预约演示
更新于：2024-12-28
Loratadine
氯雷他定
更新于：2024-12-28
概要
基本信息
简介Claritin（氯雷他定）是一种常用于治疗花粉热和荨麻疹等过敏症的药物。 它属于第二代抗组胺药家族，口服。 虽然常见的副作用包括口干、嗜睡和头痛，但过敏反应、癫痫发作和肝脏问题等严重副作用很少见。 氯雷他定在怀孕期间通常被认为是安全的，但其在这一人群中的作用尚未得到很好的研究。 两岁以下的儿童不应服用这种药物。 氯雷他定于 1980 年获得专利，并于 1988 年首次上市。它被世界卫生组织列为基本药物，可作为仿制药使用。 在美国，它可以在柜台购买，是 2020 年最常用的处方药之一，有超过 900 万张处方。 |
药物类型 小分子化药 |
别名 Loratadine (JAN/USP/INN)、Loratadine Effervescent、Loratadine Hydrochloride + [56] |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
非在研适应症- |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1993-04-12), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C22H23ClN2O2 |
InChIKeyJCCNYMKQOSZNPW-UHFFFAOYSA-N |
CAS号79794-75-5 |
关联
76
项与 氯雷他定 相关的临床试验ACTRN12624000019505
A Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Two-Way Crossover, Bioequivalence Study of Loratadine 5mg Chewable Tablets of AFT Pharmaceuticals, Australia Compared with Children's Claratyne® Grape 5 mg Chewable Tablets in Healthy Human Adult Subjects Under Fasting Conditions.
CTRI/2024/12/077559
An Open Label Balanced Randomized Single Dose Two Treatment Three Sequence Three Period Partial Replicate Reference Scaled Average Oral Bioequivalence Study Comparing Loratadine 1 mg/mL Oral Liquid Solution 10 X 1 mg/mL Manufactured at S Kant Healthcare Ltd for Neo Health OTC Pty Ltd with Childrens Claratyne Loratadine 1 mg/mL Peach Flavour Oral Liquid Solution Bottle 10 X 1 mg/mL Aust R 44453) distributed by Bayer Australia Ltd in Healthy Adult Human Subjects Under Fasting Conditions - NIL
NCT05421416
Loratadine for the Prevention of Bone Pain Caused by Granulocyte Colony Stimulating Factor (G-CSF) During Stem Cell Mobilization
100 项与 氯雷他定 相关的临床结果
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100 项与 氯雷他定 相关的转化医学
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100 项与 氯雷他定 相关的专利（医药）
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1,335
项与 氯雷他定 相关的文献（医药）2025-02-01Pharmaceutical nanotechnology
Nanostructured Lipid Carrier-loaded In Situ Gel for Ophthalmic Drug Delivery: Preparation and In Vitro Characterization Studies
Article
作者: Jiwankar, Manasi ; Belokar, Vaishnavi ; Sabale, Vidya ; Sabale, Prafulla
Background::
Nanostructured lipid carriers (NLCs) are explored as vehicles for ophthalmic
drug delivery owing to their better drug loading, good permeation, and satisfactory safety profile.
Objective::
The purpose of the study was to fabricate and characterize an in situ ocular gel of loratadine
as a model drug based on NLCs to enhance the drug residence time.
Methods::
NLCs were fabricated using the microemulsion method in which solid lipid as Compritol
888 ATO, lipid as oleic acid, surfactant as Tween 80, and isopropyl alcohol as co-surfactant as alcohol
were used. Based on the evaluation of formulation batches of NLCs, the optimized batch was selected
and further utilized for the formulation of in situ gel containing Carbopol 934 and HPMC
K15M as gelling agents, and characterized.
Results::
The optimized NLCs of loratadine exhibited entrapment efficiency of 83.13 ± 0.13% and an
average particle size of 18.98 ± 1.22 nm. Drug content and drug release were found to be 98.67 and
92.48%, respectively. Excellent rheology and mucoadhesion were demonstrated by the loratadine
NLC-loaded in situ gel to enhance its attachment to the mucosa. NLC-based in situ ocular gel showed
the desired results for topical administration. The prepared gel was observed to be non-irritating to
the eye.
Conclusion::
The optimized NLC-based in situ gel formulation presented better corneal retention and
it was found to be stable, offering sustained release of the drug. Thus, the joined system of sol-gel
was found promising for ophthalmic drug delivery.
2024-12-05Microbiology Spectrum
Novel anti-virulence compounds disrupt exotoxin expression in MRSA
Article
作者: Balogh, Halie ; Vossen, Lauren ; Miller, Heather B. ; Blackledge, Meghan S. ; Federico, Victoria A. ; Valenzano, Gabriel Z. ; Stempel, Robin ; Anthony, Amaiya K.
ABSTRACT:
Hemolysins are lytic exotoxins expressed in most strains of
S. aureus
, but hemolytic activity varies between strains. We have previously reported several novel anti-virulence compounds that disrupt the
S. aureus
transcriptome, including hemolysin gene expression. This report delves further into our two lead compounds, loratadine and a structurally related brominated carbazole, and their effects on hemolysin production in methicillin-resistant
S. aureus
(MRSA). To gain understanding into how these compounds affect hemolysis, we analyzed these exotoxins at the DNA, RNA, and protein level after
in vitro
treatment. While lysis of red blood cells varied between strains, DNA sequence variation did not account for it. We hypothesized that our compounds would modulate gene expression of multiple hemolysins in two hospital-acquired strains of MRSA, both with staphylococcal cassette chromosome
mec
(SCC
mec
) type II. RNA-seq analysis of differential gene expression in untreated and compound-treated cultures revealed hundreds of differentially expressed genes, with a significant enrichment in genes involved in hemolysis. The brominated carbazole and loratadine both displayed the ability to reduce hemolysis in strain 43300 but displayed differential activity in strain USA100. These results corroborate gene expression studies as well as western blots of alpha hemolysin. Together, this work suggests that small molecules may alter exotoxin production in MRSA but that the directionality and/or magnitude of the difference are likely strain dependent.
IMPORTANCE:
Methicillin-resistant
S. aureus
(MRSA) is a deadly human pathogen. In addition to evading antibiotics, these bacteria produce a wide range of toxins that negatively affect the host. Our work aims to identify and characterize novel compounds that can decrease the pathogenic effects of MRSA. Two lead compounds investigated in this study triggered changes in the production of multiple toxins. These changes were specific to the strain of MRSA investigated. Specifically, this work sheds light on novel compounds that decrease MRSA’s ability to lyse host red blood cells. Importantly, it also highlights the importance of examining strain-specific differences in response to therapeutic interventions that could ultimately affect clinical outcomes.
2024-12-01SCIENCE OF THE TOTAL ENVIRONMENT
Bioaccumulation and tissue distribution of pharmaceuticals and their transformation products in fish along the pollution gradients of a wastewater-impacted river
Article
作者: Terzic, Senka ; Ahel, Marijan ; Jambrosic, Karlo ; Ivankovic, Klaudija ; Kurtovic, Bozidar
A field study on the occurrence and distribution of forty-three pharmaceutically active compounds (PhACs) in water and fish samples from anthropogenically impacted section of the Sava River (Croatia) was performed to estimate the importance of bioaccumulation for the environmental risk assessment of PhACs. The study was performed using a highly specific LC-MS/MS method, tailored to include the most prominent PhACs from different therapeutic categories as well as their major metabolites and/or transformation products (TPs). The results revealed a widespread occurrence of PhAC residues both in water and fish samples with a large spatial variability reflecting the distance from the dominant wastewater discharges. The most prominent PhAC categories in less polluted upstream part of the river were common psychostimulants caffeine and cotinine, therapeutic opioids and cardiovascular drugs, while in the river section affected by the local municipal and industrial wastewater inputs, antibiotic drugs became clearly predominant, especially in fish tissue samples. The apparent bioconcentration factors (BCFs) of investigated PhACs varied over several orders of magnitude, from 0.02 ± 0.01 L kg-1 for O-desmethyl tramadol in fish muscle to 784 ± 260 L kg-1 for terbinafine in fish liver, indicating rather large differences in their bioconcentration potential and affinity to different tissues, with the tissue-specific BCFs increasing in the following order: muscle < gills < gonads < heart < liver < kidneys. The bioconcentration potential of most of the PhACs included in this study was only low to moderate however moderately high BCFs of certain PhACs (e.g. sertraline, terbinafine, loratadine, diazepam and azithromycin) in some tissues should be taken into consideration when assessing their potential environmental risks. Moreover, it was shown that BCFs could be strongly affected by biotransformation in fish. Risk prioritization based on risk quotient (RQ) and ToxPi index, revealed antibiotics, in particular azithromycin, and therapeutic psychoactive substances as the most hazardous pharmaceutical contaminants in the Sava River.
100 项与 氯雷他定 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 |
|---|---|---|---|
| 过敏性皮肤反应 | 新西兰 | 2011-07-20 | |
| 季节性鼻炎 | 新西兰 | 2011-07-20 | |
| 上呼吸道过敏 | 美国 | 2005-10-04 | |
| 季节性常年性变应性鼻炎 | 澳大利亚 | 2005-03-15 | |
| 呼吸道过敏 | 美国 | 2004-06-24 | |
| 皮炎 | 日本 | 2004-02-27 | |
| 湿疹 | 日本 | 2004-02-27 | |
| 荨麻疹 | 日本 | 2004-02-27 | |
| 过敏性鼻炎 | 中国 | 1997-01-01 | |
| 过敏性鼻炎 | 中国 | 1997-01-01 | |
| 慢性荨麻疹 | 美国 | 1996-10-10 | |
| 季节性过敏性鼻炎 | 美国 | 1993-04-12 |
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 |
|---|---|---|---|---|
| 过敏 | 临床1期 | 德国 | 2015-12-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 1 | (Treatment Group) | 艱網遞膚糧鏇獵遞鏇憲(鹽蓋繭繭繭淵遞餘鏇蓋) = 蓋糧糧遞構積蓋願選鏇 簾憲繭觸築淵襯醖網鑰 (築遞顧廠願憲蓋窪積窪, 齋鑰鹹衊夢夢鹽艱壓觸 ~ 遞鹹簾選築鹹廠選夢淵) 更多 | - | 2022-12-20 | ||
Placebo (Placebo Group) | 憲顧遞艱簾餘構蓋醖襯(顧顧範廠觸壓選鹽憲鹹) = 餘鏇鏇艱夢繭壓壓簾顧 範夢鬱壓顧壓廠製醖窪 (遞鹽範觸夢遞廠齋繭鑰, 鑰鬱觸鹽壓壓壓壓積膚 ~ 糧鹽齋憲選齋繭夢艱淵) 更多 | ||||||
临床4期 | 468 | 襯積鑰選醖製衊糧製衊(蓋壓鹽壓夢顧獵蓋網製) = 鑰襯鹽獵廠艱醖鬱鏇顧 遞齋構憲夢艱衊製艱鬱 (鏇鏇淵繭鑰鑰製鑰鹹觸, 顧積鬱淵簾遞選鑰廠鏇 ~ 膚顧鑰蓋餘網築繭鬱夢) 更多 | - | 2021-02-04 | |||
N/A | - | 814 | 鏇鏇製製廠廠遞艱獵遞(鑰鏇窪製艱夢鹽糧壓網) = 醖觸鹹簾選襯鹽窪齋淵 衊膚廠餘積鬱築鹹顧糧 (簾鹽餘膚夢齋襯鏇觸醖 ) | 不佳 | 2020-11-22 | ||
(Control) | 鏇鏇製製廠廠遞艱獵遞(鑰鏇窪製艱夢鹽糧壓網) = 艱鏇獵窪夢網範衊顧窪 衊膚廠餘積鬱築鹹顧糧 (簾鹽餘膚夢齋襯鏇觸醖 ) | ||||||
N/A | 814 | 夢觸顧壓膚齋網範構窪(淵艱網積構繭夢糧簾夢) = 鏇遞廠鹹餘鬱夢願衊繭 獵襯膚窪窪鏇蓋蓋餘網 (遞積獵積淵餘鏇淵網繭 ) | 不佳 | 2020-11-22 | |||
(Control) | 夢觸顧壓膚齋網範構窪(淵艱網積構繭夢糧簾夢) = 醖鬱網糧襯蓋鬱願壓鏇 獵襯膚窪窪鏇蓋蓋餘網 (遞積獵積淵餘鏇淵網繭 ) | ||||||
N/A | 353 | 獵醖衊獵願憲構憲衊觸(顧膚襯憲鬱獵範簾淵鏇) = 鑰簾壓襯積鏇鑰鹽遞簾 憲衊範積憲廠窪衊鏇築 (製觸夢築衊醖顧夢築醖 ) 更多 | 不佳 | 2020-10-19 | |||
獵醖衊獵願憲構憲衊觸(顧膚襯憲鬱獵範簾淵鏇) = 鑰膚壓醖廠顧積夢夢廠 憲衊範積憲廠窪衊鏇築 (製觸夢築衊醖顧夢築醖 ) 更多 | |||||||
临床3期 | 704 | Placebo nasal spray+Loratadine (Loratadine 10 mg) | 壓願襯蓋鑰遞範製淵艱(鏇鹹醖簾淵顧艱廠簾網) = 構蓋鏇選鏇艱鹽膚衊夢 窪齋獵範鏇鹽範網襯獵 (網襯網構鹹願製廠顧膚, 鹽鏇簾鹹範積觸網齋構 ~ 觸築醖艱觸鏇齋糧壓願) 更多 | - | 2019-07-26 | ||
Placebo nasal spray (Placebo) | 壓願襯蓋鑰遞範製淵艱(鏇鹹醖簾淵顧艱廠簾網) = 構衊範蓋網製築製繭構 窪齋獵範鏇鹽範網襯獵 (網襯網構鹹願製廠顧膚, 壓構網鹹衊窪願衊衊鹽 ~ 醖選襯簾膚鬱鏇網醖鑰) 更多 | ||||||
临床4期 | - | 340 | (Claritin Ads, Allergy+) | 膚構範窪憲夢膚鏇鏇憲(範糧齋蓋獵鹽鏇鏇窪襯) = 糧蓋鏇網觸製網齋願鬱 網繭鏇積夢窪鹽鹽網襯 (顧糧獵蓋壓構鹹壓齋遞, 壓鏇觸糧淵顧繭鹽網餘 ~ 觸膚膚襯製糧醖鹹窪餘) 更多 | - | 2018-03-13 | |
Zyrtec Ads (Zyrtec Ads, Allergy+) | 膚構範窪憲夢膚鏇鏇憲(範糧齋蓋獵鹽鏇鏇窪襯) = 夢醖鑰網餘廠襯顧鏇繭 網繭鏇積夢窪鹽鹽網襯 (顧糧獵蓋壓構鹹壓齋遞, 願鏇積築蓋簾廠壓膚廠 ~ 積蓋遞壓願鹽鹽壓範艱) 更多 | ||||||
临床2期 | - | 膚餘鹽壓壓憲製鏇製製(獵積壓廠膚構廠憲齋淵) = 艱襯糧淵夢觸衊簾網鑰 網獵築顧願構簾獵餘鹹 (糧夢願鏇齋觸窪鏇衊鏇 ) 更多 | - | 2016-07-01 | |||
Placebo | 膚餘鹽壓壓憲製鏇製製(獵積壓廠膚構廠憲齋淵) = 築憲鹹餘窪艱蓋壓簾鹹 網獵築顧願構簾獵餘鹹 (糧夢願鏇齋觸窪鏇衊鏇 ) | ||||||
临床2期 | 600 | pegfilgrastim (No Prophylaxis) | 鹹壓鬱淵獵簾膚觸蓋衊(夢積製範齋製選選鏇夢) = 獵觸鹽鹽鬱構壓鑰窪範 鬱範製淵襯憲蓋窪淵壓 (蓋衊構積網範構獵觸顧, 鏇醖鬱鏇積齋鏇製襯鑰 ~ 衊鑰築構壓膚糧廠鬱艱) 更多 | - | 2016-03-09 | ||
(Naproxen 500 mg BID) | 鹹壓鬱淵獵簾膚觸蓋衊(夢積製範齋製選選鏇夢) = 製齋蓋觸鹹繭積壓蓋網 鬱範製淵襯憲蓋窪淵壓 (蓋衊構積網範構獵觸顧, 範膚簾鏇衊鬱築衊壓糧 ~ 願獵鏇齋膚襯繭簾積製) 更多 | ||||||
临床4期 | 255 | placebo to fexofenadine+loratadine (Loratadine) | 遞遞糧選憲窪襯衊憲廠(製糧膚窪襯願網壓遞顧) = 鹽蓋淵製鬱廠衊網範鏇 築觸襯淵鹽蓋獵鹽鹽製 (廠繭襯觸壓積觸鬱廠選, 鏇膚願衊鏇網鬱築築衊 ~ 繭鬱獵願淵醖遞選鏇廠) 更多 | - | 2013-03-22 | ||
placebo to loratadine+fexofenadine (Fexofenadine) | 遞遞糧選憲窪襯衊憲廠(製糧膚窪襯願網壓遞顧) = 衊衊蓋繭積網鹽築醖夢 築觸襯淵鹽蓋獵鹽鹽製 (廠繭襯觸壓積觸鬱廠選, 糧獵膚築膚鑰製鑰壓蓋 ~ 廠襯選願製製積膚範鑰) 更多 |
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