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 language | English (US) |
|---|---|
| Pages (from-to) | 193-197 |
| Number of pages | 5 |
| Journal | Psychopharmacology Bulletin |
| Volume | 30 |
| Issue number | 2 |
| State | Published - Jan 1 1994 |
Keywords
- atypical neuroleptic
- major
- pharmacokinetics
- risperidone
- schizophrenia
- tranquilizing agents
ASJC Scopus subject areas
- Psychiatry and Mental health
- Pharmacology
