6533b7d4fe1ef96bd1262942

RESEARCH PRODUCT

A systematic review and combined analysis of therapeutic drug monitoring studies for longacting risperidone

Edoardo SpinaGeorgios SchoretsanitisChristoph HiemkeJose De Leon

subject

CYP2D6Therapeutic drug monitoring studiesAdministration OralPharmacologyMicrosphereInjections03 medical and health sciences0302 clinical medicineLong acting risperidonePaliperidone PalmitatemedicineAnimalsHumansPharmacology (medical)General Pharmacology Toxicology and Pharmaceutics610 Medicine & healthActive metabolitePaliperidone PalmitateRisperidonemedicine.diagnostic_testbusiness.industryGeneral MedicineRisperidoneMicrospheres030227 psychiatryAntipsychotic agents/administration & dosage; delayed-action preparations; drug monitoring; injections; risperidone/administration & dosage; risperidone/blood; risperidone/metabolism; risperidone/pharmacokinetics; risperidone/pharmacology; risperidone/therapeutic use; schizophrenia/drug therapyTherapeutic drug monitoringDelayed-Action PreparationsDrug Monitoringbusiness030217 neurology & neurosurgerymedicine.drugAntipsychotic Agents

description

Introduction: This systematic review of therapeutic drug monitoring (TDM) identifies three long-acting injectable (LAI) risperidone formulations. Areas covered: Limited data is available on two formulations (RBP-7000 and in Situ Microparticle), but 20 TDM articles on the microsphere formulation were found. Risperidone TDM includes the serum concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone, used for calculating: 1) the risperidone/9-hydroxyrisperidone (R/9-OH-R) ratio (a measure of CYP2D6; values >1 are indicative of a CYP2D6 poor metabolizer) and 2) the total risperidone concentration-to-dose (C/D) ratio (a measure of risperidone clearance with a normal value around 7 in oral risperidone). The weighted mean R/9-OH-R ratio was 0.48 (approximately twice that of oral risperidone TDM) in a combined analysis from 329 patients in 6 risperidone LAI studies without major confounders. The total C/D ratios from 297 patients in 6 risperidone LAI studies ranged from 7.4 to 9.7 ng/ml/mg/day with a weighted mean of 8.8 ng/ml/mg/day. Expert commentary: Clinicians using TDM for risperidone LAI microsphere formulation need to: 1) consider steady state to be reached ≥ 6 weeks after the first injection, 2) pay attention to a) comedications with inducers/inhibitors, b) severe inflammations/infections, and c) hepatic/renal impairment, and 3) use Castberg’s recommendation to calculate risperidone dosing.

https://dx.doi.org/10.7892/boris.108504