Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0036341 (schizophrenia)
 60,220 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Paliperidone prolonged release (PR) is a new product licensed for the treatment of schizophrenia. It is the active metabolite of risperidone, a drug that has been successfully used in the treatment of schizophrenia and mood disorder. Paliperidone PR has a unique pharmacological delivery mechanism that may incur benefits for particular patients diagnosed with schizophrenia. Studies investigating paliperidone PR are reviewed along with implications for its use by nurse prescribers and those nurses who monitor the use of medication for people with psychosis.
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PMID:What are the nursing implications when using paliperidone prolonged release for people with schizophrenia. 1901 70

Paliperidone extended-release tablet (paliperidone ER; INVEGA()) is an oral antipsychotic for the treatment of schizophrenia. The recommended dose range is 3-12 mg per day. Paliperidone ER utilizes the OROS((R)) delivery system, which allows for once-daily dosing. Its pharmacokinetic profile results in a more stable serum concentration. Paliperidone is 9-hydroxyrisperidone, the chief active metabolite of risperidone. It undergoes limited hepatic metabolism, thereby minimizing the risks of hepatic drug-drug and drug-disease interactions. Three 6-week trials in patients with acute schizophrenia reported that paliperidone ER was effective, well tolerated, and produced clinically meaningful improvements in personal and social functioning compared with placebo. Post-hoc analysis of these trials in various populations, including recently diagnosed, elderly and more severely ill patients, those with sleep disturbances and those with predominant negative symptoms demonstrated improvement as well. Paliperidone ER was also significantly better than placebo in the prevention of symptom recurrence in a 6-month maintenance study. The most common clinically relevant adverse events associated with paliperidone ER were extrapyramidal symptoms, tachycardia and somnolence. The incidence of Parkinsonism, akathisia and use of anticholinergic medications increased in a dose-related manner. Further, modest QTc interval prolongation was observed but did not produce clinical symptoms. Similar to risperidone, paliperidone ER is associated with increases in serum prolactin levels. Overall, paliperidone ER was effective, well tolerated and provides a new treatment option for patients with schizophrenia.
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PMID:Paliperidone ER: a review of the clinical trial data. 1930 Jun 22

It is proposed that to achieve a therapeutic effect in schizophrenia patients, dopamine D(2)-receptor occupancy by antipsychotics within the striatum must exceed 60-65%. However, at high levels of D(2)-receptor occupancy, the risk of extrapyramidal symptoms (EPS) is increased. Following oral dosing of antipsychotics, peaks and troughs in plasma drug concentrations may be mirrored by fluctuations in D(2)-receptor occupancy. Paliperidone, a novel antipsychotic available as extended-release tablets (paliperidone ER), is the major active metabolite of risperidone and exhibits a plasma pharmacokinetic profile with reduced peak-trough fluctuations and consistent D(2)-receptor occupancy compared with conventional oral antipsychotic formulations. Using formulations that resemble those in clinical practice, this study provides a preclinical evaluation of the pharmacological properties of paliperidone ER and risperidone immediate-release formulation in terms of consistent antipsychotic efficacy over time and extrapyramidal symptom liability. Significant fluctuations in inhibition of d-amphetamine-induced hyperlocomotion were observed for repeated subcutaneous (SC) risperidone injections, whereas stable inhibitory efficacy was demonstrated during continuous SC paliperidone infusion. Similarly, significant fluctuations in latency on-bar were observed with repeated SC risperidone injections, whereas significantly lower latency on-bar was demonstrated following continuous SC paliperidone infusion. These results in an animal model suggest that although risperidone and paliperidone demonstrate similar pharmacologic effects, continuous administration of paliperidone achieves more stable antipsychotic efficacy with reduced motor impairment, akin to the effects observed with paliperidone ER in clinical studies.
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PMID:A comparison of continuous subcutaneous paliperidone infusion and repeated subcutaneous injection of risperidone free-base in rats. 1964 Jun 86

Paliperidone extended-release tablet (paliperidone ER) is a centrally active dopamine D(2)- and serotonergic 5-HT(2A)-receptor antagonist that is registered for the treatment of schizophrenia. The controlled rate of release of paliperidone from the ER formulation is designed to have a slower absorption rate, which results in gradual ascending plasma concentrations with observed maximum plasma concentrations occurring at 24 hours after dosing on the first dosing day. On subsequent treatment days, the ER formulation provides minimal fluctuations in plasma concentrations. Paliperidone is eliminated with a terminal half-life of approximately 24 hours. Steady state is achieved after 4 daily doses. Paliperidone ER exhibits time-invariant pharmacokinetics. It shows a 3.5-fold accumulation upon steady state, mainly caused by the controlled release characteristics of the formulation. Paliperidone ER displays dose proportionality over the dose range of 3 to 15 mg; the 90% confidence intervals of the pairwise dose comparisons are all included in the 80% to 125% bioequivalence limits.
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PMID:Single- and multiple-dose pharmacokinetics and dose proportionality of the psychotropic agent paliperidone extended release. 1971 55

Transcranial magnetic stimulation is a neurophysiological method which enables direct quantitative in vivo assessment of cortical excitability and inhibition. The aim of the study was to assess the impact of paliperidone on the motor threshold and cortical silent period, in a drug-naive patient, with first episode schizophrenia using this technique. Paliperidone monotherapy caused a significant reduction of severity of schizophrenic symptomatology in the patient. At the same time, a significant prolongation of the cortical silent period, from 118.68 ms before to 185.13 ms after therapy, occurred. Because the cortical silent period is a function of GABA(B) receptors, we can assume that paliperidone may have the ability to enhance GABA(B) receptor-mediated neurotransmission.
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PMID:Paliperidon mediated modification of cortical inhibition. 1985 66

The time course of Positive and Negative Syndrome Scale (PANSS) scores in adult schizophrenia patients was modeled, and the effectiveness of paliperidone extended-release tablets (paliperidone ER) and olanzapine was quantified. Data from 3 randomized, double-blind phase III studies were used. Patients received paliperidone ER (3, 6, 9, 12, or 15 mg), olanzapine 10 mg, or matched placebo once daily for 6 consecutive weeks. An indirect response model implemented using a nonlinear mixed effects approach described the time course of the PANSS. Deterioration rate was modeled as a function of baseline PANSS score, placebo, and drug effects, and the dropout effect. An exponential decrease of the placebo response was also implemented. Paliperidone ER and olanzapine treatment were characterized by a long-lasting drug effect (13%), with a larger but short-lasting placebo effect (40%) and a notable dropout rate. The covariate exploration failed to identify any clinically relevant factors. The nonparametric bootstrap analysis confirmed the acceptable precision of parameter estimates. The visual predictive check supported the model's adequacy to reproduce observed PANSS time courses. The population model describes the time course of PANSS scores in schizophrenia patients and is appropriate for use in clinical trial simulation activities.
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PMID:Modeling the effectiveness of paliperidone ER and olanzapine in schizophrenia: meta-analysis of 3 randomized, controlled clinical trials. 2005 4

The purpose of the study is to investigate the action of one antipsychotic molecule of recent introduction on the market. Paliperidone, in this occasion used in the formulation extended-release tablets, is an oral antipsychotic who takes advantage of the OROS system. Studies about are up to now focused on the effectiveness of paliperidone ER in the acute phase of the schizophrenia. In our job we have, instead, intention to show one possible application in a case of a chronic patient with undifferentiated schizophrenia resistant to the other antipsychotic treatments. Moreover 3TRE scale has been associated to establish the effects of the new therapy. The entrance prescription has been with paliperidone ER in a dosage of 6mg once a day. Clinical effects of paliperidone ER 6 mg became obvious and meaningful, online with other jobs, already in the first days of treatment. But the improvement of the partials and totals scale's scores have been had mainly with the dosage to 12 mg, that the patient has assumed autonomously unknown to the care provider.
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PMID:[Treatment with paliperidone extended-release tablets in a case of resistant undifferentiated schizophrenia: clinical improvement with 12 mg and evaluation through 3TRE scale]. 2006 99

Intramuscular paliperidone palmitate is a long-acting, atypical antipsychotic that is indicated in the US for the acute and maintenance therapy of adult patients with schizophrenia. Paliperidone is the major active metabolite of risperidone. The noninferiority of flexible doses of intramuscular paliperidone palmitate 39-156 mg to flexible doses of intramuscular long-acting risperidone 25-50 mg was not established in an initial 53-week study. However, these data were utilized to optimize the intramuscular paliperidone palmitate dosage regimen. In four randomized, double-blind studies, intramuscular paliperidone palmitate 39-234 mg was generally effective in the treatment of adult patients with acute schizophrenia, inducing significantly greater improvements from baseline in the mean Positive and Negative Syndrome Scale (PANSS) total score than placebo (primary endpoint). In general, intramuscular paliperidone palmitate recipients achieved significantly better outcomes than placebo recipients with regard to the PANSS subscale, PANSS factor, Personal and Social Performance scale and Clinical Global Impressions-Severity scale scores. As maintenance therapy, intramuscular paliperidone palmitate 39-156 mg was significantly more effective than placebo in delaying the time to the first relapse of schizophrenia symptoms in adult patients, according to the results of a randomized, double-blind study. The beneficial effects of intramuscular paliperidone palmitate therapy on the PANSS total score were sustained in a 52-week noncomparative extension phase of the maintenance therapy study. Intramuscular paliperidone palmitate 39-234 mg was generally well tolerated in adult patients with schizophrenia.
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PMID:Intramuscular paliperidone palmitate. 2015 97

The Medication Satisfaction Questionnaire (MSQ) is a single-item questionnaire which evaluates satisfaction with antipsychotic medication in schizophrenia patients. This study evaluated the reliability and validity for its use in research and clinical settings. Data pooled across treatment groups (control vs. Paliperidone ER) from a randomized 6-week study were used to conduct four psychometric assessments of the MSQ: (1) test-retest reliability, (2) convergent validity, (3) known-groups validity, and (4) minimally important difference (MID). This analysis included 191 randomized subjects. Test-retest reliability was evaluated for patients with no change in satisfaction from weeks 2 to 4 and weeks 4 to 6 (ICC=0.80; 0.83, respectively). Convergent validity was demonstrated through large correlations with Treatment Satisfaction Questionnaire for Medication (TSQM) global score (r=0.72-0.77), and through small correlations with variables measuring clinical symptoms and functioning (e.g., Positive and Negative Syndrome Scale (PANSS) total score [r=-0.30 to -0.17], CGI-S [r=-0.35 to -0.27], SF-36 Physical Functioning Score [r=0.18] and side effects and extrapiramidal measures (including UKU, ESRS-A, SAS). Mean MSQ scores were significantly different between those who completed and discontinued the study, and between different satisfaction groups based on TSQM, demonstrating good known-groups validity. MID estimates for the MSQ ranged from 0.47 (standard error of measurement) to 0.58 (anchor-based method). Results suggest that the MSQ has acceptable reliability and validity, making this single-item questionnaire appropriate and easy to use in clinical research and potentially in clinical practice. A 1-point change on the MSQ may be considered clinically meaningful.
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PMID:Psychometric evaluation of the Medication Satisfaction Questionnaire (MSQ) to assess satisfaction with antipsychotic medication among schizophrenia patients. 2017 95

Paliperidone, the active metabolite of risperidone is a relatively recent introduction for the treatment of schizophrenia. There is paucity of data regarding the use of paliperidone in elderly patients. We have attempted to highlight the prominent aspects of the use of paliperidone in the geriatric population. The limited data indicate that paliperidone may be effective and safe in the treatment of schizophrenia in the elderly.
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PMID:Paliperidone use in the elderly. 2040 62


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