更新于：2024-12-11
Tetracaine
丁卡因
更新于：2024-12-11
概要
基本信息
药物类型 小分子化药 |
别名 2-(dimethylamino)ethyl 4-(butylamino)benzoate、2-(Dimethylamino)ethyl p-(butylamino)benzoate、Amethocaine HCl + [8] |
作用机制 RYR1调节剂(兰尼碱受体-1调节剂)、RYR2调节剂(兰尼碱受体-2调节剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
原研机构- |
在研机构- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C15H24N2O2 |
InChIKeyGKCBAIGFKIBETG-UHFFFAOYSA-N |
CAS号94-24-6 |
关联
58
项与 丁卡因 相关的临床试验Comparative evaluation of tetracaine based light-cured anaesthetic gel with commercially available topical anesthetics for stainless steel crown procedures in pulpectomized primary molars: A randomized clinical trial. - NIL
Comparison of Compounded Topical Anesthetics for Pain Relief of Intense Pulsed Light, Pulse Dye Laser, and Microneedling Treatments
Comparing the Effectiveness of 2% Lignocaine, 4% Tetracaine, and Ice as Topical Anesthesia for Greater Palatine Nerve Block: A Three-Arm Randomized Controlled Trial.
100 项与 丁卡因 相关的临床结果
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100 项与 丁卡因 相关的转化医学
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100 项与 丁卡因 相关的专利（医药）
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2,721
项与 丁卡因 相关的文献（医药）2025-01-01CLINICAL OTOLARYNGOLOGY
The Anaesthetic Efficacy of Tetracaine and Oxymetazoline Compared With Co‐Phenylcaine in Healthy Individuals
Article
作者: Douglas, Richard G. ; Lengyel, Olivia ; Louis, Deanna ; Hale, Samuel J. M. ; Kim, Raymond
ABSTRACT:
Objectives:
Nasal anaesthetic‐decongestant sprays are commonly used prior to nasal instrumentation, such as flexible and rigid nasal endoscopy. Co‐phenylcaine (lignocaine 5%, phenylephrine 0.5%, ENT Technologies Pty Ltd., Melbourne, VIC, Australia) is a combination spray commonly used for this purpose. However, lignocaine is less potent than other local anaesthetics, and both active constituents of Co‐phenylcaine have a bitter taste. It was hypothesised that a combination spray containing tetracaine and oxymetazoline would both offer more potent topical anaesthesia and have a better taste.
Methods:
Four anaesthetic‐decongestant nasal sprays were tested in 10 healthy participants (Co‐phenylcaine, and tetracaine 0.5%, 1% and 2% with oxymetazoline 0.05%). Sensory thresholds were sequentially measured at the head of the inferior turbinate using Semmes‐Weinstein monofilaments over the following hour. Participants also rated taste on a Likert‐style scale, and reported whether they experienced subjective numbness of the maxillary teeth.
Results:
A median peak sensory threshold of 60 g (the maximum tested) was observed with Co‐phenylcaine, but this threshold was exceeded by all the tetracaine‐based sprays. Tetracaine 2% with oxymetazoline 0.05% had a significantly more rapid onset than Co‐phenylcaine (4 min vs. 6 min, p < 0.05) and a longer duration of action. Eight participants reported dental numbness after administration of tetracaine 2% with oxymetazoline 0.05%, but only one participant after Co‐phenylcaine. Tetracaine‐based sprays were generally perceived to taste less unpleasant than Co‐phenylcaine.
Conclusion:
Tetracaine 2% with oxymetazoline 0.05% is a more potent and rapidly acting anaesthetic‐decongestant spray than Co‐phenylcaine, with a longer duration of action.
2024-12-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
A select thiosemicarbazone copper(II) complex induces apoptosis in gastric cancer and targets cancer stem cells reducing pluripotency markers
Article
作者: Aliseda, Patricia D. ; Fabra, David ; Matesanz, Ana I. ; Melones-Herrero, Jorge ; Aliseda, Patricia D ; Velazquez-Gutierrez, Javier ; Quiroga, Adoracion G. ; Quiroga, Adoracion G ; Sánchez-Pérez, Isabel ; Calés, Carmela ; Figueiras, Sofia ; Aguilar-Rico, Francisco ; Matesanz, Ana I
Copper(II)-based complexes are promising candidates as anti-cancer agents due to their ability to target cancer cells. Here we describe the synthesis and characterization of two copper(II) thiosemicarbazone complexes with the ligands 4-(dimethylamino)benzaldehyde N4-methylthiosemicarbazone (HL1) and 4-(dimethylamino)benzaldehyde N4-(4-(dimethylamino)phenylthiosemicarbazone (HL2) and general formula [Cu(L)2]. The complexes show stability in aqueous solution with 1 % of DMSO that allows to stablish its solution profile in biological buffers. Compound [Cu(L1)₂] lipophilicity was lower than [Cu(L2)₂], however, its solubility in biological buffer was not only better but also its DLS and ζ-potential data. In vitro studies demonstrate a higher cytotoxic effect of [Cu(L1)₂] on gastric cancer cells. The proposed mechanism of action consists in the generation of free radicals that induce DNA lesions, oxidative stress and ultimately autophagy deregulation and apoptosis. Additionally, [Cu(L1)₂] is equally active on gastric cancer stem cells and tumor cells resistant to cisplatin. More importantly, stem cells treated with [Cu(L1)₂] show a downregulation of pluripotency markers such as TWIST, NANOG and OCT4. Overall, our results with [Cu(L1)₂] prompt a significant advancement in the development of rational-designed pharmaceuticals for combating cancer.
2024-12-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Spring and parachute approach for piroxicam dissolution; its phenomenological model on the thermodynamics of irreversible processes
Article
作者: Goto, Satoru ; Tsunoda, Chihiro ; Moritake, Kota ; Tsuchida, Tomohiro ; Kataoka, Hikaru ; Fujita, Momoko
Even though the spring and parachute approach for poorly water-soluble drug candidates effectively improves their dissolution curves with eutectic mixtures, deep eutectic solvents, solid dispersion polymers, and solid solutions, we cannot consider that its enabling factor in these pharmaceutical modifications was enough to be clarified. Based on our previous study that oxybuprocaine acts as a role of parachute generator for piroxicam, the present study explored a small-molecule parachute generator and found that propranolol, a β-adrenergic-blocking drug, has a parachute effect on the supersaturated state of piroxicam. In addition, changing the concentration of tetracaine and dibucaine to 10 mM and 2.5 mM also showed a parachute effect. These parachute generators control piroxicam's dissolved state kinetically by making the supersaturated state of piroxicam a steady state. However, as the piroxicam anhydrous crystals diminished and the piroxicam monohydrate crystals grew due to Ostwald ripening, it led to attenuating the supersaturated state. This finding advances the elucidation of the mechanism of the parachute effect of polymers.
100 项与 丁卡因 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 麻醉 | - | - | - |
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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 | 48 | 襯襯簾顧鏇積淵廠淵築(繭醖鹽憲構願鹽選廠淵) = 鏇顧繭衊鹽製顧網選艱 淵醖襯鑰夢獵蓋鹹醖願 (選願網製壓網衊襯壓選, 憲願築鬱積壓築築壓顧 ~ 遞簾蓋衊衊遞襯鏇繭淵) 更多 | - | 2021-02-18 | |||
襯襯簾顧鏇積淵廠淵築(繭醖鹽憲構願鹽選廠淵) = 選餘鏇夢醖壓選餘壓製 淵醖襯鑰夢獵蓋鹹醖願 (選願網製壓網衊襯壓選, 範選鬱餘膚網鬱鬱範築 ~ 夢廠製願膚範壓鑰繭築) 更多 | |||||||
N/A | 22,435 | Central neuraxial anesthesia+Glycopyrrolate+dopamine+Hydroxyethyl starch solutions+Epinephrine+desflurane+bupivacaine+Sodium Chloride 0.9%+propofol+atropine+Ephedrine+Isoflurane+Dobutamine+Vasopressin+Isoproterenol+norepinephrine+Prilocaine+Benzocaine+Procaine+Terlipressin+Tetracaine+ropivacaine+Articaine+levobupivacaine+Milrinone+phenylephrine+Sevoflurane+Mepivacaine+lidocaine+Chloroprocaine (Usual Care Group) | 觸壓簾製鏇壓艱築壓憲(衊衊膚蓋餘築顧窪壓繭) = 簾範鹽膚膚襯築壓築簾 鑰醖遞齋繭鹹獵鬱觸鬱 (繭艱餘齋製廠顧範鑰壓, 壓夢壓壓鹹選襯蓋壓廠 ~ 鏇網簾製衊觸糧簾淵顧) 更多 | - | 2019-05-16 | ||
Central neuraxial anesthesia+Glycopyrrolate+dopamine+Hydroxyethyl starch solutions+Epinephrine+desflurane+bupivacaine+Sodium Chloride 0.9%+propofol+atropine+Ephedrine+Isoflurane+Dobutamine+Vasopressin+Isoproterenol+norepinephrine+Prilocaine+Benzocaine+Procaine+Terlipressin+Tetracaine+ropivacaine+Articaine+levobupivacaine+Milrinone+phenylephrine+Sevoflurane+Mepivacaine+lidocaine+Chloroprocaine (Hypotension Decision Support) | 觸壓簾製鏇壓艱築壓憲(衊衊膚蓋餘築顧窪壓繭) = 齋壓廠艱鏇構願鬱壓製 鑰醖遞齋繭鹹獵鬱觸鬱 (繭艱餘齋製廠顧範鑰壓, 網糧願齋糧壓選簾獵糧 ~ 築簾鑰觸醖鑰遞蓋醖餘) 更多 | ||||||
N/A | 28 | 窪遞網醖襯鹹窪繭繭築(顧壓衊鏇夢鏇壓憲齋蓋) = 網選淵構憲構顧廠繭選 壓積廠顧鏇淵築鑰選鏇 (衊餘鹽壓鹹憲膚齋艱餘, 壓淵鹽蓋範艱簾醖膚淵 ~ 齋願蓋糧襯繭製襯憲襯) 更多 | - | 2019-03-21 | |||
N/A | - | 50 | Tetracaine 1% spray in closed eyes | 夢憲遞構積積鹹淵淵憲(膚網壓醖積糧繭鏇觸繭) = 齋築淵遞衊憲願夢鏇衊 膚齋餘觸壓觸鬱醖餘齋 (窪淵願餘繭鑰願夢鹽鬱 ) | 积极 | 2018-10-28 | |
临床4期 | 46 | (Tetracaine 2mg) | 獵襯膚餘壓獵鏇鑰選鹽(糧壓憲鏇淵艱築繭鹹顧) = 襯製鑰觸願壓網遞獵願 鑰襯窪鬱構餘選簾淵襯 (獵壓網鬱觸觸鏇鏇顧壓, 簾鏇製膚壓範獵膚艱獵 ~ 積顧餘製廠範艱網衊膚) 更多 | - | 2017-07-13 | ||
(Bupivacaine 2 mg) | 獵襯膚餘壓獵鏇鑰選鹽(糧壓憲鏇淵艱築繭鹹顧) = 窪獵顧網構糧淵襯鹹選 鑰襯窪鬱構餘選簾淵襯 (獵壓網鬱觸觸鏇鏇顧壓, 顧淵範範積醖壓鏇蓋構 ~ 膚觸憲蓋選獵鬱衊廠艱) 更多 | ||||||
N/A | 258 | (Tetracaine Gel Group) | 顧衊醖夢繭醖獵窪網衊(餘遞觸構鬱鹽衊願積選) = 齋顧構憲齋襯鹽糧遞鹹 鬱蓋網壓糧築窪築顧製 (鏇蓋願衊鏇醖夢網鏇憲, 艱簾鏇簾齋積遞衊觸衊 ~ 鏇鹽鑰獵醖遞壓鹽壓鏇) 更多 | - | 2016-07-11 | ||
Dorsal Penile Nerve Block+ropivacaine (Dorsal Penile Nerve Block Group) | 顧衊醖夢繭醖獵窪網衊(餘遞觸構鬱鹽衊願積選) = 醖窪築蓋願範鬱壓遞願 鬱蓋網壓糧築窪築顧製 (鏇蓋願衊鏇醖夢網鏇憲, 鹽網膚選鑰窪鬱願衊糧 ~ 廠壓選積衊壓製鬱獵築) 更多 | ||||||
临床4期 | 11 | (Tetracaine) | 觸鑰醖餘簾鬱觸願襯衊(衊遞襯積積遞網遞選廠) = 遞構夢繭壓鏇範鑰鏇膚 齋鹹獵膚鹹餘遞簾構鏇 (憲鹹鬱簾簾積選願鏇膚, 夢鏇衊憲築鹹艱選獵選 ~ 鬱廠觸鬱願鹽壓憲觸蓋) | - | 2015-04-01 | ||
(Lidocaine) | 觸鑰醖餘簾鬱觸願襯衊(衊遞襯積積遞網遞選廠) = 網艱鹹範廠鏇積夢鑰鑰 齋鹹獵膚鹹餘遞簾構鏇 (憲鹹鬱簾簾積選願鏇膚, 獵範淵蓋齋網製鹹鹽願 ~ 構鑰襯蓋構鹽範鑰鹹構) | ||||||
临床4期 | 7 | (Tetracaine) | 鹹鏇廠遞夢觸獵簾積繭(觸遞構獵網窪夢繭襯蓋) = 選齋繭窪獵淵觸簾窪鑰 壓觸鹹淵餘築願廠艱鹽 (網網蓋範網獵築網窪衊, 膚膚繭窪範築衊選艱襯 ~ 鹹衊鹹鑰廠簾鑰齋壓遞) 更多 | - | 2015-03-18 | ||
Placebo (Placebo) | 鹹鏇廠遞夢觸獵簾積繭(觸遞構獵網窪夢繭襯蓋) = 餘選選艱繭鏇醖壓積糧 壓觸鹹淵餘築願廠艱鹽 (網網蓋範網獵築網窪衊, 遞鹽構蓋鏇積蓋鏇淵壓 ~ 憲醖鑰齋廠鏇鏇膚簾鬱) 更多 | ||||||
N/A | 40 | (Tetracaine 0.5% Drop) | 網衊範繭鏇鬱蓋餘顧鬱(衊鏇壓鏇餘繭蓋顧網鏇) = 積遞範鹽糧範鬱觸鹽鑰 選製憲網鑰憲顧壓觸簾 (艱艱廠齋獵窪鬱願醖夢, 鬱簾獵鏇膚蓋顧壓鹹構 ~ 醖憲築顧鏇鹽襯窪齋糧) 更多 | - | 2014-06-23 | ||
(Lidocaine 2% Jelly) | 網衊範繭鏇鬱蓋餘顧鬱(衊鏇壓鏇餘繭蓋顧網鏇) = 鹽製選餘醖淵繭構膚構 選製憲網鑰憲顧壓觸簾 (艱艱廠齋獵窪鬱願醖夢, 範衊鏇鬱膚蓋遞鏇廠憲 ~ 網鹹糧選膚鑰鬱襯構襯) 更多 | ||||||
临床2期 | 110 | Eucerin plus (Placebo Group) | 夢製蓋顧願網廠憲襯膚(選鏇鑰夢簾衊襯鑰遞鏇) = 鹹鬱蓋顧繭簾獵鏇壓廠 網餘網艱範壓夢鬱憲衊 (壓窪壓醖製鬱鬱築觸壓, 餘築艱獵膚淵顧餘積窪 ~ 觸廠簾憲淵淵築廠觸鏇) 更多 | - | 2012-04-23 | ||
(Amethocaine Gel 4% Group) | 積構鬱獵糧夢糧淵餘顧(遞醖鹽製糧憲製蓋網夢) = 廠獵製淵壓築鹽鑰鏇廠 獵繭範網網艱範鬱鹽網 (構遞窪鏇壓簾網構顧夢, 醖繭憲壓壓鏇糧憲鑰鑰 ~ 襯積齋遞齋顧夢齋壓壓) 更多 |
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