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1 - Sampling Times for Oral and Long-Acting Injectable Agents

Published online by Cambridge University Press:  19 October 2021

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

The use of antipsychotics to treat schizophrenia is fraught with many layers of complexity as prescribers try to tailor the pharmacodynamic properties of an agent to a specific patient based primarily on subjective response. Variations in drug metabolism related to genetic polymorphisms, or to medication or environmental exposures (e.g. smoking), and variable adherence with oral medications lead to scenarios that confound even seasoned clinicians. Excluding the realization that up to one-third of schizophrenia patients may not respond adequately to non-clozapine antipsychotics, 60 years of antipsychotic research has demonstrated that dose is a poor correlate of response likelihood, whereas plasma drug levels represent the best clinically available tool that quantifies the relationship between drug exposure and central nervous system (CNS) activity [1].

Type
Chapter
Information
The Clinical Use of Antipsychotic Plasma Levels
Stahl's Handbooks
 , pp. 13 - 33
Publisher: Cambridge University Press
Print publication year: 2021

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References

Preskorn, S. H. (2010). Outliers on the dose–response curve: How to minimize this problem using therapeutic drug monitoring, an underutilized tool in psychiatry. J Psychiatr Pract, 16, 177–182.Google Scholar
McCutcheon, R., Beck, K., D’Ambrosio, E., et al. (2018). Antipsychotic plasma levels in the assessment of poor treatment response in schizophrenia. Acta Psychiatr Scand, 137, 39–46.Google Scholar
Velligan, D. I., Wang, M., Diamond, P., et al. (2007). Relationships among subjective and objective measures of adherence to oral antipsychotic medications. Psychiatr Serv, 58, 1187–1192.Google Scholar
Velligan, D. I., Maples, N. J., Pokorny, J. J., et al. (2020). Assessment of adherence to oral antipsychotic medications: What has changed over the past decade? Schizophr Res, 215, 17–24.Google Scholar
Polasek, T. M., Tucker, G. T., Sorich, M. J., et al. (2018). Prediction of olanzapine exposure in individual patients using physiologically based pharmacokinetic modelling and simulation. Br J Clin Pharmacol, 84, 462–476.Google Scholar
Hiemke, C., Bergemann, N., Clement, H. W., et al. (2018). Consensus guidelines for therapeutic drug monitoring in neuropsychopharmacology: Update 2017. Pharmacopsychiatry, 51, 9–62.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
Wode-Helgodt, B. and Alfredsson, G. (1981). Concentrations of chlorpromazine and two of its active metabolites in plasma and cerebrospinal fluid of psychotic patients treated with fixed drug doses. Psychopharmacology (Berl), 73, 55–62.Google Scholar
Perera, V., Bies, R. R., Mo, G., et al. (2014). Optimal sampling of antipsychotic medicines: A pharmacometric approach for clinical practice. Br J Clin Pharmacol, 78, 800–814.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. 279–302.Google Scholar
Nakamura, T., Kubota, T., Iwakaji, A., et al. (2016). Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment). Drug Des Devel Ther, 10, 327–338.Google Scholar
Allergan USA Inc. (2019). Vraylar package insert. Madison, NJ.Google Scholar
Takeuchi, H., Powell, V., Geisler, S., et al. (2016). Clozapine administration in clinical practice: Once-daily versus divided dosing. Acta Psychiatr Scand, 134, 234–240.Google Scholar
Hagi, K., Tadashi, N. and Pikalov, A. (2020). S5. Does the time of drug administration alter the adverse event risk of lurasidone? Schizophr Bull, 46, S31–32.Google Scholar
Yu, C. and Gopalakrishnan, G. (2018). In vitro pharmacological characterization of SPN-810 M (molindone). J Exp Pharmacol, 10, 65–73.Google Scholar
Greenberg, W. M. and Citrome, L. (2007). Ziprasidone for schizophrenia and bipolar disorder: A review of the clinical trials. CNS Drug Rev, 13, 137–177.Google Scholar
Meyer, J. M. and Stahl, S. M. (2019). The Clozapine Handbook. Cambridge: Cambridge University Press.Google Scholar
Claghorn, J. L. (1985). Review of clinical and laboratory experiences with molindone hydrochloride. J Clin Psychiatry, 46, 30–33.Google Scholar
Meltzer, H. Y., Cucchiaro, J., Silva, R., et al. (2011). Lurasidone in the treatment of schizophrenia: A randomized, double-blind, placebo- and olanzapine-controlled study. Am J Psychiatry, 168, 957–967.Google Scholar
Loebel, A., Cucchiaro, J., Sarma, K., et al. (2013). Efficacy and safety of lurasidone 80 mg/day and 160 mg/day in the treatment of schizophrenia: A randomized, double-blind, placebo- and active-controlled trial. Schizophr Res, 145, 101–109.Google Scholar
Simpson, G. M., Cooper, T. B., Lee, J. H., et al. (1978). Clinical and plasma level characteristics of intramuscular and oral loxapine. Psychopharmacology (Berl), 56, 225–232.Google Scholar
Zetin, M., Cramer, M., Garber, D., et al. (1985). Bioavailability of oral and intramuscular molindone hydrochloride in schizophrenic patients. Clin Ther, 7, 169–175.Google Scholar
Midha, K. K., Hawes, E. M., Hubbard, J. W., et al. (1988). Variation in the single dose pharmacokinetics of fluphenazine in psychiatric patients. Psychopharmacology (Berl), 96, 206–211.Google Scholar
Dahl, M. L., Ekqvist, B., Widén, J., et al. (1991). Disposition of the neuroleptic zuclopenthixol cosegregates with the polymorphic hydroxylation of debrisoquine in humans. Acta Psychiatr Scand, 84, 99–102.Google Scholar
Midha, K. K., Hubbard, J. W., McKay, G., et al. (1993). The role of metabolites in a bioequivalence study I: Loxapine, 7-hydroxyloxapine and 8-hydroxyloxapine. Int J Clin Pharmacol Ther Toxicol, 31, 177–183.Google Scholar
Yeung, P. K., Hubbard, J. W., Korchinski, E. D., et al. (1993). Pharmacokinetics of chlorpromazine and key metabolites. Eur J Clin Pharmacol, 45, 563–569.Google Scholar
Wong, S. L. and Granneman, G. R. (1998). Modeling of sertindole pharmacokinetic disposition in healthy volunteers in short term dose-escalation studies. J Pharm Sci, 87, 1629–1631.Google Scholar
Kudo, S. and Ishizaki, T. (1999). Pharmacokinetics of haloperidol: An update. Clin Pharmacokinet, 37, 435–456.Google Scholar
Mauri, M. C., Volonteri, L. S., Colasanti, A., et al. (2007). Clinical pharmacokinetics of atypical antipsychotics: A critical review of the relationship between plasma concentrations and clinical response. Clin Pharmacokinet, 46, 359–388.Google Scholar
Meyer, J. M. (2020). Lumateperone for schizophrenia. Curr Psychiatr, 19, 33–39.Google Scholar
Spyker, D. A., Voloshko, P., Heyman, E. R., et al. (2014). Loxapine delivered as a thermally generated aerosol does not prolong QTc in a thorough QT/QTc study in healthy subjects. J Clin Pharmacol, 54, 665–674.Google Scholar
Meyer, J. M., Loebel, A. D., and Schweizer, E. (2009). Lurasidone: A new drug in development for schizophrenia. Expert Opin Investig Drugs, 18, 1715–1726.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, 1465–1472.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, 1476–1498.Google Scholar
Cheng, Y. F., Paalzow, L. K., Bondesson, U., et al. (1987). Pharmacokinetics of haloperidol in psychotic patients. Psychopharmacology (Berl), 91, 410–414.Google Scholar
Jann, M. W., Ereshefsky, L., and Saklad, S. R. (1985). Clinical pharmacokinetics of the depot antipsychotics. Clin Pharmacokinet, 10, 315–333.Google Scholar
Heres, S., Kraemer, S., Bergstrom, R. F., et al. (2014). Pharmacokinetics of olanzapine long-acting injection: The clinical perspective. Int Clin Psychopharmacol, 29, 299–312.Google Scholar
Ereshefsky, L., Saklad, S. R., Jann, M. W., et al. (1984). Future of depot neuroleptic therapy: Pharmacokinetic and pharmacodynamic approaches. J Clin Psychiatry, 45, 50–59.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, 585–600.Google Scholar
Lee, L. H., Choi, C., Collier, A. C., et al. (2015). The pharmacokinetics of second-generation long-acting injectable antipsychotics: Limitations of monograph values. CNS Drugs, 29, 975–983.Google Scholar
Meyer, J. M. (2013). Understanding depot antipsychotics: An illustrated guide to kinetics. CNS Spectr, 18, 55–68.Google Scholar
Marder, S. R., Midha, K. K., Van Putten, T., et al. (1991). Plasma levels of fluphenazine in patients receiving fluphenazine decanoate: Relationship to clinical response. Br J Psychiatry, 158, 658–665.Google Scholar
Janssen Pharmaceuticals Inc. (2020). Risperdal Consta package insert. Titusville, NJ.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, 393–401.Google Scholar
Larsen, N. E. and Hansen, L. B. (1989). Prediction of the optimal perphenazine decanoate dose based on blood samples drawn within the first three weeks. Ther Drug Monit, 11, 642–646.Google Scholar
Altamura, A. C., Sassella, F., Santini, A., et al. (2003). Intramuscular preparations of antipsychotics: Uses and relevance in clinical practice. Drugs, 63, 493–512.Google Scholar
Spanarello, S. and La Ferla, T. (2014). The pharmacokinetics of long-acting antipsychotic medications. Curr Clin Pharamacol, 9, 310–317.Google Scholar
Meyer, J. M. (2020). Monitoring and improving antipsychotic adherence in outpatient forensic diversion programs. CNS Spectr, 25, 136–144.Google Scholar
Hard, M. L., Mills, R. J., Sadler, B. M., et al. (2017). Aripiprazole lauroxil: Pharmacokinetic profile of this long-acting injectable antipsychotic in persons with schizophrenia. J Clin Psychopharmacol, 37, 289–295.Google Scholar
Hard, M. L., Mills, R. J., Sadler, B. M., et al. (2017). Pharmacokinetic profile of a 2-month dose regimen of aripiprazole lauroxil: A phase I study and a population pharmacokinetic model. CNS Drugs, 31, 617–624.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, 27–36.Google Scholar
Wiles, D. H., Kolakowska, T., McNeilly, A. S., et al. (1976). Clinical significance of plasma chlorpromazine levels. I: Plasma levels of the drug, some of its metabolites and prolactin during acute treatment. Psychol Med, 6, 407–415.Google Scholar
Kolakowska, T., Wiles, D. H., Gelder, M. G., et al. (1976). Clinical significance of plasma chlorpromazine levels. II: Plasma levels of the drug, some of its metabolites and prolactin in patients receiving long-term phenothiazine treatment. Psychopharmacology (Berl), 49, 101–107.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
Lee, J., Bies, R., Takeuchi, H., et al. (2016). Quantifying intraindividual variations in plasma clozapine levels: A population pharmacokinetic approach. J Clin Psychiatry, 77, 681–687.Google Scholar
Wei, F. C., Jann, M. W., Lin, H. N., et al. (1996). A practical loading dose method for converting schizophrenic patients from oral to depot haloperidol therapy. J Clin Psychiatry, 57, 298–302.Google Scholar
Castro, V. M., Roberson, A. M., McCoy, T. H., et al. (2016). Stratifying risk for renal insufficiency among lithium-treated patients: An electronic health record study. Neuropsychopharmacology, 41, 1138–1143.Google Scholar
Amdisen, A. (1977). Serum level monitoring and clinical pharmacokinetics of lithium. Clin Pharmacokinet, 2, 73–92.Google Scholar
Greil, W. (1981). [Pharmacokinetics and toxicology of lithium]. Bibl Psychiatr, 69–103.Google Scholar
Swartz, C. M. (1987). Correction of lithium levels for dose and blood sampling times. J Clin Psychiatry, 48, 60–64.Google Scholar

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