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Paliperidone ER: a review of the clinical trial data

By Philip G Janicak and Elizabeth A Winans

Abstract

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® 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

Topics: Expert Opinion
Publisher: Dove Medical Press
OAI identifier: oai:pubmedcentral.nih.gov:2656329
Provided by: PubMed Central
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    Citations

    1. (1976). 290.Neuropsychiatric Disease and Treatment 2007:3(6) 883 Paliperidone ER: clinical trial data Guy W.
    2. (2007). A double-blind, placebo-controlled, randomized study evaluating the effect of paliperidone extended release tablets on sleep architecture in patients with schizophrenia. Int Clin Psychopharm,
    3. (2006). A virtual comparison of paliperidone ER and oral risperidone in patients with schizophrenia.
    4. (2006). Absence of pharmacokinetic interaction between trimethoprim and paliperidone extended-release tablets in healthy subjects.
    5. (2005). Absorption, metabolism and excretion of a single oral dose of 14C-paliperidone 1 mg in healthy subjects. Eur Neuropsychopharmacol,
    6. (2006). Clinical spectrum of the osmoticcontrolled release oral delivery system (OROS®), an advanced oral delivery form. Curr Med Res Opin,
    7. (2006). Delaying symptom recurrence in patients with schizophrenia with paliperidone extended-release tablet: an international, randomized, double-blind, placebo-controlled study. Presented at the Collegium Internationale Neuro-Psychopharmacologicum,
    8. (2000). Development, reliability and acceptability of a new version of the DSM-IV Social and Occupational Functioning Assessment Scale (SOFAS) to assess routine social functioning. Acta Psychiatr Scand,
    9. (2006). Direct and indirect effects of paliperidone extended-release tablets on negative symptoms of schizophrenia.
    10. (2006). Effects of hepatic impairment on the pharmacokinetics of paliperidone immediate-release. Presented at the 46th New Clinical Drug Evaluation Unit Annual Meeting,
    11. (2007). Effects of paliperidone ER in patients with schizophrenia previously treated with olanzapine.
    12. (2007). Effects of paliperidone ER in patients with schizophrenia previously treated with risperidone.
    13. (2007). Effects of renal impairment on the pharmacokinetic profi le of paliperidone extended-release tablets. Clin Pharm Ther, 81(Suppl 1):S63.
    14. (2007). Effi cacy and safety of paliperidone extended-release tablets: results of a 6-week, randomized, placebo-controlled study. Biol Psychiatry,
    15. (2007). Effi cacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: Pooled data from three 52-week, open-label extension studies.
    16. (2006). Effi cacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia: pooled data from three 6-week placebo controlled studies.
    17. (2006). Effi cacy of paliperidone extended-release tablets in patients with schizophrenia and predominant negative symptoms.
    18. (2007). Effi cacy, safety and effect on functioning of paliperidone extended-release tablets in the treatment of acute schizophrenia: an international 6-week placebo-controlled study. Schizophrenia Res,
    19. (2007). Evaluation of the pharmacokinetics of an extended-release formulation of paliperidone with an immediate-release formulation of risperidone. Clin Pharm Ther, 81(Suppl 1):S62.
    20. (2006). Extended-release formulation of paliperidone shows dose proportional pharmacokinetics.
    21. (2006). Medical comorbidity in women and men with schizophrenia.
    22. (2006). Metabolic outcomes in patients with schizophrenia treated with oral paliperidone extended-release tablets: pooled analysis of three 6-week placebo-controlled studies.
    23. (2007). Metabolic outcomes, in terms of weight, glucose and lipid profi les, in patients with schizophrenia treated with paliperidone extended-release tablets for 52 weeks. Presented at the American Psychiatric Association Annual Meeting,
    24. (2006). Paliperidone extended-release in severely ill patients with schizophrenia. Presented at the Institute on Psychiatric Services,
    25. (2007). Paliperidone extended-release tablets for prevention of symptom recurrence in patients with schizophrenia: a randomized, double-blind, placebo-controlled study.
    26. (2006). Paliperidone extended-release tablets in patients recently diagnosed with schizophrenia.
    27. (2006). Paliperidone extended-release tablets in patients recently diagnosed with schizophrenia. Presented at Collegium Internationale Neuro-Psychopharmacologicum,
    28. (2006). Predominant role of the 9-hydroxy metabolite of risperidone in Chinese female patients with schizophrenia. Acta Pharmacol Sin,
    29. (2005). Predominant role of the 9-hydroxy metabolite of risperidone in elevating blood prolactin levels.
    30. (2007). Prescribing information for paliperidone extended-release [online]. Accessed
    31. Presented at the 45th Annual Meeting of the American College of Neuropharmacology,
    32. Presented at the American Association of Pharmaceutical Sciences Annual Meeting and Exposition,
    33. (2006). Prolactin elevation of the antipsychotic risperidone is predominantly related to its 9-hydroxy metabolite. Hum Psychopharmacol,
    34. (2006). Reliability, validity and sensitivity to change of the personal and social performance scale in patients with acute schizophrenia.
    35. (2007). Safety and tolerability of oral paliperidone extended-release tablets in elderly patients with schizophrenia: A double-blind, placebo-controlled study with long-term open-label extension. Am J Geriatric Psych,
    36. (1997). The effects of risperidone on the fi ve dimensions of schizophrenia derived by factor analysis: combined results of the North American trials.
    37. (2005). The rise and rise of drug delivery. Nat Rev Drug Discov,
    38. (2007). Treatment of schizophrenia with paliperidone extended-release tablets: A 6-week placebo-controlled trial. Schizophrenia Res,

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