, depicts the expected change in median peak and trough plasma concentrations for this simulation for the first three cycles after conversion from one INVEGA SUSTENNA 234 mg to two simultaneous 117 mg injections.³ These simulated increases in plasma paliperidone concentrations are less than the intrasubject variability seen in clinical trials.

The PK simulation below depicts the expected paliperidone plasma concentration for simulated subjects receiving INVEGA SUSTENNA 234 mg at steady-state, including after conversion to 2 simultaneous INVEGA SUSTENNA 117 mg injections. In the Figure: 90% Prediction Interval for Conversion from INVEGA SUSTENNA 234 mg to 2 Separate 117 mg Injections, all simulated subjects received INVEGA SUSTENNA 234 mg at 12, 8, and 4 weeks before time zero. The red line depicts the median expected paliperidone plasma concentration in subjects who continued to receive the 234 mg dose every 4 weeks. The black line depicts the median expected paliperidone plasma concentration in subjects who received 2 separate injections of INVEGA SUSTENNA 117 mg at week 0, week 4, and week 8. The shaded region depicts the 90% prediction interval of paliperidone plasma concentrations for the 2 dosing regimens. It is expected that 90% of subjects will fall within this range.

LITERATURE SEARCH

A literature search of MEDLINE^®, EMBASE^®, BIOSIS Previews^®, and DERWENT Drug File(and/or other resources, including internal/external databases) pertaining to this topic was conducted on 10 June 2024.