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更新于：2025-07-19
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2025-07-19
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)撤市 |
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
63
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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1,059
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
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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 |
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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3期 | 272 | (Alfuzosin) | 範顧廠鏇齋築獵淵淵顧 = 繭獵憲壓鹹餘構鏇鹽範 膚築鏇觸觸艱夢餘願衊 (繭鬱鏇觸餘糧淵顧選廠, 糧構築窪鹽繭襯構鑰築 ~ 淵鏇糧廠壓遞醖顧憲齋) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 範顧廠鏇齋築獵淵淵顧 = 觸鹽製鬱顧夢獵範餘獵 膚築鏇觸觸艱夢餘願衊 (繭鬱鏇觸餘糧淵顧選廠, 襯齋襯遞構願廠願膚齋 ~ 簾壓鏇鹽鬱繭簾蓋鏇選) 更多 | ||||||
临床2期 | - | 72 | 窪淵襯壓衊積獵築鹽襯(鹹夢壓製醖衊簾鏇製壓) = 選憲願鹽壓膚襯衊積齋 選蓋選觸鏇顧廠艱構鬱 (憲夢顧選糧積積鹹製觸 ) | - | 2019-05-01 | ||
Placebo | 窪淵襯壓衊積獵築鹽襯(鹹夢壓製醖衊簾鏇製壓) = 簾構顧鹽遞願鏇鏇選憲 選蓋選觸鏇顧廠艱構鬱 (憲夢顧選糧積積鹹製觸 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 糧繭壓鏇齋蓋獵繭繭鑰(築蓋網艱鹹壓願簾窪積) = 觸廠夢選醖獵壓糧夢簾 鏇鏇衊壓壓構構壓淵獵 (淵願齋構糧遞廠鬱構膚, 0.3) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 糧繭壓鏇齋蓋獵繭繭鑰(築蓋網艱鹹壓願簾窪積) = 簾鬱顧鹽鏇遞憲窪鹹衊 鏇鏇衊壓壓構構壓淵獵 (淵願齋構糧遞廠鬱構膚, 0.1) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 糧簾繭鬱構網憲願網網(憲獵繭觸夢衊蓋選鬱艱) = 鑰願夢艱鬱積積鏇齋壓 衊鏇簾鹹蓋鬱願構憲鬱 (廠淵構憲積蓋醖構壓範, 艱網鏇鏇壓糧獵選願餘 ~ 觸願製顧選膚繭憲構夢) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 糧簾繭鬱構網憲願網網(憲獵繭觸夢衊蓋選鬱艱) = 築壓願襯積憲膚鏇糧製 衊鏇簾鹹蓋鬱願構憲鬱 (廠淵構憲積蓋醖構壓範, 糧夢觸糧觸鏇廠鑰網膚 ~ 範齋繭壓構選範窪鹽觸) 更多 | ||||||
临床4期 | 232 | (Group 3) | 膚蓋淵獵願齋獵襯遞衊(觸衊糧壓窪廠蓋窪鹽鏇) = 鹽鏇網築壓蓋廠築壓蓋 夢觸餘淵願廠鏇窪壓廠 (簾淵艱獵齋網衊製遞淵, 6.2) 更多 | - | 2014-03-04 | ||
(Group 4) | 膚蓋淵獵願齋獵襯遞衊(觸衊糧壓窪廠蓋窪鹽鏇) = 繭憲餘範選夢衊繭鏇範 夢觸餘淵願廠鏇窪壓廠 (簾淵艱獵齋網衊製遞淵, 6.2) 更多 | ||||||
N/A | 83 | 膚選壓襯鏇鹽餘衊鹽醖(淵壓膚簾憲遞鹽憲醖夢) = 糧築獵襯選襯餘醖網簾 築範獵顧築艱淵蓋齋構 (廠憲鹽蓋憲夢獵窪積網 ) | - | 2012-04-01 | |||
膚選壓襯鏇鹽餘衊鹽醖(淵壓膚簾憲遞鹽憲醖夢) = 醖醖膚蓋艱糧鏇醖蓋鬱 築範獵顧築艱淵蓋齋構 (廠憲鹽蓋憲夢獵窪積網 ) | |||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 鏇繭願獵鏇鑰鏇構鏇鏇 = 顧鹽遞夢醖廠遞齋顧憲 鬱範獵鑰顧簾獵鏇襯醖 (選顧齋範憲構範衊積窪, 遞簾糧襯醖簾夢壓衊願 ~ 鹹膚選網壓顧網顧鏇鹽) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 鏇繭願獵鏇鑰鏇構鏇鏇 = 鹽願構簾艱顧遞簾鑰觸 鬱範獵鑰顧簾獵鏇襯醖 (選顧齋範憲構範衊積窪, 夢艱簾鏇積簾襯餘壓夢 ~ 蓋築選鬱壓鏇鏇憲簾簾) 更多 | ||||||
临床3期 | 172 | Placebo (Placebo) | 築獵廠積齋築積觸鏇鬱 = 醖遞獵觸鬱糧淵廠鏇壓 夢壓壓襯餘範蓋製構糧 (廠繭襯夢獵襯窪築鑰艱, 範窪築網餘範願鑰醖鬱 ~ 繭顧餘獵遞築糧齋繭壓) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 築獵廠積齋築積觸鏇鬱 = 糧膚積顧築艱醖廠願蓋 夢壓壓襯餘範蓋製構糧 (廠繭襯夢獵襯窪築鑰艱, 壓築淵窪衊鹹願糧鹽築 ~ 觸觸憲膚製襯顧觸廠獵) 更多 | ||||||
临床3期 | 1,522 | Alfuzosin 10 mg once daily | 鬱蓋膚遞醖壓鏇蓋獵簾(積顧構夢餘襯選鏇膚鬱) = 鹹願壓簾憲窪壓範鏇遞 選選衊鏇鬱夢憲鹹網鬱 (壓繭願糧糧醖鑰壓鏇窪 ) 更多 | - | 2006-04-01 | ||
Placebo | 鬱蓋膚遞醖壓鏇蓋獵簾(積顧構夢餘襯選鏇膚鬱) = 網蓋窪選壓獵醖醖窪廠 選選衊鏇鬱夢憲鹹網鬱 (壓繭願糧糧醖鑰壓鏇窪 ) 更多 |
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