Characterization of Intramuscular Injections of Risperidone 4 Week Long-acting Injectable (LAI) Formulation in the Buttock of Patients With Schizophrenia
Condition: Psychotic Disorders; Schizophrenia
MeSH terms: Schizophrenia; Psychotic Disorders
Study type: Interventional
Phase: Phase 1

Summary: 
      The purpose of this study is to explore the pharmacokinetics, safety and tolerability of a
      4-week long-acting injectable (LAI) formulation of risperidone after single intramuscular
      (i.m.) injection of 75 mg risperidone LAI in the gluteal muscle.
    

Detailed description: 
      An intramuscular injectable formulation of risperidone long-acting formulation is under
      development with the aim to provide a sustained and stable level of risperidone during each
      treatment cycle given every 4 weeks. As this formulation is a long acting formulation,
      patients will be treated with a 1 mg immediate release (IR) formulation in the first week to
      confirm that the patient does not develop an allergic reaction to the drug before receiving
      the long acting injectable (LAI) formulation. Each patient receives a total of two
      injections. The first one is the immediate release formulation and the second one, which is
      given at least a week later, is the new long acting formulation. Eligible patients can stay
      on their previous oral medication, no tapering of medication is needed. Blood samples will be
      collected to determine the levels of risperidone and its major metabolite in plasma. Blood
      samples will be obtained by venipuncture (needle stick) immediately before (pre-dose) and at
      5, 10, 20, 30, 45 min, 1, 1.5, 2, 4, 6, 8,12, 16, 24, 36, 48, 72, 96 hours after the 1st
      injection and at 2, 6, 12, 24, 48, 96 hrs, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32,
      34, 36, 39, 43, 50, 57, 64, 71, 78, 85 days after the second injection of risperidone. Safety
      will assessed at visits throughout the study by monitoring scores of the Clinical Global
      Impression - Severity (CGI-S), scores of Extrapyramidal Symptom Rating Scale (ESRS), adverse
      events (AE), changes in clinical laboratory results, changes in physical examinations (PE),
      changes in electrocardiograms (ECGs), as well as patient and investigator evaluation of the
      injection site. The study has two periods. In the first period all patients will receive one
      injection of 1 mg risperidone IR (immediate release) solution (liquid). The follow-up
      duration is 96 hours. In the second period, patients will receive one injection of
      risperidone 4-week formulation of 75 mg. The follow-up duration is 85 days. The injections,
      administered in the muscle of the buttocks, will be given 7 to 14 days apart.
    

Intervention name(s): risperidone IR and LAI formulation
Intervention type(s): Drug
Intervention description(s): 1 mg risperidone IR single injection, followed after 7 to 14 days with 75mg risperidone 4-week-LAI single injection
Intervention MeSH terms: Risperidone
Allocation: Non-Randomized
Intervention model: Single Group Assignment
Masking: None (Open Label)
Primary purpose: Treatment
Keywords: Risperidone; Antipsychotic; Pharmacokinetic; Long-acting Injectable