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At least 19 recordsLinked to original sources
PubMed2003

Examinations of the antioxidative properties of the topically administered drug bufexamac reveal new insights into its mechanism of action.

The effect of bufexamac on UV-irradiation-induced lipid peroxidation was investigated. Linolenic acid was used as a model lipid. Bufexamac was shown to be capable of reducing the amount of lipid peroxidation. The quantification was carried out by the thiobarbituric acid assay. Irradiation experiments were also performed using HaCaT keratinocytes as a model system. The oxidative changes were quantified by DNA synthesis measurements and cell viability determinations. Bufexamac was found to act antioxidatively again. To investigate free radical involvement, electron paramagnetic resonance studies were carried out. The influence of bufexamac on the concentration of hydroxyl radicals generated by the Fenton system was examined using the spin trapping technique. Moreover, the hydroxamic acid's ability to react with stable radicals was checked. The quantification assay of 2,2-diphenyl-1-picrylhydrazyl hydrate showed no concentration changes of the stable radical caused by bufexamac. In the Fenton assay antioxidative effects were measured after the addition of the drug. The qualitative changes after irradiating bufexamac were studied at a molecular level by electrospray mass spectrometry. Multiple-stage mass spectrometry experiments enabled the establishment of fragmentation schemes. Phenolic degradation products were detected. The results suggest a new interpretation of the controversially debated mechanism of action of bufexamac and indicate possible reasons for its eczema provoking potential.

Administration, Topical↗
PubMed1997

Epidemiological significance of bufexamac as a frequent and relevant contact sensitizer.

Bufexamac-containing ointments and creams are widely used by many patients with eczematous disorders as an alternative to topical corticosteroids. Recent studies provide evidence of a notable prevalence of contact sensitization in patch test populations. The aim of this study was to assess the frequency of use of this topically-applied drug by eczema patients in general, and to evaluate its potential to cause allergic contact reactions. 500 routinely patch tested patients (f:m = 377:123) were tested with bufexamac 5% and Parfenac ointment (the only commercial product available in Austria) in addition to the standard and other series of the German Contact Dermatitis Group. The packaging of the commercial product was shown to the entire study population, to decide whether or not they had ever used this product. In addition, their general practitioner was contacted to verify the anamnestic data. A total of 30 patients agreed that they had definitely used bufexamac, 5 others having probably applied it. The indication for and the duration of treatment were noted. Positive and relevant patch test reactions to bufexamac, as well as the bufexamac-containing ointment, were seen in 20 out of these 35 patients (57%), and sensitization occurred even after short-term application. Our study demonstrates that bufexamac has to be assumed to be a topical drug with a very high sensitization rate in an unselected patch test population (4% of 500 patients), and should therefore be added to the standard series.

Administration, Topical↗
PubMed1999

Effects of intra-articular injections of bufexamac suspension on amphotericin B-induced aseptic arthritis in horses.

OBJECTIVE: To evaluate effects of intra-articular (i.a.) injections of bufexamac on amphotericin B-induced aseptic arthritis in horses. ANIMALS: 24 Standardbred horses. PROCEDURE: Aseptic arthritis was induced in the right intercarpal joint by i.a. injection of amphotericin B (20 mg). One week later (day 0), horses were randomly assigned to four 6-horse treatment groups and treated with i.a. injection of 10, 20, or 40 mg of bufexamac suspension (20 mg/ml) or 2.0 ml of sterile saline (0.9% NaCl) solution (control). The treatment was repeated once after 7 days. Clinical lameness examinations and synovial fluid (SF) analyses were done prior to induction and at weekly intervals for 5 weeks (days 0, 7, 14, 21 and 28). RESULTS: Intra-articular injection of amphotericin B consistently resulted in aseptic arthritis with a lameness index (mean +/- SEM; scale 0 to 5) of 2.7 +/- 0.17 on day 0. Intra-articular injections of 20 and 40 mg of bufexamac significantly reduced the day-28 lameness index, compared with control values. Amphotericin B administration also resulted in a significant increase in SF beta-glucuronidase (BGLUC) activity, and i.a. injections of bufexamac significantly reduced day-28 activity of this enzyme, compared with control values. CONCLUSIONS AND CLINICAL RELEVANCE: 2 i.a. injections of 20 or 40 mg of bufexamac, at weekly intervals, were effective in reducing clinical signs of lameness and SF activity of BGLUC associated with amphotericin B-induced carpal joint arthritis. Bufexamac possesses anti-inflammatory properties useful for i.a. treatment of lameness associated with aseptic arthritis in horses.

Amphotericin B↗
PubMed2003

[Severe allergic contact dermatitis with generalized spread due to bufexamac presenting as the "baboon" syndrome].

HISTORY AND CLINICAL FINDINGS: A 48-year-old woman presented with acute, pruritic, sharply demarcated, erythematous, maculopapulous exanthem in the anogenital area with disseminated maculae over the back. Several days before, the patient had applied as topical treatment a bufexamac-containing ointment to the anal region. INVESTIGATIONS: The patch test showed an allergic test reaction to bufexamac. DIAGNOSIS: The case presents a serious allergic contact dermatitis with generalization, imitating a baboon syndrome, unequivocally linked to the previous topical treatment. CONCLUSION: During the last 10 years allergic reactions to bufexamac have increasingly been reported, sometimes with erythema multiforme-like reactions. Because of the high rate of sensitization, the serious clinical course of bufexamac allergy and the insidious symptoms of this side effect, sometimes mimicking the disease to be treated, the substance should be used neither for proctological nor for dermatological diseases, even more as these patients are considered to be at high risk of developing allergic contact dermatitis because of the abnormal skin barrier. Considering the data presented, the use of bufexamac should be critically reassessed.

Administration, Topical↗
PubMed2001

Effects of intra-articular injections of bufexamac suspension in healthy horses.

OBJECTIVE: To evaluate the effects of intra-articular (IA) injections of bufexamac in horses, focusing particularly on the effects of bufexamac on articular cartilage. ANIMALS: 20 Standardbreds. PROCEDURE: Horses were randomly allocated into 4 groups consisting of 5 horses each, and 20, 60, or 100 mg of bufexamac or 1 ml of sterile saline (0.9% NaCl) solution (control) was injected into 1 intercarpal joint at weekly intervals for 6 treatments (days 0, 7, 14, 21, 28, and 35). Clinical signs and results of hematologic, serum biochemical, and synovial fluid (SF) analyses and radiography were used to evaluate treatment effects. On day 49, all horses were euthanatized; gross necropsy and histologic examinations of internal organs and articular tissues were performed. Glycosaminoglycan concentration of the articular cartilage was evaluated in safranin O-stained sections by use of a semiquantitative microspectrophotometric method. RESULTS: No systemic signs were observed. Temporary mild to moderate heat and effusion were the only clinical signs observed in a number of joints after IA injections and more often only in the 100 mg group, compared with controls. The 100 mg dose resulted in significant increases in SF WBC counts, with relative neutrophilia and SF total protein concentration 24 hours after injection (day 1). No lesions suggestive of toxic effects were detected at necropsy or on histologic examination. No changes in articular cartilage glycosaminoglycan concentration were detected. CONCLUSIONS AND CLINICAL RELEVANCE: Six injections of 20, 60, or 100 mg of bufexamac at weekly intervals did not cause any untoward systemic or local effects. These data suggest that bufexamac is a safe nonsteroidal anti-inflammatory drug for IA administration in horses.

Animals↗
PubMed1987

[Contact allergy to bufexamac].

Thirteen cases of contact allergy to bufexamac have been seen since 1976 at the Department of Dermatology of the University of Heidelberg. Most of the patients were women (69%). Nine patients suffered from chronic eczema and four had stasis dermatitis. Four patients had used bufexamac for less than 2 weeks. Based on the case histories, about half of the patients were suspected of having contact allergy to bufexamac. The clinical picture was consistent with that of allergic contact dermatitis; a generalized eruption was observed in two cases. Eight patients had additional sensitizations; three patients were allergic to benzyl alcohol, which is used as a preservative in the bufexamac cream available commercially. Contact allergy to bufexamac seems to be rare; however, it should be considered as a cause of sensitization in patients with chronic eczema, even after short-term application.

Adult↗
PubMed1989

[Contact allergies caused by bufexamac].

Between 1983 and 1987, there were 24 cases of contact allergy due to bufexamac seen at the Dermatological Hospital of the University of Göttingen. Of these patients, 20 were female und four male. It was noticeable, that the course of disease was particularly protracted and refractory: 16 of 22 patients were hospitalized with an average duration of inpatient treatment of 2.9 weeks. Seven patients had a generalized allergic contact dermatitis. Five patients had used topical preparations containing bufexamac for only one week or less. In 15 of 24 patients, further epidermal sensitization could be found. In all forms of eczematous diseases, especially in patients with chronic eczema, contact allergy to bufexamac should be considered, even if bufexamac preparations were used for only a short time.

Administration, Topical↗
PubMed1988

[Results of a study of the resorption of bufexamac following rectal administration].

12 patients suffering from hemorrhoidal complaints were treated with hemorrhoidal suppositories containing Proctoparf-bufexamac. Using the HPCL method, we measured the concentrations of bufexamac in the serum after 30, 45 and 60 minutes as well as after 2, 3, 6, 7.5 and 20 hours. Neither bufexamac nor its major metabolite (4-butoxyphenyl acetic acid) could be detected in concentrations above 0.2 micrograms/ml and 0.5 micrograms/ml, respectively. These results prove that the application of Proctoparf suppositories is not associated with any significant systemic absorption of bufexamac.

Bufexamac↗
PubMed1987

Intra-articular treatment of inflammatory arthritis: double-blind trial comparing bufexamac with methylprednisolone acetate.

A double-blind trial was carried out to weigh the effectiveness and tolerance of intraarticular injections of bufexamac (20 mg) against methylprednisolone (40 mg) in 40 patients with an acute bout of inflammatory arthritis. Leucocyte and polymorphonuclear counts and viscosity measurement of the synovial fluid were performed before and 14 days after injection, which showed methylprednisolone to be significantly superior to bufexamac in suppressing inflammation. In both groups a statistically significant improvement of pain on mobilisation and pain index was noted, but the number of clinical remissions was significantly higher in the methylprednisolone group. The blind investigator found a statistically significantly greater improvement with methylprednisolone than with bufexamac, and patients' opinion on effectiveness did not differ significantly. Important local or general side-effects were not observed. It was concluded that, although both drugs appeared to exert a considerable anti-inflammatory effect in inflammatory arthritis, methylprednisolone was more effective.

Anti-Inflammatory Agents↗
PubMed1998

Photo Koebner phenomenon in erythema-multiforme-like eruption induced by contact dermatitis due to bufexamac.

A photo Koebner phenomenon following contact dermatitis due to bufexamac is described. A 52-year-old man presented with dermatitis on his buttocks and an erythema-multiforme (EM)-like eruption near the original lesion and on sun-exposed areas. He had been using bufexamac ointment (Anderm(R)) around and inside the anus for a few weeks before he noticed exacerbation. On patch testing, he exhibited severe contact sensitivity to bufexamac. Phototesting performed on his first visit showed that he had an abnormal reaction to UVB. An EM-like eruption similar to the original lesions developed around the irradiated sites. In this case, photosensitivity does not seem to be a drug-induced photoallergy due to systemic or topical use, but rather a photo Koebner phenomenon.

Administration, Topical↗
PubMed1977

Efficacy of bufexamac (NFN) cream in skin diseases. A double-blind multicentre trial.

The effect of a new non-steroid anti-inflammatory substance (bufexamac) in a special constituent was compared with that of 0.1% triamcinolone acetonide, 1% hydrocortisone cream, and placebo during a double-blind multicentre trial. The clinical effect of these four creams was studied in 193 patients receiving treatment for the following skin disorders: atopic dermatitis, allergic contact dermatitis, and non-allergic contact dermatitis, as well as dermatitis seborrheica. After 2 and 4 weeks' treatment, when 193 and 157 patients, respectively, were re-examined, the effect of triamcinolone acetonide and hydrocortisone cream was significantly better, than that obtained with bufexamac in the cream basis employed. On the other hand, no statistically significant difference in effect between bufexamac and placebo cream was observed.

Administration, Topical↗
PubMed1978

Double-blind trial comparing bufexamac infiltrations with triamcinolone acetonide infiltrations in patients with periarthritis of the shoulder.

A double-blind trial was carried out in 40 patients with an acute episode of periarthritis of the shoulder to compare the effectiveness and toleration of local infiltrations of bufexamac and triamcinolone acetonide. Patients received 1 or 2 local infiltrations with either 20 mg bufexamac or 40 mg triamcinolone acetonide. The results were evaluated by objective and subjective assessments of pain, loss of function, mobility, and by doctors' and patients' opinions of relief. There was a significant, comparable reduction in pain and discomfort in both groups after the first injection. Fourteen patients in each group required a second injection, with slightly more improvement in those receiving bufexamac. Local intolerance of the injections was noted in approximately 25% to 30% of the patients.

Adult↗
PubMed1988

Evaluation of the efficacy of topical bufexamac in epidermolysis bullosa simplex. A double-blind placebo-controlled crossover trial.

Although, as yet, there is no specific treatment of epidermolysis bullosa (EB) simplex, anecdotal reports suggest the possible efficacy of one of the newer topical nonsteroidal anti-inflammatory agents, bufexamac. To determine whether bufexamac has any role in the management of this disease, a double-blind placebo-controlled crossover clinical trial was undertaken with ten patients (nine, Weber-Cockayne variant; one, generalized EB simplex). Each of the two preparations was applied four times daily during the 2 four-week treatment periods. Weekly assessments included counts of blisters, crusts, and erosions, and assessments of alterations in cutaneous pain, healing times, and activity times before further blister formation. Although considerable variability in individual responses was noted, no significant difference was detectable between the active drug and its matched placebo. On the basis of these findings, it was concluded that 5% topical bufexamac is ineffective in the treatment of EB simplex.

Administration, Cutaneous↗
PubMed1999

[A severe epicutaneous test reaction to the bufexamac in a hemorrhoidal therapeutic preparation].

HISTORY AND FINDINGS: A 49-year-old woman presented with acute perianal vesicular/bullous contact dermatitis. Other areas were over the trunk, face, neck and wrists. She reported occasional application of an ointment (Mastu S) to treat her hemorrhoids. INVESTIGATION: Patch tests (basic series, anal block, own ointment, local anesthetic, cosmetics) provoked strong vesicular and bullous reactions of persisting crescendo type, spreading far beyond the site of application, to Bufexamac, to a derivative of hydroxxamine acid, and to local applied ointment with mild or moderate antiinflammatory action. TREATMENT AND COURSE: A week after the patch tests there was a flare-up of the previous foci of dermatitis. These reactions subsided two days later after intravenous injection of prednisolone. The skin lesions healed after rapid reduction of the systemic treatment and local application of corticosteroids, bathing with tanning substances and basic preparations. CONCLUSION: While Bufexamac is not absorbed when applied rectally, perianal contamination may not be avoidable on intra-anal application and can produce sensitization.

Acute Disease↗
PubMed1994

Erythema-multiforme-like, urticarial papular and plaque eruptions from bufexamac: report of 4 cases.

4 patients developed an erythema-multiforme-like reaction following acute contact dermatitis from 2 different bufexamac-containing topical preparations. Histologically, the lesions did not show changes that were typical of erythema multiforme. Patch testing gave positive reactions to bufexamac at 1, 2, 3 and 4 days. The histological picture of 2 positive test reactions was suggestive of a drug reaction in the 1st, and of an acute eczematous reaction in the 2nd, case. A systemic allergic reaction with spread of lesions could have been involved, following percutaneous absorption of the allergen.

Adult↗
PubMed1979

Efficacy of bufexamac cream versus betamethasone valerate cream in contact dermatitis: a double-blind trial.

A double-blind controlled study was carried out in 72 patients with atopic or contact dermatitis, who were randomly allocated to receive treatment with either 5% bufexamac, 0.1% betamethasone valerate or placebo creams. Patients applied the cream twice daily for 2 weeks. Assessments of the degree of severity of inflammation, induration, lichenification, crusts, scaling, and pruritus were made before and after treatment. The results showed that both active preparations were equally effective in improving the skin condition in the majority of the patients. In younger patients, however, the improvement with betamethasone valerate appeared to be somewhat better than that with bufexamac, particularly in relation to pruritus.

Administration, Topical↗
PubMed1985

[Comparative testing of Kamillosan cream and steroidal (0.25% hydrocortisone, 0.75% fluocortin butyl ester) and non-steroidal (5% bufexamac) dermatologic agents in maintenance therapy of eczematous diseases].

We report on 161 patients suffering from inflammatory dermatoses on hands, forearms, and lower legs who had been initially treated with 0.1% difluocortolone valerate. During the maintenance therapy carried out over a period of 3 to 4 weeks, we tested the efficacy of Kamillosan cream vs. 0.25% hydrocortisone, 0.75% fluocortin butyl ester, and 5% bufexamac in a bilateral comparative study. For the indications tested Kamillosan cream showed more or less equieffective therapeutic results as compared to 0.25% hydrocortisone. It is superior, however, to the non-steroidal anti-inflammatory agent 5% bufexamac as well as to 0.75% fluocortin butyl ester, a further glucocorticoid. With regard to neurodermitis, Kamillosan cream not only shows the same therapeutic effect as 0.25% hydrocortisone but is even of marked superiority towards other reference products.

Adolescent↗
PubMed1989

[Treatment of diaper rash with Parfenac lipid ointment (bufexamac). A study by Austrian pediatricians].

447 children between 0 and 24 months with diaper dermatitis were treated by topical application of Parfenac-Fettsalbe (Bufexamac). This panel was selected out of 844 patients which were originally in the protocol. The Parfenac-Fettsalbe was well tolerated, 7 children presented local side effects. 62.71% of treated girls showed very good results, whereas 59.89% of boys showed this outcome. Good results were obtained in 24.35% of girls and 21.93% of boys. Very good (no efflorescences remaining) and good results (some remaining efflorescences) were thus found in more than 80% of patients treated: with respect to corticosteroid advoidance this can be regarded as an effective antiphlogistic medication for diaper dermatitis. Non responders might have been superinfected with microorganisms as candida and staphylococci. In addition, epidemiological considerations are reported in that study.

Bufexamac↗