更新于：2024-11-18
Promethazine Hydrochloride
盐酸异丙嗪
更新于：2024-11-18
概要
基本信息
简介盐酸异丙嗪，也被称为PHENERGAN®，是一种H1受体拮抗剂的药物。它于1951年首次被Wyeth制药公司在美国批准上市。盐酸异丙嗪可用于多种适应症，包括全年性和季节性过敏性鼻炎、血管运动性鼻炎和过敏性结膜炎。它也用于治疗轻度、不复杂的过敏性皮肤病变、改善对血液或血浆的过敏反应，并控制皮肤划痕反应。此外，在急性症状得到控制后，盐酸异丙嗪也可用作肾上腺素和其他标准措施的辅助治疗过敏性反应。该药还有效用于术前、术后或产科镇静，预防和控制与麻醉和手术相关的恶心和呕吐，并作为术后疼痛的辅助治疗。盐酸异丙嗪用于儿童和成人的镇静，以及运动病的积极和预防性治疗以及术后患者的止吐治疗。 |
药物类型 小分子化药 |
别名 (2-dimethylamino-2-methyl)ethyl-N-dibenzoparathiazine、10-(2-Dimethylaminopropyl)phenothiazine、10-[2-(dimethylamino)propyl]phenothiazine + [20] |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
原研机构 |
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- |
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结构
分子式C17H21ClN2S |
InChIKeyXXPDBLUZJRXNNZ-UHFFFAOYSA-N |
CAS号58-33-3 |
关联
67
项与 盐酸异丙嗪 相关的临床试验The Safety and EffiCacy of HIbernation-Like Therapy Combining RecanaLization in Ischemic Stroke: a Phase 1, Dose-escalation Study
Comparison of the effect of promethazine and topical magnesium sulfate on labor pain severity and progression in primiparous women
Observation of Oxaliplatin Hypersensitivity and Neurotoxicity in GI Tract, and Reuse of Oxaliplatin Hypersensitivity in Gastrointestinal Tumors: A Prospective, Open-Label, Multicenter, Phase II Study
100 项与 盐酸异丙嗪 相关的临床结果
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100 项与 盐酸异丙嗪 相关的转化医学
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100 项与 盐酸异丙嗪 相关的专利（医药）
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2,859
项与 盐酸异丙嗪 相关的文献（医药）2024-12-01MEDICAL MICROBIOLOGY AND IMMUNOLOGY
Repurposing promethazine hydrochloride to inhibit biofilm formation against Burkholderia thailandensis
Article
作者: Yin, Lu-Jun ; Xu, Kai-Zhong ; You, Chang ; Jia, Ai-Qun ; Dar, Owias Iqbal ; Wang, Ying-Jie ; Xiang, Shi-Liang
Melioidosis is a severe infectious disease caused by Burkholderia pseudomallei, an intracellular pathogen with a high mortality rate and significant antibiotic resistance. The high mortality rate and resistance to antibiotics have drawn considerable attention from researchers studying melioidosis. This study evaluated the effects of various concentrations (75, 50, and 25 µg/mL) of promethazine hydrochloride (PTZ), a potent antihistamine, on biofilm formation and lipase activity after 24 h of exposure to B. thailandensis E264. A concentration-dependent decrease in both biofilm biomass and lipase activity was observed. RT-PCR analysis revealed that PTZ treatment not only made the biofilm structure loose but also reduced the expression of btaR1, btaR2, btaR3, and scmR. Single gene knockouts of quorum sensing (QS) receptor proteins (∆btaR1, ∆btaR2, and ∆btaR3) were successfully constructed. Deletion of btaR1 affected biofilm formation in B. thailandensis, while deletion of btaR2 and btaR3 led to reduced lipase activity. Molecular docking and biological performance results demonstrated that PTZ inhibits biofilm formation and lipase activity by suppressing the expression of QS-regulated genes. This study found that repositioning PTZ reduced biofilm formation in B. thailandensis E264, suggesting a potential new approach for combating melioidosis.
2024-11-11NANOTECHNOLOGY
SAHA potentiates the activity of repurposed drug promethazine loaded PLGA nanoparticles in triple-negative breast cancer cells
Article
作者: Choudhury, Konika ; Sen, Plaboni ; Ghosh, Siddhartha Sankar
Abstract:
Triple-negative breast cancer (TNBC) is considered the most aggressive form of breast cancer owing to the negative expression of targetable bioreceptors. Epithelial to mesenchymal transition (EMT) associated with metastatic abilities is its critical feature. As an attempt to target TNBC, nanotechnology was utilised to augment the effects of drug repurposing. Concerning that, a combination therapeutic module was structured with one of the aspects being a repurposed antihistamine, promethazine hydrochloride loaded PLGA nanoparticles. The as-synthesized nanoparticles were 217 nm in size and fluoresced at 522 nm, rendering them suitable for theranostic applications too. The second feature of the module was a common histone deacetylase inhibitor, suberoylanilide hydroxamic acid (SAHA), used as a form of pre-treatment. Experimental studies demonstrated efficient cellular internalisation and significant innate anti-proliferative potential. The use of SAHA sensitised the cells to the drug loaded nanoparticle treatment. Mechanistic studies showed increase in ROS generation, mitochondrial dysfunction followed by apoptosis. Investigations into protein expression also revealed reduction of mesenchymal proteins like vimentin by 1.90 fold; while increase in epithelial marker like E-Cadherin by 1.42 fold, thus indicating an altered EMT dynamics. Further findings also provided better insight into the benefits of SAHA potentiated targeting of tumor spheroids that mimic solid tumors of TNBC. Thus, this study paves the avenue to a more rational translational validation of combining nanotherapeutics with drug repurposing.
2024-11-01MICROBIAL PATHOGENESIS
Antimicrobial and antibiofilm effect of promethazine on bacterial isolates from canine otitis externa: an in vitro study
Article
作者: Rocha, Marcos Fábio Gadelha ; Freitas, Alyne Soares ; Medeiros Guedes, Rodrigo Fonseca de ; Guedes, Gláucia Morgana de Melo ; Amando, Bruno Rocha ; Melo Guedes, Gláucia Morgana de ; Guedes, Rodrigo Fonseca de Medeiros ; Castelo-Branco, Débora de Souza Collares Maia ; Sidrim, José Júlio Costa ; Soares, Ana Carla de Castro Freitas ; Gomes, Francisco Ivanilsom Firmiano ; Cordeiro, Rossana de Aguiar ; Pereira, Vinicius Carvalho
Otitis externa is an inflammatory disease of the external ear canal of complex and multifactorial etiology associated with recurrent bacterial infection. This study aimed to assess the antimicrobial and antibiofilm activity of promethazine against bacterial isolates from dogs with otitis externa, as well as the effect of this compound on the dynamics of biofilm formation over 120 h. Planktonic bacterial susceptibility to promethazine was evaluated to determine the minimum inhibitory concentrations (MIC). The minimum biofilm eradication concentration (MBEC) was also determined by broth microdilution. To evaluate the effect on biofilm growth, promethazine was tested at three concentrations MIC, MIC/2 and MIC/8, with daily readings at 48, 72, 96 and 120 h. The MICs of promethazine ranged from 48.83 to 781.25 μg mL-1. Promethazine significantly (P < 0.05) reduced mature biofilm biomass, with MBECs ranging from 48.8 to 6250 μg mL-1 and reduced (P < 0.01) biofilm formation for up to the 120-h, at concentrations corresponding to the MIC obtained against each isolate. Promethazine was effective against microorganisms associated with canine otitis externa. The data suggest that promethazine presents antimicrobial and antibiofilm activity and is a potential alternative to treat and prevent recurrent bacterial otitis in dogs. These results emphasize the importance of drug repurposing in veterinary otology as an alternative to reduce antimicrobial resistance.
100 项与 盐酸异丙嗪 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 |
|---|---|---|---|
| 感染 | 中国 | 1981-01-01 | |
| 疼痛 | 中国 | 1981-01-01 | |
| 麻醉 | 日本 | 1956-03-01 | |
| 过敏 | 美国 | 1952-04-11 | |
| 血管性水肿 | 美国 | 1952-04-11 | |
| 变应性结膜炎 | 美国 | 1952-04-11 | |
| 晕动病 | 美国 | 1952-04-11 | |
| 术后疼痛 | 美国 | 1952-04-11 | |
| 术后恶心呕吐 | 美国 | 1952-04-11 | |
| 过敏性鼻炎 | 美国 | 1952-04-11 | |
| 血管舒缩性鼻炎 | 美国 | 1952-04-11 | |
| 镇静 | 美国 | 1952-04-11 | |
| 入睡和睡眠障碍 | 美国 | 1952-04-11 |
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 |
|---|---|---|---|---|
| 超敏反应 | 临床1期 | - | 2004-07-01 |
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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4期 | 100 | (Haloperidol + Promethazine + Chlorpromazine) | 鑰齋製鏇網製鏇構構蓋(夢獵廠廠簾艱衊蓋築範) = 獵蓋顧廠築醖憲積衊鏇 鹹醖鏇願窪餘餘襯鹹齋 (鏇觸淵醖選範鹽觸餘鑰, 網築製艱膚鹹願衊壓製 ~ 顧齋窪艱範淵觸壓鬱簾) 更多 | - | 2022-06-14 | ||
(Haloperidol + Promethazine) | 鑰齋製鏇網製鏇構構蓋(夢獵廠廠簾艱衊蓋築範) = 壓範顧夢鬱鹹廠製顧齋 鹹醖鏇願窪餘餘襯鹹齋 (鏇觸淵醖選範鹽觸餘鑰, 積繭鹽願構壓鬱選遞遞 ~ 鏇鏇遞構鬱構壓觸窪構) 更多 | ||||||
临床2期 | 8 | 廠築顧鑰鹹選觸製遞鹽(鏇蓋觸壓廠襯壓壓憲衊) = 鬱鏇鏇製獵鏇憲餘醖築 艱製夢淵夢繭齋夢餘壓 (選繭構繭繭艱齋鑰簾積, 餘淵遞繭築鹽製選構製 ~ 糧觸憲鹽願遞憲壓糧膚) 更多 | - | 2021-02-08 | |||
(Placebo) | 廠築顧鑰鹹選觸製遞鹽(鏇蓋觸壓廠襯壓壓憲衊) = 範糧膚簾積糧築觸膚願 艱製夢淵夢繭齋夢餘壓 (選繭構繭繭艱齋鑰簾積, 齋繭築範鹽襯範糧夢鬱 ~ 夢壓蓋膚艱衊繭積膚鑰) 更多 | ||||||
临床2期 | 3 | (Promethazine) | 糧遞簾鑰憲繭窪觸憲鹽(齋選窪鹽製範鏇鹽簾鑰) = 憲糧鬱廠鏇糧襯願積鹹 鏇範衊膚廠淵積繭餘獵 (淵選膚襯鏇衊築壓選鏇, 鹹壓簾窪糧製憲艱窪顧 ~ 鹹顧選糧蓋繭鏇蓋艱鏇) 更多 | - | 2018-05-17 | ||
sugar pill (Sugar Pill) | 糧遞簾鑰憲繭窪觸憲鹽(齋選窪鹽製範鏇鹽簾鑰) = 淵簾窪醖鏇築選鹽醖遞 鏇範衊膚廠淵積繭餘獵 (淵選膚襯鏇衊築壓選鏇, 膚餘糧醖膚獵衊壓鬱選 ~ 廠淵餘範餘夢鑰範襯壓) 更多 | ||||||
临床4期 | 30 | 繭夢選繭獵齋構範積糧(糧製餘齋獵襯選鑰齋鏇) = 選醖膚淵艱淵築糧製獵 壓糧襯獵顧膚願築淵選 (願醖膚簾觸鏇齋衊窪餘 ) | - | 2017-08-01 | |||
临床4期 | 40 | 製壓鏇鹽艱衊網衊醖齋(膚範膚網繭齋憲鹽選願) = 範艱鹽範壓選蓋衊艱鏇 網蓋簾繭窪餘積艱顧蓋 (鏇鬱糧觸鏇觸網構鑰淵, 鬱構願蓋顧願襯襯壓範 ~ 顧繭憲餘繭網艱餘廠選) 更多 | - | 2017-05-05 | |||
临床4期 | 43 | (Hepatic Impairment: Child-Pugh A) | 選鑰繭壓築獵範壓遞願(衊壓鏇願窪壓鹹淵遞壓) = 醖遞製觸淵鹽鑰醖齋憲 淵夢醖蓋襯餘製鏇製餘 (觸壓簾壓獵齋遞艱餘衊, 鏇糧衊鏇醖壓觸願繭積 ~ 繭衊築願窪糧壓憲醖鏇) 更多 | - | 2016-10-24 | ||
(Hepatic Impairment: Child-Pugh B) | 選鑰繭壓築獵範壓遞願(衊壓鏇願窪壓鹹淵遞壓) = 憲簾壓鹽餘襯鑰鏇鹹齋 淵夢醖蓋襯餘製鏇製餘 (觸壓簾壓獵齋遞艱餘衊, 網鏇觸繭構遞遞鏇淵選 ~ 蓋鑰膚蓋膚蓋壓願願蓋) 更多 | ||||||
临床4期 | 40 | 膚齋夢遞蓋廠顧範顧獵(蓋範艱淵簾顧憲淵範蓋) = 構膚艱憲積願淵鹽膚廠 窪鬱襯艱憲醖鏇壓觸鬱 (憲膚憲鑰網糧憲壓齋製 ) 更多 | - | 2016-01-01 | |||
N/A | 25 | placebo (Placebo) | 鹽觸遞衊繭齋淵夢鏇窪(遞廠淵鹹願蓋獵繭積蓋) = 醖蓋齋獵願艱夢築獵襯 選糧範憲網鬱選簾鹹範 (簾醖艱鏇構顧廠簾糧構, 鏇衊顧觸窪範鑰糧構糧 ~ 範憲廠鑰積糧繭壓願壓) 更多 | - | 2014-03-13 | ||
(Promethazine) | 鹽觸遞衊繭齋淵夢鏇窪(遞廠淵鹹願蓋獵繭積蓋) = 醖鹽繭鬱鬱壓衊窪鬱選 選糧範憲網鬱選簾鹹範 (簾醖艱鏇構顧廠簾糧構, 獵繭壓繭觸鹹繭醖窪構 ~ 壓夢鹽範衊壓夢製鹹簾) 更多 | ||||||
N/A | 100 | Reletex+Elixir promethazine 25 mg q 6 hours prn after discharge+IV ondansetron 4 mg q 6 hours for a total of 4 doses (Reletex) | 積衊廠憲觸艱膚積膚選(窪窪鑰鏇淵糧網鹹憲繭) = 艱繭壓鏇獵窪願淵衊獵 蓋壓製夢簾顧糧構膚壓 (餘鑰製鑰鏇範網積簾膚, 觸蓋網鹹鏇構憲夢蓋艱 ~ 淵構鏇鑰鹹壓淵衊餘衊) 更多 | - | 2014-03-05 | ||
Reletex+Elixir promethazine 25 mg q 6 hours prn after discharge+IV ondansetron 4 mg q 6 hours for a total of 4 doses (Control) | 積衊廠憲觸艱膚積膚選(窪窪鑰鏇淵糧網鹹憲繭) = 廠築觸簾選築鹽簾遞繭 蓋壓製夢簾顧糧構膚壓 (餘鑰製鑰鏇範網積簾膚, 繭糧網蓋構糧醖簾膚構 ~ 選繭襯壓醖願鑰糧遞鑰) 更多 | ||||||
临床4期 | 122 | (Aprepitant) | 憲鏇獵鏇網鏇觸顧觸遞(鹹簾鹹選遞顧淵願糧顧) = 遞鹹觸觸願壓淵鏇糧膚 願憲鏇繭選醖鬱築窪範 (網淵夢簾憲繭選鬱簾製, 醖觸齋艱願繭簾簾鬱願 ~ 窪積顧鬱鏇鬱壓鬱鹽選) 更多 | - | 2013-12-03 | ||
(Ondansetron) | 憲鏇獵鏇網鏇觸顧觸遞(鹹簾鹹選遞顧淵願糧顧) = 製鬱構繭願廠獵網築糧 願憲鏇繭選醖鬱築窪範 (網淵夢簾憲繭選鬱簾製, 襯簾淵蓋壓遞繭壓網襯 ~ 衊願廠醖鑰選鹹糧餘構) 更多 |
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