Last update 16 Jul 2024

Meclizine Hydrochloride

Last update 16 Jul 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)

+ [5]

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 / RecruitingPhase 2

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 1

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

320

Literatures (Medical) associated with Meclizine Hydrochloride

01 Dec 2023·Experimental brain research

Virtual reality as a countermeasure for astronaut motion sickness during simulated post-flight water landings

Article

Author: Gopinath, A ; Kravets, V ; Allred, A R ; Bonarrigo, L ; Oman, C ; Clark, T K ; Groen, E L ; Lonner, T L ; Smith, K ; DiZio, P ; Lawson, B D

Entry motion sickness (EMS) affects crewmembers upon return to Earth following extended adaptation to microgravity. Anticholinergic pharmaceuticals (e.g., Meclizine) are often taken prior to landing; however, they have operationally adverse side effects (e.g., drowsiness). There is a need to develop non-pharmaceutical countermeasures to EMS. We assessed the efficacy of a technological countermeasure providing external visual cues following splashdown, where otherwise only nauseogenic internal cabin visual references are available. Our countermeasure provided motion-congruent visual cues of an Earth-fixed scene in virtual reality, which was compared to a control condition with a head-fixed fixation point in virtual reality in a between-subject design with 15 subjects in each group. We tested the countermeasure's effectiveness at mitigating motion sickness symptoms at the end of a ground-based reentry analog: approximately 1 h of 2Gx centrifugation followed by up to 1 h of wave-like motion. Secondarily, we explored differences in vestibular-mediated balance performance between the two conditions. While Motion Sickness Questionnaire outcomes did not differ detectably between groups, we found significantly better survival rates (with dropout dictated by reporting moderate nausea consecutively over 2 min) in the visual countermeasure group than the control group (79% survival vs. 33%, t(14) = 2.50, p = 0.027). Following the reentry analogs, subjects demonstrated significantly higher sway prior to recovery (p = 0.0004), which did not differ between control and countermeasure groups. These results imply that providing motion-congruent visual cues may be an effective mean for curbing the development of moderate nausea and increasing comfort following future space missions.

01 Dec 2023·British journal of pharmacology

Regulation of the ATP‐binding cassette transporters ABCB1, ABCG2 and ABCC5 by nuclear receptors in porcine blood–brain barrier endothelial cells

Article

Author: Torres-Vergara, Pablo ; Penny, Jeffrey ; Ho, Yu Siong

Abstract:

Background and Purpose:

Blood–brain barrier (BBB) ABCB1, ABCG2 and ABCC5 transporters influence central therapeutic drug distribution. Transporter expression is regulated by the NR3C1, NR1I3 and NR1I2 nuclear receptors, but their precise roles in brain are poorly understood. We investigated the effects of selective ligand‐based activation of NR3C1, NR1I3, NR1I2 and NR2B1 in porcine brain endothelial cells (PBECs).

Experimental Approach:

Primary cultures of PBECs were exposed to NR3C1, NR1I3 and NR1I2 ligands and ABCB1, ABCG2 and ABCC5 transporter activities determined by measuring intracellular accumulation of fluorescent probes. Western blotting was used to determine the effects of receptor ligands on expression of ABCB1, ABCG2, ABCC5, NR1I2, NR1I3, NR3C1 and NR2B1. Fluorescent immunocytochemistry was employed to assess the effects of receptor ligands on the cellular localisation of NR1I2 and NR1I3.

Key Results:

The NR1I2 agonist rifampicin significantly up‐regulated ABCG2 activity, which is counteracted by co‐treatment with NR1I2 antagonist l‐sulforaphane. The NR1I3 agonist 6‐(4‐chlorophenyl)‐imidazo[2,1‐b]thiazole‐5‐carbaldehyde and inverse agonist meclizine significantly down‐regulated ABCB1, ABCG2 and ABCC5 activity. NR3C1 agonist dexamethasone significantly increased ABCB1, ABCG2 and ABCC5 activity and ABCG2 and ABCC5 protein expression, which was counteracted by co‐treatment with the NR3C1 antagonist mifepristone. This first study demonstrates that NR1I3 and NR3C1 regulate ABCC5 activity and protein expression in BBB endothelial cells.

Conclusions and Implications:

In PBECs, expression of key ATP‐binding cassette (ABC) transporters and nuclear receptors is differentially regulated by NR1I3, NR1I2, NR3C1 and NR2B1. This will help to better understand the response of the BBB to physiological and pharmacological activation of nuclear receptors.

01 Dec 2023·Renal failure

PFKFB3 downregulation aggravates Angiotensin II-induced podocyte detachment.

Article

Author: Ding, Guohua ; Zhang, Zongwei ; Luo, Zilv ; Liang, Wei ; Huang, Xiaoxiao ; Hao, Yiqun ; Feng, Jun ; Zhu, Zijing ; Hu, Jijia ; Yang, Xueyan ; Chen, Zhaowei

Podocytes play a critical role in maintaining normal glomerular filtration, and podocyte loss from the glomerular basement membrane (GBM) initiates and worsens chronic kidney disease (CKD). However, the exact mechanism underlying podocyte loss remains unclear. Fructose-2,6-biphosphatase 3 (PFKFB3) is a bifunctional enzyme that plays crucial roles in glycolysis, cell proliferation, cell survival, and cell adhesion. This study aimed to determine the role of PFKFB3 in angiotensin II (Ang II) kidney damage. We found that mice infused with Ang II developed glomerular podocyte detachment and impaired renal function accompanied by decreased PFKFB3 expression in vivo and in vitro. Inhibition of PFKFB3 with the PFKFB3 inhibitor 3PO further aggravated podocyte loss induced by Ang II. In contrast, activating PFKFB3 with the PFKFB3 agonist meclizine alleviated the podocyte loss induced by Ang II. Mechanistically, PFKFB3 knockdown likely aggravate Ang II-induced podocyte loss by suppressing talin1 phosphorylation and integrin beta1 subunit (ITGB1) activity. Conversely, PFKFB3 overexpression protected against Ang II-induced podocyte loss. These findings suggest that Ang II leads to a decrease in podocyte adhesion by suppressing PFKFB3 expression, and indicates a potential therapeutic target for podocyte injury in CKD.

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.

to view more data

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)	pvxagdhodk(ixmhqfsmke) = wjhlzqfcfa tntxzwgexp (kjggwvszvq, kcylfjeayf - wlyzqumltn) View more	-	08 May 2014
				Meclizine (25mg Meclizine)	pvxagdhodk(ixmhqfsmke) = uxyetmrbez tntxzwgexp (kjggwvszvq, ztuvqzxgdn - ylmgdgamcj) View more

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