[Benzydamine in practice. Therapeutic results in external and parenteral administration of benzydamine in traumatology].
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Benzydamine↗
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[Comparative study on the action of benzydamine and benzydamine combined with chlortetracycline in the therapy of the mixed form of chronic respiratory disease of chickens].
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Animals↗
Effect of benzydamine on exocytosis and respiratory burst in human neutrophils and mononuclear phagocytes.
The effect of benzydamine on stimulus-dependent respiratory burst activity and enzyme release was tested in human neutrophils, monocytes and monocyte-derived macrophages. Established anti-inflammatory compounds, indomethacin, phenylbutazone and bufexamac, were tested for comparison. Care was taken to avoid cytotoxic or cytolytic concentrations of the test compounds, and their effect on release of lactate dehydrogenase was also tested. Release of specific and azurophil granules contents were induced in human neutrophils by A23187, PMA and fMLP with and without cytochalasin B pretreatment. Benzydamine inhibited stimulus-dependent release of vitamin B12-binding proteins, a marker for the specific granules, in a concentration-dependent fashion. By contrast, phenylbutazone and bufexamac were practically inactive. The effect of benzydamine on exocytosis of azurophil granules was tested in cytochalasin B-pretreated neutrophils. Benzydamine, again in contrast to the two reference anti-inflammatory compounds, inhibited release concentration-dependently also under these conditions. The concentration of the compound which inhibited exocytosis by 50% was 30-100 microM in normal and 3-10 microM in cytochalasin B-treated neutrophils. The effect of benzydamine and reference compounds on the respiratory burst was tested by assaying for superoxide formation in neutrophils and H2O2 formation in mononuclear phagocytes. Benzydamine was inactive on neutrophils and inhibited slightly the burst response of monocytes and macrophages. Two reference compounds, bufexamac and phenylbutazone, were generally more active. The strongest inhibitory effect was that of phenylbutazone on fMLP-stimulated cells. Benzydamine lacked activity under these conditions, indicating that it does not bind to the receptor of formylated chemotactic peptides.(ABSTRACT TRUNCATED AT 250 WORDS)
Benzydamine↗
Effects of benzydamine eye drops on the rabbit's eye reaction to surgical, physical, and chemical stimuli.
The effects of benzydamine eye drops on the ocular reaction to different irritating stimuli in rabbits are reported. Benzydamine at the concentration of 0.1% reduces inflammatory tissue changes induced by AgNO3 burning of the cornea and inhibits the blood-aqueous barrier breakdown due to peripheral iridectomy or laser irradiation of the iris. Benzydamine reduces the aqueous PGE2 concentration to a similar extent as a 0.5% commercially available eye drop formulation of piroxicam. This result is in contrast with previous in vitro results demonstrating that benzydamine is devoid of any effects on PG synthesis. The possibility that PGE2 reduction is an indirect effect due to other biochemical activities of benzydamine is discussed. In the normal eye benzydamine manifests a local anaesthetic effect which is not accompanied by irritative changes in the anterior segment of the eye, changes in the intraocular pressure or pupillary size. It is suggested that in the clinical use of benzydamine eye drops the local anaesthetic activity may contribute to reducing both the neurogenic component of ocular inflammation and acute pain following injuries to the eye.
Anesthesia, Local↗
Benzydamine HCl, a new agent for the treatment of radiation mucositis of the oropharynx.
Benzydamine HCl is a new nonsteroidal analgesic and anti-inflammatory compound which is not chemically related to local anesthetics such as procaine and xylocaine. A double-blind, randomized clinical investigation was carried out to determine the analgesic and anti-inflammatory effectiveness of benzydamine HCl in patients with radiation-induced mucositis of the oropharynx. Of the 67 patients in the study, 37 were on benzydamine and 30 on placebo. Patients developed radiation mucositis, hyperemia, and throat pain when the total radiation dose reached above 2,000 rad over 2 weeks (200 rad per fraction, five treatments per week). Analysis of the data showed that benzydamine HCl used as a rinse/gargle provided a statistically significant and clinically meaningful alleviation of the symptoms of oropharyngeal mucositis. There was also significant improvement in terms of reduction in hyperemia and mucositis in benzydamine group. No systemic side effects associated with benzydamine medication were noted. In view of the relative ineffectiveness of systemic analgesics and topical anesthetics for these conditions, benzydamine HCl promises to be a useful addition to the therapeutic armamentarium.
Analgesics↗
[The effect of benzydamine on various functions of human granulocytes and their interaction with endothelial cells].
The influence of the non-steroidal antiinflammatory drug benzydamine (Tantum) was studied on several functions of human polymorphonuclear leukocytes, namely their adhesion to endothelial cells, the leukocyte auto-aggregation and their locomotion into cellulose nitrate filters or on glass surfaces. The granulocytes were stimulated either by the synthetic oligopeptide N-formyl-methionyl-leucyl-phenylalanine (FMLP) or the physiologically important complement anaphylatoxins C3a and C5a-desArg. The experiments showed that benzydamine reduces effectively the attachment of granulocytes to endothelium of isolated guinea pig aortic strips (IC50 3-4 X 10(-6) mol/l). This effect seems to be exclusively due to the inhibition of granulocyte adhesiveness and cannot be washed out. Benzydamine also diminishes leukocyte aggregation induced by either the complement peptides C3a, C5a-desArg or FMLP, and in addition causes deaggregation of already formed leukocyte aggregates. However, benzydamine is inhibitory only at 1-3 X 10(-4) mol/l. Likewise, C5a-desArg-induced leukotaxis and phagocyte polarization on glass surfaces as well as spontaneous migration of unstimulated granulocytes in Boyden chambers are decreased only at 10(-4) mol/l. By contrast, benzydamine usually augments chemotaxis in Boyden chambers induced by concentration gradients of the stimuli. This effect might be explained by the prevention of the known auto-oxidative inhibition of phagocytes exerted by benzydamine. Regarding the therapeutic significance, inhibition of the leukocyte-endothelial interaction appears to be of considerable pharmacologic relevance to explain the antiphlogistic properties of benzydamine in vivo.
Animals↗
Review of pharmacological data on benzydamine.
Pharmacological results are reviewed supporting the use of benzydamine in so-called "primary inflammations" rather than in rheumatic diseases. In experimental studies, benzydamine shares with aspirin-like drugs their activity in acute inflammatory responses but not in Freund's adjuvant arthritis. The efficacy of benzydamine is mainly manifested against phenomena such as pain and oedema which depend on local mechanisms in the inflammatory focus. Other manifestations such as hyperthermia which are indicative of systemic functional involvement, are poorly affected by the drug. Benzydamine also lacks some of the typical side-effects of aspirin-like drugs which are thought to reflect their generalized activity. Finally topical application increases the analgesic and antiinflammatory activities of benzydamine much more than those of other antiinflammatory drugs. The data reported demonstrate that benzydamine specifically acts on the local mechanisms of inflammation. In order to explain this feature the chemical, pharmacokinetic and biochemical properties of benzydamine are discussed.
Administration, Topical↗
A clinical study of benzydamine for the treatment of radiotherapy-induced mucositis of the oropharynx.
A double-blind, randomized clinical study was undertaken to determine the analgesic and antiinflammatory effectiveness of benzydamine in patients with radiation-induced mucositis of the oropharynx. Of the 67 patients in the study, 37 patients were on benzydamine and 30 patients on a placebo. The results of the study showed that benzydamine possessed a significant analgesic activity as evidenced by relief of mouth and throat pain induced by radiation therapy. It is also noted that the patients on benzydamine exhibited a cumulative relief of oral pharyngeal pain and discomfort over the time of treatment, as compared to those on the placebo. These effects of benzydamine in the present study might be a result of the antiinflammatory property of the drug. The cumulative and prolonged effectiveness of benzydamine makes it of distinct value compared with the commonly available local anaesthetics such as lidocaine. Benzydamine appears to provide a useful addition to the therapeutic armamentarium for alleviating the symptoms of oral pharyngeal mucositis.
Adult↗
Pharmacokinetics of benzydamine.
Clinically, benzydamine can exert its action locally or systemically. Consequently the pharmacokinetics of this drug have been studied after its administration by several different routes. Oral doses of benzydamine are apparently well absorbed and plasma drug concentrations reach a peak fairly rapidly (e.g. 0.8 micrograms/ml after a 100-mg dose) and then decline with a half-life of about 13 h. Less than 20% of the drug is bound to plasma proteins. Assuming complete oral systemic availability, values of 193 ml/min and 213 litres respectively were calculated for the systemic clearance and volume of distribution of benzydamine. Cutaneous doses of benzydamine are more slowly absorbed and lead to peak drug levels about three-fold lower, but more persistent than those after oral administration. Although local drug concentrations are relatively large, the systemic absorption of mouthwash-gargle, vaginal and rectal doses of benzydamine is relatively low compared to oral doses: this lower absorption should greatly diminish the potential for any systemic drug side-effects when benzydamine is administered by these routes. Benzydamine is metabolized primarily by oxidation, conjugation and dealkylation.
Absorption↗
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↗
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↗
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↗
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↗
[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↗
[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↗
[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↗
[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↗
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↗