Intramuscular Injections of Paliperidone Palmitate in the Arm or Buttock of Subjects With Schizophrenia
Condition: Schizophrenia
MeSH terms: Schizophrenia
Study type: Interventional
Phase: Phase 3

Summary: 
      The purpose of the study is to compare the pharmacokinetic parameters (blood concentrations)
      of i.m. paliperidone palmitate after administration in 2 different injection sites (deltoid
      or gluteal).
    

Detailed description: 
      An i.m. paliperidone palmitate long-acting formulation is under development with the aim to
      provide a sustained and stable level of paliperidone during each treatment cycle. The goal of
      this study is to determine the similarity in pharmacokinetic (blood levels) and safety
      profile after 2 intramuscular injections of paliperidone palmitate in the arm (deltoid
      muscle) and the buttock (gluteal muscle), in the dose range that will be covered in later
      Phase 3 trials (25 - 150 mg eq.). This is a repeated-dose, open-label, parallel group study
      in patients with schizophrenia. The study consists of an up to 5-day screening period, an up
      to 3-day tolerability period, a 14-day washout period, and a 64-day treatment period. As
      paliperidone is the active metabolite of risperidone, all patients will be exposed to oral
      risperidone during the screening period to confirm that they do not develop allergic
      reactions to risperidone, and to help the investigator to assign patients to 1 of the 2
      treatment doses. There will be a washout of at least 2 weeks after the last oral risperidone
      intake before patients receive the first injection of paliperidone palmitate. Each treatment
      group (arm or buttock injection) will receive 2 consecutive i.m. injections of the
      long-acting formulation of paliperidone palmitate with a one-week interval. Whole blood
      samples will be collected for the determination of paliperidone palmitate and paliperidone
      concentrations in plasma. Whole blood samples will be obtained by venipuncture (needle stick)
      immediately before (pre-dose) and at 4, 8, 12, 24, 48, 72, and 96 hours after the 1st and 2nd
      injections of paliperidone palmitate. Following the collection of the 96-hour blood sample
      after the 2nd injection, additional samples will be collected every 3 to 7 days through the
      end of the 64-day treatment period. Safety will assessed throughout the study by monitoring
      adverse events; changes in clinical laboratory results; tardive dyskinesia will be rated
      using the Abnormal Involuntary Movement Scale (AIMS), akathisia will be rated according to
      the Barnes Akathisia Rating Scale (BARS), extrapyramidal symptoms will be evaluated using the
      Simpson-Angus Rating Scale (SAS); physical examinations; electrocardiograms (ECGs); and
      patient evaluation of the injection site. Paliperidone palmitate (25 or 150 mg eq.), 2 i.m.
      doses administered at a 1-week interval. Depending on the randomized treatment group, each
      patient will receive 3 doses of oral risperidone: either 1 mg once daily for 3 days or 2 mg
      once on the 1st day, 4 mg once on the 2nd day, and 6 mg once on the 3rd day.
    

Intervention name(s): Paliperidone Palmitate
Intervention type(s): Drug
Intervention MeSH terms: Paliperidone Palmitate
Allocation: Randomized
Intervention model: Single Group Assignment
Masking: None (Open Label)
Primary purpose: Treatment
Keywords: Schizophrenia; Paliperidone palmitate; R092670; antipsychotic