Pharmacokinetics of risperidone in different application forms - Comparing long-acting injectable and oral formulations.
Eur Neuropsychopharmacol, 2018/01;28(1):130-137.
Schoretsanitis G[1], de Leon J[2], Haen E[3], Stegmann B[3], Hiemke C[4], Gründer G[5], Paulzen M[5]
Affiliations
PMID: 29153926DOI: 10.1016/j.euroneuro.2017.11.009
Impact factor: 5.415
Abstract
We aimed to explore the differences in the pharmacokinetics of risperidone between oral and long-acting injectable (LAI) formulations using a large database of therapeutic drug monitoring (TDM). Plasma concentrations of risperidone (RIS), its active metabolite (9-OH-RIS) and the active moiety (AM) (RIS+9-OH-RIS), their concentration-to-dose (C/D) ratios and ratio of RIS/9-OH-RIS (an index of CYP2D6 metabolic activity) were used to compare patients receiving risperidone orally (n = 851) and those treated with LAI RIS (n = 63). Patients taking CYP inducers or inhibitors or with liver/renal impairment were eliminated. Our study demonstrated that patients on LAI RIS, despite slightly higher RIS doses in the oral group, showed no significant differences in total AM or 9-OH-RIS. Conversely, RIS concentration, RIS C/D ratio and total C/D ratio were slightly higher in the LAI RIS group, reaching significance due to the large sample size. More importantly, the median ratio of RIS/9-OH-RIS was 0.52 in LAI RIS vs. 0.25 in the oral group, providing a significant difference (p < 0.001). After controlling for confounding factors, we replicated the RIS/9-OH-RIS ratio increases in patients with LAI RIS, probably reflecting a decrease in first-pass metabolism. More studies are required to establish the clinical use of TDM for patients on LAI RIS.
Keywords: cytochrome P-450 CYP2D6; drug monitoring; risperidone/administration and dosage; risperidone/metabolism; risperidone/pharmacokinetics
MeSH terms
Administration, Oral; Adolescent; Adult; Aged; Aged, 80 and over; Antipsychotic Agents; Delayed-Action Preparations; Dose-Response Relationship, Drug; Female; Humans; Injections; Male; Mental Disorders; Middle Aged; Risperidone; Young Adult
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