Disease relevance of BENZYDAMINE

• Benzydamine cream for the treatment of post-herpetic neuralgia: minimum duration of treatment periods in a cross-over trial [1].
• This study compared the efficacy of two protocols for oral care using either chlorhexidine or benzydamine as oral rinses to alleviate mucositis in children undergoing chemotherapy [2].
• Prevention of oral mucositis in radiation therapy: a controlled study with benzydamine hydrochloride rinse [3].
• An anti-inflammatory drug, Benzydamine, has given mixed results but in view of its low toxicity it is worth trying in any patient with severe symptoms [4].
• Forty-four patients with sore throat participated in a placebo-controlled, double-blind clinical trial of benzydamine hydrochloride administered as a gargle [5].

High impact information on BENZYDAMINE

• 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 [6].
• Benzydamine inhibits monocyte migration and MAPK activation induced by chemotactic agonists [7].
• ERK1/12 activation in response to chemoattractants was 89-98% inhibited by a 100 microm concentration of benzydamine with an IC50 of 30 microm [7].
• 5. Under the same experimental conditions, pretreatment with 100 microm benzydamine caused a 75-89% inhibition of p38 activation (IC50 25 microm) [7].
• 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 [7].

Chemical compound and disease context of BENZYDAMINE

• PATIENTS AND METHODS: One hundred and thirty-seven patients with nimesulide-induced urticaria were submitted to a single-blind, placebo-controlled peroral challenge with increasing doses of benzydamine [8].
• Background: In this study, we aimed to compare the effectiveness of dexpanthenol pastille and benzydamine hydrochloride spray on the prevention of a sore throat [9].
• Other interventions showing some benefit in only one study were benzydamine, calcium phosphate, honey, oral care protocols, povidone and zinc sulphate.ConclusionsSeveral of the interventions were found to have some benefit at preventing or reducing the severity of mucositis associated with cancer treatment [10].
• The literature supports use of benzydamine for prophylaxis of mucositis caused by conventional fractionationated head and neck radiotherapy, and cryotherapy for short-half-life stomatoxic chemotherapy, such as bolus fluorouracil [11].
• Clinical tolerability of Nimesulide was better than that of Benzydamine: one case of moderate gastric pyrosis and drowsiness was complained of by the Nimesulide-treated patients versus eleven cases of gastro-intestinal discomfort, mouth dryness, and/or drowsiness which were complained of by the Benzydamine-treated patients [12].

Biological context of BENZYDAMINE

• 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 [7].
• Benzydamine (BZD) N-oxidation was evaluated as an index reaction for FMO as was the impact of genetic polymorphisms of FMO3 on activity [13].
• Use of ultrasound to enhance percutaneous absorption of benzydamine [14].
• 1. Benzydamine (BZ), a non-steroidal anti-inflammatory drug used in human and veterinary medicine, is not licensed for use in food-producing species [15].
• RESULTS: Benzydamine, administered at 20 mg/kg s.c. simultaneously with the endotoxin, significantly increased LPS LD50 up to 230 micrograms/mouse (p < 0.05) [16].

Anatomical context of BENZYDAMINE

• Effects of benzydamine on the lipolytic system of fat cells [17].
• Flavin-containing monooxygenase activity in hepatocytes and microsomes: in vitro characterization and in vivo scaling of benzydamine clearance [18].
• In contrast, rat hepatocytes successfully predicted rat in vivo benzydamine clearance to within approximately 30% (>68 versus 48 ml/min/kg) [18].
• Benzydamine N-oxidation in liver microsomes from all common preclinical species demonstrated heat sensitivity [18].
• Photodegradation of benzydamine: phototoxicity of an isolated photoproduct on erythrocytes [19].

Associations of BENZYDAMINE with other chemical compounds

• High doses of indomethacin, aspirin, benoxaprofen and FPL 55712 given i.p. failed to inhibit the effects of an LD80 of Paf, while BW 755C (50-100 mg kg-1) exerted a dose-dependent protection and benzydamine (50 mg kg-1) and nordihydroguaiaretic acid (200 mg kg-1) were partially active [20].
• High-performance liquid chromatography assay for the measurement of benzydamine hydrochloride in topical pharmaceutical preparations [21].
• Products of caffeine and benzydamine metabolism were analysed by reversed-phase h.p.l.c. with u.v. and fluorescence detection [22].
• Evidence suggests that cryotherapy, topical benzydamine and amifostine might provide some benefit in specific situations [23].
• The IC50 for benzydamine against thromboxane synthetase was 100 mug/ml and 250 mug/ml against RSV [24].

Gene context of BENZYDAMINE

• CONCLUSIONS: FMO1 and FMO3 catalyse benzydamine N-oxygenation with the highest efficiency [22].
• The metabolism of benzydamine to its major metabolite, the N-oxide, is mediated by FMO3 in humans [18].
• Under the same conditions, benzydamine had modest or no effect on production of interleukin (IL-1), IL-6 and IL-8 [25].
• AIMS To determine the FMO and P450 isoform selectivity for metabolism of benzydamine and caffeine, two potential in vivo probes for human FMO [22].
• Benzydamine also blocked monocyte chemotactic protein-1 secretion, but it did not affect interleukin-8 production [26].

Analytical, diagnostic and therapeutic context of BENZYDAMINE

• In a double-blind multiple-dose cross-over study benzydamine 3% cream was compared with placebo for the treatment of post-herpetic neuralgia [1].
• An assay system of flavin-containing monooxygenase was developed by fluorometric determination of benzydamine (BZY) N-oxidation with HPLC [27].
• Determination of benzydamine and its N-oxide in biological fluids by high-performance liquid chromatography [28].
• The method has been successfully applied to the analysis of these compounds in biological fluids after administration of intravenous and oral doses of benzydamine to human volunteers [28].
• The development and application of a flow-through amperometric biosensor for benzydamine determination in anti-inflammatory drugs is described [29].

References