Pharmacokinetics and D2 receptor occupancy of long-acting injectable risperidone (Risperdal Consta™) in patients with schizophrenia
Open accessAbstract
Thirteen patients with schizophrenia received injections of 25, 50, or 75 mg of long-acting risperidone every 2 wk. Brain D2 receptor occupancy was assessed with [11C]raclopride 2 wk after the last (fifth) injection (day 71) in seven subjects and 2 wk after the third injection (day 44) in one subject. Stable plasma concentrations were reached after the third injection and steady-state concentrations of the active moiety (risperidone + 9-hydroxyrisperidone) after the fourth injection. Steady-state plasma concentrations were maintained for 4-5 wk after the last injection and then declined rapidly. After injections of 25, 50 and 75 mg on day 44 or day 71, D2 receptor occupancy ranged from 25-48%, 59-83% and 62-72% respectively, while plasma active-moiety levels ranged from 4.4-8.8, 15.0-31.1 and 22.5-26.3 ng/ml respectively. The results indicate that brain D2 receptor occupancy at steady state after injections of long-acting risperidone was in the range found in patients effectively treated with 2-6 mg of oral risperidone.
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?
Administration of RLAI-MS every 2 weeks provides peak plasma concentration levels at approximately 4 weeks and a terminal apparent half-life of 3-6 days.
“Administration of RLAI-MS every 2 weeks provides peak plasma concentration levels at approximately 4 weeks and a terminal apparent half-life of 3–6 days [88].”
From Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview (2021) · cites this paper as [88]
The Introduction describes therapeutic plasma concentrations beginning 3–4 weeks after an injection, and the Pharmacokinetics section reports injections every two weeks. It does not identify approximately four weeks as the time of peak concentration; it reports a small initial peak at 8–24 hours and a mean plasma half-life of 4–6 days, rather than 3–6 days. Page numbers are unavailable in our copy. (LLM, conf=0.88)
Experimental — accuracy not yet measured
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
Clozapine for the Treatment-Resistant Schizophrenic: A Double-blind Comparison With Chlorpromazine
Kane, J. (1988) · Archives of General Psychiatry · doi:10.1001/archpsyc.1988.01800330013001 · Cited by 4,156 · see citing works
Farde, L. (1992) · Archives of General Psychiatry · doi:10.1001/archpsyc.1992.01820070032005 · Cited by 1,420 · see citing works
Risperidone in the treatment of schizophrenia
Marder, S. R., & Meibach, R. C. (1994) · American Journal of Psychiatry · doi:10.1176/ajp.151.6.825 · Cited by 1,194 · see citing works
Kapur, S., Zipursky, R. B., & Remington, G. J. (1999) · American Journal of Psychiatry · doi:10.1176/ajp.156.2.286 · Cited by 711 · see citing works
Wienhard, K., Dahlbom, M. L., Eriksson, L., Michel, C. J., Bruckbauer, T., Pietrzyk, U., & Heiss, W. (1994) · Journal of Computer Assisted Tomography · doi:10.1097/00004728-199401000-00023 · Cited by 561 · see citing works
Nordström, A., Farde, L., Wiesel, F., Forslund, K., Pauli, S., Halldin, C., & Uppfeldt, G. (1993) · Biological Psychiatry · doi:10.1016/0006-3223(93)90288-o · Cited by 527 · see citing works
Farde, L., Eriksson, L. I., Blomquist, G., & Halldin, C. (1989) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1038/jcbfm.1989.98 · Cited by 448 · see citing works
Davis, J. M., Metalon, L., Watanabe, M. D., & Blake, L. M. (1994) · Drugs · doi:10.2165/00003495-199447050-00004 · Cited by 295 · see citing works
Treatment of Schizophrenia With Long-Acting Injectable Risperidone
Fleischhacker, W. W., Eerdekens, M., Karcher, K., Remington, G. J., Llorca, P., Chrzanowski, W., Martin, S. D., & Gefvert, O. (2003) · The Journal of Clinical Psychiatry · doi:10.4088/jcp.v64n1017 · Cited by 288 · see citing works
Self-citationBeasley, C. M., Hamilton, S. H., Crawford, A. M., Dellva, M. A., Tollefson, G. D., Trân, P. V., Blin, O. J., & Beuzen, J. N. (1997) · European Neuropsychopharmacology · doi:10.1016/s0924-977x(96)00392-6 · Cited by 277 · see citing works
Dopamine blockade and clinical response: evidence for two biological subgroups of schizophrenia
Wolkin, A., Barouche, F., Wolf, A. P., Rotrosen, J., Fowler, J. S. L., Shiue, C., Cooper, T. B., & Brodie, J. D. (1989) · American Journal of Psychiatry · doi:10.1176/ajp.146.7.905 · Cited by 258 · see citing works
Nyberg, S., Eriksson, B., Oxenstierna, G., Halldin, C., & Farde, L. (1999) · American Journal of Psychiatry · doi:10.1176/ajp.156.6.869 · Cited by 251 · see citing works
Self-citationNeuroleptic Withdrawal in Schizophrenic Patients
Baldessarini, R. J. (1995) · Archives of General Psychiatry · doi:10.1001/archpsyc.1995.03950150021002 · Cited by 194 · see citing works
A depot neuroleptic withdrawal study
Wistedt, B., J�rgensen, A., & Wiles, D. (1982) · Psychopharmacology · doi:10.1007/bf00433729 · Cited by 133 · see citing works
Comparative Effectiveness of Fluphenazine Decanoate Injections Every 2 Weeks Versus Every 6 Weeks
Carpenter, W. T., Buchanan, R. W., Kirkpatrick, B., et al. (1999) · American Journal of Psychiatry · doi:10.1176/ajp.156.3.412 · Cited by 54 · see citing works
Ramstack, M., Grandolfi, G. P., Mannaert, E., D'Hoore, P., & Lasser, R. A. (2003) · Schizophrenia Research · doi:10.1016/s0920-9964(03)80260-8 · Cited by 35 · see citing works
Self-citationOral versus depot administration of neuroleptics in relapse prevention
Gerlach, J. (1994) · Acta Psychiatrica Scandinavica · doi:10.1111/j.1600-0447.1994.tb05862.x · Cited by 31 · see citing works
Large Variations of Plasma Levels During Maintenance Treatment with Depot Neuroleptics
Tuninger, E., & Levander, S. E. (1996) · The British Journal of Psychiatry · doi:10.1192/bjp.169.5.618 · Cited by 23 · see citing works
Dencker, S. J., Giös, I., Mårtensson, E., Nordén, T., Nyberg, G., Persson, R., Román, G. C., Stockman, O., & Svärd, K.-O. (1994) · Psychopharmacology · doi:10.1007/bf02245440 · Cited by 22 · see citing works
Dosing issues and depot medication in the maintenance treatment of schizophrenia.
Kane, J. M. (1995) · PubMed · Cited by 15 · see citing works
Flagged first, then by citations
Research works printed but not linked: 3
- Davis J (1975). Overview : maintenance therapy in psychiatry. American Journal of Psychiatry 132, 1237-1245.
- Halldin C, Farde L, Hogberg T, Hall H, Strom P, Ohlberger A, Solin O (1991). A comparative study of five carbon-11 or fluorine-18 labeled salicylamides. Preparation and in vitro dopamine D-2 receptor binding. International Journal of Radiation Applications and Instrumentation B 18, 871-881.
- Kane JM, Eerdekens M, Lindenmayer J-P, Keith SJ, Lesem M, Karcher K (2003). Long-acting risperidone : efficacy and safety of the first long-acting atypical antipsychotic. American Journal of Psychiatry 160, 1125-1132.
Cited by
Sorted by citations
The role of long-acting injectable antipsychotics in schizophrenia: a critical appraisal
Brissos, S., Veguilla, M. R., Taylor, D., & Balanzá-Martinez, V. (2014) · Therapeutic Advances in Psychopharmacology · doi:10.1177/2045125314540297 · Cited by 297 · see citing works
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
Uchida, H., Takeuchi, H., Graff-Guerrero, A., Suzuki, T., Watanabe, K., & Mamo, D. C. (2011) · Journal of Clinical Psychopharmacology · doi:10.1097/jcp.0b013e318218d339 · Cited by 94 · see citing works
Gomeni, R., Heidbreder, C., Fudala, P. J., & Nasser, A. F. (2013) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.141 · Cited by 38 · see citing works
Malla, A., Chue, P., Jordan, G., Stip, E., Koczerginski, D., Milliken, H., Joseph, A., Williams, R., Adams, B., Manchanda, R., et al. (2016) · Clinical Schizophrenia & Related Psychoses · doi:10.3371/csrp.mach.061213 · Cited by 30 · see citing works
Lee, L. H. N., Choi, C., Collier, A. C., Barr, A. M., Honer, W. G., & Procyshyn, R. M. (2015) · CNS Drugs · doi:10.1007/s40263-015-0295-2 · Cited by 19 · see citing works
- Authors
- Gefvert, O., Eriksson, B., Persson, P., Helldin, L., Björner, A., Mannaert, E., Remmerie, B., Eerdekens, M., & Nyberg, S.
- Affiliations
- Uppsala University (SE)
- Johnson & Johnson (Sweden) (SE)
- Norra Älvsborgs Länssjukhus (SE)
- University of Gothenburg (SE)
- Karolinska University Hospital (SE)
- Corresponding author
- Gefvert, Ola
- Venue
- The International Journal of Neuropsychopharmacology
- Publisher
- Oxford University Press (OUP)
- Published
- 2005-03
- Volume
- 8
- Issue
- 1
- Pages
- 27-36
- ISSN
- 1461-1457 (ISSN-L)
- 1469-5111
- OpenAlex
- W2172236423
- Cited by
- 119
- References
- 20
- Citations by year
- 2026: 2 · 2025: 6 · 2024: 1 · 2023: 3 · 2022: 3 · 2021: 12 · 2020: 5 · 2019: 2 · 2018: 5 · 2017: 5 · 2016: 4 · 2015: 2 · 2014: 8 · 2013: 8 · 2012: 3
- FWCI
- 5.60
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- The International Journal of Neuropsychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Cilag
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- long-acting injectable risperidone, Risperdal Consta, schizophrenia, pharmacokinetics, dopamine D2 receptor occupancy, [11C]raclopride PET, steady-state plasma concentration, paliperidone, antipsychotic drug delivery
- MeSH terms
- Paliperidone Palmitate, Administration, Oral, Adult, Binding, Competitive, Brain, Delayed-Action Preparations, Dose-Response Relationship, Drug, Drug Administration Schedule, Female, Humans, Image Processing, Computer-Assisted, Injections, Intramuscular, Isoxazoles, Male, Middle Aged, Pyrimidines, Radioimmunoassay, Schizophrenia, Scintillation Counting, Antipsychotic Agents, Receptors, Dopamine D2, Dopamine Antagonists, Risperidone, Positron-Emission Tomography
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
