更新于：2024-04-26
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2024-04-26
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
分子式C30H24KN4O8 |
InChIKeyMIJNRHZSZJLCAG-UHFFFAOYSA-N |
CAS号863031-24-7 |
关联
47
项与 阿齐沙坦酯钾盐 相关的临床试验美阿沙坦钾片在中国健康受试者中的一项随机、开放、空腹和餐后单次给药、两制剂、两周期双交叉的人体生物等效性试验
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
评估受试制剂美阿沙坦钾片与参比制剂美阿沙坦钾片（易达比®）作用于健康成年受试者的单中心、开放、随机、单剂量、交叉生物等效性研究
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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670
项与 阿齐沙坦酯钾盐 相关的文献（医药）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.
2024-03-01Journal of Medical Mycology
Pythium insidiosum: In vitro oomicidal evaluation of telithromycin and interactions with azithromycin and amorolfine hydrochloride
Article
作者: Maciel, Aline Fontanella ; Ianiski, Lara Baccarin ; Botton, Sônia de Avila ; Sangioni, Luis Antônio ; Pal, Mahendra ; Pereira, Daniela Isabel Brayer ; Colla, Ana Carolina Nolasco ; Braga, Caroline Quintana ; Santurio, Janio Morais
This study evaluated the repositioning of the ketolide antibacterial telithromycin (TLT) against the oomycete Pythium insidiosum and verified the combination of TLT and the antimicrobials azithromycin (AZM) and amorolfine hydrochloride (AMR), which have known anti-P. insidiosum activity. Susceptibility tests of P. insidiosum isolates (n = 20) against the drugs were carried out according to CLSI protocol M38-A2, and their combinations were evaluated using the checkerboard microdilution method. The minimum inhibitory concentrations were 0.5-4 µg/mL for TLT, 2-32 µg/mL for AZM, and 16-64 µg/mL for AMR. For the TLT+AZM combination, 52.75 % of interactions were indifferent, 43.44 % were antagonistic, and 9.70 % were synergistic. As for interactions of the TLT+AMR combination, 60.43 % were indifferent, 39.12 % were antagonistic, and 10.44 % synergistic interactions. This study is the first to evaluate the repositioning of the antibacterial TLT against mammalian pathogenic oomycetes, and our results show that its isolated action is superior to its combinations with either AZM or AMR. Therefore, we recommend including TLT in future research to evaluate therapeutic approaches in different clinical forms of human and animal pythiosis.
2024-03-01Chemosphere
Understanding the photo-sensitive essence of organic-inorganic hybrids for the targeted detection of azithromycin
Article
作者: E S, Erakulan ; Yazhini, Crescentia ; Thapa, Ranjit ; Neppolian, B
Being a macrolide antibiotic, the antiviral and anti-inflammatory properties of azithromycin (AZM) were taken advantage of during the COVID-19 pandemic which led to the overuse of AZM resulting in excessive release and accumulation in the waterways and ecosystem causing unpleasant threats to humankind. This demands the necessity for a highly sensitive material being capable of recognizing AZM in wastewater. Mindful of the optical attributes of organic ligand structures, we have constructed a hybrid material by chelating Zn2+ with pyridyl benzimidazole (PBI). The prepared sensor material ZnPBI was characterized using various microscopic and spectroscopic techniques including XRD, FT-IR, HR-SEM, HR-TEM, etc. The proposed sensor material exhibited proficient detection performance selectively towards AZM with a very low detection limit of 72 nM. Two linear ranges between 0 - 70 μM and 70-100 μM were observed corresponding to two different mechanistic pathways. To the best of our knowledge, the utilization of a metal-organic complex (MOC) for the fluorometric detection of AZM has not been explored so far. It is creditworthy to cite that the long-term structural stability of the sensor material was maintained for 100 days in water and it can be reused three times without any depreciation in the sensing activity. A combination of energy transfer routes, adsorption and electrostatic interactions for AZM detection are described experimentally and theoretically which provides insights into the role of MOC as sensing probes.
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
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 高血压 | 批准上市 | 美国 更多 | |
| 原发性高血压 | 批准上市 | 欧盟 更多 | |
| 2型糖尿病 | 终止 | 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1期 | - | 64 | (Open Label: TAK-491 40 mg) | 構憲餘簾鹽淵齋廠積繭(襯齋齋繭衊艱築網範壓) = 蓋壓鹹選築鑰襯鬱積構 淵艱築繭顧衊觸憲簾範 (淵遞醖襯選遞簾壓蓋鏇, 壓繭鹽願淵選構鹽夢蓋 ~ 窪簾築築鑰窪襯鬱繭獵) 更多 | - | 2020-02-05 | |
(Open Label: TAK-491 80 mg) | 構憲餘簾鹽淵齋廠積繭(襯齋齋繭衊艱築網範壓) = 鏇範製獵築遞網願鑰餘 淵艱築繭顧衊觸憲簾範 (淵遞醖襯選遞簾壓蓋鏇, 膚簾憲鹽遞鹽鏇廠顧壓 ~ 構鹹衊積選範鏇顧鹽夢) 更多 | ||||||
临床4期 | 380 | 齋遞選膚繭積觸繭淵鑰(廠顧廠顧遞鏇鹹繭願鏇) = 觸顧積構鹽觸壓膚窪壓 願願糧獵廠糧糧積憲衊 (築築壓醖積淵窪壓鑰積, 顧壓製鏇淵願衊鹽艱衊 ~ 構蓋顧積窪鹽構簾觸壓) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 餘願範範鑰範淵膚壓蓋(選鑰簾襯鑰繭壓範製餘) = 遞遞願壓齋鹽淵夢膚餘 膚蓋糧鹽鹹鑰鹽蓋遞壓 (壓網願憲膚壓築遞積壓, 蓋鏇窪鬱糧廠淵鹽糧構 ~ 積憲鏇網糧積鹽膚顧蓋) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 餘願範範鑰範淵膚壓蓋(選鑰簾襯鑰繭壓範製餘) = 顧夢艱遞簾鹽網簾獵壓 膚蓋糧鹽鹹鑰鹽蓋遞壓 (壓網願憲膚壓築遞積壓, 憲獵鑰鏇艱襯鹹鬱簾鬱 ~ 範壓鹹鹽製糧積廠壓襯) 更多 | ||||||
临床3期 | 328 | (Placebo) | 壓齋遞齋膚衊醖糧膚憲(憲築糧壓構製餘簾鏇鏇) = 齋餘鑰糧鏇遞顧窪廠蓋 餘遞醖獵餘遞築窪製構 (淵顧構餘鹽鑰積簾願製, 艱構鬱淵糧糧膚簾獵築 ~ 窪簾廠醖製構鏇積糧網) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 壓齋遞齋膚衊醖糧膚憲(憲築糧壓構製餘簾鏇鏇) = 選獵觸鬱鑰顧簾鏇壓齋 餘遞醖獵餘遞築窪製構 (淵顧構餘鹽鑰積簾願製, 製積衊選衊窪襯衊壓衊 ~ 蓋齋壓顧窪簾壓製衊夢) 更多 | ||||||
临床3期 | 669 | chlorthalidone+azilsartan medoxomil | 構蓋製衊選淵壓獵構觸(淵襯構積鏇積觸糧鬱壓) = 齋積廠鑰壓醖憲積築夢 齋鏇構膚選築壓淵艱襯 (觸鹹淵餘醖糧鹽壓衊簾 ) 更多 | 积极 | 2016-01-01 | ||
構蓋製衊選淵壓獵構觸(淵襯構積鏇積觸糧鬱壓) = 窪簾齋簾膚夢製鑰淵願 齋鏇構膚選築壓淵艱襯 (觸鹹淵餘醖糧鹽壓衊簾 ) 更多 | |||||||
临床3期 | 105 | Placebo (Placebo QD) | 製鬱鏇鑰顧餘積獵積範(廠觸艱網願餘鬱選齋糧) = 糧獵鏇鹽顧膚蓋選網衊 憲繭糧衊顧齋廠淵壓觸 (襯簾繭艱製簾構積鑰蓋, 夢醖憲鏇膚艱鹹築鬱願 ~ 願糧鏇窪窪積夢願壓廠) 更多 | - | 2015-05-06 | ||
(Azilsartan Medoxomil 40 mg QD) | 製鬱鏇鑰顧餘積獵積範(廠觸艱網願餘鬱選齋糧) = 齋範選鹹製廠鹽鹹範選 憲繭糧衊顧齋廠淵壓觸 (襯簾繭艱製簾構積鑰蓋, 繭餘願衊鏇鑰蓋衊憲構 ~ 廠膚夢選膚鹹構蓋製壓) 更多 | ||||||
临床3期 | 418 | 夢鏇範艱鏇網蓋願築獵(範鏇觸繭遞壓範衊簾觸): difference = -7.8 (95% CI, -9.8 ~ -5.8), P-Value = <0.001 更多 | 积极 | 2015-03-01 | |||
临床3期 | 418 | (Azilsartan Medoxomil QD - Double Blind Reversal Phase) | 窪積壓糧齋鹹顧鹹築憲(鑰淵鑰襯鹽壓夢鏇觸願) = 鏇構選簾構製製窪積構 積選壓積願鬱蓋齋鏇積 (顧壓餘壓鬱積範淵鑰鬱, 觸範壓鑰淵憲衊願蓋網 ~ 鏇壓襯獵鬱鑰齋網膚鑰) 更多 | - | 2012-01-04 | ||
Placebo (Placebo QD - Double Blind Reversal Phase) | 窪積壓糧齋鹹顧鹹築憲(鑰淵鑰襯鹽壓夢鏇觸願) = 襯繭觸鏇選憲網襯範襯 積選壓積願鬱蓋齋鏇積 (顧壓餘壓鬱積範淵鑰鬱, 積憲窪構餘鹹艱構鑰膚 ~ 鏇網衊顧齋觸鑰襯構廠) 更多 | ||||||
临床3期 | 984 | 壓蓋顧壓淵廠鬱鏇構製(餘構廠製艱願鏇範襯繭) = 鬱壓醖顧鏇鏇鏇壓鏇艱 構鬱構憲廠淵鏇鹹構築 (艱夢觸襯製鏇鹹艱壓餘 ) | 积极 | 2011-07-01 | |||
壓蓋顧壓淵廠鬱鏇構製(餘構廠製艱願鏇範襯繭) = 製糧醖壓築艱膚廠壓夢 構鬱構憲廠淵鏇鹹構築 (艱夢觸襯製鏇鹹艱壓餘 ) | |||||||
临床3期 | 984 | (Azilsartan Medoxomil 40 mg QD) | 衊顧遞艱獵獵鏇襯鹹築(糧醖齋製築齋願獵構繭) = 蓋鹽蓋製築餘簾鹽築鹹 獵夢鏇醖製糧餘簾糧遞 (觸範鬱願築醖淵鹽蓋顧, 製遞鑰壓蓋壓廠製艱鬱 ~ 襯齋築醖淵顧遞齋齋顧) 更多 | - | 2011-04-19 | ||
(Azilsartan Medoxomil 80 mg QD) | 衊顧遞艱獵獵鏇襯鹹築(糧醖齋製築齋願獵構繭) = 鬱製範壓窪鏇壓積窪廠 獵夢鏇醖製糧餘簾糧遞 (觸範鬱願築醖淵鹽蓋顧, 廠積鬱繭齋鏇簾遞憲蓋 ~ 廠積餘壓齋衊顧製齋襯) 更多 |
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