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
[11]   Citation bias in reported smoking prevalence in people with schizophrenia [J].
Chapman, Simon ;
Ragg, Mark ;
McGeechan, Kevin .
AUSTRALIAN AND NEW ZEALAND JOURNAL OF PSYCHIATRY, 2009, 43 (03) :277-282
[12]   Repeated effects of asenapine on adrenergic and cholinergic muscarinic receptors [J].
Choi, Yong Kee ;
Wong, Erik H. F. ;
Henry, Brian ;
Shahid, Mohammed ;
Tarazi, Frank I. .
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY, 2010, 13 (03) :405-410
[13]   Asenapine for schizophrenia and bipolar disorder: a review of the efficacy and safety profile for this newly approved sublingually absorbed second-generation antipsychotic [J].
Citrome, L. .
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2009, 63 (12) :1762-1784
[14]   Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT1A receptors expressed in HeLa cells [J].
Cosi, C ;
Koek, W .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2001, 433 (01) :55-62
[15]   ACTIONS OF ORG-5222 AS A NOVEL PSYCHOTROPIC AGENT [J].
COSTALL, B ;
DOMENEY, AM ;
KELLY, ME ;
NAYLOR, RJ ;
TOMKINS, DM .
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1990, 35 (03) :607-615
[16]   Long-acting risperidone improves negative symptoms in stable psychotic patients [J].
Curtis, V. A. ;
Katsafouros, K. ;
Moeller, H.-J. ;
Medori, R. ;
Sacchetti, E. .
JOURNAL OF PSYCHOPHARMACOLOGY, 2008, 22 (03) :254-261
[17]   TREATMENT OF SCHIZOPHRENIA - A CLINICAL AND PRECLINICAL EVALUATION OF NEUROLEPTIC DRUGS [J].
ELLENBROEK, BA .
PHARMACOLOGY & THERAPEUTICS, 1993, 57 (01) :1-78
[18]   Quality of life and tolerability in patients with schizophrenia taking atypical antipsychotics [J].
Fleming, K. ;
Potkin, S. G. ;
Binneman, B. ;
Keller, D. ;
Alphs, L. ;
Panagides, J. .
EUROPEAN NEUROPSYCHOPHARMACOLOGY, 2007, 17 :S466-S467
[19]   Asenapine, a novel psychopharmacologic agent:: preclinical evidence for clinical effects in schizophrenia [J].
Franberg, Olivia ;
Wiker, Charlotte ;
Marcus, Monica M. ;
Konradsson, Asa ;
Jardemark, Kent ;
Schilstrom, Bjorn ;
Shahid, Mohammed ;
Wong, Erik H. F. ;
Svensson, Torgny H. .
PSYCHOPHARMACOLOGY, 2008, 196 (03) :417-429
[20]   Modeling and Simulation of the Time Course of Asenapine Exposure Response and Dropout Patterns in Acute Schizophrenia [J].
Friberg, L. E. ;
de Greef, R. ;
Kerbusch, T. ;
Karlsson, M. O. .
CLINICAL PHARMACOLOGY & THERAPEUTICS, 2009, 86 (01) :84-91