预约演示
更新于：2025-01-13
Doxepin hydrochloride
盐酸多塞平
更新于：2025-01-13
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 |
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/序列
分子式C19H22ClNO |
InChIKeyMHNSPTUQQIYJOT-UHFFFAOYSA-N |
CAS号1229-29-4 |
关联
34
项与 盐酸多塞平 相关的临床试验CTR20240056
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
CTIS2023-508117-16-00
- P23-01
IRCT20230928059539N1
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
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100 项与 盐酸多塞平 相关的转化医学
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100 项与 盐酸多塞平 相关的专利（医药）
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1,392
项与 盐酸多塞平 相关的文献（医药）2025-04-01JOURNAL OF COLLOID AND INTERFACE SCIENCE
Spontaneous formation of small and ultrasmall unilamellar vesicles in mixtures of drug surfactant and phospholipid: Effect of chemical structure of phospholipid tails on vesicle size
Article
作者: Edwards, Katarina ; Gedda, Lars ; Forooqi Motlaq, Vahid ; Doutch, James ; Bergström, L Magnus
We have investigated the effect of length and chemical structure of phospholipid tails on the spontaneous formation of unilamellar liposomal vesicles in binary solute mixtures of cationic drug surfactant and zwitterionic phosphatidylcholine phospholipids. Binary drug surfactant-phospholipid mixtures with four different phospholipids with identical headgroups (two saturated phospholipids 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC, 14:0) and 1,2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC, 16:0), and two unsaturated lipids 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC, 18:1) and 1,2-Dierucoyl-sn-Glycero-3-Phosphatidylcholine (DEPC, 22:1)) combined with two different tricyclic antidepressant drugs (amitriptyline hydrochloride (AMT) and doxepin hydrochloride (DXP)) have been investigated with small-angle neutron scattering (SANS) and cryo-transmission electron microscopy (cryo-TEM). We observe a conspicuous impact of phospholipid tail structure on both micelle-to-vesicle transition point and vesicle size. In particular, ultrasmall unilamellar vesicles, i.e. with a diameter less than 20 nm, were observed in several samples with the two unsaturated phospholipids DOPC and DEPC, but not in any samples with the saturated phospholipids DMPC and DPPC. The smallest vesicles observed in DOPC and DEPC mixtures were smaller than 18 nm in diameter. In contrast, the smallest vesicles observed in DMPC mixtures were about 30 nm in diameter and always larger than 100 nm in DPPC mixtures. The ultrasmall vesicles showed exceptional colloidal stability. Moreover, bilayer vesicles predominated over micelles in a much wider range of concentrations for DOPC and DEPC mixtures as a result of having a smaller phospholipid mole fraction in the aggregates at the micelle-to-vesicle transition. Our results have been theoretically rationalized by combining solution thermodynamics with bending elasticity theory.
2025-01-01CLEVELAND CLINIC JOURNAL OF MEDICINE
Insomnia in older adults: A review of treatment options
Review
作者: León-Barriera, Roberto ; Modesto-Lowe, Vania ; Chaplin, Margaret M ; Kaur, Jasleen
Insomnia is a common and challenging complaint in older adults (> 65 years) because of age-related alterations in sleep physiology. Cognitive behavioral therapy for insomnia is the gold standard for treatment of insomnia in young as well as older patients. Both clinicians and patients often prefer the simplicity of medication, but risks associated with some hypnotics increase with age. Pharmacologic options for older adults include low-dose doxepin, melatonin, ramelteon, and the dual orexin receptor antagonists. A well-informed clinician can help patients navigate the risks and benefits of both pharmacologic and behavioral options.
2024-12-01Alzheimers & Dementia
Differential Effects of Anticholinergic Medications in Patient hiPSC‐Derived Neurons
Article
作者: Zhu, Ruowei ; Pranoto, Inez ; Gray, Shelly L ; Hui, Katherine ; Ogg, Jordan ; Young, Jessica E. ; Crane, Paul K. ; Schwarze‐Taufiq, Tiara A.
Abstract:
Background:
Anticholinergic (AC) use remains common in older adults despite evidence of safety risks, including dementia risk. Evidence from population studies suggests that dementia risk may vary by AC class. This variation might be explained by confounding by indication. In vitro models, using human neural cells where cells are directly experimentally exposed to a drug and phenotypic outcomes are measured, may address this issue. We identified classes of AC medications with and without an association with dementia based on population studies. We treated human induced pluripotent stem cell‐derived neurons (hiPSC‐Ns) with each AC medication and performed cellular assays to examine the effects on AD phenotypes.
Method:
We have generated hiPSC lines from participants in the Adult Changes in Thought Study (ACT), a longitudinal study in Seattle, WA. We differentiated hiPSC‐Ns from ACT cell lines using protocols in our laboratory. We treated neurons with different classes of AC medications: antidepressants (amitriptyline, doxepin, paroxetine), antihistamines (diphenhydramine, chlorpheniramine), bladder antimuscarinics (oxybutynin, tolterodine), and antispasmodics (atropine). As a control, we treated cells with the classic cholinergic compound carbachol. Cells were treated with two drug doses (10 uM, 50 uM) at two time points (24 hours, 48 hours). We used molecular assays to test AD‐associated cellular outcomes (neurotoxicity, synaptic gene expression and Amyloid beta [Aβ]).
Result:
We document differential effects of medications on cytotoxicity, secreted Aβ levels, and synaptic gene expression. Several drugs demonstrated dose‐dependent (doxepin, oxybutynin, paroxetine, amitriptyline) and/or time dependent (oxybutynin, paroxetine) neurotoxicity. We also observed differential effects on Aβ secretion. Oxybutynin, a bladder antimuscarinic, consistently induced an increase in the Aβ42/40 ratio, largely driven by increased secreted Aβ42. Further, all antidepressants and bladder antimuscarinics tested increased the secreted Aβ42/40 ratio at 50 uM. These findings are consistent across lines of different genetic backgrounds.
Conclusion:
Stem cell‐derived neuronal models provide a useful strategy to complement pharmacoepidemiological studies to help distinguish molecular pathways versus confounding by indication of drugs associated with dementia risk. Preliminary results suggest that different AC medications have differential effects on AD‐associated cellular outcomes that are consistent across hiPSC‐Ns derived from individuals with various genetic backgrounds, indicating a molecular effect of the drug.
100 项与 盐酸多塞平 相关的药物交易
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研发状态
批准上市
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 |
|---|---|---|---|
| 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
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 头颈部肿瘤 | 临床3期 | 美国 | 2010-12-01 | |
| 粘膜炎 | 临床3期 | 美国 | 2010-12-01 | |
| 疼痛 | 临床3期 | 美国 | 2010-12-01 | |
| 辐射损伤 | 临床3期 | 美国 | 2010-12-01 | |
| 口腔炎 | 临床3期 | 美国 | 2010-12-01 | |
| 食管癌 | 临床2期 | 美国 | 2014-04-14 | |
| 食管炎 | 临床2期 | 美国 | 2014-04-14 | |
| 下咽癌 | 临床2期 | 美国 | 2014-04-14 | |
| 喉肿瘤 | 临床2期 | 美国 | 2014-04-14 | |
| 淋巴瘤 | 临床2期 | 美国 | 2014-04-14 |
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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 | 5 | placebo | 選餘醖膚鏇鹽觸廠鑰蓋(衊衊獵積齋顧鹹鏇蓋鹽) = 醖壓憲糧獵醖蓋醖獵構 選鹹齋鏇艱夢糧製鏇選 (窪鹽齋窪鏇夢築蓋淵積, 壓夢窪襯願顧網遞夢壓 ~ 顧夢範窪願鏇繭艱簾製) 更多 | - | 2019-10-01 | ||
临床3期 | 275 | 選醖壓壓網壓鏇築網餘(廠鏇鑰顧顧憲鏇顧廠餘) = 遞觸鬱鹹鑰膚簾廠遞膚 夢顧糧鑰艱淵鬱獵鑰餘 (範選襯範壓醖膚襯艱糧 ) 更多 | 积极 | 2019-04-16 | |||
临床3期 | 155 | Placebo+Doxepin (Arm I (Doxepin-Placebo)) | 鹽築顧窪艱餘獵襯範餘(選顧觸襯醖鏇襯齋醖憲) = 鬱選遞廠艱網夢淵齋簾 簾遞網廠築襯鏇夢觸齋 (構簾艱衊範繭網廠齋窪, 憲壓鹹願夢衊繭鏇願襯 ~ 獵衊夢鏇製鬱鬱膚蓋獵) 更多 | - | 2017-05-08 | ||
Placebo+Doxepin (Arm II (Placebo-Doxepin)) | 鹽築顧窪艱餘獵襯範餘(選顧觸襯醖鏇襯齋醖憲) = 齋簾蓋齋艱鏇膚襯夢獵 簾遞網廠築襯鏇夢觸齋 (構簾艱衊範繭網廠齋窪, 願醖顧鏇餘糧壓繭遞憲 ~ 夢餘簾鏇願顧餘網繭顧) 更多 | ||||||
临床3期 | 275 | (Doxepin) | 餘繭遞鹽鏇製築製繭壓(鬱構蓋鏇簾蓋範糧積鬱) = 鬱顧網艱醖壓衊齋網憲 憲窪憲範鹹衊範鑰獵簾 (網範觸衊廠衊糧觸夢齋, 網餘鏇醖選壓衊顧壓獵 ~ 膚鑰壓憲醖構憲鹽願獵) 更多 | - | 2017-04-10 | ||
(DLA (Diphenhydramine, Lidocaine and Antacid)) | 餘繭遞鹽鏇製築製繭壓(鬱構蓋鏇簾蓋範糧積鬱) = 夢艱襯遞夢餘構艱網糧 憲窪憲範鹹衊範鑰獵簾 (網範觸衊廠衊糧觸夢齋, 遞糧蓋夢壓壓觸構夢憲 ~ 遞鏇顧衊窪繭範積積膚) 更多 | ||||||
N/A | - | 簾獵鹹廠顧膚夢繭窪鬱(齋淵鏇顧憲繭製餘齋窪) = 窪壓淵選淵淵憲積憲鏇 製範蓋鬱顧餘鑰淵餘淵 (觸醖鹹齋窪範鏇鏇鹹艱 ) | 积极 | 2016-10-01 | |||
簾獵鹹廠顧膚夢繭窪鬱(齋淵鏇顧憲繭製餘齋窪) = 艱廠廠積願獵餘鑰憲鹹 製範蓋鬱顧餘鑰淵餘淵 (觸醖鹹齋窪範鏇鏇鹹艱 ) | |||||||
临床4期 | 44 | Placebo | 襯鹹鑰築觸鬱鑰壓艱夢(鏇鹹鹽鬱繭鬱觸觸選鬱) = 夢築獵淵顧獵壓夢鹹繭 廠淵構衊夢鹽蓋簾艱鬱 (簾醖膚艱衊夢淵壓餘衊, 觸衊鹹壓鏇顧鑰襯夢獵 ~ 壓鏇齋築選膚糧夢艱鏇) 更多 | - | 2013-07-30 |
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