Delving into the Latest Updates on Labetalol Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

拉贝洛尔

+ [10]

Target

ADRA1 x β-adrenoceptors

Mechanism

ADRA1 antagonists(Adrenergic receptor alpha-1 antagonists), β-adrenoceptors antagonists(Beta adrenergic receptors antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

HypertensionEssential Hypertension

Inactive Indication-

Originator Organization

GSK Plc

Active Organization

Jiangsu Desano Pharmaceutical Co. Ltd.Hikma Pharmaceuticals USA, Inc.Sandoz AG

Inactive Organization

Schering Corp.

Alvogen, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (07 Oct 1982),

Essential Hypertension

Regulation-

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Structure

Molecular FormulaC19H24N2O3

InChIKeySGUAFYQXFOLMHL-UHFFFAOYSA-N

CAS Registry36894-69-6

View All Structures (2)

Though intravenous thrombolysis has been shown to improve symptoms in acute ischemic stroke patients, the recanalization rate remains low (22.6%) and only around 30% of patients benefit from the treatment. Recently, endovascular thrombectomy using stent retrievers or catheters has proven to be more effective, with a success rate of nearly 80%. However, only 50% of patients experience clinical improvement, highlighting the need for new treatment strategies to enhance outcomes. Current guidelines recommend maintaining systolic blood pressure (BP) below 180 mmHg after thrombectomy, but there is a lack of evidence regarding optimal blood pressure management post-reperfusion.
Four randomized clinical trials, including the OPTIMAL-BP trial, have examined blood pressure control following thrombectomy. Meta-analyses showed that intensive BP lowering did not reduce symptomatic hemorrhage and was associated with worse functional outcomes at 3 months. Specifically, lowering BP too aggressively after successful reperfusion could worsen outcomes by reducing perfusion to the ischemic penumbra. Therefore, this study will investigate whether a more targeted blood pressure elevation strategy could improve patient prognosis compared to standard BP control in those with post-thrombectomy systolic BP below 140 mmHg.
This is a prospective, randomized, open-label trial with blinded endpoint assessment (PROBE) design, aimed at comparing intensive and standard BP control strategies in acute ischemic stroke patients. Participants will be randomized 1:1 into either an intensive BP control group (targeting a 20% systolic BP increase, capped at 180 mmHg) or a standard BP control group (systolic BP below 180 mmHg).

Start Date01 Dec 2024

Sponsor / Collaborator

Yonsei University

NCT05551104 / RecruitingPhase 3IIT

Safest Choice of Antihypertensive Regimen for Postpartum Hypertension: A Randomized Control Trial (SCARPH)

The purpose of this investigator-initiated randomized control trial is to determine whether oral Nifedipine versus oral Labetalol is superior in controlling high blood pressures in the postpartum period.

Start Date01 Dec 2024

Sponsor / Collaborator

Loma Linda University

CTRI/2024/11/076120 / Not yet recruitingNot ApplicableIIT

Comparitive study of esmolol and labetalol in attenuation of pressor response to laryngoscopy and endotracheal intubation in patients posted under general anaesthesia:a randomised double blind study. - NIL

Start Date10 Nov 2024

Sponsor / Collaborator-

100 Clinical Results associated with Labetalol Hydrochloride

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100 Translational Medicine associated with Labetalol Hydrochloride

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100 Patents (Medical) associated with Labetalol Hydrochloride

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2,324

Literatures (Medical) associated with Labetalol Hydrochloride

31 Dec 2024·Hypertension in Pregnancy

Anti-hypertensive therapy for preeclampsia: a network meta-analysis and systematic review

Review

Author: Wang, Ting ; Jiang, Ruoan ; Yao, Yingsha ; Xu, Ting ; Li, Na

BACKGROUNDPreeclampsia (PE) is a pregnancy disorder that represents a major cause of maternal and perinatal morbidity and mortality.METHODSThis network meta-analysis was registered with PROSPERO. We searched the PubMed, ClinicalTrials.gov. and Embase databases for studies published from inception to the 31^st 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.RESULTSWe 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.CONCLUSIONAccording 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.

01 Dec 2024·European Journal of Obstetrics & Gynecology and Reproductive Biology

Comparative efficacy and safety between intravenous labetalol and intravenous hydralazine for hypertensive disorders in pregnancy: A systematic review and meta-analysis of 19 randomized controlled trials

Review

Author: de Macedo Lins, Cynthia Dantas ; Soares, Victor Gonçalves ; Faria, Hilária Saugo ; Ribeiro, Bianca Leal ; Simoni, Gabriel Henrique ; de Araújo Melo, Keliany C. Duarte ; da Silva Júnior, Arlindo Bispo ; de Araújo Melo, Keliany Carla Duarte ; de Abreu, Victoria Städler ; Bendaham, Lucas Cael Azevedo Ramos ; Kojima, Giovana Schlichta Adriano ; de Azevedo, Benjamim Barbosa ; Gonçalves, Ocílio Ribeiro

INTRODUCTIONHypertensive disorders during pregnancy elevate the likelihood of unfavorable outcomes for both mother and fetus. In cases of acute hypertension, several pharmacological interventions are available to lower blood pressure, such as hydralazine, a direct arteriolar vasodilator, and labetalol, a combined alpha and beta-blocker.OBJECTIVESThis systematic review and meta-analysis of randomized controlled trials (RCTs) aims to compare the efficacy and safety of intravenous labetalol and intravenous hydralazine for acute hypertensive disorders during pregnancy.METHODSWe systematically searched PubMed, Embase and Cochrane for studies comparing labetalol versus hydralazine in pregnant patients. The primary outcomes were median arterial blood pressure (MABP), diastolic blood pressure (DBP) and systolic blood pressure (SBP). We performed statistical analyses using R 4.1.1. Heterogeneity was examined with the Cochran Q test and I² statistics. Risk ratios (RR) and mean differences (MD) with 95% confidence intervals (CI), were computed with a random-effects model.RESULTSNineteen RCTs were included in this meta-analysis, comprising 2,261 patients. Among them, 1,131 (50 %) received treatment with labetalol. There was no statistically significant difference between groups in terms of SBP (MD -1.74; 95 % CI -6.72 to 3.23; p = 0.49; I² = 93 %), MABP (MD -0.72; 95 % CI -2.34 to 0.90; p = 0.39; I² = 0 %), DBP (MD 0.25; 95 % CI -4.72 to 5.21; p = 0.92; I² = 96 %), tachycardia (RR 0.42; 95 % CI 0.15 to 1.18; p = 0.099; I² = 41 %), and placenta abruption (RR 0.42; 95 % CI 0.15 to 1.16; p = 0.093; I² = 0 %). However, labetalol significantly reduced maternal hypotension (RR 0.26; 95 % CI 0.21 to 0.33; p < 0.001; I² = 41 %) compared with hydralazine.CONCLUSIONThis systematic review and meta-analysis of RCTs found that labetalol and hydralazine were efficient for hypertension disorders in pregnancy. However, labetalol reduced the incidence of maternal hypotension.

01 Dec 2024·European Journal of Obstetrics & Gynecology and Reproductive Biology: X

A rapid diagnostic technique based on metabolomics to differentiate between preeclampsia (PE) and chronic kidney disease (CKD) using maternal urine

Article

Author: Zhuang, Xu ; Hou, Jingli ; Lv, Xin ; Gao, Boyan

Similar clinical manifestations between preeclampsia and chronic kidney diseases can lead to potential misdiagnosis. Therefore, it is crucial to investigate effective diagnostic approaches that can reduce misdiagnosis and ensure the well-being of pregnant women. In this study, urine samples collected from 44 individuals with preeclampsia, 37 individuals with chronic kidney disease, and 37 healthy pregnant women were analyzed using metabolomic and proteomic strategies to distinguish between these two diseases. A total of 15 small molecules were tentatively identified as biomarkers to differentiate these two diseases, including potential internally exposed drugs and their metabolites like labetalol and SN-38, metabolites of exogenous substances like 3-phenylpropyl glucosinolate, and endogenous substances related to metabolism such as isoglobotriaose and chitobiose. Metabolic differences between preeclampsia from healthy pregnant women, as well as the differences between chronic kidney disease and healthy pregnant women were also investigated. Major mechanistic pathways were investigated based on the combination of metabolomic and proteomic, amino acid metabolisms and folate metabolism play key roles in distinguishing preeclampsia and chronic kidney disease. Two patients who were initially diagnosed with chronic kidney disease were found to have a closer association with preeclampsia following metabolomic analysis. Subsequent clinical symptoms and manifestations further supported the diagnosis of preeclampsia, and one of patient's pregnancy was ultimately terminated due to severe preeclampsia. Results of this study contribute to a better understanding of the pathogenesis and clinical diagnosis of preeclampsia, offering insights that could potentially improve future diagnostic and management approaches.

3

News (Medical) associated with Labetalol Hydrochloride

03 Sep 2024

·www.pharmaceutical-technology.com

ESC 2024: Beta blocker treatment paradigm shifts for myocardial infarction

At the ESC Congress, Dr. Milton Packer highlighted recent research into beta blocker treatment for myocardial infarction. Credit: luchschenF via Shutterstock. A shift in the beta-blocker treatment paradigm has arrived with the changing myocardial infarction treatment landscape, said a researcher at the European Society of Cardiology (ESC) Congress, held from 31 August to 2 September. Over the past 40 years, the research space has operated on an understanding that immediate inhibition by beta-blockers reduces left ventricular rupture, and further myocardial infarction , said Dr. Milton Packer, distinguished scholar in cardiovascular science at Baylor University Medical Center, Dallas. Additionally, the belief was that delayed long-term blockade can lead to left ventricular dysfunction, he said. Beta-blockers are a class of drugs that act by inhibiting the actions of hormones such as adrenaline to slow down the heart. Commonly used beta blockers include Abbott ’s Tenormin (atenolol), MSD’s Cardicor (bisoprolol), and GSK ’s Trandate (labetalol). However, Packer explained that the beta blocker response has changed as percutaneous interventions, reperfusion therapies, antiplatelet drugs and more have entered the treatment landscape for myocardial infarction. At the ongoing ESC Congress talk titled “Should we give beta blockers post-myocardial infarction?” Packer said that questions have been raised surrounding the use of the drugs in patients with myocardial infarction and preserved ejection fraction, referencing the Phase IIII REDUCE-AMI study (NCT03278509). See Also: Novavax wins FDA emergency approval for updated Covid-19 vaccine Combating Pharmaceutical Crime with On-Dose Authentication REDUCE-AMI, which was funded by the Swedish Research Council, tested the use of beta-blockers after myocardial infarction and preserved ejection fraction. The study found that for patients with acute myocardial infarction who underwent early coronary angiography and had preserved left ventricular ejection fraction, long-term beta-blocker treatment did not lower the risk of death from any cause or new myocardial infarctions compared to no beta-blocker use. Despite the conclusion of the REDUCE-AMI study, Packer highlighted the fact that researchers have only investigated and proven the effectiveness of non-selective beta blockers in post-myocardial infarction trials, so further research is required. He added that physicians will have to take into account the degree of beta-blockade in future treatment regimens.

VaccinePhase 3Drug ApprovalClinical Result

17 Jun 2024

·www.drugs.com

2008 to 2021 Saw Increase in Prevalence of Chronic HTN in Pregnancy

MONDAY, June 17, 2024 -- For pregnant individuals, the prevalence of chronic hypertension more than doubled between 2008 and 2021, according to a study published online June 17 in Hypertension . Stephanie A. Leonard, Ph.D., from the Stanford University School of Medicine in California, and colleagues analyzed commercial insurance claims from 2007 to 2021 and assessed the prevalence of chronic hypertension during pregnancy and trends in oral antihypertensive medication use. The researchers found that between 2008 and 2021, the prevalence of chronic hypertension increased steadily from 1.8 to 3.7 percent among 1,900,196 pregnancies. During the study period, antihypertensive medication use among those with chronic hypertension was relatively stable (57 to 60 percent). There was a decrease seen in the proportion of pregnant individuals with chronic hypertension treated with methyldopa or hydrochlorothiazide (from 29 to 2 percent and from 11 to 5 percent, respectively), and there was an increase seen in the proportion treated with labetalol or nifedipine (from 19 to 42 percent and from 9 to 17 percent, respectively). Following the 2017 American College of Cardiology and American Heart Association hypertension guidelines, there was no change observed in the prevalence or treatment of chronic hypertension during pregnancy. "There were large shifts in the medications used to treat chronic hypertension in pregnancy, with labetalol supplanting methyldopa as the most commonly used antihypertensive medication," the authors write. One author disclosed ties to the pharmaceutical industry.

AHAClinical Study

23 May 2024

·www.fiercepharma.com

Pfizer's Hospira recalls 5 injectable drug lots due to report of leak, potential seal issues

Recalled batches of Hospira's buprenorphine hydrochloride (HCI) injection and its labetalol hydrocholoride injection were distributed to hospitals and wholesalers nationwide between September 2023 and April 2024, according to a notice posted on the FDA website. After a report of leaking product, Pfizer’s Hospira unit is pulling five lots of sterile injectable medicines from distribution. The recall affects certain batches of the company’s buprenorphine hydrochloride (HCI) injection and its labetalol hydrocholoride injection, both of which come in Pfizer’s Carpuject syringe device. While the company has not yet received reports of “any relevant” adverse events tied to the recalled batches, it opted to pull the meds due to the potential for incomplete crimp seals. The concern followed one custumer complaint about a leaking product, Pfizer said in a notice posted by the FDA. Hospira’s buprenorphine product is indicated for intravenous or intramuscular administration to treat pain management that requires an opioid analgesic, while the labetalol HCI product controls blood pressure during severe hypertension. The recalled batches were distributed to wholesalers and hospitals across the U.S. between September 2023 and April of this year. The buprenorphine HCI lots expire in September and October of this year, while the three lots of labetalol injections carry expiration dates in 2025. Pfizer is arranging for the return of the affected products and instructed those with remaining inventory to discontinue use, stop distribution and quarantine the injections immediately. Late last year, contamination concerns led to mutiple recalls for the Pfizer subsidiary. First, the company yanked one lot of its injectable cancer med bleomycin after a customer flagged glass particulates in one vial. Then, two strengths of injectable sodium bicarbonate and one lot of atropine sulfate injection were pulled due to the “potential presence of glass particulate matter” spotted during routine product inspections. The spree continued with another market pull of one lot of vancomycin hydrochloride injection vials. That recall was attributed to a report of two visible glass particles in one vial.

Drug ApprovalClinical Result

100 Deals associated with Labetalol Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00600	Labetalol Hydrochloride	C07AG01	DB00598

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	CN	Jiangsu Desano Pharmaceutical Co. Ltd.	01 Jan 1985
Essential Hypertension	JP	Sandoz AG	07 Oct 1982

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04343235 (CTgov)	Phase 4	Hypertension, Pregnancy-Induced	13	labetalol+Furosemide (Labetalol + Furosemide)	wwgjjhfoli(mkcqupezxn) = zxpkaizxas lrwfogymat (uvdzulqbgj, wfqpilmdvi - iipjykdglm) View more	-	23 Oct 2023
				labetalol (Labetalol Only)	wwgjjhfoli(mkcqupezxn) = zmfppgcvpd lrwfogymat (uvdzulqbgj, nlzgbbsqun - hdsyylyyvw) View more
NCT04116112 (BEST-II, CTgov)	Phase 2	Thrombosis \| Stroke	120	Labetalol+Nicardipine+Hydralazine (Higher Systolic Blood Pressure (SBP) Target)	yzbsjmxocs(hunkrzejhm) = hgtxoigylu lvvpdewgcs (mtdveqylft, mndzjtgtvw - bihzcnscyu) View more	-	12 Oct 2023
				Labetalol+Nicardipine+Hydralazine (Lower SBP (<160 mmHg) Target)	yzbsjmxocs(hunkrzejhm) = ykdtytxhlk lvvpdewgcs (mtdveqylft, adrwrphtzc - qyctqtiugz) View more
NCT04539379 (ZU-IRB#: 6353-23-3-2020, Pubmed \| J Clin Monit Comput)	Not Applicable	Pre-Eclampsia	-	Magnesium sulfate	ehqtpgbpqu(ubehskxxob) = inrwlevipr hrddcxmkfw (gknueppkml )	Positive	01 Aug 2023
				Labetalol	ehqtpgbpqu(ubehskxxob) = btfxivbsmq hrddcxmkfw (gknueppkml )
NCT04688203 (Pubmed)	Phase 1/2	-	50	Magnesium sulfate	vxhxtcpgag(ahcieohzkz) = ojkafuhjbc nalnrqtixx (yfmsmwrnht )	-	19 Aug 2022
				Labetalol	vxhxtcpgag(ahcieohzkz) = ogjxthlhrw nalnrqtixx (yfmsmwrnht )
NCT03809065 (Pubmed)	Phase 4	Hypotension	40	Nitroglycerin	lyvcxnljov(qscbkelgmd) = qagaxwcqiq pmvhsfggne (oyaywmzglg )	-	17 Apr 2020
				Labetalol	lyvcxnljov(qscbkelgmd) = iubdzpbfxp pmvhsfggne (oyaywmzglg )
ISN WCN2020	Not Applicable	First line \| Add-on	56	IV Labetalol	drakwdsrif(nmzlivsatr) = onsfmeypvy zodqxbxaqc (zimvglqivf ) View more	Positive	01 Mar 2020
				IV Nitroprusside/Nitroglycerine	drakwdsrif(nmzlivsatr) = ffbpykrrnp zodqxbxaqc (zimvglqivf ) View more
NCT01114971 (CTgov)	Phase 4	Pain, Postoperative	75	Esmolol+Labetalol (Fentanyl)	slmwrjkzfc(hqxwvfmzmv) = mdpkqmgtvv uhrdtnrdwr (zmsvvbtggv, lxlfsnivau - qzgrwwhoez) View more	-	20 Feb 2020
				Esmolol+Fentanyl (Labetalol)	slmwrjkzfc(hqxwvfmzmv) = grrwtqmpyj uhrdtnrdwr (zmsvvbtggv, xbdyanorpi - hwmfonuyhl) View more
ISRCTN40973936 (Pubmed \| Curr Hypertens Rep)	Not Applicable	Hypertension, Pregnancy-Induced First line	112	Labetalol	dsrshkqevr(mpbgbvaeic) = 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 jffsovycmt (jmmbwjzbfm )	-	01 Nov 2017
				Nifedipine-modified release
NCT00765648 (CLUE, CTgov)	Phase 4	Hypertension	226	Nicardipine (Nicardipine)	okcqpsojfs(kyrxhfhmqo) = dtzfylfuth rlzipyfdkj (abslnleihk, yujqmzugbb - hjkijktfhw) View more	-	11 Dec 2014
				Labetalol (Labetalol)	okcqpsojfs(kyrxhfhmqo) = vnviwefmty rlzipyfdkj (abslnleihk, rfhcajujux - mnawmaerhu) View more
ISC2013	Not Applicable	Hypotension	212	Nicardipine	ktcjtdkcxi(bhmzbjyzzf) = ihlnjlqxpt uqxhcfuwyi (arapfdmtff )	-	01 Feb 2013
				Intermittent IV labetalol	ktcjtdkcxi(bhmzbjyzzf) = yvgooflsip uqxhcfuwyi (arapfdmtff ) View more