Pharmacokinetics of risperidone in chronic schizophrenic patients

R. L. Borison, B. Diamond, Ananda Pathiraja, R. C. Meibach

Research output: Contribution to journalArticle

32 Scopus citations

Abstract

In a randomized, crossover study, 24 schizophrenic patients received a single 4-mg dose of risperidone in caplet or tablet form. Each of the two study periods lasted 5 days. Blood samples to determine (by radioimmunoassay) plasma levels of risperidone and its major metabolite, 9-hydroxy-risperidone (9-OH-risperidone), were obtained each day. The two formulations of risperidone were bioequivalent. Following are the mean pharmacokinetics of risperidone and risperidone + 9-OH-risperidone: area under the plasma concentration curve (AUC) from 0 to 96 hours; 278.0 and 716.9 ng · hr/mL; AUC from 0 to infinity, 291.9 and 762.4 ng · hr/mL; peak plasma concentration, 33.0 and 44.5 ng/mL; time to peak concentration, 1.39 and 1.78 hours; and elimination half-life, 14.93 and 23.04 hours. These results demonstrate that the active moiety (risperidone plus 9-OH-risperidone) has a half-life of 23 hours and reveal a pool of risperidone (terminal half-life, 14.9 hours) that may allow twice-daily or even once-daily dosing.

Original languageEnglish (US)
Pages (from-to)193-197
Number of pages5
JournalPsychopharmacology Bulletin
Volume30
Issue number2
StatePublished - Jan 1 1994

Keywords

  • atypical neuroleptic
  • major
  • pharmacokinetics
  • risperidone
  • schizophrenia
  • tranquilizing agents

ASJC Scopus subject areas

  • Psychiatry and Mental health
  • Pharmacology

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    Borison, R. L., Diamond, B., Pathiraja, A., & Meibach, R. C. (1994). Pharmacokinetics of risperidone in chronic schizophrenic patients. Psychopharmacology Bulletin, 30(2), 193-197.