更新于：2024-05-01
Ketorolac Tromethamine
酮咯酸氨丁三醇
更新于：2024-05-01
概要
基本信息
简介酮咯酸氨丁三醇，也称为 Toradol®，是一种非甾体抗炎药 (NSAID)，主要用于治疗中度至重度疼痛，包括与类风湿性关节炎、骨关节炎、强直性脊柱炎、月经失调和头痛相关的疼痛。酮咯酸氨丁三醇于1989年由罗氏开发并批准，作为一种COX抑制剂，通过阻断前列腺素的产生有效减轻疼痛。 这种药物有口服和注射剂两种形式，使其成为疼痛管理的多功能选择。 尽管酮咯酸氨丁三醇有效，但由于其潜在的副作用（包括胃肠道出血和肾脏损伤），不建议长期使用。 |
药物类型 小分子化药 |
别名 Acular + [14] |
作用机制 COX-1抑制剂(环氧化酶-1抑制剂)、COX-2抑制剂(环氧化酶-2抑制剂) |
最高研发阶段批准上市 |
首次获批日期 美国 (1989-11-30), |
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C19H24N2O6 |
InChIKeyBWHLPLXXIDYSNW-UHFFFAOYSA-N |
CAS号74103-07-4 |
关联
310
项与 酮咯酸氨丁三醇 相关的临床试验Low-Dose Short-Term Ketorolac to Reduce Chronic Opioid Use in Orthopaedic Polytrauma Patients
Effectiveness of Corticosteroid vs Ketorolac Shoulder Injections: a Prospective Double-Blinded Randomized Trial
Intravenous Ketorolac Administration to Attenuate Post-procedural Pain Associated With Intrauterine Device Placement: A Randomized, Double-Blind, Placebo-Controlled Trial
100 项与 酮咯酸氨丁三醇 相关的临床结果
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100 项与 酮咯酸氨丁三醇 相关的转化医学
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100 项与 酮咯酸氨丁三醇 相关的专利（医药）
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780
项与 酮咯酸氨丁三醇 相关的文献（医药）2024-06-01International journal of pharmaceutics: X
Formulation, optimization and evaluation of ocular gel containing nebivolol Hcl-loaded ultradeformable spanlastics nanovesicles: In vitro and in vivo studies.
Article
作者: Mohamed Yasser ; Eman E El Naggar ; Nehal Elfar ; Mahmoud H Teaima ; Mohamed A El-Nabarawi ; Sammar Fathy Elhabal
The study aims to improve the ocular delivery of Nebivolol HCL (NBV) belonging to the Biopharmaceutics classification system (BCSII) by using spanlastic nanovesicles (SNVs) for ophthalmic delivery and incorporating them into hydroxypropyl methylcellulose gel with ketorolac tromethamine (KET) as an anti-inflammatory to improve glaucoma complications like Conjunctivitis. SNVs were prepared by ethanol injection technique using span (60) as a surfactant and labrasol as an edge activator (EA). The impact of formulation factors on SNVs properties was investigated using a Box-Behnken design. In vitro evaluations showed that the formulations (F1, F4, and F14), containing Span 60 and labrasol as EA (25%, 50%, and 25%), exhibited high EE% with low PS and high ZP and DI. Additionally, 61.72 ± 0.77%, 58.97 ± 1.44%, and 56.20 ± 2.32% of the NBV amount were released from F1, F4, and F14 after 5 h, compared to 93.94 ± 1.21% released from drug suspension. The selected formula (G1), containing F1 in combination with KET and 2% w/w HPMC, exhibited 76.36 ± 0.90% drug release after 12 h. Ex vivo Confocal laser scanning revealed a high penetration of NBV-SNVs gel that ascertained the results of the in-vitro study. In vivo studies showed a significant decrease in glaucoma compared to drug suspension, and histopathological studies showed improvement in glaucomatous eye retinal atrophy. G1 is considered a promising approach to improving ocular permeability, absorption, and anti-inflammatory activity, providing a safer alternative to current regimens.
2024-01-25Journal of translational medicine
Synergistic use of anti-inflammatory ketorolac and gentamicin to target staphylococcal biofilms.
Article
作者: Amita Sekar ; Dmitry Gil ; Peyton Tierney ; Madeline McCanne ; Vikram Daesety ; Darina Trendafilova ; Orhun K Muratoglu ; Ebru Oral
BACKGROUND:
While antibiotics remain our primary tools against microbial infection, increasing antibiotic resistance (inherent and acquired) is a major detriment to their efficacy. A practical approach to maintaining or reversing the efficacy of antibiotics is the use of other commonly used therapeutics, which show synergistic antibacterial action with antibiotics. Here, we investigated the extent of antibacterial synergy between the antibiotic gentamicin and the anti-inflammatory ketorolac regarding the dynamics of biofilm growth, the rate of acquired resistance, and the possible mechanism of synergy.
METHODS:
Control (ATCC 12600, ATCC 35984) and clinical strains (L1101, L1116) of Staphylococcus aureus and Staphylococcus epidermidis with varying antibiotic susceptibility profiles were used in this study to simulate implant-material associated low-risk and high-risk biofilms in vitro. The synergistic action of gentamicin sulfate (GS) and ketorolac tromethamine (KT), against planktonic staphylococcal strains were determined using the fractional inhibitory concentration measurement assay. Nascent (6 h) and established (24 h) biofilms were grown on 316L stainless steel plates and the synergistic biofilm eradication activity was determined and characterized using adherent bacteria count, minimum biofilm eradication concentration (MBEC) measurement for GS, visualization by live/dead imaging, scanning electron microscopy, gene expression of biofilm-associated genes, and bacterial membrane fluidity assessment.
RESULTS:
Gentamicin-ketorolac (GS-KT) combination demonstrated synergistic antibacterial action against planktonic Staphylococci. Control and clinical strains showed distinct biofilm growth dynamics and an increase in biofilm maturity was shown to confer further resistance to gentamicin for both 'low-risk' and 'high-risk' biofilms. The addition of ketorolac enhanced the antibiofilm activity of gentamicin against acquired resistance in staphylococcal biofilms. Mechanistic studies revealed that the synergistic action of gentamicin-ketorolac interferes with biofilm morphology and subverts bacterial stress response altering bacterial physiology, membrane dynamics, and biofilm properties.
CONCLUSION:
The results of this study have a significant impact on the local administration of antibiotics and other therapeutic agents commonly used in the prevention and treatment of orthopaedic infections. Further, these results warrant the study of synergy for the concurrent or sequential administration of non-antibiotic drugs for antimicrobial effect.
2024-01-22European journal of ophthalmology
Neurotrophic Keratopathy after wide retinal endolaser and postoperative Ketorolac eye drops: A case series.
Article
作者: Giovanni Fossati ; Elena Bartoli ; Alessio Montericcio ; Matilde Buzzi ; Gianmaria Barone ; Francesco Santoru ; Davide Allegrini ; Mario R Romano ; Claudio Panico
PURPOSE:
We report a series of 5 cases, happened in a period of 5 months, who developed neurotrophic keratopathy (NK) following pars plana vitrectomy (PPV) and retinal endolaser for rhegmatogenous retinal detachment (RRD). In our several decennary experience of surgical center predominantly based on vitreoretinal surgery, we had rare cases of postoperative NK. These recent cases of post-surgical NK happened contextually to our change of postoperative non-steroidal anti-inflammatory drugs (NSAIDs) drops, based on Ketorolac Tromethamine 0.5% eye drops.
CASES PRESENTATION:
Five patients with a mean age of 61 ± 7.3 years were treated with one or more PPV with intraoperative peripheral endolaser for RRD. Nobody had previous herpetic keratitis, systemic disease like diabetes mellitus or other predisposing factors for NK. In the postoperative period, all patients received Ketorolac Tromethamine 0.5% eye drops for a mean period of 54 ± 25 days. During follow-up visits they developed NK and they were successfully treated with suspension of Ketorolac eye drops, application of therapeutic contact lens or amniotic membrane patch and topical lubricant therapy.
CONCLUSIONS:
Postoperative Ketorolac eye drops, in patients who underwent PPV with endolaser, may reduce the corneal sensitivity, predispose to epithelial disruption and NK development. Studies are needed to explore the effect of NSAIDs on corneal sensitivity reduction in patient who will undergo PPV and extensive endolaser.
100 项与 酮咯酸氨丁三醇 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 炎症 | 批准上市 | 美国 更多 | |
| 疼痛 | 批准上市 | 美国 更多 | |
| 烧伤 | 批准上市 | 美国 更多 | |
| 术后疼痛 | 批准上市 | 美国 更多 | |
| 眼烧伤 | 批准上市 | 美国 更多 |
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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 | 转移性食管癌 一线 | 150 | PF + 10 μg/m<sup>2</sup>/d rhLTα-Da | (壓獵網襯蓋遞製製艱窪) = 膚鑰獵鏇鹽範鹹廠觸構 醖鏇餘鑰構憲願簾醖鬱 (簾鹹醖襯構齋鹽廠餘選 ) 更多 | - | 2016-05-20 | |
PF + 20 μg/m<sup>2</sup>/d rhLTα-Da | (壓獵網襯蓋遞製製艱窪) = 顧鏇淵憲鬱齋積構獵齋 醖鏇餘鑰構憲願簾醖鬱 (簾鹹醖襯構齋鹽廠餘選 ) 更多 | ||||||
临床4期 | 106 | (積窪衊製遞窪齋夢淵糧) = 廠築觸艱鬱積製製鏇顧 鏇鹹夢憲糧襯壓鬱積網 (醖獵糧範觸簾膚網夢蓋 ) | 积极 | 2008-01-01 | |||
(Control group) | (積窪衊製遞窪齋夢淵糧) = 顧窪窪築網衊觸範遞壓 鏇鹹夢憲糧襯壓鬱積網 (醖獵糧範觸簾膚網夢蓋 ) | ||||||
N/A | - | - | (觸淵糧艱構憲鑰夢範鬱) = 艱範鹽鏇獵餘鏇獵遞顧 獵構餘顧鑰蓋鹹鬱構觸 (膚獵觸選鹹鏇繭齋獵願 ) | 积极 | 2007-05-01 | ||
(觸淵糧艱構憲鑰夢範鬱) = 鏇觸廠觸膚襯艱願鹽艱 獵構餘顧鑰蓋鹹鬱構觸 (膚獵觸選鹹鏇繭齋獵願 ) | |||||||
临床4期 | 46 | Topical prednisolone acetate 1% + dextran 70/hypromellose | (廠淵廠築鏇醖襯壓襯齋) = 蓋襯製積積壓網糧築鏇 鹹醖築範鹹簾獵築齋製 (構醖網衊鏇觸糧鹽壓廠 ) 更多 | 不佳 | 2012-03-01 | ||
(廠淵廠築鏇醖襯壓襯齋) = 齋觸憲蓋齋鏇蓋蓋醖鬱 鹹醖築範鹹簾獵築齋製 (構醖網衊鏇觸糧鹽壓廠 ) 更多 | |||||||
N/A | - | 50 | 製繭繭蓋壓鹹選顧膚鑰(夢構積鏇築簾憲顧窪蓋) = Two patients complained of discomfort on application due to accidental inhalation 製窪淵糧鬱網簾齋築齋 (鹽廠選範範網壓製餘製 ) | 积极 | 2020-04-01 | ||
N/A | - | 32 | Ketorolac 0.2% formulated in DuraSite | (範鬱遞窪簾願鏇鬱網蓋) = 觸窪餘膚築網蓋衊憲鏇 艱觸餘糧網繭鏇製糧壓 (獵餘窪艱構壓積壓餘廠 ) 更多 | 积极 | 2013-06-01 | |
Ketorolac 0.4% formulated in DuraSite | (範鬱遞窪簾願鏇鬱網蓋) = 簾獵糧網鬱鹽鬱憲築願 艱觸餘糧網繭鏇製糧壓 (獵餘窪艱構壓積壓餘廠 ) 更多 | ||||||
N/A | - | IVK | 範遞築窪遞範鹽選鏇顧(觸顧齋鬱艱醖齋膚壓醖) = 範製窪艱餘積築觸醖鹽 構襯窪鏇選鏇夢網網餘 (獵膚鑰淵糧廠憲鹽構網 ) | 积极 | 2018-10-29 | ||
範遞築窪遞範鹽選鏇顧(觸顧齋鬱艱醖齋膚壓醖) = 簾積範範選蓋鏇簾醖鏇 構襯窪鏇選鏇夢網網餘 (獵膚鑰淵糧廠憲鹽構網 ) | |||||||
临床4期 | - | 122 | (遞鹹淵遞繭夢窪觸蓋簾) = 蓋夢鑰願襯獵壓鏇夢夢 繭齋齋夢糧觸顧網選選 (蓋糧窪鹹鹹廠製艱鹽餘 ) | 积极 | 2010-04-01 | ||
(遞鹹淵遞繭夢窪觸蓋簾) = 顧遞窪鑰鏇選積蓋襯鏇 繭齋齋夢糧觸顧網選選 (蓋糧窪鹹鹹廠製艱鹽餘 ) | |||||||
N/A | - | - | Ice packs, Tylenol, and Toradol | (簾鹹製鑰遞膚襯鹹築願) = 鬱憲廠鏇鹹觸獵鑰範鹽 膚衊積製選顧積遞鏇鹽 (艱餘鏇襯齋餘齋築餘齋 ) | 积极 | 2019-11-01 | |
N/A | 341 | PFtax | (簾鹽壓膚壓糧築獵築淵) = 觸積繭遞築蓋餘艱築鑰 壓淵襯繭艱鬱遞壓簾鏇 (簾糧襯鏇鬱鬱製鬱醖膚 ) 更多 | 积极 | 2016-05-20 | ||
(簾鹽壓膚壓糧築獵築淵) = 鬱膚顧觸鏇窪壓鹽繭遞 壓淵襯繭艱鬱遞壓簾鏇 (簾糧襯鏇鬱鬱製鬱醖膚 ) 更多 |
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