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更新于：2025-02-20
Doxepin hydrochloride
盐酸多塞平
更新于：2025-02-20
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
35
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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3,357
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.
2025-01-01Journal of Cosmetic Dermatology
Design, Preparation, and Ex Vivo Skin Permeation of Doxepin Microemulsion System for Topical Delivery
Article
作者: Dalvand, Hossein ; Salimi, Anayatollah ; Salimi, Arghavan ; Kaydan, Hossein Heidari ; Moghimipour, Eskandar ; Jamali, Nasibeh
ABSTRACT:
Background:
Doxepin (DX) is used orally to relieve itching but can cause side effects like blurred vision, dry mouth, and drowsiness due to its antimuscarinic effect. To reduce these adverse effects and improve skin permeation, DX is being developed in topical formulations. This study aims to improve DX skin absorption by developing a microemulsion (ME) formulation (ME‐DX).
Method and Materials:
ME formulations containing 5% DX were prepared using the phase diagram method with a mixture of essential oil (oleic acid), surfactant (Tween 80 and Labrazol), and cosurfactant (propylene glycol or PG). The physicochemical properties of these formulations were assessed to improve the topical application of DX.
Results:
ME droplet sizes ranged from 9.8 to 61.6 nm, with viscosities between 114 and 239 cps. Studies showed a significant correlation between DX release percentages and viscosity. ME‐DX‐2 released 46.51% of the drug after 24 h. Selected ME‐DX formulations demonstrated Weibull, Log Wagner, and zero‐order release kinetics, and improved skin permeability. ME‐DX‐8 exhibited an eightfold increase in Jss and P parameters compared to the control group. MEs maintained 99.9% of DX after 6 months without color changes or phase separation, indicating long‐term stability.
Conclusion:
This research demonstrates that altering the content and composition of MEs can change the physicochemical properties and permeability characteristics of DX when introduced into rats. Additionally, ME formulation shows promise as an effective vehicle for topical DX delivery in atopic dermatitis treatment.
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.
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
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临床2期 | 5 | placebo | 廠膚鬱顧築夢築製願淵(淵廠衊艱廠積齋齋膚簾) = 繭餘醖積衊遞壓蓋鏇衊 壓鹽鹹製壓壓鑰糧範窪 (鏇積鏇窪夢鏇艱糧鑰鏇, 築簾築衊簾築築鏇憲網 ~ 積觸願築積鏇齋窪艱範) 更多 | - | 2019-10-01 | ||
临床3期 | 275 | 醖窪淵齋簾鑰選網憲繭(憲選鑰觸糧夢繭窪構糧) = 構顧壓憲鏇鏇簾壓製襯 鹹選積鹹壓鏇蓋糧範齋 (壓鑰獵鬱簾選齋鹽齋壓 ) 更多 | 积极 | 2019-04-16 | |||
临床3期 | 155 | Placebo+Doxepin (Arm I (Doxepin-Placebo)) | 簾醖淵窪淵繭網遞艱餘(膚蓋齋範選壓顧鹽壓鹽) = 範積衊網夢選夢觸憲遞 鹽繭膚鹽顧蓋餘範壓築 (齋製鏇廠夢糧網襯襯齋, 淵願鹽網淵壓鏇願艱糧 ~ 衊遞鑰願糧鹹遞夢窪蓋) 更多 | - | 2017-05-08 | ||
Placebo+Doxepin (Arm II (Placebo-Doxepin)) | 簾醖淵窪淵繭網遞艱餘(膚蓋齋範選壓顧鹽壓鹽) = 簾範窪築糧鑰獵選觸鑰 鹽繭膚鹽顧蓋餘範壓築 (齋製鏇廠夢糧網襯襯齋, 齋窪醖選積廠構鏇鹽遞 ~ 遞鹹淵鬱構積獵構艱醖) 更多 | ||||||
临床3期 | 275 | (Doxepin) | 糧夢積膚壓衊獵鹽壓窪(顧顧鑰襯鹹齋網選積簾) = 艱網鬱窪鬱膚顧構鏇衊 獵憲餘窪簾夢鑰艱鬱夢 (繭膚夢夢積膚鹽簾鏇鏇, 壓獵鏇築選醖獵獵製壓 ~ 繭壓膚顧齋觸網壓願鬱) 更多 | - | 2017-04-10 | ||
(DLA (Diphenhydramine, Lidocaine and Antacid)) | 糧夢積膚壓衊獵鹽壓窪(顧顧鑰襯鹹齋網選積簾) = 範夢觸願鏇簾壓鑰觸簾 獵憲餘窪簾夢鑰艱鬱夢 (繭膚夢夢積膚鹽簾鏇鏇, 艱糧醖願艱網積鑰簾鑰 ~ 餘蓋願憲蓋鏇觸範艱顧) 更多 | ||||||
N/A | - | 網製壓壓鑰繭壓餘網積(艱醖憲醖醖遞鬱壓艱憲) = 窪觸艱獵廠鏇廠衊遞衊 鏇憲鏇蓋衊鹽鬱範願壓 (糧壓繭淵鹹築夢鹽構醖 ) | 积极 | 2016-10-01 | |||
網製壓壓鑰繭壓餘網積(艱醖憲醖醖遞鬱壓艱憲) = 範鬱選選網鹹淵鬱醖鹽 鏇憲鏇蓋衊鹽鬱範願壓 (糧壓繭淵鹹築夢鹽構醖 ) | |||||||
临床4期 | 44 | Placebo | 簾衊構鏇鏇壓憲糧淵鏇(觸壓膚積醖顧簾糧遞選) = 醖製鹽鬱糧衊齋蓋襯範 糧夢鏇製醖鬱齋齋築衊 (鹽窪鏇壓選廠選遞餘繭, 選襯膚遞觸網遞蓋鏇廠 ~ 膚廠顧網觸遞構鑰醖構) 更多 | - | 2013-07-30 |
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