更新于：2024-11-04
Doxepin hydrochloride
盐酸多塞平
更新于：2024-11-04
概要
基本信息
简介多塞平是一种小分子药物，作为一种有效的治疗剂，靶向去甲肾上腺素转运蛋白 (NET) 和血清素转运蛋白亚型 5 (SERT-5)。通过抑制大脑中去甲肾上腺素和 5-羟色胺再摄取的双重作用，多塞平起到了出色的抗抑郁药的作用，导致突触间隙内这些神经递质的水平升高。这种神经化学改变有助于稳定情绪、减轻焦虑和提高睡眠质量，从而产生许多好处。自 1969 年 9 月问世以来，多塞平一直是那些与抑郁症、焦虑症和失眠症作斗争的人们的希望灯塔。尽管如此，必须认识到多塞平会引起一些不良反应，包括但不限于嗜睡、口干、便秘和体重增加，甚至可能与其他药物相互作用。因此，明智的做法是在医疗保健专家的指导下谨慎使用多塞平。 |
药物类型 小分子化药 |
别名 Doxepin、Doxepin hydrochloride (USP)、Doxepin Hydrochloride Cream + [16] |
作用机制 NET抑制剂(去甲肾上腺素转运蛋白抑制剂)、5-羟色胺重摄取抑制剂 |
非在研适应症- |
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- |
登录后查看时间轴
结构
分子式C19H22ClNO |
InChIKeyMHNSPTUQQIYJOT-UHFFFAOYSA-N |
CAS号1229-29-4 |
关联
33
项与 盐酸多塞平 相关的临床试验评价盐酸多塞平口颊膜治疗失眠障碍患者疗效和安全性的多中心Ⅲ期临床研究
- P23-01
A Triple-Blinded, Randomized, Placebo-Controlled Trial to Examine the Safety and Efficacy of Doxepin Rinse in Managing Oral Mucositis in Children Older than 7 Years of Age Receiving Chemotherapy
100 项与 盐酸多塞平 相关的临床结果
登录后查看更多信息
100 项与 盐酸多塞平 相关的转化医学
登录后查看更多信息
100 项与 盐酸多塞平 相关的专利（医药）
登录后查看更多信息
1,357
项与 盐酸多塞平 相关的文献（医药）2024-09-01CLINICAL TOXICOLOGY
Evolving trends of pharmaceutical poisonings associated with QRS complex prolongation
Article
作者: Burns, Michele M. ; Simpson, Michael D. ; Tang, Katherine B.
INTRODUCTION:
Tricyclic antidepressants often cause drug-induced QRS complex prolongation in overdose but are now less commonly prescribed. We sought to determine, among a contemporary cohort of patients, the pharmaceuticals independently associated with QRS complex prolongation in acute overdose.
METHODS:
We performed secondary analysis of data from the Toxicology Investigators Consortium (ToxIC) Core Registry. We included adult patients presenting from January 2016 through March 2023 with acute or acute-on-chronic pharmaceutical exposures. The primary outcome was QRS complex prolongation >0.12 s. Secondary outcomes included cardiac arrest, death, ventricular dysrhythmia, intensive care unit admission, initiation of vasopressors, and treatment with sodium bicarbonate. We used a multivariable logistic regression model with QRS complex prolongation as the outcome and individual pharmaceuticals of interest as independent variables. We assessed yearly trends of the contribution of relevant pharmaceuticals to QRS complex prolongation since 2016.
RESULTS:
Of 11,945 patients in the total cohort (median age 37 years, 6,652 [55.7%] female), 366 (3.1%) developed QRS complex prolongation. Of 9,417 patients included in the model, 290 (3.1%) developed QRS complex prolongation. Amitriptyline, nortriptyline, doxepin, imipramine, noxiptiline, bupropion, flecainide, carvedilol, propranolol, diphenhydramine, and lamotrigine poisonings were independent predictors of QRS complex prolongation. Flecainide poisoning conferred the greatest odds of QRS complex prolongation (OR 574.1; 95% CI: 88.3-12,747). The contribution of tricyclic antidepressants to QRS complex prolongation decreased from 38.8% to 17.6% of all patients with QRS complex prolongation from 2016 to 2022. In 2022, the proportion of QRS complex prolongation from diphenhydramine (20.6%) surpassed that of tricyclic antidepressants.
DISCUSSION:
This study provides insights into contemporary pharmaceutical poisoning associated with QRS complex prolongation. Tricyclic antidepressants remain clinically relevant exposures but are no longer the most common cause of drug-induced QRS complex prolongation.
CONCLUSIONS:
Bupropion, diphenhydramine, and antidysrhythmics are increasingly common causes of QRS complex prolongation, each associated with numerous severe outcomes in poisoning. Greater safety measures to protect patients from cardiovascular toxicity from these pharmaceuticals are warranted.
2024-09-01JOURNAL OF MOLECULAR RECOGNITION
Binding characteristics of the doxepin E/Z‐isomers to the histamine H1 receptor revealed by receptor‐bound ligand analysis and molecular dynamics study
Article
作者: Kaneko, Hiroto ; Shiroishi, Mitsunori ; Nakamura, Ryota ; Kawai, Shinnosuke ; Korenaga, Ryunosuke ; Ando, Tadashi
Abstract:
Doxepin is an antihistamine and tricyclic antidepressant that binds to the histamine H1 receptor (H1R) with high affinity. Doxepin is an 85:15 mixture of the E‐ and Z‐isomers. The Z‐isomer is well known to be more effective than the E‐isomer, whereas based on the crystal structure of the H1R/doxepin complex, the hydroxyl group of Thr1123.37 is close enough to form a hydrogen bond with the oxygen atom of the E‐isomer. The detailed binding characteristics and reasons for the differences remain unclear. In this study, we analyzed doxepin isomers bound to the receptor following extraction from a purified H1R protein complexed with doxepin. The ratio of the E‐ and Z‐isomers bound to wild‐type (WT) H1R was 55:45, indicating that the Z‐isomer was bound to WT H1R with an approximately 5.2‐fold higher affinity than the E‐isomer. For the T1123.37V mutant, the E/Z ratio was 89:11, indicating that both isomers have similar affinities. Free energy calculations using molecular dynamics (MD) simulations also reproduced the experimental results of the relative binding free energy differences between the isomers for WT and T1123.37V. Furthermore, MD simulations revealed that the hydroxyl group of T1123.37 did not form hydrogen bonds with the E‐isomer, but with the adjacent residues in the binding pocket. Analysis of the receptor‐bound doxepin and MD simulations suggested that the hydroxyl group of T1123.37 contributes to the formation of a chemical environment in the binding pocket, which is slightly more favorable for the Z‐isomer without hydrogen bonding with doxepin.
2024-09-01Current molecular medicine
Untargeted Metabolomic Analyses of Body Fluids to Differentiate
TBI DOC and NTBI DOC
Article
作者: Lu, Hezhen ; Guo, Zhengguang ; Xu, Long ; Sun, Haidan ; Niu, Xia ; Chen, Xueling ; He, Jianghong ; Geng, Xiaoli ; Lan, Ying ; Qi, Feng ; Zhuang, Yutong ; Wang, Aiwei ; Ge, Qianqian ; Sun, Jiameng ; Xiao, Xiaoping ; Sun, Wei ; Liu, Xiaoyan
Objective::
To investigate the metabolomic differences between Traumatic
brain injury (TBI) disorder of consciousness (DOC) patients and non-traumatic brain
injury (NTBI) DOC patients by using cerebrospinal fluid (CSF), serum and urine
samples beneficial to understand the pathological mechanism differences between the
two etiologies, provide potential clues for the subsequent treatment and prognosis, and
investigate the metabolome differences and similarities between TBI and NTBI among
three different body fluids.
Methods::
In total, 24 TBI DOC subjects and 29 NTBI DOC subjects were enrolled.
CSF, serum and urine samples from TBI DOC and NTBI DOC patients were collected
and analyzed by performing UPLC-MS. The statistical methods and pathway analyses
were applied to discover potential biomarkers and altered metabolic functions.
Results::
When comparing TBI DOC and NTBI DOC, 36, 31 and 52 differential
metabolites were obtained in CSF, serum and urine, respectively. The functional
analysis of differential metabolites obtained in CSF, serum and urine were all related to
amino acid metabolism. Except for amino acid metabolism, metabolic biomarkers in
CSF, serum and urine mainly focus on central function, cognitive function, necrosis
and apoptosis and neurological function, respectively. In CSF, the highest AUC was
0.864 (Isoproturon) and 0.816 (Proline betaine). Then, the AUC of NFurfurylformamide
in serum was 0.941, while the AUC of Dihydronepetalactone and
Doxepin N-oxide glucuronide were 1.0 in urine.
Conclusion::
CSF, serum and urine metabolomic analyses could differentiate TBI
DOC from NTBI DOC and functional analyses showed a metabolic change difference
between TBI DOC and NTBI DOC.
100 项与 盐酸多塞平 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 入睡和睡眠障碍 | 美国 | 2010-03-17 | |
| 特应性皮炎 | 美国 | 1994-04-01 | |
| 神经性皮炎 | 美国 | 1994-04-01 | |
| 瘙痒 | 美国 | 1994-04-01 | |
| 焦虑症 | 美国 | 1969-09-23 | |
| 抑郁症 | 美国 | 1969-09-23 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 口腔炎 | 临床3期 | - | 2014-05-20 |
登录后查看更多信息
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 | 5 | placebo | 鹹選衊醖襯蓋鑰簾齋衊(醖醖構憲糧窪構遞鹽選) = 憲醖憲選觸鑰願憲簾壓 鏇繭鬱衊願蓋製鏇鑰淵 (齋鹽網鏇蓋簾觸遞繭獵, 製糧鑰餘觸淵觸築獵衊 ~ 齋遞蓋構壓網憲憲醖網) 更多 | - | 2019-10-01 | ||
临床3期 | 155 | Placebo+Doxepin (Arm I (Doxepin-Placebo)) | 醖膚憲願廠鹹簾獵夢範(襯艱壓餘襯艱繭簾膚窪) = 繭構鹹鏇壓夢鹹蓋願齋 積窪鹽鏇遞顧膚積憲膚 (簾廠艱壓夢餘鬱淵鑰製, 鬱選餘簾選壓構範壓願 ~ 齋衊遞餘鹽衊窪窪網製) 更多 | - | 2017-05-08 | ||
Placebo+Doxepin (Arm II (Placebo-Doxepin)) | 醖膚憲願廠鹹簾獵夢範(襯艱壓餘襯艱繭簾膚窪) = 鹽夢廠蓋顧憲鹽選淵願 積窪鹽鏇遞顧膚積憲膚 (簾廠艱壓夢餘鬱淵鑰製, 構廠壓憲齋顧艱鏇鏇製 ~ 積鹹鑰憲觸鬱繭繭蓋鏇) 更多 | ||||||
临床4期 | 44 | Placebo | 艱願鑰餘淵襯網衊鬱製(遞廠齋餘觸選夢餘淵顧) = 網淵醖鹹簾製構積獵築 構夢築襯積築艱醖構鬱 (艱夢衊窪窪構衊簾衊鬱, 淵顧積醖醖膚廠廠齋顧 ~ 夢壓繭願醖構繭願淵積) 更多 | - | 2013-07-30 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用