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1.
Wiad Lek ; 76(9): 2000-2007, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37898936

RESUMO

OBJECTIVE: The aim: Different gels composed of benzydamine and flavonoids that were developed for treatment of periodontal diseases in the orthodontic patients will be compared regarding their effects on survival of mammalian cells of various tissue origin and their DNA intactness. PATIENTS AND METHODS: Materials and methods: Effect of different variants of patented gel composition «Benzidaflaziverdine¼ including a gel base and «Proteflazid®¼ containing flavonoids and benzydamine hydrochloride in powder form («T-Sept®¼) towards survival (MTT) of murine BALB-3T3 fibroblasts, J774.2 macrophages, human HaCaT keratinocytes was studied. Their effect on nativity of DNA of J774.2 macrophages was evaluated using DNA-comet assay. RESULTS: Results: Three gel compositions were used. Sample 1 was prepared on gel basis including benzydamine in liquid form and demonstrated inhibitory effect towards pseudonormal murine BALB-3T3 fibroblasts and murine J774.2 macrophages, however, normal human НаСаТ keratinocytes were resistant to its action. Sample 2 included BH in powder form and it did not affect significantly НаСаТ keratinocytes аnd BALB-3T3 fibroblasts, but it suppressed J774.2 macrophages. Sample 3 («Benzidaflaziverdine¼) was developed and patented by us as a gel composed of benzydamine in powder form and flavonoid drops «Proteflazid®¼. It did not suppress tested mammalian cells and was not genotoxic (measured as % of DNA in comet tail and Olive Tail Moment) for murine J774.2 macrophages. CONCLUSION: Conclusions: Inclusion of flavonoids in gel composition «Benzidaflaziverdine¼ blocked cytotoxic and genotoxic actions of benzydamine. Developed gel com¬position might be efficient in clinical periodontology, in particular, for treatment of periodontal diseases in orthodontic patients.


Assuntos
Benzidamina , Doenças Periodontais , Humanos , Animais , Camundongos , Pós , Géis , Doenças Periodontais/tratamento farmacológico , DNA , Mamíferos
2.
AAPS PharmSciTech ; 24(8): 214, 2023 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-37848623

RESUMO

Benzydamine hydrochloride (BZD) having analgesic, anesthetic, and anti-inflammatory effects is used orally or topically in the treatment of disorders such as joint inflammation and muscle pain. Within the scope of this study, sprayable thermosensitive BZD hydrogels were developed using thermoresponsive poloxamers to avoid systemic side effects and to provide better compliance for topical administration. Also, hydroxypropyl methyl cellulose (HPMC) was employed to improve the mechanical strength and bioadhesive properties of the hydrogel. The addition of BZD generally decreased the viscosity of the formulations (p < 0.05), while increasing the gelation temperature (p < 0.05). The formulations that did not have any clogs or leaks in the nozzle of the bottle during the spraying process were considered lead formulations. To spray the formulations easily, it was found that the viscosity at RT should be less than 200 mPa·s, and their gelation temperature should be between 26 and 34°C. Increasing HPMC and poloxamer improved bioadhesion. The amount of HPMC and poloxamers did not cause a significant change in the release characteristics of the formulations (p > 0.05); the release profiles of BZD from the formulations were similar according to model-independent kinetic (f2 > 50). HPMC and poloxamers had important roles in the accumulation of BZD in the skin. In vitro biological activity studies demonstrated that the formulations presented their anti-inflammatory activity with TNF-α inhibition but did not have any effect on the inhibition of COX enzymes as expected. As a result, thermosensitive hydrogels containing BZD might be an appropriate alternative, providing an advantage in terms of easier application compared to conventional gels.


Assuntos
Benzidamina , Hidrogéis , Poloxâmero , Géis , Temperatura , Anti-Inflamatórios/farmacologia , Derivados da Hipromelose , Viscosidade
3.
Mol Pain ; 19: 17448069231204191, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37710969

RESUMO

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 Nav1.8 channel but had no effect over Kv7.2, Kv7.3, 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.


Assuntos
Benzidamina , Humanos , Benzidamina/metabolismo , Benzidamina/farmacologia , Benzidamina/uso terapêutico , Dor/tratamento farmacológico , Dor/metabolismo , Nociceptores/metabolismo , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Anti-Inflamatórios/uso terapêutico , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Analgésicos/metabolismo
4.
Support Care Cancer ; 31(10): 557, 2023 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-37668773

RESUMO

PURPOSE: It is important to determine the approaches for oral mucositis (OM) care in pediatric oncology clinics to reflect the profile of practices. The aim of this study was to report on current nursing care approaches for OM in Türkiye. METHODS: The descriptive, cross-sectional study was conducted with nurse managers in pediatric oncology centers in Türkiye between April and December 2022. The data were obtained online by reaching pediatric oncology nurse managers. The data was collected with the "Oral Mucositis Care Application Form" developed by the researchers based on current literature. RESULTS: The study reached approximately 60% (n = 41) of pediatric oncology clinics across Türkiye. Oral assessment of children was mainly conducted by nurses (95.1%), and 53.7% of clinics used the WHO Oral Mucositis Assessment Scale. To prevent OM, oral care routines were performed twice a day (36.6%) using sodium bicarbonate (61%) and 0.9% sodium chloride (26.8%) agents. For oral mucositis management, pharmacological agents included glutamine (oral) (51.2%), chlorhexidine (43.9%), and benzydamine hydrochloride (36.6%), while non-pharmacological agents included black mulberry syrup (41.5%), honey (19.8%), and chewing gum (9.8%). Chlorhexidine and benzydamine hydrochloride were used for all mucositis grades, while glutamine was frequently used for grades 2 and above. CONCLUSIONS: The study revealed that the practices related to preventing and managing oral mucositis in pediatric oncology clinics in Türkiye are heterogeneous. These findings will contribute to the existing literature on the multidisciplinary, systematic, and evidence-based approaches used in oral mucositis care in Türkiye.


Assuntos
Benzidamina , Mucosite , Neoplasias , Estomatite , Criança , Humanos , Estudos Transversais , Clorexidina , Glutamina , Estomatite/tratamento farmacológico , Estomatite/etiologia , Neoplasias/complicações
5.
J Cancer Res Clin Oncol ; 149(10): 7427-7439, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36947237

RESUMO

BACKGROUND: Radiation-induced oral mucositis (OM) largely impairs the quality of life (QoL) of patients with head and neck cancer (HNC). Few choices with limited efficacy are available to prevent this adverse effect. This randomized trial was conducted to compare the efficacy of benzydamine (standard) and a new combination (sumac and rose water) in preventing radiation-induced OM. METHODS: This was a phase II, triple-blind, active-controlled, randomized trial. The primary endpoint was OM, and the secondary endpoints were oral pain and QoL. Besides, the possible variables defining the outcomes were analyzed using the chi-squared test (univariate analysis) and binomial regression model (multivariate analysis). RESULTS: Sumac-rose group had fewer high-grade OM (33% vs. 63%, odds ratio [OR] 0.28, 95% confidence interval [CI 95%] 0.08-0.93, P = 0.03) and better QoL (P < 0.05). Multivariate analysis confirmed these findings. Sumac-rose rinsing could also postpone the start of oral pain (hazard ratio [HR] 0.02, CI 95% 0.001-0.32, P = 0.001) and high-grade OM (HR 0.28, P = 0.03) compared with benzydamine. CONCLUSIONS: The sumac-rose group had a lower OM rate and grade and higher QoL than the benzydamine group. In addition, the experimental group developed high-grade OM and oral pain later during the radiotherapy course. Further studies need to be conducted to assess the role of sumac and rose water in reducing grade 3-4 mucositis in patients who undergo chemoradiation for head and neck cancer.


Assuntos
Benzidamina , Neoplasias de Cabeça e Pescoço , Lesões por Radiação , Rhus , Estomatite , Humanos , Benzidamina/uso terapêutico , Antissépticos Bucais/uso terapêutico , Qualidade de Vida , Estomatite/etiologia , Estomatite/prevenção & controle , Neoplasias de Cabeça e Pescoço/radioterapia , Dor , Água , Método Duplo-Cego
6.
Medicine (Baltimore) ; 102(13): e33367, 2023 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-37000110

RESUMO

BACKGROUND: Acute sore throat (ST) can occur as part of a common cold of viral origin or caused by pharyngeal bacterial pathogens. The majority of patients with acute ST complain of pain on swallowing and dry scratchiness which can have a negative impact on the quality of life (QoL). This study aimed to evaluate the time to pain relief in patients with acute ST, following a single administration of benzydamine hydrochloride (HCl) 0.3% oromucosal spray or benzydamine HCl 3 mg lozenges. METHODS: This multicenter, randomized, active-controlled, open label, parallel-group, international phase IV study was conducted at 12 investigational centers in Poland, Hungary, and Russian Federation. The study population consisted of 363 adult patients with recent onset (≤3 days) of ST and a diagnosis of tonsillopharyngitis. The primary endpoint was to assess the efficacy of benzydamine HCl in ST pain relief at 2 minutes after a single-dose administration. Secondary endpoints included, among others, the assessment of a first perceived ST relief at 1 minute after a single-dose administration of benzydamine HCl spray or lozenge. RESULTS: Both the spray and lozenges are effective in providing a ST relief starting already at 2 minutes after a single administration, with an effect lasting up to up to 4 hours. Clinical efficacy after 7 days of treatment and a good safety profile were also demonstrated. CONCLUSION: Anesthetic and analgesic properties of benzydamine spray and lozenges effectively addressed the patient priority of a rapid relief of symptoms of upper respiratory tract infections (URTI).


Assuntos
Benzidamina , Resfriado Comum , Faringite , Adulto , Humanos , Benzidamina/uso terapêutico , Qualidade de Vida , Resfriado Comum/tratamento farmacológico , Faringite/etiologia , Comprimidos , Dor/tratamento farmacológico , Método Duplo-Cego
7.
Eur J Hosp Pharm ; 30(4): 202-207, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34285108

RESUMO

OBJECTIVE: The primary endpoint of the present study was to assess the potential therapeutic effects of three different mouthwashes for alleviation and treatment of oral complications (OCs). The secondary endpoint was to assess patients' perceptions and daily functional activities after therapy of OCs in patients with colon cancer receiving 5-fluorouracil (5-FU)-based chemotherapy regimens. METHODS: A prospective, randomised controlled study carried out on 90 patients with colon cancer eligible for 5-FU-based chemotherapy regimens at the oncology centre, Istanbul, Turkey. Patients were randomly randomised into three groups (30 patients in each group) and received a single mouthwash. The first group (group A) received benzydamine at a dose of 15 mL; the second group (group B) received sodium bicarbonate at a dose of 1.2-2.4 g in 240 mL of water; and the third group (group C) received glutamine suspension 10 g. Patients were assessed for the occurrence of oral complications based on the WHO scale for oral mucosa evaluation and National Cancer Institute Common Terminology Criteria for Adverse Events version 4.0. Oral pain was assessed using a visual analogue scale alongside assessment of patients' perceptions and daily functional activities based on the Rotterdam Symptom Checklist. RESULTS: A total of 119 oral complications were reported, including mouth dryness (n=56, 47.1%), oral mucositis (n=31, 26.1%) and oral pain (n=32, 26.8%). At the end of the study, patients of group A and group B significantly suffered from mouth dryness (p=0.0001), oral mucositis (p=0.029) and oral pain (p=0.039) compared with patients in group C. Although there was no significant change, group C patients showed a slight improvement in psychological discomfort, activity levels and quality of life at the end of the study. CONCLUSION: The present study showed that benzydamine and sodium bicarbonate mouthwashes were significantly less effective for the alleviation and treatment of oral complications compared with glutamine among patients with colon cancer receiving 5-FU-based chemotherapy regimens.


Assuntos
Benzidamina , Neoplasias do Colo , Estomatite , Xerostomia , Humanos , Fluoruracila , Antissépticos Bucais/efeitos adversos , Benzidamina/uso terapêutico , Bicarbonato de Sódio/uso terapêutico , Estudos Prospectivos , Qualidade de Vida , Glutamina/uso terapêutico , Estomatite/induzido quimicamente , Estomatite/tratamento farmacológico , Estomatite/epidemiologia , Neoplasias do Colo/tratamento farmacológico , Neoplasias do Colo/induzido quimicamente , Neoplasias do Colo/complicações , Dor/tratamento farmacológico , Xerostomia/induzido quimicamente , Xerostomia/complicações , Xerostomia/tratamento farmacológico
8.
Cancer Nurs ; 46(1): 36-44, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36066336

RESUMO

BACKGROUND: Oral mucositis is the most severe and debilitating adverse effect of cancer treatment, resulting in inadequate nutritional intake, treatment disruptions, and dose alteration, leading to increased hospital costs and decreased tumor control. OBJECTIVE: The aim of this study was to determine the effectiveness of turmeric mouthwash on oral health status and onset and severity of treatment-induced oral mucositis and associated oral dysfunctions among head and neck cancer patients. METHODS: A randomized controlled design was adopted (CTRI/2018/06/014367). Turmeric mouthwash was administered to the experimental group (n = 46) and benzydamine mouthwash was given to the control group (n = 46). Oral health status and mucositis were graded using the Oral Health Assessment Tool and the World Health Organization oral toxicity criteria, respectively. Oral dysfunctions were measured by a patient-reported oral mucositis symptom scale and xerostomia short-form inventory. All outcome variables were measured weekly during the entire course of radiation therapy. RESULTS: Both groups were comparable with regard to their demographic and outcome variables ( P > .05). The incidence of intolerable mucositis in the control group was 100% compared with 17.8% in the experimental group. Repeated-measures analysis of variance demonstrated significant differences in the onset and severity of oral mucositis ( P = .001), oral health status ( P = .001), and oral dysfunctions ( P = .001) between the experimental and control groups. CONCLUSION: Turmeric mouthwash was effective in reducing the severity of oral mucositis and associated oral dysfunctions as compared with benzydamine mouthwash. IMPLICATIONS: Use of turmeric, a nontoxic and cost-effective intervention, can be an alternative to the traditional management of oral mucositis.


Assuntos
Benzidamina , Neoplasias de Cabeça e Pescoço , Mucosite , Lesões por Radiação , Estomatite , Humanos , Benzidamina/uso terapêutico , Curcuma , Neoplasias de Cabeça e Pescoço/complicações , Neoplasias de Cabeça e Pescoço/tratamento farmacológico , Antissépticos Bucais/farmacologia , Antissépticos Bucais/uso terapêutico , Mucosite/complicações , Mucosite/tratamento farmacológico , Saúde Bucal , Lesões por Radiação/etiologia , Estomatite/induzido quimicamente , Estomatite/tratamento farmacológico
9.
Front Med ; 17(2): 290-303, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36580233

RESUMO

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.


Assuntos
Benzidamina , Neoplasias Esofágicas , Carcinoma de Células Escamosas do Esôfago , Humanos , Neoplasias Esofágicas/tratamento farmacológico , Carcinoma de Células Escamosas do Esôfago/tratamento farmacológico , Simulação de Acoplamento Molecular , Fosforilação , Proliferação de Células , Linhagem Celular Tumoral , Apoptose , Quinase 2 Dependente de Ciclina
10.
Support Care Cancer ; 30(12): 10255-10262, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36355214

RESUMO

INTRODUCTION: Among the evidence-based agents outlined in the Multinational Association of Supportive Care in Cancer/International Society of Oral Oncology (MASCC/ISOO) mucositis guidelines, benzydamine and morphine are advised for the management of oral mucositis (OM) in certain cancer patients. This study is aimed to collect information from a group of highly experienced healthcare professionals in the field of oral mucositis about their clinical experience with these agents. METHODS: A survey questionnaire about the clinical experience with topical benzydamine and morphine to manage oral mucositis and their related adverse effects (AEs) was electronically distributed to the members of the Mucositis Study Group of MASCC/ISOO. RESULTS: Eighty-eight entries were recorded (response rate 25%), and 54 entries submitted complete questionnaires about the drug-related AE (completion rate 65%) and were used for the data analysis. Of the respondents, 44% and 27.7% prescribed benzydamine and morphine to manage their patients' oral mucositis, respectively. Lack of availability in the respondent's country was the common reason for not prescribing benzydamine and morphine (18.9% and 5.4%, respectively); however, a large portion of the respondents indicated that 'another reason' stopped them from prescribing these agents (51.3% and 73%, respectively). AEs to benzydamine or morphine were observed by 25.9% and 12.9% of respondents, respectively, with mild numbness and tingling as the most common drug-related AE for both agents. CONCLUSION: The use of topical benzydamine and morphine for the management of OM varies between countries. While relatively common, the AEs related to these agents are mild. Mitigating the barriers for prescribing them may increase their use.


Assuntos
Benzidamina , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Mucosite , Neoplasias , Estomatite , Humanos , Benzidamina/efeitos adversos , Morfina/efeitos adversos , Estomatite/induzido quimicamente , Estomatite/tratamento farmacológico
11.
BMC Prim Care ; 23(1): 296, 2022 11 23.
Artigo em Inglês | MEDLINE | ID: mdl-36419002

RESUMO

BACKGROUND: Benzydamine hydrochloride is a locally-acting Non-Steroidal Anti-Inflammatory Drug (NSAID) with combined local anesthetic and analgesic properties, indicated for the symptomatic relief of pain in acute sore throat. The aim of this study was to obtain an European Consensus among pharmacists, general practitioners and pediatricians on the appropriate use of benzydamine hydrochloride in the treatment of sore throat. METHODS: The authors developed a Delphi questionnaire organized into 15 statements focused on 4 topics: the mechanism of action of benzydamine, the benzydamine treatment in an adult patient and in a pediatric patient, and the advantages of benzydamine over other topical treatments. The survey was administered to a panel of to 320 participants including general practitioners, pediatricians, and pharmacists from 6 European countries (Italy, Germany, Portugal, Romania, Russia, and Spain), who rated their level of agreement or disagreement with each statement on a 6-point Likert scale. Consensus was predefined as more than 66% of the panel agreeing/disagreeing with each statement. RESULTS: Panelists' agreement on statements was very high. Consensus was reached for all 15 statements in the Delphi survey, with more than 98% positive agreement on topic 4, suggesting a shared view among European healthcare professionals (HCPs) about the advantages of benzydamine over other topical treatments. A strong consensus (> 99%) was reached for all the statements of topic 1 regarding the mechanism of action of benzydamine, except for its anesthetic properties (79%). Strong agreement was reached for all statements in topics 2 and 3 regarding the treatment of acute sore throat symptoms in the adult and pediatric patient, except for one on the efficacy of benzydamine in preventing post-operative sore throat, for which it was 67%. CONCLUSION: Because all relevant publications on benzydamine are dated and there are no recommendations on its use for the symptomatic treatment of sore throat in European guidelines, this Delphi-based international consensus may be important in reinforcing the appropriate use and effect of benzydamine in the treatment of sore throat among health care professionals.


Assuntos
Benzidamina , Clínicos Gerais , Faringite , Adulto , Humanos , Criança , Consenso , Faringite/tratamento farmacológico , Dor
12.
Vestn Otorinolaringol ; 87(5): 99-103, 2022.
Artigo em Russo | MEDLINE | ID: mdl-36404699

RESUMO

THE AIM: Share with healthcare practitioners personal experience of using benzydamine spray (Oralsept) in pediatric practice; present a clinical case, which, according to the author, can help doctors optimize approaches to the treatment of patients with acute respiratory viral infections (including COVID-19), thereby improving the quality of life of pediatric patients.


Assuntos
Benzidamina , COVID-19 , Infecções Respiratórias , Viroses , Humanos , Criança , Benzidamina/uso terapêutico , Qualidade de Vida , Infecções Respiratórias/tratamento farmacológico
13.
Ann Palliat Med ; 11(9): 2980-3000, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36096743

RESUMO

BACKGROUND: To study and review the effectiveness of oral care interventions for palliative patients for amelioration of clinical conditions affecting oral cavity. METHODS: Following PRISMA standard, a systematic evaluation of articles published between 2000 and 2021 was undertaken utilising five databases on interventions studies. This comprehensive review consists of randomised controlled trials (RCTs) and specific types of non-randomised studies (NRS) examining oral care interventions for palliative patients. Three independent authors screened search records, identified related studies, extracted data and evaluated risk of bias. The key findings of each study were summarised according to the research questions and data that generated during the data extraction procedure. RESULTS: Out of the 67 identified studies, seven were included in this review (five RCTs and two NRSs) involving head-and-neck cancer, oral cancer, oral mucositis, xerostomia and individuals with malignant disease. Interventions studied were: Ziziphus honey, artificial saliva, CAM2028-Benzydamine, morphine mouthwash, ketamine mouthwash, bethanechol tablets and caphosol with regular oral-care. The durations of interventions in the included studies were largely short-term (six weeks or less). Overall, six studies revealed good results in support of the intervention, with magnitudes of effect ranging from 13.2-10,110.0%. However, just four researches found significant changes, with magnitudes of effect ranging from 50.0-10,110.0%. Although two of the trials have not revealed significant changes in the results, investigations have indicated a reduction in oral conditions in the group with interventions. Only one trial has not indicated an improvement in oral conditions in the groups which received the interventions. DISCUSSION: By assessing the efficacy of available oral hygiene interventions for palliative patients, this systematic review can help palliative team finds the viable strategies to apply in controlling oral problems among hospice patients. Even though only four of the seven research found a statistically significant difference, most studies found great effectiveness in favour of intervention.


Assuntos
Benzidamina , Neoplasias de Cabeça e Pescoço , Ketamina , Betanecol , Neoplasias de Cabeça e Pescoço/terapia , Humanos , Derivados da Morfina , Antissépticos Bucais/uso terapêutico , Cuidados Paliativos , Saliva Artificial
14.
Drug Metab Pharmacokinet ; 46: 100465, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35853340

RESUMO

The number of single-nucleotide substitutions of human flavin-containing monooxygenase 3 (FMO3) recorded in mega-databases is increasing. Moreover, phenotype-gene analyses have revealed impaired FMO3 variants associated with the metabolic disorder trimethylaminuria. In this study, four novel amino-acid substituted FMO3 variants, namely p.(Gly191Asp), p.(Glu414Gln), p.(Phe510Ser), and p.(Val530CysfsTer1), were identified in the whole-genome sequences in the Japanese population reference panel (8.3K JPN) of the Tohoku Medical Megabank Organization. Additionally, four variants, namely p.(Ile369Thr), p.(Phe463Val), p.(Arg500Gln), and p.(Ala526Thr) FMO3, were found in the 8.3K JPN database but were already recorded in the National Center for Biotechnology Information database. Novel FMO3 variants p.[(Met1Leu)] and p.[(Trp231Ter)] were also identified in phenotype-gene analyses of 290 unrelated subjects with self-reported malodor. Among the eight recombinant FMO3 variants tested (except for p.[(Met1Leu)] and p.[(Trp231Ter)]), Arg500Gln and Gly191Asp FMO3, respectively, had lower and much lower capacities for trimethylamine and/or benzydamine N-oxygenation activities than wild-type FMO3. Because another FMO3 mutation p.[(Gly191Cys)] with diminished recombinant protein activity was previously detected in two independent probands, Gly191 would appear to be important for FMO3 catalytic function. Analysis of whole-genome sequence data and trimethylaminuria phenotypes revealed missense FMO3 variants that severely impaired FMO3-mediated N-oxygenations in Japanese subjects that could be susceptible to low drug clearances.


Assuntos
Benzidamina , Humanos , Japão , Proteínas Recombinantes , Nucleotídeos
15.
Dent Mater J ; 41(4): 545-551, 2022 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-35676045

RESUMO

The aim of the present study was to evaluate IL-1ß, IL-6 and TNF-α expression levels of macrophage cells induced by benzydamine hydrochloride (BNZ), BNZ with chitosan, calcium hydroxide (CH) and chlorhexidine (CHX) medicaments. Half maximal inhibitory concentrations (IC50) were assessed on THP-1, Saos-2, and CRL-2014 cells using MTT assay. THP-1 cells were differentiated into macrophages with phorbol12-myristate13-acetate and activated with lipopolysaccharide. IL-1ß, IL-6 and TNF-α levels in supernatants were determined using enzyme-linked immunosorbent assay (ELISA). The data were examined with one-way ANOVA and Tukey's multiple comparison test (p=0.05). At the selected concentrations, the cell viability was higher than 50% for chitosan and CH, whereas CHX presented lower IC50 values than BNZ and BNZ+chitosan. According to ELISA results, the lowest IL-1ß, IL-6 and TNF-α values were observed with BNZ+Chitosan 50 µg/mL and BNZ 50 µg/mL. BNZ+chitosan 50 µg/mL combination has revealed promising anti-inflammatory effects. Nevertheless, these findings need to be examined in clinical conditions.


Assuntos
Benzidamina , Quitosana , Benzidamina/farmacologia , Hidróxido de Cálcio/farmacologia , Quitosana/farmacologia , Clorexidina/farmacologia , Ensaio de Imunoadsorção Enzimática , Interleucina-6 , Macrófagos , Fator de Necrose Tumoral alfa/farmacologia
16.
BMC Prim Care ; 23(1): 154, 2022 06 17.
Artigo em Inglês | MEDLINE | ID: mdl-35715725

RESUMO

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.


Assuntos
Benzidamina , Clínicos Gerais , Faringite , Anti-Inflamatórios não Esteroides , Benzidamina/uso terapêutico , Criança , Humanos , Dor/complicações , Farmacêuticos , Faringite/tratamento farmacológico
17.
Carbohydr Polym ; 288: 119368, 2022 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-35450630

RESUMO

The objective of this research was to develop a novel mucoadhesive polymer for drug delivery applications based on N-(2-aminoethyl) maleimide-functionalized carboxymethyl cellulose in which the weight ratios of the materials were tuned to explore the condition providing the highest maleimide content on the polymer. The polymers were synthesized from N-(2-aminoethyl) maleimide that was conjugated to carboxymethyl cellulose with their mucoadhesive properties examined by tensile testing, rheology, and flow-through analysis and their biocompatibilities evaluated on the human gingival fibroblast cell line (HGF-1). The anti-inflammatory drug benzydamine was loaded into mucoadhesive-polymer-based tablets and used to demonstrate the application of the synthesized polymer. The polymer exhibited superior mucoadhesive capability compared to carboxymethyl cellulose through the interaction between maleimide moiety and mucin. The functionalized polymer also possessed the ability to control the release of benzydamine with Higuchi's release model and was proven to be a potential candidate in mucoadhesive drug delivery.


Assuntos
Benzidamina , Polímeros , Carboximetilcelulose Sódica , Sistemas de Liberação de Medicamentos , Humanos , Maleimidas
18.
Clin Oral Investig ; 26(4): 3613-3625, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35066687

RESUMO

OBJECTIVES: To assess the effects of benzydamine and mouthwashes (MoWs) containing benzydamine on different stages of Candida albicans biofilm: adhesion, formation, persistence, and regrowth (if perturbed). MATERIALS AND METHODS: C. albicans CA1398, carrying the bioluminescence ACT1p-gLUC59 fusion product, was employed. Fungal cells were exposed for 1', 5', or 15' to 4 different benzydamine concentrations (0.075 to 0.6%) to 2 mouthwashes (MoWs) containing benzydamine and to a placebo MoW (without benzydamine). Treated cells were tested for adhesion (90 min) and biofilm formation (24-h assay). Next, 24- and 48-h-old biofilms were exposed to benzydamine and MoWs to assess regrowth and persistence, respectively. The effects of benzydamine, MoWs containing benzydamine, and placebo on different biofilm stages were quantified by bioluminescence assay and by the production of quorum sensing (QS) molecules. RESULTS: Benzydamine and MoWs containing benzydamine impaired C. albicans ability to adhere and form biofilm, counteracted C. albicans persistence and regrowth, and impaired a 48-h-old biofilm. Some of these effects paralleled with alterations in QS molecule secretion. CONCLUSIONS: Our results show for the first time that benzydamine and MoWs containing benzydamine impair C. albicans capacity to form biofilm and counteract biofilm persistence and regrowth. CLINICAL RELEVANCE: Benzydamine and MoWs containing benzydamine capacity to affect C. albicans biofilm provides an interesting tool to prevent and treat oral candidiasis. Likely, restraining C. albicans colonization through daily oral hygiene may counteract colonization and persistence by other critical oral pathogens, such as Streptococcus mutans, whose increased virulence has been linked to the presence of C. albicans biofilm.


Assuntos
Benzidamina , Candida albicans , Benzidamina/farmacologia , Biofilmes , Antissépticos Bucais/farmacologia , Streptococcus mutans
19.
Commun Biol ; 4(1): 1328, 2021 11 25.
Artigo em Inglês | MEDLINE | ID: mdl-34824393

RESUMO

Antimicrobial resistance has been a growing concern that gradually undermines our tradition treatment regimens. The fact that few antibacterial drugs with new scaffolds or targets have been approved in the past two decades aggravates this crisis. Repurposing 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 clinically important pathogens, including MRSA, VRE, MCRPEC and tet(X)-positive Gram-negative bacteria. Mechanistic studies showed that benzydamine dissipated membrane potential (▵Ψ) in both Gram-positive and Gram-negative bacteria, which in turn upregulated the transmembrane proton gradient (▵pH) 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 involve persister cells. As a proof-of-concept, the in vivo efficacy of this drug combination was evidenced in multiple animal infection models. These findings indicate that benzydamine is a potential tetracyclines adjuvant to address life-threatening infections by MDR bacteria.


Assuntos
Adjuvantes Farmacêuticos/farmacologia , Antibacterianos/farmacologia , Benzidamina/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana
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