Intra- and Interindividual Variations in Steady-State Plasma Concentrations of Risperidone and 9-Hydroxyrisperidone in Schizophrenic Patients Treated Chronically with Various Doses of Risperidone

Therapeutic Drug Monitoring

Volumn 25, Issue 6, 2003, Pages 657-664

  Aravagiri, Manickam ^a   Marder, Stephen R ^a   Nuechterlein, Keith H ^a   Gitlin, Michael J ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

9 hydroxyrisperidone; Inter and intraindividual variations; LC MS MS; Plasma level monitoring; Risperidone; Steady state plasma levels

Indexed keywords

PALIPERIDONE; RISPERIDONE;

ADULT; ARTICLE; CHRONIC DISEASE; CLINICAL ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG METABOLISM; DRUG MONITORING; FEMALE; HUMAN; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; PRIORITY JOURNAL; SCHIZOPHRENIA; STEADY STATE;

ADULT; ANTIPSYCHOTIC AGENTS; DRUG MONITORING; FEMALE; HUMANS; ISOXAZOLES; MALE; PYRIMIDINES; RISPERIDONE;

EID: 0344198465     PISSN: 01634356     EISSN: None     Source Type: Journal    
DOI: 10.1097/00007691-200312000-00003     Document Type: Article

References (32)

1. Janssen PAJ, Niemegeers CJE, Awouters F, et al. Pharmacology of risperidone (R 64 766). A new antipsychotic with serotonin-S2 and dopamine-D2 antagonistic properties. J Pharmacol Exp Ther. 1988; 244:685-693.
2. Leysen JE, Gommeren W, Eens A, et al. Biochemical profile of risperidone, a new antipsychotic. J Pharmacol Exp Ther. 1988;247:661-670.
3. Megens AAHP, Awouters FHL, Schotte A, et al. Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994;114:9-23.
4. Farde L, Nyberg S, Oxenstiema G, et al. Positron emission tomography studies on D2 and 5-HT2 receptor binding in risperidone-treated schizophrenic patients. J Clin Psychopharmacol. 1995;15: 19S-23S.
5. He H, Richardson JS. A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5-HT2 and dopamine D2 receptors. Int Clin Psychopharmacol. 1995;10:19-30.
6. Borison RL, Diamond B, Pathiraja A, et al. Pharmacokinetics of risperidone in chronic schizophrenic patients. Psychopharmacol Bull. 1994;30:193-197.
7. Ereshefsky L. Pharmacokinetic and drug interactions: update for new antipsychotics. J Clin Psychiatry. 1996;11(suppl):12-25.
8. Fang J, Bourin M, Baker GB. Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn-Schmiedebergs Arch Pharmacol. 1999;359:147-151.
9. Scordo MG, Spina E, Facciolà G, et al. Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology. 1999;147:300-305.
10. Mannens G, Huang M-L, Meuldermans W, et al. Absorption, metabolism, and excretion of risperidone in humans. Drug Metab Dispos. 1993;21:1134-1141.
11. Meuldermans W, Hendrickx J, Mannens G, et al. The metabolism and excretion of risperidone after oral administration in rats and dogs. Drug Metab Dispos. 1994;22:129-138.
12. Aravagiri M, Yuwiler A, Marder SR. Distribution after repeated oral administration of different dose levels of risperidone and 9-hydroxyrisperidone in the brain and other tissues of rat. Psychopharmacology (Berl). 1998;139:356-363.
13. Aravagiri M, Marder SR. Brain, plasma and tissue pharmacokinetics of risperidone and 9-hydroxyrisperidone after separate oral administration to rats. Psychopharmacology (Berl). 2002;159:424-431.
14. Van Beijsterveldt LEC, Geerts RJF, Leysen JE, et al. Regional brain distribution of risperidone and its active metabolite 9-hydroxyrisperidone in the rat. Psychopharmacology (Berl). 1994;114:53-62.
15. Huang ML, Van Peer A, Woestenborghs R, et al. Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects. Clin Pharmacol Ther. 1993;54:257-268.
16. Nyberg S, Dahl ML, Halldin C. A PET study of D2 and 5-HT2 receptor occupancy induced by risperidone in poor metabolizers of debrisoquin and risperidone. Psychopharmacology (Berl). 1995;119:345-348.
17. Darby JK, Pasta DJ, Elfand L, et al. Accumulation effects and interindividual and intraindividual variability in the nonresponder patient in the clinical practice setting. J Clin Pharmacol. 1997;17:478-484.
18. Spina E, Avenoso A, Facciolà G, et al. Relationship between plasma risperidone and 9-hydroxyrisperidone concentrations and clinical response in patients with schizophrenia. Psychopharmacology (Berl). 2001;153:238-243.
19. Odou P, Levron JC, Luyckx M, et al. Risperidone drug monitoring. A useful clinical tool? Clin Drug Invest. 2000;19:283-292.
20. Heykants J, Huang ML, Mannens G, et al. The pharmacokinetics of risperidone in humans: a summary. J Clin Psychiatry. 1994;55(suppl):13-17.
21. Olesen OV, Licht RW, Thomsen E, et al. Serum concentrations and side effects in psychiatric patients during risperidone therapy. Ther Drug Monit. 1998; 20:380-384.
22. Yasui-Furukori N, Hidestrand M, Spina E, et al. Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos. 2001;29:1263-1268.
23. Prior TI, Baker GB. Interactions between the cytochrome P450 system and the second-generation antipsychotics. J Psychiatry Neurosci. 2003;28:99-112.
24. Aravagiri M, Marder SR, Ames D, et al. Plasma concentrations of risperidone and its 9-hydroxy metabolite and their relationship to dose in schizophrenic patients: Simultaneous determination by a high performance liquid chromatography with electrochemical detection. Pharmacopsychiatry. 1998;31: 102-109.
25. Lee HS, Tan CH, Khoo YM, et al. Serum concentrations and clinical effects of risperidone in schizophrenic patients in Singapore - A preliminary report. Br J Clin Pharmacol. 1999;47:460-461.
26. Aravagiri M, Marder SR. Simultaneous determination of risperidone and 9-hydroxyrisperidone in plasma by liquid chromatography/electrospray tandem mass spectrometry. J Mass Spectrom. 2000;35:718-724.
27. Spina E, Avenoso A, Scordo MG, et al. Inhibition of risperidone metabolism by fluoxetine in patients with schizophrenia: a clinically relevant pharmacokinetic drug interaction. J Clin Psychopharmacol. 2002;22:419-423.
28. Kastelova A, Yanev S. Propranolol as an inhibitor of some cytochrome P450-dependent monooxygenase activities in native and induced rat liver microsomes. Methods Find Exp Clin Pharmacol. 2002;24:189-194.
29. Narimatsu S, Arai T, Masubuchi Y, et al. Inactivation of rat cytochrome P450 2D enzyme by a further metabolite of 4-hydroxypropranolol, the major and active metabolite of propranolol. Biol Pharm Bull. 2001;24:988-994.
30. Ohyama K, Nakajima M, Suzuki M, et al. Inhibitory effects of amiodarone and its N-deethylated metabolite on human cytochrome P450 activities: prediction of in vivo drug interactions. Br J Clin Pharmacol. 2000;49:244-253.
31. de Leon J, Bork J. Risperidone and cytochrome P450 3A. J Clin Psychiatry. 1997;58:450.
32. Spina E, Avenoso A, Facciolà G, et al. Plasma concentrations of risperidone and 9-hydroxyrisperidone: effect of comedication with carbamazepine or valproate. Ther Drug Monit. 2000;22:484-485.