Delving into the Latest Updates on Demeclocycline Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

6-demethyl-7-chlorotetracycline, 7-chloro-6-demethyltetracycline, DMCT

+ [16]

Target

30S subunit

Mechanism

30S subunit inhibitors(30S ribosomal subunit inhibitors), Protein biosynthesis inhibitors

Therapeutic Areas

Infectious DiseasesEndocrinology and Metabolic DiseaseEye Diseases+ [7]

Active Indication

Bacterial InfectionsHyponatremiaAcute Bronchitis+ [25]

Inactive Indication-

Originator Organization

Lederle Laboratories

Active Organization

Sun Pharma Japan Ltd.Mercury Pharmaceuticals Ltd.

Inactive Organization

Lederle LaboratoriesLederle Cyanamid Canada Inc

Drug Highest PhaseApproved

First Approval Date

US (14 Jan 1960),

Bacterial Infections

Regulation-

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Structure

Molecular FormulaC21H21ClN2O8

InChIKeyFMTDIUIBLCQGJB-SEYHBJAFSA-N

CAS Registry127-33-3

View All Structures (2)

As widely used antibiotics, tetracycline residues exist in food and environmental media, which pose certain hidden dangers and negative effects on public health. Therefore, the sensing and discrimination of tetracycline analogs (TCs) have great significance for improving food safety and preventing environmental pollution. Herein, a 7-hydroxycoumarin-3-carboxylic acid-embedded Eu-MOF (HC@Eu-MOF) material was constructed and then developed for the detection of TCs. Upon addition of TCs, the synthesized sensor displays opposite fluorescence changes at two different wavelengths due to the simultaneous presence of the inner filter effect (IFE) and the antenna effect (AE), and achieves a stable ratio signal response within 90 s. In addition, six important tetracycline analogs, including chlortetracycline (CTC), oxytetracycline (OTC), tetracycline (TC), metacycline (MC), doxycycline (DC) and demeclocycline (DMC) can be discriminated with 100 % accuracy through the principal component analysis even in extremely complicated mixtures. Further, a smartphone-assisted portable device was applied for visual sensing of TCs. The as-developed platform possessed the characteristics of simple synthesis, fast response, high sensitivity, and high stability, which further lays a further foundation for the on-site visual detection and discrimination of TCs in real samples.

01 Dec 2024·European Journal of Pharmacology

Anti-nociceptive effects of non-antibiotic derivatives of demeclocycline and doxycycline against formalin-induced pain stimulation

Article

Author: Del Bel, Elaine ; Figadere, Bruno ; Ferrié, Laurent ; Nascimento, Glauce Crivelaro ; Vivanco-Estela, Airam Nicole ; Michel, Patrick Pierre ; Raisman-Vozari, Rita

In previous studies, some tetracycline (TC) antibiotics showed potential as analgesic. We investigated here the analgesic activity of new non-antibiotic TC derivatives using the formalin-induced nociceptive pain model in adult C57BL/6 mice. Specifically, we tested the effects of i.p. injections of DDMC (5, 10, 20 mg kg^-1) and DDOX (10, 20, 40 mg kg^-1), which are non-antibiotic derivatives of demeclocycline and doxycycline, respectively. Repeated treatments with DDMC remarkably reduced nociceptive pain in both phases of the test, at 10 mg kg^-1 its efficacy was comparable to that of 10 mg kg^-1 of morphine. DDOX was also effective in this paradigm but intrinsically less potent than DDMC, exerting analgesic effects between 20 and 40 mg kg^-1. Interestingly, a single injection of DDMC (10 mg kg^-1) was sufficient to produce a robust anti-nociceptive effect similar to that of morphine. A single injection of DDOX (40 mg kg^-1) also produced anti-nociceptive effects but only in the second phase of the test. Noticeably, male mice exhibited a better analgesic response to DDMC (10 mg kg^-1) than females. A single injection of DDMC (10 mg kg^-1) and morphine but not of DDOX (40 mg kg^-1), powerfully inhibited formalin-induced spinal cord c-Fos expression whereas both TC derivatives restrained the activation of Iba-1-immunoreactive cells, indicating a potential indirect effect on inflamed microglial cells. In summary, the non-antibiotic TCs, DDMC and DDOX, demonstrated notable analgesic efficacy against formalin-induced pain, suggesting their potential as alternatives for analgesic treatment.

04 Nov 2024·Journal of Antimicrobial Chemotherapy

Clinically important interactions of macrolides and tetracyclines with dietary interventions—a systematic review with meta-analyses

Review

Author: Wiesner, Agnieszka ; Zagrodzki, Paweł ; Paśko, Paweł ; Gawalska, Alicja

AbstractBackgroundEffective management of drug–food interactions is crucial for enhancing antibiotics’ efficacy/safety. Adhering to PRISMA guidelines, we conducted a systematic review to assess the impact of dietary interventions on the bioavailability of 15 macrolides and 10 tetracyclines.MethodsWe included studies examining the influence of food, beverages, antacids, and mineral supplements on the pharmacokinetic parameters of orally administered macrolides and tetracyclines. We searched Medline (via PubMed), Embase and Cochrane Library databases up to December 2022. Risk of bias was assessed using Cochrane and NIH tools. Quantitative analyses were conducted if two or more comparable food-effect studies were available; otherwise, a qualitative summary was provided.ResultsWe included 120 studies from 97 reports. Meta-analyses were conducted for 8 macrolides and 4 tetracyclines, with qualitative synthesis for 10 and 9, respectively. About 64% of the studies were open-label, crossover designs. Our assessment found that 37% of the studies had a high risk of bias, while only 6% had low risk. Food significantly affected 10 of 13 macrolides (77%) and 6 of 7 tetracyclines (86%). High positive effects on bioavailability were seen with extended-release azithromycin and clarithromycin, and erythromycin estolate. High negative impacts were observed with erythromycin propionate and stearate, azithromycin capsules, demeclocycline and omadacycline. Antacids and mineral supplements significantly decreased tetracyclines absorption. Milk and grapefruit juice showed variable impacts on absorption.DiscussionInteractions depend on antibiotics’ physicochemical characteristics, intervention type, drug formulation and potential patient factors. The quality of evidence was rated low due to outdated studies, methodological diversity and unequal data availability.

100 Deals associated with Demeclocycline Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00290	Demeclocycline Hydrochloride	J01AA01 D06AA01	DB00618

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Acute Bronchitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Cystitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Dacryocystitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Gonorrhea	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Intrauterine infection	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Laryngitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Lung Abscess	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Lymphadenitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Lymphogranuloma Venereum	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Mastitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Osteomyelitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Otitis Media	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Pneumonia	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Pyelonephritis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Scarlet Fever	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Sinusitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Skin and skin structure infections	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Tonsillitis	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Typhus, Endemic Flea-Borne	JP	Sun Pharma Japan Ltd.	01 Nov 1965
Urethritis	JP	Sun Pharma Japan Ltd.	01 Nov 1965

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCLC2015	Not Applicable	Small Cell Lung Cancer	132	Chemotherapy alone	(yzxlltmrgd) = gnbttwgyvi wcavbkzvvr (oplttkseuj )	-	08 Sep 2015
				Chemotherapy plus Demeclocycline	(yzxlltmrgd) = axdxtfijzt wcavbkzvvr (oplttkseuj )