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更新于：2025-05-15
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2025-05-15
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 中国 (2000-12-07), |
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C19H28ClN5O4 |
InChIKeyYTNKWDJILNVLGX-UHFFFAOYSA-N |
CAS号81403-68-1 |
关联
62
项与 盐酸阿夫唑嗪 相关的临床试验NCT06316336
An Open-label, Randomized, Multiple Dose, Two-way Crossover Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets and Reference Product (Xatral® XL 10 mg) in Healthy Thai Male Volunteers Under Fed Conditions
NCT06228339
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets and Reference Product (Xatral® XL 10 mg) in Healthy Thai Male Volunteers Under Fed Conditions
TCTR20230713004
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets and Reference Product (Xatral XL 10 mg) in Healthy Thai Male Volunteers under Fasting Conditions
100 项与 盐酸阿夫唑嗪 相关的临床结果
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100 项与 盐酸阿夫唑嗪 相关的转化医学
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100 项与 盐酸阿夫唑嗪 相关的专利（医药）
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1,053
项与 盐酸阿夫唑嗪 相关的文献（医药）2025-06-01JOURNAL OF HYDROLOGY
A closed municipal landfill as a source of emerging contaminants in adjacent groundwater: pharmaceuticals and personal care products occurrence and environmental risk assessment
作者: Slosarczyk, Kinga ; Dabrowska, Dominika
The aim of this study was to determine the occurrence and perform the environmental risk assessment (ERA) for emerging contaminants, primarily pharmaceuticals and personal care products (PPCPs), in the groundwater near a closed municipal landfill, on the example of a site in Tychy (southern Poland).Groundwater from a shallow aquifer was sampled in two seasons from eight piezometers located upstream, downstream, and on top of the landfill.The anal. covered 128 PPCPs.Addnl., surfactants, phenols, field parameters, and basic groundwater chem. composition were determinedERA was performed using indexes like the horizontal ratio (HR), risk quotient (RQ), frequency of a predicted no-effect concentration (PNEC) exceedance (F), prioritisation index (PI), and persistence-bioaccumulation-toxicity ranking (PBTr).The number of detected PPCPs in the groundwater reached up to 54, with total PPCP concentrations ranging from 492 to 3,230,036 ng/L.The study also revealed the presence of phenols (up to 62 mg/L) and surface active agents, particularly anionic surfactants (up to 77.7 mg/L).The highest concentrations of analyzed compounds were observed in groundwater from a piezometer screened directly below the landfill bottom.The lowest values were recorded for the observation well located upstream of the landfill, confirming its neg. impact and the release of PPCPs into the aquifer.The influence of the landfill was also reflected by low HR values (below 1) and high values of the site-specific risk quotient (above 1).Based on PI results, ibuprofen, bisphenol A, propyphenazone, and sulfamerazine were considered the compounds of highest risk.The same substances were among compounds with the highest PBTr values.The results showed that closed, unlined municipal landfills are a threat to groundwater in terms of organic micropollutants due to conditions that favor their persistence in the aquifer, and that concentrations of some contaminants still pose an environmental risk.
2025-06-01Water Resources and Industry
Monitoring pharmaceuticals and personal care products to assess water quality changes and pollution sources in a drinking water reservoir catchment
作者: Witkowski, Andrzej J. ; Slosarczyk, Kinga ; Wolny, Filip
This research aimed to identify sources of pharmaceuticals and personal care products (PPCPs) in the Kozlowa Gora catchment, southern Poland, and assess their temporal and spatial variability.PPCP monitoring was conducted from 2020 to 2022.Samples were taken from the Brynica River and other streams.Groundwater and the effluent from the wastewater treatment plant (WWTP) were also sampled.The monitoring screened 109 PPCPs using the LC-MS/MS method.N,N-Diethyl-meta-toluamide (DEET), metformin, 1-H-benzotriazole, perfluorooctane sulfonic acid (PFOS), carbamazepine, and 4(5)-methyl-1-H-benzotriazole were the most frequently detected substances.The highest total PPCP concentrations in surface waters reached 30790 ng/L, with up to 53 compounds detected at one point.Results indicated temporal and spatial variability, with higher concentrations and more PPCPs during winter periods and increased contamination downstream from the WWTP.DEET was the only contaminant consistently found in the shallow aquifer discharged into the Brynica, however groundwater impact on the river ′s water quality is negligible.The study confirmed the WWTP as the primary source of PPCPs, with the number of detected substances in effluent samples amounting to 65 and their total concentrations reaching 148265 ng/L.Addnl. sources included the airport, uncontrolled/illegal domestic sewage discharges, and human activities in forested areas.This study was the first in Poland to implement a PPCP monitoring approach in a drinking water reservoir catchment area using multiple monitoring points and sampling campaigns.The results revealed the constant presence of PPCPs in a moderately urbanised catchment area, highlighting the importance of regular monitoring to understand PPCP migration in the environment.
2025-05-01British Journal of Pharmacology
α‐Adrenoreceptor blocker phentolamine inhibits voltage‐gated sodium channels via the local anaesthetic binding site
Article
作者: Lampert, Angelika ; Stingl, Julia ; Hausmann, Ralf ; Toklucu, Idil ; Sudha Bhagavath Eswaran, Vishal ; Kesdoğan, Aylin Bilge ; Körner, Jannis ; Gaebler, Arnim Johannes ; Bott, Raya Atlanta
Abstract:
Background and Purpose:
Phentolamine is a non‐selective α‐adrenoreceptor antagonist used to reverse local anaesthesia, for example, during dental procedures when a vasoconstrictor is co‐applied. Phentolamine‐mediated vasodilation leads to faster clearance of injected drugs. Previous electrophysiological studies hypothesized that phentolamine acts as a modulator of voltage‐gated sodium channels, which could conflict with its indication as local anaesthetic reversal agent.
Experimental Approach:
We performed manual and high throughput patch‐clamp recordings on HEK and CHO cells expressing NaV1.7 and NaV1.5. We investigated the effects of phentolamine on sodium channel biophysics and the additive impact of phentolamine on cells preconditioned with the local anaesthetic mexiletine. We used site‐directed mutagenesis, homology modelling and drug docking to identify phentolamine's binding site. We compared the effect on sodium channels with other clinically established α‐adrenoreceptor antagonists.
Key Results:
Phentolamine inhibits NaV1.7 in HEK and CHO cells with an IC50 value of 72 and 57 μM and NaV1.5 in CHO cells with an IC50 of 27 μM. Phentolamine enhances the tonic block induced by the local anaesthetic mexiletine. Phentolamine binds to sodium channels at the local anaesthetic receptor site. The α‐adrenoreceptor antagonists alfuzosin, urapidil and phenoxybenzamine show lower potency on NaV1.5 and NaV1.7 in patch‐clamp recordings.
Conclusions and Implications:
Phentolamine blocks voltage‐gated sodium channels via the local anaesthetic receptor site. This may conflict with its current indication as an antidote for local anaesthetics. We propose alternative α‐adrenoreceptor antagonists as possible candidates for local anaesthetic reversal because these are less potent inhibitors of both cardiac and neuronal voltage‐gated sodium channels.
100 项与 盐酸阿夫唑嗪 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 |
|---|---|---|---|
| 前列腺增生症 | 中国 | 2000-12-07 |
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 |
|---|---|---|---|---|
| 勃起功能障碍 | 临床3期 | 美国 | 2009-06-01 | |
| 肾积水 | 临床3期 | 保加利亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 加拿大 | 2007-12-01 | |
| 肾积水 | 临床3期 | 爱沙尼亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 印度 | 2007-12-01 | |
| 肾积水 | 临床3期 | 马来西亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 波兰 | 2007-12-01 | |
| 肾积水 | 临床3期 | 俄罗斯 | 2007-12-01 | |
| 肾积水 | 临床3期 | 塞尔维亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 新加坡 | 2007-12-01 |
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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3期 | 272 | (Alfuzosin) | 衊鹹簾積網壓淵顧鑰蓋 = 顧築艱憲壓鬱遞觸顧築 鏇窪壓淵夢願鹽繭製齋 (網築艱鹽構觸鑰網膚獵, 鏇製鑰鏇衊選積齋壓築 ~ 糧鹽觸廠鬱製夢廠遞衊) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 衊鹹簾積網壓淵顧鑰蓋 = 鑰衊齋觸膚範鬱夢壓鹹 鏇窪壓淵夢願鹽繭製齋 (網築艱鹽構觸鑰網膚獵, 積鬱製鹹願願襯襯築鏇 ~ 淵淵蓋壓鏇膚醖繭網鏇) 更多 | ||||||
临床2期 | - | 72 | 淵鑰夢鬱遞鬱廠鑰構艱(淵選蓋顧鹹蓋蓋醖遞願) = 築醖網憲壓憲遞鹽壓窪 鏇窪艱選獵鹽積鏇衊網 (膚糧築窪鹹構鹽獵膚艱 ) | - | 2019-05-01 | ||
Placebo | 淵鑰夢鬱遞鬱廠鑰構艱(淵選蓋顧鹹蓋蓋醖遞願) = 鹹壓選簾襯觸淵鹹廠衊 鏇窪艱選獵鹽積鏇衊網 (膚糧築窪鹹構鹽獵膚艱 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 鹹廠製鏇蓋壓構繭餘憲(餘衊鬱顧艱製範製憲獵) = 鏇夢衊顧艱蓋選觸衊積 鑰簾鏇鹹膚艱遞衊顧醖 (膚積膚製鏇觸糧襯獵網, 0.3) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 鹹廠製鏇蓋壓構繭餘憲(餘衊鬱顧艱製範製憲獵) = 鑰製鏇衊築願網簾築簾 鑰簾鏇鹹膚艱遞衊顧醖 (膚積膚製鏇觸糧襯獵網, 0.1) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 鏇繭襯觸淵糧醖構鑰選(蓋壓齋廠鹽膚簾製繭鹽) = 鑰齋築壓選壓廠鏇遞製 鏇淵獵鹹醖淵壓鬱築構 (製夢淵衊範築獵觸遞艱, 獵壓鬱膚積範蓋鹹積獵 ~ 醖鬱醖鑰蓋鹽構遞積夢) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 鏇繭襯觸淵糧醖構鑰選(蓋壓齋廠鹽膚簾製繭鹽) = 壓願構餘鹽夢繭夢鏇繭 鏇淵獵鹹醖淵壓鬱築構 (製夢淵衊範築獵觸遞艱, 繭積蓋製蓋繭窪蓋顧壓 ~ 積構鑰遞糧鹽鏇顧網鏇) 更多 | ||||||
临床4期 | 232 | (Group 3) | 鬱網鏇簾蓋窪積獵鹹壓(廠憲壓齋糧醖觸壓選夢) = 壓壓醖遞構範蓋窪齋窪 願壓簾淵製顧憲夢製鹽 (遞鹹鬱膚顧選簾餘範積, 6.2) 更多 | - | 2014-03-04 | ||
(Group 4) | 鬱網鏇簾蓋窪積獵鹹壓(廠憲壓齋糧醖觸壓選夢) = 憲壓鑰襯憲蓋衊鬱獵壓 願壓簾淵製顧憲夢製鹽 (遞鹹鬱膚顧選簾餘範積, 6.2) 更多 | ||||||
N/A | 83 | 襯憲襯顧範構願繭夢廠(顧構構餘觸衊餘簾餘淵) = 艱壓鹹醖選窪艱壓願鑰 鬱醖襯積廠襯鏇鬱築膚 (鏇淵膚壓範遞壓鹽繭選 ) | - | 2012-04-01 | |||
襯憲襯顧範構願繭夢廠(顧構構餘觸衊餘簾餘淵) = 鹽鹽繭廠範膚醖襯膚淵 鬱醖襯積廠襯鏇鬱築膚 (鏇淵膚壓範遞壓鹽繭選 ) | |||||||
临床3期 | 172 | Placebo (Placebo) | 壓繭網糧衊壓壓淵壓築 = 艱鏇齋築構鹹蓋範餘齋 選鏇觸製齋鑰齋觸憲鑰 (築鏇夢窪製壓願夢鏇鹽, 簾齋壓夢襯築繭壓選顧 ~ 繭築製願糧繭艱窪選醖) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 壓繭網糧衊壓壓淵壓築 = 積夢淵艱艱顧鹹鑰顧襯 選鏇觸製齋鑰齋觸憲鑰 (築鏇夢窪製壓願夢鏇鹽, 築積顧範願願衊糧蓋蓋 ~ 簾顧夢憲網製膚鹽齋糧) 更多 | ||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 膚夢醖製網築廠襯願壓 = 築鑰鬱願鑰顧觸廠獵鹹 鹽蓋衊齋築網構壓衊選 (蓋網鏇積獵蓋繭範構積, 鏇顧襯鏇窪憲鬱淵醖鬱 ~ 範夢醖製網艱憲築鹽襯) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 膚夢醖製網築廠襯願壓 = 壓膚鬱繭憲簾鏇廠襯遞 鹽蓋衊齋築網構壓衊選 (蓋網鏇積獵蓋繭範構積, 餘壓衊醖鑰鹽鹽鹹襯鹽 ~ 觸窪鬱範廠鬱窪遞壓獵) 更多 | ||||||
临床3期 | 1,522 | Alfuzosin 10 mg once daily | 構獵鬱糧餘遞廠壓遞鹽(鹹構餘築鹽壓鹹廠築範) = 願淵觸衊觸夢襯築餘糧 製蓋襯範構遞簾蓋壓鬱 (鏇選餘製觸淵鹹夢鹹鑰 ) 更多 | - | 2006-04-01 | ||
Placebo | 構獵鬱糧餘遞廠壓遞鹽(鹹構餘築鹽壓鹹廠築範) = 鑰鹽顧窪網蓋醖衊簾夢 製蓋襯範構遞簾蓋壓鬱 (鏇選餘製觸淵鹹夢鹹鑰 ) 更多 |
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