依替唑仑(Etizolam) - 药物靶点：GABAA receptor_在研适应症：焦虑症，抑郁症，入睡和睡眠障碍_专利_临床

概要

基本信息

药物类型

小分子化药

别名

4-(o-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine、Etizolam (JP17/INN)

+ [5]

靶点

GABAA receptor

作用机制

GABAA receptor激动剂(γ-氨基丁酸 A 受体激动剂)

治疗领域

神经系统疾病其他疾病

在研适应症

焦虑症抑郁症入睡和睡眠障碍

非在研适应症-

原研机构

Mitsubishi Tanabe Pharma Factory Ltd.

在研机构

Mitsubishi Tanabe Pharma Factory Ltd.

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (1983-01-01),

焦虑症抑郁症入睡和睡眠障碍

最高研发阶段(中国)-

特殊审评-

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结构

分子式C17H15ClN4S

InChIKeyVMZUTJCNQWMAGF-UHFFFAOYSA-N

CAS号40054-69-1

关联

4

项与依替唑仑相关的临床试验

CTRI/2021/09/036486 / CompletedN/AIIT

Comparative evaluation of Etizolam and Music distraction on success of Inferior Alveolar Nerve Block in mandibular molars with symptomatic irreversible pulpitis

开始日期2021-09-20

申办/合作机构-

CTRI/2020/08/026974 / Completed临床4期

An Open Label, Multicentre, Post-Marketing Surveillance study to Monitor the Safety and Efficacy of Combination Therapy of Escitalopram 5 mg/10 mg and Etizolam 0.5 mg in Subjects with Major Depressive Disorder with Associated Anxiety in Regular Practice

开始日期2020-08-14

申办/合作机构-

JPRN-UMIN000011279 / Completed

Independent study: Researching drug-drug interaction bitween etizolam and itraconazole - Independent clinical study (University of Tokyo)

开始日期2013-03-25

申办/合作机构-

100 项与依替唑仑相关的临床结果

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100 项与依替唑仑相关的转化医学

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100 项与依替唑仑相关的专利（医药）

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272

项与依替唑仑相关的文献（医药）

2024-12-01·Psychiatry and Clinical Neurosciences Reports

A case report of benzodiazepine withdrawal delirium due to accidental discontinuation of benzodiazepines in cancer perioperative period

Article

作者: Yamaguchi, Junji ; Nakahara, Rika ; Terada, Tatsuto ; Wada, Saho ; Sadahiro, Ryoichi ; Matsuoka, Hiromichi ; Nishikawa, Eri

AbstractBackgroundBenzodiazepines are known for their possible risk of delirium, especially when administered to older adults or during the perioperative period. However, the risk of sudden discontinuation of benzodiazepines and subsequent withdrawal delirium seems to be underappreciated and not properly recognized in cancer treatment, even among healthcare workers.Case PresentationA man in his late 70s was diagnosed with rectal cancer and had a history of taking etizolam and alprazolam for over 15 years. After hospitalization for cancer, these benzodiazepines were discontinued abruptly 2 days before the surgery, due to concerns about benzodiazepine‐related delirium. After half a day, severe benzodiazepine withdrawal symptoms, such as disorientation, agitation, tachycardia, diaphoresis, and muscle twitching, appeared. The patient was diagnosed with delirium associated with benzodiazepine withdrawal, and his symptoms subsided soon after re‐administration of benzodiazepines. Despite development of mild postoperative delirium, the operation was performed safely.ConclusionThe rapid and abrupt discontinuation of benzodiazepines before cancer surgery could impose a high risk of benzodiazepine withdrawal delirium in patients, which makes the management of psychiatric symptoms in the perioperative period more complex and difficult. We believe that it is necessary to highlight the risks of withdrawal delirium and abrupt benzodiazepine discontinuation in cancer treatment. Moreover, re‐education on this topic is essential for healthcare workers.

2024-11-15·Journal of Analytical Toxicology

Deaths involving novel benzodiazepines in Victoria, Australia from 2018 to 2022

Article

作者: Di Rago, Matthew ; Glowacki, Linda ; Crump, Kerryn ; Gerostamoulos, Dimitri ; Joubert, Samantha ; Drummer, Olaf H ; Castle, Jared W

AbstractNovel benzodiazepine (NBz) detections in Victorian coronial cases started early in 2018 and have continued to increase in number and type up to December 2022. The 11 different NBz detections included etizolam (n = 82), flualprazolam (n = 43), clonazolam or 8-aminoclonazolam (n = 30), bromazolam (n = 15), clobromazolam (n = 13), phenazepam (n = 13), flubromazolam (n = 12), flubromazepam (n = 8), desalkylflurazepam (n = 6), diclazepam (n = 2), and estazolam (n = 1). The pattern of detections varied over the 5-year period, with different compounds appearing over different time frames. The most recent NBz to appear were bromazolam, clobromazolam, flubromazepam, and phenazepam, whereas etizolam had been seen regularly in case work since 2018. Of the total 133 deaths, 95 were considered drug-related deaths by forensic pathologists with at least one additional CNS depressant also present capable of contributing to death. All deaths involved other (non-benzodiazepine) CNS active drugs, although many involved multiple NBz, with five or more different benzodiazepines detected in eight cases.

2024-10-28·Journal of Analytical Toxicology

The emergence of bromazolam in Jefferson County, AL: a case series

Article

作者: McCleskey, Brandi C ; Green, Kesley D ; Scott, Karen S ; Bianco, Lisa M

AbstractPostmortem toxicology is an ever-changing landscape presenting challenges for toxicologists and medical examiners. Trends can vary for certain benzodiazepines. While diazepam use tends to remain constant, alprazolam and clonazepam ebb and flow depending on prescription trends and street popularity. Novel benzodiazepines like etizolam vary in casework depending on legal restrictions and black market availability. In May 2022, the first case of the designer benzodiazepine, bromazolam, was detected in Jefferson County Coroner/Medical Examiner’s Office casework. Between then and December 2023, an additional nine cases have been observed. Bromazolam is the brominated analog of the low-dose benzodiazepine, alprazolam, and is likely similar in potency. As bromazolam is a potent benzodiazepine, low concentrations of this novel drug are likely to contribute to central nervous system depression in opioid overdose cases. We present 10 cases in which bromazolam was detected in postmortem samples at the University of Alabama at Birmingham toxicology laboratory. The decedents ranged in age from 20 to 41 years. Most of the decedents were White (n = 8; 80%) and male (n = 7; 70%). Bromazolam concentrations ranged from 21 to 3220 ng/mL (mean 401 ng/mL). All but one case were polydrug, and all deaths were related to drug toxicity. Fentanyl was detected in 8 of the 10 decedents, with concentrations ranging from <2.5 to 97 ng/mL (mean 30 ng/mL). Additional drugs detected were methamphetamine, ethanol, oxycodone, methadone, cocaine, amphetamine, morphine, and diphenhydramine. While all manners of death were ruled as accidental, bromazolam was included in the cause of death statements in 9 of the 10 cases. Capturing important emerging drug trends in the death certificate is critical to help inform public health and medical colleagues for preventive measures and treatment in the continued drug epidemic.

100 项与依替唑仑相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01514	依替唑仑	N05BA19	DB09166

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
焦虑症	日本	Mitsubishi Tanabe Pharma Factory Ltd.	1983-01-01
抑郁症	日本	Mitsubishi Tanabe Pharma Factory Ltd.	1983-01-01
入睡和睡眠障碍	日本	Mitsubishi Tanabe Pharma Factory Ltd.	1983-01-01