ILOPERIDONE: NEWER ATYPICAL ANTIPSYCHOTIC FOR SCHIZOPHRENIA
The optimal treatment of schizophrenia poses a challenge to develop more effective treatments and safer drugs, to overcome poor compliance, discontinuation and frequent switching with available antipsychotics. Many antipsychotic medications are currently approved by FDA for the treatment of schizophrenia, but response to these agents remains highly variable. Iloperidone is a new dopamine type 2/serotonin type 2A (D2/5-HT2A) antagonist structurally related to risperidone, expected to give better efficacy with less extrapyramidal symptoms than D2 receptor antagonist antipsychotics. Iloperidone is more efficacious in terms of cognitive functions, less problematic regarding weight gain and metabolic disturbances.
Keywords: iloperidone, pharmacology, pharmacokinetics, efficacy, safety
2. Tonin FS, Wiens A, Llimos FF, Pontarolo R. Iloperidone in the treatment of schizophrenia- an evidence based review of its place in therapy. Core Evid 2016; 11:49-61.
3. Cutler AJ, Kalali AH, Mattingly GW, Kunovac J, Meng X. Long term safety and tolerability of iloperidone: results from a 25week, open label extension trial. CNS Spectr. 2013Í¾18(1):43â€“54.
4. Albers LJ, Musenga A, Raggi MA. Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? Expert Opin Investig Drugs 2008; 17:61-75.
5. Kongsamut S, Roehr JE, Cai J, et al. Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol 1996; 317:417â€“23.
6. Kalkman HO, Subramanian N, Hoyer D. Extended radioligand binding profile of iloperidone: A broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. Neuropsycho pharmacology 2001; 25:904â€“14.
7. Richelson E, Souder T. Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compounds. Life Sci. 2000; 68:29-39.
8. Kalkman HO, Feuerbach D, Lotscher E, Schoeffter P. Functional characterization of the novel antipsychotic iloperidone at human D2, D3, alpha2C,5-HT6 , and 5-HT1A receptors. Life Sci. 2003; 73:1151â€“59.
9. CacciaS, Pasina L, Nobili A. New atypical antipsychotics for schizophrenia: Iloperidone. Drug Des Devel Ther. 2010:4:33-48.
10. Subramaian N, Kalkman HO. Receptor profile of P88-8991 and P95-12113, metabolites of the novel antipsychotic iloperidone. Prog Neuropsycho pharmacol Biol Psychiatry. 2002;26 :553-60.
11. Jain KK. An assessment of iloperidone for the treatment of schizophrenia. Expert Opin Investig Drugs. 2000; 9(12):2935â€“43.
12. Sainati SM, Hubbard JW, Chi E, Grasing K, Brecher MB. Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol. 1995; 35:713â€“20.
13. Potkin SG, Litman RE, Torres R et al. Efficacy of iloperidone in the treatment of schizophrenia: initial phase 3 studies. J Clin Psycho pharmacol. 2008; 28(suppl 1):S4-11.
14. Cutler AJ, Kalali AH, Weiden PJ et al. Four week, double-blind, placebo and ziprasidone controlled trial of iloperidone in patients with acute exacerbations of schizophrenia. J Clin Psycho pharmacol 2008; 28(suppl1):S20-8.
15. Weiden PJ, Cutler AJ, Polymeropoulos MH et al. Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivitol trials. J Clin Psycho pharmacol 2008; 28(suppl 1):S12- 9.
16. Kane JM, Lauriello J, Laska E et al. Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia. J Clin Psychopharmacol 2008; 28(suppl 1):S29-35.
17. Dutta A, Baruna S, Dan A, Chakraborty K, Mandal M. Iloperidone-induced galactorrhea in middle aged female. Indian J Psychol Med.2012; 34(4):396-98.
18. Dargani NV, Malhotra AK. Safety profile of iloperidone in the treatment of schizophrenia. Expert Opin Drug Saf 2014; 13(2):241-46.
19. Citrome L, Weiden PJ, Alva G, Glick ID, Jackson R, Mattingly G, Kianifard F et al. Switching to iloperidone: An omnibus of clinically relevant observations from a 12week, open label, randomized clinical trial in 500 persons with schizophrenia. Clin Schizo phr Relat Psychoses 2015; 8(4):183-95.
20. Weiden PJ, Manning R, Wolfgang CD, Ryan JM, MancioneL, HanG, Ahmed S, Mayo MG. Randomized trial of iloperidone for prevention of relapse in Schizophrenia: The REPRIEVE study.CNS Drugs 2016;30(8):735-47.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).