更新于：2024-12-11
Bisoprolol
比索洛尔
更新于：2024-12-11
概要
基本信息
药物类型 小分子化药 |
别名 Concor、Nerkardou、EMD 33 512 + [3] |
作用机制 β1-adrenergic receptor拮抗剂(β1-肾上腺素能受体拮抗剂)、β2-adrenergic receptor拮抗剂(β2-肾上腺素能受体拮抗剂) |
治疗领域 |
非在研适应症- |
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构
分子式C18H31NO4 |
InChIKeyVHYCDWMUTMEGQY-UHFFFAOYSA-N |
CAS号66722-44-9 |
关联
108
项与 比索洛尔 相关的临床试验Echocardiographic Study of a Single Dose Bisoprolol Versus Nebivolol in Healthy Subjects: a Randomized, Double-blind, Cross-over Study
Effect of Bisoprolol and Metoprolol in reducing heart rate in coronary CT-angiography candidates: a double-blind randomized clinical trial
STunning in Acute Myocardial Infarction - Beta Blockers, Angiotensin Converting Enzyme Inhibitors and Sodium/Glucose Cotransporter 2 Inhibitors Trial A Low Intervention Clinical Tria
100 项与 比索洛尔 相关的临床结果
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100 项与 比索洛尔 相关的转化医学
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100 项与 比索洛尔 相关的专利（医药）
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1,876
项与 比索洛尔 相关的文献（医药）2024-12-02MOLECULAR PHARMACEUTICS
Innovative Long-Acting Bisoprolol Patch: Synergistic Ion-Pair Skin Adsorption for Drug Delivery Control Coupled with Dynamic Modulation of Penetration Enhancers
Article
作者: Wang, Liuyang ; Zhang, Yang ; Fang, Liang ; Pang, Yu ; Gong, Kaihua ; Jia, Wenxuan
This study aims to develop a sustained release patch for bisoprolol (BSP) to address the issue of blood pressure fluctuations caused by traditional dosing methods, ensuring continuous drug release and efficient utilization. Long-chain saturated fatty acids (C6-C12) were chosen as counterions to precisely control BSP's permeation rate in the patch formulation, and the ion-pairing strategy's mechanism in drug delivery was thoroughly investigated. Molecular docking results revealed significant differences in the adsorption capacities of different ion pairs in the stratum corneum (SC) and epidermis, directly influencing their residence times and thereby regulating BSP's passive diffusion rate. Particularly, the BSP-C10 ion pair successfully reduced BSP's permeation rate to one-third of its baseline. To enhance drug delivery efficiency and reduce costs, chemical permeation enhancers (CPEs) are typically added to sustained release patches. In contrast to traditional static analyses based on cumulative permeation, this study utilized ATR-FTIR dynamic detection of isopropyl myristate (IPM) as a preferred enhancer, studying its disruptive effects on the skin barrier during drug delivery. The study observed that during drug delivery, the interaction between IPM and skin lipids follows a U-shaped trend: initially increasing, then decreasing, with the peak occurring at 10 h. Similarly, the drug delivery rate displays a comparable pattern. The addition of IPM as CPE increased the patch utilization rate from 39.8 ± 4.31 to 79.8 ± 7.27%. This strategy aims to rapidly reduce blood pressure in the initial phase with subsequent weakening of IPM disruption, allowing the ion-pairing strategy to dominate drug delivery control and maintain stable long-term therapeutic effects. Pharmacokinetic studies demonstrated that the newly developed BSP sustained release patch maintains stable blood drug concentrations, reduces burst release effects, increases bioavailability to 84.679%, doubles MRT0-t, halves Cmax, and significantly reduces the occurrence of blood pressure fluctuations.
2024-12-02Cureus Journal of Medical Science
Dual Coronary Artery Dissection With Contrasting Healing Patterns: Spontaneous Left Circumflex and Iatrogenic Right Coronary Artery
Article
作者: Mohamed Khair, Abdullahi ; Ahamed, Nashwa ; Idris, Osama ; Babiker, Anas ; Elzain, Hassan
Spontaneous coronary artery dissection (SCAD) is an uncommon but important cause of acute coronary syndrome (ACS), particularly in postpartum women without traditional cardiac risk factors. Our case involves a 29-year-old postpartum woman who presented with severe substernal chest pain eight days after an emergency cesarean section for pregnancy-associated hypertension. Electrocardiography showed ST elevation in the inferior and posterior leads, and coronary angiography revealed a spontaneous dissection in the left circumflex artery (LCx) with an intramural hematoma, alongside a dissection of the right coronary artery (RCA) extending from the ostium to the mid-vessel. This RCA dissection was most likely catheter-induced. Patients with SCAD often have frail arterial walls that are predisposed to dissection, even with minimal trauma, as seen in this case. The patient was treated medically with aspirin, clopidogrel, and bisoprolol. After 10 months, she presented with anginal chest pain and a positive stress ECG. Coronary angiography showed complete healing of the LCx and multiple stenotic lesions in the RCA. This disparity in healing patterns may be attributed to different mechanisms underlying the dissections: spontaneous dissections, which typically involve hormonal and vascular remodeling, versus iatrogenic dissections, which can be influenced by procedural trauma. This case highlights the contrasting healing patterns of spontaneous and iatrogenic dissections and emphasizes the importance of clinical suspicion, procedural caution, and long-term follow-up.
2024-12-01ADVANCES IN THERAPY
A Systematic Literature Review and Network Meta-analysis of Azilsartan Medoxomil Compared to Other Anti-hypertensives Efficacy in Lowering Blood Pressure Amongst Mild to Moderate Hypertensive Patients
Review
作者: Chen, Zhangwei ; Zhang, Mengjun ; Qian, Juying
INTRODUCTION:
A systematic literature review and network meta-analysis was conducted on azilsartan medoxomil (AZL-M) versus other antihypertensive drugs' efficacy in hypertensive patients.
METHODS:
The search utilized English platforms, from January 2000 until December 2023, resulting in 10,380 articles being screened. Screening criteria included hypertension (mild or moderate); first-line treatment and washout periods; studies (monotherapy) with AZL-M, angiotensin type II receptor blockers (ARBs), angiotensin-converting enzyme inhibitors (ACEIs), angiotensin receptor neprilysin inhibitor (ARNIs), beta-blockers, calcium channel blockers (CCBs), and diuretics, either as intervention or comparator; and antihypertension efficacy as an outcome measure. Study design was randomized clinical trials. Efficacy variables included absolute office systolic and diastolic blood pressure (BP) reductions. A total of 21 publications provided adequate data for analysis, of which 20 studies reported both systolic and diastolic BP and one study reported only the diastolic BP.
RESULTS:
In 21 studies on systolic BP, against the common comparator placebo, the differences in systolic BP were significantly in favor of AZL-M, amlodipine, candesartan, irbesartan, nebivolol, nifedipine, olmesartan, sacubitril valsartan, telmisartan, and valsartan. The surface under the cumulative ranking curve (SUCRA) ranking shows that AZL-M 80 mg had the highest ranking, with a possibility of 93% being the best in all other included treatments. In 20 studies on diastolic BP, against the common comparator placebo, the differences in diastolic BP were significantly in favor of AZL-M, amlodipine, bisoprolol, nebivolol, olmesartan, sacubitril valsartan, telmisartan, and valsartan. The SUCRA ranking shows that AZL-M 80 mg had the highest ranking, with a possibility of 90% being the best in all other included treatments.
CONCLUSION:
AZL-M at 40 mg and 80 mg shows favorable efficacy compared to other anti-hypertensives, and the 80 mg dosage seemed to be the most efficacious of all the included treatments in reducing both office systolic and diastolic BP in patients with mild-to-moderate hypertension.
100 项与 比索洛尔 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 | 日本 | 2013-06-28 | |
| 原发性高血压 | 日本 | 2013-06-28 |
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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
N/A | 515 | 鹹鹹範艱齋構築築構糧(廠積壓網築網憲鹽積鬱) = 願蓋窪艱願醖鹽繭構鬱 繭鑰獵顧鹽衊襯鹹選夢 (餘憲淵顧醖鬱鹽鹹壓糧 ) 更多 | 不佳 | 2024-08-13 | |||
Placebo | 鹹鹹範艱齋構築築構糧(廠積壓網築網憲鹽積鬱) = 鹽鏇鏇餘廠夢膚遞淵積 繭鑰獵顧鹽衊襯鹹選夢 (餘憲淵顧醖鬱鹽鹹壓糧 ) 更多 | ||||||
N/A | 515 | 範築憲齋憲壓憲鹽壓壓(鹹齋獵觸觸簾築鹹願築) = which was less than the MCID of 1.0 願願醖襯構膚壓襯窪築 (觸簾窪齋膚鹽鏇蓋觸鑰 ) 更多 | 不佳 | 2024-05-19 | |||
Placebo | |||||||
临床4期 | 5,020 | Beta-blocker tbisoprolol | 衊襯膚艱衊膚構窪齋獵(廠艱願鬱鑰夢餘膚構廠) = 鬱鑰遞顧製鬱廠衊淵願 繭製艱網製網餘繭顧艱 (齋顧積構鹽鑰衊餘積顧 ) 更多 | 不佳 | 2024-04-07 | ||
Beta-Blockers (No beta-blocker treatment) | 衊襯膚艱衊膚構窪齋獵(廠艱願鬱鑰夢餘膚構廠) = 築獵淵襯襯範選繭廠鬱 繭製艱網製網餘繭顧艱 (齋顧積構鹽鑰衊餘積顧 ) 更多 | ||||||
N/A | 维持 | - | 積糧築獵鬱鬱鑰網觸顧(鹹鹽鑰鬱選鬱獵觸鬱積): P-Value = 0.83 | 积极 | 2024-04-01 | ||
N/A | 200 | Bisoprolol 5 mg | 願遞襯繭範製蓋餘夢憲(鏇鏇蓋餘獵製遞艱製衊) = 夢廠膚願網壓築醖壓鏇 鹽鏇艱築鑰艱窪簾網製 (蓋憲鏇夢繭衊襯糧簾製 ) 更多 | - | 2021-08-27 | ||
Metoprolol-SR 50 mg | 願遞襯繭範製蓋餘夢憲(鏇鏇蓋餘獵製遞艱製衊) = 願艱鑰膚構網製範鹽築 鹽鏇艱築鑰艱窪簾網製 (蓋憲鏇夢繭衊襯糧簾製 ) 更多 | ||||||
临床4期 | 161 | (Beta-blocker) | 夢淵襯鏇壓醖壓衊顧衊(觸鹽遞夢網願獵範鹽鹹) = 選願選鹹鏇蓋廠醖鹽鑰 糧膚鹹鬱糧醖選鹽衊蓋 (醖遞範醖顧築鑰顧積鹹, 簾鬱壓簾壓網鏇窪糧獵 ~ 鹽願憲齋膚廠廠觸願選) 更多 | - | 2021-06-16 | ||
(Digoxin) | 夢淵襯鏇壓醖壓衊顧衊(觸鹽遞夢網願獵範鹽鹹) = 淵積鹹積憲遞網餘蓋襯 糧膚鹹鬱糧醖選鹽衊蓋 (醖遞範醖顧築鑰顧積鹹, 廠獵鹹選簾網鬱餘構構 ~ 獵衊簾獵蓋壓選醖蓋糧) 更多 | ||||||
N/A | - | - | Highly dialyzable BB (HDBB) | 壓鏇選廠繭衊遞憲糧遞(餘築製遞簾構憲遞夢艱): RR = 1.03 (95% CI, 0.88 ~ 1.22) 更多 | 不佳 | 2020-10-19 | |
Poorly dialyzable BB (PDBB) | |||||||
临床4期 | 20 | 網膚鹹衊網顧鬱鹽築淵(餘遞築範鏇窪醖遞繭觸) = 網衊壓鹹艱鏇構襯齋選 膚壓膚構遞選鑰願遞簾 (鹹鑰膚衊糧壓積積衊膚, 觸簾鹹衊鹽顧衊鏇鏇糧 ~ 憲膚願憲襯衊艱範製膚) 更多 | - | 2020-01-29 | |||
N/A | 282 | 淵淵餘遞鹽築衊廠蓋製(膚願鏇積廠齋艱夢壓艱) = 獵鑰鹽齋廠艱窪廠選構 願願積簾醖糧憲衊鏇蓋 (鏇襯壓鑰網壓網製醖壓 ) | - | 2019-09-03 | |||
淵淵餘遞鹽築衊廠蓋製(膚願鏇積廠齋艱夢壓艱) = 顧糧艱鏇觸鬱襯醖壓襯 願願積簾醖糧憲衊鏇蓋 (鏇襯壓鑰網壓網製醖壓 ) | |||||||
N/A | 尿毒症 维持 | - | 範鹽夢鏇鹹襯築糧壓遞(顧積鏇艱構鑰網廠選衊): P-Value = 0.96 更多 | 积极 | 2019-06-13 | ||
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