Skip to main content
Log in

Aripiprazole

  • Adis New Drug Profile
  • Published:
CNS Drugs Aims and scope Submit manuscript

Abstract

▴ Aripiprazole is a quinolinone derivative and the first of a new class of atypical antipsychotics. The drug has partial agonist activity at dopamine D2 and serotonin 5-HT1a receptors, and is also an antagonist at 5-HT2A receptors.

▴ In patients with acute relapse of schizophrenia or schizoaffective disorder, aripiprazole 15 to 30 mg/day was at least as effective as haloperidol 10 mg/day and had similar efficacy to risperidone 6 mg/day in well designed, 4-week, placebo-controlled trials.

▴ Negative symptoms improved earlier in the aripiprazole than the risperidone group. Efficacy of aripiprazole was observed at week 1 in several trials and was sustained throughout the study periods.

▴ Aripiprazole was superior to placebo in a 26-week trial in patients with stable, chronic schizophrenia. In a 52-week trial involving patients with acute relapsing disease, aripiprazole was similar to haloperidol as assessed by time to failure to maintain response and was superior in ameliorating negative and depressive symptoms.

▴ The incidence of extrapyramidal symptoms during aripiprazole therapy was similar to that with risperidone and placebo but lower than with haloperidol.

▴ Compared with placebo, the proportion of patients with increased plasma prolactin levels and QTc prolongation was similar in patients treated with aripiprazole 15 to 30 mg/day but was significantly increased with haloperidol and risperidone.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1

Similar content being viewed by others

References

  1. Work Group on S chizophrenia. Practice guidelines for the treatment of patients with schizophrenia. Am J Psychiatry 1997 Apr; 154(4 Suppl.): 1–63

    Google Scholar 

  2. Campbell M, Young PI, Bateman DN, et al. The use of atypical antipsychotics in the management of schizophrenia. Br J Clin Pharmacol 1999 Jan; 47: 13–22

    Article  PubMed  CAS  Google Scholar 

  3. Lehman AF. Managing schizophrenia: interventions and outcomes. Dis Manage Health Outcomes 1997 Jun; 1(6): 286–95

    Article  Google Scholar 

  4. Blin O. A comparative review of new antipsychotics. Can J Psychiatry 1999 Apr; 44(3): 235–44

    PubMed  CAS  Google Scholar 

  5. American Psychiatric Association. Practice guidelines for the treatment of patients with schizophrenia. III. Treatment principles and alternatives [online]. Available from URL: http://www.sych.org/clin_res/pg_schizo_3.cfm [Accessed 2002 Sep 24]

  6. Burris KD, Molski TF, Xu C, et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther 2002; 302(1): 381–9

    Article  PubMed  CAS  Google Scholar 

  7. Jordan S, Koprivica V, Chen R, et al. The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT(1A) receptor. Eur J Pharmacol 2002; 441: 137–40

    Article  PubMed  CAS  Google Scholar 

  8. McQuade RD, Burris KD, Jordan S, et al. Aripiprazole: a dopamine-serotonin system stabilizer [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  9. Inoue A, Miki S, Seto M, et al. Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum. Eur J Pharmacol 1997Feb 19; 321(1): 105–11

    Article  PubMed  Google Scholar 

  10. Lawler CP, Prioleau C, Lewis MM, et al. Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacol 1999 Jun; 20(6): 612–27

    Article  CAS  Google Scholar 

  11. Bymaster FP, Calligaro DO, Falcone JF, et al. Radioreceptorbinding profile of the atypical antipsychotic olanzapine. Neuropsychopharmacol 1996; 14(2): 87–96

    Article  CAS  Google Scholar 

  12. Yokoi F, Gründer G, Biziere K, et al. Dopamine D2 and D3 receptor occupancy in normal humans treated with the antipsychotic drug aripiprazole (OPC 14597): a study using positron emission tomography and [11C]raclopride. Neuropsycho-pharmacol 2002; 27(2): 248–59

    Article  CAS  Google Scholar 

  13. Sasa M, Amano T. Unique pharmacological profile of a novel antipsychotic drug, aripiprazole (OPC-14597). CNS Drug Rev 1997; 3(1): 24–33

    Article  CAS  Google Scholar 

  14. Fujikawa M, Nagashima M, Inoue T, et al. Partial agonistic effects of OPC-14597, a potential antipsychotic agent, on yawning behavior in rats. Pharmacol Biochem Behav 1996 Apr; 53(4): 903–9

    Article  PubMed  CAS  Google Scholar 

  15. Kikuchi T, Uwahodo Y, Tottori K, et al. Behavioral pharmacological studies of OPC-14597, a novel antipsychotic drug: comparison with OPC-4392, clozapine and haloperidol [abstract no. P-507]. Jpn J Pharmacol 1996; 71Suppl. I: 185P

    Google Scholar 

  16. Uwahodo Y, Kikuchi T, Tottori K, et al. Pharmacological profile of OPC-14597, a novel anti-psychotic drug (2): weak extrapyramidal side effects [abstract no. P1-236]. Jpn J Pharmacol 1995; 67Suppl. I: 144P

    Google Scholar 

  17. Hirose T, Nakai S, Uwahodo Y, et al. Influence of aripiprazole (OPC-14597) on the induction of catalepsy and brain dopamine metabolism after chronic treatment: a comparison with haloperidol or risperidone [abstract no. O-82]. Jpn J Pharmacol 2000; 82 Suppl. 1: 62

    Google Scholar 

  18. Nakai S, Hirose T, Uwahodo Y, et al. Catalepsy and striatolimbic dopamine metabolism following chronic aripiprazole, risperidone and haloperidol. Int J Neuropsychopharmacol 2000 Jul; 3Suppl. 1: S97

    Google Scholar 

  19. Cañive JM, Lewine JD, Edgar JC, et al. Spontaneous brain magnetic activity in schizophrenia patients treated with aripiprazole. Psychopharmacol Bull 1998; 34(1): 101–5

    PubMed  Google Scholar 

  20. Mallikaarjun S, Salazar DE, Bramer SL. Pharmacokinetics, tolerability, and safety of aripiprazole following single and multiple oral dose administration. Eur Neuropsychopharmacol 2000 Sep; 10 Suppl. 3: 306–7

    Article  Google Scholar 

  21. Mallikaarjun S, Tammara BK, Salazar DE, et al. The effects of hepatic impairment on the pharmacokinetics of aripiprazole [abstract no. TPII-91]. Clin Pharmacol Ther 2002 Feb; 71(2): 66

    Google Scholar 

  22. Mallikaarjun S, Ali MW, Salazar DE, et al. The effects of age and gender on the pharmacokinetics of aripiprazole [abstract no. TPII-90]. Clin Pharmacol Ther 2002 Feb; 71(2): 66

    Google Scholar 

  23. Citrome L, Josiassen R, Bark N, et al. Pharmacokinetics and safety of aripiprazole and concomitant mood stabilizers [abstract no. P.4.E.035]. Int J Neuropsychopharmacol 2002; 5Suppl. 1 (Jun): S187

    Google Scholar 

  24. Citrome L, Josiassen R, Bark N, et al. Pharmacokinetics and safety of aripiprazole and concomitant mood stabilizers [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  25. Kane JM, Carson WH, Saha AR, et al. Efficacy and safety of aripiprazole and haloperidol versus placebo in patients with schizophrenia and schizoaffective disorder. J Clin Psychiatry 2002 Sep; 63: 1–9

    Article  Google Scholar 

  26. Yeung PP, Carson WH, Saha A, et al. Efficacy of aripiprazole, a novel antipsychotic, in schizophrenia and schizoaffective disorder: results of a placebo-controlled trial with risperidone [abstract no. P.2.040]. Eur Neuropsychopharmacol 2001 Oct; 11Suppl. 3: S259–60

    Article  Google Scholar 

  27. Daniel DG, Saha AR, Ingenito G, et al. Aripiprazole, a novel antipsychotic: overview of a phase II study result [abstract no. P.01.242]. Int J Neuropsychopharmacol 2000 Jul; 3Suppl. 1: S157

    Google Scholar 

  28. Petrie JL, Saha AR, McEvoy JP. Aripiprazole, a new typical antipsychotic: phase 2 clinical trial result [abstract no. P.2.114]. Eur Neuropsychopharmacol 1997 Sep; 7Suppl. 2: S227

    Article  Google Scholar 

  29. Kujawa M, Saha AR, Ingenito GG, et al. Aripiprazole for long-term maintenance treatment of schizophrenia [abstract no. P.4.E.032]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. l: S186–7

    Google Scholar 

  30. Kujawa M, Saha A, Ingenito G, et al. Aripiprazole for long-term maintenance treatment of schizophrenia [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  31. Carson WH, Pigott TA, Saha AR, et al. Aripiprazole vs. placebo in the treatment of chronic schizophrenia [abstract no. P.4.E.033]. Int J Neuropsychopharmacol 2002 Jun; 5 Suppl. 1:S187

    Google Scholar 

  32. Carson WH, Pigott TA, Saha AR, et al. Aripiprazole vs placebo in the treatment of stable, chronic schizophrenia [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  33. Casey D, Saha AR, Ali MW, et al. Switching to aripiprazole monotherapy [abstract no. P.4.E.034]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S187

    Google Scholar 

  34. Casey DE, Saha A, Ali M, et al. Switching to aripiprazole monotherapy [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  35. Lieberman J, Carson WH, Saha AR, et al. Meta-analysis of the efficacy of aripiprazole in schizophrenia [abstract no. P.4.E.031]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S186

    Google Scholar 

  36. Lieberman JA, Carson WH, Saha A, et al. Meta-analysis of the efficacy of aripiprazole in schizophrenia [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  37. Cornblatt B, Kern RS, Carson WH, et al. Neurocognitive effects of aripiprazole vs olanzapine in stable psychosis [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  38. Cornblatt B, Kern RS, Carson WH, et al. Neurocognitive effects of aripirazole vs olanzapine in stable psychosis [abstract no. P.4.E.027]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S185

    Google Scholar 

  39. Stock E, Marder SR, Saha AR, et al. Safety and tolerability meta-analysis of aripiprazole in schizophrenia [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  40. Stock E, Marder SR, Saha AR, et al. Safety and tolerability meta-analysis of aripiprazole in schizophrenia [abstract no. P.4.E.025]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S186

    Google Scholar 

  41. Carson W, Saha AR, Iwamoto R, et al. Meta-analysis of prolactin effects with aripiprazole [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  42. Carson W, Saha AR, Iwamoto T, et al. Meta-analysis of prolactin effects with aripiprazole [abstract no. P.4.E.028]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S186

    Google Scholar 

  43. Stock E, Saha A, Brunell R, et al. Meta-analysis of cardiac safety with aripiprazole [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  44. Stock E, Marder SR, Saha AR, et al. Safety and tolerability meta-analysis of aripiprazole in schizophrenia [abstract no. P.4.E.029]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S186

    Google Scholar 

  45. Jody D, Saha AR, Iwamoto T, et al. Meta-analysis of weight effects with aripiprazole [poster]. XXIII CINP Congress; 2002 Jun 23–27; Montreal

  46. Jody D, Saha AR, Iwamoto T, et al. Meta-analysis of weight effects with aripiprazole [abstract no. P.4.E.030]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S186

    Google Scholar 

  47. Saha A, Ali MW, Ingenito GG, et al. Safety and tolerability of aripiprazole at doses higher than 30 mg [abstract no. P.4 E. 026]. Int J Neuropsychopharmacol 2002 Jun; 5Suppl. 1: S185

    Google Scholar 

  48. Anon. FDA issues approvable letter for Abilify™ [online]. Available from URL: http://www.bms.com/news/press/data/fg_press_release_2897.html [Accessed 2002 Sep 5]

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Karen L. Goa.

Rights and permissions

Reprints and permissions

About this article

Cite this article

McGavin, J.K., Goa, K.L. Aripiprazole. Mol Diag Ther 16, 779–786 (2002). https://doi.org/10.2165/00023210-200216110-00008

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00023210-200216110-00008

Keywords

Navigation