Delving into the Latest Updates on Methylephedrine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

DL-Methylephrine Hydrochloride, dl -Methylephedrine Hydrochloride, dl-Methylephedrine Hydrochloride

+ [6]

Target

adrenergic receptor

Action

agonists

Mechanism

adrenergic receptor agonists(Adrenergic receptors agonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesOtorhinolaryngologic Diseases+ [2]

Active Indication

Acute BronchitisAcute upper respiratory tract inflammationAsthma+ [6]

Inactive Indication-

Originator Organization

Nipro ES Pharma KK

Active Organization

Nipro ES Pharma KK

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (28 Oct 1976),

Acute BronchitisAcute upper respiratory tract inflammationAsthma+ [4]

Regulation-

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Structure/Sequence

Molecular FormulaC11H17NO

InChIKeyFMCGSUUBYTWNDP-ONGXEEELSA-N

CAS Registry552-79-4

View All Structures (2)

A method using QuEChERS coupled with ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was developed for the determination of the residues of 19 veterinary drugs in ten animal-derived matrices, including beef, pork, sheep, horse, chicken, prawn, fish, liver, milk, and fat. This method was based on the enactment of veterinary drug compounds by Korea, Canada, the United States, and the European Union in recent years. The samples were extracted using 85% acetonitrile and separated on an ACQUITY UPLC HSS T3 column (2.1 mm × 100 mm, 1.8 μm) with a gradient elution of methanol-0.2% formic acid water as the mobile phase. The detection of the analytes was achieved through the use of positive ion electrospray ionization (ESI) and multiple reaction monitoring (MRM) modes, while the quantification was conducted via the matrix-matched external standard method. Following optimization, the linearity of the target veterinary residues in the ten matrices was observed to be satisfactory, having a range of 0.5-50.0 ng/mL (R² > 0.991). The limits of detection (LOD) were in the range of 0.01-1.29 μg/kg, while the limits of quantification (LOQ) were in the range of 0.02-4.31 μg/kg. The recoveries were observed to be in the range of 60.6-117.7 %, with relative standard deviations (RSDs) of ≤20.6 %. The method is straightforward and highly sensitive, and it satisfies the maximum limits set by the relevant standards of Korea, Canada, the USA, and the EU. It is well-suited for the rapid screening, qualitative, and quantitative analyses of metomidate, acetanilide, dl-methylephedrine, and other substances in foods of animal origin, providing technical assistance for cross-border food safety and testing.

01 Mar 2025·Journal of Pharmaceutical and Biomedical Analysis

Identification of anti-SARS-CoV-2 compounds from Qingwen Zhike prescription and exploration of their underlying mechanism by UPLC-Q-Exactive Orbitrap MS, high-throughput screening assays and transmission electron microscopy

Article

Author: Zhang, Lin ; Zhang, Cai ; Su, Zeqi ; Che, Yue ; Zhao, Ping ; Wang, Ting ; Lin, Hongmei ; Peng, Xiyi ; Zhang, Zilan ; Kang, Qianli

Qingwen Zhike prescription (QWZK), a traditional Chinese medicine (TCM) hospital prescription developed in response to the corona virus disease 2019 (COVID-19) pandemic, has demonstrated efficacy in clinical practice. Nevertheless, its specific antiviral components and mechanisms of action remain unclear. This study screened the antiviral compounds against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) from Qingwen Zhike prescription and explored the underlying mechanism through chemical composition analysis, serum and lung exposure proﬁles analysis, high-throughput screening, and transmission electron microscopy (TEM) observation. Utilizing the UPLC-Q-Exactive Orbitrap MS system, a total of 279 components were identified from Qingwen Zhike. Among these, 49 components were detected in the serum and lungs of dosed rat, with 26 components distributed abundantly in the lungs. Subsequently, a SARS-CoV-2 pseudovirus-based assay and a main protease (M^pro) enzymatic assay were used to screen for viral entry inhibitors and M^pro inhibitors. The results showed that two alkaloids (ephedrine and pseudoephedrine) and five polymethoxy-flavonoids (3,5,6,7,8,3',4'-heptamethoxyflavone, nobiletin, isosinensetin, tangeretin, and sinensetin) exhibited potent inhibitory effects on viral invasion. Further observation by TEM indicated that these two alkaloids could dissolve the viral envelope, while these five polymethoxy-flavonoids could cause leakage of virus contents, deformation of viral envelope or decomposition of the virus. Collectively, these seven compounds may serve as key antiviral components of QWZK.

01 Feb 2025·YAKUGAKU ZASSHI

Survey on Characteristics of Potentially Abused Japanese OTC Pharmaceuticals in Japan

Article

Author: Imanishi, Takashi ; Uemura, Riko

INTRODUCTIONThis study examines current OTC pharmaceuticals in Japan categorized as potential substances for abuse and discusses future initiatives for drug abuse prevention.METHODSThe Pharmaceuticals and Medical Devices Agency package inserts search function was used to identify OTC pharmaceuticals containing substances prone to abuse. Subsequently, the corresponding OTC pharmaceuticals containing the designated ingredients were investigated, analyzing their therapeutic and risk categories.RESULTSIn total, 1427 (13.9%) OTC pharmaceuticals contained the designated ingredients, with those containing methylephedrine and dihydrocodeine accounting for the majority (1245/1427, 87.2%). Among the therapeutic categories, oral cold medicines were predominant at 564, followed by antitussives and expectorants at 213, and oral rhinitis medicines at 100. Regarding risk categories, designated schedule II pharmaceuticals predominated in 9 out of 11 therapeutic category classifications.CONCLUSIONDesignated schedule II pharmaceuticals, such as oral cold medicines, antitussives and expectorants, and oral rhinitis medicines, pose a high risk of drug abuse. Addressing this challenge necessitates collaboration between pharmacists and registered sales clerks to implement preventive measures aligned with current trends in drug abuse.

100 Deals associated with Methylephedrine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Methylephedrine Hydrochloride	R01AA03	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Acute Bronchitis	Japan	Nipro ES Pharma KK	28 Oct 1976
Acute upper respiratory tract inflammation	Japan	Nipro ES Pharma KK	28 Oct 1976
Asthma	Japan	Nipro ES Pharma KK	28 Oct 1976
Bronchitis, Chronic	Japan	Nipro ES Pharma KK	28 Oct 1976
Eczema	Japan	Nipro ES Pharma KK	28 Oct 1976
Pulmonary Tuberculosis	Japan	Nipro ES Pharma KK	28 Oct 1976
Urticaria	Japan	Nipro ES Pharma KK	28 Oct 1976
Bronchiectasis	-	-	-
Nasal Obstruction	-	-	-