Long-acting injectable risperidone and metabolic ratio: a possible index of clinical outcome in treatment-resistant schizophrenic patients

Psychopharmacology (Berl). 2010 Jul;210(4):489-97. doi: 10.1007/s00213-010-1852-5. Epub 2010 Apr 27.

Abstract

Rationale: It is still common to encounter a partial or no response to antipsychotic treatment in clinical practice, but only individual case reports are currently available concerning the efficacy of long-acting risperidone (RLAI) in treatment-resistant schizophrenia. The relationship between RSP and 9-OH-RSP plasma levels, and clinical response or tolerability has not yet been thoroughly assessed.

Methods: This open-label, non-randomised study involved 30 outpatients with treatment-resistant schizophrenia, who were prescribed RLAI for 6 months, and clinically evaluated using the Brief Psychiatric Rating Scale (BPRS), the Positive and Negative Symptoms Scale (PANSS), the Clinical Global Impression-Improvement Scale (CGI-I), and the Simpson and Angus Scale for Extrapyramidal Side Effects (EPSE). Plasma RSP and 9-OH-RSP levels were determined at steady-state, and the metabolic ratio (MR) was calculated as plasma 9-OH-RSP/RSP levels.

Results: At the end of the study, 60% of the patients responded to RLAI (a >or=20% reduction in the PANSS score). Linear regression analysis showed a significant positive relationship between the RSP dose and active moiety (RSP + 9-OH-RSP) (r = 0.4; p = 0.02). There was a significant positive relationship between active moiety and EPSE scores (r = 0.6; p = 0.00). The BPRS responders had a significantly higher mean MR than the non-responders (3.41 +/- 1.87 SD vs 1.60 +/- 0.98 SD) (p = 0.00).

Conclusions: Therapeutic drug monitoring seems to be useful in optimising the dose of RLAI, especially in the case of tolerability problems. MR might be a better index of clinical response to RLAI than the value of the active moiety, although this needs to be confirmed by further data.

Publication types

  • Clinical Trial

MeSH terms

  • Adolescent
  • Adult
  • Antipsychotic Agents / administration & dosage
  • Antipsychotic Agents / blood*
  • Biomarkers, Pharmacological / blood*
  • Brief Psychiatric Rating Scale
  • Delayed-Action Preparations / metabolism*
  • Dose-Response Relationship, Drug
  • Drug Monitoring / methods*
  • Drug Resistance
  • Female
  • Humans
  • Injections, Intramuscular
  • Isoxazoles / blood*
  • Male
  • Middle Aged
  • Paliperidone Palmitate
  • Psychiatric Status Rating Scales
  • Pyrimidines / blood*
  • Risperidone / administration & dosage
  • Risperidone / adverse effects
  • Risperidone / blood*
  • Schizophrenia / blood
  • Schizophrenia / diagnosis
  • Schizophrenia / drug therapy*
  • Severity of Illness Index

Substances

  • Antipsychotic Agents
  • Biomarkers, Pharmacological
  • Delayed-Action Preparations
  • Isoxazoles
  • Pyrimidines
  • Risperidone
  • Paliperidone Palmitate