How do I transition a patient from risperidone oral to paliperidone palmitate (Invega Sustenna) long-acting injectable (LAI)?

When transitioning a patient from risperidone oral to paliperidone palmitate (Invega Sustenna), information on the manufacturerā€™s current website states that all patients transitioning from oral antipsychotics must follow the recommended initiation dosing of 234 mg (day 1), 156 mg (day 8), both administered in the deltoid muscle. No oral supplementation is required.

The paliperidone palmitate label does not specifically address conversion of risperidone tablets to paliperidone palmitate. Patients stabilized on risperidone tablets can attain similar steady-state exposure with INVEGA SUSTENNAĀ® as depicted in Table. The INVEGA SUSTENNAĀ® Prescribing Information does not specifically address conversion of RISPERDALĀ® tablets to INVEGA SUSTENNAĀ®. This information is based on pharmacokinetic (PK) modeling performed to compare steady-state exposure during maintenance treatment between RISPERDALĀ® tablets and INVEGA SUSTENNAĀ® (after both the 234 mg/156 mg deltoid starting doses):

Risperdal Tablet

INVEGA SUSTENNAĀ®
(once monthly injection) 

1 mg

39 mg

2 mg

78 mg

3 mg

117 mg

4 mg

156 mg

6 mg

234 mg

References:
1. : Russu A, Sliwa JK, Ravestijn 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;e13089. 
2. https://www.invegasustennahcp.com/dosing/transitioning

The patientā€™s third injection will be at the maintenance dose designated by their clinician, either 117 mg, 156 mg, or 234 mg.

Paliperidone is OH-risperidone, the active metabolite of risperidone, which explains the drugsā€™ similarities, as well as ability to establish tolerance by using either oral risperidone or paliperidone.

FDA medication label

Information on this topic is found in the FDA medication label.Ā Here is the most recent label, at time of writing. Medication labels can be found by searching Drugs@FDA at theĀ FDA website. Labels are also available using the Drugs@FDA app for Apple or Android devices.Ā Labels change over time, and the current label should always be consulted.

If you would like more information on this topic, or would like to provide any feedback, please send us a message using ourĀ consultation system. Be sure to let us know about which tip you are writing. We would love to hear from you, and the consultation system is free to use and confidential. Thank you!
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