Paliperidone is a well known dopamine antagonist of the atypical antipsychotic class. In the present study Paliperidone was formulated as ER release tablets using natural and synthetic polymers separately or in combination. The aim of ER release formulation is to reduce the frequency of dosing. Tablets are prepared by direct compression method. The optimized formulations contain Paliperidone as...

The schizophrenia is a psychiatric disease, characterized by symptoms alterating the mind, behaviour and emotion. The terms antipsychotic and neuroleptic define a group of drugs mainly used to treat schizophrenia. The antipsychotics may be divided into two classes: classic or typical and atypical. The paliperidone, the major metabolite of risperidone, shares with the native drug the characteris...

Polyunsaturated fatty acids (PUFA), a lipid family comprised of omega-3 (n-3) and n-6 fatty acids, are a critical component of cellular membranes, and recent in vitro studies have found that antipsychotic medications up-regulate genes responsible for PUFA biosynthesis. To evaluate this effect in vivo, rats were treated with risperidone (1.5, 3, 6mg/kg/day), paliperidone (1.5, 3, 6mg/kg/day), ol...

BACKGROUND The purpose of this study was to compare incidence rates and time course of extrapyramidal symptom (EPS)-related treatment-emergent adverse events (TEAEs) between oral and long-acting injectable (LAI) paliperidone. METHODS The analysis included pooled data (safety analysis set, 2,256 antipsychotic-treated and 865 placebo-treated patients with schizophrenia) from seven randomized, d...

BACKGROUND Schizophrenia is a severe form of mental illness which is associated with significant and long-lasting health, social and financial burdens.The aim of this project is to assess the efficiency of the antipsychotics used in Spain in reducing schizophrenia relapses under the Spanish Health System perspective. MATERIAL AND METHODS A decision-analytic model was developed to explore the ...

A 34-year-old white man in whom schizophrenia was diagnosed at the age of 24 years was trialed over the course of illness on risperidone, olanzapine and aripiprazole. Although he responded well to these medications, he experienced relapses secondary to nonadherence. After discussing options to improve compliance and prevent relapse, he agreed to try longacting injectable paliperidone palmitate....

Absorption, metabolism, and excretion of paliperidone, an atypical antipsychotic, was studied in five healthy male subjects after a single dose of 1 mg of [(14)C]paliperidone oral solution ( approximately 16 microCi/subject). One week after dosing, 88.4 to 93.8% (mean 91.1%) of the administered radioactivity was excreted: 77.1 to 87.1% (mean 79.6%) in urine and 6.8 to 14.4% (mean 11.4%) in the ...

Identification of early clinical markers that predict later treatment outcomes in first-episode psychosis is highly valuable. The present study was conducted to determine the best time at which to predict the late treatment response in first-episode psychosis patients treated with paliperidone extended release (ER), the factors predicting early treatment responses (at Week 2 and Week 3) and the...

Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans. We examined whether two semimechanistic models could describe prolactin response in rats and subsequently be translated to predict pituitary dopamine D2 receptor occupancy and plasma prolactin concentrations in humans following administration of paliperidone or remoxipride....

BACKGROUND Paliperidone palmitate is a long-acting injectable atypical antipsychotic for the acute and maintenance treatment of adults with schizophrenia. The recommended initiation dosing regimen is 234 mg on Day 1 and 156 mg on Day 8 via intramuscular (deltoid) injection; followed by 39 to 234 mg once-monthly thereafter (deltoid or gluteal). These post-hoc analyses addressed two commonly enco...