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PubMed2001

In vitro cytotoxicity of chlorhexidine gluconate, benzydamine-HCl and povidone iodine mouthrinses on human gingival fibroblasts.

Mouthrinses are frequently prescribed for the treatment of ulcerative diseases of the oral mucosa. In this study the in vitro cytotoxic effect of 0.2% chlorhexidine gluconate in water, 0.15% benzydamine-HCl in 8.5% ethanol and 1% povidone iodine in 10% ethanol were determined. Results of photographs and cell counts revealed that all the cells exposed to chlorhexidine gluconate, benzydamine-HCl and povidone iodine were immediately fixated onto the tissue culture surfaces. The three agents were then diluted in phosphate buffered saline to concentrations varying between 10% and 90% and fibroblasts were once again exposed to the dilutions of the test agents. Photographs were taken and cell concentrations in the wells were determined immediately after exposure and after 2, 4 and 24 hours. Results indicated that cells were immediately fixated by 10% chlorhexidine gluconate in water, 20% povidone iodine and 70% benzydamine-HCl. Fibroblasts survived and recovered from the exposure to 8.5% and 10% ethanol, which indicated that the fixation effect is not the result of the ethanol, but should be ascribed to the activity of the active ingredients in the mouthrinses.

Administration, Topical↗
PubMed1989

[Photocontact allergy caused by benzydamine (Tantum)].

Three women with a photoallergic dermatitis precipitated by benzydamine are reported. In one patient the cause of the photosensitization was a cream containing benzydamine (Tantum cream), whereas in the other two the reaction occurred after oral administration (Tantum drops). In all three cases the photosensitization was confirmed by a photopatch test that was positive for the active ingredient benzydamine.

Administration, Oral↗
PubMed1988

[Combination therapy of transcutaneous electric nerve stimulation and iontophoresis with benzydamine and diclofenac].

Combined Therapy of Transcutaneous Electrical Nerve Stimulation and Iontophoresis with Benzydamine and Diclofenac. The combination of transcutaneous electrical nerve stimulation (TENS) and the iontophoresis of benzydamine and diclofenac in a counter-current field is a new method in the treatment of chronical pain of the head and neck region. Prior to a clinical study this method was tested in a preliminary examination in 15 healthy volunteers. Clinical and physical data were investigated from which a theoretical maximum value of the quantity of iontophorised non-steroidal antiphlogistics (NSAI) could be calculated. The actual achievable absorption is discussed. Based on these data it is concluded that a good effective tissue concentration of benzydamine and diclofenac can be achieved with iontophoresis by means of TENS.

Benzydamine↗
PubMed1987

[New aspects on the clinical use of benzydamine].

Recent results of research show that benzydamine (Tantum) has a different biochemical and pharmacological therapeutic mechanism in comparison with other non-steroidal antiinflammatory drugs (NSAID). The inhibition of the generation of reactive oxygen species, the membrane-stabilising effect and the reduction of vascular permeability causes the anti-edematous and antiinflammatory effects. Contrary to the indications and contra-indications of NSAID, benzydamine can be used in the following diseases: inflammatory and edematous diseases of the gastrointestinal tract, of the kidney and genitourinary tract, of the stoma and oropharynx and of the respiratory tract, after soft-tissue injuries and surgical interventions. It is not necessary to exclude patients with acetylsalicylic acid-induced asthma from the therapy with benzydamine.

Benzydamine↗
PubMed1987

Topical benzydamine in the treatment of vaginal radiomucositis.

Radiotherapy for invasive cervical cancer involves a high risk of local complications. Classically, the critical structures are the rectum, the bladder and the bony ring of the pelvis. However, endocavitary curietherapy is an important component in the radiological treatment since it delivers the highest dose to the vaginal mucosa. The anti-inflammatory efficacy of benzydamine in gynaecology, already well documented, was investigated in our controlled clinical study (benzydamine vs. placebo) involving 32 consecutive unselected patients treated by endocavitary curietherapy with 137caesium sources, alone, after radical surgery, or in association with megavoltage external irradiation. In the group with topical benzydamine, we have observed a statistically significant improvement of subjective symptomatology and colposcopic view. On the contrary in the placebo group a worsening of all the clinical parameters considered became evident.

Administration, Intravaginal↗
PubMed1987

Benzydamine, an unique model of anti-inflammatory activity.

Benzydamine is an anti-inflammatory drug with unique medical uses, namely the topical treatment of oro-pharyngeal and gynaecological conditions. This paper illustrates the rationale for the medical use of benzydamine. Its differences from aspirin-like drugs are pointed out, and evidence is presented that benzydamine does not primarily affect the PGs system, but rather reduces the cell response to injury.

Anesthetics, Local↗
PubMed1987

[The action of benzydamine on phospholipase activation].

The effects of the antiinflammatory drug benzydamine (Tantum) on phospholipase activities were determined in vitro, employing various enzyme preparations (rat liver plasma membranes, endoplasmic reticulum, lysosomes; human seminal plasma) and stereospecifically radiolabeled phosphatidylethanolamines as substrates. Fatty acid release from the sn-2 position was inhibited at drug concentrations above 10(-5) mol/l. Concerning the mode of inhibition, a mixed type was found for the soluble phospholipase A2. Impaired fatty acid release from the sn-2 position might contribute to the mechanism of antiinflammatory action of benzydamine by rendering less free precursor acid available for the synthesis of eicosanoids. Fatty acid release from the sn-1 position was inhibited at benzydamine concentrations from 10(-6)-10(-2) mol/l only in lysosomes, whereas in plasma membranes and endoplasmic reticulum it was stimulated, maximally (at 10(-3) mol/l) about 25% and 50%, respectively.

Animals↗
PubMedDate not supplied

Ocular absorption of benzydamine by the rabbit.

An aqueous solution of 0.15 per cent benzydamine hydrochloride, a non-steroidal anti-inflammatory drug, was applied to the rabbit eye. Following topical application to the cornea, the drug was soon detected in the aqueous fluid of the treated eye, whereas the plasma levels were negligible. The possibility that benzydamine can inhibit inflammatory processes in the eye without the risk of side-effects is discussed.

Absorption↗
PubMedDate not supplied

Bioequivalence study of two liquid formulations of benzydamine.

A bioequivalence study of two liquid formulations containing benzydamine hydrochloride was carried out to evaluate the influence of a change of the excipients and the addition of a flavouring agent, ICEBERG AR 84/05/15, on the absorption of benzydamine. No statistically significant differences were observed suggesting that the two formulations are bioequivalent.

Administration, Oral↗
PubMed1993

Photodegradation of benzydamine: phototoxicity of an isolated photoproduct on erythrocytes.

Benzydamine hydrochloride (Tantum, 1) is a photoallergic and phototoxic anti-inflammatory and analgesic agent. This drug is photolabile under aerobic and anaerobic conditions. Irradiation of a methanol solution of benzydamine under oxygen or argon at 300 nm affords 5-hydroxybenzydamine (2) and 2-beta-dimethylaminopropyl-1-benzylindalolin-3-one (3) as the main isolated and spectroscopically identified photoproducts. A radical intermediate was evidenced by thiobarbituric acid that was used as a radical sonde, as well as by the dimerization of cysteine. Erythrocyte lysis photosensitized by 1, 2, and 3 was investigated.

Benzydamine↗
PubMed2000

Differential effect of benzydamine on pro- versus anti-inflammatory cytokine production: lack of inhibition of interleukin-10 and interleukin-1 receptor antagonist.

The production and action of primary proinflammatory cytokines are strictly controlled by a series of circuits to avoid damage that they can cause if produced in excess. Interleukin-10 and interleukin-1 receptor antagonist contribute to the control of the magnitude of the inflammatory responses in vivo. Benzydamine, a non-steroidal anti-inflammatory drug that has been shown to have suppressive activity for the proinflammatory cytokines, tumor necrosis factor-alpha and interleukin-1beta, was investigated for its effects on interleukin-10 and interleukin-1ra production. The drug did not modify the production of interleukin-10 and interleukin-1ra by peripheral blood mononuclear cells stimulated with lipopolysaccharide, under conditions where tumor necrosis factor-alpha and interleukin-1beta were decreased. The antiinflammatory capacity of benzydamine might thus result from its ability to reduce the production of proinflammatory cytokines, without affecting antiinflammatory factors.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1993

Photoproducts of benzydamine and azapropazone: demonstration of their phototoxicity in vitro.

Red blood cell lysis, photosensitized by the products of the aerobic photolysis of benzydamine (1) and azapropazone (4), was investigated. Irradiation of a methanol solution of 1 and 4 under oxygen produces the photoproducts 3-hydroxy-benzydamine, (2), 2-(3-dimethylaminopropyl)-1-benzylindazolin-3-one (3) and 3-dimethylamino-7-methyl-1,2,4-benzotriazine (5). The mechanism of the photodegradation of 1 was examined. Photoproducts 3 and 5 produce singlet oxygen as demonstrated by trapping with 2,5-dimethylfuran. The photohemolysis rate for the photoproducts 3 and 5 was enhanced by deuterium oxide and oxygen. No change was observed in the presence of reduced glutathione. The photohemolysis rate was low under anaerobic conditions.

Apazone↗
PubMed2002

Biotransformation of benzydamine by microsomes and precision-cut slices prepared from cattle liver.

1. Benzydamine (BZ), a non-steroidal anti-inflammatory drug used in human and veterinary medicine, is not licensed for use in food-producing species. Biotransformation of BZ in cattle has not been reported previously and is investigated here using liver microsomes and precision-cut liver slices. 2. BZ was metabolized by cattle liver microsomes to benzydamine N-oxide (BZ-NO) and monodesmethyl-BZ (Nor-BZ). Both reactions followed Michaelis-Menten kinetics (Km = 76.4 +/- 16.0 and 58.9 +/- 0.4 microM Vmax = 6.5 +/- 0.8 and 7.4 +/- 0.5 nmolmg(-1) min(-1) respectively); sensitivity to heat and pH suggested that the N-oxidation is catalysed by the flavin-containing monooxygenases. 3. BZ-NO and Nor-BZ were the most abundant products derived from liver slice incubations, and nine other BZ metabolites were found and tentatively identified by LC-MS. Desbenzylated and hydroxylated BZ-NO analogues and a hydroxylated product of BZ were detected, which have been reported in other species. Product ion mass spectra of other metabolites, which are described here for the first time, indicated the formation of a BZ N- -glucuronide and five hydroxylated and N+-glucuronidated derivatives of BZ, BZ-NO and Nor-BZ. 4. The results indicate that BZ is extensively metabolized in cattle. Clearly, differences in metabolism compared with, for example, rat and human, will need to be considered in the event of submission for marketing authorization for use in food animals.

Animals↗
PubMed2006

Dexpanthenol pastille and benzydamine hydrochloride spray for the prevention of post-operative sore throat.

BACKGROUND: In this study, we aimed to compare the effectiveness of dexpanthenol pastille and benzydamine hydrochloride spray on the prevention of a sore throat. METHODS: One hundred and eighty patients undergoing general anaesthesia, who were ASA I-II and with their ages ranging between 15 and 70 years, were randomly allocated to three groups, each consisting of 60 patients. For group B, four puffs of benzydamine hydrochloride were sprayed into the mouth initially 30 min before the operation and repeatedly 5 min before anaesthesia induction. For group D, two pastilles of dexpanthenol were administered orally to be sucked 30 min before the operation. For group P, four puffs of distilled water were sprayed into the mouth initially 30 min before the operation. Post-operatively, patients were evaluated for a sore throat for the duration of 24 h. RESULTS: The incidence of a sore throat was significantly lower for group D when compared with group B and group P. The incidence of a sore throat was similar for group B and group P. According to the sore throat grading system, the number of patients experiencing no complaints was significantly higher for group D when compared with group B and group P. The number of patients achieving moderate scores was significantly higher for group B when compared with group D. CONCLUSION: The administration of 200 mg of dexpanthenol prophylactically before endotracheal intubation is effective in the prevention of post-operative sore throat.

Administration, Oral↗
PubMed1993

Efficacy of oxytetracycline and tetracycline-benzydamine in the prevention of infection after placental retention in cattle.

The efficacy of intrauterine oxytetracycline and a combination of benzydamine and tetracycline in preventing uterine infections in 150 Italian Friesian cows with retained placentas were compared. The animals were divided into three equal groups. Sixteen per cent of the oxytetracycline-treated group, 12 per cent of the benzydamine-tetracycline-treated group and 76 per cent of the untreated group developed endometritis. The difference between the two treatment groups was not significant but both treatments were effective in preventing septic complications in cows with retained placentas.

Animals↗
PubMed1999

Acute overdose due to benzydamine.

Benzydamine is a nonsteroidal anti-inflammatory drug, currently available as mouthwash, aerosol, dermal cream, vaginal douche preparation, pills and otic drops. Up to now no cases of poisoning due to this drug have been reported. A 6-year-old girl with an accidental poisoning with benzydamine is described. The episode consisted of hallucinosis without other symptoms and resolved spontaneously in 17 h.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1976

Benzydamine: a new weapon in the treatment of interstitial cystitis.

Benzydamine hydrochloride was synthesized in 1966 and developed in Italy. It belongs to a chemical class that has not been used previously in the treatment of inflammatory conditions. Benzydamine is not related to steroids or other anti-inflammatory drugs, it is given by mouth and its toxicity is low. A pilot trial was done in 25 cases of interstitial cystitis and virtually complete relief of pain was noted in 18 cases.

Adult↗
PubMed1987

[Effect of benzydamine on release of prostaglandin E2 and prostacyclin from rabbit gastric mucosa cells].

The effect of the antiinflammatory drug benzydamine (Tantum) on prostaglandin E2 (PGE2) release from rabbit gastric mucosal cells was investigated. Up to 1 mmol/l benzydamine had no significant effect on PGE2 and prostacyclin (PGI2) formation and release. The lack of interference with gastric mucosal prostaglandin synthesis might explain the non-ulcerogenicity of this compound compared to other non-steroidal antiinflammatory drugs (e.g. indomethacin).

Animals↗