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PubMedDate not supplied

A pilot study of chlorhexidine and benzydamine oral rinses for the prevention and treatment of irradiation mucositis in patients with head and neck cancer.

This pilot study was designed to compare the efficacy of 0.2% wt/vol chlorhexidine gluconate and 0.15% wt/vol benzydamine hydrochloride oral rinses in alleviating irradiation oropharyngeal mucositis for patients with head and neck cancer. This was a prospective, randomized, and double-blinded study. Fourteen subjects were stratified based on nasopharyngeal cancer and non-nasopharyngeal head and neck cancer, and were randomly assigned to receive oral care protocol either containing with chlorhexidine (n = 7) or benzydamine (n = 7) from the first day to 2 weeks after the completion of radiotherapy. Subjects were evaluated twice weekly through days 1 to 64 using the World Health Organization mucositis scale and the 10 cm visual analogue scale for mouth pain and dysphagia. In the chlorhexidine arm, 4 subjects (57%) had grade 2, and 3 subjects (43%) had grade 3 mucositis. In the benzydamine arm, 5 subjects (71%) had grade 2, and 2 subjects (29%) had grade 3 mucositis (P > .05). The mean area-under-the-curve values of mucositis were 26.5 +/- 13.6 (median 26) and 24.1 +/- 6.1 (median 22) in the chlorhexidine group and benzydamine group, respectively (P > .05). The mean area-under-the-curve values of pain and dysphagia were 70.8 +/- 33 (median 88.5) and 71.5 +/- 39 (median 101), and 62.1 +/- 17.2 (median 72) and 66 +/- 22.3 (median 57.5) in the chlorhexidine and benzydamine groups, respectively (P > .05). A trend has emerged of a lessening of severity of mucositis, pain, and dysphagia for patients with head and neck cancer receiving benzydamine oral rinse. The beneficial effects, however, need to be confirmed in a larger trial.

Adult↗
PubMed2006

Benzydamine N-oxygenation as a measure of flavin-containing monooxygenase activity.

Benzydamine is a nonsteroidal anti-inflammatory drug that undergoes flavin-containing monooxygenase (FMO)-dependent metabolism to a stable N-oxide. This metabolite can be quantified with high specificity and sensitivity by using a simple reverse-phase high-performance liquid chromatography (HPLC) assay with fluorescence detection. Studies with recombinant FMO enzymes demonstrate that FMOI and FMO3 are the primary catalysts of benzydamine N-oxygenation, with minimal contributions from cytochrome P450 enzymes. Investigations conducted with human liver microsomes confirm that FMO3, in large part, is responsible for benzydamine N-oxide formation in this tissue. These features render benzydamine a useful in vitro probe for FMO activity in a wide range of tissues and cell types. In addition, benzydamine appears to be a suitable in vivo probe for human liver FMO3. This chapter provides a detailed account of the experimental protocol for determining rates of formation of benzydamine N-oxide by FMO-containing enzyme fractions.

Benzydamine↗
PubMed1987

The use of benzydamine HCl for the management of cancer therapy-induced mucositis: preliminary report of a multicentre study.

A multicentre study was undertaken to determine the effectiveness of benzydamine, a non-steroidal antiinflammatory drug, in relieving oral pain and inflammation due to cancer chemotherapy or chemoradiotherapy-induced mucositis. Benzydamine or placebo mouthwash was administered in a double-blind fashion to patients with established mucositis who complained of at least moderate mucositis pain. Preliminary review of the data reveals encouraging trends, subjects who received benzydamine consistently reporting more effective pain relief than those receiving placebo. Benzydamine mouthwash provided good to excellent relief of oral mucositis pain when rated by patients after one day (68% vs 47%) and by examiners both after one day (60% vs 40%) and overall (60% vs 42%). When only very good to excellent responses were considered, observer impressions of benzydamine's effectiveness were found to be statistically significant (p less than .04). These initial results are encouraging and, though not all results are statistically significant, appear to support the potential usefulness of benzydamine mouthwash in managing oral mucositis due to cancer therapy.

Administration, Topical↗
PubMed1993

Pharmacokinetics of benzydamine in dairy cows following intravenous or intramuscular administration.

Five lactating cows were given benzydamine hydrochloride by rapid intravenous (0.45 mg/kg) and by intramuscular (0.45 and 1.2 mg/kg) injection in a crossover design. The bioavailability, pharmacokinetic parameters and excretion in milk of benzydamine were evaluated. After intravenous administration, the disposition kinetics of benzydamine was best described using a two-compartment open model. Drug disposition and elimination were fast (t1/2 alpha: 11.13 +/- 3.76 min; t1/2 beta: 71.98 +/- 24.75 min; MRT 70.69 +/- 11.97 min). Benzydamine was widely distributed in the body fluids and tissues (Vd(area): 3.549 +/- 1.301 L/kg) and characterized by a high value for body clearance (33.00 +/- 5.54 ml/kg per min). After intramuscular administration the serum concentration-time curves fitted a one-compartment open model. Following a dose of 0.45 mg/kg, the Cmax value was 38.13 +/- 4.2 ng/ml at a tmax of 67.13 +/- 4.00 min; MAT and MRT were 207.33 +/- 22.64 min and 278.01 +/- 12.22 min, respectively. Benzydamine bioavailability was very high (92.07% +/- 7.08%). An increased intramuscular dose (1.2 mg/kg) resulted in longer serum persistence (MRT 420.34 +/- 86.39 min) of the drug, which was also detectable in milk samples collected from both the first and second milking after treatment.

Animals↗
PubMed1987

Clinical evaluation of benzydamine, chlorhexidine, and placebo mouthwashes in the management of recurrent aphthous stomatitis.

Eighteen patients with minor recurrent aphthous stomatitis were given alcoholic benzydamine hydrochloride, aqueous chlorhexidine, or a benzydamine-free placebo mouthwash in random order. Each patient used each preparation for a 3-month period. Ulcer diaries were marked at the same time each week during the 9-month test period. Records were made of the number, size, sites, and pain severity of any ulcers present. Statistical analysis of the results showed no significant differences between any of the treatments tested. Stinging of the oral mucosa was the only consistent side effects noted by nine patients using benzydamine, nine patients using placebo, and three patients using chlorhexidine. Eight patients stated a personal preference for benzydamine because of the transient local anesthetic effect of benzydamine, which gave pain relief.

Benzydamine↗
PubMed1990

Determination of benzydamine and its N-oxide in biological fluids by high-performance liquid chromatography.

A simple, sensitive and selective method for the determination of benzydamine in human plasma and urine, and for benzydamine N-oxide in urine, has been developed using high-performance liquid chromatography in the reversed-phase mode. The limit of reliable determination of benzydamine in plasma was 0.5 ng/ml and that in urine 1 ng/ml; the limit of reliable determination of benzydamine N-oxide in urine was 50 ng/ml. 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.

Benzydamine↗
PubMed1999

Estimation of flavin-containing monooxygenase activity in intact hepatocyte monolayers of rat, hamster, rabbit, dog and human by using N-oxidation of benzydamine.

The flavin-containing monooxygenase (FMO)-dependent N-oxidation of benzydamine has been assessed as a method for monitoring the activity of FMOs in monolayer cultures of hepatocytes from rat, dog, rabbit, hamster and human. The advantage of this substrate is that benzydamine N-oxide formation can be measured directly in extracts of cellular incubations without an intensive work-up procedure. Benzydamine and its N-oxide are readily separated by HPLC with fluorometric detection. This assay proved sensitive enough to monitor FMOs activity in intact monolayer of cultured hepatocytes. The formation of benzydamine N-oxide was inhibited when hepatocytes were coincubated with methimazole (another FMO substrate) in a dose-dependent manner, whereas N-octylamine (an inhibitor of cytochrome P450) had no inhibitory effect. In contrast to cytochrome P450, FMO activity assessed by benzydamine N-oxidation was relatively stable for all species studied during 72-h cultures.

Animals↗
PubMed2002

Flavin-containing monooxygenase activity in hepatocytes and microsomes: in vitro characterization and in vivo scaling of benzydamine clearance.

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.

Animals↗
PubMed1990

[Evaluation of benzydamine in treatment of secondary inflammation following extraction of third molars].

A comparative, double-blind, observant, prospective and longitudinal study was performed over 27 patients treated at the maxillofacial surgery unit of the "Adolfo López Mateos" General Hospital, ISSSTE, for the purpose of evaluating the efficacy and tolerability of benzydamine oral spray in post-extraction inflammation. Patients of either sex and assorted ages were selected, with a prerequisite of no current pathology or previous history of hipersensibility. They were divided in two groups, the first one receiving a placebo, and 1.5% oral benzydamine spray applied to the second group. Each patient was instructed to apply the medication six times per day (with four sprays per application) for five days, and clinically evaluated before the study and after two and after five days of treatment. Female patients were predominant, and ages averaged 30.9 years in the benzydamine group and 28.4 years in the lot receiving placebo. Clinical and laboratory evaluations were performed after treatment, with superior results as to clinical course observed in the group treated with benzydamine, as compared to the placebo lot. Usefulness of benzydamine spray in the postop treatment of dental trauma (i.e., extraction of third molars), as well is its antiseptic and analgesic properties, were objectively verified in the patients.

Adult↗
PubMed1987

[The effect of benzydamine on the generation and interaction of reactive oxygen species and cyclo- and lipoxygenase].

Pharmacological mechanisms of benzydamine (Tantum) are studied which are of relevance for the antiinflammatory properties of this non-steroidal antiinflammatory drug (NSAID). Benzydamine most effectively inhibits the generation of reactive oxygen species by murine neutrophils (IC50 1.7 X 10(-5) mol/l). Piroxicam, indomethacin and acetylsalicylic acid are ineffective. Benzydamine, however, does not interfere with xanthine oxidase-dependent superoxide anion radical formation or epinephrine oxidation. The other tested NSAID are as well inactive. The findings confirm the missing cyclooxygenase inhibition of benzydamine (IC50 greater than 10(-3) mol/l), contrary to the other NSAID which are strong (indomethacin IC50 6 X 10(-8) mol/l; piroxicam IC50 2 X 10(-7) mol/l) or moderate cyclooxygenase inhibitors (acetylsalicylic acid IC50 10(-5) mol/l). LTB4 generation via the lipoxygenase is only inhibited by indomethacin (EC50 3.6 X 10(-5) mol/l). Benzydamine appears unique among other NSAID by its relatively strong interference with the generation of reactive oxygen radicals and the lack of cyclooxygenase inhibition.

Animals↗
PubMed1987

[Effects of benzydamine on leukocyte aggregation].

The effect of benzydamine (Tantum) on the aggregation of rat leukocytes was compared to some commonly used nonsteroidal antiinflammatory drugs (NSAID). The aggregation response was induced by various activators such as the tumour promoter phorbol myristate acetate, the chemotactic peptide N-formyl-methionyl-leucyl-phenylalanine (FMLP), arachidonic acid, sodium arachidonate, platelet activating factor (PAF) and a combination of cytochalasin B and Ca++-ionophore A 23187. As compared to indomethacin, piroxicam and acetylsalicylic acid benzydamine was inhibitory against most of the activators, i.e. the receptor-mediated induction of the aggregation by FMLP, the phorbol ester and sodium arachidonate. No effect could be observed against PAF induced aggregation. Under the assay conditions benzydamine exerted cytolytic effects at 2 X 10(-4) mol/l. Cytolysis reached 100% at 5 X 10(-4) mol/l benzydamine, as could be shown microscopically and by measurement of free cytosolic lactate dehydrogenase. Thus benzydamine exerted a broad spectrum inhibitory activity against rat leukocyte aggregation, possibly explained by its unspecific membrane affinity.

Animals↗
PubMed1987

[New pharmacologic and biochemical findings on the mechanism of action of the non-steroidal antiphlogistic, benzydamine. A synopsis].

Benzydamine (Tantum) is an indolic non-steroidal antiinflammatory drug (NSAID) for systemic use in acute traumatic lesions and locally as mouth gargle wash. Benzydamine is lipophilic at pH 7.2, has an affinity for membranes and shows membrane stabilizing properties with local anaesthetic effects. Contrary to other NSAID, benzydamine does not inhibit the cyclo- nor the lipoxygenase (10(-4) mol/l) and is also not ulcerogenic in the rat. Phospholipase A2 is slightly inhibited as well as the lysophosphatide-acyltransferase (greater than 10(-4) mol/l). Macrophage PGE2 synthesis is enhanced at 10(-4) mol/l. The production of reactive oxygen species by phagocytes is effectively inhibited (10(-5)-10(-4) mol/l). Phagocyte degranulation and aggregation are also inhibited (10(-4) mol/l). The strongest in vitro effect is the inhibition of leukocyte adhesion to vascular endothelium (3-4 X 10(-6) mol/l). Benzydamine is also antithrombotic in the rat (ED35 8.5 mg/kg p.o.) and reduces PAF (platelet activating factor)-induced mortality in the mouse (50 mg/kg p.o.; p less than 0.05). It is concluded that benzydamine is antiinflammatory by preventing vessel wall damage from activated, adhering and emigrating leukocytes i.e. being vasoprotective.

Animals↗
PubMed1987

Concentration of benzydamine in vaginal mucosa following local application: an experimental and clinical study.

The results of an experimental and clinical study on the benzydamine binding and distribution in vaginal mucosa are presented, employing benzydamine solution for gynaecological use. When applied first to rats, the mean amount of the drug in their vaginal mucosa became 3.65 +/- 2.99 micrograms/g of fresh tissue with a significant difference between control and treated animals, without detectable amounts in the plasma. When applied to humans, the mean amount of benzydamine assayed in 17 specimens of vaginal mucosa was 9.72 +/- 6.24 micrograms/g. It was greater than the range of animal anti-inflammatory concentration (2-8 micrograms/g) established by pharmacological studies on this drug and justified the local benefits from benzydamine treatment of vaginal inflammation. Benzydamine assayed in seven volunteers with healthy vaginas showed that the drug cannot be detected in the plasma.

Absorption↗
PubMed1985

Double-blind study of benzydamine hydrochloride, a new treatment for sore throat.

Forty-four patients with sore throat participated in a placebo-controlled, double-blind clinical trial of benzydamine hydrochloride administered as a gargle. After medical evaluation and throat culture, 21 patients were treated with a solution containing benzydamine and 23 patients with a placebo solution. Statistical analysis of scores from patients' diaries showed that benzydamine solution afforded significantly greater (P less than 0.001) relief of pain and dysphagia at 24 hours than did the placebo solution. Physician evaluations at 24 hours showed that the benzydamine solution had significantly greater effect than did placebo on hyperemia (P less than 0.004) and edema (P less than 0.005). Side effects were minimal and of no clinical significance. The findings indicate that benzydamine hydrochloride is safe and effective therapy for the signs and symptoms of sore throat.

Adolescent↗
PubMed1981

Use of topical benzydamine in gynecology.

To evaluate the topical anti-inflammatory activity of benzydamine when used as 0.1% solution for vaginal douche, a double blind, parallel group, randomized clinical trial was carried out on 30 patients with vaginitis following internal radiotherapy for carcinoma of the uterus. The patients were divided into 3 groups, one being treated with 0.1% benzydamine plus tricetol as preservative, one with 0.1% benzydamine alone, and one with placebo. Treatment began 12-24 hours after radiotherapy. Benzydamine was found to be significantly superior to placebo in its overall topical anti-inflammatory activity both after 5 and 15 days of treatment. Tricetol did not interfere with the therapeutic effect of benzydamine.

Administration, Topical↗
PubMed1991

Pharmacokinetics of benzydamine after intravenous, oral, and topical doses to human subjects.

The pharmacokinetics of the anti-inflammatory drug benzydamine were determined after intravenous infusion of 5 mg to six healthy male subjects. Benzydamine was characterized as a drug of relatively low systemic clearance (ca. 160 ml min-1) but high volume of distribution (ca. 1101); the apparent terminal half-life in plasma was ca. 8 h. Benzydamine was well absorbed after oral administration, as indicated by a mean systemic availability of 87 per cent. However, absorption of the drug was low (less than 10 per cent of the dose) after its use by male subjects as a mouthwash, or after its application to female subjects as dermal cream and vaginal douche preparations. The data suggest that benzydamine is generally not well absorbed through the skin and non-specialized mucosae, thereby limiting unrequired systemic exposure to this drug when it is used by these routes.

Administration, Cutaneous↗
PubMed1986

Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy.

Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for approval from the Food and Drug Administration.

Adult↗
PubMed2005

Effect of lipophilic counter-ions on membrane diffusion of benzydamine.

Many topically applied drugs are ionized molecules that exhibit poor penetration across the lipid domains of the stratum corneum. Reduction of the charge on the molecule would be expected to enhance skin penetration. The objective of this study was to investigate the interaction of the non-steroidal anti-inflammatory drug benzydamine hydrochloride with suitable counter-ions including ibuprofen sodium. The influence of pH of the donor solution and hence degree of ionization on partitioning between n-octanol:buffer and the flux of benzydamine hydrochloride across polydimethyl siloxane (PDMS) membrane and human epidermis was determined. The maximum flux was determined at pH 7.6 when the fraction unionized was 2.51%, rather than at pH 9 when the fraction unionized was 38.7%. This suggests that at higher pH, although the permeability coefficient is increased, the decrease in solubility and therefore concentration of dissolved benzydamine in the medium results in a decrease in flux across the PDMS membrane. Ion-pair formation or interaction with each of the counter-ions was confirmed by NMR spectroscopy. Significant increases in logP and flux across PDMS membrane were determined for the ion-pairs (0.087, 12.54, 11.31, 0.121 microg cm(-2)h(-1) for benzydamine hydrochloride and ion-pairs with ibuprofen sodium, sodium benzoate and sodium octane sulfonate respectively). This study shows that it is possible to significantly enhance the flux of salts across a lipophilic membrane in the presence of counter-ions, resulting from intermolecular interaction and/or ion-pair formation.

Adjuvants, Pharmaceutic↗