Risperidone Long‐Acting Injection: Pharmacokinetics Following Administration in Deltoid Versus Gluteal Muscle in Schizophrenic Patients
Abstract
Long‐acting injectable (LAI) risperidone for intramuscular injection into the gluteal muscle every 2 weeks is approved for schizophrenia. The deltoid muscle provides a more accessible injection site and could therefore facilitate patient acceptance of an injectable medication. Two studies in chronic schizophrenic subjects evaluated the pharmacokinetics and tolerability of LAI risperidone administered into the deltoid muscle. The pharmacokinetics following deltoid injection and bioequivalence between deltoid and gluteal administration were assessed in an open‐label, single‐dose, crossover, fully powered bioavailability study. Tolerability and safety of deltoid LAI risperidone were investigated in an open‐label multiple‐dose study in subjects who were previously being treated with gluteal injections of LAI risperidone. Patients received 4 sequential intramuscular injections of LAI risperidone, administered every 2 weeks into the deltoid muscle. Deltoid and gluteal injections of LAI risperidone were shown to be bioequivalent at equal doses with respect to peak and total plasma exposure and exhibited dose‐proportional pharmacokinetics, independent of injection site. In addition, deltoid injection was safe and well tolerated. Injection of LAI risperidone into the deltoid muscle can be considered an alternative route of administration, because deltoid and gluteal injections are interchangeable in terms of drug exposure, with no additional safety or tolerability issues.
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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 [86]
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 [86]
RLAI-MS is administered via intramuscular injection in either the deltoid or the gluteal regions; deltoid and gluteal injections have been shown to be bioequivalent in terms of peak and total plasma exposure, and both injection sites exhibited dose-proportional pharmacokinetics.
“RLAI-MS formulation is administered via intramuscular injection in either the deltoid or the gluteal regions. Deltoid and gluteal injections have been shown to be bioequivalent in terms of peak and total plasma exposure, and both injection sites exhibited dose-proportional pharmacokinetics [86].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [86]
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 [86]
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- Authors
- Thyssen, A., Rusch, S., Herben, V., Quiroz, J., & Mannaert, E.
- Corresponding author
- Thyssen, An
- Venue
- The Journal of Clinical Pharmacology
- Publisher
- Wiley
- Published
- 2010-09
- Volume
- 50
- Issue
- 9
- Pages
- 1011-1021
- ISSN
- 0021-9754 (ISSN-L)
- 0091-2700
- 1552-4604
- OpenAlex
- W2162814669
- Cited by
- 26
- References
- 16
- Citations by year
- 2025: 3 · 2021: 2 · 2020: 2 · 2018: 1 · 2017: 2 · 2016: 3 · 2014: 2 · 2013: 3
- FWCI
- 2.40
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Journal of Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Health Sciences › Medicine › Emergency Medicine › Intramuscular injections and effects
- Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
- Keywords
- risperidone, long-acting injectable antipsychotics, injection site, pharmacokinetics, bioequivalence, schizophrenia, tolerability, dose proportionality
- MeSH terms
- Adult, Buttocks, Delayed-Action Preparations, Drug Administration Routes, Female, Humans, Injections, Intramuscular, Male, Middle Aged, Psychiatric Status Rating Scales, Schizophrenia, Shoulder, Therapeutic Equivalency, Antipsychotic Agents, Risperidone, Deltoid Muscle
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