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Pharmaceuticals (Basel, Switzerland) Apr 2023Benzydamine is a non-steroidal anti-inflammatory drug with distinct pharmacological properties from other compounds in the same therapeutic class. The differences are... (Review)
Review
Benzydamine is a non-steroidal anti-inflammatory drug with distinct pharmacological properties from other compounds in the same therapeutic class. The differences are structural and pharmacological in nature; the anti-inflammatory mechanism is not strictly explained by the ability to interfere with the synthesis of prostaglandins. The compound is used strictly in local inflammatory diseases (inflammation in the oral and vaginal mucosa). In addition to the therapeutic indications found in the summary of product characteristics (SPC), the compound is used, in high doses, as a psychotropic substance for oral administration, having similar properties to lysergic acid diethylamide (LSD). As an over-the-counter (OTC) compound, it is easy to obtain, and the consequences of using it for purposes other than those assumed by the manufacturer raise various concerns. The reasons are related to the pharmacodynamic and pharmaco-toxicological properties, since neither the mechanism of action nor the possible side effects that would result from systemic consumption, in high doses, even occasionally, have been fully elucidated. The present review aims to analyze the pharmacodynamic properties of benzydamine, starting from the chemical structure, by comparison with structurally similar compounds registered in therapy (as an anti-inflammatory or analgesic) or used for recreational purposes.
PubMed: 37111323
DOI: 10.3390/ph16040566 -
Pharmaceuticals (Basel, Switzerland) Sep 2021Recently, a novel efflux pump gene cluster called and its variants have been identified, which undermine the antibacterial activity of tigecycline, one of the last...
Recently, a novel efflux pump gene cluster called and its variants have been identified, which undermine the antibacterial activity of tigecycline, one of the last remaining options effective against multidrug-resistant (MDR) Gram-negative bacteria. Herein, we report the potent synergistic effect of the non-steroidal anti-inflammatory drug benzydamine in combination with tigecycline at sub-inhibitory concentrations against various -positive Gram-negative pathogens. The combination of benzydamine and tigecycline killed all drug-resistant pathogens during 24 h of incubation. In addition, the evolution of tigecycline resistance was significantly suppressed in the presence of benzydamine. Studies on the mechanisms of synergism showed that benzydamine disrupted the bacterial proton motive force and the functionality of this kind of novel plasmid-encoded resistance-nodulation-division efflux pump, thereby promoting the intracellular accumulation of tigecycline. Most importantly, the combination therapy of benzydamine and tigecycline effectively improved the survival of larvae compared to tigecycline monotherapy. Our findings provide a promising drug combination therapeutic strategy for combating superbugs carrying the gene.
PubMed: 34577607
DOI: 10.3390/ph14090907 -
Canadian Journal of Anaesthesia =... Mar 2014Sore throat is a common postoperative complaint. The etiology of postoperative sore throat (POST) is considered the result of damage to airway mucosa after insertion of... (Meta-Analysis)
Meta-Analysis Review
PURPOSE
Sore throat is a common postoperative complaint. The etiology of postoperative sore throat (POST) is considered the result of damage to airway mucosa after insertion of a laryngeal mask airway device or endotracheal tube. This paper proposes benzydamine hydrochloride (BH), a topical nonsteroidal anti-inflammatory drug (NSAID) with additional analgesic and local anesthetic properties, for POST prevention.
SOURCE
We systematically searched PubMed, EMBASE™, Cochrane, and other relevant databases for randomized controlled trials (RCTs) that investigated the outcome of topical application of BH vs non-application in patients undergoing general anesthesia. Using a random effects model, meta-analyses were conducted to assess the relative risks of the incidence of POST within 24 hr following the surgical procedure. The secondary outcomes included postoperative nausea and vomiting, dry mouth, coughing, and local irritation.
PRINCIPAL FINDINGS
We reviewed five trials that included 824 patients in total. Our results indicated that the incidence of POST was significantly reduced in the BH group, with risk ratios (RRs) of 0.37 (95% confidence interval [CI]: 0.20 to 0.68) at zero to one hour, 0.39 (95% CI: 0.27 to 0.57) at one to two hours, 0.42 (95% CI: 0.22 to 0.81) at four to six hours, 0.29 (95% CI: 0.10 to 0.88) at six to 12 hr, and 0.32 (95% CI: 0.18 to 0.56) at 12 to 24 hr, compared with the control groups. Patients reported local irritation, but no major BH-related complications were observed.
CONCLUSION
Our results indicate that the incidence of POST can be significantly reduced by prophylactic BH topical application to the oral cavity or airway devices. Further RCTs are required to overcome the limitations of heterogeneity and to determine the optimal dosage and application of BH for managing POST.
Topics: Administration, Topical; Anesthesia, General; Anti-Inflammatory Agents, Non-Steroidal; Benzydamine; Humans; Intubation, Intratracheal; Laryngeal Masks; Pharyngitis; Postoperative Complications; Randomized Controlled Trials as Topic; Time Factors
PubMed: 24263969
DOI: 10.1007/s12630-013-0080-y -
Molecular Pain 2023Benzydamine is an active pharmaceutical compound used in the oral care pharmaceutical preparation as NSAID. Beside from its anti-inflammatory action, benzydamine local...
Benzydamine is an active pharmaceutical compound used in the oral care pharmaceutical preparation as NSAID. Beside from its anti-inflammatory action, benzydamine local application effectively reliefs pain showing analgesic and anaesthetic properties. Benzydamine mechanism of action has been characterized on inflammatory cell types and mediators highlighting its capacity to inhibit pro-inflammatory mediators' synthesis and release. On the other hand, the role of benzydamine as neuronal excitability modulator has not yet fully explored. Thus, we studied benzydamine's effect over primary cultured DRG nociceptors excitability and after acute and chronic inflammatory sensitization, as a model to evaluate relative nociceptive response. Benzydamine demonstrated to effectively inhibit neuronal basal excitability reducing its firing frequency and increasing rheobase and afterhyperpolarization amplitude. Its effect was time and dose-dependent. At higher doses, benzydamine induced changes in action potential wavelength, decreasing its height and slightly increasing its duration. Moreover, the compound reduced neuronal acute and chronic inflammatory sensitization. It inhibited neuronal excitability mediated either by an inflammatory cocktail, acidic pH or high external KCl. Notably, higher potency was evidenced under inflammatory sensitized conditions. This effect could be explained either by modulation of inflammatory and/or neuronal sensitizing signalling cascades or by direct modulation of proalgesic and action potential firing initiating ion channels. Apparently, the compound inhibited Na1.8 channel but had no effect over K7.2, K7.3, TRPV1 and TRPA1. In conclusion, the obtained results strengthen the analgesic and anti-inflammatory effect of benzydamine, highlighting its mode of action on local pain and inflammatory signalling.
Topics: Humans; Benzydamine; Pain; Nociceptors; Inflammation; Anti-Inflammatory Agents; Analgesics
PubMed: 37710969
DOI: 10.1177/17448069231204191 -
BMC Primary Care Jun 2022Benzydamine for oromucosal use is indicated in the relief of pain and irritation of the mouth and throat. It is an indazole derivative, non-steroidal anti-inflammatory...
Benzydamine hydrochloride for the treatment of sore throat and irritative/inflammatory conditions of the oropharynx: a cross-national survey among pharmacists and general practitioners.
BACKGROUND
Benzydamine for oromucosal use is indicated in the relief of pain and irritation of the mouth and throat. It is an indazole derivative, non-steroidal anti-inflammatory drug, with combined local anesthetic and analgesic properties, and antiseptic activity, marketed under the brand name "Tantum Verde". The aim of this study was to explore knowledge and prescriptive/advising attitudes among general practitioners (GPs) and pharmacists (PHs) with regard to the topical treatment of sore throat and other irritative/inflammatory conditions of the oropharynx, with a focus on benzydamine. These findings could be important to increase awareness on benzydamine efficacy in sore throat and stomatological conditions, and to reinforce knowledge on the characteristics of benzydamine and its mechanisms of action among healthcare professionals (pediatricians, otolaryngologists, oncologists, etc.).
MATERIALS AND METHODS
An online questionnaire survey was performed among PHs and GPs in four European countries (Italy, Germany, Russia and Poland).
RESULTS
Both GPs and PHs proved to have an excellent knowledge and mastery of the constituents effective against oral symptoms. Among all the principles, benzydamine hydrochloride is the most recognized as certainly suitable for the topical treatment of sore throat symptoms and various inflammatory/irritative conditions of the oral cavity. It is recommended by about 90% of PHs and prescribed by 80% of GPs, mainly to solve the ailments caused by sore throats and stomatitis, especially for its anti-inflammatory, analgesic and anesthetic characteristics. Also in the pediatric field, benzydamine hydrochloride is recommended: among GPs, a high percentage (about 40%) prescribes it like the remedies based on dichlorobenzyl alcohol-sodium benzoate, which are instead more often recommended by PHs (44% against 37%).
CONCLUSION
Although the public has a lot of confidence in this treatment, GPs and PHs do not recommend/prescribe benzydamine as a first-line treatment of sore throat and other irritative/inflammatory conditions of the oropharynx. To increase the knowledge of benzydamine among these healthcare professionals, it would be important to emphasize its characteristics and the different irritative/inflammatory conditions of the oropharynx in which it can be used.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Benzydamine; Child; General Practitioners; Humans; Pain; Pharmacists; Pharyngitis
PubMed: 35715725
DOI: 10.1186/s12875-022-01762-3 -
Frontiers of Medicine Apr 2023Esophageal squamous cell carcinoma (ESCC) is one of the leading causes of cancer death worldwide. It is urgent to develop new drugs to improve the prognosis of ESCC...
Esophageal squamous cell carcinoma (ESCC) is one of the leading causes of cancer death worldwide. It is urgent to develop new drugs to improve the prognosis of ESCC patients. Here, we found benzydamine, a locally acting non-steroidal anti-inflammatory drug, had potent cytotoxic effect on ESCC cells. Benzydamine could suppress ESCC proliferation in vivo and in vitro. In terms of mechanism, CDK2 was identified as a target of benzydamine by molecular docking, pull-down assay and in vitro kinase assay. Specifically, benzydamine inhibited the growth of ESCC cells by inhibiting CDK2 activity and affecting downstream phosphorylation of MCM2, c-Myc and Rb, resulting in cell cycle arrest. Our study illustrates that benzydamine inhibits the growth of ESCC cells by downregulating the CDK2 pathway.
Topics: Humans; Benzydamine; Esophageal Neoplasms; Esophageal Squamous Cell Carcinoma; Molecular Docking Simulation; Phosphorylation; Cell Proliferation; Cell Line, Tumor; Apoptosis; Cyclin-Dependent Kinase 2
PubMed: 36580233
DOI: 10.1007/s11684-022-0956-8 -
Inflammopharmacology 1998Benzydamine is a topical anti-inflammatory drug which is widely available and used topically for the treatment of the mouth. It is also used as a gel for application to...
Benzydamine is a topical anti-inflammatory drug which is widely available and used topically for the treatment of the mouth. It is also used as a gel for application to inflamed joints. It has physicochemical properties and pharmacological activities which differ markedly from those of the aspirin-line non-steroidal anti-inflammatory drugs. Benzydamine is a weak base unlike the aspirin-like drugs which are acids or metabolized to acids. A major contrast with the aspirin-like drugs is that benzydamine is a weak inhibitor of the synthesis of prostaglandins but it has several properties which may contribute to its anti-inflammatory activity. These properties include inhibition of the synthesis of the inflammatory cytokine, tumour necrosis factor-alpha (EC(50), 25 micromol/L). Inhibition of the oxidative burst of neutrophils occurs under some conditions at concentrations of 30 to 100 micromol/L, concentrations which may be produced within oral tissues after local application. A further activity of benzydamine is a general activity known as membrane stabilization which is demonstrated by several actions including inhibition of granule release from neutrophils at concentrations ranging from 3 to 30 micromol/L and stabilization of lysosomes. Lack of knowledge of the tissue concentrations of benzydamine limit the correlation between pharmacological activities in vitro and in vivo. The concentration of benzydamine in the mouthwash is 4 mmol/L but the concentrations in oral tissues have not been studied adequately. Limited data in the rat indicates that concentrations of benzydamine in oral tissues are approximately 100 micromol/L.
PubMed: 17694367
DOI: 10.1007/s10787-998-0026-0 -
Materials (Basel, Switzerland) Feb 2022This research aims to investigate the properties of nano- and micro-sized casein hydrogels crosslinked by sodium tripolyphosphate as drug delivery systems. Benzydamine...
This research aims to investigate the properties of nano- and micro-sized casein hydrogels crosslinked by sodium tripolyphosphate as drug delivery systems. Benzydamine hydrochloride was chosen as a model hydrophilic drug. The gels were synthesized by varying different parameters: casein concentration, casein/crosslinking ratio, and addition of ethanol as a co-solvent. The electrostatic attractive interactions between the casein and the sodium tripolyphosphate were confirmed by FTIR spectroscopy. The particle sizes was determined by dynamic light scattering and varied in the range between several hundred nanometers and several microns. The yield of the gelation process was high for all investigated samples and varied between 55.3% and 78.3%. The encapsulation efficiency of the particles was strongly influenced by the casein concentration and casein/crosslinker ratio and its values were between 4.6% and 22.4%. The release study confirmed that casein particles are useful as benzydamine carriers and ensured prolonged release over 72 h.
PubMed: 35207872
DOI: 10.3390/ma15041333