Iloperidone for the Treatment of Schizophrenia

Marino, Jehan; Caballero, Joshua

doi:10.1345/aph.1m603

Cited by 26 publications

(6 citation statements)

References 16 publications

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“…These pharmacological properties of risperidone have been shown in separate studies that compared their properties with haloperidol (Cohen 1994; He and Richardson 1995). Iloperidone can also be an efficient antipsychotic agent in schizophrenia treatment (Marino and Caballero 2010). In fact, iloperidone was more effective than other benzisoxazole antipsychotics in antagonizing climbing behavior in mice (Jain 2000).…”

Section: Contribution Of Structure To Therapeutic Actionsmentioning

confidence: 99%

Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects

Jafari

Fernandez

Huang

2011

Journal of Neurochemistry

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Antipsychotic drugs have various neuropharmacological properties as a result of their structural diversity. Despite their therapeutic benefits, most of the prescribed atypical antipsychotics can induce severe side effects, including weight gain, type II diabetes mellitus, and cardiovascular diseases. Among the developed atypical antipsychotic agents, tetracyclic dibenzodiazepine and thienobenzodiazepine compounds, particularly clozapine and olanzapine, are associated with the greatest weight gain and metabolic disturbances. However, the unique chemical structure of these compounds causes the low risk of side effects reported for typical antipsychotics (e.g. extrapyramidal symptoms and tardive dyskinesia). This report reviews the recent discovery of the potential role of the chemical structure of antipsychotics in their therapeutic properties and metabolic disturbances. By developing structureactivity relationship studies for atypical antipsychotics, we will improve our understanding of the structural modifications of these chemical classes that lead to reduced weight gain, which will be an invaluable step toward the discovery of the next generation of atypical antipsychotics. In this review, we suggest that a novel dibenzodiazepine or thienobenzodiazepine antipsychotic drug with lower affinity for H 1 receptors may significantly advance schizophrenia therapy.

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Section: Contribution Of Structure To Therapeutic Actionsmentioning

confidence: 99%

Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects

Jafari

Fernandez

Huang

2011

Journal of Neurochemistry

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“…In Kane et al (2008) akathesia rates were negligible when compared to haloperidol in a three-week trial. Any changes in QTc intervals were small, and resembled that of risperidone, as did weight gain changes; both these affects appeared to be dose dependent (Marino & Caballero, 2010). In a four-week trial where iloperodone was compared to ziprazadone treatment, "Iloperidone was associated with lower rates of many adverse events (AEs) that are particularly troublesome with antipsychotics, including sedation, somnolence, extrapyramidal symptoms, akathesia, agitation, and restlessness; iloperidone was associated with higher rates of weight gain, tachycardia, orthostatic hypotension, dizziness (Cutler, Kalali, Weiden, Hamilton, & Wolfgang, 2008, p. S20).…”

Section: Adverse Experiences/side Effect Profilesmentioning

confidence: 93%

Atypical Antipsychotics: The Two New Arrivals

Roman

2011

Issues in Mental Health Nursing

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“…Consistent with atypical antipsychotics, iloperidone exhibits high affinity for 5-HT 2 and D 2 receptors [12]. Iloperidone exhibits antipsychotic efficacy; furthermore some preclinical evidence suggests that it may ameliorate negative symptoms (see review by [13]). Bifeprunox, similarly to aripiprazole, is a partial D 2 receptor agonist while also exhibiting little efficacy at 5-HT 2A , 5-HT 2C , or noradrenergic receptors [14].…”

Section: Overview Of the Marketmentioning

confidence: 99%

Evaluation of the clinical efficacy of asenapine in schizophrenia

Minassian¹,

Young²

2010

Expert Opinion on Pharmacotherapy

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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 United States. 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. Pre-clinical 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: a) causes a reduction in symptoms of schizophrenia; b) has a side-effect profile minimizing extrapyramidal symptoms, weight gain, and cardiac effects; and c) affects negative and/or cognitive symptoms.Take home message-Asenapine is a recently approved agent with an acceptable cardiometabolic profile that exhibits similar efficacy as other antipsychotic medications, primarily on positive symptoms of schizophrenia. Relatively less weight gain compared to 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 further investigation.

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Iloperidone for the Treatment of Schizophrenia

Cited by 26 publications

References 16 publications

Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects

Structural contributions of antipsychotic drugs to their therapeutic profiles and metabolic side effects

Atypical Antipsychotics: The Two New Arrivals

Evaluation of the clinical efficacy of asenapine in schizophrenia

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