Last update 26 Nov 2024

Meclizine Hydrochloride

Last update 26 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummaryMeclizine is a small molecule drug that acts as an antagonist of histamine (H1) receptors. It is marketed under the trade names Antivert, Bonine, and Navicalm and is approved for the treatment of motion sickness, nausea, and vomiting. It's a white or slightly yellowish, crystalline powder that was first approved by Casper Pharma on February 14, 1957, in the United States. As an H1 receptor antagonist, meclizine is thought to work by reducing the activity of histamine in the brain, which can help to alleviate the symptoms of motion sickness and other conditions. There is always available in tablet form and is typically taken by mouth. It is important to follow the dosing instructions provided by a healthcare provider and to be aware of any potential side effects or drug interactions that may occur.

Drug Type

Small molecule drug

Synonyms

Meclizine, Meclizine dihydrochloride monohydrate, Meclizine hydrochloride (JAN/USP)

+ [6]

Target

Histamine receptor

Mechanism

Histamine receptor antagonists

Therapeutic Areas

Nervous System DiseasesOtorhinolaryngologic DiseasesOther Diseases

Active Indication

VertigoMotion SicknessNausea+ [1]

Inactive Indication-

Originator Organization

Casper Pharma LLC

Active Organization

Casper Pharma LLC

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (14 Feb 1957),

Motion SicknessNauseaVomiting

Regulation-

Structure

Molecular FormulaC25H31Cl3N2O

InChIKeyKDLHYOMCWBWLMM-UHFFFAOYSA-N

CAS Registry31884-77-2

Clinical Trials associated with Meclizine Hydrochloride

JPRN-jRCT2041230001 / Not yet recruitingPhase 2IIT

An exploratory clinical trial to Investigate the efficacy and safety of Meclizine hydrochloride in Achondroplasia patients (pediatrics). - MACH trial

Start Date15 May 2023

Sponsor / Collaborator-

NCT05852730 / RecruitingPhase 2

Optimizing the Combination of Intranasal Scopolamine and Sensory Augmentation to Mitigate G-transition Induced Motion Sickness and Enhance Sensorimotor Performance. Motion Sickness Countermeasures Field Test

The primary specific aim of this Field Test aim is to evaluate the feasibility and efficacy of administering the intranasal scopolamine gel in operational field settings using both astronaut and ground-control subjects that are exposed to provocative motion as part of their assigned duties. For the ground-control subjects, these may include motion simulations (e.g., centrifuge), parabolic flights and/or Orion capsule recovery operations. Astronaut participants may choose to test Inscop during provocative preflight training exercises (e.g., centrifugation), and can choose to take the medication prophylactically to prevent symptoms or after symptom onset to treat motion sickness during the launch and/or landing mission phases. Both ground-control and astronaut participants will be required to test the medication during a training session to monitor for adverse side effects. Participants in the field test aim will complete short debrief questionnaires to capture motion sickness symptoms, side effects, and feasibility comments. The investigators will also include field "control" subjects who did not take (INSCOP) to comment on what countermeasures subjects used and their effectiveness. The investigators will be recruiting astronaut participants from free-flier missions (e.g., SpaceX Polaris Dawn), Private Astronaut Missions (e.g., Axiom), and standard missions to the International Space Station.

Start Date10 Aug 2021

Sponsor / Collaborator

Repurposed Therapeutics, Inc.

[+1]

JPRN-jRCT2041200114 / CompletedPhase 1IIT

A Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Meclizine Hydrochloride Administered for 2 Weeks in Achondroplasia patients (pediatrics).

Start Date14 Apr 2021

Sponsor / Collaborator-

100 Clinical Results associated with Meclizine Hydrochloride

100 Translational Medicine associated with Meclizine Hydrochloride

100 Patents (Medical) associated with Meclizine Hydrochloride

319

Literatures (Medical) associated with Meclizine Hydrochloride

01 Oct 2024·Revue neurologique

Importance of glucose and its metabolism in neurodegenerative disorder, as well as the combination of multiple therapeutic strategies targeting α-synuclein and neuroprotection in the treatment of Parkinson's disease

Review

Author: Kale, P P ; Siddique, A H H

According to recent findings, Phosphoglycerate Kinase 1 (pgk-1) enzyme is linked to Parkinson's disease (PD). Mutations in the PGK-1 gene lead to decreases in the pgk-1 enzyme which causes an imbalance in the levels of energy demand and supply. An increase in glycolytic adenosine triphosphate (ATP) production would help alleviate energy deficiency and sustain the acute energetic need of neurons. Neurodegeneration is caused by an imbalance or reduction in ATP levels. Recent data suggest that medications that increase glycolysis and neuroprotection can be used to treat PD. The current study focuses on treatment options for disorders associated with the pgk-1 enzyme, GLP-1, and A_2A receptor which can be utilized to treat PD. A combination of metformin and terazosin, exenatide and meclizine, istradefylline and salbutamol treatments may benefit parkinsonism. The review also looked at potential target-specific new techniques that might assist in satisfying unfulfilled requirements in the treatment of PD.

01 Jul 2024·American journal of obstetrics and gynecology

Meclizine improves endometrial repair and reduces simulated menstrual bleeding in mice with induced adenomyosis

Article

Author: Liu, Xishi ; Mao, Chenyu ; Guo, Sun-Wei

BACKGROUND:

Adenomyosis is one of the structural causes of abnormal uterine bleeding, which often presents as heavy menstrual bleeding. Mostly because of the poor understanding of its pathophysiology, medical management of adenomyosis-induced heavy menstrual bleeding is still a challenge. We have previously reported that glycolysis is crucial to endometrial repair following menstruation and that suppressed glycolysis can cause heavy menstrual bleeding.

OBJECTIVE:

This study aimed to test the hypothesis that meclizine, a drug with an excellent safety profile, alleviates heavy menstrual bleeding in mice with induced adenomyosis using a simulated menstruation model.

STUDY DESIGN:

Adenomyosis was induced in 36 female C57BL/6 mice using endometrial-myometrial interface disruption. Three months after induction, the mice were randomly divided into the following 3 groups: low-dose meclizine, high-dose meclizine, and controls. Treatment with meclizine or vehicle started shortly before the simulated menstruation procedure and ended before progesterone withdrawal. The amount of blood loss was quantified and uterine tissue was harvested for histologic evaluation of the grade of endometrial repair. We performed immunohistochemistry analysis of 4 proteins critically involved in glycolysis: Glut1 (glucose transporter 1), Hk2 (hexokinase 2), Pfkfb3 (6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3), and Pkm2 (pyruvate kinase M2). The extent of tissue fibrosis in both ectopic and eutopic endometria was evaluated using Masson trichrome staining.

RESULTS:

In mice with induced adenomyosis, meclizine accelerated endometrial repair in a dose-dependent manner and reduced the amount of menstrual bleeding. Meclizine administration raised endometrial immunoexpression of Hk2 and Pfkfb3 but not of Glut1 or Pkm2. The extent of endometrial fibrosis was reduced following the meclizine administration. Remarkably, these favorable changes were accompanied by the suppression of lesional progression, as evidenced by the dose-dependent reduction in the extent of fibrosis (a surrogate for lesional progression).

CONCLUSION:

These encouraging results, taken together, suggest that glycolysis may be a promising therapeutic target and that meclizine may hold therapeutic potential as a nonhormonal treatment for adenomyosis-induced heavy menstrual bleeding without exacerbating the disease.

01 Jul 2024·STROKE

ATF5-Mediated Mitochondrial Unfolded Protein Response (UPR ^mt ) Protects Neurons Against Oxygen-Glucose Deprivation and Cerebral Ischemia

Article

Author: Guo, Shuzhen ; Ji, Xunming ; Durán Laforet, Violeta ; An, Hong ; Park, Ji-Hyun ; Liu, Ning ; Wu, Di ; Lo, Eng H ; Yu, Zhanyang ; Hayakawa, Kazuhide ; Shi, Jingfei ; Zhou, Bing ; Nakamura, Yoshihiko ; Mandeville, Emiri T ; Li, Wenlu

BACKGROUND::

The mitochondrial unfolded protein response (UPR mt ) is an evolutionarily conserved mitochondrial response that is critical for maintaining mitochondrial and energetic homeostasis under cellular stress after tissue injury and disease. Here, we ask whether UPR mt may be a potential therapeutic target for ischemic stroke.

METHODS::

We performed the middle cerebral artery occlusion and oxygen-glucose deprivation models to mimic ischemic stroke in vivo and in vitro, respectively. Oligomycin and meclizine were used to trigger the UPR mt . We used 2,3,5-triphenyltetrazolium chloride staining, behavioral tests, and Nissl staining to evaluate cerebral injury in vivo. The Cell Counting Kit-8 assay and the Calcein AM Assay Kit were conducted to test cerebral injury in vitro.

RESULTS::

Inducing UPR mt with oligomycin protected neuronal cultures against oxygen-glucose deprivation. UPR mt could also be triggered with meclizine, and this Food and Drug Administration-approved drug also protected neurons against oxygen-glucose deprivation. Blocking UPR mt with siRNA against activating transcription factor 5 eliminated the neuroprotective effects of meclizine. In a mouse model of focal cerebral ischemia, pretreatment with meclizine was able to induce UPR mt in vivo, which reduced infarction and improved neurological outcomes.

CONCLUSIONS::

These findings suggest that the UPR mt is important in maintaining the survival of neurons facing ischemic/hypoxic stress. The UPR mt mechanism may provide a new therapeutic avenue for ischemic stroke.

News (Medical) associated with Meclizine Hydrochloride

04 Apr 2023

·www.prnewswire.com

WellSpring Consumer Healthcare Acquires Iconic OTC Skin Care Brands from Bayer

Addition of A+D® and Solarcaine® bolsters scale, product diversity, and opportunities to accelerate WellSpring's innovation pipeline NEW YORK and SARASOTA, Fla., April 4, 2023 /PRNewswire/ -- WellSpring Consumer Healthcare, a developer and marketer of leading over-the-counter and personal care brands, today announced the acquisition of a portfolio of well-recognized and trusted over-the-counter (OTC) skin care brands from Bayer AG. Financial terms of the transaction were not disclosed. WellSpring Consumer Healthcare is a portfolio company of Avista Capital Partners, a leading middle-market healthcare private equity firm with expertise in building OTC platforms. The brands include A+D®, a leading diaper rash and skin protectant brand, Solarcaine®, the leading sunburn relief brand, and Cortate® and Complex 15®, two Canadian therapeutic skincare brands. A+D® is a widely recognized brand that has been endorsed by pediatricians and trusted by consumers for over 80+ years. Solarcaine® is a pharmacist-recommended medicated burn relief brand that has been relied upon by consumers for generations. Chris Brown, CEO of WellSpring Consumer Healthcare, said: "We are thrilled with the additions of A+D® and Solarcaine®. These trusted, iconic brands align with our core mission to improve the health and wellness of our consumers and will reinforce our position as a leader in important needs-based segments, such as therapeutic skincare. WellSpring's growth model continues to deliver strong results with our focus on new product innovation, distribution expansion, and strategic acquisitions. A+D® and Solarcaine® offer unique opportunities to accelerate our robust product pipeline." Alex Yu, Partner at Avista Capital Partners, said: "This is a highly strategic acquisition for WellSpring, which not only adds established OTC brands to the WellSpring portfolio, but also provides attractive scale, future growth opportunities, and expands our presence in one of WellSpring's core product categories. We are excited for WellSpring to continue building upon the strong heritage of these brands through innovative and high-quality new product development." The acquisition of A+D® and Solarcaine ® represents WellSpring's first add-on acquisition since Avista's investment in WellSpring in August 2022. WellSpring is currently evaluating additional opportunities to further its strong growth trajectory. ABOUT WELLSPRING CONSUMER HEALTHCARE Founded in 1999 in Sarasota, Florida, WellSpring develops and markets a diversified portfolio of trusted OTC brands in the U.S. and Canada, with several that enjoy leading positions in important needs-based product segments such as therapeutic skincare and digestive health. The WellSpring portfolio now includes well-known therapeutic skincare brands such as A+D® (diaper rash and skin protectant), Bactine® (germ-focused skincare) and Solarcaine® (medicated sunburn relief), and category-leaders in digestive health such as Bonine® (motion sickness) and Emetrol® (anti-nausea). WellSpring is an established consumer healthcare platform with a sophisticated omni-channel distribution network that includes leading brick and mortar and e-commerce retailers, a robust new product innovation infrastructure, and a strong growth trajectory. Learn more at . ABOUT AVISTA CAPITAL PARTNERS Founded in 2005, Avista Capital is a leading New York-based private equity firm with over $8 billion invested in more than 40 growth-oriented healthcare businesses globally. Avista partners with businesses that feature strong management teams, stable cash flows and robust growth prospects – investing in the medical devices and technologies, pharmaceuticals, outsourced pharmaceutical services, healthcare technology, healthcare distribution, and consumer healthcare sectors. Avista helps its portfolio companies to accelerate growth through strategic acquisitions, having completed over 100 add-on acquisitions historically across its healthcare portfolio. Avista's Operating Executives and Advisors are an integral part of the team, providing strategic insight, operational oversight and senior counsel, which helps drive growth and performance, while fostering sustainable businesses and creating long-term value for all stakeholders. For more information, visit . Media contacts: Daniel Yunger and Hallie Wolff Kekst CNC 212.521.4800 [email protected] / [email protected] SOURCE Avista Capital Partners

Acquisition

100 Deals associated with Meclizine Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D01317	Meclizine Hydrochloride	R06AE05	DB00737

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Vertigo	US	Casper Pharma LLC	13 Apr 2018
Motion Sickness	US	Casper Pharma LLC	14 Feb 1957
Nausea	US	Casper Pharma LLC	14 Feb 1957
Vomiting	US	Casper Pharma LLC	14 Feb 1957

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01443858 (CTgov)	Phase 2	Smoking Cessation	146	Nicotine+placebo+meclizine (Control)	wespxyyoer(uihnphbfop) = zuikzmgeft sqfslialwk (faeuwgawsm, wkpzssukkv - gpjksyfkan) View more	-	08 May 2014
				Meclizine (25mg Meclizine)	wespxyyoer(uihnphbfop) = xurtzvpfmk sqfslialwk (faeuwgawsm, kdjpeofyuu - qwbdrbcpun) View more

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