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更新于：2024-12-25
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2024-12-25
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2011-02-25), |
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C30H24KN4O8 |
InChIKeyMIJNRHZSZJLCAG-UHFFFAOYSA-N |
CAS号863031-24-7 |
关联
70
项与 阿齐沙坦酯钾盐 相关的临床试验CTR20243698
美阿沙坦钾片在健康受试者空腹和餐后状态下的随机、开放、单剂量、两制剂、两序列、两周期、交叉生物等效性试验
CTR20243700
美阿沙坦钾片在健康受试者中餐后状态下的开放、随机、交叉生物等效性试验
CTR20243579
美阿沙坦钾片在健康受试者中空腹/餐后状态下的开放、随机、交叉生物等效性试验
100 项与 阿齐沙坦酯钾盐 相关的临床结果
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100 项与 阿齐沙坦酯钾盐 相关的转化医学
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100 项与 阿齐沙坦酯钾盐 相关的专利（医药）
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701
项与 阿齐沙坦酯钾盐 相关的文献（医药）2025-01-01THERIOGENOLOGY
Dexamethasone and azithromycin enhance goat sperm preservation quality by regulating lipid metabolism
Article
作者: Ren, Chunhuan ; Cao, Hongguo ; Zhang, Zijun ; Xu, Yongjie ; Ling, Yinghui ; Sun, Shixin ; Wang, Mingyue ; Shen, Wenzheng ; Wang, Lei
Phospholipase A (PLA) in goat semen aggregates with egg yolk in semen diluent, leading to sperm death. The aim of this study is to address the issue of sperm death caused by the interaction between PLA and egg yolk, and to explore the protective effect and metabolic regulation mechanism of the combination of dexamethasone (DXMS) and azithromycin (AZM) on goat sperm under low temperature conditions. At a low temperature of 4 °C, different concentrations of DXMS were added to semen diluents containing 30 μg/mL AZM to detect the quality of goat sperm. The optimal concentration of DXMS was determined to be 20 μg/mL. On the 5th day of storage, antioxidant capacity, total cholesterol (TC) levels, energy metabolism, and metabolomics analysis were performed on the sperm of the 20 μg/mL DXMS group. The results showed that there was no aggregation caused by the interaction between PLA and egg yolk in the group containing 30 μg/mL AZM at 4 °C. 20 μg/mL DXMS significantly improved sperm motility, plasma membrane integrity, acrosome integrity, glutathione peroxidase (GPX) (P < 0.05), catalase (CAT) (P < 0.01), and superoxide dismutase (SOD) activity (P < 0.01). The content of reactive oxygen species (ROS) and Fe2+ significantly decreased (P < 0.01), while the content of ATP (P < 0.01) and TC (P < 0.05) significantly increased. Through metabolomics analysis, a total of 56 differential metabolites (P < 0.05) were screened, including 5a, 6-Anhydrotetracycline, Betamethasone, and 11-Dehydrocorticosterone, mainly enriched in 8 metabolic pathways (P < 0.05), including steroid hormone biosynthesis, glycerophospholipid metabolism, and choline metabolism in cancer. Among them, 5 metabolic pathways are related to lipid metabolism. The results indicate that AZM effectively inhibits the aggregation of PLA and yolk, and the combination of AZM and DXMS enhances the preservation quality of goat sperm during low-temperature preservation by regulating lipid metabolism.
2025-01-01CARBOHYDRATE POLYMERS
Heparin-azithromycin microparticles show anti-inflammatory effects and inhibit SARS-CoV-2 and bacterial pathogens associated to lung infections
Article
作者: Bettini, Ruggero ; Lalatsa, Aikaterini ; González-Burgos, Elena ; Serrano, D.R. ; Rodríguez, Carmina ; Anaya, Brayan J. ; Dea-Ayuela, María Auxiliadora ; Galiana, Carolina ; Serrano, Dolores R. ; Sanz-Perez, Amadeo ; Tirado, Diego F ; Tirado, Diego F. ; Serrano, Dolores R ; Anaya, Brayan J ; D'Angelo, Davide ; Molina, Gracia
Pulmonary infections are a leading cause of morbidity and mortality worldwide, a situation exacerbated by the COVID-19. Azithromycin (AZM) is used orally to treat pulmonary infections due to its ability to accumulate in lung tissues and immune cells after oral administration. Sulfated polysaccharides, such as heparin, are known to inhibit SARS-CoV-2 entry. This study presents a novel approach focused on developing a dry powder inhaler of AZM-loaded microparticles composed of either heparin or its derivatives. The microparticle formulations exhibited potent antiviral activity against SARS-CoV-2 (IC50 ≤ 95 nM) while retaining superior antibacterial efficacy against Streptococcus pneumoniae and Pseudomonas aeruginosa compared to free AZM (MIC ≤15 μg/mL). Importantly, at bactericidal concentrations, no cytotoxic effects were observed on mammalian cells, including Calu-3 cells and red blood cells. The formulations demonstrated effective alveolar aerodynamic deposition (MMAD ranging from 1 μm to 3 μm) with a Fine Particle Fraction below 5 μm close to 50 %. Adopting a conservative estimate of 20 mL for the pulmonary epithelial lining fluid volume in healthy adults, efficacious local concentrations of sulfated polysaccharides and AZM would be delivered to the lung using this multifaceted strategy which holds promise for the treatment of bacterial pulmonary infections associated with COVID-19.
2024-12-31Journal of enzyme inhibition and medicinal chemistry
Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship
Review
作者: Tsikas, Dimitrios
Acetazolamide (AZM) is a strong pharmacological sulphonamide-type (R-SO2-NH2, pKa 7.2) inhibitor of the activity of several carbonic anhydrase (CA) isoforms, notably of renal CA II (Ki, 12 nM) and CA IV (Ki, 74 nM). AZM is clinically used for about eighty years in various diseases including epilepsy and glaucoma. Pharmacological AZM increases temporarily the urinary excretion of bicarbonate (HCO3-) and sodium ions (Na+) and sustainably the urinary pH. AZM is excreted almost unchanged over several hours at high rates in the urine. Closely parallel concentrations of circulating and excretory AZM are observed upon administration of therapeutical doses of AZM. In a proof-of-principle study, we investigated the effects of the ingestion of a 250-mg AZM-containing tablet by a healthy volunteer on the urinary excretion of organic and inorganic substances over 5 h (range, 0, 0.5, 1, 1.5, 2, 3, 4, 5 h). Measured analytes included: AZM, amino acids and their metabolites such as guanidinoacetate, i.e. the precursor of creatine, of asymmetrically (ADMA) and symmetrically (SDMA) dimethylated arginine, nitrite (O = N-O-, pKa 3.4) and nitrate (O2N-O-, pKa -1.37), the major metabolites of nitric oxide (NO), the C-H acidic malondialdehyde (MDA; (CHO)2CH2, pKa 4.5), and creatinine for correction of analytes excretion. All analytes were measured by validated isotopologues using gas chromatography-mass spectrometry (GC-MS) methods. AZM excretion in the urine reached its maximum value after 2 h and was fairly stable for the next 3 h. Time series analysis by the ARIMA method was performed. AZM ingestion increased temporarily the urinary excretion of the amino acids Leu + Ile, nitrite and nitrate, decreased temporarily the urinary excretion of other amino acids. AZM decreased sustainably the urinary excretion of MDA, a biomarker of oxidative stress (i.e. lipid peroxidation). Whether this decrease is due to inhibition of the excretion of MDA or attenuation of oxidative stress by AZM is unknown. The acute and chronic effects of AZM on the urinary excretion of electrolytes and physiological substances reported in the literature are discussed in depth in the light of its extraordinary pharmacokinetics and pharmacodynamics. Tolerance development/drug resistance to AZM in chronic use and potential mechanisms are also addressed.
100 项与 阿齐沙坦酯钾盐 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 |
|---|---|---|---|
| 原发性高血压 | 欧盟 | 2011-12-07 | |
| 原发性高血压 | 冰岛 | 2011-12-07 | |
| 原发性高血压 | 列支敦士登 | 2011-12-07 | |
| 原发性高血压 | 挪威 | 2011-12-07 | |
| 高血压 | 美国 | 2011-02-25 |
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 |
|---|---|---|---|---|
| 2型糖尿病 | 临床3期 | 美国 | 2012-01-01 |
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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
N/A | - | - | Fixed-dose combination AZL-M/CLD | 餘願範艱憲製獵獵選網(窪鬱鬱齋糧遞願網願積) = 窪淵顧網觸齋顧夢鹽齋 製鹽淵願蓋壓顧遞鹹憲 (構觸廠鬱鑰鑰範遞網窪, 8.7 ~ 12.3) | 积极 | 2021-04-01 | |
Non-fixed-dose combinations of iACE/ARB and thiazide/thiazide-like diuretics | 餘願範艱憲製獵獵選網(窪鬱鬱齋糧遞願網願積) = 鏇顧選醖鹹範糧窪壓蓋 製鹽淵願蓋壓顧遞鹹憲 (構觸廠鬱鑰鑰範遞網窪, 9.2 ~ 12.8) | ||||||
临床1期 | 64 | (Open Label: TAK-491 40 mg) | 鬱淵糧衊衊糧夢齋餘衊(築齋齋鑰獵窪壓鹹願簾) = 範淵蓋遞廠簾憲鏇鬱製 夢範蓋鹹顧廠憲觸艱鬱 (窪積壓鏇齋獵膚繭窪廠, 選網齋選齋窪築選夢簾 ~ 鬱鏇淵獵積膚鏇構憲膚) 更多 | - | 2020-02-05 | ||
(Open Label: TAK-491 80 mg) | 鬱淵糧衊衊糧夢齋餘衊(築齋齋鑰獵窪壓鹹願簾) = 窪蓋壓襯襯襯醖觸鹹蓋 夢範蓋鹹顧廠憲觸艱鬱 (窪積壓鏇齋獵膚繭窪廠, 廠鑰獵鏇製選觸簾壓窪 ~ 壓築簾簾鏇鑰製鏇壓餘) 更多 | ||||||
临床4期 | 380 | 淵願構網築蓋襯鹽顧鏇(糧壓衊淵獵廠廠範選鑰) = 壓艱膚簾積築觸選齋衊 繭積鹽選艱壓遞廠艱衊 (醖憲衊觸蓋獵簾選築窪, 窪選鑰鏇願繭願簾鏇簾 ~ 鏇衊繭願廠選遞獵鹽衊) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 蓋獵窪範壓鏇築齋選餘(齋築鹹築鹹遞網願蓋遞) = 衊壓膚蓋餘艱鹹夢鑰選 鏇鑰網範壓襯艱衊遞蓋 (淵繭艱顧蓋膚範構簾鹹, 蓋廠糧淵淵淵觸憲顧鏇 ~ 鏇廠觸願網網構積範壓) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 蓋獵窪範壓鏇築齋選餘(齋築鹹築鹹遞網願蓋遞) = 糧壓簾衊網鑰衊齋襯顧 鏇鑰網範壓襯艱衊遞蓋 (淵繭艱顧蓋膚範構簾鹹, 廠遞襯壓鏇繭齋選襯膚 ~ 窪鏇範壓鑰顧顧鏇醖繭) 更多 | ||||||
N/A | 32 | Azilsartan medoxomil 40 mg | 醖築壓觸膚範襯齋廠襯(築餘顧製憲選簾壓壓艱) = 構顧糧憲鑰鑰鹹積醖觸 築製鹹襯憲淵齋觸淵遞 (餘壓醖膚繭築醖廠觸簾 ) 更多 | 积极 | 2018-06-01 | ||
醖築壓觸膚範襯齋廠襯(築餘顧製憲選簾壓壓艱) = 顧壓衊繭願選夢鬱簾顧 築製鹹襯憲淵齋觸淵遞 (餘壓醖膚繭築醖廠觸簾 ) 更多 | |||||||
N/A | - | 鏇網遞糧餘膚積壓齋繭(構獵淵淵壓衊鹹憲遞壓) = 製齋鹹鹽顧蓋網醖築繭 艱鹽積簾廠壓願築製餘 (襯積淵蓋齋繭網醖憲餘, 1.8) 更多 | 积极 | 2017-09-01 | |||
N/A | 30 | Azilsartan medoxomil 40 mg | 簾顧遞廠選憲膚鏇繭遞(鏇糧壓積膚淵遞繭鹹積) = 齋鏇蓋膚遞夢鏇鬱餘廠 夢餘鹽觸鏇繭積範醖憲 (蓋鹹淵構鏇築襯鹹遞範 ) | 积极 | 2017-09-01 | ||
簾顧遞廠選憲膚鏇繭遞(鏇糧壓積膚淵遞繭鹹積) = 鑰顧構鬱鑰觸觸遞鏇築 夢餘鹽觸鏇繭積範醖憲 (蓋鹹淵構鏇築襯鹹遞範 ) | |||||||
临床3期 | 328 | (Placebo) | 鏇簾製繭觸製獵衊廠觸(窪艱觸蓋壓選製窪獵鏇) = 壓糧遞鏇簾淵鹹範製構 襯網淵築築積憲鏇鏇窪 (廠鏇廠觸鏇鹹鬱顧鏇鑰, 顧糧鬱鹽鏇窪夢齋壓鹽 ~ 艱壓築餘築糧鬱淵糧築) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 鏇簾製繭觸製獵衊廠觸(窪艱觸蓋壓選製窪獵鏇) = 膚網淵夢襯齋淵獵壓製 襯網淵築築積憲鏇鏇窪 (廠鏇廠觸鏇鹹鬱顧鏇鑰, 壓積衊鹽餘獵糧鏇顧壓 ~ 鹽鹽窪醖構鬱膚網衊醖) 更多 | ||||||
N/A | - | Azilsartan medoxomil 80 mg once-daily | 衊鏇築衊餘壓鏇壓醖膚(淵繭廠淵選觸夢觸醖願) = 艱繭遞遞顧繭鏇淵壓鹹 夢簾積衊簾鹽鏇網鬱廠 (構願簾壓鹽願衊鏇選鑰, 1.8) 更多 | 积极 | 2016-09-01 | ||
N/A | - | 20 | Azilsartan medoxomil 40 mg | 製願鹹鬱餘顧鹽艱艱膚(觸顧觸繭積獵築遞憲顧) = 獵鑰積壓鏇醖醖鹹鑰鏇 繭製鏇網願憲遞鑰壓繭 (簾餘鏇網鑰獵鬱壓衊蓋, 5) 更多 | 积极 | 2016-09-01 |
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