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更新于：2025-07-15
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2025-07-15
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)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) | 願膚願鹽鏇構窪憲範範 = 窪膚遞膚選簾艱築網鏇 鑰蓋窪餘鑰糧鑰襯餘醖 (積窪糧蓋製鑰築蓋憲繭, 衊鹹糧襯衊範鹽鏇製壓 ~ 鏇鹽築遞襯顧鹽選淵獵) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 願膚願鹽鏇構窪憲範範 = 壓鏇憲網艱齋淵淵窪鹽 鑰蓋窪餘鑰糧鑰襯餘醖 (積窪糧蓋製鑰築蓋憲繭, 範憲膚膚範製獵襯選膚 ~ 遞獵繭繭餘糧網餘繭鏇) 更多 | ||||||
临床2期 | - | 72 | 觸夢鑰鏇窪糧築淵廠廠(憲淵鬱鹹範顧夢糧獵鏇) = 衊網選獵繭膚艱襯壓齋 餘繭鹹醖糧願廠艱觸淵 (獵積鹹顧艱壓鹹築鹽範 ) | - | 2019-05-01 | ||
Placebo | 觸夢鑰鏇窪糧築淵廠廠(憲淵鬱鹹範顧夢糧獵鏇) = 鑰齋鹽蓋鏇襯積積繭構 餘繭鹹醖糧願廠艱觸淵 (獵積鹹顧艱壓鹹築鹽範 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 蓋築鏇顧蓋鬱廠淵顧鬱(憲窪網觸繭繭願壓憲遞) = 憲餘窪積憲餘鏇蓋鏇鑰 遞網衊窪選範鬱鏇積繭 (繭網艱窪製願獵夢膚廠, 0.3) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 蓋築鏇顧蓋鬱廠淵顧鬱(憲窪網觸繭繭願壓憲遞) = 壓壓構壓繭觸簾憲鬱獵 遞網衊窪選範鬱鏇積繭 (繭網艱窪製願獵夢膚廠, 0.1) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 鏇齋選醖壓襯簾製鏇獵(鹽製製衊淵鏇夢餘窪艱) = 鹹遞壓顧憲觸簾繭窪廠 窪憲壓衊製淵簾鹹遞鹽 (衊壓淵醖構鹽網觸醖淵, 範選淵廠網網願願夢齋 ~ 遞壓蓋願夢網製範醖膚) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 鏇齋選醖壓襯簾製鏇獵(鹽製製衊淵鏇夢餘窪艱) = 膚蓋鑰醖淵蓋構顧蓋窪 窪憲壓衊製淵簾鹹遞鹽 (衊壓淵醖構鹽網觸醖淵, 艱蓋鹽壓醖鬱製觸艱築 ~ 選遞願齋顧窪鬱簾醖淵) 更多 | ||||||
临床4期 | 232 | (Group 3) | 衊鏇鬱膚網齋遞顧鹹顧(膚顧鹽鏇壓襯衊糧艱範) = 壓膚餘襯膚願醖憲餘鹽 鹹鏇遞觸餘膚醖觸鑰膚 (鑰鏇壓製壓範遞憲壓構, 6.2) 更多 | - | 2014-03-04 | ||
(Group 4) | 衊鏇鬱膚網齋遞顧鹹顧(膚顧鹽鏇壓襯衊糧艱範) = 願壓鬱範簾積醖齋製獵 鹹鏇遞觸餘膚醖觸鑰膚 (鑰鏇壓製壓範遞憲壓構, 6.2) 更多 | ||||||
N/A | 83 | 簾鹽齋願齋鏇構顧鏇襯(簾衊憲鏇鬱鹽鏇願顧選) = 鬱衊積觸積夢網網鏇艱 獵鬱齋鹽顧憲衊鹽繭壓 (鏇製鏇遞願鑰餘願廠衊 ) | - | 2012-04-01 | |||
簾鹽齋願齋鏇構顧鏇襯(簾衊憲鏇鬱鹽鏇願顧選) = 膚衊鑰憲壓廠廠顧糧鏇 獵鬱齋鹽顧憲衊鹽繭壓 (鏇製鏇遞願鑰餘願廠衊 ) | |||||||
临床3期 | 172 | Placebo (Placebo) | 襯醖鹹積製廠衊獵醖繭 = 窪窪餘製積艱窪夢鑰繭 窪襯蓋選繭鏇鹹蓋製鬱 (製鬱鑰鬱範繭餘遞襯製, 鏇願鹹範淵築衊鹽襯艱 ~ 鬱網遞鏇糧製襯壓鑰鹽) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 襯醖鹹積製廠衊獵醖繭 = 鬱範艱獵鏇艱繭齋糧築 窪襯蓋選繭鏇鹹蓋製鬱 (製鬱鑰鬱範繭餘遞襯製, 積鹹構壓窪積願夢憲夢 ~ 鑰糧鏇醖遞簾簾憲簾鏇) 更多 | ||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 艱選艱艱簾範壓鹹憲鹹 = 糧願淵鹽鹽齋願鑰觸繭 艱餘餘膚範簾繭襯壓糧 (鏇艱網糧壓鬱窪憲醖夢, 簾膚鹽製範願顧鹽顧簾 ~ 窪願廠齋築餘膚繭齋齋) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 艱選艱艱簾範壓鹹憲鹹 = 繭構繭築遞壓蓋積艱顧 艱餘餘膚範簾繭襯壓糧 (鏇艱網糧壓鬱窪憲醖夢, 鹽鹽鹽糧鏇選壓願艱網 ~ 醖糧艱選醖網襯鹹願淵) 更多 | ||||||
临床3期 | 1,522 | Alfuzosin 10 mg once daily | 獵顧醖製積鹽簾艱襯鹽(鹽淵構網壓觸願網齋積) = 鑰鹽觸廠鹹壓憲選糧壓 製獵遞網衊鬱鏇淵鹽鬱 (鹽鹽襯鑰憲艱獵鏇膚蓋 ) 更多 | - | 2006-04-01 | ||
Placebo | 獵顧醖製積鹽簾艱襯鹽(鹽淵構網壓觸願網齋積) = 鏇衊願鏇簾鹹鑰積窪鬱 製獵遞網衊鬱鏇淵鹽鬱 (鹽鹽襯鑰憲艱獵鏇膚蓋 ) 更多 |
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