A Visual Guide to Expected Blood Levels of Long-Acting Injectable Risperidone in Clinical Practice
Abstract
OBJECTIVE: Risperidone is the only second-generation (atypical) antipsychotic medication available in a long-acting injectable formulation. The mechanism of drug delivery and the pharmacokinetics of this medication are distinctively different from the first-generation injectable depot medications. Antipsychotic blood levels have been reported in carefully managed single-dose and multiple-dose studies of long-acting risperidone. However, there have been no studies of blood levels produced by the variability in doses and schedules that may occur in clinical practice. Mathematical modeling allows for estimation of blood levels in a variety of clinical scenarios that have yet to be studied empirically. This paper presents mathematically modeled representations of antipsychotic blood levels in clinical situations with long-acting risperidone, with the goal of helping professionals, patients, and family members make informed decisions regarding treatment. METHODS: A model of single-dose pharmacokinetics was derived from a published, empirical single-dose study. The model was used to prepare graphs of expected multiple-dose schedules consistent with clinical situations, using empirically validated assumptions. RESULTS: The model was validated by comparison of the results of multiple-dose modeling with published empirical multi-dose data. Graphs of expected blood levels in several clinical situations are presented. Future empirical studies are required to fully validate these results. CONCLUSIONS: Mathematical models of antipsychotic blood levels in various common situations allow a better appreciation of the novel pharmacokinetics of long-acting injectable risperidone, which may lead to more informed decision-making.
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The RLAI-MS formulation exhibits linear pharmacokinetics.
“The RLAI-MS formulation exhibits linear pharmacokinetics [85, 86]”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [85]
The main release of risperidone into systemic circulation begins 3 weeks after injection, and most active drug is released from weeks 4 to 6.
“The main release of risperidone into systemic circulation begins 3 weeks after injection, and most active drug is released from weeks 4 to 6 [85, 87].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [85]
The risperidone long-acting injection microspheres (RLAI-MS) formulation was the first second-generation LAI developed, formulated as an aqueous suspension of microspheres of risperidone micro-encapsulated in 7525 polylactide-co-glycolide.
“The risperidone long-acting injection microspheres (RLAI-MS) formulation was the first second-generation LAI developed, formulated as an aqueous suspension of microspheres of risperidone micro-encapsulated in 7525 polylactide-co-glycolide [84–86].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [85]
Oral supplementation with risperidone or another oral antipsychotic is recommended for the first 3 weeks after initiation of RLAI-MS.
“Oral supplementation with risperidone or another oral antipsychotic is recommended for the first 3 weeks after initiation [85, 86].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [85]
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- Authors
- WILSON, W. H.
- Affiliations
- Oregon Health & Science University (US)
- Corresponding author
- WILSON, WILLIAM H.
- Venue
- Journal of Psychiatric Practice
- Published
- 2004-11
- Volume
- 10
- Issue
- 6
- Pages
- 393-401
- ISSN
- 1527-4160 (ISSN-L)
- 1538-1145
- OpenAlex
- W2093439082
- Cited by
- 180
- References
- 11
- Citations by year
- 2025: 4 · 2023: 1 · 2021: 3 · 2020: 158 · 2019: 1 · 2014: 1 · 2013: 1 · 2012: 3
- FWCI
- 0.41
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Psychiatric Practice (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- long-acting injectable risperidone, atypical antipsychotics, pharmacokinetics, blood concentration, mathematical modeling, dose variation, clinical decision-making, antipsychotic dosing
- MeSH terms
- Adolescent, Adult, Decision Making, Dose-Response Relationship, Drug, Female, Humans, Male, Models, Theoretical, Schizophrenia, Antipsychotic Agents, Guidelines as Topic, Risperidone
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