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Ziprasidone

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An Erratum to this article was published on 01 April 1998

Summary

▴ Ziprasidone is a novel antipsychotic drug. It has high affinity for serotonin 5-HT2 and dopamine D2 receptors in vitro, with an 11-fold higher affinity for 5-HT2 than for D2 receptors, suggestive of a low potential for inducing motor disturbance [including extrapyramidal symptoms (EPS)].

▴ The effects of ziprasidone in receptor binding studies reflected its in vitro pharmacology, with more potent effects against 5-HT2 receptor- than against D2 receptor-mediated behaviour.

▴ Because ziprasidone inhibits serotonin (5-hydroxytryptamine; 5-HT) and noradrenaline (norepinephrine) reuptake, it may have anxiolytic and antidepressant effects.

▴ Data from phase II and III clinical trials have shown ziprasidone to be effective in reducing the positive and negative symptoms of, and depression associated with, schizophrenia, and in reducing anxiety in patients about to undergo dental surgery.

▴ Ziprasidone was generally well tolerated in phase II and III clinical trials, with somnolence and nausea being the most frequently reported adverse events in placebo-controlled studies. Motor disturbances, including EPS, were infrequently observed.

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References

  1. Meltzer HY. Role of serotonin in the action of atypical antipsychotic drugs. Clin Neurosci 1995; 3(2): 64–75

    PubMed  CAS  Google Scholar 

  2. Meltzer HY. Pre-clinical pharmacology of atypical antipsychotic drugs: a selective review. Br J Psychiatry 1996 May; 168 Suppl. 29: 23–31

    Google Scholar 

  3. Hesselink JMK, Sambunaris A. Behavioral pharmacology of serotonin receptor subtypes: hypotheses for clinical applications of selective serotonin ligands. Int Rev-Psych 1995; 7(1): 41–53

    Article  Google Scholar 

  4. Tandon R, Harrigan E. Ziprasidone: a novel antipsychotic with unique pharmacology and therapeutic potential. J Ser Res. In press

  5. Seeger TF, Seymour PA, Schmidt AW, et al. Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J Pharmacol Exp Ther 1995 Oct; 275: 101–13

    PubMed  CAS  Google Scholar 

  6. Bench CJ, Lammertsma AA, Dolan RJ, et al. Dose dependent occupancy of central dopamine D2 receptors by the novel neuroleptic CP-88,059-01: a study using positron emission tomography and 11C-raclopride. Psychopharmacology 1993 Sep; 112: 308–14

    Article  PubMed  CAS  Google Scholar 

  7. Fischman A, Bonab AA, Babich JW, et al. Positron emission tomographic analysis of central 5-hydroxytryptamine2 receptor occupancy in healthy volunteers treated with the novel antipsychotic agent, ziprasidone. J Pharmacol Exp Ther 1996; 279(2): 939–47

    PubMed  CAS  Google Scholar 

  8. O’Connor R, Harrigan E, Heym J, et al. The efficacy and safety profile of a new antipsychotic, ziprasidone [abstract]. Xth World Congress of Psychiatry; 1996 May 23–28; Madrid

    Google Scholar 

  9. Miceli JJ, Hunt T, Cole MJ, et al. The pharmacokinetics (PK) of CP-88,059 (CP) in healthy male volunteers following oral (PO) and intravenous (IV) administration [abstract no. PI-78]. 95th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics; 1994 Mar 30–Apr 1; New Orleans, 142

    Google Scholar 

  10. Wilner KD, Hansen RA, Johnson AC, et al. Single and multiple dose pharmacokinetics of ziprasidone in healthy males [abstract no. P-2-7]. Eur Neuropsychopharmacol 1996 Jun; 6 Suppl. 3: 38

    Google Scholar 

  11. Tensfeldt TG, Wilner KD, Baris B, et al. Steady-state pharmacokinetics of ziprasidone in healthy elderly and young volunteers [abstract]. Annual Meeting of the American Psychiatric Association; 1997 May 16–23; San Diego

    Google Scholar 

  12. Prakash C, Kamel A, Anderson W. Absorption, metabolism and excretion of antipsychotic drug ziprasidone in rat and mouse [abstract]. Proceedings of 6th North American International Society for the Study of Xenobiotics Meeting; 1994 Oct 23–7; Raleigh, USA, 107

    Google Scholar 

  13. Prakash C, Kamel A, Cui D, et al. Ziprasidone metabolism and cytochrome P450 isoforms [poster]. Annual Meeting of the American Psychiatric Association; 1997 May 16–23; San Diego

    Google Scholar 

  14. Wilner KD, DeMattos SB, Anziano RJ, et al. Lack of CYP 2D6 inhibition by ziprasidone in healthy volunteers [poster]. Annual Meeting of the American Psychiatric Association; 1997 May 16–23; San Diego

    Google Scholar 

  15. Wilner KD, Anziano RJ, Tensfeldt TG, et al. The effects of ziprasidone on steady-state lithium levels and renal clearance of lithium [abstract no. P-2-8]. Eur Neuropsychopharmacol 1996 Jun; 6 Suppl. 3: 38

    Google Scholar 

  16. Muirhead GJ, Holt PR, Oliver S, et al. The effect of ziprasidone on steady-state pharmacokinetics of a combined oral contraceptive [abstract P-2-6]. Eur Neuropsychopharmacol 1996 Jun; 6 Suppl. 3: 38

    Article  Google Scholar 

  17. Wilner KD, Hansen RA, Folger CJ, et al. Effects of Cimetidine or Maalox® on ziprasidone pharmacokinetics [poster]. Annual Meeting of the American Psychiatric Association; 1997 May 16–23; San Diego

    Google Scholar 

  18. Reeves KR, Harrigan EP. The efficacy and safety of two fixed doses of ziprasidone in schizophrenia and schizoaffective disorder [poster]. 20th Collegium Internationale Neuro-Psychopharmacologicum (C.I.N.P.) Congress; 1996 Jun 23–27; Melbourne

    Google Scholar 

  19. Harrigan E, Morrissey M, Ziprasidone Working Group. The efficacy and safety of 28-day treatment with ziprasidone in schizophrenia/schizoaffective disorder [poster]. 20th Collegium Internationale Neuro-Psychopharmacologicum (C.I.N.P.) Congress; 1996 Jun 23–27; Melbourne

    Google Scholar 

  20. O’Connor R, Harrigan E, Heym J, et al. The efficacy and safety profile of a new antipsychotic, ziprasidone [poster]. VIIIth Congress of the European College of Neuropsychopharmacology; 1995 Sep 30–Oct 4; Venice

    Google Scholar 

  21. Daniel D, Reeves K, Harrigan EP, et al. The efficacy and safety of ziprasidone 80 mg/day and 160 mg/day in schizophrenia and schizoaffective disorder [abstract]. Schizophr Res 1997; 24: 204

    Article  Google Scholar 

  22. American Psychiatric Association. Diagnostic and statistical manual of mental disorders. 3rd rev. ed. Washington, DC: American Psychiatric Association, 1987

    Google Scholar 

  23. Brook S, Swift R, Harrigan EP. The tolerability and efficacy of intramuscular ziprasidone [poster]. Annual Meeting of the American Psychiatric Association; 1997 May 16–23; San Diego

    Google Scholar 

  24. Wilner KD, Anziano RJ, Johnson AC, et al. Anxiolytic effects of ziprasidone compared with diazepam and placebo prior to dental surgery [poster]. 20th Collegium Internationale Neuro-Psychopharmacologicum (C.I.N.P.) Congress; 1996 Jun 23–27; Melbourne

    Google Scholar 

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Correspondence to Anthony Markham.

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An erratum to this article is available at http://dx.doi.org/10.1007/BF03257357.

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Davis, R., Markham, A. Ziprasidone. CNS Drugs 8, 153–159 (1997). https://doi.org/10.2165/00023210-199708020-00006

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