Schoretsanitis, Georgios and de Leon, Jose and Haen, Ekkehard and Stegmann, Benedikt and Hiemke, Christoph and Gruender, Gerhard and Paulzen, Michael (2018) Pharmacokinetics of risperidone in different application forms - Comparing long-acting injectable and oral formulations. EUROPEAN NEUROPSYCHOPHARMACOLOGY, 28 (1). pp. 130-137. ISSN 0924-977X, 1873-7862
Full text not available from this repository. (Request a copy)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/9OH-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/9-0H-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/9-0H-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. (C) 2017 Elsevier B.V. and ECNP. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DRUG-DRUG INTERACTIONS; STEADY-STATE; SERUM CONCENTRATIONS; CYP2D6; ANTIPSYCHOTICS; SCHIZOPHRENIA; EFFICACY; 9-HYDROXYRISPERIDONE; METABOLISM; PSYCHIATRY; drug monitoring; cytochrome P-450 CYP2D6; risperidone/administration and dosage; risperidone/metabolism; risperidone/pharmacokinetics |
| Subjects: | 600 Technology > 610 Medical sciences Medicine 600 Technology > 615 Pharmacy |
| Divisions: | Medicine > Lehrstuhl für Psychiatrie und Psychotherapie Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 24 Mar 2020 08:02 |
| Last Modified: | 24 Mar 2020 08:02 |
| URI: | https://pred.uni-regensburg.de/id/eprint/15484 |
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