Book contents
- The Clinical Use of Antipsychotic Plasma Levels
- Reviews
- The Clinical Use of Antipsychotic Plasma Levels
- Copyright page
- Half title page
- Contents
- Foreword
- Preface: How to Use This Handbook and Useful Tables for Handy Reference
- Introduction
- 1 Sampling Times for Oral and Long-Acting Injectable Agents
- 2 The Therapeutic Threshold and the Point of Futility
- 3 Level Interpretation Including Laboratory Reporting Issues, Responding to High Plasma Levels, Special Situations (Hepatic Dysfunction, Renal Dysfunction and Hemodialysis, Bariatric Surgery)
- 4 Tracking Oral Antipsychotic Adherence
- 5 What Is an Adequate Antipsychotic Trial? Using Plasma Levels to Optimize Psychiatric Response and Tolerability
- 6 Important Concepts about First-Generation Antipsychotics
- 7 Haloperidol and Haloperidol Decanoate
- 8 Fluphenazine and Fluphenazine Decanoate
- 9 Perphenazine and Perphenazine Decanoate
- 10 Zuclopenthixol and Zuclopenthixol Decanoate; Flupenthixol and Flupenthixol Decanoate
- 11 Chlorpromazine, Loxapine, Thiothixene, Trifluoperazine
- 12 Important Concepts about Second-Generation Antipsychotics
- 13 Clozapine
- 14 Risperidone Oral and Long-Acting Injectable; Paliperidone Oral and Long-Acting Injectable
- 15 Olanzapine and Olanzapine Pamoate
- 16 Aripiprazole, Aripiprazole Monohydrate, and Aripiprazole Lauroxil
- 17 Amisulpride, Asenapine, Lurasidone, Brexpiprazole, Cariprazine
- Appendix Therapeutic Threshold, Point of Futility, AGNP/ASCP Laboratory Alert Level, and Average Oral Concentration–Dose Relationships
- Index
- References
6 - Important Concepts about First-Generation Antipsychotics
Published online by Cambridge University Press: 19 October 2021
Book contents
- The Clinical Use of Antipsychotic Plasma Levels
- Reviews
- The Clinical Use of Antipsychotic Plasma Levels
- Copyright page
- Half title page
- Contents
- Foreword
- Preface: How to Use This Handbook and Useful Tables for Handy Reference
- Introduction
- 1 Sampling Times for Oral and Long-Acting Injectable Agents
- 2 The Therapeutic Threshold and the Point of Futility
- 3 Level Interpretation Including Laboratory Reporting Issues, Responding to High Plasma Levels, Special Situations (Hepatic Dysfunction, Renal Dysfunction and Hemodialysis, Bariatric Surgery)
- 4 Tracking Oral Antipsychotic Adherence
- 5 What Is an Adequate Antipsychotic Trial? Using Plasma Levels to Optimize Psychiatric Response and Tolerability
- 6 Important Concepts about First-Generation Antipsychotics
- 7 Haloperidol and Haloperidol Decanoate
- 8 Fluphenazine and Fluphenazine Decanoate
- 9 Perphenazine and Perphenazine Decanoate
- 10 Zuclopenthixol and Zuclopenthixol Decanoate; Flupenthixol and Flupenthixol Decanoate
- 11 Chlorpromazine, Loxapine, Thiothixene, Trifluoperazine
- 12 Important Concepts about Second-Generation Antipsychotics
- 13 Clozapine
- 14 Risperidone Oral and Long-Acting Injectable; Paliperidone Oral and Long-Acting Injectable
- 15 Olanzapine and Olanzapine Pamoate
- 16 Aripiprazole, Aripiprazole Monohydrate, and Aripiprazole Lauroxil
- 17 Amisulpride, Asenapine, Lurasidone, Brexpiprazole, Cariprazine
- Appendix Therapeutic Threshold, Point of Futility, AGNP/ASCP Laboratory Alert Level, and Average Oral Concentration–Dose Relationships
- Index
- References
Summary
First-generation antipsychotics (FGAs) have no unique therapeutic benefit compared to newer antipsychotics, but their utility derives from the fact that they are inexpensive, that multiple formulations exist including long-acting injectable (LAI) preparations, and that there is an extensive trove of plasma level studies for the more commonly used medications [1–5]. Large randomized trials such as the UK Cost Utility of the Latest Antipsychotic Drugs in Schizophrenia Study (CUtLASS-1) (n = 227) found that there was no disadvantage over 1 year of treatment in terms of quality of life, symptoms, or associated costs of care when using FGAs, compared to second-generation antipsychotics (SGAs) (clozapine excepted) [6].
- Type
- Chapter
- Information
- The Clinical Use of Antipsychotic Plasma LevelsStahl's Handbooks, pp. 147 - 156Publisher: Cambridge University PressPrint publication year: 2021
References
Van Putten, T., Marder, S. R., and Mintz, J. (1985). Plasma haloperidol levels: Clinical response and fancy mathematics. Arch Gen Psychiatry, 42, 835–838.Google Scholar
Van Putten, T., Marder, S. R., Wirshing, W. C., et al. (1991). Neuroleptic plasma levels. Schizophr Bull, 17, 197–216.Google Scholar
Midha, K. K., Hubbard, J. W., Marder, S. R., et al. (1994). Impact of clinical pharmacokinetics on neuroleptic therapy in patients with schizophrenia. J Psychiatry Neurosci, 19, 254–264.Google Scholar
de Oliveira, I. R., de Sena, E. P., Pereira, E. L., et al. (1996). Haloperidol blood levels and clinical outcome: A meta-analysis of studies relevant to testing the therapeutic window hypothesis. J Clin Pharm Ther, 21, 229–236.Google Scholar
Ulrich, S., Wurthmann, C., Brosz, M., et al. (1998). The relationship between serum concentration and therapeutic effect of haloperidol in patients with acute schizophrenia. Clin Pharmacokinet, 34, 227–263.Google Scholar
Jones, P. B., Barnes, T. R. E., Davies, L., et al. (2006). Randomized controlled trial of the effect on quality of life of second- vs first-generation antipsychotic drugs in schizophrenia: Cost Utility of the Latest Antipsychotic Drugs in Schizophrenia Study (CUtLASS 1). Arch Gen Psychiatry, 63, 1079–1087.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
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, 939–951.Google Scholar
Pillinger, T., McCutcheon, R. A., Vano, L., et al. (2020). Comparative effects of 18 antipsychotics on metabolic function in patients with schizophrenia, predictors of metabolic dysregulation, and association with psychopathology: A systematic review and network meta-analysis. Lancet Psychiatry, 7, 64–77.Google Scholar
Kahn, R. S., Winter van Rossum, I., Leucht, S., et al. (2018). Amisulpride and olanzapine followed by open-label treatment with clozapine in first-episode schizophrenia and schizophreniform disorder (OPTiMiSE): A three-phase switching study. Lancet Psychiatry, 5, 797–807.Google Scholar
Meyer, J. M. and Stahl, S. M. (2019). The Clozapine Handbook. Cambridge: Cambridge University Press.Google Scholar
Lieberman, J. A., Stroup, T. S., McEvoy, J. P., et al. (2005). Effectiveness of antipsychotic drugs in patients with chronic schizophrenia. N Engl J Med, 353, 1209–1223.Google Scholar
Xiong, G. L., Pinkhasov, A., Mangal, J. P., et al. (2020). QTc monitoring in adults with medical and psychiatric comorbidities: Expert consensus from the Association of Medicine and Psychiatry. J Psychosom Res, 135, 110138.Google Scholar
Van Putten, T., Marder, S. R., Mintz, J., et al. (1992). Haloperidol plasma levels and clinical response: A therapeutic window relationship. Am J Psychiatry, 149, 500–505.Google Scholar
Salem, H., Nagpal, C., Pigott, T., et al. (2017). Revisiting antipsychotic-induced akathisia: Current issues and prospective challenges. Curr Neuropharmacol, 15, 789–798.Google Scholar
Vinogradov, S., Fisher, M., Warm, H., et al. (2009). The cognitive cost of anticholinergic burden: Decreased response to cognitive training in schizophrenia. Am J Psychiatry, 166, 1055–1062.Google Scholar
Ang, M. S., Abdul Rashid, N. A., Lam, M., et al. (2017). The impact of medication anticholinergic burden on cognitive performance in people with schizophrenia. J Clin Psychopharmacol, 37, 651–656.Google Scholar
Eum, S., Hill, S. K., Rubin, L. H., et al. (2017). Cognitive burden of anticholinergic medications in psychotic disorders. Schizophr Res, 190, 129–135.Google Scholar
Meyer, J. M. and Koro, C. E. (2004). The effects of antipsychotic therapy on serum lipids: A comprehensive review. Schizophr Res, 70, 1–17.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, 342–353.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, 1237–1253.Google Scholar
de Leon, J., Wynn, G., and Sandson, N. B. (2010). The pharmacokinetics of paliperidone versus risperidone. Psychosomatics, 51, 80–88.Google Scholar
Covell, N. H., McEvoy, J. P., Schooler, N. R., et al. (2012). Effectiveness of switching from long-acting injectable fluphenazine or haloperidol decanoate to long-acting injectable risperidone microspheres: An open-label, randomized controlled trial. J Clin Psychiatry, 73, 669–675.Google Scholar
Leucht, S., Samara, M., Heres, S., et al. (2016). Dose equivalents for antipsychotic drugs: The DDD method. Schizophr Bull, 42 Suppl 1, S90–94.Google Scholar
Asmal, L., Flegar, S. J., Wang, J., et al. (2013). Quetiapine versus other atypical antipsychotics for schizophrenia. Cochrane Database Syst Rev, CD006625.Google Scholar
Vanasse, A., Blais, L., Courteau, J., et al. (2016). Comparative effectiveness and safety of antipsychotic drugs in schizophrenia treatment: A real-world observational study. Acta Psychiatr Scand, 134, 374–384.Google Scholar
Meyer, J. M., Davis, V. G., Goff, D. C., et al. (2008). Change in metabolic syndrome parameters with antipsychotic treatment in the CATIE Schizophrenia Trial: Prospective data from phase 1. Schizophr Res, 101, 273–286.Google Scholar
Meyer, J. M. (2010). Antipsychotics and metabolics in the post-CATIE era. Curr Top Behav Neurosci, 4, 23–42.Google Scholar
Regenthal, R., Kunstler, U., Junhold, U., et al. (1997). Haloperidol serum concentrations and D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate. Int Clin Psychopharmacol, 12, 255–261.Google Scholar
Fitzgerald, P. B., Kapur, S., Remington, G., et al. (2000). Predicting haloperidol occupancy of central dopamine D2 receptors from plasma levels. Psychopharmacology, 149, 1–5.Google Scholar
Nyberg, S., Farde, L., Bartfai, A., et al. (1995). Central D2 receptor occupancy and effects of zuclopenthixol acetate in humans. Int Clin Psychopharmacol, 10, 221–227.Google Scholar
Lundbeck Australia (2013). Clopixol, Clopixol Acuphase, Clopixol Depot package insert. North Ryde, NSW, Australia.Google Scholar
Chang, W. H., Lin, S. K., Juang, D. J., et al. (1993). Prolonged haloperidol and reduced haloperidol plasma concentrations after decanoate withdrawal. Schizophr Res, 9, 35–40.Google Scholar
Nyberg, S., Farde, L., and Halldin, C. (1996). Long-time persistence of D2 dopamine receptor occupancy after discontinuation of haloperidol decanoate. Schizophr Res, 18, 199–200.Google Scholar
Talvik, M., Nordstrom, A. L., Larsen, N. E., et al. (2004). A cross-validation study on the relationship between central D2 receptor occupancy and serum perphenazine concentration. Psychopharmacology, 175, 148–153.Google Scholar
Ereshefsky, L., Toney, G., Saklad, S. R., et al. (1993). A loading-dose strategy for converting from oral to depot haloperidol. Hosp Community Psychiatry, 44, 1155–1161.Google Scholar
Taylor, D. (2009). Psychopharmacology and adverse effects of antipsychotic long-acting injections: A review. Br J Psychiatry Suppl, 52, S13–19.Google Scholar
Dencker, S. J., Giös, I., Mårtensson, E., et al. (1994). A long-term cross-over pharmacokinetic study comparing perphenazine decanoate and haloperidol decanoate in schizophrenic patients. Psychopharmacology (Berl), 114, 24–30.Google Scholar