Summary

• When switching from INVEGA TRINZA injection to INVEGA SUSTENNA (paliperidone palmitate 1-month) extended-release injectable suspension, INVEGA SUSTENNA should be started 3 months after the last INVEGA TRINZA dose, using the equivalent 3.5-fold lower dose. INVEGA SUSTENNA should then continue, dosed at monthly intervals.¹
• A patient who has been appropriately switched to the INVEGA SUSTENNA formulation from INVEGA TRINZA, as described above, may be switched back to INVEGA TRINZA if desired when the next INVEGA SUSTENNA dose is scheduled. For example, a patient taking INVEGA TRINZA is switched to INVEGA SUSTENNA due to drug availability issues and wishes to resume INVEGA TRINZA treatment. In this scenario, the patient may return to INVEGA TRINZA when the next dose is scheduled.²

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 milligrams 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.
• INVEGA TRINZA doses expressed as 273, 410, 546, and 819 mg of paliperidone palmitate are equal to 175, 263, 350, and 525 mg eq of paliperidone, respectively.

SWITCHING TO INVEGA SUSTENNA

Please refer to the local labeling for complete information. The information regarding conversion to INVEGA SUSTENNA is summarized in Table: Conversion from INVEGA TRINZA to INVEGA SUSTENNA.

PUBLISHED DATA

Gopal et al (2015)¹ conducted a population pharmacokinetic (POP-PK) model to simulate a transition from INVEGA SUSTENNA to INVEGA TRINZA with continuing maintenance treatment with INVEGA TRINZA, and then a switch from INVEGA TRINZA back to INVEGA SUSTENNA. Simulations considered the following dosing schedules: treatment was initiated with INVEGA SUSTENNA 234 mg on day 1 (deltoid), 156 mg on day 8 (deltoid) and thereafter, one of 4 doses, 78, 117, 156, or 234 mg, on weeks 5, 9 and 13 (deltoid or gluteal). For maintenance treatment, patients were either continued at week 17 with deltoid or gluteal INVEGA SUSTENNA injections (every 4 weeks) up to week 77 or switched to respective 3.5-fold doses of INVEGA TRINZA, 273, 410, 546 or 819 mg, every 12 weeks, up to week 65. After stabilization on INVEGA TRINZA, patients switched back to INVEGA SUSTENNA at weeks 65, 69 and 73. See Figure: Simulated Paliperidone Plasma Concentrations versus Time for INVEGA TRINZA 546 and 819 mg Dose Groups and Figure: Simulated Paliperidone Plasma Concentrations versus Time for INVEGA TRINZA 273 and 410 mg Dose Groups.

At week 29, the simulated median minimum concentration (C_min) was 2.5 ng/mL (8.7%) higher (819 mg INVEGA TRINZA deltoid injections versus 234 mg INVEGA SUSTENNA deltoid injections), and 0.85 ng/mL (2.7%) lower (819 mg INVEGA TRINZA gluteal injections versus 234 mg INVEGA SUSTENNA gluteal injections). At week 65, the simulated steady-state median C_min was 0.35 ng/mL (1.1%) lower (819 mg INVEGA TRINZA deltoid injections versus 234 mg INVEGA SUSTENNA deltoid injections), and 8.4 ng/mL (23%) lower (819 mg INVEGA TRINZA gluteal injections versus 234 mg INVEGA SUSTENNA gluteal injections).

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 13 January 2025.