10.4088/JCP.v69n0515.Canuso CM, Dirks B, Carothers J, Kosik-Gonzalez C, Bossie CA, Zhu Y, Damaraju CV, Kalali AH, Mahmoud R: Randomized, double-blind, placebo-controlled study of paliperidone extended-release and quetiapine in inpatients with recently exacerbated schizophrenia.
Int J Neuropsychopharmacol. Comparison between oral risperidone 3 mg once‐daily and Comparison between oral risperidone 6 mg once‐daily and 10.1056/NEJMoa051688.Canuso CM, Bossie CA, Turkoz I, Alphs L: Paliperidone extended-release for schizophrenia: effects on symptoms and functioning in acutely ill patients with negative symptoms. 10.1124/dmd.107.018275.Kramer M, Simpson G, Maciulis V, Kushner S, Liu Y, Lim P, Hough D, Palumbo J, Eerdekens M: One-year open-label safety and efficacy study of paliperidone extended-release tablets in patients with schizophrenia. J Clin Psychiatry. Am J Psychiatry. The conversion does not take into account the potential effects of CYP2D6 inhibitors (ie paroxetine, sertraline or fluoxetine) or CYP3A and PgP inducers (ie carbamazepine) on active‐moiety concentrations.This analysis provides the clinician with a practical guidance to establish suitable maintenance dose levels of PP1M and oral risperidone when transitioning patients from one formulation to another, such that SS active‐moiety exposures are similar between the two drugs.
from oral risperidone to paliperidone ER. TABLE 1 Doses of oral risperidone and PP1M expected to result in similar active moiety at steady-state based on pharmacokinetic simulations Oral risperidone (mg) Paliperidone palmitate 1- mo (PP1M)a (mg eq.) Indications and contraindications to switching should be considered on an individual patient basis [It is important to note that the greater the differences in receptor binding affinities between pre- and post-switch antipsychotic medications, the more care should be taken when switching. 10.1177/0269881110391123.Buchanan RW, Kreyenbuhl J, Kelly DL, Noel JM, Boggs DL, Fischer BA, Himelhoch S, Fang B, Peterson E, Aquino PR, Keller W, Schizophrenia Patient Outcomes Research Team (PORT): The 2009 schizophrenia PORT psychopharmacological treatment recommendations and summary statements. When switching from antipsychotics that have sedative and/or significant anticholinergic activity, the pre-switch antipsychotic should be tapered off gradually.
2012, 32: 449-457. 10.2165/00023210-200519010-00003.Gray JA, Roth BL: The pipeline and future of drug development in schizophrenia. Recently diagnosed patients, those with renal impairment, or patients who have previously experienced tolerability issues with other antipsychotics may require lower doses. 10.4088/JCP.09m05564yel.Canuso CM, Youssef EA, Bossie CA, Turkoz I, Schreiner A, Simpson GM: Paliperidone extended-release tablets in schizophrenia patients previously treated with risperidone.
2009, 113: 56-64. We assessed the dosage strengths of paliperidone palmitate 1‐month (PP1M) long‐acting injectable resulting in similar steady‐state (SS) exposures to the dosage strengths of oral risperidone using pharmacokinetic (PK) simulations.Population PK simulations of SS PK were performed using the PK models of oral risperidone and PP1M. These considerations impact both the tapering period of the pre-switch medication (for instance, requiring prolongation) and the dosing of the new antipsychotic medication.Switching strategies should take account of the specific medications involved; for example, switching from a sedating to a non-sedating antipsychotic requires different considerations than switching between two sedating antipsychotics. The authors drew on their clinical experience supported by detailed discussion of literature describing antipsychotic switching techniques and strategies and findings from paliperidone ER clinical trials. Furthermore, the paliperidone long-acting injectable (LAI) package insert does not recommend bridging with oral antipsychotics, which may result in inadequate serum concentrations in patients on ≥4 mg/d risperidone.
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