Characterization of Intramuscular Injections of Risperidone 4 Week Long-acting Injectable (LAI) Formulation in the Buttock of Patients With Schizophrenia

Schizophrenia Clinical Trial

Official title:

Single-Dose, Open-Label Pilot Study to Explore the Pharmacokinetics, Safety and Tolerability of a Gluteal Intramuscular Injection of a 4-Week Long-Acting Injectable Formulation of Risperidone in Patients With Chronic Stable Schizophrenia

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT00821600
• Other study ID #: CR015742
• Status: Completed
• Phase: Phase 1
• First received: January 9, 2009
• Last updated: May 20, 2014
• Start date: December 2008
• Est. completion date: June 2009

Study information

• Verified date: May 2014
• Source: Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
• Contact: n/a
• Is FDA regulated: No
• Health authority: United States: Food and Drug Administration
• Study type: Interventional

Clinical Trial 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.

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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 24
• Est. completion date: June 2009
• Est. primary completion date: June 2009
• Accepts healthy volunteers: No
• Gender: Both
• Age group: 18 Years to 55 Years

Eligibility

Inclusion Criteria:

• Patients with a diagnosis of schizophrenia

• Clinically stable with no change in current antipsychotic medications

• Meet Positive and Negative Symptom Score (PANSS) and Clinical Global Impression (CGI) score criteria

• Have a body mass index (BMI) between 18 and 35 kilogram (kg)/meter (m)2

• If a woman, is postmenopausal surgically sterile, abstinent, or, if sexually active, is practicing before entry into the study and agrees to practice throughout the study an effective method of birth control

• If a man, agrees to use an adequate contraception method as deemed appropriate by the investigator

Exclusion Criteria:

• Alcohol or substance dependence, with the exception of nicotine or caffeine dependence

• Involuntarily-committed or unable to provide an informed consent

• Has tardive dyskinesia, History of Neuroleptic Malignant Syndrome

• History of or current clinically significant medical illness

• Treatment with any protocol disallowed therapies

• Clinically significant result from screening laboratory or ECG

Study Design

Allocation: Non-Randomized, Endpoint Classification: Pharmacokinetics Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment

Related Conditions & MeSH terms

• Mental Disorders
• Psychotic Disorders
• Schizophrenia

Intervention

Drug:
• risperidone IR and LAI formulation
1 mg risperidone IR single injection, followed after 7 to 14 days with 75mg risperidone 4-week-LAI single injection

Locations

Country	Name	City	State
n/a

Sponsors (1)

Lead Sponsor	Collaborator
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	To explore the pharmacokinetics of a 4-week long acting injectable (LAI) formulation of risperidone after single intramuscular (IM) injection of 75 mg in the gluteal muscle.		Up to 85 days for 4-week LAI formulation of risperidone and up to 96 hrs for immediate release (IR) formulation	No
Secondary	To explore safety and tolerability of a 4-week LAI formulation of risperidone by monitoring scores on CGI-S, scores on ESRS, AEs, PE, lab values, ECG values and injection site reactions.		Up to 85 days	No

External Links

•   Single Dose, Open Label Pilot Study to Explore the Pharmacokinetics, Safety and Tolerability of a Gluteal Intramuscular Injection of a 4 Week Long Acting Injectable Formulation of Risperidone in Subjects With Chronic Stable Schizophrenia