Serum Concentrations of Paliperidone After Administration of the Long-Acting Injectable Formulation
Open accessAbstract
Background: The pharmacokinetics of long-acting intramuscular paliperidone in a naturalistic setting is not well documented. The objective of this study was to investigate the relationship between dose and serum concentrations of paliperidone using data from a routine therapeutic drug monitoring service. Methods: Serum concentration measurements in 310 samples from 110 male and 75 female patients receiving depot injections of paliperidone were retrospectively retrieved from the therapeutic drug monitoring database. Results: The median dose was 100 mg every 28 days. The median concentration/dose (C/D) ratio of paliperidone was 16.1 (nmol/L)/(mg/d), with a 10–90 percentile range of 7.8–31.0 (nmol/L)/(mg/d). Dose-adjusted serum concentrations were 33% higher in patients 65 years or older and more than 50% lower in patients taking the p-glycoprotein inducer carbamazepine. There were no significant effects of sex or dose on the C/D ratio. The median serum concentrations of paliperidone at the end of the dose interval were 31 nmol/L at an intramuscular dose of 50 mg/28 d, 53 nmol/L after a dose of 75 mg/28 d, 59 nmol/L after a dose of 100 mg/28 d, and 93 nmol/L after a dose of 150 mg/28 d. Forty-five percent of the measurements were lower than the suggested therapeutic range of 20–60 ng/mL (47–140 nmol/L). Conclusions: The data show a 4-fold interindividual difference in dose-adjusted serum concentrations within the 10–90 percentile range and illustrate the significant effects of age and p-glycoprotein induction on the pharmacokinetics of paliperidone. The study also indicates that at least in some patients, it might take longer time than anticipated to reach steady state.
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Therefore, paliperidone has low potential for drug-drug interactions, and the CYP2D6 genotype should not affect serum concentrations.
“Therefore, paliperidone has low potential for drug–drug interactions, and the CYP2D6 genotype should not affect serum concentrations [79].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [79]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Cites
AGNP Consensus Guidelines for Therapeutic Drug Monitoring in Psychiatry: Update 2011
Hiemke, C., Baumann, P., Bergemann, N., Conca, A., Dietmaier, O., Egberts, K. M., Fric, M., Gerlach, M., Greiner, C., Gründer, G., et al. (2011) · Pharmacopsychiatry · doi:10.1055/s-0031-1286287 · Cited by 871 · see citing works
Systematic review of patient and nurse attitudes to depot antipsychotic medication
Walburn, J., Gray, R. J., Gournay, K., Quraishi, S. N., & David, A. S. (2001) · The British Journal of Psychiatry · doi:10.1192/bjp.179.4.300 · Cited by 187 · see citing works
Samtani, M. N., Vermeulen, A., & Stuyckens, K. (2009) · Clinical Pharmacokinetics · doi:10.2165/11316870-000000000-00000 · Cited by 170 · see citing works
Changes in body mass index for individuals with and without schizophrenia, 1987–1996
Homel, P., Casey, D. E., & Allison, D. B. (2002) · Schizophrenia Research · doi:10.1016/s0920-9964(01)00256-0 · Cited by 160 · see citing works
Absorption, Metabolism, and Excretion of Paliperidone, a New Monoaminergic Antagonist, in Humans
Vermeir, M., Naessens, I., Remmerie, B., Mannens, G., Hendrickx, J., Sterkens, P., Talluri, K., Boom, S., Eerdekens, M., van Osselaer, N., et al. (2008) · Drug Metabolism and Disposition · doi:10.1124/dmd.107.018275 · Cited by 158 · see citing works
The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein
Wang, J.-S., Ruan, Y., Taylor, R. M., et al. (2004) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145704004390 · Cited by 141 · see citing works
Long-acting injectable formulations of antipsychotic drugs for the treatment of schizophrenia
Park, E. J., Amatya, S., Kim, M. S., Park, J. H., Seol, E., Lee, H., Shin, Y.-H., & Na, D. H. (2013) · Archives of Pharmacal Research · doi:10.1007/s12272-013-0105-7 · Cited by 120 · see citing works
Body composition in psychotic disorders: a general population survey
Saarni, S. E., Saarni, S. I., Fogelholm, M., Heliövaara, M., Perälä, J., Suvisaari, J., & Lönnqvist, J. K. (2008) · Psychological Medicine · doi:10.1017/s0033291708004194 · Cited by 71 · see citing works
Nakagami, T., Yasui‐Furukori, N., SAITO, M., TATEISHI, T., & KANEO, S. (2005) · Clinical Pharmacology & Therapeutics · doi:10.1016/j.clpt.2005.03.009 · Cited by 68 · see citing works
Dosing and Switching Strategies for Paliperidone Palmitate
Samtani, M. N., Gopal, S., Gassmann-Mayer, C., Alphs, L. D., & Palumbo, J. (2011) · CNS Drugs · doi:10.2165/11591690-000000000-00000 · Cited by 68 · see citing works
Lisbeth, P., Haufroid, V., Kristof, M., et al. (2015) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-015-1965-1 · Cited by 64 · see citing works
Serum concentrations of paliperidone versus risperidone and clinical effects
Nazirizadeh, Y., Vogel, F., Bader, W., Haen, E., Pfuhlmann, B., Gründer, G., Paulzen, M., Schwarz, M., Zernig, G., & Hiemke, C. (2010) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-010-0812-7 · Cited by 51 · see citing works
Lopez, L. V., & Kane, J. M. (2013) · Schizophrenia Research · doi:10.1016/j.schres.2013.04.002 · Cited by 48 · see citing works
Castberg, I., & Spigset, O. (2005) · Therapeutic Drug Monitoring · doi:10.1097/00007691-200502000-00019 · Cited by 43 · see citing works
Self-citationBoom, S., Talluri, K., Janssens, L., Remmerie, B. M. M., Meulder, M. D., Rossenu, S., Osselaer, N. V., Eerdekens, M., & Cleton, A. (2009) · The Journal of Clinical Pharmacology · doi:10.1177/0091270009339190 · Cited by 35 · see citing works
Suzuki, Y., Tsuneyama, N., Fukui, N., et al. (2013) · Journal of Clinical Psychopharmacology · doi:10.1097/jcp.0b013e31828ecd52 · Cited by 25 · see citing works
Interaction Between Paliperidone and Carbamazepine
Yasui‐Furukori, N., Kubo, K., Ishioka, M., Tsuchimine, S., & Inoue, Y. (2013) · Therapeutic Drug Monitoring · doi:10.1097/ftd.0b013e3182966c2f · Cited by 24 · see citing works
Multiple inductive effects of carbamazepine on combined therapy with paliperidone and amlodipine
Akamine, Y., Uehara, H., Miura, M., et al. (2015) · Journal of Clinical Pharmacy and Therapeutics · doi:10.1111/jcpt.12286 · Cited by 14 · see citing works
Suzuki, H., Gen, K., Otomo, M., Inoue, Y., Hibino, H., Mikami, A. S., Matsumoto, H., & Mikami, K. (2014) · Human Psychopharmacology Clinical and Experimental · doi:10.1002/hup.2393 · Cited by 14 · see citing works
Helland, A., Syrstad, V. E. G., & Spigset, O. (2014) · Journal of Clinical Psychopharmacology · doi:10.1097/jcp.0000000000000240 · Cited by 9 · see citing works
Self-citation
Flagged first, then by citations
Cited by
Sorted by citations
Correll, 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 · see citing works
- Authors
- Helland, A., & Spigset, O.
- Affiliations
- Norwegian University of Science and Technology (NO)
- Corresponding author
- Helland, Arne
- Spigset, Olav
- Venue
- Therapeutic Drug Monitoring
- Published
- 2017-12
- Volume
- 39
- Issue
- 6
- Pages
- 659-662
- ISSN
- 0163-4356 (ISSN-L)
- PMC
- PMC5690301
- OpenAlex
- W2767154475
- Cited by
- 27
- References
- 20
- Citations by year
- 2026: 1 · 2025: 4 · 2024: 2 · 2023: 5 · 2022: 3 · 2021: 5 · 2020: 2 · 2019: 1 · 2018: 3 · 2017: 1
- FWCI
- 1.57
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Therapeutic Drug Monitoring (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- NORA - Norwegian Open Research Archives (submittedVersion, cc-by-nc-nd)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
- Keywords
- paliperidone, long-acting injectable antipsychotics, pharmacokinetics, carbamazepine, P-glycoprotein induction, age effects, interindividual variability, atypical antipsychotics
- MeSH terms
- Paliperidone Palmitate, Adult, Aged, Delayed-Action Preparations, Female, Humans, Male, Middle Aged, Antipsychotic Agents, Young Adult
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
