paliperidone-palmitate and Pain

To evaluate injection site reactions and pain following paliperidone palmitate 1-month (PP1M) and 3-month (PP3M) administration using safety data of double-blind (DB), noninferiority study.. Patients (n = 1,429) with schizophrenia, treated with PP1M (50-150 mg-eq, 17-week open-label [OL] phase) were randomized to PP1M or PP3M in 48-week DB phase.. PP1M and PP3M injections were well tolerated. Incidence of induration, redness, and swelling were low in both phases (OL: 9-12%; DB: 7-13%), and were mostly mild in both groups. Mean (SD) visual analog scale scores decreased from OL-baseline (22.0 [21.6]) to DB-baseline (19.5 [20.6] vs. 18.4 [20.4]) and DB-endpoint (15.6 [17.9] vs. 15.5 [18.3]).. Injection site reactions and pain were low and similar between both treatments, regardless of administration site and dose.

Topics: Adolescent; Adult; Aged; Antipsychotic Agents; Double-Blind Method; Drug Administration Schedule; Female; Humans; Injection Site Reaction; Male; Middle Aged; Pain; Paliperidone Palmitate; Schizophrenia; Visual Analog Scale; Young Adult

The objective of this study was to characterize the pharmacokinetics of 25, 100, and 150 mg equivalents (eq.) of paliperidone long-acting injection in Chinese subjects with schizophrenia.. This was an open-label, randomized, parallel group, multicenter study. A total of 48 patients were randomized in a 1:1:1 ratio to one of three groups. Sequential blood samples were collected immediately before injection on day 1 and up to 210 days after the first injection. The plasma paliperidone concentrations were determined by a validated high-performance liquid chromatography/tandem mass spectrometry method.. A total of 47 patients received at least one injection of the study medication, and 43 completed the study. The pharmacokinetic (PK) parameters, such as time to maximum concentration, t1/2, and CL/F, were comparable across the three treatment groups (p = 0.935, 0.349, and 0.794, respectively). The differences in maximum plasma concentration, AUC (035 days), AUC (0-210 days), and AUC (0-∞) were significant (p < 0.001) and dose proportional. The inter-individual variation of PK parameters was large. The most frequent treatment-emergent adverse events were prolactin level increasing, injection site pain, tremor, dry mouth, and constipation.. The pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150 mg eq.

Topics: Antipsychotic Agents; Asian People; Chromatography, High Pressure Liquid; Constipation; Dose-Response Relationship, Drug; Female; Humans; Injections, Intramuscular; Isoxazoles; Linear Models; Male; Middle Aged; Pain; Paliperidone Palmitate; Palmitates; Prolactin; Schizophrenia; Tandem Mass Spectrometry; Time Factors; Treatment Outcome; Tremor

This study assessed the efficacy and the safety of a dosing regimen that was revised from earlier studies for the investigational injectable atypical antipsychotic paliperidone palmitate (approved in the USA, August 2009) for adult patients with acutely exacerbated schizophrenia. The patients (N = 652) were randomly assigned (1:1:1:1) to paliperidone palmitate at 25, 100, or 150 mg eq. or placebo in this 13-week double-blind study. The patients received an injection of paliperidone palmitate at 150 mg eq. or placebo in the deltoid muscle on day 1 and the assigned fixed dose or placebo in the deltoid or gluteal [corrected] on day 8 and then once monthly (days 36 and 64). No oral supplementation was used. Target plasma levels were achieved by day 8 in all paliperidone palmitate groups. The mean change in Positive and Negative Syndrome Scale total score from baseline to end point improved significantly (P < or = 0.034) in all the paliperidone palmitate dose-groups versus placebo. Paliperidone palmitate treatment with this revised dosing regimen led to the achievement of rapid and consistent therapeutically effective plasma levels that were maintained by once-monthly dosing in either the deltoid or gluteal muscle. Common treatment-emergent adverse events (> or =2% of patients in any of the treatment groups) that occurred more frequently in the total paliperidone palmitate group versus the placebo group (with > or =1% difference) were injection-site pain (7.6% vs 3.7%), dizziness (2.5% vs 1.2%), sedation (2.3% vs 0.6%), pain in the extremity (1.6% vs 0.0%), and myalgia (1.0% vs 0.0%). The paliperidone palmitate treatment was efficacious and generally tolerated across the dose range (25, 100, or 150 mg eq.) in adult patients with acutely exacerbated schizophrenia.

Topics: Acute Disease; Adult; Dizziness; Dose-Response Relationship, Drug; Double-Blind Method; Female; Humans; Isoxazoles; Male; Pain; Paliperidone Palmitate; Palmitates; Schizophrenia; Treatment Outcome; Young Adult