Skip to main content Accessibility help
×
Hostname: page-component-7bb8b95d7b-wpx69 Total loading time: 0 Render date: 2024-09-12T12:18:47.923Z Has data issue: false hasContentIssue false

14 - Risperidone Oral and Long-Acting Injectable; Paliperidone Oral and Long-Acting Injectable

Published online by Cambridge University Press:  19 October 2021

Jonathan M. Meyer
Affiliation:
University of California, San Diego
Stephen M. Stahl
Affiliation:
University of California, Riverside and San Diego
Get access

Summary

Zotepine was approved in Japan in 1982, and is the first antipsychotic modeled on clozapine with relatively high serotonin 5HT2A affinity, lower dopamine D2 affinity, and a corresponding Positron Emission Tomography (PET) imaging profile that demonstrates wide separation between the 5HT2A and D2 occupancy curves in a manner unlike first-generation antipsychotics (FGAs) such as loxapine (see Chapter 11) [12–14]. Zotepine was never approved in the United States (US), Canada, the United Kingdom, Australia, or most European countries, leaving risperidone (US approval December 29, 1993) as the first commercially successful second-generation antipsychotic [15].

Type
Chapter
Information
The Clinical Use of Antipsychotic Plasma Levels
Stahl's Handbooks
, pp. 267 - 295
Publisher: Cambridge University Press
Print publication year: 2021

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

References

de Leon, J., Wynn, G., and Sandson, N. B. (2010). The pharmacokinetics of paliperidone versus risperidone. Psychosomatics, 51, 8088.Google Scholar
Remington, G., Mamo, D., Labelle, A., et al. (2006). A PET study evaluating dopamine D2 receptor occupancy for long-acting injectable risperidone. Am J Psychiatry, 163, 396401.Google Scholar
Uchida, H., Takeuchi, H., Graff-Guerrero, A., et al. (2011). Predicting dopamine D2 receptor occupancy from plasma levels of antipsychotic drugs: a systematic review and pooled analysis. J Clin Psychopharmacol, 31, 318325.Google Scholar
Leucht, S., Samara, M., Heres, S., et al. (2014). Dose equivalents for second-generation antipsychotics: the minimum effective dose method. Schizophr Bull, 40, 314326.Google Scholar
Schoretsanitis, G., Spina, E., Hiemke, C., et al. (2017). A systematic review and combined analysis of therapeutic drug monitoring studies for long-acting risperidone. Expert Rev Clin Pharmacol, 10, 965981.Google Scholar
Schoretsanitis, G., Kane, J. M., Correll, C. U., et al. (2020). Blood levels to optimize antipsychotic treatment in clinical practice; a joint consensus statement of the American Society of Clinical Psychopharmacology (ASCP) and the Therapeutic Drug Monitoring (TDM) Task Force of the Arbeitsgemeinschaft für Neuropsychopharmakologie und Pharmakopsychiatrie (AGNP). J Clin Psychiatry, 81, https://doi.org/10.4088/JCP.4019cs13169.Google Scholar
Ezewuzie, N. and Taylor, D. (2006). Establishing a dose-response relationship for oral risperidone in relapsed schizophrenia. J Psychopharmacol, 20, 8690.Google Scholar
Ikai, S., Remington, G., Suzuki, T., et al. (2012). A cross-sectional study of plasma risperidone levels with risperidone long-acting injectable: implications for dopamine D2 receptor occupancy during maintenance treatment in schizophrenia. J Clin Psychiatry, 73, 11471152.Google Scholar
Meyer, J. M. (2014). A rational approach to employing high plasma levels of antipsychotics for violence associated with schizophrenia: case vignettes. CNS Spectr, 19, 432438.Google Scholar
Schoretsanitis, G., Spina, E., Hiemke, C., et al. (2018). A systematic review and combined analysis of therapeutic drug monitoring studies for oral paliperidone. Expert Rev Clin Pharmacol, 11, 625639.Google Scholar
Arakawa, R., Ito, H., Takano, A., et al. (2008). Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia. Psychopharmacology, 197, 229235.Google Scholar
Kapur, S., Zipursky, R., Remington, G., et al. (1997). PET evidence that loxapine is an equipotent blocker of 5-HT2 and D2 receptors: implications for the therapeutics of schizophrenia. Am J Psychiatry, 154, 15251529.Google Scholar
Barnas, C., Quiner, S., Tauscher, J., et al. (2001). In vivo (123)I IBZM SPECT imaging of striatal dopamine 2 receptor occupancy in schizophrenic patients. Psychopharmacology (Berl), 157, 236242.Google Scholar
Tauscher, J., Kufferle, B., Asenbaum, S., et al. (2002). Striatal dopamine-2 receptor occupancy as measured with [123I]iodobenzamide and SPECT predicted the occurrence of EPS in patients treated with atypical antipsychotics and haloperidol. Psychopharmacology, 162, 4249.Google Scholar
Nyberg, S., Farde, L., Eriksson, L., et al. (1993). 5-HT2 and D2 dopamine receptor occupancy in the living human brain: a PET study with risperidone. Psychopharmacology, 110, 265272.Google Scholar
Ereshefsky, L. and Mascarenas, C. A. (2003). Comparison of the effects of different routes of antipsychotic administration on pharmacokinetics and pharmacodynamics. J Clin Psychiatry, 64, 1823.Google Scholar
Samtani, M. N., Vermeulen, A., and Stuyckens, K. (2009). Population pharmacokinetics of intramuscular paliperidone palmitate in patients with schizophrenia: a novel once-monthly, long-acting formulation of an atypical antipsychotic. Clin Pharmacokinet, 48, 585600.Google Scholar
Gomeni, R., Heidbreder, C., Fudala, P. J., et al. (2013). A model-based approach to characterize the population pharmacokinetics and the relationship between the pharmacokinetic and safety profiles of RBP-7000, a new, long-acting, sustained-released formulation of risperidone. J Clin Pharmacol, 53, 10101019.Google Scholar
Kapur, S., Zipursky, R. B., and Remington, G. (1999). Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia. Am J Psychiatry, 156, 286293.Google Scholar
Huhn, M., Nikolakopoulou, A., Schneider-Thoma, J., et al. (2019). Comparative efficacy and tolerability of 32 oral antipsychotics for the acute treatment of adults with multi-episode schizophrenia: a systematic review and network meta-analysis. Lancet, 394, 939951.Google Scholar
Gaebel, W., Riesbeck, M., von Wilmsdorff, M., et al. (2010). Drug attitude as predictor for effectiveness in first-episode schizophrenia: results of an open randomized trial (EUFEST). Eur Neuropsychopharmacol, 20, 310316.Google Scholar
Boulton, D. W., DeVane, C. L., Liston, H. L., et al. (2002). In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sciences, 71, 163169.Google Scholar
Nakagami, T., Yasui-Furukori, N., Saito, M., et al. (2005). Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition. Clin Pharmacol Ther, 78, 4351.Google Scholar
Wang, R., Sun, X., Deng, Y. S., et al. (2018). ABCB1 1199G > A polymorphism impacts transport ability of P-gp-mediated antipsychotics. DNA Cell Biol, 37, 325329.+A+polymorphism+impacts+transport+ability+of+P-gp-mediated+antipsychotics.+DNA+Cell+Biol,+37,+325–329.>Google Scholar
Linnet, K. and Ejsing, T. B. (2008). A review on the impact of P-glycoprotein on the penetration of drugs into the brain: focus on psychotropic drugs. Eur Neuropsychopharmacol, 18, 157169.Google Scholar
Hartter, S., Huwel, S., Lohmann, T., et al. (2003). How does the benzamide antipsychotic amisulpride get into the brain? – An in vitro approach comparing amisulpride with clozapine. Neuropsychopharmacology, 28, 19161922.Google Scholar
Janssen Pharmaceuticals Inc. (2019). Invega package insert. Titusville, NJ.Google Scholar
Janssen Pharmaceuticals Inc. (2020). Risperdal package insert. Titusville, NJ.Google Scholar
O’Brien, F. E., Dinan, T. G., Griffin, B. T., et al. (2012). Interactions between antidepressants and P-glycoprotein at the blood-brain barrier: clinical significance of in vitro and in vivo findings. Br J Pharmacol, 165, 289312.Google Scholar
Zanger, U. M. and Schwab, M. (2013). Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation. Pharmacol Ther, 138, 103141.Google Scholar
de Leon, J., Sandson, N. B., and Cozza, K. L. (2008). A preliminary attempt to personalize risperidone dosing using drug–drug interactions and genetics, Part II. Psychosomatics, 48, 347361.Google Scholar
Verbeeck, R. K. (2008). Pharmacokinetics and dosage adjustment in patients with hepatic dysfunction. Eur J Clin Pharmacol, 64, 11471161.Google Scholar
Meyer, J. M. (2018). Pharmacotherapy of psychosis and mania. In Brunton, L. L., Hilal-Dandan, R. and Knollmann, B. C., eds., Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 13th edn. Chicago, IL: McGraw-Hill, pp. 279302.Google Scholar
Selmin, F., Blasi, P., and DeLuca, P. P. (2012). Accelerated polymer biodegradation of risperidone poly(D, L-lactide-co-glycolide) microspheres. AAPS PharmSciTech, 13, 14651472.Google Scholar
Fleischhacker, W. W., Eerdekens, M., Karcher, K., et al. (2003). Treatment of schizophrenia with long-acting injectable risperidone: a 12-month open-label trial of the first long-acting second-generation antipsychotic. J Clin Psychiatry, 64, 12501257.Google Scholar
Wilson, W. H. (2004). A visual guide to expected blood levels of long-acting injectable risperidone in clinical practice. J Psychiatr Pract, 10, 393401.Google Scholar
Kane, J. M., Eerdekens, M., Lindenmayer, J. P., et al. (2003). Long-acting injectable risperidone: efficacy and safety of the first long-acting atypical antipsychotic. Am J Psychiatry, 160, 11251132.Google Scholar
Meltzer, H. Y., Lindenmayer, J. P., Kwentus, J., et al. (2014). A six month randomized controlled trial of long acting injectable risperidone 50 and 100mg in treatment resistant schizophrenia. Schizophr Res, 154, 1422, https://doi.org/10.1016/j.schres.2014.1002.1015.Google Scholar
Schoretsanitis, G., Spina, E., Hiemke, C., et al. (2018). A systematic review and combined analysis of therapeutic drug monitoring studies for long-acting paliperidone. Expert Rev Clin Pharmacol, 11, 12371253.Google Scholar
Janssen Pharmaceuticals Inc. (2020). Risperdal Consta package insert. Titusville, NJ.Google Scholar
Gefvert, O., Eriksson, B., Persson, P., et al. (2005). Pharmacokinetics and D2 receptor occupancy of long-acting injectable risperidone (Risperdal Consta) in patients with schizophrenia. Int J Neuropsychopharmacol, 8, 2736.Google Scholar
Janssen Pharmaceuticals Inc. (2019). Invega Trinza package insert. Titusville, NJ.Google Scholar
Haddad, P., Lambert, T., and Lauriello, J., eds. (2016). Antipsychotic Long-Acting Injections, 2nd edn. New York: Oxford University Press.Google Scholar
Nasser, A. F., Henderson, D. C., Fava, M., et al. (2016). Efficacy, safety, and tolerability of RBP-7000 once-monthly risperidone for the treatment of acute schizophrenia: an 8-week, randomized, double-blind, placebo-controlled, multicenter phase 3 study. J Clin Psychopharmacol, 36, 130140.Google Scholar
Ivaturi, V., Gopalakrishnan, M., Gobburu, J. V. S., et al. (2017). Exposure-response analysis after subcutaneous administration of RBP-7000, a once-a-month long-acting Atrigel formulation of risperidone. Br J Clin Pharmacol, 83, 14761498.Google Scholar
Southard, G. L., Dunn, R. L., and Garrett, S. (1998). The drug delivery and biomaterial attributes of the ATRIGEL technology in the treatment of periodontal disease. Expert Opin Investig Drugs, 7, 14831491.Google Scholar
Meyer, J. M. (2018). Risperidone extended-release injectable suspension. Curr Psychiatr, 17, 2333.Google Scholar
Laffont, C. M., Gomeni, R., Zheng, B., et al. (2014). Population pharmacokinetics and prediction of dopamine D2 receptor occupancy after multiple doses of RBP-7000, a new sustained-release formulation of risperidone, in schizophrenia patients on stable oral risperidone treatment. Clin Pharmacokinet, 53, 533543.Google Scholar
Laffont, C. M., Gomeni, R., Zheng, B., et al. (2015). Population pharmacokinetic modeling and simulation to guide dose selection for RBP-7000, a new sustained-release formulation of risperidone. J Clin Pharmacol, 55, 93103.Google Scholar
Indivior Inc. (2019). Perseris package insert. North Chesterfield, VA 23235.Google Scholar
Janssen Pharmaceuticals Inc. (2019). Invega Sustenna package insert. Titusville, NJ.Google Scholar
Pandina, G. J., Lindenmayer, J. P., Lull, J., et al. (2010). A randomized, placebo-controlled study to assess the efficacy and safety of 3 doses of paliperidone palmitate in adults with acutely exacerbated schizophrenia. J Clin Psychopharmacol, 30, 235244, https://doi.org/210.1097/JCP.1090b1013e3181dd3103.Google Scholar
Chouinard, G., Jones, B., Remington, G., et al. (1993). A Canadian multicenter placebo-controlled study of fixed doses of risperidone and haloperidol in the treatment of chronic schizophrenic patients. J Clin Psychopharmacol, 13, 2540.Google Scholar
Marder, S. R. and Meibach, R. C. (1994). Risperidone in the treatment of schizophrenia. Am J Psychiatry, 151, 825835.Google Scholar
Peuskens, J. (1995). Risperidone in the treatment of patients with chronic schizophrenia: a multi-national, multi-centre, double-blind, parallel-group study versus haloperidol. Risperidone Study Group. Br J Psychiatry, 166, 712726; discussion 727733.Google Scholar
Merlo, M. C., Hofer, H., Gekle, W., et al. (2002). Risperidone, 2 mg/day vs. 4 mg/day, in first-episode, acutely psychotic patients: treatment efficacy and effects on fine motor functioning. J Clin Psychiatry, 63, 885891.Google Scholar
Li, C., Xia, J., and Wang, J. (2009). Risperidone dose for schizophrenia. Cochrane Database Syst Rev, CD007474.Google Scholar
Kapur, S., Zipursky, R., Jones, C., et al. (2000). Relationship between dopamine D(2) occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia. Am J Psychiatry, 157, 514520.Google Scholar
Remington, G., Kapur, S., and Zipursky, R. (1998). The relationship between risperidone plasma levels and dopamine D2 occupancy: a positron emission tomographic study. J Clin Psychopharmacol, 18, 8283.Google Scholar
Karlsson, P., Hargarter, L., Dencker, E., et al. (2007). Pharmacokinetics and dopamine D2 and serotonin 5-HT2a receptor occupancy of paliperidone in healthy subjects: two open-label, single-dose studies (PAL-115). Pharmacopsychiatry, 40, A106.Google Scholar
Leucht, S., Crippa, A., Siafis, S., et al. (2020). Dose-response meta-analysis of antipsychotic drugs for acute schizophrenia. Am J Psychiatry, 177, 342353.Google Scholar
Samtani, M. N., Gopal, S., Gassmann-Mayer, C., et al. (2011). Dosing and switching strategies for paliperidone palmitate: based on population pharmacokinetic modelling and clinical trial data. CNS Drugs, 25, 829845.Google Scholar

Save book to Kindle

To save this book to your Kindle, first ensure [email protected] is added to your Approved Personal Document E-mail List under your Personal Document Settings on the Manage Your Content and Devices page of your Amazon account. Then enter the ‘name’ part of your Kindle email address below. Find out more about saving to your Kindle.

Note you can select to save to either the @free.kindle.com or @kindle.com variations. ‘@free.kindle.com’ emails are free but can only be saved to your device when it is connected to wi-fi. ‘@kindle.com’ emails can be delivered even when you are not connected to wi-fi, but note that service fees apply.

Find out more about the Kindle Personal Document Service.

Available formats
×

Save book to Dropbox

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Dropbox.

Available formats
×

Save book to Google Drive

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Google Drive.

Available formats
×