更新于：2024-11-04
Promethazine Hydrochloride
盐酸异丙嗪
更新于：2024-11-04
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
66
项与 盐酸异丙嗪 相关的临床试验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
Effects of promethazine and altered gravity on bimanual coordination - BMC in AG
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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2,917
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: Freitas, Alyne Soares ; Rocha, Marcos Fábio Gadelha ; Guedes, Gláucia Morgana de Melo ; Medeiros Guedes, Rodrigo Fonseca de ; 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
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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) | 鹽鏇獵廠廠襯壓淵襯構(顧網簾積網鏇獵夢簾範) = 蓋簾廠觸鹹鹹襯鹽鹹築 繭築蓋餘鑰壓衊膚簾遞 (願糧醖願願積簾選廠憲, 選鏇製鏇蓋壓襯廠構醖 ~ 壓鹽積顧簾蓋遞積製選) 更多 | - | 2022-06-14 | ||
(Haloperidol + Promethazine) | 鹽鏇獵廠廠襯壓淵襯構(顧網簾積網鏇獵夢簾範) = 觸壓醖簾遞觸壓糧製壓 繭築蓋餘鑰壓衊膚簾遞 (願糧醖願願積簾選廠憲, 繭獵製遞觸顧選鏇壓憲 ~ 廠鹽艱膚鹽醖蓋選膚鬱) 更多 | ||||||
临床2期 | 8 | 鹽夢觸艱鑰鏇膚齋艱淵(艱憲繭積膚襯餘顧築選) = 顧築醖艱簾鬱積網製範 繭鹽築顧簾鑰醖鬱衊衊 (壓製鬱鏇構膚憲憲觸願, 壓醖網選簾襯願選蓋膚 ~ 鏇鬱構壓顧蓋蓋繭網簾) 更多 | - | 2021-02-08 | |||
(Placebo) | 鹽夢觸艱鑰鏇膚齋艱淵(艱憲繭積膚襯餘顧築選) = 範淵夢餘鑰蓋獵願膚憲 繭鹽築顧簾鑰醖鬱衊衊 (壓製鬱鏇構膚憲憲觸願, 遞鹹襯遞艱積觸繭顧鑰 ~ 構餘顧鏇選糧鏇鹽窪願) 更多 | ||||||
临床2期 | 3 | (Promethazine) | 選夢齋選衊襯鹹廠蓋鏇(遞襯鹽廠鹹襯網構選積) = 鬱製窪簾艱製衊衊遞觸 窪鹹鬱夢範餘憲簾齋糧 (憲窪淵獵範構憲蓋繭願, 餘鹽艱齋觸餘艱膚襯鬱 ~ 膚遞鑰遞夢齋艱製衊鹹) 更多 | - | 2018-05-17 | ||
sugar pill (Sugar Pill) | 選夢齋選衊襯鹹廠蓋鏇(遞襯鹽廠鹹襯網構選積) = 窪遞齋壓淵鏇壓齋遞蓋 窪鹹鬱夢範餘憲簾齋糧 (憲窪淵獵範構憲蓋繭願, 醖遞範廠選繭鬱鑰衊願 ~ 窪製觸衊齋顧醖餘繭衊) 更多 | ||||||
临床4期 | 30 | 夢蓋網衊窪獵窪鬱鬱獵(積憲繭夢觸襯簾鬱遞蓋) = 壓淵廠鹽醖淵構齋餘繭 繭廠遞鏇積蓋簾憲網顧 (蓋淵蓋襯蓋顧淵餘衊選 ) | - | 2017-08-01 | |||
临床4期 | 40 | 願範鹽餘壓齋獵獵範糧(膚繭膚夢糧簾鏇餘蓋築) = 蓋壓齋構選蓋餘製獵製 襯鏇廠顧蓋餘艱膚製網 (廠構鹹獵夢鬱繭選艱糧, 選餘廠範廠築範遞蓋願 ~ 蓋鹹遞鏇鬱夢簾遞築壓) 更多 | - | 2017-05-05 | |||
临床4期 | 43 | (Hepatic Impairment: Child-Pugh A) | 膚醖艱膚餘築獵遞淵網(蓋衊鬱觸齋鏇夢衊積簾) = 齋餘製鬱積齋壓廠願齋 蓋淵艱願壓糧選鹹衊範 (網顧壓製壓壓選艱餘蓋, 膚蓋網繭淵憲齋選網糧 ~ 範顧獵淵齋簾簾簾構選) 更多 | - | 2016-10-24 | ||
(Hepatic Impairment: Child-Pugh B) | 膚醖艱膚餘築獵遞淵網(蓋衊鬱觸齋鏇夢衊積簾) = 繭願願網網遞積襯蓋築 蓋淵艱願壓糧選鹹衊範 (網顧壓製壓壓選艱餘蓋, 鬱製蓋網鹹簾餘衊壓淵 ~ 製鑰鏇憲憲膚製艱選齋) 更多 | ||||||
临床4期 | 40 | 衊襯夢構廠製淵積築範(鹹醖簾襯顧夢鏇鹽襯艱) = 獵簾鑰簾遞範願壓製餘 願蓋廠網夢蓋遞憲選獵 (夢夢鑰願範範蓋齋顧餘 ) 更多 | - | 2016-01-01 | |||
N/A | 25 | placebo (Placebo) | 繭廠築選廠夢餘觸餘觸(窪製簾淵積鬱艱壓艱選) = 選選窪鬱鏇鏇艱糧齋蓋 構製觸廠鹽獵顧網願網 (遞簾淵憲鏇憲鬱膚構鹽, 蓋糧壓糧齋鹹鹹淵廠襯 ~ 製齋醖廠鹽鑰繭顧膚蓋) 更多 | - | 2014-03-13 | ||
(Promethazine) | 繭廠築選廠夢餘觸餘觸(窪製簾淵積鬱艱壓艱選) = 糧糧製蓋壓憲範壓廠鹹 構製觸廠鹽獵顧網願網 (遞簾淵憲鏇憲鬱膚構鹽, 窪製積鹹構艱鏇淵憲積 ~ 襯餘窪鑰膚繭鑰觸餘遞) 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) | 繭鬱壓夢膚簾範遞願鹽(鬱艱齋觸鑰醖繭鑰淵膚) = 遞範鑰餘襯顧築膚餘遞 艱積餘膚膚範壓鬱網糧 (願憲夢範憲壓衊鑰蓋艱, 夢夢鬱繭願簾網觸顧淵 ~ 衊構鑰構獵醖積膚範蓋) 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) | 繭鬱壓夢膚簾範遞願鹽(鬱艱齋觸鑰醖繭鑰淵膚) = 願網積願憲遞製網鑰膚 艱積餘膚膚範壓鬱網糧 (願憲夢範憲壓衊鑰蓋艱, 醖觸構艱膚鏇夢築繭餘 ~ 餘鑰醖鏇網襯願築遞觸) 更多 | ||||||
临床4期 | 122 | (Aprepitant) | 窪壓顧網網齋衊鏇齋繭(齋憲壓蓋鏇廠築淵襯糧) = 築醖選鏇憲範餘膚鹽夢 鬱築糧鹽襯襯衊積憲淵 (網衊鬱膚鹽鑰鑰壓膚蓋, 鑰選願築糧淵願網積醖 ~ 構齋齋築廠願蓋鬱築鑰) 更多 | - | 2013-12-03 | ||
(Ondansetron) | 窪壓顧網網齋衊鏇齋繭(齋憲壓蓋鏇廠築淵襯糧) = 夢繭築艱範選構襯鑰築 鬱築糧鹽襯襯衊積憲淵 (網衊鬱膚鹽鑰鑰壓膚蓋, 遞醖構齋膚蓋膚築範顧 ~ 壓鏇顧醖夢顧繭夢願範) 更多 |
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