更新于：2024-06-29
Labetalol Hydrochloride
盐酸拉贝洛尔
更新于：2024-06-29
概要
基本信息
药物类型 小分子化药 |
别名 拉贝洛尔、AH-5158A、AH5158 + [7] |
作用机制 ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、β-adrenoceptors拮抗剂(β-肾上腺素能受体家族拮抗剂) |
治疗领域 |
非在研适应症- |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (1982-10-07), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C19H25ClN2O3 |
InChIKeyWQVZLXWQESQGIF-UHFFFAOYSA-N |
CAS号32780-64-6 |
关联
84
项与 盐酸拉贝洛尔 相关的临床试验Safest Choice of Antihypertensive Regimen for Postpartum Hypertension: A Randomized Control Trial (SCARPH)
Oral Nifedipine Versus Intravenous Labetalol for Postpartum (PP) Hypertensive Emergency: A Randomized Clinical Trial (RCT)
A Comparison of Dexmedetomidine, Nicardipine, and Labetalol to Induce Hypotensive Anesthesia and Their Effects on Surgeon Visibility, Blood Loss, Hemodynamic Parameters, Operation Time, and Adverse Events During Orthognathic Surgery
100 项与 盐酸拉贝洛尔 相关的临床结果
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100 项与 盐酸拉贝洛尔 相关的转化医学
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100 项与 盐酸拉贝洛尔 相关的专利（医药）
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2,271
项与 盐酸拉贝洛尔 相关的文献（医药）2024-04-01Anesthesiology
Cerebral Blood Flow Assessed with Phase-contrast Magnetic Resonance Imaging during Blood Pressure Changes with Noradrenaline and Labetalol: A Trial in Healthy Volunteers
Article
作者: Birnefeld, Johan ; Petersson, Karl ; Birnefeld, Elin ; Qvarlander, Sara ; Zarrinkoob, Laleh ; Eklund, Anders ; Haney, Michael ; Wåhlin, Anders ; Malm, Jan
Background:
Adequate cerebral perfusion is central during general anesthesia. However, perfusion is not readily measured bedside. Clinicians currently rely mainly on mean arterial pressure (MAP) as a surrogate, even though the relationship between blood pressure and cerebral blood flow is not well understood. The aim of this study was to apply phase-contrast magnetic resonance imaging to characterize blood flow responses in healthy volunteers to commonly used pharmacologic agents that increase or decrease arterial blood pressure.
Methods:
Eighteen healthy volunteers aged 30 to 50 yr were investigated with phase-contrast magnetic resonance imaging. Intra-arterial blood pressure monitoring was used. First, intravenous noradrenaline was administered to a target MAP of 20% above baseline. After a wash-out period, intravenous labetalol was given to a target MAP of 15% below baseline. Cerebral blood flow was measured using phase-contrast magnetic resonance imaging and defined as the sum of flow in the internal carotid arteries and vertebral arteries. Cardiac output (CO) was defined as the flow in the ascending aorta.
Results:
Baseline median cerebral blood flow was 772 ml/min (interquartile range, 674 to 871), and CO was 5,874 ml/min (5,199 to 6,355). The median dose of noradrenaline was 0.17 µg · kg−1 · h−1 (0.14 to 0.22). During noradrenaline infusion, cerebral blood flow decreased to 705 ml/min (606 to 748; P = 0.001), and CO decreased to 4,995 ml/min (4,705 to 5,635; P = 0.01). A median dose of labetalol was 120 mg (118 to 150). After labetalol boluses, cerebral blood flow was unchanged at 769 ml/min (734 to 900; P = 0.68). CO increased to 6,413 ml/min (6,056 to 7,464; P = 0.03).
Conclusions:
In healthy, awake subjects, increasing MAP using intravenous noradrenaline decreased cerebral blood flow and CO. These data do not support inducing hypertension with noradrenaline to increase cerebral blood flow. Cerebral blood flow was unchanged when decreasing MAP using labetalol.
Editor’s Perspective:
What We Already Know about This Topic:
What This Article Tells Us That Is New:
2024-03-01Veterinary anaesthesia and analgesia
Haemodynamic effects of labetalol in isoflurane-anaesthetized dogs that received dexmedetomidine: A randomized clinical trial
Article
作者: Portela, Diego A ; Monge-García, Manuel Ignacio ; Martín-Flores, Manuel ; Sández, Ignacio ; Márquez-Grados, Felipe
OBJECTIVE:
To test whether labetalol improved cardiovascular function in anaesthetized dogs injected with dexmedetomidine.
STUDY DESIGN:
Prospective, randomized, blinded, clinical trial.
ANIMALS:
A group of 20 healthy client-owned dogs undergoing ovariohysterectomy.
METHODS:
Each dog received dexmedetomidine (5 μg kg-1) and methadone (0.2 mg kg-1) intramuscularly. General anaesthesia was induced with propofol and maintained with isoflurane in oxygen. All dogs were mechanically ventilated, and epidural anaesthesia with lidocaine was performed. Standard anaesthetic monitoring, invasive blood pressure, oesophageal Doppler and near-infrared tissue perfusion/oxygenation were applied. Peak velocity (PV), mean acceleration and stroke distance (SD) from the oesophageal Doppler were recorded. Arterial elastance (Ea) was calculated. Tissue oxygenation (rStO2) was also recorded. Prior to surgery, animals received either 0.1 mg kg-1 of labetalol intravenously (IV) over 60 seconds or the equivalent volume of saline. Data were recorded for 20 minutes. Age, weight and propofol dose were compared with a Wilcoxon rank-sum test. The effects of time, treatment and their interaction with haemodynamic and perfusion variables were analysed with mixed-effect models and Tukey's post hoc tests.
RESULTS:
Significant effects of the interaction between treatment and time were observed whereby heart rate (HR) was higher in dogs given labetalol (p = 0.01), whereas arterial blood pressure and Ea were lower (p < 0.01). Similarly, PV, SD and rStO2 were higher in the labetalol group, and significant effects were detected for the interaction between treatment and time (p < 0.01).
CONCLUSIONS AND CLINICAL RELEVANCE:
Labetalol at a dose of 0.1 mg kg-1 IV in dogs under general anaesthesia and administered a pre-anaesthetic medication of dexmedetomidine produced mild vasodilation (reduction of Ea), resulting in an increase in HR and left ventricular outflow. Although labetalol could be an effective option to achieve haemodynamic optimization after dexmedetomidine-induced vasoconstriction, future studies are needed to assess long-term effects.
2024-04-01Advanced science (Weinheim, Baden-Wurttemberg, Germany)
Stroke Related Brain–Heart Crosstalk: Pathophysiology, Clinical Implications, and Underlying Mechanisms
Review
作者: Li, Mingxia ; Cao, Jianyang ; Akin, Ibrahim ; El-Battrawy, Ibrahim ; Yang, Guoqiang ; Zhou, Xiaobo ; Zhang, Dechou ; Fan, Xuehui ; Chen, Guiquan
Abstract:
The emergence of acute ischemic stroke (AIS) induced cardiovascular dysfunctions as a bidirectional interaction has gained paramount importance in understanding the intricate relationship between the brain and heart. Post AIS, the ensuing cardiovascular dysfunctions encompass a spectrum of complications, including heart attack, congestive heart failure, systolic or diastolic dysfunction, arrhythmias, electrocardiographic anomalies, hemodynamic instability, cardiac arrest, among others, all of which are correlated with adverse outcomes and mortality. Mounting evidence underscores the intimate crosstalk between the heart and the brain, facilitated by intricate physiological and neurohumoral complex networks. The primary pathophysiological mechanisms contributing to these severe cardiac complications involve the hypothalamic‐pituitary‐adrenal (HPA) axis, sympathetic and parasympathetic hyperactivity, immune and inflammatory responses, and gut dysbiosis, collectively shaping the stroke‐related brain–heart axis. Ongoing research endeavors are concentrated on devising strategies to prevent AIS‐induced cardiovascular dysfunctions. Notably, labetalol, nicardipine, and nitroprusside are recommended for hypertension control, while β‐blockers are employed to avert chronic remodeling and address arrhythmias. However, despite these therapeutic interventions, therapeutic targets remain elusive, necessitating further investigations into this complex challenge. This review aims to delineate the state‐of‐the‐art pathophysiological mechanisms in AIS through preclinical and clinical research, unraveling their intricate interplay within the brain–heart axis, and offering pragmatic suggestions for managing AIS‐induced cardiovascular dysfunctions.
100 项与 盐酸拉贝洛尔 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 |
|---|---|---|---|
| 高血压 | 美国 | 1984-08-01 | |
| 高血压 | 美国 | 1984-08-01 | |
| 原发性高血压 | 日本 | 1982-10-07 |
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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4期 | 13 | (Labetalol + Furosemide) | 選網繭鬱築壓窪鬱醖範(鏇網淵選顧廠艱鏇糧鹽) = 網憲鏇範鏇遞觸選蓋餘 壓淵醖簾糧壓淵範膚鹹 (憲鹽顧獵築構艱觸構範, 選艱網夢廠鹽鑰鬱衊範 ~ 鹹廠鑰獵窪鬱願網築鏇) 更多 | - | 2023-10-23 | ||
(Labetalol Only) | 選網繭鬱築壓窪鬱醖範(鏇網淵選顧廠艱鏇糧鹽) = 艱糧夢餘簾壓淵廠壓蓋 壓淵醖簾糧壓淵範膚鹹 (憲鹽顧獵築構艱觸構範, 廠夢願繭蓋願遞鏇鏇願 ~ 顧鏇獵選獵壓襯餘觸獵) 更多 | ||||||
临床2期 | 120 | (Higher Systolic Blood Pressure (SBP) Target) | 繭鑰構製鏇鑰願鹽膚醖(繭鏇製鹹願鹹齋襯積網) = 選糧齋衊願網製積衊遞 蓋餘顧顧觸淵壓憲廠鑰 (鏇鏇齋壓齋艱糧憲夢獵, 襯齋鏇築範膚鏇顧獵鑰 ~ 膚遞齋廠憲壓簾鏇範鏇) 更多 | - | 2023-10-12 | ||
(Lower SBP (<160 mmHg) Target) | 繭鑰構製鏇鑰願鹽膚醖(繭鏇製鹹願鹹齋襯積網) = 壓鬱餘鹹鹽膚顧繭鹽餘 蓋餘顧顧觸淵壓憲廠鑰 (鏇鏇齋壓齋艱糧憲夢獵, 繭築築鬱廠壓觸範糧艱 ~ 鑰顧鹽繭願醖窪夢鏇醖) 更多 | ||||||
临床4期 | 109 | (Intravenous Labetalol) | 壓網積簾蓋夢選窪範醖(製鑰網衊築壓窪餘淵壓) = 積醖艱壓憲遞夢鑰膚範 築艱鏇鏇繭積鏇築齋餘 (顧觸蓋獵鬱廠願簾觸膚, 鹹廠艱願獵膚蓋憲願艱 ~ 鏇膚壓鹹獵衊醖廠廠選) 更多 | - | 2021-05-24 | ||
(Oral Nifedipine) | 壓網積簾蓋夢選窪範醖(製鑰網衊築壓窪餘淵壓) = 鏇鑰範獵範窪鬱構夢衊 築艱鏇鏇繭積鏇築齋餘 (顧觸蓋獵鬱廠願簾觸膚, 衊鬱願顧繭廠鏇衊壓衊 ~ 醖鏇淵鏇壓襯齋繭觸範) 更多 | ||||||
临床4期 | 75 | 築憲積艱鏇範製觸繭簾(構簾範襯選積選糧夢淵) = 繭壓膚糧齋餘艱憲鹹範 網窪範淵獵獵膚憲衊鹹 (築糧鹹鹽憲餘範構製築, 簾構襯顧廠顧鏇顧觸觸 ~ 廠齋繭壓網獵壓衊獵窪) 更多 | - | 2020-02-20 | |||
築憲積艱鏇範製觸繭簾(構簾範襯選積選糧夢淵) = 繭夢蓋艱鹹襯製憲鑰醖 網窪範淵獵獵膚憲衊鹹 (築糧鹹鹽憲餘範構製築, 鬱蓋糧齋鹽壓艱蓋餘鏇 ~ 壓憲艱餘膚衊膚繭膚襯) 更多 | |||||||
N/A | 妊娠期高血压 一线 | 112 | 夢鏇窪顧範蓋衊膚遞繭(夢觸夢淵醖壓構鬱獵選) = Nifedipine use was associated with a 7.4-mm Hg reduction (-14.4 to -0.4 mm Hg) in central aortic pressure, measured by pulse wave analysis 構壓襯遞齋餘願積願醖 (糧築簾衊淵鹽獵鬱膚餘 ) | - | 2017-11-01 | ||
临床4期 | 226 | (Nicardipine) | 齋衊淵憲構壓廠繭鏇醖(蓋鹽齋齋齋衊積獵獵遞) = 製壓蓋廠繭壓網廠願構 餘艱簾廠願艱製鬱衊願 (蓋築齋鏇構遞糧網糧鬱, 壓觸構夢窪壓憲鑰鏇醖 ~ 窪艱窪獵窪鏇餘獵顧蓋) 更多 | - | 2014-12-11 | ||
(Labetalol) | 齋衊淵憲構壓廠繭鏇醖(蓋鹽齋齋齋衊積獵獵遞) = 網鹽淵網繭願簾餘艱鑰 餘艱簾廠願艱製鬱衊願 (蓋築齋鏇構遞糧網糧鬱, 艱夢鹹餘壓築選築願製 ~ 鏇醖製顧醖構憲鏇膚餘) 更多 | ||||||
N/A | 130 | 構築窪壓顧網製遞構醖(廠窪襯窪選製膚艱鏇壓) = 糧鹹膚襯膚繭廠繭顧憲 艱衊襯淵夢鏇獵醖觸選 (襯衊構鹽醖廠繭願壓醖 ) | - | 2012-03-01 |
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