Paliperidone Extended-Release: Safety and Tolerability from a Metabolic Profile Perspective
- 274 Downloads
Pharmacologic management strategies for schizophrenia, a relatively common psychotic disorder, include the use of typical and atypical antipsychotic drugs. In general, typical (or conventional) antipsychotics have a proven track record in effectively managing the positive symptoms of schizophrenia but sometimes lack efficacy in treating negative symptoms. The conventional agents are also associated with adverse neurologic effects such as extrapyramidal symptoms (EPS). The development of atypical antipsychotics has partly ameliorated the issue of EPS induced by typical antipsychotics. However, several of these atypical antipsychotic agents have been associated with adverse metabolic effects, including weight gain, dyslipidemia, and increased serum glucose levels. Paliperidone (9-hydroxy-riperidone) extended-release (ER) is an atypical antipsychotic indicated for the treatment of schizophrenia which utilizes a patented oral osmotic system technology that provides constant drug delivery over the course of the day. The efficacy and safety of paliperidone ER in patients with schizophrenia have been established. This review focuses on the metabolic safety of paliperidone ER in patients with schizophrenia. Clinical trials have demonstrated a lack of significant change in lipid profiles with paliperidone ER; furthermore, reported incidences of glucose-related adverse events in clinical trials were very low and similar to those seen with placebo. While dose-related increases in bodyweight of 1–2 kg have been observed with paliperidone ER, there are few reports of clinically relevant increases in bodyweight during treatment. Placebo-controlled trials indicate that the risk of developing metabolic disorders with paliperidone ER is low and similar to that seen with placebo. Furthermore, the ER formulation of paliperidone may offer potential advantages over atypical antipsychotics such as risperidone, particularly with regard to side effects and compliance, but comparative studies are needed.
The authors would like to thank Stephanie Blick and Simone Boniface of inScience Communications, Springer Healthcare, for medical writing assistance in the preparation of this manuscript. This assistance was funded by Janssen-Cilag, Spain. Carlos Quilo is an employee of Janssen Cilag, Spain. Alfonso Rodríguez Martínez declares no conflicts of interest pertaining to this manuscript.
- 28.Schooler NR, Gharabawi G, Bossie C, et al. A “virtual” comparison of paliperidone ER and oral risperidone in patients with schizophrenia [abstract]. 45th Annual Meeting of the American College of Neuropharmacology. 2006 Dec 3–7, Hollywood, p. S241–42.Google Scholar
- 30.Buckley PF. Update on the treatment and management of schizophrenia and bipolar disorder. CNS Spectr. 2008;13(2 Suppl 1):1–10 (quiz 1–2).Google Scholar
- 37.Ortho-McNeil-Janssen Pharmaceuticals, Inc. Invega™ (paliperidone) extended-release tablets: US prescribing information [online]. Available from http://invega.com/assets/prescribing-information.pdf. Accessed 24 May 2011.
- 38.European Medicines Agency. Invega™ (paliperidone): summary of product characteristics. 2006. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000746/WC500034925.pdf. Accessed 21 Oct 2013.
- 40.Tzimos A, Samokhvalov V, Kramer M, et al. 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.PubMedCrossRefGoogle Scholar
- 41.Schreiner A, Tessier C, Hoeben D, et al. A prospective randomized controlled trial of paliperidone ER versus oral olanzapine in patients with schizophrenia. 15th Winter Workshop in Psychoses (WWP); 2009 Nov 15–18; Barcelona.Google Scholar
- 44.European Medicines Agency. Risperdal (risperidone): summary of product characteristics. 2011. http://www.medicines.org.uk/EMC/medicine/12818/SPC/Risperdal+Tablets,+Liquid+%26+Quicklet/. Accessed 24 Oct 2013.