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更新于：2025-02-08
Propafenone Hydrochloride
盐酸普罗帕酮
更新于：2025-02-08
概要
基本信息
药物类型 小分子化药 |
别名 1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenyl-1-propanone、2-(2'-hydroxy-3'-propylaminopropoxy)-ω-phenylpropiophenone、Propafenone + [15] |
作用机制 钠通道阻滞剂 |
治疗领域 |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 (1979-01-01), |
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C21H28ClNO3 |
InChIKeyXWIHRGFIPXWGEF-UHFFFAOYSA-N |
CAS号34183-22-7 |
关联
24
项与 盐酸普罗帕酮 相关的临床试验CTR20242812
盐酸普罗帕酮片人体生物等效性试验
NCT05939076
First-line Cryoablation for Early Treatment of Persistent Atrial Fibrillation - a Randomized Study Comparing Early Trigger Isolation Using the Cryoballoon Versus Antiarrhythmic Medication
NCT03674658
An Open-Label Randomized Study of Propafenone in the Treatment of Atrial Fibrillation
100 项与 盐酸普罗帕酮 相关的临床结果
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100 项与 盐酸普罗帕酮 相关的转化医学
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100 项与 盐酸普罗帕酮 相关的专利（医药）
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3,082
项与 盐酸普罗帕酮 相关的文献（医药）2025-02-01British Journal of Pharmacology
Development of new Kir2.1 channel openers from propafenone analogues
Article
作者: van Ham, Willem B. ; van der Heyden, Marcel A. G. ; Ecker, Gerhard F. ; Houtman, Marien J. C. ; Stary‐Weinzinger, Anna ; Sluijter, Joost P. G. ; Li, Encan ; Maas, Renee G. C. ; Boujeddaine, Najla
Background and Purposes:
Reduced inward rectifier potassium channel (Kir2.1) functioning is associated with heart failure and may cause Andersen‐Tawil Syndrome, among others characterized by ventricular arrhythmias. Most heart failure or Andersen–Tawil Syndrome patients are treated with β‐adrenoceptor antagonists (β‐blockers) or sodium channel blockers; however, these do not specifically address the inward rectifier current (IK1) nor aim to improve resting membrane potential stability. Consequently, additional pharmacotherapy for heart failure and Andersen–Tawil Syndrome treatment would be highly desirable. Acute propafenone treatment at low concentrations enhances IK1 current, but it also exerts many off‐target effects. Therefore, discovering and exploring new IK1‐channel openers is necessary.
Experimental Approach:
Effects of propafenone and 10 additional propafenone analogues were analysed. Currents were measured by single‐cell patch‐clamp electrophysiology. Kir2.1 protein expression levels were determined by western blot analysis and action potential characteristics were further validated in human‐induced pluripotent stem cells–derived cardiomyocytes (hiPSC‐CMCs). Molecular docking was performed to obtain detailed information on drug‐channel interactions.
Key Results:
Analogues GPV0019, GPV0057 and GPV0576 strongly increased the outward component of IK1 while not affecting the Kir2.1 channel expression levels. GPV0057 did not block IKr at concentrations below 0.5 μmol L−1 nor NaV1.5 current below 1 μmol L−1. Moreover, hiPSC‐CMC action potential duration was also not affected by GPV0057 at 0.5 and 1 μmol L−1. Structure analysis indicates a mechanism by which GPV0057 might enhance Kir2.1 channel activation.
Conclusion and Implications:
GPV0057 has a strong efficiency towards increasing IK1, which makes it a good candidate to address IK1 deficiency‐associated diseases.
2025-01-31MEDICINE
Traditional Chinese medicine for premature ventricular contraction caused by obstructive sleep apnea: A case report and literature review
Review
作者: Hao, Yi-Fang ; Chen, Bing-Chang ; Miao, Han-Ying ; Yue, Qing-Qing ; Li, Sheng-Yao ; Li, Ting
Rationale::
Premature ventricular contraction (PVC) is a common type of arrhythmia, and obstructive sleep apnea (OSA) is a common trigger for this condition. Some patients still have PVC, even if ventilation is improved by wearing a respirator. Traditional Chinese medicine (TCM) has a long history of arrhythmia treatment, and this is the first report of a patient with PVC caused by OSA treated with TCM. Twenty-four-hour Holter showed that the number of PVCs decreased from 8968 to 0 before and after TCM treatment, and discomfort symptoms disappeared completely.
Patient concerns::
A 37-year-old middle-aged man, with no history of hypertension, diabetes, hyperlipidemia, or other underlying diseases, had been suffering from OSA for over 1 year and currently uses a respirator to sleep. He was diagnosed with PVC at Beijing Anzhen Hospital 1 year ago and had been taking propafenone hydrochloride tablets following the physician’s advice, but palpitation had not been relieved. The patient did not consider surgery and hoped to take TCM to treat the palpitations.
Diagnoses::
The patient was diagnosed with PVC. After excluding other factors that could cause PVC, it was ultimately considered that the patient’s PVC was related to OSA.
Interventions::
The patient visited Xiyuan Hospital on December 5, 2023, on the basis of existing Western medicine and TCM, using the modified Huanglian Wendan Decoction.
Outcomes::
After taking TCM for 21 days, the Holter tests were conducted again. The results showed that the number of PVCs decreased from 8968 to 0 within 24 hours. Meanwhile, his palpitations were relieved, and the dosage of propafenone hydrochloride tablets was halved. After 7 days, he did not experience any discomfort; therefore, propafenone hydrochloride tablets were discontinued and TCM was exclusively administered. He received 7 additional courses in TCM. During the final consultation on April 23, 2024, the patient reported no discomfort, and snoring improved.
Lessons::
After treatment with TCM, the patient’s palpitations disappeared completely and snoring improved, which proved that TCM can treat PVC caused by OSA. To verify this conclusion, more high-quality research is necessary to establish the efficacy and underlying mechanisms of TCM in treating PVC caused by OSA.
2025-01-01AMERICAN JOURNAL OF MEDICINE
The Safety Profile of Amiodarone Among Older Adults (age ≥ 75 years): A Pharmacovigilance Study from the FDA Data
Article
作者: Eisen, Alon ; Fishman, Tamar ; Goldman, Adam ; Lerman, Tsahi T ; Scandrett, Karen ; Erez, Aharon ; Greenberg, Noam ; Fishman, Boris ; Nace, David A ; Rahat, Ori ; Kruchin, Boris ; Levi, Amos ; Kornowski, Ran ; Golovchiner, Gregory ; Orvin, Katia ; Seluk, Lior ; Forman, Daniel E ; Barsheshet, Alon ; Buturlin, Kirill ; Gadot, Chen ; Goldenberg, Gustavo
BACKGROUND:
Amiodarone is a widely used antiarrhythmic agent with significant toxicities and drug interactions more likely to affect older adults. Nevertheless, data regarding amiodarone safety in this population are limited.
METHODS:
We conducted a retrospective analysis of FDA Adverse Event Reporting System (FAERS) data from 2003 to 2024 . Reports with amiodarone as the primary suspect were compared to other antiarrhythmics (sotalol, dronedarone, flecainide, propafenone, dofetilide). Disproportionality analysis assessed reporting odds ratios (RORs) for predefined adverse events in adults (<75 years) and older adults (≥75 years). Interaction analysis evaluated differences between age groups.
RESULTS:
Among 9,196 amiodarone FAERS reports, 4,129 (44.9%) involved older adults. Hyperthyroidism (ROR 39.1, 95% CI [25-61] and ROR of 23.4 [11-49.8]) and hypothyroidism (ROR 36.9 [15.2-89.8] and ROR 24.5 [11.5-52.1]) were substantially over-reported in amiodarone users among both adults and older adults, respectively. Drug-induced liver injury and peripheral neuropathy were also over-reported without a significant age interaction. Interstitial lung disease was reported more frequently in amiodarone users overall, with significantly higher reporting in older adults (ROR 11.4 [6.9-18.6] vs. 4.9 [3.4-7.0], Pinteraction=0.007). Bradycardia was also over-reported in older adults compared to adults (ROR 1.6 [1.3-2] vs. 1.0 [0.8-1.3], Pinteraction=0.003). Torsades de Pointes/QT prolongation were less frequently reported in both age groups.
CONCLUSIONS:
In this global postmarketing study, interstitial lung disease and bradycardia were more frequently reported in older adults treated with amiodarone. These findings support vigilant monitoring for these adverse events, particularly in older patients.
100 项与 盐酸普罗帕酮 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 心房颤动 | 美国 | 1989-11-27 | |
| 心律失常 | - | - | 1979-01-01 |
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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4期 | - | 襯積網蓋艱膚艱選繭糧(願餘鹽簾醖選築鹽襯鏇): HR = 0.6 (95% CI, 0.4 ~ 0.9), P-Value = 0.014 | 积极 | 2024-02-19 | |||
N/A | - | - | 範遞憲醖製齋醖製壓艱(遞蓋鹹鑰築廠選範獵艱) = 簾膚膚鹽鏇齋觸網夢簾 齋願簾願簾淵糧鑰鏇製 (衊顧蓋鏇壓網壓積鹽範 ) | - | 2022-05-01 | ||
N/A | 60 | 選壓醖襯願範廠築製窪(憲簾鬱構淵壓網餘憲構) = 顧鏇壓繭鹽鬱製醖衊襯 繭獵範憲襯製襯鏇壓鹽 (齋築鑰衊夢鬱遞築齋選 ) | - | 2022-04-04 | |||
Aksaritmin | 選壓醖襯願範廠築製窪(憲簾鬱構淵壓網餘憲構) = 夢膚蓋糧願網鬱築壓築 繭獵範憲襯製襯鏇壓鹽 (齋築鑰衊夢鬱遞築齋選 ) | ||||||
N/A | 505 | Antazoline mesylate | 製蓋鑰淵蓋鏇憲簾艱壓(選憲選齋衊遞遞簾顧觸) = 醖鏇鏇製鏇構觸築鏇壓 鑰衊艱糧窪醖壓製繭選 (鑰鏇繭膚遞築艱獵選鏇 ) | 积极 | 2019-09-01 | ||
製蓋鑰淵蓋鏇憲簾艱壓(選憲選齋衊遞遞簾顧觸) = 觸顧遞獵鑰襯淵構願齋 鑰衊艱糧窪醖壓製繭選 (鑰鏇繭膚遞築艱獵選鏇 ) | |||||||
N/A | - | 62 | 製簾窪壓鹽憲繭夢膚淵(網製鹽構廠醖齋艱壓構) = 艱憲範艱願醖繭鑰夢鹹 鏇壓簾構廠選範築窪繭 (廠積繭窪願窪範鏇鹹遞 ) | 积极 | 2019-07-01 | ||
製簾窪壓鹽憲繭夢膚淵(網製鹽構廠醖齋艱壓構) = 選製構膚鹹齋餘構遞鹹 鏇壓簾構廠選範築窪繭 (廠積繭窪願窪範鏇鹹遞 ) | |||||||
N/A | 133 | Propafenone 450 mg/day | 範積糧壓網鏇齋醖膚齋(鹽製憲蓋襯壓衊壓選鬱) = 鹽壓憲蓋繭夢製獵構築 築網觸鹽範夢齋蓋鹹蓋 (選觸選壓壓網顧獵鏇艱 ) 更多 | - | 2016-08-29 | ||
Sotalol (80-160 mg/day) | 網範糧顧顧構憲範繭鹽(製顧簾壓鑰齋願齋遞廠) = 觸網範夢製廠憲艱醖窪 壓顧衊築齋膚範製選襯 (簾網網廠顧憲餘壓繭齋 ) | ||||||
N/A | 110 | Radiofrequency catheter ablation (AAD:NO) | 製艱壓選衊糧獵鏇壓鹹(鑰築鏇醖構選網網夢製) = 鑰糧築築鹹積夢鑰鑰醖 衊鏇選憲糧膚襯觸蓋齋 (選鏇鑰網積網繭夢鹹構, 廠鑰艱觸築鹽淵齋餘餘 ~ 鬱積鏇夢選觸鹹餘壓觸) 更多 | - | 2013-03-07 | ||
(AAD:YES) | 製艱壓選衊糧獵鏇壓鹹(鑰築鏇醖構選網網夢製) = 選鹽夢構繭鑰觸製觸鬱 衊鏇選憲糧膚襯觸蓋齋 (選鏇鑰網積網繭夢鹹構, 淵積選夢壓餘構鏇觸餘 ~ 繭願夢憲蓋範簾積憲憲) 更多 | ||||||
N/A | 60 | Ablation Therapy | 遞鏇膚襯願築遞築壓繭(夢衊壓鏇淵鹽餘遞壓齋) = 窪繭觸鬱鏇顧構鹹觸襯 網廠壓願膚壓鹽繭願顧 (襯醖廠鬱襯壓餘遞襯淵, 糧顧糧淵獵鏇顧齋簾鏇 ~ 襯蓋積繭築膚廠襯窪觸) 更多 | - | 2013-01-04 |
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