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.
Emerging Topics
Published in Demissie Alemayehu, Birol Emir, Michael Gaffney, Interface between Regulation and Statistics in Drug Development, 2020
Demissie Alemayehu, Birol Emir, Michael Gaffney
An example of label expansion using a pragmatic study concerns paliperidone palmitate, originally indicated for the treatment of schizophrenia in adults and treatment of schizoaffective disorder in adults as monotherapy and as an adjunct to mood stabilizers or antidepressants (Alphs et al. 2016).
A post hoc analysis on hospitalization risk in Asian patients with schizophrenia switching to once-monthly paliperidone palmitate from oral antipsychotics
Published in Expert Opinion on Pharmacotherapy, 2019
Nan Li, Jian Min Zhuo, Ibrahim Turkoz, Maju Mathews, Yu Feng, Wilson Tan
Once-monthly paliperidone palmitate (PP1M), an atypical LAI antipsychotic, has been proven to be effective and safe for acute and maintenance treatment of schizophrenia [12–14]. Several global clinical studies have established that PP1M delayed time to relapse in patients with schizophrenia [15–18]. In the PROSIPAL and PRIDE studies, PP1M was superior to oral antipsychotics in reducing the risk of relapse and treatment failure along with psychiatric hospitalization, respectively [19,20]. In a recent real-world evidence study with 29,823 patients, the risk of rehospitalization due to psychiatric relapse was reduced by up to 30% with LAI treatments in comparison to other equivalent oral formulations (hazard ratio [HR]: 0.78; 95% CI, 0.72–0.84). Furthermore, the risk of psychiatric rehospitalization was the lowest with PP1M treatment (HR: 0.51; 95% CI, 0.41–0.64) in that analysis [21]. Additional real-world systematic review using data generated from pragmatic-randomized clinical trials and observational studies suggested that treatment with PP1M was superior to oral antipsychotics in delaying the time to relapse or treatment [22].
Rats and rabbits as pharmacokinetic screening tools for long acting intramuscular depots: case study with paliperidone palmitate suspension
Published in Xenobiotica, 2019
Harilal Patel, Prakash Patel, Nirav Modi, Pinakin Patel, Yogesh Wagh, Alex George, Nirmal Desai, Nuggehally R. Srinivas
This study involved New Zealand white rabbits (n = 4; body weight: 3.38–4 kg) aged between 3–4 months and the entire pharmacokinetic profile comprising several sampling time points were collected from individual rabbits (Figure 2). The rabbits employed were provided food and free access of water during experimental period. A ready to use formulation of paliperidone palmitate was injected via intramuscular route to rabbits (4.5 mg/kg equivalent to paliperidone) in the thigh muscles of the hind limbs. The injection volume was 0.158–0.177 mL for rabbits with a needle gauge corresponding to 26. The pharmacokinetic blood sampling was via marginal ear vein and approximately 0.5 mL blood/time point was collected and mixed with 20 IU/mL of sodium heparin which served as anti-coagulant. The blood collection time points were performed at pre dose (0.0), 1, 2, 3, 4, 6, 8, 24, 48, 72 h (3 days), 120 (5 days), 168 (7 days), 240, 336 (14 days), 504 (21 days), 672 (28 days) and post-dose administration, respectively. The blood samples were placed on an ice bath, followed by centrifugation at 4000 rpm for 15 min (approximately 10 °C) and the plasma was separated and stored frozen at −70 °C until analysis.
TDM in psychiatry and neurology: A comprehensive summary of the consensus guidelines for therapeutic drug monitoring in neuropsychopharmacology, update 2017; a tool for clinicians*
Published in The World Journal of Biological Psychiatry, 2018
Georgios Schoretsanitis, Michael Paulzen, Stefan Unterecker, Markus Schwarz, Andreas Conca, Gerald Zernig, Gerhard Gründer, Ekkerhard Haen, Pierre Baumann, Niels Bergemann, Hans Willi Clement, Katharina Domschke, Gabriel Eckermann, Karin Egberts, Manfred Gerlach, Christine Greiner, Ursula Havemann-Reinecke, Gudrun Hefner, Renate Helmer, Ger Janssen, Eveline Jaquenoud-Sirot, Gerd Laux, Thomas Messer, Rainald Mössner, Matthias J. Müller, Bruno Pfuhlmann, Peter Riederer, Alois Saria, Bernd Schoppek, Margarete Silva Gracia, Benedikt Stegmann, Werner Steimer, Julia C. Stingl, Manfred Uhr, Sven Ulrich, Roland Waschgler, Gabriela Zurek, Christoph Hiemke
Depot formulations of antipsychotic drugs follow different pharmacokinetic patterns than oral forms; in patients receiving long-acting injectables (LAI), blood should be sampled immediately before the next injection. Maximum plasma concentration of first-generation depot antipsychotics, as well as paliperidone palmitate, are reached within 1–14 days after injection, and the apparent elimination half-life is about 2–3 weeks (Taylor 2009; Spanarello and La Ferla 2014). Note that the new 3-month depot formulation of paliperidone palmitate is expected to follow different pharmacokinetics; however, until sufficient data are available, no conclusions can be made. For risperidone LAI the mean time to peak concentrations is 4 weeks, and its plasma half-life is 4–6 days (Taylor 2009). Maximal drug concentrations for aripiprazole LAI are reached 5-7 days after injection; the mean apparent terminal elimination half-life after 400 or 300 mg aripiprazole monthly is 47 and 30 days, respectively (Mallikaarjun et al. 2013; Fleischhacker et al. 2014).