Schizophrenia paliperidone

Increases in serum prolactin concentrations after the administration of risperidone have been attributed by some to its active metabolite, 9-hydroxyrisperidone (paliperidone). Serum prolactin concentrations after the administration of paliperidone extended-release and risperidone immediate-release tablets have therefore been compared in a double-bund, randomized, paraUel-group study in patients with schizophrenia [iso ll. On day 6, serum prolactin concentration-time profiles were similar with both treatments, with overaU higher serum prolactin concentrations than on day 1. 

Paliperidone, or 9-hydroxyrisperidone, is the major active metabolite of risperidone. It binds to both dopamine Dj and serotonin 5-HT2A receptors, and antagonism at these receptors is thought to account for its therapeutic activity in schizophrenia. It was approved by the US Food and Drug Administration in 2007 for acute and maintenance treatment of schizophrenia it is available in modified-release tablets. The available literature on the pharmacodynamics, pharmacokinetics, clinical efficacy, and tolerability of paliperidone has been extensively reviewed [101 ]. 

Placebo-controlled studies Paliperidone modified-release, quetiapine, and placebo have been compared in patients with recently exacerbated schizophrenia requiring hospitalization in a 6-week double-blind study [102 ]. In-patients were randomly assigned to paliperidone modified-release (n = 160), quetiapine (n = 159), or placebo (n = 80). A 2-week monotherapy phase was followed by a 4-week additive-therapy phase target doses were at the... 

Canuso CM, Dirks B, Carothers J, Kosik-Gonzalez C, Bossie CA, Zhu Y, Damaraju CV, Kalali AH, Mahmoud R. Randomized, double-blind, placebo-con-trolled study of paliperidone extended-release and quetiapine in inpatients with recently exacerbated schizophrenia. Am J Psychiatry 2009 166(6) 691-701. 

Tzimos A, Samokhvalov V, Kramer M, Ford L, Gassmann-Mayer C, Lim P, Eerdekens M. Safety and tolerability of oral paliperidone extended-release tablets in elderly patients with schizophrenia a double-blind, placebo-controlled study with six-month open-label extension. Am J Geriatr Psychiatry 2008 16(1) 31-43. 

Meltzer HY, Bobo WV, Nuamah IF, Lane R, Hough D, Kramer M, Eerdekens M. Efficacy and tolerability of oral paliperidone extended-release tablets in the treatment of acute schizophrenia pooled data from three 6-week, placebo-controlled studies. J Clin Psychiatry 2008 69(5) 817-29. 

Haematologic A case of recurrent neutropenia on a combination of paliperidone long-acting injection and oral risperidone in a 45-year-old male with schizophrenia, alcohol dependence and hepatitis C cirrhosis is reported [196 ]. It is postulated that as drug-induced neutropenia may be dose-related the combination and effectively the greater exposure to risperidone and paliperidone contributed to the development of the blood dyscrasia. 

Schreiner A, Niehaus D, Shuriquie NA, Aadamsoo K, Korcsog P, Salinas R, et al. Metabolic effects of paliperidone extended release versus oral olanzapine in patients with schizophrenia a prospective, randomized, controlled trial. J Clin Psychopharmacol 2012 32(4) 449-57. 

Alphs L, Bossie CA, Sliwa JK, Fu D-J, Ma Y-W, Hulihan J. Paliperidone pahnitate and risperidone long-acting injectable in subjects with schizophrenia recently treated with oral risperidone or other oral antipsychotics. Neuropsychiatr EHs Treat 2013 9 341-50. 

Kim SW, Chung YC, Lee YH, Lee JH, KimSY, BaeBCY, et al. Paliperidone ER versus risperidone for neurocognitive function in patients with schizophrenia a randomized, open-label, controlled trial. Int Qin Psychopharmacol 2012 27(5) 267-74. 

De Hert M, Yu W, Detraux J, Sweers K, van V ffnkel R, CorreU CU. Body weight and metaboUc adverse effects of asenapine, iloperidone, lurasidone and paliperidone in the treatment of schizophrenia and bipolar disorder a systematic review and exploratory meta-analysis. CNS Drugs 2012 26(9) 733-59. 

Kim EY, Chang SM, Shim JC, Joo EJ, Kim JJ, Kim YS, et al. Long-term effectiveness of flexibly dosed paliperidone extended-release comparison among patients with schizophrenia switching from risperidone and other antipsychotic agents. Curr Med Res Opin 2013 29(10) 1231-40. 

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