Drug Detail:Invega sustenna (Paliperidone (injection) [ pal-ee-per-i-done ])
Generic Name: paliperidone palmitate 39mg in 0.25mL
Dosage Form: injection
Drug Class: Atypical antipsychotics
Administration Instructions
Each injection must be administered only by a healthcare professional.
Parenteral drug products should be inspected visually for foreign matter and discoloration prior to administration, whenever product and container permit.
INVEGA SUSTENNA® is intended for intramuscular use only. Do not administer by any other route. Avoid inadvertent injection into a blood vessel. Administer the dose in a single injection; do not administer the dose in divided injections. Inject slowly, deep into the deltoid or gluteal muscle.
INVEGA SUSTENNA® must be administered using only the needles that are provided in the INVEGA SUSTENNA® kit.
The recommended needle size for administration of INVEGA SUSTENNA® into the deltoid muscle is determined by the patient's weight:
- For patients weighing less than 90 kg, the 1-inch, 23 gauge needle is recommended.
- For patients weighing 90 kg or more, the 1½-inch, 22 gauge needle is recommended.
Deltoid injections should be alternated between the two deltoid muscles.
The recommended needle size for administration of INVEGA SUSTENNA® into the gluteal muscle is the 1½-inch, 22 gauge needle regardless of patient weight.
Administer into the upper-outer quadrant of the gluteal muscle. Gluteal injections should be alternated between the two gluteal muscles.
Schizophrenia and Schizoaffective Disorder
For patients who have never taken oral paliperidone or oral or injectable risperidone, it is recommended to establish tolerability with oral paliperidone or oral risperidone prior to initiating treatment with INVEGA SUSTENNA®.
The recommended dosing of INVEGA SUSTENNA® for each approved indication is displayed in Table 1. The recommended initiation of INVEGA SUSTENNA® is with a dose of 234 mg on treatment day 1 and 156 mg one week later, both administered in the deltoid muscle. Following the second initiation dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle.
| Indication | Initiation Dosing (deltoid) |
Monthly Maintenance Dose* (deltoid or gluteal) |
Maximum Monthly Dose | |
|---|---|---|---|---|
| Day 1 | Day 8 | |||
|
||||
| Schizophrenia | 234 mg | 156 mg | 39–234 mg† | 234 mg |
| Schizoaffective disorder | 234 mg | 156 mg | 78–234 mg‡ | 234 mg |
Adjustment of the maintenance dose may be made monthly. When making dose adjustments, the prolonged-release characteristics of INVEGA SUSTENNA® should be considered [see Clinical Pharmacology (12.3)], as the full effect of the dose adjustment may not be evident for several months.
Missed Doses
Avoiding Missed Doses
It is recommended that the second initiation dose of INVEGA SUSTENNA® be given one week after the first dose. To avoid a missed dose, patients may be given the second dose 4 days before or after the one-week time point. Similarly, the third and subsequent injections after the initiation regimen are recommended to be given monthly. To avoid a missed monthly dose, patients may be given the injection up to 7 days before or after the monthly time point.
Management of a Missed Second Initiation Dose
If the target date for the second INVEGA SUSTENNA® injection (one week ± 4 days) is missed, the recommended reinitiation depends on the length of time which has elapsed since the patient's first injection. In case of a missed second initiation dose follow the dosing instructions provided in Table 2.
| TIMING OF MISSED SECOND INITIATION DOSE | DOSING |
|---|---|
| Less than 4 weeks since first injection | Administer the second initiation dose of 156 mg in the deltoid muscle as soon as possible.
|
| 4 to 7 weeks since first injection | Resume dosing with two injections of 156 mg in the following manner:
|
| More than 7 weeks since first injection | Restart dosing with recommended initiation (see Section 2.2, Table 1):
|
Management of a Missed Maintenance Dose
In case of a missed maintenance dose follow the dosing instructions provided in Table 3.
| TIMING OF MISSED MAINTENANCE DOSE | DOSING |
|---|---|
| 4 to 6 weeks since last injection | Resume regular monthly dosing as soon as possible at the patient's previously stabilized dose, followed by injections at monthly intervals. |
| More than 6 weeks to 6 months since last injection | Resume the same dose the patient was previously stabilized on (unless the patient was stabilized on a dose of 234 mg, then the first 2 injections should each be 156 mg) in the following manner:
|
| More than 6 months since last injection | Restart dosing with recommended initiation (see Section 2.2, Table 1):
|
Use with Risperidone or with Oral Paliperidone
Since paliperidone is the major active metabolite of risperidone, caution should be exercised when INVEGA SUSTENNA® is coadministered with risperidone or with oral paliperidone for extended periods of time. Safety data involving concomitant use of INVEGA SUSTENNA® with other antipsychotics is limited.
Dosage Adjustments
Patients with Renal Impairment
INVEGA SUSTENNA® has not been systematically studied in patients with renal impairment [see Clinical Pharmacology (12.3)].
For patients with mild renal impairment (creatinine clearance ≥ 50 mL/min to < 80 mL/min [Cockcroft-Gault Formula]), initiate INVEGA SUSTENNA® with a dose of 156 mg on treatment Day 1 and 117 mg on Day 8, both in the deltoid muscle. Follow with the recommended monthly maintenance dose of 78 mg, administered in either the deltoid or gluteal muscle. Adjust monthly maintenance dose based on tolerability and/or efficacy within the strengths of 39 mg, 78 mg, 117 mg, or 156 mg. The maximum monthly dose is 156 mg for patients with mild renal impairment [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
INVEGA SUSTENNA® is not recommended in patients with moderate or severe renal impairment (creatinine clearance < 50 mL/min) [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)].
Coadministration with Strong CYP3A4/P-glycoprotein (P-gp) Inducers
Avoid using a strong inducer of CYP3A4 and/or P-gp (e.g., carbamazepine, rifampin, St John's Wort) during the 1-month dosing interval for INVEGA SUSTENNA®, if possible. If administering a strong inducer is necessary, consider managing the patient using paliperidone extended release tablets [see Drug Interactions (7.1) and Clinical Pharmacology (12.3)].
Switching from Other Antipsychotics
There are no systematically collected data to specifically address switching patients with schizophrenia or schizoaffective disorder from other antipsychotics to INVEGA SUSTENNA®, or concerning concomitant administration with other antipsychotics.
Switching from Oral Antipsychotics
For patients who have never taken oral paliperidone or oral or injectable risperidone, tolerability should be established with oral paliperidone or oral risperidone prior to initiating treatment with INVEGA SUSTENNA®.
Previous oral antipsychotics can be gradually discontinued at the time of initiation of treatment with INVEGA SUSTENNA®. Recommended initiation of INVEGA SUSTENNA® is with a dose of 234 mg on treatment day 1 and 156 mg one week later, both administered in the deltoid muscle [see Dosage and Administration (2.2)]. Patients previously stabilized on different doses of INVEGA® Extended-Release tablets can attain similar paliperidone steady-state exposure during maintenance treatment with INVEGA SUSTENNA® monthly doses as depicted in Table 4.
| Formulation | INVEGA® Extended-Release Tablet | INVEGA SUSTENNA® Injection |
|---|---|---|
| Dosing Frequency | Once Daily | Once every 4 weeks |
| Dose (mg) | 12 | 234 |
| 9 | 156 | |
| 6 | 117 | |
| 3 | 39–78 |
Switching from Long-Acting Injectable Antipsychotics
For patients who have never taken oral paliperidone or oral or injectable risperidone, tolerability should be established with oral paliperidone or oral risperidone prior to initiating treatment with INVEGA SUSTENNA®.
When switching patients currently at steady-state on a long-acting injectable antipsychotic, initiate INVEGA SUSTENNA® therapy in place of the next scheduled injection. INVEGA SUSTENNA® should then be continued at monthly intervals. The one-week initiation dosing regimen as described in Section 2.2 is not required. See Table 1 above for recommended monthly maintenance dosing. Based on previous clinical history of tolerability and/or efficacy, some patients may benefit from lower or higher maintenance doses within the available strengths (39 mg, 78 mg, 117 mg, 156 mg, and 234 mg). The 39 mg strength was not studied in the long-term schizoaffective disorder study. Monthly maintenance doses can be administered in either the deltoid or gluteal muscle [see Dosage and Administration (2.2)].
If INVEGA SUSTENNA® is discontinued, its prolonged-release characteristics must be considered. As recommended with other antipsychotic medications, the need for continuing existing extrapyramidal symptoms (EPS) medication should be re-evaluated periodically.
Instructions for Use
Each injection must be administered only by a healthcare professional.
The kit contains a prefilled syringe and 2 safety needles (a 1 ½-inch 22 gauge needle and a 1-inch 23 gauge needle) for intramuscular injection.
INVEGA SUSTENNA® is for single use only.
- a.
- Shake the syringe vigorously for a minimum of 10 seconds to ensure a homogeneous suspension.
- b.
- Select the appropriate needle.
For DELTOID injection:- If the patient weighs less than 90 kg, use the 1-inch 23 gauge needle (needle with blue colored hub).
- If the patient weighs 90 kg or more, use the 1 ½-inch 22 gauge needle (needle with gray colored hub).
For GLUTEAL injection:
Use the 1 ½-inch 22 gauge needle (needle with gray colored hub) regardless of patient's weight.
- c.
- While holding the syringe upright, remove the rubber tip cap with an easy clockwise twisting motion.
- d.
- Peel the safety needle pouch half way open. Grasp the needle sheath using the plastic peel pouch. Attach the safety needle to the luer connection of the syringe with an easy clockwise twisting motion.
- e.
- Pull the needle sheath away from the needle with a straight pull. Do not twist the sheath as the needle may be loosened from the syringe.
- f.
- Bring the syringe with the attached needle in upright position to de-aerate. De-aerate the syringe by moving the plunger rod carefully forward.
- g.
- Inject the entire contents intramuscularly slowly, deep into the selected deltoid or gluteal muscle of the patient. Do not administer by any other route.
- h.
- After the injection is complete, use either thumb or finger of one hand (h1, h2) or a flat surface (h3) to activate the needle protection system. The needle protection system is fully activated when a 'click' is heard. Discard the syringe with needle appropriately.
| h1 | |
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| h2 | |
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| h3 | |
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