Aripiprazole is the new generation class of antipsychotic. Chemically, aripiprazole is a quinolinone derivative. Aripiprazole gives its action through the partial agonist mechanism at dopamine D2 and 5- HT1A receptors, and is also an antagonist at 5-HT2A receptors. Preclinical and placebo controlled trials of aripiprazole have evaluated 2A that aripiprazole is effective in the treatment of schizophrenia. Comparative trials of aripiprazole with typical and atypical antipsychotics have shown that aripiprazole has similar efficacy as haloperidol and olanzapine. Data also suggest that aripiprazole is safe and its tolerability profile is good. This molecule is also showing promising results in the treatment of bipolar disorders but the evidence is still inadequate. This article critically examines the various clinical trials conducted in various countries regarding the therapeutic profile of aripiprazole.
Millan MJ. Improving the treatment of schizophrenia: focus on serotonin (5Ht)(1A) receptors. J Phartmacol Exp Ther 2000; 295: 853-61.
Burris KD, Molski TF, Xu C, Ryan E, Tottori K, Kikuchi T, Yocca FD, Molinoff PB. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther 2002; 302:381-9
Jordan S, et al. the antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor. Eur J Pharmacol 2002; 441: 137-40.
Lawler CP, Prioleau C, Lewis MM, et al. Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology 1999; 20: 612-27.
Kikuchi T, Tottori K, Uwahodo Y, et al. OPC-14597, a new putative antipsychotic drugwith both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity. J Pharmacol Ther 1995; 274. 329-36.
Stahl SM. Dopamine system stabi l izers, aripiprazole, and the next generation of antipsychotics, part 1, “Goldilocks” actions at dopamine receptors. J Clin Psychiatry 2001; 62: 8241-42.
Kane JM, Meltzer HY, Carson WH Jr, McQuade RD, Marcus RN, Sanchez R; Aripiprazole Study Group. Aripiprazole for treatment-resistant schizophrenia: results of a multicenter, randomized, double-blind, comparison study versus perphenazine. J Clin Psychiatry. 2007; 68: 1812-3.
Mallikaarjum S, Salazar DE, Bramer SL. Pharmacokinetics, tolerability, and safety of aripiprazole following multiple oral dosing in normal healthy volunteers. J Clin Pharmacol 2004; 44: 179-87.
Swainston HT, Perry CM. Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs 2004, 64: 1715-1736
Deleon A, Patel NC, Crismon ML. Aripiprazole: a comparative review of its pharmacology, clinical efficacy, and tolerability. Clin Ther 2004;26:649-66.
Tamminga CA. Partial Dopamine agonist in the treatment of psychosis. J Neural Transm 2002; 109: 411-20.
Kane JM, Carson WH, Saha AR, McQuade RD, Ingenito GG, Zimbroff DL, Ali MW. Efficacy and Safety of Aripiprazole and Haloperidol Versus Placebo in patients With Schizophrenia and Schizoaffective Disorder. J Clin Psychiatry. 2002; 63: 763-771.
McQuade R, Carson W, Saha A, Ingenito G, Ali M. Aripiprazole for long-term maintenance treatment of schizophrenia. European Neuropsychopharmacology. 2002a; 12: S288-S288.
Chrzanowski WK, Marcus RN, Torbeyns A, Nyilas M, McQuade RD. Effectiveness of long-term aripiprazole therapy in patients with acutely relapsing or chronic, stable schizophrenia: a 52- week, open-label comparison with olanzapine. Psychopharmacology (Berl). 2006; 189:259–266.
Tandon R and Jibson MD. Comparing efficacy of first line antipsychotic; no evidence of differential efficacy between risperidone, olanzapine, quetiapine, ziprasidone and aripiprazole. Int. Journal Psychiatry in Clin Pract. 2005; 9:204-12.
Kane JM, Osuntokun O, Kryzhanovskaya LA, Xu W, Stauffer VL, Watson SB, Brier A. A 28-week, randomized, double-blind study of olanzapine versus ar ipiprazole in the t reatment of schizophrenia. J Clin Psychiatry. 2009; 70: 572-81.
Kinon BJ, Stauffer VL, Kollack-Walker S, Chen L, Sniadecki J. Olanzapine Versus Aripiprazole for the Treatment of Agitation in acutely ill patients with Schizophrenia. J Clin Psychopharmacol. 2008; 28:601-7.
Taylor D, Hanssens L, Loze JY, Pans M, L'Italien G, Marcus RN. Preference of medicine and patientreported quality of life in community-treated schizophrenic patients receiving aripiprazole vs standard of care: results from the STAR study. Eur Psychiatry. 2008; 23: 336-43.
Casey DE, Carson WH, Saha AR, Liebeskind A, Ali MW, Jody D, Ingenito GG. Switching patients to aripiprazole from other antipsychotic agents: amulti center and omized study. Psychopharmacology (Berl) 2003; 166: 391-9.
Medori R, Gharbia N, Saha A, Ali M, Stock E, Ingenito G. Switching to Aripiprazole Monotherapy. European Neuropsychopharmacology. 2002;12:S292
McQuade RD, Stock E, Marcus R, Jody D, Gharbia NA, Vanveggel S, et al. A Comparison of weight change during treatment with olanzapine or aripiprazole: result from a randomized, double-blind study. J Clin Psychiatry 2004; 65:47-56.
Newcomer JW, Meyer JM, Baker RA, Eudicone JM, Pikalov A, Vester-Blokland E, Mcquade RD, Crandall DT, Carson WH, Marcus RN, L'italien G. Changes in non-high-density lipoprotein cholesterol levels and triglyceride/high-density lipoprotein cholesterol ratios among patients randomized to aripiprazole versus olanzapine. Schizophr Res. 2008; 106: 300-7.
Newcomer JW, Campos JA, Marcus RN, Breder C, et al. Amulticentre, randomized, double-blind study of the effects of aripiprazole in overweight subjects with schizophrenia or schizoaffective disorder switched from olanzapine. J Clin Psychiatry 2008; 69: 1046-56.
Keck PE, Marcus R, Tourkodimitris S, Ali M, Liebeskind A, Saha A, Ingenito G. A Placebo- Controlled, Double-Blind Study of the Efficacy and Safety of Aripiprazole in Patients with Acute Bipolar Mania. Am J Psychiatry 2003; 160:1651-1658.