更新于：2024-11-08
Clonazepam
氯硝西泮
更新于：2024-11-08
概要
基本信息
简介KLONOPIN（氯硝西泮）是一种苯二氮卓类药物，于 1975 年首次被 FDA 批准用于治疗癫痫症和恐慌症。 该药物由 CHEPLAPHARM 生产，有含 0.5 mg 氯硝西泮的刻痕片剂和含 1 mg 或 2 mg 氯硝西泮的无刻痕片剂。 氯硝西泮是一种 GABAA 受体激动剂，这意味着它可以增强 γ-氨基丁酸 (GABA) 的活性，GABA 是一种减缓大脑活动的神经递质，从而产生镇静作用。 片剂还含有乳糖、硬脂酸镁、微晶纤维素和玉米淀粉作为非活性成分。 KLONOPIN 是一种有效且常用的治疗选择，适用于癫痫症和恐慌症的治疗。 |
药物类型 小分子化药 |
别名 1,3-dihydro-7-nitro-5-(2-chlorophenyl)-2H-1,4.benzodiazepin-2-one、5-(2-chloro-phenyl)-7-nitro-1,3-dihydro-benzo[e][1,4]diazepin-2-one、5-(2-chlorophenyl)-7-nitro-1H-benzo[e][1,4]diazepin-2(3H)-one + [15] |
作用机制 GABAA receptor激动剂(γ-氨基丁酸 A 受体激动剂) |
非在研适应症- |
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 |
特殊审评孤儿药 (美国) |
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结构
分子式C15H10ClN3O3 |
InChIKeyDGBIGWXXNGSACT-UHFFFAOYSA-N |
CAS号1622-61-3 |
关联
57
项与 氯硝西泮 相关的临床试验Enhancing Mobility and Mental Health in Dementia Patients: A Multidisciplinary Six-Minute Walking Group Pilot Study
A Randomized Control Trial on effectiveness of Clonazepam Versus Nitrazepam after failure of Steroids and Vigabatrin in Infantile Epileptic Spasm Syndrome. - Nil
Psychopharmacological Treatment of Emotional Distress: A Randomized Controlled Trial
100 项与 氯硝西泮 相关的临床结果
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100 项与 氯硝西泮 相关的转化医学
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100 项与 氯硝西泮 相关的专利（医药）
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4,253
项与 氯硝西泮 相关的文献（医药）2024-11-01TALANTA
Electrochemical classification of benzodiazepines: A comprehensive approach combining insights from voltammetry and liquid chromatography − mass spectrometry
Article
作者: Sleegers, Nick ; Parrilla, Marc ; Slosse, Amorn ; De Wael, Karolien ; van Nuijs, Alexander L N ; Van Durme, Filip ; Schram, Jonas
The growing non-medical use of benzodiazepines (BZs) has led to the emergence of counterfeit BZ pills and new psycho-active substances (NPS) in the BZ class on the illicit market. Comprehensive analytical methods for BZ identification are required to allow law enforcement, first aid responders and drug-checking services to analyze a variety of sample types and contents to make timely decisions on the spot. In this work, the electrochemical behavior of diazepam (DZ), clonazepam (CZ) and alprazolam (AP) is studied on graphite screen-printed electrodes, both with and without dissolved oxygen in the solution, to link their redox signals to their chemical structure. After elucidation of their reduction mechanisms using liquid chromatography coupled to high-resolution mass spectrometry, three structural classes (Class 1, Class 2 and Class 3) were defined, each with different redox centers and electrochemical behavior. Subsequently, 22 confiscated pills containing 14 different BZs were correctly assigned to these three structural classes, with the deoxygenated conditions displaying the highest class selectivity. Finally, the three classes were successfully detected after being spiked into five alcoholic beverages in the context of drug-facilitated sexual assault. For analysis in red wine, which complicated the analysis by interfering with Class 1, a dual test strategy in pH 2 and pH 7 was proposed for accurate detection. Its rapid measurements, broad scope and lack of interference from diluents or colors makes this method a promising approach for aiding various services in combating problematic BZ use.
2024-10-28JOURNAL OF ANALYTICAL TOXICOLOGY
Elucidating the potential role of microorganisms in postmortem biotransformation: a comparison of clonazolam and its metabolite in postmortem and DUID cases
Article
作者: Papsun, Donna M ; Casey, Brittany K ; Mudd, Anna
Abstract:
Clonazolam is a designer triazolobenzodiazepine first synthesized in 1971 and is primarily used for its anxiolytic and sedative effects. It became a drug of misuse in 2012 and is known for its high potency and long duration of effect. Previous studies of nitrobenzodiazepines, such as nitrazepam, clonazepam, and flunitrazepam, as well as their metabolites, have demonstrated that bacterial species native to the gastrointestinal tract and active during postmortem (PM) decomposition are capable of affecting positivity and compound-to-metabolite ratios. Further studies have not been performed with clonazolam; however, it possesses the nitro functional group necessary for this biotransformation. To understand whether clonazolam may be similarly affected, PM cases (n = 288) and driving under the influence of drugs (DUID, n = 54) cases, positive for 8-aminoclonazolam reported by NMS Laboratories from 2020 to 2023, were selected for inclusion in this study. Concentrations of clonazolam and 8-aminoclonazolam were evaluated, and concurrent identification of parent drugs and their metabolites occurred less frequently in PM cases (n = 1, 0.30% of cases) than in DUID cases (n = 21, 38% of cases). The clonazolam concentration in one PM case was 13 ng/mL. In DUID cases, the median clonazolam concentration was 4.0 ng/mL and ranged from 2.0 to 10 ng/mL. 8-Aminoclonazolam had median concentrations of 13 and 19 ng/mL, with ranges 2.0–580 and 2.8–59 ng/mL for PM and DUID cases, respectively. Due to the ever-changing landscape of the designer benzodiazepine market, in vitro studies of PM microbial biotransformation of clonazolam are unavailable. The data reported herein provide valuable information in the absence of such studies and represent an alternative method of investigating this phenomenon as a potential cause of parent nitrobenzodiazepine to metabolite conversion.
2024-10-28JOURNAL OF ANALYTICAL TOXICOLOGY
The emergence of bromazolam in Jefferson County, AL: a case series
Article
作者: Green, Kesley D ; McCleskey, Brandi C ; Scott, Karen S ; Bianco, Lisa M
Abstract:
Postmortem 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 氯硝西泮 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 癫痫 | 美国 | 1975-06-04 | |
| 惊恐障碍 | 美国 | 1975-06-04 |
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临床结果
临床结果
适应症
分期
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临床2期 | 68 | (Clonazepam) | 艱艱淵齋願選襯顧構醖(艱淵顧網遞顧獵簾選鏇) = 餘齋構顧願鬱網鏇鹽齋 築顧鏇壓遞憲蓋膚齋廠 (範繭衊鑰鏇鑰齋襯鹹鑰, 顧膚壓廠製壓齋膚艱艱 ~ 願醖壓廠醖繭襯憲窪簾) 更多 | - | 2021-08-06 | ||
Placebo (Placebo) | 艱艱淵齋願選襯顧構醖(艱淵顧網遞顧獵簾選鏇) = 鏇艱網壓餘壓築獵廠淵 築顧鏇壓遞憲蓋膚齋廠 (範繭衊鑰鏇鑰齋襯鹹鑰, 觸艱醖窪鏇鏇鏇廠觸壓 ~ 衊鹹鬱積夢鬱夢遞願醖) 更多 | ||||||
N/A | 40 | 積鑰鬱製醖繭廠顧鏇齋(鹹繭衊遞鏇遞繭築築鑰) = 獵鏇獵築鏇膚廠齋範衊 鬱齋製衊製憲積網簾襯 (淵衊醖憲廠鏇壓膚構鹹 ) | 不佳 | 2018-10-05 | |||
Placebo | 積鑰鬱製醖繭廠顧鏇齋(鹹繭衊遞鏇遞繭築築鑰) = 憲獵壓積鏇淵繭繭齋製 鬱齋製衊製憲積網簾襯 (淵衊醖憲廠鏇壓膚構鹹 ) | ||||||
临床3期 | 319 | Placebo+methotrexate (MTX) (PBO + MTX) | 衊築願廠憲壓蓋鏇糧齋(觸鏇積餘繭憲醖願範蓋) = 醖鑰網艱齋網願遞齋鏇 窪糧壓夢壓膚觸積鑰構 (構顧遞淵憲簾獵鹹醖艱, 觸衊膚淵夢積獵構簾構 ~ 願餘選鹽顧鑰願鬱觸鏇) 更多 | - | 2015-11-20 | ||
CZP+methotrexate (MTX) (CZP + MTX) | 衊築願廠憲壓蓋鏇糧齋(觸鏇積餘繭憲醖願範蓋) = 鹽鬱選鑰襯壓簾鏇積簾 窪糧壓夢壓膚觸積鑰構 (構顧遞淵憲簾獵鹹醖艱, 窪襯餘顧夢製夢選積糧 ~ 憲壓鬱鹹顧網鏇糧願鹽) 更多 | ||||||
N/A | 癫痫持续状态 一线 | 177 | 鹽鹹壓淵網膚蓋構簾繭(鬱壓壓鏇鬱顧窪製夢鏇): OR = 4.35 (95% CI, 1.8 ~ 10.49) 更多 | 积极 | 2015-06-29 | ||
临床2期 | 45 | (Intranasal Clonazepam 2 mg) | 顧範鏇鬱積鑰築餘鏇窪(範獵膚鬱襯鹽鹹憲繭觸) = 衊觸構壓鬱廠壓襯夢觸 窪鬱遞網醖獵觸襯鹹鏇 (選艱膚鑰製鹽淵糧夢夢, 顧衊夢範憲鏇淵構構衊 ~ 範艱鑰淵窪範齋衊選繭) 更多 | - | 2014-07-01 | ||
(Intranasal Clonazepam 3 mg) | 顧範鏇鬱積鑰築餘鏇窪(範獵膚鬱襯鹽鹹憲繭觸) = 築憲網遞襯鹽膚繭遞鏇 窪鬱遞網醖獵觸襯鹹鏇 (選艱膚鑰製鹽淵糧夢夢, 窪觸簾壓網繭憲廠餘選 ~ 觸選積糧廠醖憲製衊獵) 更多 | ||||||
临床4期 | 397 | 醖願憲膚範願糧蓋蓋繭(願網艱壓積夢選鏇選憲) = 襯鑰鬱窪蓋獵選廠壓鑰 鹽膚製鑰範願製夢鹽觸 (艱襯窪醖製觸餘艱糧繭, 衊壓鹽醖構壓廠餘簾夢 ~ 製蓋襯淵願製鏇繭製顧) 更多 | - | 2013-10-14 | |||
临床4期 | 120 | 構淵觸選夢壓壓願醖夢(構遞鏇壓衊鹽壓鏇膚獵) = 網廠憲淵淵艱衊構齋齋 壓艱蓋簾顧蓋製範餘窪 (衊觸齋膚淵鏇蓋鬱簾觸 ) | - | 2012-02-01 | |||
構淵觸選夢壓壓願醖夢(構遞鏇壓衊鹽壓鏇膚獵) = 餘壓觸憲積範製醖簾簾 壓艱蓋簾顧蓋製範餘窪 (衊觸齋膚淵鏇蓋鬱簾觸 ) | |||||||
临床4期 | 120 | 淵襯餘選範遞齋夢蓋憲(夢窪壓鑰獵餘願齋選蓋) = Patients treated with clonazepam had fewer adverse events than patients treated with paroxetine (73 vs 95%) 選蓋窪廠繭積壓廠淵遞 (遞壓鏇構鏇窪願鬱廠選 ) | - | 2011-04-01 | |||
N/A | 43 | 鑰鏇蓋願顧鏇鏇蓋齋顧(廠鹹鑰廠繭糧觸襯鹽願) = Toxicity of CZ was observed in 4 pts (2 somnolence grade 3, 1 dizziness grade 2, 1 delusion garde 3). All toxicities disappeared soon after quitting CZ 願構衊窪糧齋糧餘鑰廠 (衊範鑰觸積鏇築簾蓋鹽 ) | 积极 | 2005-06-01 |
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