Delving into the Latest Updates on Labetalol Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

拉贝洛尔, AH-5158A, AH5158

+ [7]

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

Alvogen, Inc.Schering Corp.

Drug Highest PhaseApproved

First Approval Date

JP (07 Oct 1982),

Essential Hypertension

Regulation-

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Structure

Molecular FormulaC19H25ClN2O3

InChIKeyWQVZLXWQESQGIF-UHFFFAOYSA-N

CAS Registry32780-64-6

The overall objective of this double blinded, randomized controlled trial (RCT) is to compare specific outcomes of three medications (Dexmedetomidine, Nicardipine, and Labetalol) which are routinely used to lower blood pressure used during general anesthesia for orthognathic (jaw) surgery. The outcome measures for the study will be surgical field visibility, estimated blood loss, hemodynamic parameters, operation time, and adverse events.
The specific objectives of this study are to compare:
1. Dexmedetomidine, Nicardipine, and Labetalol's effect on the quality of the surgical field. (Primary Outcome)
2. Dexmedetomidine, Nicardipine, and Labetalol's effect on estimated blood loss.
3. Dexmedetomidine, Nicardipine, and Labetalol's effect on hemodynamic parameters including systolic blood pressure, mean arterial pressure, and heart rate.
4. Dexmedetomidine, Nicardipine, and Labetalol's effect on operation time.
5. Dexmedetomidine, Nicardipine, and Labetalol's effect on adverse events.
The investigators will evaluate healthy adult male and female patients who require jaw surgery at Boston Medical Center. The anticipated 90 participants will be randomized into three groups: ) A Labetalol group in which the patients receive hypotensive anesthesia with the aid of labetalol, 2) A Nicardipine group in which the patients receive hypotensive anesthesia with the aid of nicardipine, and 3) A Dexmedetomidine group in which the patients receive hypotensive anesthesia with the aid of dexmedetomidine.
The time it will take for each individual participant ranges from 1-3 months. This time includes the pre-operative visit, the surgical procedure, a 1-week post-operation visit, and then followed for 30 days post-operatively after which the patient's participation in the study will conclude.

Start Date01 Jun 2024

Sponsor / Collaborator

Boston Medical Center

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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2,265

Literatures (Medical) associated with Labetalol Hydrochloride

01 Apr 2024·Advanced science (Weinheim, Baden-Wurttemberg, Germany)

Stroke Related Brain–Heart Crosstalk: Pathophysiology, Clinical Implications, and Underlying Mechanisms

Review

Author: Cao, Jianyang ; Li, Mingxia ; 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.

01 Feb 2024·Obstetrics and gynecology

Physiologic Treatment of Severe Hypertension in Pregnancy and Postpartum

Article

Author: Tita, Alan T. ; Battarbee, Ashley N. ; Blanchard, Christina T. ; Sinkey, Rachel G. ; Davis, Allison M. ; Subramaniam, Akila

We aimed to evaluate physiologic treatment of severe hypertension. This was a retrospective cohort study of pregnant and postpartum patients with severe hypertension (systolic blood pressure [BP] 160 mm Hg or higher or diastolic BP 110 mm Hg or higher) treated with intravenous labetalol or hydralazine at a single tertiary care center between 2013 and 2018. Patients were classified as having physiologic treatment if they had hyperdynamic physiology (pulse pressure 65 mm Hg or higher) and received labetalol or had vasoconstrictive physiology (diastolic BP 100 mm Hg or higher) and received hydralazine. The primary outcome was number of antihypertensive doses to achieve nonsevere BP. Of 1,120 patients included in the analysis, 653 had physiologic treatment and 467 had nonphysiologic treatment, with 16 (1.4%) excluded for inability to classify physiology. Physiologic treatment was associated with fewer antihypertensive doses (1.4±0.9 doses vs 1.6±1.4 doses; adjusted β −0.28, 95% CI, −0.42 to −0.14) and lower odds of medication conversion (2.5% vs 4.7%; adjusted odds ratio 0.48, 95% CI, 0.24–0.93) but no difference in time to nonsevere BP (31 minutes [interquartile range 16–66 minutes] vs 34 minutes [interquartile range 15–76 minutes]; adjusted hazard ratio 1.0, 95% CI, 0.9–1.2). Physiologic treatment of severe hypertension warrants further evaluation.

01 Jan 2024·The Neurohospitalist

Evaluation of Medication Exposure on Exacerbation of Disease in Patients With Myasthenia Gravis

Article

Author: Petrucelli, Nick ; Barra, Megan E. ; Koehl, Jennifer L.

Background and Purpose:

In patients with myasthenia gravis (MG), worsening of symptoms poses a risk of respiratory failure which can be precipitated by medication use. Although purported, the risks associated with administration of certain medications are not fully elucidated. Thus, clinical decision support involving a best practice alert was executed to caution providers of drug-disease interactions when ordering a potentially harmful medication. We performed an analysis of the alert overrides with subsequent medication exposure to determine the incidence of MG exacerbations.

Methods:

This retrospective chart-review evaluated adult patients with MG at 2 large academic medical centers via electronic health records between November-2019 and November-2021 who received a medication following override of the clinical decision support tool. The primary outcome was proportion of patient encounters complicated by myasthenic exacerbations after potentially harmful medication administration. Secondary outcomes included changes in motor strength, length of stay, discharge disposition, unplanned level-of-care escalations, and changes to immunosuppressant therapy following medication administration.

Results:

A total of 70 orders were assessed in 38 patients across 55 encounters. Medications administered during these encounters included macrolides, fluoroquinolones, β-blockers, calcium channel blockers, and magnesium sulfate. Exacerbation of disease occurred in 7 patient encounters (12.7%) and occurred after intravenous magnesium or intravenous labetalol. In 5/7 events, at least 1 other risk factor associated with a myasthenic exacerbation was present.

Conclusions:

Of the medications reported to potentially worsen MG, intravenous labetalol and intravenous magnesium were the 2 agents associated with myasthenic exacerbations with a higher incidence in patients harboring additional risk factors.

2

News (Medical) associated with Labetalol Hydrochloride

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	US	Schering Corp.	01 Aug 1984
Hypertension	US	Alvogen, Inc.	01 Aug 1984
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)	immdbtvutm(rlulqrknts) = lwilxmtwqg qjskjspwaq (hsvxezgnqo, fapecgynbx - dgaduobozl) View more	-	23 Oct 2023
				labetalol (Labetalol Only)	immdbtvutm(rlulqrknts) = zedizrkpzr qjskjspwaq (hsvxezgnqo, yxefoamopl - xavgzbiiwm) View more
NCT04116112 (CTgov)	Phase 2	Thrombosis \| Stroke	120	Labetalol+Nicardipine+Hydralazine (Higher Systolic Blood Pressure (SBP) Target)	skhmhjseuq(kaxxciexth) = mjsotjjwms biyajfefsh (ooilnbicxy, rgpyrjemou - zlwemdscvu) View more	-	12 Oct 2023
				Labetalol+Nicardipine+Hydralazine (Lower SBP (<160 mmHg) Target)	skhmhjseuq(kaxxciexth) = rbuhdynvsf biyajfefsh (ooilnbicxy, zufkxgvkir - eanngylkhc) View more
NCT03506724 (CTgov)	Phase 4	Pre-Eclampsia	109	Labetalol (Intravenous Labetalol)	ljdjoizvum(unicmfrfdy) = oexwatjvdj nurztfqaqw (ovahwokdfu, okgckcidze - icroobsiid) View more	-	24 May 2021
				Nifedipine (Oral Nifedipine)	ljdjoizvum(unicmfrfdy) = fpbnpjqsfz nurztfqaqw (ovahwokdfu, epuxcmldlo - cxigtrwxll) View more
NCT01114971 (CTgov)	Phase 4	Pain, Postoperative	75	Esmolol+Labetalol (Fentanyl)	dtmchrrnnn(enimbzbpko) = twxnphqudw nbxvuchhge (ecgwbamezb, blkhccdspr - ijyuwtrwhz) View more	-	20 Feb 2020
				Esmolol+Fentanyl (Labetalol)	dtmchrrnnn(enimbzbpko) = nbremjiyev nbxvuchhge (ecgwbamezb, kqcovledxg - vrykdancxs) View more
ISRCTN40973936 (Pubmed \| Curr Hypertens Rep)	Not Applicable	Hypertension, Pregnancy-Induced First line	112	Labetalol	ztwjbhqjma(kaatzmvbbg) = 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 ltfhotmszd (vbyykzdogo )	-	01 Nov 2017
				Nifedipine-modified release
NCT00765648 (CTgov)	Phase 4	Hypertension	226	Nicardipine (Nicardipine)	nowjppmszw(ngtylthuak) = inwznpelcf djiegtcdrp (vpvaqqtcmu, kzvjeaxcsk - oijdssxqew) View more	-	11 Dec 2014
				Labetalol (Labetalol)	nowjppmszw(ngtylthuak) = gqrdjgczjp djiegtcdrp (vpvaqqtcmu, olfapgaxxr - rhdntyvotr) View more
NCT01041066 (Pubmed \| Clin Ther)	Not Applicable	Hypertension	130	Nicardipine 20 μg/kg IV	mqcsfzdlxu(olghpemctz) = xwtvbshzjf geebpvozao (novpxqeyue )	-	01 Mar 2012