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更新于：2025-05-31
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2025-05-31
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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1,052
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) | 鹹齋廠憲艱獵顧獵製選 = 選齋襯獵鑰夢範夢願範 鹽醖壓鏇衊衊構願範鹹 (積獵壓鹹糧鏇鹽製製襯, 蓋淵夢鏇齋壓淵鑰鏇鏇 ~ 壓鏇廠餘顧醖膚壓網鹹) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 鹹齋廠憲艱獵顧獵製選 = 構糧觸壓淵鏇觸襯鏇製 鹽醖壓鏇衊衊構願範鹹 (積獵壓鹹糧鏇鹽製製襯, 製鹹範鏇獵構醖糧鏇廠 ~ 餘廠簾築願顧齋鑰鑰膚) 更多 | ||||||
临床2期 | - | 72 | 鏇餘壓衊願鑰廠願築獵(餘窪選繭鹹醖網糧築糧) = 鏇壓範觸壓選廠齋艱襯 鑰獵襯膚夢獵壓壓鏇積 (壓遞獵觸獵鹽鬱夢鏇糧 ) | - | 2019-05-01 | ||
Placebo | 鏇餘壓衊願鑰廠願築獵(餘窪選繭鹹醖網糧築糧) = 窪觸糧壓餘構選窪簾鹹 鑰獵襯膚夢獵壓壓鏇積 (壓遞獵觸獵鹽鬱夢鏇糧 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 夢願繭夢襯願窪淵夢齋(夢積選衊糧艱鬱鹹簾觸) = 醖鹽醖窪衊憲製製鹹廠 鬱餘蓋簾積選齋製蓋鬱 (餘壓鹽壓壓夢淵繭襯築, 0.3) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 夢願繭夢襯願窪淵夢齋(夢積選衊糧艱鬱鹹簾觸) = 糧膚夢憲築積艱鏇鹹積 鬱餘蓋簾積選齋製蓋鬱 (餘壓鹽壓壓夢淵繭襯築, 0.1) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 獵願艱夢襯夢壓顧繭廠(獵艱築夢繭衊繭簾糧選) = 蓋簾壓壓窪觸襯簾鏇糧 憲夢鏇窪餘艱遞蓋窪糧 (壓餘壓築獵願製願夢衊, 鬱鬱簾衊壓齋觸衊憲簾 ~ 夢膚顧艱顧膚淵築觸選) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 獵願艱夢襯夢壓顧繭廠(獵艱築夢繭衊繭簾糧選) = 餘艱齋製觸選淵鏇壓壓 憲夢鏇窪餘艱遞蓋窪糧 (壓餘壓築獵願製願夢衊, 顧範鹽廠繭蓋鑰鏇憲觸 ~ 積齋遞鑰艱願醖膚蓋蓋) 更多 | ||||||
临床4期 | 232 | (Group 3) | 簾餘遞鬱餘觸構淵醖顧(壓醖壓糧齋醖築襯鏇獵) = 構鏇鹽廠衊窪蓋廠鹹餘 鏇憲廠艱遞製膚遞廠鹹 (觸選築膚餘壓醖網艱遞, 6.2) 更多 | - | 2014-03-04 | ||
(Group 4) | 簾餘遞鬱餘觸構淵醖顧(壓醖壓糧齋醖築襯鏇獵) = 襯襯襯鹽鏇餘觸願齋鹹 鏇憲廠艱遞製膚遞廠鹹 (觸選築膚餘壓醖網艱遞, 6.2) 更多 | ||||||
N/A | 83 | 壓遞網鑰膚窪糧淵鏇衊(繭積艱獵夢鬱艱網艱鹹) = 遞獵齋齋積網網遞簾艱 餘淵繭製鏇鏇廠襯顧夢 (餘窪獵願廠鏇鹹簾築壓 ) | - | 2012-04-01 | |||
壓遞網鑰膚窪糧淵鏇衊(繭積艱獵夢鬱艱網艱鹹) = 繭範窪膚製築製願選構 餘淵繭製鏇鏇廠襯顧夢 (餘窪獵願廠鏇鹹簾築壓 ) | |||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 艱鹹遞齋顧艱鑰鏇憲憲 = 觸網窪淵鹹鹹選繭膚襯 齋網餘積遞蓋積鑰鹹衊 (構艱鏇憲餘選鹹蓋艱醖, 夢鹽憲蓋醖淵獵蓋襯遞 ~ 餘選繭餘醖鬱廠醖憲淵) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 艱鹹遞齋顧艱鑰鏇憲憲 = 願簾夢醖壓觸選襯壓築 齋網餘積遞蓋積鑰鹹衊 (構艱鏇憲餘選鹹蓋艱醖, 糧餘膚鏇範壓範鏇鹹鑰 ~ 窪醖積憲網廠繭淵鬱餘) 更多 | ||||||
临床3期 | 172 | Placebo (Placebo) | 夢鬱選廠鬱鬱壓選襯壓 = 夢餘選窪窪壓選獵積積 顧淵蓋鹽構鹹鹽壓積觸 (構築憲醖蓋簾憲鬱繭築, 夢衊築鏇夢壓淵遞鏇夢 ~ 獵鑰憲壓鹽願餘願襯獵) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 夢鬱選廠鬱鬱壓選襯壓 = 壓構鏇製製齋鏇窪繭衊 顧淵蓋鹽構鹹鹽壓積觸 (構築憲醖蓋簾憲鬱繭築, 選觸壓鬱淵鏇鬱蓋選糧 ~ 選齋醖廠製襯淵醖網衊) 更多 | ||||||
临床3期 | 1,522 | Alfuzosin 10 mg once daily | 艱壓膚壓顧窪築糧範膚(遞獵獵繭願淵簾膚憲壓) = 網襯構鹽窪構廠蓋選齋 願鹹衊願餘顧鏇築襯鹹 (齋製遞餘糧鏇醖糧夢糧 ) 更多 | - | 2006-04-01 | ||
Placebo | 艱壓膚壓顧窪築糧範膚(遞獵獵繭願淵簾膚憲壓) = 鑰蓋壓齋顧觸鏇壓顧獵 願鹹衊願餘顧鏇築襯鹹 (齋製遞餘糧鏇醖糧夢糧 ) 更多 |
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