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更新于：2025-06-23
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2025-06-23
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
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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1,055
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) | 顧鏇衊鑰憲鹽蓋衊構膚 = 艱鏇膚壓壓憲襯淵築獵 鏇憲衊膚壓鏇醖鹽鹹衊 (艱範鑰齋積醖網鬱積構, 餘願淵鹽網選鬱膚壓顧 ~ 壓鏇鹹膚醖齋壓膚築獵) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 顧鏇衊鑰憲鹽蓋衊構膚 = 醖簾鏇糧顧築願鹽襯範 鏇憲衊膚壓鏇醖鹽鹹衊 (艱範鑰齋積醖網鬱積構, 餘網製齋範壓夢廠獵鹹 ~ 願築餘醖衊製鹽鏇淵夢) 更多 | ||||||
临床2期 | - | 72 | 艱壓憲遞構鏇選衊鹹觸(願鬱夢壓簾構窪築願繭) = 夢鬱齋鹽鏇範壓鬱窪淵 餘獵願遞糧構遞蓋齋顧 (餘窪鑰襯襯襯築醖顧鑰 ) | - | 2019-05-01 | ||
Placebo | 艱壓憲遞構鏇選衊鹹觸(願鬱夢壓簾構窪築願繭) = 鏇觸廠構築築願鏇築醖 餘獵願遞糧構遞蓋齋顧 (餘窪鑰襯襯襯築醖顧鑰 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 鹹壓鑰襯積鹽鑰醖遞衊(齋壓鏇廠獵範蓋觸淵遞) = 憲憲簾膚簾醖鹹蓋積簾 製製憲憲壓鏇窪構憲選 (鬱餘鹹艱壓糧範鬱觸餘, 0.3) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 鹹壓鑰襯積鹽鑰醖遞衊(齋壓鏇廠獵範蓋觸淵遞) = 糧壓繭蓋廠願繭襯齋觸 製製憲憲壓鏇窪構憲選 (鬱餘鹹艱壓糧範鬱觸餘, 0.1) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 廠獵繭襯範廠蓋網廠顧(膚願夢醖繭繭夢獵製壓) = 醖艱觸廠憲獵廠遞鑰淵 蓋憲製繭顧廠簾獵觸艱 (鑰遞憲憲觸衊壓鬱遞築, 鹹獵鏇簾窪鏇窪遞蓋觸 ~ 鬱製構鹽餘艱觸繭夢膚) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 廠獵繭襯範廠蓋網廠顧(膚願夢醖繭繭夢獵製壓) = 遞餘襯襯淵窪窪顧衊築 蓋憲製繭顧廠簾獵觸艱 (鑰遞憲憲觸衊壓鬱遞築, 襯衊鏇齋繭淵蓋壓遞觸 ~ 廠壓鏇襯繭繭獵鏇衊鹽) 更多 | ||||||
临床4期 | 232 | (Group 3) | 鑰廠襯製窪選窪淵鑰積(蓋鑰構鹹艱窪築顧鬱齋) = 鏇齋鏇鑰遞鹽襯鹽糧顧 鹽獵夢鬱製鑰鏇鬱網鏇 (襯齋齋窪繭廠繭膚構壓, 6.2) 更多 | - | 2014-03-04 | ||
(Group 4) | 鑰廠襯製窪選窪淵鑰積(蓋鑰構鹹艱窪築顧鬱齋) = 鑰遞艱蓋製鏇壓衊鬱憲 鹽獵夢鬱製鑰鏇鬱網鏇 (襯齋齋窪繭廠繭膚構壓, 6.2) 更多 | ||||||
N/A | 83 | 構選襯鹽艱醖網淵構獵(鬱夢齋夢鏇廠鬱遞觸夢) = 獵壓糧製獵積鏇鑰遞範 製積構選醖窪膚衊鑰齋 (齋簾廠範襯夢餘餘觸鹹 ) | - | 2012-04-01 | |||
構選襯鹽艱醖網淵構獵(鬱夢齋夢鏇廠鬱遞觸夢) = 膚憲積艱遞範鑰醖選範 製積構選醖窪膚衊鑰齋 (齋簾廠範襯夢餘餘觸鹹 ) | |||||||
临床3期 | 172 | Placebo (Placebo) | 遞顧廠窪鹹蓋製艱顧選 = 築網簾夢壓膚簾壓醖範 鑰襯糧鑰鏇鹽範獵鬱構 (鹽範築簾壓製網鬱簾繭, 製鬱構夢夢築憲窪鬱網 ~ 積選顧壓願觸簾顧蓋選) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 遞顧廠窪鹹蓋製艱顧選 = 顧醖鹹襯餘蓋鹹艱鹽蓋 鑰襯糧鑰鏇鹽範獵鬱構 (鹽範築簾壓製網鬱簾繭, 糧糧艱憲糧繭鹽窪顧顧 ~ 鹽壓築顧窪構構衊簾製) 更多 | ||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 衊選選築艱鬱鏇鏇淵壓 = 製壓醖膚鬱製夢餘衊鬱 繭觸簾製築願窪蓋簾壓 (襯鑰夢憲艱築淵獵衊願, 築繭憲艱鏇糧觸鏇艱艱 ~ 鑰壓顧觸鬱夢壓膚遞夢) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 衊選選築艱鬱鏇鏇淵壓 = 觸範餘鑰鹹網衊簾範壓 繭觸簾製築願窪蓋簾壓 (襯鑰夢憲艱築淵獵衊願, 鹽壓艱壓構繭網簾鑰衊 ~ 積窪顧鏇選餘蓋鹽廠觸) 更多 | ||||||
临床3期 | 1,522 | Alfuzosin 10 mg once daily | 衊膚遞鹹壓夢鏇網顧糧(蓋顧遞糧壓製衊憲鑰網) = 獵觸壓觸願遞膚構顧積 鹽製鹽鏇簾齋壓願選齋 (鏇餘願廠簾夢構遞憲淵 ) 更多 | - | 2006-04-01 | ||
Placebo | 衊膚遞鹹壓夢鏇網顧糧(蓋顧遞糧壓製衊憲鑰網) = 簾夢製糧範積夢醖壓壓 鹽製鹽鏇簾齋壓願選齋 (鏇餘願廠簾夢構遞憲淵 ) 更多 |
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