China
Africa
Explore chapters and articles related to this topic
Real-World Data and Real-World Evidence
Published in Wei Zhang, Fangrong Yan, Feng Chen, Shein-Chung Chow, Advanced Statistics in Regulatory Critical Clinical Initiatives, 2022
Explanatory trials among relatively homogenous study populations under well-defined and highly controlled conditions demonstrated that treatments for schizophrenia with once-monthly paliperidone palmitate (PP) significantly delayed treatment failure, compared with daily oral antipsychotic (OA)80. However, explanatory trials typically exclude complicated patients, such as those with comorbid substance abuse and suboptimal disease management, who may be of particular interest to population health decision-makers as well as clinicians because these patients are more likely to be high resource utilizers. Another question of interest is whether the effectiveness of long-acting injectable (LAI) antipsychotic therapies is better than daily oral antipsychotic (OA) for treating schizophrenia in actual practice.
Drug Nanocrystals
Published in Carla Vitorino, Andreia Jorge, Alberto Pais, Nanoparticles for Brain Drug Delivery, 2021
M. Ermelinda S. Eusébio, Ricardo A. E. Castro, Joäo Canotilho
Some nanocrystal-based products for poorly water-soluble drugs have been formulated for parenteral administration [162] (Table 7.1). Invega Sustenna® was the first injectable nanocrystal product, approved by FDA, brought to market, an aqueous nanosuspension of the antipsychotic paliperidone palmitate (Fig. 7.5d) which allows delivery of the drug in small volume via intramuscular injection. The parent drug, paliperidone, does not have solubility issues: the use of a nanosuspension of the drug palmitate enables limiting its solubility such that sustained release of the drug is achieved, allowing once-monthly administration, with improved patient compliance [163, 164]. The optimum particle size of nanosuspension products may depend on the intended propose, and for extended release of paliperidone Leng et al. [165] showed that nanosuspensions of paliperidone palmitate with sizes about 1000 nm have improved pharmacokinetic parameters when compared to a 500 nm batch.
P
Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Paliperidone is the active metabolite of risperidone. Four metabolic pathways have been identified in vivo, none of which accounted for more than 6.5% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Following administration of [14C]-paliperidone, 59% of the dose was excreted unchanged into urine, indicating that paliperidone is not extensively metabolised in the liver. Approximately 80% of the administered radioactivity was recovered in urine and 11% in the faeces.
The preclinical discovery and development of paliperidone for the treatment of schizophrenia
Published in Expert Opinion on Drug Discovery, 2020
Anna Wesołowska, Magdalena Jastrzębska-Więsek, Agnieszka Cios, Anna Partyka
Paliperidone is an antipsychotic medicine that received approval from the American and European agencies for the short- and long-term treatment of schizophrenia in adults. A little later, the indications were extended to the acute treatment of schizoaffective disorder either as monotherapy or adjunctive therapy to mood stabilizers and/or antidepressants, as well as to treat schizophrenia in adolescents 12–17 years of age in US or older than 15 years in Europe. Paliperidone is formulated as ER tablets based on an osmotic-controlled release oral push-pull delivery system or as paliperidone palmitate racemic suspension which utilizes nanoparticle technology. It is available in the market as 1-month or 3-month injections (so-called LAI) for maintenance treatment of schizophrenia in adults. The recommended dose of paliperidone in ER tablets for the treatment of schizophrenia or schizoaffective disorder in adults is 6 mg once daily, administered in the morning, consistently in relation to food to decrease any potential variability in exposure. In adolescents, the recommended starting dose is 3 mg per day. Initial dose titration is not required and variability in the plasma levels of paliperidone, as a result of smoking status, is not expected. But the LAI forms of paliperidone are prepared and injected intramuscularly into either the deltoid or the gluteal muscle. An active compound, i.e. paliperidone is released as a result of the action of muscle esterases during the 1-month or 3-month period depending on the LAI form.
The prescribing pattern of paliperidone in a pediatric population
Published in Psychiatry and Clinical Psychopharmacology, 2018
Çiğdem Yektaş, Başak Paşabeyoğlu, Caner Mutlu, Ayten Erdoğan
Our results reflect the particular use of paliperidone in the present study population. In line with the published data, the results of this study show that paliperidone are generally used in those with psychotic disorders. These findings also underline the widespread off-label use of paliperidone in the treatment of other psychiatric disorders. However, the role for these medications in non-psychotics mental disorders still remains unclear since there is no specific indication, but also because of the documented increased risk of various side effects of paliperidone. This study also highlights the important differences existing among guidelines’ recommendations and physicians’ paliperidone prescribing behaviour for psychiatric patients.
A systematic review and combined analysis of therapeutic drug monitoring studies for oral paliperidone
Published in Expert Review of Clinical Pharmacology, 2018
Georgios Schoretsanitis, Edoardo Spina, Christoph Hiemke, Jose de Leon
The pharmacodynamic effects of paliperidone are mainly explained by the blocking of neurotransmitter receptors in the brain and/or periphery. Box 1 [5–8] provides in vitro neurotransmitter receptor affinities for paliperidone and risperidone but does not take into account the effects of the blood–brain barrier (BBB) (See Section 1.3.4.). Supplemental Box S1 describes paliperidone’s pharmacodynamic effects at the cardiac potassium channels [9–24].