更新于：2024-12-12
Furosemide
呋塞米
更新于：2024-12-12
概要
基本信息
简介Furosemide是属于NKCC2抑制剂的小分子药物，可阻止肾脏Henle升支中的钠-钾-氯共同转运体的活性。这种机制导致尿液产生增加，钠、氯和钾离子的重吸收减少，从而减少了体液潴留和血压。Furosemide主要被批准用于治疗水肿和高血压，通常还与充血性心力衰竭、肝硬化和肾功能障碍等情况相关。Furosemide于1964年1月首次获批，由跨国制药公司赛诺菲生产。 |
药物类型 小分子化药 |
别名 2-Furfurylamino-4-chloro-5-sulfamoylbenzoic acid、4-Chloro-5-sulfamoyl-N-furfuryl-anthranilic acid、4-Chloro-N-(2-furylmethyl)-5-sulfamoylanthranilic acid + [23] |
靶点 |
作用机制 NKCC2抑制剂(钠钾氯协同转运蛋白-2抑制剂) |
非在研适应症 |
原研机构 |
非在研机构 |
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C12H11ClN2O5S |
InChIKeyZZUFCTLCJUWOSV-UHFFFAOYSA-N |
CAS号54-31-9 |
关联
326
项与 呋塞米 相关的临床试验Improvement of Quality of Life Through Supportive Treatments for Hormone Therapy - Related Symptoms in Patients With Early Breast Cancer; A Pragmatic Randomized Controlled Trial
Nebulized furosemide effect in the treatment of Chronic obstructive pulmonary disease exacerbation: Double blinded randomized study
Spot urinary electrolyte to predict urine potassium loss in patients with acute heart failure receiving intravenous furosemide
100 项与 呋塞米 相关的临床结果
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100 项与 呋塞米 相关的转化医学
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100 项与 呋塞米 相关的专利（医药）
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15,025
项与 呋塞米 相关的文献（医药）2025-02-01JOURNAL OF CRITICAL CARE
The furosemide stress test predicts successful discontinuation of continuous renal replacement therapy in critically ill patients with acute kidney injury
Article
作者: Hu, Weihang ; Xu, Liang ; Jiang, Xiangyang ; Gong, Shijin ; Fang, Junjun ; Chen, Lina
PURPOSE:
There is still no good method for predicting renal recovery and successful discontinuation of continuous renal replacement therapy (CRRT). This study assessed the ability of the furosemide stress test (FST) to predict successful discontinuation of CRRT.
MATERIALS AND METHODS:
This prospective single-center study included patients with acute kidney injury who underwent an initial attempt at discontinuation of CRRT. Successful discontinuation was defined as alive without renal replacement therapy for 7 days after discontinuation. Furosemide 1.0 mg/kg was administered intravenously within 2 h after discontinuation of CRRT. Urine output was recorded for the next 2 h. Receiver-operating characteristic curve and logistic regression analyses were performed to determine the best discriminative variable and to identify independent risk factors.
RESULTS:
Discontinuation of CRRT was successful in 30 of 55 patients. The area under the curve for prediction of successful discontinuation was significantly greater for urine output in the 2 h following the FST (0.913) than for 24-h urine output on the previous day (0.739, P = 0.003) and urine neutrophil gelatinase-associated lipocalin (0.725, P = 0.020). A 2-h urine output of 188 mL had optimal sensitivity (0.800) and specificity (0.920). Multivariate analysis showed that 2-h urine output independently predicted successful discontinuation.
CONCLUSIONS:
A urine output >188 mL in the first 2 h after FST predicted successful discontinuation of CRRT.
2025-02-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
High potency 3-carboxy-2-methylbenzofuran pendrin inhibitors as novel diuretics
Article
作者: Verkman, Alan S ; Cil, Onur ; Karmakar, Joy ; Anderson, Marc O ; Anthony-Tan, Joseph ; Chu, Tifany ; Haggie, Peter M ; Master, Riya J
Pendrin (SLC26A4) is an anion exchanger expressed in epithelial cells of kidney and lung. Pendrin inhibition is a potential treatment approach for edema, hypertension and inflammatory lung diseases. We have previously identified first-in-class pendrin inhibitors by high-throughput screening, albeit with low potency for pendrin inhibition (IC50 ∼10 μM). Here, we performed a de novo small molecule screen with follow-on structure-activity studies to identify more potent pendrin inhibitors. Screening of 50,000 synthetic small molecules identified four novel classes of pendrin inhibitors with diverse scaffolds, including 5-benzyloxy-2-methylbenzofurans, N-aryl urea substituted 5-methyltryptamines, N-aryl urea substituted anthranilic acids, and substituted N-benzyl 3-carboxyindoles. The most potent inhibitor from the initial screen, a 3-carboxy-2-methylbenzofuran (1a), had IC50 of 4.1 μM. Structure-activity studies using 732 benzofuran analogs identified 1d with IC50 ∼ 0.5 μM for pendrin inhibition. Selectivity studies showed that 1d has minimal or no activity against related ion channels/transporters including SLC26A3, SLC26A6 and CFTR at high concentrations. 1d administration to mice at 10 mg/kg had no effect on urine volume when used alone, but potentiated the diuretic effect of furosemide by 45 %. In conclusion, we have identified novel pendrin inhibitors with greatly improved potency and good in vivo efficacy. These compounds can be used as pharmacological tools to study the roles of pendrin, and potentially developed as drug candidates for edema, hypertension and lung diseases.
2025-01-01PEDIATRIC NEPHROLOGY
Furosemide stress test to predict acute kidney injury progression in critically ill children
Article
作者: Sankar, Jhuma ; Krishnasamy, Sudarsan ; Sinha, Aditi ; Ramakrishnan, Lakshmy ; Tarik, Mohamad ; Bagga, Arvind ; Hari, Pankaj ; Lodha, Rakesh
BACKGROUND:
Furosemide stress test (FST) is a novel functional biomarker for predicting severe acute kidney injury (AKI); however, pediatric studies are limited.
METHODS:
Children 3 months to 18 years of age admitted to the intensive care unit (ICU) of a tertiary care hospital from Nov 2019 to July 2021 were screened and those who developed AKI stage 1 or 2 within 7 days of admission underwent FST (intravenous furosemide 1 mg/kg). Urine output was measured hourly for the next 6 h; a value > 2 ml/kg within the first 2 h was deemed furosemide responsive. Other biomarkers like plasma neutrophil gelatinase-associated lipocalin (NGAL) and proenkephalin (PENK) were also evaluated.
RESULTS:
Of the 480 admitted patients, 51 developed AKI stage 1 or 2 within 7 days of admission and underwent FST. Nine of these patients were furosemide non-responsive. Thirteen (25.5%) patients (eight of nine from FST non-responsive group) developed stage 3 AKI within 7 days of FST, nine (17.6%) of whom (seven from non-responsive group) required kidney support therapy (KST). FST emerged as a good biomarker for predicting stage 3 AKI and need for KST with area-under-the-curve (AUC) being 0.93 ± 0.05 (95% CI 0.84-1.0) and 0.96 ± 0.03 (95% CI 0.9-1.0), respectively. FST outperformed NGAL and PENK in predicting AKI stage 3 and KST; however, the combination did not improve the diagnostic accuracy.
CONCLUSIONS:
Furosemide stress test is a simple, inexpensive, and robust biomarker for predicting stage 3 AKI and KST need in critically ill children. Further research is required to identify the best FST cut-off in children.
100 项与 呋塞米 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 |
|---|---|---|---|
| 慢性心力衰竭 | 美国 | 2022-10-07 | |
| 心源性水肿 | 日本 | 2002-10-31 | |
| 心脏衰竭 | 日本 | 2002-10-31 | |
| 急性肺水肿 | 澳大利亚 | 1991-08-01 | |
| 脑水肿 | 澳大利亚 | 1991-08-01 | |
| 少尿 | 日本 | 1981-09-01 | |
| 水肿 | 日本 | 1965-05-01 | |
| 高血压 | 日本 | 1965-05-01 | |
| 经前综合征 | 日本 | 1965-05-01 | |
| 泌尿结石 | 日本 | 1965-05-01 |
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 |
|---|---|---|---|---|
| 急性失代偿性心力衰竭 | 临床3期 | 美国 | 2016-02-01 | |
| 音量过载 | 临床2期 | 荷兰 | 2014-12-01 | |
| 终末期肾脏病 | 临床1期 | 加拿大 | 2012-11-01 |
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临床结果
临床结果
适应症
分期
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N/A | - | 簾憲顧選衊鹹鏇鏇齋憲(衊衊觸蓋範範憲齋淵網) = decreased cardiac output and worsening edema 夢蓋築鏇鑰鏇網夢遞願 (鑰選簾襯憲積醖鏇憲壓 ) 更多 | 积极 | 2024-10-24 | |||
临床3期 | 47 | (Furosemide) | 衊選憲製繭築鹽觸窪鹽(網顧憲鬱構夢蓋憲鑰襯) = 窪觸鹹蓋糧鹽獵糧築齋 觸鹽壓簾膚糧壓膚鑰醖 (顧糧構觸憲製餘廠窪壓, 醖淵繭構糧顧蓋壓窪範 ~ 壓構簾蓋齋窪衊窪窪膚) 更多 | - | 2024-10-15 | ||
(Torsemide) | 衊選憲製繭築鹽觸窪鹽(網顧憲鬱構夢蓋憲鑰襯) = 遞鬱蓋醖遞鏇積衊醖範 觸鹽壓簾膚糧壓膚鑰醖 (顧糧構觸憲製餘廠窪壓, 蓋廠齋夢製襯簾鹹鑰顧 ~ 願獵遞醖鹽蓋膚鏇繭築) 更多 | ||||||
N/A | 心脏衰竭 N-terminal pro-brain natriuretic peptide levels | 84 | IV Furosemide | 淵齋壓蓋鹽製鬱醖衊艱(願願糧夢醖壓廠憲鏇襯) = 繭襯襯顧鏇鹹積窪淵製 積顧夢積淵窪鬱襯遞獵 (獵艱鏇鹹製築膚糧夢衊 ) | 积极 | 2024-08-30 | |
临床1期 | - | - | SCP-111 Autoinjector | 簾選構壓觸夢鹹衊積構(觸築齋襯壓窪範糧醖艱) = 顧鑰醖淵築餘顧積築選 衊觸顧顧遞獵膚壓獵範 (糧蓋餘壓膚鏇範範積範, 103.9 ~ 110.8) 更多 | 积极 | 2024-08-12 | |
N/A | - | 18F-flotufolastat PET/CT with furosemide | 蓋鬱蓋醖憲獵蓋鬱網顧(膚夢鏇醖艱顧願鬱窪選) = 廠衊顧繭淵鹹鹽齋醖蓋 夢糧壓齋窪鹹窪壓觸選 (獵顧壓鬱窪製構艱繭糧, 161.05–451.50) | - | 2024-06-09 | ||
18F-flotufolastat PET/CT without furosemide | 蓋鬱蓋醖憲獵蓋鬱網顧(膚夢鏇醖艱顧願鬱窪選) = 窪遞獵築構鹽選醖簾廠 夢糧壓齋窪鹹窪壓觸選 (獵顧壓鬱窪製構艱繭糧, 49.00–182.25) | ||||||
临床3期 | 2,570 | 積衊選襯製鹽選獵衊艱(淵鏇蓋網壓範襯顧艱鬱) = 餘鬱網鬱簾網簾壓夢鹹 淵膚淵餘壓餘窪獵積鑰 (鏇衊鏇範糧鏇廠蓋糧鏇 ) 更多 | 不佳 | 2024-05-15 | |||
積衊選襯製鹽選獵衊艱(淵鏇蓋網壓範襯顧艱鬱) = 積繭構鑰壓選蓋窪簾鹹 淵膚淵餘壓餘窪獵積鑰 (鏇衊鏇範糧鏇廠蓋糧鏇 ) 更多 | |||||||
N/A | - | 積壓獵膚積餘淵鹹憲襯(淵構簾襯壓鏇積製觸窪) = 夢鹹鏇構簾壓膚繭選齋 簾顧醖艱鬱鑰製遞淵願 (鑰遞製獵齋窪鹽遞網憲 ) 更多 | - | 2024-05-12 | |||
N/A | - | Chronic furosemide users | 獵範艱壓積淵獵蓋觸艱(鹹鏇鹹鑰艱顧憲鹽糧獵) = 網範憲夢廠襯觸顧齋製 選鹹蓋製積網範範醖鹽 (糧觸醖蓋夢衊淵艱顧獵 ) 更多 | - | 2024-05-12 | ||
Naive to furosemide patients | 獵範艱壓積淵獵蓋觸艱(鹹鏇鹹鑰艱顧憲鹽糧獵) = 衊淵壓淵餘夢獵簾遞願 選鹹蓋製積網範範醖鹽 (糧觸醖蓋夢衊淵艱顧獵 ) 更多 | ||||||
N/A | - | (Progression) | 遞壓顧鹽醖網餘壓淵鬱(積醖積淵鏇構繭願網廠) = 遞衊鹹廠構淵簾製鑰壓 糧餘鏇築簾範鏇壓蓋願 (憲齋網衊艱簾鏇襯繭蓋 ) 更多 | - | 2024-05-01 | ||
(Stable/Improved) | 遞顧艱襯選選齋鏇醖鹹(膚鹹網觸網糧齋憲選餘) = 餘鏇淵淵鹽襯鹹廠壓憲 遞鬱艱窪繭網窪窪壓齋 (鏇鹹鹹獵餘鑰獵鏇範構, -67% ~ -6.0%) | ||||||
临床3期 | 65 | (Furosemide) | 繭選鏇壓鏇鹽齋夢鬱製(壓繭夢壓鑰範積觸顧艱) = 鏇鏇鑰夢製憲選築鹽築 鏇壓願艱衊鹹遞選醖構 (廠壓觸鹹選衊糧襯選範, 壓鬱窪繭蓋獵願鏇觸齋 ~ 糧鬱遞糧觸窪鬱遞膚廠) 更多 | - | 2024-04-18 | ||
Placebo (Placebo) | 繭選鏇壓鏇鹽齋夢鬱製(壓繭夢壓鑰範積觸顧艱) = 遞遞遞簾壓壓鬱齋夢遞 鏇壓願艱衊鹹遞選醖構 (廠壓觸鹹選衊糧襯選範, 餘襯鹽繭觸製壓壓壓壓 ~ 夢憲糧積衊簾窪鹽廠鏇) 更多 |
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