Delving into the Latest Updates on Mefenamic Acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Mefemarnic Acid, Mefenamic, Mefenamic acid (JP17/USP/INN)

+ [15]

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

InflammationTumescencePrimary dysmenorrhea+ [1]

Inactive Indication-

Originator Organization

Shionogi & Co., Ltd.

Active Organization

Ginwa Enterprise (Group) Inc. Xi'An Jinhua Pharmaceutical Factory

Shanxi Xingbang Pharmaceutical Co. Ltd.

Avion Pharmaceuticals LLC

+ [2]

Inactive Organization

Plethora Solutions Ltd.

Drug Highest PhaseApproved

First Approval Date

(01 Jan 1962),

Pain

Regulation-

Login to view timeline

Structure

Molecular FormulaC15H15NO2

InChIKeyHYYBABOKPJLUIN-UHFFFAOYSA-N

CAS Registry61-68-7

PURPOSEPan-retinal photocoagulation (PRP) is the mainstay of treatment for proliferative diabetic retinopathy (PDR), reducing the risk of severe vision loss. Pain poses a potential obstacle to effective laser delivery and patient compliance. Therefore, implementing pain relief strategies can enhance both treatment efficacy and patient comfort.DESIGNA systematic review and meta-analysis.METHODSWe conducted a systematic review and meta-analysis according to PRISMA guidelines. The PubMed, Embase and Cochrane Central Register of Controlled Trials databases were searched for randomized controlled trials (RCTs) that enrolled patients undergoing PRP due to DR and compared analgesics or non-steroidal anti-inflammatory drugs (NSAID) to placebo. Pain was evaluated with the visual analogue scale. The version 2 of the Cochrane Collaboration's Risk of Bias in Randomized Controlled Trials tool and its version for crossover trials were used to assess the risk of bias. The Grading of Recommendations, Assessment, Development, and Evaluation tool was used to measure the certainty of evidence.RESULTSA total of 13 studies were included, comprising 1404 eyes from RCTs, nine of which were crossover. Patients who were administered analgesia reported a significantly lower pain sensitivity compared to those who received placebo (Standardized mean difference [SMD] -0.38; 95% confidence interval [CI] -0.58, -0.17; P < .01; I² = 69%). Subgroup analysis of systemic administration of analgesics/NSAIDs (metamizole, Entonox, acetaminophen, ibuprofen, caffeine, mefenamic acid, intramuscular ketorolac tromethamine, and potassium diclofenac) also showed a statistically significant reduction in pain when compared to placebo (SMD -0.28; 95% CI -0.50, -0.07; P < .01; I² = 43%). Exclusive eye drops administration (ketorolac tromethamine 0.5% and sodium diclofenac 0.1%) also showed a significant difference in pain sensitivity (SMD -0.46; 95% CI -0.88, -0.05; I² = 83%), however with a more significant heterogeneity.CONCLUSIONSThe results of this meta-analysis including over 1000 patients demonstrated that the use of analgesics significantly reduced pain sensitivity during PRP, and systemic analgesia is potentially better than topical administration when compared to placebo.

02 Oct 2024·Therapeutic Delivery

Synthesis and release studies on amylose-based ester prodrugs of fenamic acid NSAIDs

Article

Author: Chugh, Shraddha ; Sharma, Mousmee ; Prasher, Parteek ; Chandrasen, Garima ; Mudila, Harish

Aim: To achieve colon-targeted release of mefenamic acid from its ester-linked amylose prodrugs.Materials & methods: The prodrug was characterized by 1H NMR and IR spectroscopy. Drug activation and release profile was studied in enzyme enriched simulated physiological media via UV-vis spectroscopy and was validated with HPLC analysis. ELISA assay was employed for evaluating the % inhibition of COX-1 and COX-2 inhibition at different concentrations of the prodrug preincubated with ester and/ or amylose hydrolyzing enzymes. SEM studies further validated the performance of the prodrug under simulated physiological conditions.Results: Pancreatin was essential for the prodrug activation in SIM to make the ester bonds in prodrug vulnerable to hydrolysis by esterase. This evidence was confirmed by drug release studies, HPLC analysis, ELISA assay and SEM investigation where the ester conjugated prodrug showed marked stability in physiological media only to get activated in the presence of amylose degrading enzyme.Conclusion: Ester linked amylose-mefenamic acid conjugate showed both enzyme responsive activation and release in SIM.

01 Oct 2024·Phytochemistry

The Nicotiana tabacum UGT89A2 enzyme catalyzes the glycosylation of di- and trihydroxylated benzoic acid derivatives

Article

Author: Lara-González, Samuel ; Rivera-Chávez, José ; Duque-Ortiz, Arianna ; Pastor-Palacios, Guillermo

Glycosyltransferases catalyze the transfer of a glycoside group to a wide range of acceptor compounds to produce glycoconjugates with diverse biological and pharmacological activities. The present work reports the identification and biochemical characterization of Nicotiana tabacum UGT89A2 glycosyltransferase (NtUGT89A2). The enzyme is a monomer in solution that catalyzes the O-β-glucosylation of di- and tri-hydroxylated and chlorinated derivatives of benzoic acid. NtUGT89A2 has a preference for 2,5-dihydroxybenzoic acid (2,5-DHBA) over 2,3-dihydroxybenzoic acid (2,3-DHBA) and 2,4-dihydroxybenzoic acid (2,4-DHBA). Other substrates that can be used by NtUGT89A2 include 3,4,5-trihydroxybenzoic acid and chlorinated derivatives such as 2-chloro-5-hydroxybenzoic acid (2-Cl-5-HBA). The substrates of NtUGT89A2 were identified by thermal stability experiments, where we observed a maximum increase of the thermal denaturation midpoint (T_m) of 10 °C in the presence of 2,5-DHBA and UDP-glucose. On the other hand, the highest specific activity was obtained with 2,5-DHBA (225 ± 1.7 nkat/mg). Further characterization revealed that the enzyme has a micromolar affinity for its substrates. Notably, the enzyme retains full activity after incubation at 70 °C for 1 h. These results provide a basis for future functional and structural studies of NtUGT89A2.

100 Deals associated with Mefenamic Acid

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00151	Mefenamic Acid	M01AG01	DB00784

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Inflammation	JP	Pfizer Japan, Inc.	29 Jun 1968
Tumescence	JP	Pfizer Japan, Inc.	29 Jun 1968
Primary dysmenorrhea	US	Avion Pharmaceuticals LLC	28 Mar 1967
Pain	-	Shionogi & Co., Ltd.	01 Jan 1962