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Dose correspondence between olanzapine long-acting injection and oral olanzapine: recommendations for switching
Abstract
Oral-to-depot dose correspondence was explored in a 24-week study of olanzapine long-acting injection (LAI). Patients with schizophrenia stabilized on oral olanzapine of 10, 15, or 20 mg/day (n=1065) were randomized to continue their oral treatment or switch directly to a fixed dose of olanzapine LAI [(mg/weeks) 45/4, 150/2, 405/4, or 300/2] without oral supplementation. Six-month relapse rates for each LAI-dose group stratified by earlier oral dose were analyzed using a Cox proportional hazard model assessing risk of relapse relative to each oral dose. Relapse rates for the therapeutic LAI doses (≥ 150 mg) varied depending on earlier oral dose, ranging from 1.5% (patients switched from 10 mg/day to 300 mg/2 weeks) to 18.8% (patients switched from 20 mg/day to 150 mg/2 weeks). Switching from 10 mg/day to 405 mg/4 weeks produced a comparable risk of relapse as remaining on that oral dose [Hazard ratio (HR)=1.03]. Switching from 15 or 20 mg/day to 300 mg/2 weeks produced comparable risk of relapse as remaining on those oral doses (HR=0.68 and 1.13, respectively). Pharmacokinetic modeling was conducted to evaluate the resulting dosing recommendations. Findings suggest that patients can be switched directly from oral to olanzapine LAI without the need for oral supplementation and with a low risk of relapse when initiated on an appropriate LAI dose.
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“Although plasma concentrations of olanzapine can be lower after the first dose of olanzapine pamoate than those maintained by a corresponding oral dose, the concentrations achieved by the LAI dose are in the therapeutically effective range, suggesting that oral supplementation is not needed during LAI initiation [73].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [73]
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Hasan, A., Falkai, P., Wobrock, T., Lieberman, J. A., Glenthoj, B. Y., Gattaz, W. F., Thibaut, F., Möller, H., & WFSBP Task force on Treatment Guidelines for Schizophrenia (2012) · The World Journal of Biological Psychiatry · doi:10.3109/15622975.2012.739708 · Cited by 424
“Patients receiving oral olanzapine in a dose of 10 mg/day can be switched to 405 mg/4 weeks, and patients receiving 15 or 20 mg/day can be switched to 300 mg/2 weeks without increasing risk of relapse (Detke et al. 2011).”
BackgroundCorrell, C. U., Kim, E., Sliwa, J. K., Hamm, W., Gopal, S., Mathews, M., Venkatasubramanian, R., & Saklad, S. R. (2021) · CNS Drugs · doi:10.1007/s40263-020-00779-5 · Cited by 205
Converting oral to long-acting injectable antipsychotics: a guide for the perplexed
Meyer, J. M. (2017) · CNS Spectrums · doi:10.1017/s1092852917000840 · Cited by 196
“Kinetic profiles of different 8-week loading strategies of olanzapine pamoate.(40) 24 J.”
BackgroundInfluentialRauch, A.-S., & Fleischhacker, W. W. (2013) · CNS Drugs · doi:10.1007/s40263-013-0083-9 · Cited by 64
Stahl, S. M. (2020) · Cambridge University Press eBooks · doi:10.1017/9781108921275 · Cited by 52
Metadata
- Authors
- Detke, H. C., Zhao, F., Garhyan, P., Carlson, J., & McDonnell, D.
- Affiliations
- Eli Lilly (United States) (US)
- Corresponding author
- Detke, Holland C.
- Venue
- International Clinical Psychopharmacology
- Published
- 2011-01
- Volume
- 26
- Issue
- 1
- Pages
- 35-42
- ISSN
- 0268-1315 (ISSN-L)
- OpenAlex
- W2090734001
- Cited by
- 185
- References
- 0
- Citations by year
- 2026: 1 · 2025: 3 · 2024: 1 · 2023: 1 · 2021: 2 · 2020: 158 · 2017: 2 · 2014: 3 · 2013: 6 · 2012: 3
- FWCI
- 3.05
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Clinical Psychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Eli Lilly and Company
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Health Sciences › Medicine › Pharmacology (medical) › Treatment of Major Depression
- Social Sciences › Psychology › Clinical Psychology › Historical Psychiatry and Medical Practices
- Keywords
- schizophrenia, relapse risk, pharmacokinetic modeling, antipsychotic dosing
- MeSH terms
- Olanzapine, Administration, Oral, Adult, Aged, Benzodiazepines, Delayed-Action Preparations, Double-Blind Method, Drug Administration Routes, Female, Humans, Injections, Intramuscular, Male, Middle Aged, Recurrence, Schizophrenia, Antipsychotic Agents, Drug Substitution
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