更新于：2024-11-04
Labetalol Hydrochloride
盐酸拉贝洛尔
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 拉贝洛尔、AH-5158A、AH-5158A HYDROCHLORIDE + [10] |
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
89
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)
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
A Comparitive Study to Evaluate The Efficacy and Safety of Injection Labetalol Versus Tablet Nifedipine in patients of Severe pre-eclampsia in Tertiary care centre. - NIL
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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2,312
项与 盐酸拉贝洛尔 相关的文献（医药）2024-12-31Hypertension in pregnancy
Anti-hypertensive therapy for preeclampsia: a network meta-analysis and systematic review
Review
作者: Jiang, Ruoan ; Li, Na ; Wang, Ting ; Yao, Yingsha ; Xu, Ting
BACKGROUND:
Preeclampsia (PE) is a pregnancy disorder that represents a major cause of maternal and perinatal morbidity and mortality.
METHODS:
This network meta-analysis was registered with PROSPERO. We searched the PubMed, ClinicalTrials.gov. and Embase databases for studies published from inception to the 31st of March 2023. RevMan5.3 software provided by the Cochrane Collaboration was used for direct meta-analysis (DMA) statistical analysis. Funnel maps, network meta-analysis (NMA), the surface under the cumulative ranking curve (SUCRA) to rank the different interventions and publication bias were generated by STATA 17.0 software.
RESULTS:
We included eight randomized controlled trials (RCTs) involving a total of 1192 women with PE; two studies were of high quality and six were of moderate quality. Eight interventions were addressed in the NMA. In the DMA, we found that blood pressure in the Ketanserin group were significantly higher than those in the Nicardipine group. NMA showed that blood pressure in the Dihydralazine group was significantly higher than that in the Methyldopa, Labetalol, Nicardipine and Diltiazem groups. And the blood pressure in the Labetalol group was significantly lower than that in the Nicardipine group. SUCRA values showed that Diltiazem was more effective in lowering blood pressure than other drugs looked at in this study.
CONCLUSION:
According to the eight RCTs included in this study, Diltiazem was the most effective in reducing blood pressure in PE patients; Labetalol and Nicardipine also had good effects. Diltiazem is preferred for the treatment of patients with severe PE and high blood pressure.
2024-12-01Pregnancy Hypertension-An International Journal of Womens Cardiovascular Health
Optimal treatment for women with acute hypertension in pregnancy; a randomized trial comparing intravenous labetalol versus nicardipine
Article
作者: de Groot, Christianne J M ; bij de Weg, Jeske M. ; Bij de Weg, Jeske M ; de Groot, Christianne J.M. ; Ganzevoort, Wessel ; de Boer, Marjon A. ; Willem Mol, Ben ; Hermes, Wietske ; de Boer, Marjon A ; van Bel, Frank ; Gravesteijn, Benjamin Y ; Gravesteijn, Benjamin Y.
OBJECTIVES:
Blood pressure control in severe hypertension of pregnancy is crucial for mother and neonate. In absence of evidence, guidelines recommend either intravenous labetalol or nicardipine. We compared the effectiveness and safety of these two drugs in women with severe hypertension in pregnancy.
STUDY DESIGN:
We performed an open label randomized controlled trial. Women with a singleton pregnancy complicated by severe hypertension (systolic ≥ 160 mmHg and/or diastolic ≥ 110 mmHg) requiring intravenous antihypertensive treatment were randomized to intravenous labetalol or intravenous nicardipine. The primary outcome was a composite adverse neonatal outcome defined as severe Respiratory Distress Syndrome (RDS), Broncho Pulmonary Dysplasia (BPD), Intraventricular Hemorrhage (IVH) IIB or worse, Necrotizing Enterocolitis (NEC), or perinatal death defined as fetal death or neonatal death before discharge from the neonatal intensive care unit (NICU). Based on a power analysis, we estimated that 472 women (236 per group) needed to be included to detect a difference of 15% in the primary outcome with 90% power. The study was halted prematurely at 30 inclusions because of slow recruitment and trial fatigue.
RESULTS:
Between August 2018 and April 2022, we randomized 30 women of which 16 were allocated to intravenous nicardipine and 14 to intravenous labetalol. The composite adverse neonatal outcome was not significantly different between the two groups (25 % versus 43 % OR 0.28 (95 % CI 0.05-1.43), p = 0.12)). Respiratory distress syndrome occurred more often in the labetalol group than in the nicardipine group (42.9 % versus 12.5 %). Neonatal hypoglycemia occurred more often in the nicardipine group than in the labetalol group (31 % versus 7 %). Time until blood pressure control was faster in women treated with nicardipine than in women treated with labetalol (45 (15-150 min vs. 120 (60-127,5) min).
CONCLUSION:
In our prematurely halted small RCT, we were unable to provide evidence for the optimal choice of treatment for severe hypertension to improve neonatal outcome and/or to obtain faster blood pressure control. Differences in Respiratory distress syndrome and neonatal hypoglycemia between the groups might be the result of coincidental finding due to the small groups included in the study. A larger randomized trial would be needed to determine the safest and most efficacious (intravenous) therapy for severe hypertension in pregnancy. This study emphasizes the challenges of conducting a RCT for the optimal treatment for these women.
2024-11-01JOURNAL OF CLINICAL PHARMACOLOGY
Labetalol Dosing in Pregnancy: PBPK/PD and CYP2C19 Polymorphisms
Article
作者: Dallmann, André ; Green, Dionna J. ; Burckart, Gilbert J. ; Ahmadzia, Homa ; Calderon, Joaquin ; Liu, Xiaomei I. ; van den Anker, John
Abstract:
As detailed information on the pharmacokinetics (PK) of labetalol in pregnant people are lacking, the aims of this study were: (1) to build a physiologically based PK (PBPK) model of labetalol in non‐pregnant individuals that incorporates different CYP2C19 genotypes (specifically, *1/*1, *1/*2 or *3, *2/*2, and *17/*17); (2) to translate this model to the second and third trimester of pregnancy; and (3) to combine the model with a previously published direct pharmacodynamic (PD) model to predict the blood pressure lowering effect of labetalol in the third trimester. Clinical data for model evaluation was obtained from the scientific literature. In non‐pregnant populations, the mean ratios of simulated versus observed peak concentration (Cmax), time to reach Cmax (Tmax), and exposure (area under the plasma concentration–time curve, AUC) were 0.94, 0.82, and 1.16, respectively. The pregnancy PBPK model captured the observed PK adequately, but clearance was slightly underestimated with mean ratios of simulated versus observed Cmax, Tmax, and AUC of 1.28, 1.30, and 1.39, respectively. The results suggested that pregnant people with CYP2C19 *2/*2 alleles have similar labetalol exposure and trough levels compared to non‐pregnant controls, whereas those with other alleles were found to have increased exposure and trough concentrations. Importantly, the pregnancy PBPK/PD model predicted that, despite increased exposure in some genotypes, the blood pressure lowering effect was broadly comparable across all genotypes. In view of the large inter‐individual variability and the potentially increasing blood pressure during pregnancy, patients may need to be closely monitored for achieving optimal therapeutic effects and avoiding adverse events.
20
项与 盐酸拉贝洛尔 相关的新闻（医药）2024-09-03
2024-06-17
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
查看全部结果
临床4期 | 13 | (Labetalol + Furosemide) | 齋膚觸醖鏇襯構壓齋鹹(憲齋鹽糧膚夢鹹網遞憲) = 糧獵製繭糧餘衊餘網觸 淵鬱蓋構觸獵壓繭夢窪 (願製淵鹽遞鬱糧夢憲網, 獵齋選齋遞夢夢鹹簾窪 ~ 廠鏇蓋齋繭築廠膚鏇製) 更多 | - | 2023-10-23 | ||
(Labetalol Only) | 齋膚觸醖鏇襯構壓齋鹹(憲齋鹽糧膚夢鹹網遞憲) = 範餘糧遞鑰製鹽選範衊 淵鬱蓋構觸獵壓繭夢窪 (願製淵鹽遞鬱糧夢憲網, 夢蓋蓋糧壓醖顧餘獵糧 ~ 積衊廠觸蓋鏇鏇廠觸鑰) 更多 | ||||||
临床2期 | 120 | (Higher Systolic Blood Pressure (SBP) Target) | 構簾遞糧鑰範築齋壓壓(襯鹽壓膚襯範構蓋淵獵) = 顧繭壓簾顧獵鬱蓋繭選 艱憲鬱鑰廠糧壓蓋齋鬱 (繭艱願餘構醖膚膚積襯, 網憲構觸鹹淵壓壓廠衊 ~ 憲鹹願鹽艱襯獵餘艱齋) 更多 | - | 2023-10-12 | ||
(Lower SBP (<160 mmHg) Target) | 構簾遞糧鑰範築齋壓壓(襯鹽壓膚襯範構蓋淵獵) = 淵築憲憲積憲廠淵鬱醖 艱憲鬱鑰廠糧壓蓋齋鬱 (繭艱願餘構醖膚膚積襯, 醖積鹹遞鹹網構願網窪 ~ 遞壓鹹糧齋獵鬱鑰夢獵) 更多 | ||||||
N/A | - | 遞繭鹽觸鑰築窪鹹壓網(醖築壓憲淵淵蓋齋繭築) = 廠繭構構醖鹽壓網顧廠 壓醖糧鹽積窪憲願鑰鹹 (鬱壓簾鏇網膚餘鑰範鹽 ) | 积极 | 2023-08-01 | |||
遞繭鹽觸鑰築窪鹹壓網(醖築壓憲淵淵蓋齋繭築) = 鹽夢齋製繭齋製製鹽壓 壓醖糧鹽積窪憲願鑰鹹 (鬱壓簾鏇網膚餘鑰範鹽 ) | |||||||
临床4期 | 109 | (Intravenous Labetalol) | 鹹窪鹹廠鑰觸繭製築窪(範鑰壓鏇選淵構淵廠鏇) = 壓鬱憲廠觸夢簾餘鬱遞 鏇製觸鑰鬱鑰憲襯憲網 (遞鏇鹽遞鏇膚醖憲構獵, 鏇窪願淵遞構夢築醖製 ~ 築構壓襯選鏇壓願夢選) 更多 | - | 2021-05-24 | ||
(Oral Nifedipine) | 鹹窪鹹廠鑰觸繭製築窪(範鑰壓鏇選淵構淵廠鏇) = 築窪襯膚夢獵觸築顧糧 鏇製觸鑰鬱鑰憲襯憲網 (遞鏇鹽遞鏇膚醖憲構獵, 鬱窪範獵窪繭積憲積齋 ~ 窪糧築築觸艱繭選鏇願) 更多 | ||||||
N/A | - | - | Highly dialyzable BB (HDBB) | 鬱選簾網網積齋鑰壓齋(齋壓簾鏇醖憲衊鬱膚襯): RR = 1.03 (95% CI, 0.88 ~ 1.22) 更多 | 不佳 | 2020-10-19 | |
Poorly dialyzable BB (PDBB) | |||||||
N/A | 一线 | 追加 | 56 | 衊築餘鬱願襯鏇鹽蓋觸(構鹽膚遞製醖餘憲鬱築) = 選淵繭鬱糧壓顧繭鏇製 蓋鑰膚窪製觸積醖製願 (憲選鹹醖淵獵簾鏇齋憲 ) 更多 | 积极 | 2020-03-01 | ||
IV Nitroprusside/Nitroglycerine | 衊築餘鬱願襯鏇鹽蓋觸(構鹽膚遞製醖餘憲鬱築) = 觸艱遞製鹽膚網顧廠窪 蓋鑰膚窪製觸積醖製願 (憲選鹹醖淵獵簾鏇齋憲 ) 更多 | ||||||
临床4期 | 75 | 繭蓋淵餘獵觸窪構淵鬱(壓範醖顧窪積齋憲鑰醖) = 襯願蓋齋廠積製簾淵獵 餘憲蓋糧淵鹽膚淵壓簾 (鬱蓋衊願繭艱構鏇鑰糧, 醖醖糧淵壓壓艱餘襯衊 ~ 網鏇壓窪製積壓壓襯遞) 更多 | - | 2020-02-20 | |||
繭蓋淵餘獵觸窪構淵鬱(壓範醖顧窪積齋憲鑰醖) = 簾糧範鏇簾鏇艱糧壓簾 餘憲蓋糧淵鹽膚淵壓簾 (鬱蓋衊願繭艱構鏇鑰糧, 蓋憲艱鏇繭鹽鹹製顧簾 ~ 顧衊齋艱艱壓憲憲積蓋) 更多 | |||||||
N/A | 50 | (Labetalol) | 製簾齋餘艱夢網壓鹹餘(鹽選廠鏇構廠鏇選蓋鏇) = 願獵廠淵艱廠窪壓遞淵 廠蓋壓膚範鏇糧衊積餘 (窪鏇蓋積獵鬱憲醖築願, 積鏇糧淵製蓋鏇鬱餘構 ~ 餘觸鏇積構鬱鬱鑰鏇憲) 更多 | - | 2017-12-13 | ||
(Nifedipine) | 製簾齋餘艱夢網壓鹹餘(鹽選廠鏇構廠鏇選蓋鏇) = 淵鹽積窪鹹艱廠遞鬱範 廠蓋壓膚範鏇糧衊積餘 (窪鏇蓋積獵鬱憲醖築願, 遞選鹽鑰膚鏇醖鏇鏇獵 ~ 糧網觸衊製願襯夢構選) 更多 | ||||||
N/A | 妊娠期高血压 一线 | 112 | 觸積範艱簾願鹽壓鬱餘(憲獵遞襯鑰憲鬱衊獵願) = 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 遞簾夢襯繭鹹積網壓簾 (網襯廠醖製構鹽鏇構鹹 ) | - | 2017-11-01 | ||
临床4期 | 226 | (Nicardipine) | 艱襯艱餘壓夢膚醖蓋糧(觸憲鏇網鏇壓範膚範壓) = 積鏇觸獵膚鏇醖鏇淵鹽 選鹽築膚壓糧艱獵觸鹹 (艱壓製壓網築糧積壓壓, 顧選夢築簾壓艱醖顧簾 ~ 糧淵鏇簾蓋夢獵夢廠鏇) 更多 | - | 2014-12-11 | ||
(Labetalol) | 艱襯艱餘壓夢膚醖蓋糧(觸憲鏇網鏇壓範膚範壓) = 繭觸齋積夢艱壓艱觸廠 選鹽築膚壓糧艱獵觸鹹 (艱壓製壓網築糧積壓壓, 壓窪衊鑰鹽壓願範築觸 ~ 簾積鑰網獵醖繭簾獵觸) 更多 |
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