Evaluation of the clinical efficacy of asenapine in schizophrenia

被引:26
作者
Minassian, Arpi [1 ]
Young, Jared W. [1 ]
机构
[1] Univ Calif San Diego, Dept Psychiat, La Jolla, CA 92093 USA
关键词
antipsychotic; asenapine; bipolar disorder; dopamine; SAPHRIS; schizophrenia; serotonin; PSYCHOPHARMACOLOGICAL AGENT; BEHAVIORAL PHARMACOLOGY; N-DESMETHYLCLOZAPINE; ANTIPSYCHOTIC-DRUGS; ACUTE EXACERBATION; EXPOSURE-RESPONSE; CONTROLLED TRIAL; DOUBLE-BLIND; ACUTE MANIA; IN-VIVO;
D O I
10.1517/14656566.2010.506188
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Importance of the field: Asenapine is a new atypical antipsychotic medication with high affinity for D-2 and 5HT(2A) receptors that has been approved by the FDA in adults for the acute treatment of schizophrenia in the USA. The purpose of this review is to describe the compound and examine whether it addresses some of the unmet clinical needs in treating schizophrenia. Areas covered in this review: The development of asenapine is described with attention to its chemistry, pharmacodynamic and pharmacokinetic profile. Preclinical and clinical trials of safety and efficacy are reviewed. The advantages and disadvantages of asenapine relative to other antipsychotic medications are discussed. What the reader will gain: Asenapine will be evaluated for whether it: i) causes a reduction in symptoms of schizophrenia; ii) has a side-effect profile minimizing extrapyramidal symptoms, weight gain and cardiac effects; and iii) affects negative and/or cognitive symptoms. Take home message: Asenapine is a recently approved agent with an acceptable cardiometabolic profile and exhibits similar efficacy as other antipsychotic medications, primarily on positive symptoms of schizophrenia. Relatively less weight gain compared with other agents may confer a notable advantage. Sublingual administration may have positive and negative effects on patient compliance. Potential 'pro-cognitive' effects of asenapine are preliminary and require more investigation.
引用
收藏
页码:2107 / 2115
页数:9
相关论文
共 65 条
[1]   Selecting Paradigms From Cognitive Neuroscience for Translation into Use in Clinical Trials: Proceedings of the Third CNTRICS Meeting [J].
Barch, Deanna M. ;
Carter, Cameron S. ;
Arnsten, Amy ;
Buchanan, Robert W. ;
Cohen, Jonathan D. ;
Geyer, Mark ;
Green, Michael F. ;
Krystal, John H. ;
Nuechterlein, Keith ;
Robbins, Trevor ;
Silverstein, Steven ;
Smith, Edward E. ;
Strauss, Milton ;
Wykes, Til ;
Heinssen, Robert .
SCHIZOPHRENIA BULLETIN, 2009, 35 (01) :109-114
[2]   Upcoming Agents for the Treatment of Schizophrenia Mechanism of Action, Efficacy and Tolerability [J].
Bishara, Delia ;
Taylor, David .
DRUGS, 2008, 68 (16) :2269-2292
[3]  
BROEKKAMP CLE, 1990, ARZNEIMITTELFORSCH, V40-1, P544
[4]   A summary of the FDA-NIMH-MATRICS Workshop on Clinical Trial Design for Neurocognitive Drugs for Schizophrenia. [J].
Buchanan, RW ;
Davis, M ;
Goff, D ;
Green, MF ;
Keefe, RSE ;
Leon, AC ;
Nuechterlein, KH ;
Laughren, T ;
Levin, R ;
Stover, E ;
Fenton, W ;
Marder, SR .
SCHIZOPHRENIA BULLETIN, 2005, 31 (01) :5-19
[5]   Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors:: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist [J].
Burstein, ES ;
Ma, J ;
Wong, S ;
Gao, Y ;
Pham, E ;
Knapp, AE ;
Nash, NR ;
Olsson, R ;
Davis, RE ;
Hacksell, U ;
Weiner, DM ;
Brann, MR .
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2005, 315 (03) :1278-1287
[6]   Neurochemical evidence for antagonism by olanzapine of dopamine, serotonin, alpha(1)-adrenergic and muscarinic receptors in vivo in rats [J].
Bymaster, FP ;
HemrickLuecke, SK ;
Perry, KW ;
Fuller, RW .
PSYCHOPHARMACOLOGY, 1996, 124 (1-2) :87-94
[7]  
Carpenter WT, 2008, PSYCHIAT SERV, V59, P523, DOI 10.1176/ps.2008.59.5.523
[8]   Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study [J].
Casey, Daniel E. ;
Sands, Earl E. ;
Heisterberg, Jens ;
Yang, Hwa-Ming .
PSYCHOPHARMACOLOGY, 2008, 200 (03) :317-331
[9]  
Casey DE, 2004, J CLIN PSYCHIAT, V65, P4
[10]   Exposure-Response Analysis in Patients With Schizophrenia to Assess the Effect of Asenapine on QTc Prolongation [J].
Chapel, Sunny ;
Hutmacher, Matt M. ;
Haig, George ;
Bockbrader, Howard ;
de Greef, Rik ;
Preskorn, Sheldon H. ;
Lalonde, Richard L. .
JOURNAL OF CLINICAL PHARMACOLOGY, 2009, 49 (11) :1297-1308