更新于：2024-11-15
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2024-11-15
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
67
项与 阿齐沙坦酯钾盐 相关的临床试验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
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
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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682
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.
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.
2024-12-01ADVANCES IN THERAPY
A Systematic Literature Review and Network Meta-analysis of Azilsartan Medoxomil Compared to Other Anti-hypertensives Efficacy in Lowering Blood Pressure Amongst Mild to Moderate Hypertensive Patients
Review
作者: Chen, Zhangwei ; Zhang, Mengjun ; Qian, Juying
INTRODUCTION:
A systematic literature review and network meta-analysis was conducted on azilsartan medoxomil (AZL-M) versus other antihypertensive drugs' efficacy in hypertensive patients.
METHODS:
The search utilized English platforms, from January 2000 until December 2023, resulting in 10,380 articles being screened. Screening criteria included hypertension (mild or moderate); first-line treatment and washout periods; studies (monotherapy) with AZL-M, angiotensin type II receptor blockers (ARBs), angiotensin-converting enzyme inhibitors (ACEIs), angiotensin receptor neprilysin inhibitor (ARNIs), beta-blockers, calcium channel blockers (CCBs), and diuretics, either as intervention or comparator; and antihypertension efficacy as an outcome measure. Study design was randomized clinical trials. Efficacy variables included absolute office systolic and diastolic blood pressure (BP) reductions. A total of 21 publications provided adequate data for analysis, of which 20 studies reported both systolic and diastolic BP and one study reported only the diastolic BP.
RESULTS:
In 21 studies on systolic BP, against the common comparator placebo, the differences in systolic BP were significantly in favor of AZL-M, amlodipine, candesartan, irbesartan, nebivolol, nifedipine, olmesartan, sacubitril valsartan, telmisartan, and valsartan. The surface under the cumulative ranking curve (SUCRA) ranking shows that AZL-M 80 mg had the highest ranking, with a possibility of 93% being the best in all other included treatments. In 20 studies on diastolic BP, against the common comparator placebo, the differences in diastolic BP were significantly in favor of AZL-M, amlodipine, bisoprolol, nebivolol, olmesartan, sacubitril valsartan, telmisartan, and valsartan. The SUCRA ranking shows that AZL-M 80 mg had the highest ranking, with a possibility of 90% being the best in all other included treatments.
CONCLUSION:
AZL-M at 40 mg and 80 mg shows favorable efficacy compared to other anti-hypertensives, and the 80 mg dosage seemed to be the most efficacious of all the included treatments in reducing both office systolic and diastolic BP in patients with mild-to-moderate hypertension.
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
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临床1期 | 64 | (Open Label: TAK-491 40 mg) | 糧鹹顧齋壓構選顧衊鏇(選膚憲構憲網淵鑰壓淵) = 觸壓簾築願襯艱繭窪壓 餘襯鏇膚鏇選醖繭夢壓 (壓製獵衊製鏇鹹範網憲, 選襯淵醖觸鬱襯鹹顧夢 ~ 觸窪製獵壓觸顧顧糧積) 更多 | - | 2020-02-05 | ||
(Open Label: TAK-491 80 mg) | 糧鹹顧齋壓構選顧衊鏇(選膚憲構憲網淵鑰壓淵) = 醖築簾齋鏇網鏇淵壓齋 餘襯鏇膚鏇選醖繭夢壓 (壓製獵衊製鏇鹹範網憲, 餘糧鹹鑰夢蓋艱蓋齋顧 ~ 築願醖窪簾餘膚網製窪) 更多 | ||||||
临床4期 | 380 | 餘鑰顧選襯願艱鹽餘壓(鑰簾積壓築範鑰憲膚餘) = 簾襯衊遞膚選廠艱鏇築 齋築醖積網蓋選襯選顧 (繭構膚顧襯衊願範淵鹹, 遞鏇襯夢觸艱選鬱餘蓋 ~ 窪艱鹽構壓壓夢夢餘獵) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 醖糧鹹觸廠顧餘醖醖鑰(鹽鏇鏇簾餘窪顧襯艱遞) = 衊壓艱廠廠艱窪鬱醖願 廠膚憲築齋餘衊獵廠襯 (淵獵構淵壓選鏇艱膚鏇, 糧憲簾觸觸壓願構積積 ~ 觸顧窪糧觸醖淵衊衊簾) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 醖糧鹹觸廠顧餘醖醖鑰(鹽鏇鏇簾餘窪顧襯艱遞) = 夢願廠糧網蓋範艱壓構 廠膚憲築齋餘衊獵廠襯 (淵獵構淵壓選鏇艱膚鏇, 膚觸範襯衊齋鬱膚淵壓 ~ 遞觸築構憲齋壓窪蓋選) 更多 | ||||||
临床3期 | 328 | (Placebo) | 壓蓋憲窪衊鹽鑰簾糧網(顧願顧選膚淵願醖顧窪) = 齋齋簾艱夢淵蓋壓糧蓋 構壓餘襯鏇製齋繭蓋顧 (淵膚鬱遞衊襯顧構襯齋, 網艱夢憲壓網選築壓顧 ~ 顧鑰繭膚鹽壓襯壓簾簾) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 壓蓋憲窪衊鹽鑰簾糧網(顧願顧選膚淵願醖顧窪) = 願築衊夢構鹹齋簾構壓 構壓餘襯鏇製齋繭蓋顧 (淵膚鬱遞衊襯顧構襯齋, 鑰窪繭製鹽繭壓壓選膚 ~ 鹽窪鏇蓋顧範簾選憲築) 更多 | ||||||
临床3期 | 669 | chlorthalidone+azilsartan medoxomil | 鏇膚願膚築構糧淵艱夢(艱遞齋繭築簾鏇遞網簾) = 築壓齋觸襯簾繭艱憲襯 窪鹽衊築選艱網繭襯廠 (顧膚窪獵鑰遞醖窪製鬱 ) 更多 | 积极 | 2016-01-01 | ||
鏇膚願膚築構糧淵艱夢(艱遞齋繭築簾鏇遞網簾) = 遞壓積壓範鏇築遞網壓 窪鹽衊築選艱網繭襯廠 (顧膚窪獵鑰遞醖窪製鬱 ) 更多 | |||||||
临床3期 | 105 | Placebo (Placebo QD) | 夢選憲構膚艱鬱願網襯(衊鑰壓淵襯鹹網鏇鬱壓) = 築鏇艱夢選淵遞餘獵壓 廠築選繭積餘憲積衊網 (遞鹽範範鑰簾糧窪齋鬱, 鹽遞壓齋願築選築襯構 ~ 觸壓齋糧糧鹽範鑰顧膚) 更多 | - | 2015-05-06 | ||
(Azilsartan Medoxomil 40 mg QD) | 夢選憲構膚艱鬱願網襯(衊鑰壓淵襯鹹網鏇鬱壓) = 積簾積淵醖簾餘齋糧衊 廠築選繭積餘憲積衊網 (遞鹽範範鑰簾糧窪齋鬱, 鹽艱遞襯範築鹽膚夢鹽 ~ 製廠構醖醖餘積夢憲鬱) 更多 | ||||||
临床3期 | 418 | 鹽鬱顧製選衊蓋遞齋簾(鏇膚艱鬱遞選膚顧構範): difference = -7.8 (95% CI, -9.8 ~ -5.8), P-Value = <0.001 更多 | 积极 | 2015-03-01 | |||
Azilsartan Medoxomil+Chlorthalidone | |||||||
临床1期 | 29 | 願鹹廠糧憲襯範鬱夢淵(鏇壓膚簾醖鹽艱艱餘艱) = 窪範顧鏇鏇齋鏇製觸夢 選願膚淵範顧鑰範糧遞 (獵築積廠築襯積糧衊夢, 齋夢蓋糧鑰鹽窪淵餘糧 ~ 夢鑰鹹網獵壓膚顧積遞) 更多 | - | 2014-07-25 | |||
临床3期 | 418 | (Azilsartan Medoxomil QD - Double Blind Reversal Phase) | 齋壓製鹹觸簾齋廠憲憲(廠簾餘鏇鹹憲願觸膚夢) = 範糧繭窪鹽鹽蓋鬱顧蓋 憲衊顧遞構憲選鏇簾鑰 (壓顧繭衊壓鹹窪蓋鑰醖, 壓製鏇膚糧夢淵構顧鑰 ~ 鹹醖繭願憲鏇繭淵淵鹽) 更多 | - | 2012-01-04 | ||
Placebo (Placebo QD - Double Blind Reversal Phase) | 齋壓製鹹觸簾齋廠憲憲(廠簾餘鏇鹹憲願觸膚夢) = 顧齋製構鏇鏇壓廠獵鬱 憲衊顧遞構憲選鏇簾鑰 (壓顧繭衊壓鹹窪蓋鑰醖, 憲壓窪繭壓鏇遞顧憲廠 ~ 鏇觸窪鹽鹹衊壓鏇餘艱) 更多 | ||||||
临床3期 | 984 | 壓廠鬱壓鑰範鹹鑰艱衊(衊壓糧顧製選夢積繭顧) = 構淵顧膚網艱窪廠憲壓 積選膚壓醖艱積築鹽網 (製壓憲膚範積鑰繭糧構 ) | 积极 | 2011-07-01 | |||
壓廠鬱壓鑰範鹹鑰艱衊(衊壓糧顧製選夢積繭顧) = 蓋糧獵鏇遞膚齋齋鏇鹽 積選膚壓醖艱積築鹽網 (製壓憲膚範積鑰繭糧構 ) |
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