Emerging treatments in the management of schizophrenia - focus on sertindole

Drug Design, Development and Therapy

Volumn 4, Issue , 2010, Pages 187-201

  Muscatello, Maria Rosaria A ^a   Bruno, Antonio ^a   Pandolfo, Gianluca ^a   Micò, Umberto ^a   Settineri, Salvatore ^a   Zoccali, Rocco ^a  

^a UNIVERSITY OF MESSINA   (Italy)

Author keywords

Antipsychotics; Efficacy; Pharmacokinetics; Pharmacology; Safety

Indexed keywords

ALPRAZOLAM; ATYPICAL ANTIPSYCHOTIC AGENT; CLOZAPINE; ERYTHROMYCIN; FLUOXETINE; HALOPERIDOL; INDINAVIR; KETOCONAZOLE; NEUROLEPTIC AGENT; PAROXETINE; PLACEBO; QUINIDINE; RISPERIDONE; SERTINDOLE; TERFENADINE; IMIDAZOLE DERIVATIVE; INDOLE DERIVATIVE;

AKATHISIA; AMNESIA; AREA UNDER THE CURVE; ARTICLE; BODY MASS; CHOLESTEROL BLOOD LEVEL; COGNITIVE DEFECT; CONSTIPATION; CONVULSION; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG DOSE REDUCTION; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG ELIMINATION; DRUG FATALITY; DRUG HALF LIFE; DRUG MEGADOSE; DRUG METABOLISM; DRUG OVERDOSE; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SUBSTITUTION; DRUG TOLERABILITY; DRUG WITHDRAWAL; DYSKINESIA; DYSTONIA; EJACULATION; EXTRAPYRAMIDAL SYMPTOM; EXTRAPYRAMIDAL SYNDROME; FOOD DRUG INTERACTION; GLUCOSE BLOOD LEVEL; HEADACHE; HEART ARRHYTHMIA; HUMAN; INSOMNIA; MALE SEXUAL DYSFUNCTION; MAXIMUM PLASMA CONCENTRATION; METABOLIC DISORDER; METABOLIC SYNDROME X; MORTALITY; MOTOR DYSFUNCTION; MUSCLE HYPERTONIA; MUSCLE RIGIDITY; NEGATIVE SYNDROME; NONHUMAN; NOSE CONGESTION; NUTRITIONAL DISORDER; ORTHOSTATIC HYPOTENSION; PARKINSONISM; POSITIVE AND NEGATIVE SYNDROME SCALE; POSITIVE SYNDROME; PSYCHOSIS; QT INTERVAL; QT PROLONGATION; RHINITIS; SCHIZOPHRENIA; SIDE EFFECT; SINGLE DRUG DOSE; SUDDEN DEATH; SUICIDE; SUICIDE ATTEMPT; T WAVE; TARDIVE DYSKINESIA; TREMOR; TRIACYLGLYCEROL BLOOD LEVEL; WEIGHT GAIN; XEROSTOMIA; ANIMAL; COMPARATIVE STUDY; CONTROLLED CLINICAL TRIAL (TOPIC); FEMALE; MALE; PATHOPHYSIOLOGY; PATIENT COMPLIANCE; REVIEW;

ANIMALS; ANTIPSYCHOTIC AGENTS; CONTROLLED CLINICAL TRIALS AS TOPIC; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HUMANS; IMIDAZOLES; INDOLES; MALE; MEDICATION ADHERENCE; SCHIZOPHRENIA;

EID: 78649235116     PISSN: 11778881     EISSN: None     Source Type: Journal    
DOI: 10.2147/DDDT.S6591     Document Type: Article

References (85)

1. Saha S, Chant D, Welham J, McGrath J. A systematic review of the prevalence of schizophrenia. PLoS Med. 2005;2:e141.
2. Tamminga CA, Holcomb HH. Phenotype of schizophrenia: a review and formulation. Mol Psychiatry. 2005;10:27-39.
3. Arnt J, Skarsfeldt T. Do novel antipsychotics have similar pharmachological characteristics? A review of the evidence. Neuropsychopharmachology. 1998;18:63-101.
4. American Psychiatric Association. Practice guidelines for the treatment of patients with schizophrenia. 2nd Edition. Am J Psychiatry. 2004;16: 1-114.
5. Gaebel W, Falkai P, Weinmann S, Wobrock T. Treatment guidelines for schizophrenia [Behandlungsleitlinie Schizophrenie]. Stuttgart, Germany: Steinkopf; 2006.
6. Miyamoto S, Duncan GE, Marx CE, Lieberman JA. Treatments for schizophrenia: a critical review of pharmacology and mechanisms of action of antipsychotic drugs. Mol Psychiatry. 2005;10:79-104.
7. Haddad PM, Sharma SG. Adverse effects of atypical antipsychotics: differential risk and clinical implications. CNS Drugs. 2007;21: 911-936.
8. Henderson DC, Cagliero E, Copeland PM, et al. Glucose metabolism in patients with schizophrenia treated with atypical antipsychotic agents: a frequently sampled intravenous glucose tolerance test and minimal model analysis. Arch Gen Psychiatry. 2005;62:19-28.
9. Luft B, Taylor D. A review of atypical antipsychotic drugs versus conventional medication in schizophrenia. Expert Opin Pharmacother. 2006;7:1739-1748.
10. Lieberman JA, Stroup TS, McEvoy JP, et al. Effectiveness of antipsychotic drugs in patients with chronic schizophrenia. New Engl J Med. 2005;353:1209-1223.
11. Stroup TS, Lieberman JA, McEvoy JP, et al. Results of phase 3 of the CATIE schizophrenia trial. Schizophr Res. 2009;107:1-12.
12. Eckardt L, Haverkamp W, Mertens M, et al. Drug-related torsade de pointes in the isolated rabbit heart: comparison of clofilium, d,l-sotalol and erythromycin. J Cardiovasc Pharmacol. 1998;32:425-434.
13. Hondeghem LM, Carlsson L, Duker G. Instability and triangulation of the action potential predict serious proarrhythmia, but action potential duration prolongation is antiarrhythmic. Circulation. 2001;103: 2004-2013.
14. Eckardt L, Breithardt G, Haverkamp W. Electrophysiologic characterization of the antipsychotic drug sertindole in a rabbit heart model of torsades de pointes: low torsadogenic potential despite QT prolongation. J Pharmacol Exp Ther. 2002;300:64-71.
15. Wilton LV, Heeley EL, Pickering RM, Shakir SA. Comparative study of mortality rates and cardiac dysrhythmias in postmarketing surveillance studies of sertindole and two other atypical antipsychotic drugs, risperidone and olanzapine. J Psychopharmacol. 2001;15:120-126.
16. Moore N. Higher cardiovascular mortality with sertindole in ADROIT: a signal not confirmed. Int J Psychiatry Clin Pract. 2002;6 Suppl 1: S3-S9.
17. Lindstrom E, Levander S. Sertindole: efficacy and safety in schizophrenia. Exp Opin Drug Saf. 2006;1825-1834.
18. Sanchez C, Arnt J, Dragsted N, et al. Neurochemical and in vivo pharmacological profile of sertindole, a limbic-selective neuroleptic compound. Drug Dev Res. 1991;22:239-242.
19. Hyttel L, Nielsen JB, Nowak G. The acute effect of sertindole on brain 5-HT2, D2 and alpha one receptors. J Neural Transm. 1992;89: 61-69.
20. Mørk A, Witten LM, Arnt J. Effect of sertindole on extracellular dopamine, acetylcholine, and glutamate in the medial prefrontal cortex of conscious rats: a comparison with risperidone and exploration of mechanisms involved. Psychopharmacology. 2009;206:39-49.
21. Gleason S, Shannon H. Blockade of phencyclidine-induced hyperlocomotion by olanzapine, clozapine and serotonin receptor subtype selective antagonists in mice. Psychopharmacology (Berl). 1997;129: 79-84.
22. Horacek J, Bubenikowa-Valesova V, Kopecek M, et al. Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs. 2006;20:389-409.
23. Wood MD, Scott C, Clarke K, et al. Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets. 2006;5:445-452.
24. Petit-Taboué MC, Landeau B, Barré L, et al. Parametric PET imaging of 5-HT2A receptor distribution with 18F-setoperone in the normal human cortex. J Nucl Med. 1999;40:25-32.
25. Skarsfeldt T. Electrophysiological profile of the new atypical neuroleptic, sertindole, on midbrain dopamine neurons in rats: acute and repeated treatment. Synapse. 1992;10:25-32.
26. Zimbroff DL, Kane JM, Tamminga CA, et al. Controlled, dose-response study of sertindole and haloperidol in the treatment of schizophrenia. Am J Psychiatry. 1997;154:782-791.
27. Hietala J, Kuoppamaki M, Majasuo H, et al. Sertindole is a serotonin 5-HT2C inverse agonist and decreases agonist but not antagonist binding to 5-HT2C receptors after chronic treatment. Psychopharmacology. 2001;157:180-187.
28. Nyberg S, Olsson H, Nilsson U, et al. Low striatal and extra-striatal D2 receptor occupancy during treatment with the atypical antipsychotic sertindole. Psychopharmachology. 2002;162:37-41.
29. Didriksen M, Skarsfeldt T, Arnt J. Reversal of PCP-induced learning and memory deficits in the Morris' water maze by sertindole and other antipsychotics. Psychopharmacology (Berl). 2007;193:225-233.
30. Goetghebeur P, Dias R. Comparison of haloperidol, risperidone, sertindole, and modafinil to reverse an attentional set-shifting impairment following subchronic PCP administration in the rat-a back translational study. Psychopharmacology (Berl). 2009;202:287-293.
31. Rodefer JS, Nguyen TN, Karlsson JJ, Arnt J. Reversal of subchronic PCP-induced deficits in attentional set shifting in rats by sertindole and a 5-HT(6) receptor antagonist: comparison among antipsychotics. Neuropsychopharmacology. 2008;33:2657-2666.
32. Broberg BV, Glenthøj BY, Dias R, Larsen DB, Olsen CK. Reversal of cognitive deficits by an ampakine (CX516) and sertindole in two animal models of schizophrenia - sub-chronic and early postnatal PCP treatment in attentional set-shifting. Psychopharmacology (Berl). 2009;206: 631-640.
33. Idris N, Neill J, Grayson B, et al. Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms. Psychopharmacology (Berl). 2010;208:23-36.
34. Wong SL, Linen P, Mack RJ, Granneman GR. Effects of food, antacid, and dosage form on the pharmacokinetics and relative bioavailability of sertindole in healthy volunteers. Biopharm Drug Dispos. 1997;18:533-541.
35. Wong SL, Cao G, Mack RJ, Granneman GR. Pharmacokinetics of sertindole in healthy young and elderly male and female subjects. Clin Pharmacol Ther. 1997;62:157-164.
36. Wong SL, Menacherry S, Mulford D, et al. Parmacokinetics of sertindole and dehydrosertindole in volunteers with normal or impaired renal function. Eur J Clin Pharmacol. 1997;52:223-227.
37. Wong SL, Granneman R. Modeling of sertindole pharmacokinetic disposition in healthy volunteers in short-term dose-escalation studies. J Pharm Sci. 1998;87:1629-1631.
38. H. Lundbeck A/S. Serdolect (sertindole) monograph. Copenhagen: H. Lundbeck A/S 2005 Sep.
39. Doran A, Obach RS, Smith BJ, et al. The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos. 2005;33:165-174.
40. Wang JS, Zhu HJ, Markowitz JS, Donovan JL, De Vane CL. Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology. 2006;187:415-423.
41. Wong SL, Cao G, Mack RJ, Granneman GR. The effect of erythromycin on the CYP3A component of sertindole clearance in healthy volunteers. J Clin Pharmacol. 1997;37:1056-1061.
42. Haduch A, Ogórca T, Boksa J, Daniel WA. Interactions between neuroleptics and CYP2C6 in rat liver - in vitro and ex vivo study. Pharmacol Rep. 2005;57:872-877.
43. Wong SL, Locke C, Staser J, Granneman GR. Lack of multiple dosing effect of sertindole on the pharmacokinetics of alprazolam in healthy volunteers. Psychopharmacology. 1998;135:236-241.
44. Wong SL, Cao G, Mack R, Granneman GR. Lack of CYP3A inhibition effects of sertindole on terfenadine in healthy volunteers. Int J Clin Pharmacol Ther. 1998;36:146-151.
45. van Kammen DP, McEvoy JP, Targum SD, et al. A randomized, controlled, dose-ranging trial of sertindole in patients with schizophrenia. Psychopharmacology. 1996;124:168-175.
46. Zimbroff A, Kane JM, Tamminga CA, et al. Controlled, dose-response study of sertindole and haloperidol in the treatment of schizophrenia: results of a phase III trial. Int J Psychiatry Clin Pract. 2000;4:55-62.
47. Hale A, Azorin JM, Kasper S, et al. Sertindole improves both the positive and negative symptoms of schizophrenia: results of a phase III trial. Int J Psychiatry Clin Pract. 2000;4:55-62.
48. Daniel DG, Wozniak P, Mack RJ, et al. Long-term efficacy and safety comparison of sertindole and haloperidol in the treatment of schizophrenia. Psychopharmacol Bull. 1998;34:61-69.
49. Azorin JM, Strub N, Loft H. A double-blind, controlled study of sertindole versus risperidone in the treatment of moderate-to-severe schizophrenia. Int Clin Psychopharmacol. 2006;21:49-56.
50. Azorin JM, Murteira S, Hansen K, Toumi M. Evaluation of patients on sertindole treatment after failure of other antipsychotics: A retrospective analysis. BMC Psychiatry. 2008;8-16.
51. Leucht S, Corves C, Arbter D, Engel RR, Li C, Davis JM. Secondgeneration versus first-generation antipsychotic drugs for schizophrenia: a meta-analysis. Lancet. 2009;373:31-41
52. Komossa K, Rummel-Kluge C, Hunger H, et al. Sertindole versus other atypical antipsychotics for schizophrenia (Review). Cochrane Database Syst Rev. 2010;2:CD006752.
53. Kasper S. Do we need another atypical antipsychotic? Eur Neuropsychopharmacol. 2008;18:S146-S152.
54. Gallhofer B, Jaanson P, Mittoux A, Tanghøj P, Lis S, Krieger S. Course of recovery of cognitive impairment in patients with schizophrenia: A randomised double-blind study comparing sertindole and haloperidol. Pharmacopsychiatry. 2007;40:275-286.
55. Mortimer AM. Cognitive function in schizophrenia-do neuroleptics make a difference? Pharmacol Biochem Behav. 1997;56:789-795.
56. Cleghorn JM, Kaplan RD, Szechtman B, Szechtman H, Brown GM. Neuroleptic drug effects on cognitive function in schizophrenia. Schizophr Res. 1990;3:211-219.
57. Cutmore TR, Beninger RJ. Do neuroleptics impair learning in schizophrenic patients? Schizophr Res. 1990;3:173-186.
58. Stone JM, Morrison PD, Pilowsky LS. Glutamate and dopamine dysregulation in schizophrenia - a synthesis and selective review. J Psychopharmacol. 2007;21:440-452.
59. Buchsbaum MS, Haznedar M, Newmark RE, et al. FDG-PET and MRI imaging of the effects of sertindole and haloperidol in the prefrontal lobe in schizophrenia. Schizophr Res. 2009;114:161-171.
60. Peuskens J, Moore N, Azorin JM, Toumi M, Cochran J. The European sertindole safety and exposure survey: a follow-up study of 8600 patients. Pharmacoepidemiol Drug Saf. 2007;16:804-811.
61. Peuskens J, Tanghøj P, Mittoux A. The Sertindole Cohort Prospective (SCoP) study: rationale, design and methodology. Pharmacoepidemiol Drug Saf. 2008;17:425-433
62. Lançon C, Toumi M, Sapin C, Hansen K. The Sertindole Safety Survey: A retrospective analysis under a named patient use programme in Europe. BMC Psychiatry. 2008;8:57.
63. Thomas SHL, Drici MD, Hall GC, et al. Safety of sertindole versus risperidone in schizophrenia: principal results of the sertindole cohort prospective study (SCoP). Acta Psychiatr Scand. 2010:1-11.
64. Kasper S, Möller HJ, Hale A. The European Post-marketing Observational Sertindole Study: an investigation of the safety of antipsychotic drug treatment. Eur Arch Psychiatry Clin Neurosci. 2010;260: 59-68.
65. Perquin LN, Steinert T. A review of the efficacy, tolerability and safety of sertindole in clinical trials. CNS Drugs. 2004;18 Suppl 2: 19-30.
66. Haverkamp W, Eckhardt L, Matz J, Frederiksen K. Sertindole: Cardiac electrophysiological profile. Int J Psychiatry Clin Pract. 2002;6: 11-20.
67. Neckelmann D, Mæhlum E, Waage IM. Sertindole and fluoxetine overdose with benign outcome. Nord J Psychiatry. 2010 Feb 18.
68. Canal-Raffin M, Déridet E, Titier K, Frakra E, Molimard M, Moore N. Simplified ultraviolet liquid chromatographic method for determination of sertindole, dehydrosertindole and norsertindole in human plasma. J Chromatography B. 2005;814:61-67.
69. Lewis R, Bagnall AM, Leitner M. Sertindole for schizophrenia. Cochrane Database Syst Rev. 2005;3:CD001715.
70. Gao XM, Sakai K, Tamminga CA. Chronic olanzapine or sertindole treatment results in reduced oral chewing movements in rats compared to haloperidol. Neuropsychopharmacology. 1998;19(5): 428-433.
71. Perquin LN. Treatment with the new antipsychotic sertindole for lateoccurring undesirable movement effects. Int Clin Psychopharmacol. 2005;20:335-338.
72. Yap YG, Camm J. Risk of torsades de pointes with non-cardiac drugs. Br Med J. 2000;320:1158-1159.
73. Kasper S, Tuomi M. The clinical safety and tolerability profile of sertindole. Int J Neuropsychopharmacology. 2004;7:S422.
74. Mack R, Driscoll R, Silber C. The long term cardiovascular safety of sertindole. Eur Neuropsychopharmacology. 1997;7:S207.
75. Titier K, Canal M, Déridet C, et al. Determination of myocardium to plasma concentration ratios of five antipsychotic drugs: comparison with their ability to induce arrhythmia and sudden death in clinical practice. Toxicol Appl Pharmacol. 2004;199:52-60.
76. Harrigan EP, Miceli JJ, Anziano R, et al. A randomized evaluation of the effects of six antipsychotic agents on QTc, in the absence and presence of metabolic inhibition. J Clin Psychopharmacol. 2004;24: 62-69.
77. DuBuske LM. Second-generation antihistamines: the risk of ventricular arrhythmias. Clin Ther. 1999;21:281-295.
78. Witchel HJ, Hancox JC. Familial and acquired long QT syndrome and the cardiac rapid delayed rectifier potassium current. Clin Exp Pharmacol Physiol. 2000;27:753-766.
79. Glassman AH, Bigger, JT. Antipsychotic drugs: Prolonged QTc interval, torsade de pointes, and sudden death. Am J Psychiatry. 2001;158:1774-1782.
80. Nielsen J, Graff C, Hardahl T, et al. Sertindole causes distinct electrocardiographic T-wave morphology changes. Eur Neuropsychopharmacol. 2009;19:702-707.
81. Nielsen J, Andersen MP, Graff C, et al. The effect of sertindole on QTD and TPTE. Acta Psychiatr Scand. 2010;121:385-388.
82. Ray WA, Chung CP, Murray KT, Hall K, Stein CM. Atypical antipsychotic drugs and the risk of sudden cardiac death. N Engl J Med. 2009;360:225-235.
83. Tiihonen J, Lönnqvist J, Wahlbeck K, et al. 11-year follow-up of mortality in patients with schizophrenia: a population-based cohort study (FIN11 study). Lancet. 2009;374:620-627.
84. Spina E, Zoccali R. Sertindole: pharmacological and clinical profile and role in the treatment of schizophrenia. Expert Opin Drug Metab Toxicol. 2008;4(5):629-638.
85. Caccia S, Pasina L, Nobili A. New atypical antipsychotics for schizophrenia: iloperidone. Drug Des Devel Ther. 2010;18;4:33-48.