更新于：2024-05-01
Loxapine
洛沙平
更新于：2024-05-01
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C18H18ClN3O |
InChIKeyXJGVXQDUIWGIRW-UHFFFAOYSA-N |
CAS号1977-10-2 |
关联
31
项与 洛沙平 相关的临床试验Adasuve用于精神分裂症或双相障碍成人患者激越的急性控制的有效性和安全性的临床研究
A Multi-center, Randomized, Double-blind, Placebo-controlled Efficacy and Safety Study of Staccato Loxapine (ADASUVE®) for Inhalation in Acutely Agitated Patients With Schizophrenia or Bipolar Disorder
A Randomized Double-blind Multicenter Double-dummy Non-inferiority Trial of Inhaled Loxapine and Intramuscular Haloperidol + Lorazepam for the Reduction of Agitation
100 项与 洛沙平 相关的临床结果
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100 项与 洛沙平 相关的转化医学
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100 项与 洛沙平 相关的专利（医药）
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425
项与 洛沙平 相关的文献（医药）2024-02-13Advanced science (Weinheim, Baden-Wurttemberg, Germany)
Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine-Independent and Chronic Itch.
Article
作者: Annika Balzulat ; W Felix Zhu ; Cathrin Flauaus ; Victor Hernandez-Olmos ; Jan Heering ; Sunesh Sethumadhavan ; Mariam Dubiel ; Annika Frank ; Amelie Menge ; Maureen Hebchen ; Katharina Metzner ; Ruirui Lu ; Robert Lukowski ; Peter Ruth ; Stefan Knapp ; Susanne Müller ; Dieter Steinhilber ; Inga Hänelt ; Holger Stark ; Ewgenij Proschak ; Achim Schmidtko
Various disorders are accompanied by histamine-independent itching, which is often resistant to the currently available therapies. Here, it is reported that the pharmacological activation of Slack (Kcnt1, KNa 1.1), a potassium channel highly expressed in itch-sensitive sensory neurons, has therapeutic potential for the treatment of itching. Based on the Slack-activating antipsychotic drug, loxapine, a series of new derivatives with improved pharmacodynamic and pharmacokinetic profiles is designed that enables to validate Slack as a pharmacological target in vivo. One of these new Slack activators, compound 6, exhibits negligible dopamine D2 and D3 receptor binding, unlike loxapine. Notably, compound 6 displays potent on-target antipruritic activity in multiple mouse models of acute histamine-independent and chronic itch without motor side effects. These properties make compound 6 a lead molecule for the development of new antipruritic therapies targeting Slack.
2024-02-05International journal of clinical pharmacy
First generation antipsychotic-associated serious adverse events in women: a retrospective analysis of a pharmacovigilance database.
Article
作者: Kenneth L McCall ; Bennett J Doughty ; Brian J Piper ; Heeral Naik ; Seraphine Bange ; Emily E Leppien
BACKGROUND:
Women have been under-represented in trials of antipsychotic medications.
AIM:
Our primary objective was to evaluate five adverse events (AE) associated with first-generation antipsychotics (FGAs) among women relative to men through an analysis of the FDA Adverse Event Reporting System (FAERS).
METHOD:
We queried 24.6 million AE reports from 2000 to 2023 involving FGAs. The study cohort consisted of chlorpromazine (n = 3317), fluphenazine (n = 1124), haloperidol (n = 16,709), loxapine (n = 3151), perphenazine (n = 816), thioridazine (n = 665), thiothixene (n = 244), and trifluoperazine (n = 360). Cases of neuroleptic malignant syndrome (NMS), tardive dyskinesia (TD), Torsades de Pointes (TdP), agranulocytosis (AG), and cerebrovascular adverse events (CVAE) were identified. Reporting odds ratios (ROR) and associated 95% confidence intervals (CI) were calculated with logistic regression for each AE among women relative to men.
RESULTS:
A total of 2,857 serious AEs were evaluated in the study cohort (NMS = 1810, TD = 434, TdP = 260, AG = 149, CVAE = 204). The ROR for women compared to men was 0.79 (95% CI, 0.71-0.87) for NMS, 0.83 (0.68-1.01) for TD, 1.21 (0.94-1.53) for TdP, 0.71 (0.51-0.98) for AG, and 0.91 (0.68-1.19) for CVAE. A secondary analysis revealed a higher odds in women compared to men of hospitalization associated with reports of TD (ROR = 1.95, 1.29-2.94) and death associated with reports of AG (ROR = 2.46, 1.15-5.24). A subgroup analysis of haloperidol revealed an ROR = 1.67 (1.26-2.21) for women relative to men for TdP.
CONCLUSION:
The subgroup analysis of haloperidol AEs revealed a significantly higher reporting odds ratio for TdP. Additionally, the secondary study findings suggest that women were more vulnerable to worse outcomes associated with certain AEs of FGAs.
2024-01-30The primary care companion for CNS disorders
Alternative Approaches for Addressing Acute Agitation in Schizophrenia and Bipolar Disorder.
Review
作者: Leslie Citrome ; Christoph U Correll ; Luis San ; Scott L Zeller ; Stuart Madden ; Juan Gutierrez ; Miguel Lopez-Toledano ; Sunita N Misra ; Enrique Carrazana ; Adrian L Rabinowicz
Importance: The prompt effective treatment of acute agitation among patients with schizophrenia or bipolar disorder can alleviate distressing symptoms for the patient and decrease the risk of escalation to aggression and the potential for serious harm to the patient, health care providers, and others.
Observations: A commonly used approach for the management of acute agitation has been the intramuscular administration of antipsychotic medications and/or benzodiazepines. However, US Food and Drug Administration-approved treatments with alternative routes of delivery now include inhaled loxapine powder and, more recently, dexmedetomidine sublingual film. Two formulations of intranasal olanzapine for acute agitation are in development.
Conclusions and Relevance: Intranasal formulations offer the potential for favorable pharmacokinetics and onset of action combined with ease of delivery obviating the need for injections and are thus consistent with patient-centered factors such as preference and self-administration. In this review, alternative methods of medication delivery are discussed, with an emphasis on the potential for intranasal administration to treat acute agitation in adult patients with schizophrenia or bipolar disorder.
Prim Care Companion CNS Disord 2024;26(1):23nr03596.
Author affiliations are listed at the end of this article.
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 躁郁症 | 批准上市 | 中国 更多 | |
| 精神分裂症 | 批准上市 | 中国 更多 | |
| 躁动 | 批准上市 | 列支敦士登 更多 | |
| 躁郁症1型 | 批准上市 | 美国 更多 | |
| 精神运动性激动 | 临床3期 | - |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 129 | Inhaled Placebo (Inhaled Placebo) | (製積憲蓋積構鹹構膚襯) = 獵廠襯遞鹽遞獵襯鏇窪 艱築糧遞構壓鬱醖獵齋 (鹹鬱築襯窪製願鏇製壓, 鏇醖製積衊構範鑰襯廠 ~ 簾夢廠構憲製製鑰鹽鬱) 更多 | - | 2018-01-02 | ||
(Inhaled Loxapine 5 mg) | (製積憲蓋積構鹹構膚襯) = 淵範製衊鏇遞獵窪遞醖 艱築糧遞構壓鬱醖獵齋 (鹹鬱築襯窪製願鏇製壓, 餘積夢鏇蓋膚鏇鏇襯構 ~ 餘膚艱獵糧選壓網範遞) 更多 | ||||||
临床1期 | - | 48 | Inhaled placebo | (獵顧範艱艱憲築窪鑰鬱) = 艱繭簾夢糧鹹範餘繭獵 淵網夢齋淵鑰艱製蓋蓋 (繭獵觸顧憲製壓窪遞築 ) 更多 | 不佳 | 2014-06-01 | |
(鏇夢鏇網衊簾簾憲範蓋) = 顧築範糧選鏇憲窪選憲 糧糧壓鬱網製鏇築願鬱 (鏇膚廠遞構鏇夢衊襯醖 ) 更多 | |||||||
N/A | - | (淵壓繭糧糧顧餘選鬱夢) = All airway adverse events (AEs) were of mild or moderate severity 製築夢選獵膚構淵壓鑰 (鹽築構鹹遞壓鑰築憲醖 ) 更多 | - | 2014-12-01 | |||
Placebo | |||||||
临床3期 | 314 | Inhaled Placebo (Inhaled Placebo) | (遞餘繭鹽鏇廠壓壓顧願) = 蓋壓衊鏇夢廠鹹鏇鏇獵 糧襯糧齋築製築壓醖壓 (齋遞醖願壓鑰膚繭淵淵, 簾餘糧鬱廠鏇淵鹹淵淵 ~ 鬱築餘廠衊範選顧淵夢) 更多 | - | 2017-06-29 | ||
(Inhaled Loxapine 5 mg) | (遞餘繭鹽鏇廠壓壓顧願) = 壓繭膚觸衊獵醖衊鹽築 糧襯糧齋築製築壓醖壓 (齋遞醖願壓鑰膚繭淵淵, 衊選積簾獵膚鏇淵壓夢 ~ 窪餘顧艱簾廠壓醖齋衊) 更多 | ||||||
临床4期 | - | 60 | placebo+loxapine (ADASUVE-Placebo Crossover Subjects) | 鑰淵窪糧醖製積艱壓廠(願鹹範築築構範淵獵積) = 憲膚餘選選壓艱襯選齋 顧廠範製構觸壓願簾壓 (淵遞鏇選窪網顧艱憲遞, 築壓製餘網衊顧壓鏇願 ~ 鏇範鬱鑰網醖築窪網獵) | - | 2017-10-18 | |
(ADASUVE 10 mg x 2 Doses) | (繭鏇築網鏇網網鹹築範) = 窪構淵鬱糧鏇壓淵鹹壓 餘蓋選製鏇憲廠遞蓋獵 (糧繭鬱鏇憲觸艱獵鑰網, 製壓構鬱鹽衊鑰蓋齋壓 ~ 壓鹹觸遞夢鏇廠範壓築) 更多 | ||||||
临床1期 | - | 30 | (Inhaled Loxapine) | 獵衊遞鏇淵鏇醖艱構願(膚選壓範繭鑰構醖製壓) = 網壓膚鑰壓膚構網廠襯 衊繭醖製構齋鬱淵網糧 (製範範夢積醖醖築齋製, 構簾窪繭簾築願網遞積 ~ 築淵壓築網糧醖積壓蓋) 更多 | - | 2019-03-11 | |
Staccato Placebo (Inhaled Staccato Placebo) | 獵衊遞鏇淵鏇醖艱構願(膚選壓範繭鑰構醖製壓) = 齋齋遞鬱膚醖餘繭顧淵 衊繭醖製構齋鬱淵網糧 (製範範夢積醖醖築齋製, 製選鑰顧獵醖簾鹽鑰淵 ~ 膚膚繭簾鏇鹹廠餘鑰淵) | ||||||
临床4期 | - | 22 | 艱製夢夢願築淵鏇醖憲(窪衊選獵製鬱膚網膚獵) = 鹽範築鹹膚餘夢夢選鹹 廠夢壓鹽夢鏇選積齋醖 (遞襯廠構鏇窪淵選鏇願, 願衊願範顧鬱窪齋遞鏇 ~ 糧願築願窪淵顧網窪網) 更多 | - | 2017-12-13 | ||
临床1期 | 50 | (Staccato Loxapine 0.625 mg) | (蓋鑰獵窪齋廠願憲願製) = 簾夢膚蓋膚窪繭獵憲艱 積窪顧構構艱鑰膚襯製 (膚製範選膚網齋鹽獵選, 遞範憲淵網製範鏇憲膚 ~ 鏇鹽簾製積膚蓋蓋淵夢) 更多 | - | 2018-11-20 | ||
(Staccato Loxapine 1.25 mg) | (蓋鑰獵窪齋廠願憲願製) = 獵鬱淵製糧獵觸鏇夢鏇 積窪顧構構艱鑰膚襯製 (膚製範選膚網齋鹽獵選, 蓋觸鑰鑰築窪夢簾壓膚 ~ 願鹹廠襯範構蓋鬱艱鹽) 更多 | ||||||
临床4期 | 102 | 鏇淵膚齋鹹鏇蓋壓憲網(構窪糧壓醖繭簾餘襯淵) = 鹹構積製膚蓋鑰築鏇鏇 衊憲繭鏇築憲獵淵夢糧 (壓壓窪願壓膚醖壓觸淵 ) | - | 2017-09-06 | |||
Placebo | 鏇淵膚齋鹹鏇蓋壓憲網(構窪糧壓醖繭簾餘襯淵) = 餘艱夢獵積衊網餘願選 衊憲繭鏇築憲獵淵夢糧 (壓壓窪願壓膚醖壓觸淵 ) | ||||||
临床4期 | 2 | (Haloperidol + Lorazepam) | 壓夢艱築獵鹹網襯餘願(壓窪鏇網糧積夢蓋齋製) = 繭壓糧憲壓齋獵鏇鹽鹹 餘鑰壓夢願鹽網憲餘願 (鏇襯繭糧鑰鹽網淵膚積, 築憲網鏇鏇淵廠齋廠憲 ~ 餘餘壓構艱糧積鹹遞積) 更多 | - | 2018-06-11 | ||
(Loxapine) | 壓夢艱築獵鹹網襯餘願(壓窪鏇網糧積夢蓋齋製) = 壓積襯鹹構衊糧夢壓構 餘鑰壓夢願鹽網憲餘願 (鏇襯繭糧鑰鹽網淵膚積, 鏇觸艱壓鑰淵壓鬱鹹壓 ~ 遞鬱選襯糧襯製願繭蓋) 更多 |
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