Intramuscular Injections of Paliperidone Palmitate in the Arm or Buttock of Subjects With Schizophrenia

2014-08-26 22:54:45 | BioPortfolio


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).


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.

Study Design

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




Paliperidone Palmitate




Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

Results (where available)

View Results


Published on BioPortfolio: 2014-08-26T22:54:45-0400

Clinical Trials [739 Associated Clinical Trials listed on BioPortfolio]

A Safety and Pharmacokinetic Study of Paliperidone Palmitate in Patients With Schizophrenia

The purpose of this study is to evaluate the long-term safety of flexible doses (50 to 150 mg equivalent) of paliperidone palmitate in the treatment of patients with schizophrenia and to d...

A Safety and Tolerability Study of Paliperidone Palmitate Injected in the Shoulder or the Buttock Muscle in Patients With Schizophrenia

The purpose of this study is to evaluate the safety and tolerability of intramuscular injections (to the buttocks or to the shoulders) of paliperidone palmitate in patients with schizophre...

A Study of Paliperidone Blood Concentrations in Patients With Schizophrenia After Administration of Paliperidone Palmitate

The purpose of this study is to evaluate the concentration of paliperidone in the blood after intramuscular injection in upper arm (deltoid muscle) or in the buttock (gluteal muscle) in pa...

A Study to Compare the Effectiveness and Safety of Flexibly Varied Doses of Paliperidone Palmitate and Risperidone in Treating Patients With Schizophrenia

The purpose of this study is to compare the effectiveness and safety over 1 year of treatment of intramuscular injections of paliperidone palmitate and long-acting risperidone in patients ...

Comparison of Paliperidone Palmitate and Risperdal Consta in Patients With Schizophrenia

The primary objective of this study is to demonstrate that the effectiveness of paliperidone palmitate in patient with Schizophrenia.

PubMed Articles [863 Associated PubMed Articles listed on BioPortfolio]

Qualify: a randomized head-to-head study of aripiprazole once-monthly and paliperidone palmitate in the treatment of schizophrenia.

To directly compare aripiprazole once-monthly 400mg (AOM 400) and paliperidone palmitate once-monthly (PP) on the Heinrichs-Carpenter Quality-of-Life Scale (QLS), a validated health-related quality of...

Paliperidone Palmitate Long-Acting Injectable Given Intramuscularly in the Deltoid Versus the Gluteal Muscle: Are They Therapeutically Equivalent?

Paliperidone palmitate long-acting injectable is a second-generation antipsychotic indicated for the treatment of schizophrenia. According to the product monograph, the monthly maintenance dose of pal...

Effectiveness and Predictors of Continuation of Paliperidone Palmitate Long-Acting Injection Treatment: A 12-Month Naturalistic Cohort Study.

Antipsychotic long-acting injectable (LAI) medication has an important place as a treatment option in schizophrenia with evolving evidence to support clinical benefit over oral medication. Paliperidon...

Long-Term Safety of Paliperidone Extended Release in Adolescents with Schizophrenia: An Open-Label, Flexible Dose Study.

The purpose of this study was to evaluate the long-term safety and tolerability of paliperidone extended-release (ER) in adolescents with schizophrenia.

Effectiveness of long-acting paliperidone palmitate in borderline personality disorder.

The aim of the present study is to test the efficacy of palmitate paliperidone long-acting injection for patients with borderline personality disorder (BPD). A total of 16 patients with BPD were treat...

Medical and Biotech [MESH] Definitions

A chronic form of schizophrenia characterized primarily by the presence of persecutory or grandiose delusions, often associated with hallucination.

A type of schizophrenia characterized by abnormality of motor behavior which may involve particular forms of stupor, rigidity, excitement or inappropriate posture.

An obsolete concept, historically used for childhood mental disorders thought to be a form of schizophrenia.

Enzyme catalyzing reversibly the hydrolysis of palmitoyl-CoA or other long-chain acyl coenzyme A compounds to yield CoA and palmitate or other acyl esters. The enzyme is involved in the esterification of fatty acids to form triglycerides. EC

A type of schizophrenia characterized by frequent incoherence; marked loosening of associations, or grossly disorganized behavior and flat or grossly inappropriate affect that does not meet the criteria for the catatonic type; associated features include extreme social withdrawal, grimacing, mannerisms, mirror gazing, inappropriate giggling, and other odd behavior. (Dorland, 27th ed)

More From BioPortfolio on "Intramuscular Injections of Paliperidone Palmitate in the Arm or Buttock of Subjects With Schizophrenia"


Relevant Topic

Arthritis Fibromyalgia Gout Lupus Rheumatic Rheumatology is the medical specialty concerned with the diagnosis and management of disease involving joints, tendons, muscles, ligaments and associated structures (Oxford Medical Diction...

Searches Linking to this Trial