Benzydamine: an alternative nonsteroidal anti‐inflammatory drug in patients with nimesulide‐induced urticaria

Nettis, Eustachio; Paola, Roberto Di; Napoli, Grazia; Ferrannini, A.; Tursi, A.

doi:10.1034/j.1398-9995.2002.13325.x

Cited by 21 publications

(12 citation statements)

References 18 publications

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“…15,16 Benzydamine hydrochloride (B-HCl) is a nonsteroidal anti-inflammatory analgesic agent that acts partly through an inhibitory effect on the phospholipase A 2 by diminishing the liberation of arachidonic acid from phospholipids and partly as a weak inhibitor of prostaglandin endoperoxide H synthase (PGHS) 1 and/or 2 by reducing the production of prostaglandins. 23 The use of B-HCl as a topical anti-inflammatory agent in the mouth has long been proved. It is known that B-HCl has a transient local anesthetic effect by providing pain relief.…”

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confidence: 99%

The Effects of Three Oral Sprays on Plaque and Gingival Inflammation

Bozkurt

Öztürk

Yetkin

2005

Journal of Periodontology

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confidence: 99%

The Effects of Three Oral Sprays on Plaque and Gingival Inflammation

Bozkurt

Öztürk

Yetkin

2005

Journal of Periodontology

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“…Benzydamine is a nonsteroidal anti-inflammatory drug [9], and primarily converted into N -oxide metabolite by FMO3 in human liver. The N -oxygenation of benzydamine as a marker reaction can reflect FMO3 activity [10, 11].…”

Section: Introductionmentioning

confidence: 99%

Drug metabolite synthesis by immobilized human FMO3 and whole cell catalysts

Gao

Zheng

2019

Microb Cell Fact

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Background Sufficient reference standards of drug metabolites are required in the drug discovery and development process. However, such drug standards are often expensive or not commercially available. Chemical synthesis of drug metabolite is often difficulty due to the highly regio- and stereo-chemically demanding. The present work aims to construct stable and efficient biocatalysts for the generation of drug metabolites in vitro. Result In this work, using benzydamine as a model drug, two easy-to-perform approaches (whole cell catalysis and enzyme immobilization) were investigated for the synthesis of FMO3-generated drug metabolites. The whole cell catalysis was carried out by using cell suspensions of E. coli JM109 harboring FMO3 and E. coli BL21 harboring GDH (glucose dehydrogenase), giving 1.2 g/L benzydamine N -oxide within 9 h under the optimized conditions. While for another approach, two HisTrap HP columns respectively carrying His 6 -GDH and His 6 -FMO3 were connected in series used for the biocatalysis. In this case, 0.47 g/L benzydamine N -oxide was generated within 2.5 h under the optimized conditions. In addition, FMO3 immobilization at the C-terminal (membrane anchor region) significantly improved its enzymatic thermostability by more than 10 times. Moreover, the high efficiency of these two biocatalytic approaches was also confirmed by the N -oxidation of tamoxifen. Conclusions The results presented in this work provides new possibilities for the drug-metabolizing enzymes-mediated biocatalysis. Electronic supplementary material The online version of this article (10.1186/s12934-019-1189-7) contains supplementary material, which is available to authorized users.

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“…Benzydamine is a locally-acting nonsteroidal anti-inflammatory drug with local anaesthetic and analgesic properties by selectively binding to prostaglandin synthetase (Avvisati et al, 2018;Nettis et al, 2002). Recently, benzydamine was found to inhibit osteoclast differentiation and bone resorption by down-regulating the expression of interleukin-1β (Son et al, 2020).…”

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confidence: 99%

Reversion of antibiotic resistance in drug-resistant bacteria using non-steroidal anti-inflammatory drug benzydamine

Tong²,

Shi³

et al. 2021

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Antimicrobial resistance has been a growing concern that gradually undermines our tradition treatment regimen. The fact that few antibacterial drugs with new scaffolds or targets have been approved in the past two decades aggravates this crisis. Repurposing previously approved drugs as potent antibiotic adjuvants offers a cost effective strategy to mitigate the development of resistance and tackle the increasing infections by multidrug resistant (MDR) bacteria. Herein, we found that benzydamine, a widely used non-steroidal anti-inflammatory drug in clinic, remarkably potentiated broad spectrum antibiotic tetracyclines activity against a panel of clinical important resistant pathogens, including MRSA, VRE, MCRPEC and tet (X)-positive Gram negative bacteria. Further mechanistically experiments showed that benzydamine dissipated membrane potential (ΔΨ) in both Gram positive and negative bacteria, which in turn upregulated the transmembrane proton gradient (ΔpH) and promoted the uptake of tetracyclines. Additionally, benzydamine exacerbated the oxidative stress by triggering the production of ROS and suppressing GAD system mediated oxidative defensive. This mode of action explains the great bactericidal activity of the doxycycline benzydamine combination against different metabolic states of bacteria including persister cells. As a proof of concept, the in vivo efficacy of this combination therapy was evidenced in multiple animal infection models. These findings revealed that benzydamine is a promising tetracycline antibiotics adjuvant and has the potential to address life threatening infections by MDR bacteria.

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Benzydamine: an alternative nonsteroidal anti‐inflammatory drug in patients with nimesulide‐induced urticaria

Abstract: Benzydamine is a well tolerated drug in patients with nimesulide-induced urticaria and it may represent a valid alternative NSAID in nimesulide-sensitive patients.

Cited by 21 publications

References 18 publications

The Effects of Three Oral Sprays on Plaque and Gingival Inflammation

The Effects of Three Oral Sprays on Plaque and Gingival Inflammation

Drug metabolite synthesis by immobilized human FMO3 and whole cell catalysts

Reversion of antibiotic resistance in drug-resistant bacteria using non-steroidal anti-inflammatory drug benzydamine

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