A benzyl-indazole having analgesic, antipyretic, and anti-inflammatory effects. It is used to reduce post-surgical and post-traumatic pain and edema and to promote healing. It is also used topically in treatment of RHEUMATIC DISEASES and INFLAMMATION of the mouth and throat.
Oxidases that specifically introduce DIOXYGEN-derived oxygen atoms into a variety of organic molecules.

Antifungal activity of local anesthetics against Candida species. (1/17)

OBJECTIVE: To evaluate the activity of benzydamine, lidocaine, and bupivacaine, three drugs with local anesthetic activity, against Candida albicans and non-albicans strains and to clarify their mechanism of activity. METHODS: The minimal inhibitory concentration (MIC) was determined for 20 Candida strains (18 clinical isolates and two American Type Culture Collection strains). The fungistatic activity was studied with the fluorescent probe FUN-1 and observation under epifluorescence microscopy and flow cytometry. The fungicidal activity of the three drugs was assayed by viability counts. Membrane alterations induced in the yeast cells were evaluated by staining with propidium iodide, by quantitation of intracellular K+ leakage and by transmission electron microscopy of intact yeast cells and prepared spheroplasts. RESULTS: The MIC ranged from 12.5-50.0 microg/mL, 5.0-40.0 mg/mL, and 2.5-10.0 mg/mL for benzydamine, lidocaine, and bupivacaine, respectively. The inhibitory activity of these concentrations could be detected with the fluorescent probe FUN-1 after incubation for 60 minutes. A very fast fungicidal activity was shown by 0.2, 50, and 30 mg/mL of benzydamine, lidocaine, and bupivacaine, respectively. CONCLUSIONS: At lower concentrations, the tested drugs have a fungistatic activity, due to yeast metabolic impairment, while at higher concentrations they are fungicidal, due to direct damage to the cytoplasmic membrane.  (+info)

In vitro evaluation of potential in vivo probes for human flavin-containing monooxygenase (FMO): metabolism of benzydamine and caffeine by FMO and P450 isoforms. (2/17)

AIMS To determine the FMO and P450 isoform selectivity for metabolism of benzydamine and caffeine, two potential in vivo probes for human FMO. METHODS Metabolic incubations were conducted at physiological pH using substrate concentrations of 0.01-10 mM with either recombinant human FMOs, P450s or human liver microsomes serving as the enzyme source. Products of caffeine and benzydamine metabolism were analysed by reversed-phase h.p.l.c. with u.v. and fluorescence detection. RESULTS CYP1A2, but none of the human FMOs, catalysed metabolism of caffeine. In contrast, benzydamine was a substrate for human FMO1, FMO3, FMO4 and FMO5. Apparent Km values for benzydamine N-oxygenation were 60 +/- 8 microM, 80 +/- 8 microM, > 3 mM and > 2 mM, for FMO1, FMO3, FMO4 and FMO5, respectively. The corresponding Vmax values were 46 +/- 2 min-1, 36 +/- 2 min-1, < 75 min-1 and < 1 min-1. Small quantities of benzydamine N-oxide were also formed by CYPs 1A1, 1A2, 2C19, 2D6 and 3A4. CONCLUSIONS: FMO1 and FMO3 catalyse benzydamine N-oxygenation with the highest efficiency. However, it is likely that the metabolic capacity of hepatic FMO3 is a much greater contributor to plasma levels of the N-oxide metabolite in vivo than is extrahepatic FMO1. Therefore, benzydamine, but not caffeine, is a potential in vivo probe for human FMO3.  (+info)

Benzydamine N-oxidation as an index reaction reflecting FMO activity in human liver microsomes and impact of FMO3 polymorphisms on enzyme activity. (3/17)

AIMS: The role of flavin containing monooxygenases (FMO) on the disposition of many drugs has been insufficiently explored. In vitro and in vivo tests are required to study FMO activity in humans. Benzydamine (BZD) N-oxidation was evaluated as an index reaction for FMO as was the impact of genetic polymorphisms of FMO3 on activity. METHODS: BZD was incubated with human liver microsomes (HLM) and recombinant enzymes. Human liver samples were genotyped using PCR-RFLP. RESULTS: BZD N-oxide formation rates in HLM followed Michaelis-Menten kinetics (mean Km = 64.0 microM, mean Vmax = 6.9 nmol mg-1 protein min-1; n = 35). N-benzylimidazole, a nonspecific CYP inhibitor, and various CYP isoform selective inhibitors did not affect BZD N-oxidation. In contrast, formation of BZD N-oxide was almost abolished by heat treatment of microsomes in the absence of NADPH and strongly inhibited by methimazole, a competitive FMO inhibitor. Recombinant FMO3 and FMO1 (which is not expressed in human liver), but not FMO5, showed BZD N-oxidase activity. Respective Km values for FMO3 and FMO1 were 40.4 microM and 23.6 microM, and respective Vmax values for FMO3 and FMO1 were 29.1 and 40.8 nmol mg-1 protein min-1. Human liver samples (n = 35) were analysed for six known FMO3 polymorphisms. The variants I66M, P135L and E305X were not detected. Samples homozygous for the K158 variant showed significantly reduced Vmax values (median 2.7 nmol mg-1 protein min-1) compared to the carriers of at least one wild type allele (median 6.2 nmol mg-1 protein min-1) (P < 0.05, Mann-Whitney-U-test). The V257M and E308G substitutions had no effect on enzyme activity. CONCLUSIONS: BZD N-oxidation in human liver is mainly catalysed by FMO3 and enzyme activity is affected by FMO3 genotype. BZD may be used as a model substrate for human liver FMO3 activity in vitro and may be further developed as an in vivo probe reflecting FMO3 activity.  (+info)

Flavin-containing monooxygenase activity in hepatocytes and microsomes: in vitro characterization and in vivo scaling of benzydamine clearance. (4/17)

Liver microsomes, and more recently cryopreserved hepatocytes, are commonly used in the in vitro characterization of the metabolism of new xenobiotics. The flavin-containing monooxygenases (FMO) are a major non p450 oxidase present in liver microsomes and hepatocytes. Since FMO is known to be thermally labile, and this enzyme may be involved in the metabolic clearance of some drugs, we sought to more completely characterize the metabolic competency of this enzyme in cryopreserved hepatocytes and in liver microsomes preincubated under various conditions using benzydamine as an in vitro and in vivo probe. The metabolism of benzydamine to its major metabolite, the N-oxide, is mediated by FMO3 in humans. We found that the in vitro microsomal t(1/2) was 70% longer when incubations were prewarmed at 37 degrees C in the absence of NADPH compared with prewarming in the presence of an NADPH-regenerating system, and N-oxide formation was inhibited >99%. Interestingly, the in vivo clearance predicted from these incubations and from human hepatocytes overpredicted the observed clearance of benzydamine in humans (>10.5 versus 2.4 ml/min/kg). In contrast, rat hepatocytes successfully predicted rat in vivo benzydamine clearance to within approximately 30% (>68 versus 48 ml/min/kg). Benzydamine N-oxidation in liver microsomes from all common preclinical species demonstrated heat sensitivity. This information should be considered when extrapolating metabolism data of xenobiotics from these in vitro systems.  (+info)

Benzydamine inhibits monocyte migration and MAPK activation induced by chemotactic agonists. (5/17)

1. The present study was aimed to investigate the effect of benzydamine, an anti-inflammatory drug devoid of activity on arachidonic acid metabolism, on monocyte chemotaxis and to define the possible biochemical correlates of activity. 2. Benzydamine inhibited monocyte chemotaxis in response to three classes of chemoattractants: the prototypic CC-chemokine CCL2 (MCP-1), the microbial product fMLP and the complement cascade component C5a. The effect was dose-dependent with IC50's of 100, 50 and 45 microm for MCP-1/CCL2, fMLP and C5a, respectively. At the dose of 100 microm, the effect resulted in a 50+/-10% inhibition of MCP-1/CCL2-induced chemotaxis and 53+/-6 and 54+/-5% inhibitions of chemotaxis in response of fMLP and C5a, respectively (n=3). 3. Receptor expression as well as calcium fluxes in response to chemoattractants were not affected by benzydamine. 4. Benzydamine strongly inhibited chemoattractant-induced activation of the mitogen-activated protein kinase (MAPK) ERK1/2, and of its upstream activator kinase MEK1/2. ERK1/12 activation in response to chemoattractants was 89-98% inhibited by a 100 microm concentration of benzydamine with an IC50 of 30 microm. 5. Under the same experimental conditions, pretreatment with 100 microm benzydamine caused a 75-89% inhibition of p38 activation (IC50 25 microm). 6. These results indicate that the anti-inflammatory activity of benzydamine is exerted at multiple levels, including monocyte migration to chemotactic factors associated to a blockage of ERK and p38 MAPK pathways.  (+info)

Effect of genetic variants of the human flavin-containing monooxygenase 3 on N- and S-oxygenation activities. (6/17)

The decreased capacity of the flavin-containing monooxygenase 3 (FMO3) to oxygenate xenobiotics including trimethylamine is believed to contribute to metabolic disorders. The aim of this study was to functionally characterize FMO3 variants recently found in a Japanese population and compare them with selective functional activity of other FMO3 variants. Recombinant Glu158Lys and Glu158Lys-Glu308Gly FMO3 expressed in Escherichia coli membranes showed slightly decreased N-oxygenation of benzydamine and trimethylamine. Selective functional S-oxygenation of these variants by methyl p-tolyl sulfide or sulindac sulfide was comparable to that of wild-type FMO3. The Glu158Lys-Thr201Lys-Glu308Gly and Val257Met-Met260Val variants showed significantly decreased oxygenation of typical FMO3 substrates (i.e., approximately one-tenth of the V(max)/K(m) values). Val257Met FMO3 had a lower catalytic efficiency for methyl p-tolyl sulfide and sulindac sulfide S-oxygenation. However, compared with wild-type FMO3, Val257Met FMO3 showed a similar catalytic efficiency for N-oxygenation of benzydamine and trimethylamine. The catalytic efficiency for benzydamine and trimethylamine N-oxygenation by Arg205Cys FMO3 was only moderately decreased, but it possessed decreased sulindac sulfide S-oxygenation activity. Kinetic analysis showed that Arg205Cys FMO3 was inhibited by sulindac in a substrate-dependent manner, presumably because of selective interaction between the variant enzyme and the substrate. The results suggest that the effects of genetic variation of human FMO3 could operate at the functional level for N- and S-oxygenation for typical FMO3 substrates. Genetic polymorphism in the human FMO3 gene might lead to unexpected changes of catalytic efficiency for N- and S-oxygenation of xenobiotics and endogenous materials.  (+info)

Inter-individual variation in flavin-containing monooxygenase 3 in livers from Japanese: correlation with hepatic transcription factors. (7/17)

Human flavin-containing monooxygenase 3 (FMO3)-mediated microsomal oxygenation activity, levels of FMO3 protein and FMO3 mRNA and modifications were investigated in Japanese livers genotyped for the FMO3 gene. Significant correlations were observed for benzydamine N-oxygenation or methyl p-tolyl sulfide S-oxygenation activity (in the range of approximately 20- to approximately 40-fold) and FMO3 levels determined immunochemically in liver microsomes (r(2)=0.73-0.75, p<0.0001, n=16). Preincubation with the reducing agent ascorbate revealed that FMO3 activity in some liver samples is suppressed. Microsomal FMO3 protein content (approximately 40-fold) was correlated with FMO3 mRNA levels (r(2)=0.55, p=0.0010, n=16), but FMO3 haplotypes did not affect FMO3 mRNA expression (approximately 100-fold) under the conditions used. FMO3 mRNA levels were multivariately correlated with trans-acting factors, i.e. hepatic nuclear factor 4 (HNF-4) mRNA and nuclear factor Y box-binding protein (NF-Y) mRNA (r(2)=0.31, p=0.0017, n=37). These results suggest that considerable individual differences in FMO3 levels may exist in Japanese livers. The liver-enriched transcription factor HNF-4 appears to be a determinant of FMO3 expression in livers, as well as the ubiquitous factor NF-Y.  (+info)

Recreational use of benzydamine as a hallucinogen among street youth in Brazil. (8/17)

 (+info)

"Benzydamine oral rinse". Medicinenet. "Difflam spray (benzydamine)". Net Doctor, UK. 8 March 2020. "Tantum Verde (benzydamine ... There are no contraindications to the use of benzydamine except for known hypersensitivity. Benzydamine is well tolerated. ... Fanaki NH, El-Nakeeb MA (March 1996). "Antibacterial activity of benzydamine and antibiotic-benzydamine combinations against ... Benzydamine (also known as Tantum Verde and branded in some countries as Maxtra Gargle, Difflam and Septabene), available as ...
Use of chloroacetamide in the alkylation step, followed by acid hydrolysis produces bendazac (instead of benzydamine). ... Benzydamine Balfour JA, Clissold SP (April 1990). "Bendazac lysine. A review of its pharmacological properties and therapeutic ...
Benztropine Benzydamine Chlorpheniramine Singh A. Herbalism, Phytochemistry and Ethnopharmacology. Science Publishers. p. 45. ...
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QM01AH95 Enflicoxib M01AX01 Nabumetone M01AX02 Niflumic acid M01AX04 Azapropazone M01AX05 Glucosamine M01AX07 Benzydamine ...
Amantadine Amphetamine Amylone Atropine Benztropine Benzydamine Benzylpiperazine Bromocriptine Bupropion Butorphanol Cathinone ...
... benzydamine (deliriant and stimulant, used medically as a non-steroidal anti-inflammatory drug) butorphanol (agonist-antagonist ...
... benzydamine MeSH D03.438.449.350 - granisetron MeSH D03.438.473.025 - adrenochrome MeSH D03.438.473.050 - alcian blue MeSH ... benzydamine MeSH D03.383.129.539.487.350 - granisetron MeSH D03.383.129.539.550 - muzolimine MeSH D03.383.129.539.650 - ...
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ADB 5F-AMB 5F-APINACA AB-CHFUPYCA AB-CHMINACA AB-PINACA ADB-CHMINACA ADB-FUBINACA ADBICA AMB-FUBINACA APICA APINACA Benzydamine ...
Benzocaine R02AD02 Lidocaine R02AD03 Cocaine R02AD04 Dyclonine R02AX01 Flurbiprofen R02AX02 Ibuprofen R02AX03 Benzydamine "ATC ...
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In painful oral conditions such as aphthous stomatitis, analgesic mouthrinses (e.g. benzydamine mouthwash, or "Difflam") are ...
M02AA01 Phenylbutazone M02AA02 Mofebutazone M02AA03 Clofezone M02AA04 Oxyphenbutazone M02AA05 Benzydamine M02AA06 Etofenamate ...
Benzydamine (INN) Benzyl Benzoate Benzylpenicillin (INN) Benzylsulfamide (INN) Bepadin Bepafant (INN) Beperidium iodide (INN) ...
Cabergoline G02CB04 Quinagolide G02CB05 Metergoline G02CB06 Terguride G02CC01 Ibuprofen G02CC02 Naproxen G02CC03 Benzydamine ...
The molecular formula C19H23N3O (molar mass: 309.40 g/mol, exact mass: 309.1841 u) may refer to: A-412,997 Benzydamine This set ...
Benzydamine metabolism in vivo is impaired in patients with deficiency of flavin-containing monooxygenase 3 Ertan Mayatepek 1 ... Benzydamine N-oxygenation as a measure of flavin-containing monooxygenase activity. Yeung CK, Rettie AE. Yeung CK, et al. ... Benzydamine metabolism in vivo is impaired in patients with deficiency of flavin-containing monooxygenase 3 Ertan Mayatepek et ... Benzydamine N-oxidation as an index reaction reflecting FMO activity in human liver microsomes and impact of FMO3 polymorphisms ...
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3. [Effect of benzydamine on release of prostaglandin E2 and prostacyclin from rabbit gastric mucosa cells].. Hell M; Bauer AC ... Antithrombotic action of benzydamine].. Jansen JW. Arzneimittelforschung; 1987 May; 37(5A):626-8. PubMed ID: 3619983. [TBL] ... 2. [The effect of benzydamine on prostaglandin synthesis in macrophages].. Goppelt-Strübe M; Röbbecke K; Golombek M; Resch K. ... New pharmacologic and biochemical findings on the mechanism of action of the non-steroidal antiphlogistic, benzydamine. A ...
Similar results were obtained when benzydamine N-oxygenation was monitored. A homology model for FMO3 was constructed based on ...
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Benzydamine Monohydrochloride Difflam Lonol Novo-Benzydamine Opalgyne PMS-Benzydamine Ratio-Benzydamine Rosalgin Sun-Benz ... PMS-Benzydamine Narrower Concept UI. M0477228. Registry Number. 0. Terms. PMS-Benzydamine Preferred Term Term UI T622510. Date ... Novo-Benzydamine Narrower Concept UI. M0477226. Registry Number. 0. Terms. Novo-Benzydamine Preferred Term Term UI T622506. ... Ratio-Benzydamine Narrower Concept UI. M0477229. Registry Number. 0. Terms. Ratio-Benzydamine Preferred Term Term UI T000913100 ...
Other interventions with potential effect (based on only one study at the time) included benzydamine, calcium phosphate, honey ... With respect to the treatment of oral mucositis, recent evidence suggests that benzydamine hydrochloride (Tantum) 0.15% taken ... The authors found that the research evidence for the use of benzydamine HCL, sucralfate, tetrachlorodecaoxide, chlorhexidine, ... Roopashri G, Jayanthi K, Guruprasad R. Efficacy of benzydamine hydrochloride, chlorhexidine, and povidone iodine in the ...
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The standard oral protocol of salt-soda and benzydamine gargle every 3 h was done by patients during the course of EBRT and ... Along with the honey, the patients were advised to do salt-soda and benzydamine mouth gargles alternatively, every 3 h as the ... All patients were advised to do salt-soda and benzydamine mouth gargles, alternatively every 3 hours. Test group patients ...
Benzydamine_Hydrochloride,modify,24-FEB-06,(null),(null) C48390,Fowlpox_Virus_Vaccine_Vector,modify,24-FEB-06,(null),(null) ...
Novo Benzydamine. Novo-Benzydamine. Opalgyne. PMS Benzydamine. PMS-Benzydamine. Ratio Benzydamine. Ratio-Benzydamine. Rosalgin ... Benzydamine Hydrochloride Entry term(s). Benzydamine Monohydrochloride Hydrochloride, Benzydamine Monohydrochloride, ... Benzydamine Entry term(s):. Benzidamine. Benzindamine. Benzydamine Hydrochloride. Benzydamine Monohydrochloride. Difflam. ... Benzydamine - Preferred Concept UI. M0002384. Scope note. A benzyl-indazole having analgesic, antipyretic, and anti- ...
Benzydamine D3.438.449.130 D3.633.100.449.130 Benzylisoquinolines D3.438.531.85 D3.633.100.531.85 Berberine D3.549.168.100 ...
Benzydamine Monohydrochloride Difflam Lonol Novo-Benzydamine Opalgyne PMS-Benzydamine Ratio-Benzydamine Rosalgin Sun-Benz ... PMS-Benzydamine Narrower Concept UI. M0477228. Registry Number. 0. Terms. PMS-Benzydamine Preferred Term Term UI T622510. Date ... Novo-Benzydamine Narrower Concept UI. M0477226. Registry Number. 0. Terms. Novo-Benzydamine Preferred Term Term UI T622506. ... Ratio-Benzydamine Narrower Concept UI. M0477229. Registry Number. 0. Terms. Ratio-Benzydamine Preferred Term Term UI T000913100 ...
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Usefulness of benzydamine spray in the postop treatment of dental trauma (i.e., extraction of third molars), as well is its ... Benzydamine and etoricoxib are drugs that can be used as an alternative therapy in patients with hypersensitivity to thenon- ... Benzydamine N-oxygenation was observed in lung microsomes and lung slices. Thermal inactivation of FMO and CYP inhibition ... Although benzydamine clearance in rat appears to be predominantly mediated by hepatic metabolism, the data suggest that the ...
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Benzydamine. Ibuprofen. Indomethacin. Ketoprofen. Naproxen. Columns:. L-Column2 C18, 3 μm, 150 x 4.6mm ID. ...
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  • The safety of Benzydamine hydrochloride has not been established in pregnant patients. (mims.com)
  • Benzydamine hydrochloride 0.15% w/v. (mccabespharmacy.com)
  • The active ingredient in Difflam Mouthwash is benzydamine hydrochloride, which is one of a group of medications called Non-Steroidal Anti-Inflammatory Drugs (NSAIDs). (chemist-4-u.com)
  • Do not use this product if you are allergic to benzydamine hydrochloride or any of the other listed ingredients. (chemist-4-u.com)
  • How will the benzydamine in Difflam Mouthwash help to ease my sore throat? (chemist-4-u.com)
  • Benzydamine is a painkiller that you can take in a mouthwash. (boomja.com)
  • Furthermore, the contribution of rat lung to the clearance of benzydamine was investigated using an in vivo pulmonary extraction model. (bvsalud.org)
  • For example, this enzyme is likely needed to break down the anticancer drug tamoxifen, the anti-inflammatory medication benzydamine, the antifungal drug ketoconazole, and certain medications used to treat depression (antidepressants). (medlineplus.gov)
  • All patients were advised to do salt-soda and benzydamine mouth gargles, alternatively every 3 hours. (jpalliativecare.com)
  • We investigated the metabolism of benzydamine (BZD) in controls as well as patients with severe FMO3 deficiency and found evidence of markedly reduced N-oxygenation capacity both in serum and urine samples. (nih.gov)
  • Benzydamine and etoricoxib are drugs that can be used as an alternative therapy in patients with hypersensitivity to thenon-steroidal anti-inflammatory drugs (NSAIDs). (bvsalud.org)
  • 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. (bvsalud.org)
  • Of the respondents, 44% and 27.7% prescribed benzydamine and morphine to manage their patients' oral mucositis, respectively. (bvsalud.org)
  • Similar results were obtained when benzydamine N-oxygenation was monitored. (nih.gov)
  • Although benzydamine clearance in rat appears to be predominantly mediated by hepatic metabolism, the data suggest that the lung may also make a smaller contribution to its whole body clearance. (bvsalud.org)
  • 11. [Antithrombotic action of benzydamine]. (nih.gov)
  • 13. [New pharmacologic and biochemical findings on the mechanism of action of the non-steroidal antiphlogistic, benzydamine. (nih.gov)
  • 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. (bvsalud.org)
  • Benzydamine N-oxidation as an index reaction reflecting FMO activity in human liver microsomes and impact of FMO3 polymorphisms on enzyme activity. (nih.gov)
  • The aim of this study was to investigate the pulmonary FMO activity in rat using benzydamine. (bvsalud.org)
  • 33. Effect of Honey-Lemon Spray Versus Benzydamine Hydrochloride Spray on Radiation-Induced Acute Oral Mucositis in Head and Neck Cancer Patients: A Pilot, Randomized, Double-Blind, Active-Controlled Clinical Trial. (nih.gov)
  • For example, this enzyme is likely needed to break down the anticancer drug tamoxifen, the anti-inflammatory medication benzydamine, the antifungal drug ketoconazole, and certain medications used to treat depression (antidepressants). (medlineplus.gov)