The initiation regimen for INVEGA SUSTENNA was designed to rapidly attain steady-state paliperidone concentrations when initiating therapy without the use of oral antipsychotic supplementation.

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.¹

Switching From INVEGA ER tablet or Oral Risperidone

• From INVEGA ER tablet

  Doses of INVEGA and INVEGA SUSTENNA needed to attain similar steady-state paliperidone exposure during maintenance treatment ¹

  

  Formulation	INVEGA ER tablet	INVEGA SUSTENNA injection
  Dosing frequency	Once daily	Once every 4 weeks
  Dose	12 mg	234 mg
  	9 mg	156 mg
  	6 mg	117 mg
  	3 mg	39-78 mg

  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. 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.¹

  ER, extended-release.

  Reference

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  1. INVEGA SUSTENNA [(paliperidone palmitate) Extended-Release Injectable Suspension] [Prescribing Information]. Titusville, NJ: Janssen Pharmaceuticals, Inc; https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf.

• From Oral Risperidone

  Doses of RIS and INVEGA SUSTENNA needed to attain similar exposure to active moiety at steady-state¹

  

  Formulation	RIS Orala	INVEGA SUSTENNA
  Dosing frequency	Daily	Once every 4 weeks
  Dose	1 mg	39 mg
  	2 mg	78 mg
  	3 mg	117 mg
  	4 mg	156 mg
  	6 mg	234 mg

  ^aConversion factor: 1 mg oral RIS = 39 mg INVEGA SUSTENNA. Note: The conversion does not take into account the potential effects of CYP2D6 inhibitors (i.e. paroxetine, sertraline or fluoxetine) or inducers (i.e. carbamazepine) on active moiety concentrations.

  Population PK simulations^2,3 were conducted to determine which dose levels of oral RIS result in similar pharmacokinetics to the INVEGA SUSTENNA 78-234 mg dose levels at steady-state. For oral RIS, active moiety concentrations (risperidone and 9-OH-risperidone [paliperidone]) were compared to paliperidone concentrations for INVEGA SUSTENNA . The results suggest that patients stabilized with oral RIS can attain similar steady-state exposure to active moiety during maintenance treatment with monthly doses of INVEGA SUSTENNA administered via deltoid or gluteal injection. The recommended initiation regimen for INVEGA SUSTENNA (234 mg on day 1 and 156 mg on day 8 via deltoid injection) is required for this transition. However, no oral antipsychotic supplementation is required.¹

  CYP, cytochrome P450; ER, extended release; PK, pharmacokinetic; RIS, risperidone.

  References

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  1. INVEGA SUSTENNA [(paliperidone palmitate) Extended-Release Injectable Suspension] [Prescribing Information]. Titusville, NJ: Janssen Pharmaceuticals, Inc; https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/INVEGA+SUSTENNA-pi.pdf.

  2. Russu A, Kern Sliwa J, Ravenstijn P, et al. Maintenance dose conversion between oral risperidone and paliperidone palmitate 1 month: practical guidance based on pharmacokinetic simulations. Int J Clin Pract. 2018;72(6):e13089

  3. Data on File. PK simulations to assess similarity between oral risperidone, risperidone long-acting injection and paliperidone palmitate. Janssen Research & Development. 2016