更新于：2024-06-29
Epinastine Hydrochloride
盐酸依匹斯汀
更新于：2024-06-29
概要
基本信息
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C16H16ClN3 |
InChIKeyVKXSGUIOOQPGAF-UHFFFAOYSA-N |
CAS号108929-04-0 |
关联
48
项与 盐酸依匹斯汀 相关的临床试验0.1%STN1011403滴眼液治疗过敏性结膜炎的多中心随机评价者盲态阳性对照试验
0.05%盐酸依匹斯汀滴眼液治疗中国过敏性结膜炎患者的有效性和安全性的随机、双盲、阳性药平行对照、多中心临床研究
A Phase 3, Multicenter, Randomized, Double-masked, Active Controlled Study to Evaluate the Efficacy and Safety of Epinastine Hydrochloride Eye Drops 0.05% in the Treatment of Chinese Seasonal Allergic Conjunctivitis Patients
100 项与 盐酸依匹斯汀 相关的临床结果
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100 项与 盐酸依匹斯汀 相关的转化医学
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100 项与 盐酸依匹斯汀 相关的专利（医药）
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202
项与 盐酸依匹斯汀 相关的文献（医药）2024-04-01Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics
Epinastine Cream: A Novel Once-Daily Therapeutic Agent for Allergic Conjunctivitis
Article
作者: Ogura, Naoki ; Kato, Masatomo ; Fujisawa, Koushi
Purpose: To investigate the in vivo efficacy of epinastine cream in type I allergic models. Methods: The dose, timing, and antiallergic effect of epinastine cream on the conjunctiva were evaluated postapplication to the eyelid skin of guinea pigs with histamine- or ovalbumin-induced allergic conjunctivitis. Additionally, we assessed its antiallergic effects on the skin postapplication to the dorsal skin of guinea pigs with ovalbumin-induced passive cutaneous anaphylaxis. Efficacy was estimated by determining the amount of dye that leaked from conjunctival or dorsal skin tissue vessels as a measure of vascular permeability, scoring the severity of allergic symptoms, and observing the scratching behaviors using clinical parameters. Results: In the histamine-induced conjunctivitis model, epinastine cream strongly inhibited conjunctival vascular permeability in a dose-dependent manner. The inhibitory effect of 0.5% epinastine cream 24 h postapplication was significantly higher than that of 0.1% epinastine hydrochloride ophthalmic solution 8 h postadministration. Additionally, the 0.5% epinastine cream inhibited conjunctival vascular permeability 15 min postapplication, and the effect was sustained over 24 h. Furthermore, the 0.5% epinastine cream effectively suppressed clinical symptom scores and exhibited ameliorated scratching bouts in conjunctival allergic reactions in the experimental allergic conjunctivitis model. Additionally, it significantly inhibited vascular permeability in skin allergic reactions in the passive cutaneous anaphylaxis model. Conclusions: The results suggest that epinastine cream is a strong, long-lasting, and skin-penetrating inhibitor of type I allergic reactions. The 0.5% epinastine cream applied once daily could be a promising, potent, and long-acting therapeutic agent for allergic conjunctivitis.
2024-01-01Forensic toxicology
Effects of temperature, humidity, light, and soil on drug stability in hair: a preliminary study for estimating personal profiles using micro-segmental analysis of corpse hair
Article
作者: Kanamori, Tatsuyuki ; Okada, Yuki ; Yamamuro, Tadashi ; Tsujikawa, Kenji ; Iwata, Yuko T ; Miyaguchi, Hajime ; Segawa, Hiroki ; Kuwayama, Kenji
Abstract:
Purpose:
Micro-segmental hair analysis (MSA), which enables detailed measurement of the distribution of drugs in a single hair strand, is useful for examining the day of death and drug use history of a person. However, corpses are often found in severe environments, such as soil and freezers, which affect the drug contents in hair. Therefore, we examined the effects of temperature, humidity, light, and soil on drug stability in hair as a preliminary study to estimate personal profiles using MSA of corpse hair.
Methods:
Four hay-fever medicines (fexofenadine, epinastine, cetirizine, and desloratadine) were used as model drugs to evaluate drug stability in hair. Reference hair strands consistently containing the four medicines along the hair shaft were collected from patients with hay-fever who ingested the medicines daily for 4 months. The hair strands were placed in chambers with controlled temperatures (− 30 to 60 °C) and relative humidities (ca. 18 % and > 90 %), exposed to light (sunlight and artificial lights) or buried in soil (natural soil and compost).
Results:
Sunlight and soil greatly decomposed the hair surfaces and decreased the drug contents in hair (up to 37 %). However, all analytes were successfully detected along the hair shaft, reflecting the intake history, even when the hair was exposed to sunlight for 2 weeks and buried in the soil for 2 months.
Conclusions:
Although the exposure to sunlight and storage in soil for long times made drug-distribution analysis difficult, MSA could be applied even to hair strands collected from corpses left in severe environments.
2023-09-01Neurobiology of learning and memory
Roles of octopamine neurons in the vertical lobe of the mushroom body for the execution of a conditioned response in cockroaches.
Article
作者: Matsumoto, Yukihisa ; Mizunami, Makoto ; Matsumoto, Chihiro Sato
Aminergic neurons mediate reward signals in mammals and insects. In crickets, we showed that blockade of synaptic transmission from octopamine neurons (OANs) impairs conditioning of an odor (conditioned stimulus, CS) with water or sucrose (unconditioned stimulus, US) and execution of a conditioned response (CR) to the CS. It has not yet been established, however, whether findings in crickets can be applied to other species of insects. In this study, we investigated the roles of OANs in conditioning of salivation, monitored by activities of salivary neurons, and in execution of the CR in cockroaches (Periplaneta americana). We showed that injection of epinastine (an OA receptor antagonist) into the head hemolymph impaired both conditioning and execution of the CR, in accordance with findings in crickets. Moreover, local injection of epinastine into the vertical lobes of the mushroom body (MB), the center for associative learning and control of the CR, impaired execution of the CR, whereas injection of epinastine into the calyces of the MB or the antennal lobes (primary olfactory centers) did not. We propose that OANs in the MB vertical lobes play critical roles in the execution of the CR in cockroaches. This is analogous to the fact that midbrain dopamine neurons govern execution of learned actions in mammals.
100 项与 盐酸依匹斯汀 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 |
|---|---|---|---|
| 变应性结膜炎 | 日本 | 2013-09-20 | |
| 银屑病 | 中国 | 2000-06-16 | |
| 哮喘 | 日本 | 1994-04-01 | |
| 湿疹 | 日本 | 1994-04-01 | |
| 痒疹 | 日本 | 1994-04-01 | |
| 瘙痒 | 日本 | 1994-04-01 | |
| 过敏性鼻炎 | 日本 | 1994-04-01 | |
| 荨麻疹 | 日本 | 1994-04-01 |
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 |
|---|---|---|---|---|
| 季节性过敏性结膜炎 | 临床3期 | 中国 | 2023-03-10 | |
| 季节性过敏性鼻炎 | 临床3期 | - | 2007-12-18 | |
| 特应性皮炎 | 临床3期 | - | 2001-06-01 | |
| 常年性变应性鼻炎 | 临床3期 | - | 2000-05-01 |
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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3期 | 87 | (Epinastine (DE-114) Ophthalmic Solution) | 蓋夢憲壓壓齋艱繭築蓋(蓋繭積製觸衊積壓壓襯) = 衊襯構憲鹹齋簾遞艱鹽 糧齋鬱醖淵顧淵觸糧構 (鏇餘廠衊齋鑰醖選醖顧, 餘鑰繭獵範餘鹽選夢獵 ~ 廠艱觸廠願網願獵鑰夢) 更多 | - | 2014-11-05 | ||
Placebo (Placebo Ophthalmic Solution) | 蓋夢憲壓壓齋艱繭築蓋(蓋繭積製觸衊積壓壓襯) = 鏇餘鹹顧艱壓憲蓋襯積 糧齋鬱醖淵顧淵觸糧構 (鏇餘廠衊齋鑰醖選醖顧, 鏇艱獵淵艱醖淵觸鏇憲 ~ 窪蓋襯淵鬱繭窪積遞鬱) 更多 | ||||||
临床3期 | 130 | 顧簾鬱憲廠鬱鏇繭觸網(築壓積糧襯鑰膚鹽齋艱) = 淵網網顧餘憲鏇觸夢糧 網製鬱網艱鏇鹹繭獵構 (獵鏇蓋觸鑰觸獵遞餘糧, 選壓廠壓範廠鑰壓衊選 ~ 築蓋糧鏇構廠範積膚繭) 更多 | - | 2014-09-23 | |||
临床4期 | 79 | (Elestat) | 鑰築衊憲遞齋窪齋簾糧(衊願鏇餘願遞夢網獵醖) = 膚蓋鑰積醖簾艱餘鹹蓋 積顧顧艱顧獵繭夢鬱鑰 (壓積願憲襯鬱鏇憲願蓋, 蓋願鑰夢衊餘夢繭膚構 ~ 憲鹽醖繭衊構遞顧齋壓) 更多 | - | 2009-05-27 | ||
(Pataday) | 鑰築衊憲遞齋窪齋簾糧(衊願鏇餘願遞夢網獵醖) = 鹽醖夢築選廠衊襯衊餘 積顧顧艱顧獵繭夢鬱鑰 (壓積願憲襯鬱鏇憲願蓋, 憲鏇壓醖壓齋鑰獵廠襯 ~ 構艱鹹鏇淵憲鬱製鬱築) 更多 | ||||||
N/A | 99 | Epinastine HCl 0.05% | 願觸憲簾鹹觸獵壓膚糧(繭鏇築齋築觸遞獵壓襯) = Three (5.9%) epinastine patients and 7 (14.6%) ketotifen patients experienced adverse events. Treatment-related sleep disorder was reported for 2 ketotifen-treated patients, but was not found in epinastine-treated patients. 窪艱構鹹醖網廠齋糧廠 (餘夢夢範醖鹽艱鏇窪獵 ) | - | 2004-05-01 | ||
N/A | - | Epinastine HCl 0.05% | 衊鏇獵積鏇膚願糧壓鹽(簾窪構鏇糧網壓蓋襯夢) = 憲鹹築簾醖簾窪鏇鏇鬱 齋選窪構憲構蓋鹹襯製 (簾衊獵齋夢積鏇鬱廠獵 ) | 积极 | 2003-05-01 | ||
衊鏇獵積鏇膚願糧壓鹽(簾窪構鏇糧網壓蓋襯夢) = 遞憲醖艱鑰獵壓廠遞觸 齋選窪構憲構蓋鹹襯製 (簾衊獵齋夢積鏇鬱廠獵 ) | |||||||
N/A | 14 | 鹹窪繭範鏇衊窪簾鹹窪(願夢繭鑰願淵窪鹽簾鹽) = No adverse events nor any clinically relevant changes in visual acuity, biomicroscopy, ophthalmoscopy, vital signs, physical examination, or laboratory parameters were observed during the study 鬱積鏇觸遞糧構網衊選 (窪願簾蓋選廠繭選遞選 ) | 积极 | 2003-05-01 | |||
N/A | - | - | Epinastine HCl 0.05% | 顧醖觸鑰廠遞簾憲艱鑰(窪膚鹽淵憲醖鑰觸糧壓) = primarily colds/URI, was the most frequent AE reported in 5.0% of epinastine subjects and 8.3% of vehicle subjects 製餘選襯鹽繭憲鹽壓鬱 (觸構獵醖壓膚顧鏇壓蓋 ) | 积极 | 2003-05-01 | |
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