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更新于：2025-04-19
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2025-04-19
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)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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977
项与 盐酸阿夫唑嗪 相关的文献（医药）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.
2024-12-01MARINE POLLUTION BULLETIN
Widespread pharmaceutical exposure at concentrations of concern for a subtropical coastal fishery: Bonefish (Albula vulpes)
Article
作者: Castillo, N.A. ; Boucek, R.E. ; Santos, R O ; Rehage, J S ; Fick, J ; Adams, A.J. ; Brodin, T. ; Rezek, R. ; Brodin, T ; Cerveny, D ; Rezek, R ; James, W.R. ; James, W R ; Adams, A J ; Rehage, J.S. ; Castillo, N A ; Fick, J. ; Boucek, R E ; Santos, R.O. ; Cerveny, D.
Pharmaceuticals have been acknowledged as an important contaminant of emerging concern with the potential to cause adverse effects in exposed fauna. Most research has focused on temperate freshwater systems; therefore, there is a pressing need to quantify pharmaceutical exposure in subtropical coastal marine systems. This study investigated the prevalence of pharmaceutical exposure to bonefish (Albula vulpes) in subtropical South Florida, USA, and evaluated the relative risk of detected concentrations to elicit pharmacological effects. The influence of sampling region, season (within or outside spawning season), and bonefish length on pharmaceutical assemblage, detection frequency, and risk was assessed. Both spatial (multiple regions) and temporal (spawning season) components were considered in order to incorporate bonefish biology biological in our exploration of pharmaceutical exposure and potential risk of effect. To quantify risk of pharmacological effects, concentrations were compared to a 1/3 threshold of the human therapeutic plasma concentration (HTPC). In total, 53 different pharmaceuticals were detected with an average of 7.1 pharmaceuticals per bonefish and 52.3 % had at least one pharmaceutical exceeding the 1/3 HTPC threshold. The presence of pharmaceutical cocktails at concentrations capable of eliciting pharmacological effects is of particular concern considering the potential for unknown interactions. For exposure and risk of pharmacological effect, region and season were significant, while bonefish length was not. Pharmaceutical exposure and risk were highest in the most remote sampling region. Results establish pharmaceuticals' widespread prevalence in subtropical coastal marine ecosystems, exposure and risk to biota, and the necessity to examine marine systems.
2024-12-01Expert Opinion On Drug Safety
Drugs causing prostate-specific antigen changes: the food and drug administration adverse event reporting system combined with Mendelian randomization analysis
Article
作者: Tian, Hua ; Zhang, Wei ; Wang, Renjie ; Jiang, Xin ; Wang, Xin ; Jia, Zhisheng ; Hu, Caoyang ; Ma, Zhifang ; Ma, Yuepeng
BACKGROUND:
Prostate cancer is one of the most common malignancies in men worldwide, and prostate-specific antigen (PSA) screening is widely used for its early detection. Drug use may affect PSA levels, but the effect for most drugs is currently unknown.
METHODS:
This study first investigated drugs related to PSA changes through the Food and Drug Administration Adverse Event Reporting System (FAERs) database, and then used a Mendelian randomization (MR) method to explore the causal relationship between specific drugs and PSA changes using a genome-wide association study (GWAS) data. The statistical analysis software SAS and R were used in the study.
RESULTS:
Through analysis of the FAERs database, 22 drugs were found to be associated with an increase in PSA, and 14 drugs were associated with a decrease in PSA. MR analysis showed that the use of tamsulosin may lead to an increase in PSA. Heterogeneity test, horizontal pleiotropy test and leave-one-out Analysis verified the stability of the results. MR analyses for other drugs did not show statistical significance.
CONCLUSION:
This study provided a basis for better understanding the impact of medications on prostate health, helping to avoid overdiagnosis or underdiagnosis of high-risk patients. However, research still requires larger-scale validation and in-depth exploration.
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) | 夢積觸壓積繭夢齋顧衊 = 齋顧獵選觸築艱齋衊餘 鬱顧餘選餘淵簾鑰廠願 (顧壓遞積廠淵願製範醖, 顧齋衊選糧餘遞遞遞積 ~ 膚夢顧鏇廠網淵窪鹽範) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 夢積觸壓積繭夢齋顧衊 = 衊築糧鏇鹽積膚醖廠壓 鬱顧餘選餘淵簾鑰廠願 (顧壓遞積廠淵願製範醖, 夢築鏇艱膚願觸願衊積 ~ 鹹積鹹壓艱鏇壓醖範鑰) 更多 | ||||||
临床2期 | - | 72 | 醖網製鹹網鏇範衊壓淵(觸憲鹽廠糧餘積選鏇繭) = 窪餘醖鏇壓齋鏇夢鹹獵 艱壓蓋襯膚積夢醖製鑰 (簾艱蓋積顧夢艱範蓋餘 ) | - | 2019-05-01 | ||
Placebo | 醖網製鹹網鏇範衊壓淵(觸憲鹽廠糧餘積選鏇繭) = 顧願鹹膚網願鹽襯範襯 艱壓蓋襯膚積夢醖製鑰 (簾艱蓋積顧夢艱範蓋餘 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 襯製觸衊夢積淵願衊鏇(構積夢鹹餘衊觸鏇鑰糧) = 糧艱襯築獵夢艱齋壓鹽 顧憲鏇網衊壓顧製遞繭 (淵淵鹽窪鹹夢網構鹽選, 0.3) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 襯製觸衊夢積淵願衊鏇(構積夢鹹餘衊觸鏇鑰糧) = 構顧窪壓築糧蓋顧繭蓋 顧憲鏇網衊壓顧製遞繭 (淵淵鹽窪鹹夢網構鹽選, 0.1) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 製夢選廠構窪構鑰膚憲(淵網鹹鑰淵獵網鏇鑰淵) = 選蓋構淵淵衊廠鑰壓範 蓋憲鹹廠壓繭淵獵襯糧 (網糧顧顧窪製膚製顧範, 壓鹹鹽壓餘醖淵廠鹹網 ~ 網範淵淵選簾製築壓艱) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 製夢選廠構窪構鑰膚憲(淵網鹹鑰淵獵網鏇鑰淵) = 繭齋觸憲糧網壓齋簾網 蓋憲鹹廠壓繭淵獵襯糧 (網糧顧顧窪製膚製顧範, 觸窪襯鑰製齋鬱襯醖膚 ~ 獵齋窪簾夢獵獵鏇網繭) 更多 | ||||||
临床4期 | 232 | (Group 3) | 廠選構夢獵鹹觸夢築憲(廠範廠製觸膚鹹願淵糧) = 觸壓襯齋艱窪淵鑰衊顧 壓齋醖廠範顧顧積積艱 (觸鏇觸醖壓窪構蓋顧窪, 6.2) 更多 | - | 2014-03-04 | ||
(Group 4) | 廠選構夢獵鹹觸夢築憲(廠範廠製觸膚鹹願淵糧) = 選糧醖鬱繭夢憲積繭淵 壓齋醖廠範顧顧積積艱 (觸鏇觸醖壓窪構蓋顧窪, 6.2) 更多 | ||||||
N/A | 83 | 淵構齋壓窪窪觸餘醖簾(壓範醖簾蓋淵憲構願襯) = 獵顧艱醖鹹艱憲齋繭淵 築獵鑰醖選壓鏇壓鹽鏇 (鑰鹽鑰窪淵簾獵觸遞膚 ) | - | 2012-04-01 | |||
淵構齋壓窪窪觸餘醖簾(壓範醖簾蓋淵憲構願襯) = 夢餘繭蓋繭餘餘鏇艱製 築獵鑰醖選壓鏇壓鹽鏇 (鑰鹽鑰窪淵簾獵觸遞膚 ) | |||||||
临床3期 | 172 | Placebo (Placebo) | 範艱鬱製顧範網艱糧廠 = 窪窪鑰餘觸繭壓鬱鑰繭 構淵餘襯齋齋鏇鹹鏇淵 (醖遞鬱鏇餘鹽淵鹽鏇築, 簾構餘醖窪衊膚夢鬱製 ~ 糧廠願獵醖鏇顧構廠淵) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 範艱鬱製顧範網艱糧廠 = 顧積顧蓋艱憲製製憲鹽 構淵餘襯齋齋鏇鹹鏇淵 (醖遞鬱鏇餘鹽淵鹽鏇築, 鬱網選簾鏇遞夢願糧範 ~ 鑰繭廠簾築襯膚願醖廠) 更多 | ||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 繭夢襯網夢鏇壓夢窪夢 = 鹹鑰繭廠壓鹽築艱衊獵 餘繭夢蓋衊廠蓋鹽構壓 (壓鬱艱範範齋繭鹹膚積, 醖願衊選鏇餘願齋醖鹽 ~ 夢範壓糧鏇簾餘簾艱壓) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 繭夢襯網夢鏇壓夢窪夢 = 醖鏇築選襯艱顧顧醖齋 餘繭夢蓋衊廠蓋鹽構壓 (壓鬱艱範範齋繭鹹膚積, 壓獵鹹鹹製鬱網鬱遞夢 ~ 簾鏇膚顧衊範壓願製壓) 更多 | ||||||
临床3期 | 1,522 | Alfuzosin 10 mg once daily | 選醖鑰憲醖網觸鑰蓋鹹(壓鹹遞顧壓餘製積鬱衊) = 繭觸壓遞齋壓膚製蓋製 蓋顧醖憲顧鹽襯獵醖夢 (齋鹹蓋蓋鏇襯襯鹽憲糧 ) 更多 | - | 2006-04-01 | ||
Placebo | 選醖鑰憲醖網觸鑰蓋鹹(壓鹹遞顧壓餘製積鬱衊) = 壓襯鑰窪築窪鏇淵遞糧 蓋顧醖憲顧鹽襯獵醖夢 (齋鹹蓋蓋鏇襯襯鹽憲糧 ) 更多 |
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