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Intrinsic potencies of novel thiol ester corticosteroids RS-85095 and RS-21314 as compared with clobetasol 17-propionate and fluocinonide.

The intrinsic potencies of two novel topical thiol ester corticosteroids, RS-85095 and RS-21314, were compared with the high potency corticosteroids clobetasol 17-propionate and fluocinonide, using human vasoconstriction assays. In these assays, four or five concentrations (0.03 to 3 mg/L) of the corticosteroids in 95% ethanol (alcohol, USP) were applied to predetermined sites on the forearm of volunteers and were occluded following evaporation of the alcohol. The responses were scored in terms of the presence or absence of vasoconstriction and the degree of vasoconstrictive intensity. No statistically significant difference was found in the intrinsic potencies of RS-85095, RS-21314, and clobetasol 17-propionate, and all three corticosteroids were significantly more potent than fluocinonide.

Administration, Topical↗

Multicenter study comparing 0.05% gel formulations of desoximetasone and fluocinonide in patients with scalp psoriasis.

A double-blind, multicenter study was conducted to evaluate and compare the safety and efficacy of desoximetasone gel 0.05% and fluocinonide gel 0.05% in patients with scalp psoriasis. One hundred twenty-five patients were enrolled in this randomized, parallel-group trial. Responses based on clinical assessment in 123 patients showed that the desoximetasone gel formulation is a safe and effective treatment for psoriasis of the scalp. Although efficacy appears equivalent to that of fluocinonide gel 0.05% in treating psoriasis of the scalp, desoximetasone appears to be slightly better tolerated and better accepted cosmetically.

Administration, Topical↗

Comparative study of desoximetasone ointment 0.25% versus fluocinonide ointment 0.05% in patients with psoriasis.

In a multicenter, investigator-blind study, desoximetasone ointment 0.25% was compared with fluocinonide ointment 0.05% in the treatment of patients with psoriasis. Evaluations were made before treatment and after 4, 7, and 14 days of treatment. Both drugs were shown to be safe and effective. Desoximetasone was significantly superior to fluocinonide in improving severity scores from baseline for thickening (days 7 and 14) and erythema (day 14); in numbers of subjects cleared of thickening (day 4); in overall evaluation ratings as compared to baseline (day 14); and in number of patients receiving an overall evaluation of excellent. No side effects were reported for either treatment group during the study.

Adolescent↗

Comparison of amcinonide ointment 0.1 percent twice daily and fluocinonide ointment 0.05 percent three times daily in the treatment of psoriasis.

Thirty-nine patients with psoriasis were treated either with amcinonide ointment 0.1 percent twice a day or with fluocinonide ointment 0.05 percent three times a day in a two-week, randomized, parallel-group, double-blind study. The severities of the skin lesions at baseline and at weekly intervals and the overall improvement at weekly intervals were evaluated by the investigator and the patient. The skin lesions improved significantly (p less than or equal to 0.01) over their condition at baseline, with good overall improvement attained by both treatment groups within one week. Both treatments were well tolerated. Amcinonide ointment 0.1 percent applied twice a day was found to be as effective and acceptable to patients as was fluocinonide ointment 0.05 percent applied three times a day in the treatment of psoriasis.

Double-Blind Method↗

Betamethasone valerate ointment compared with fluocinonide FAPG.

Betamethasone 0.1% as valerate in an ointment base and fluocinonide 0.05% in a fatty alcohol propylene glycol (FAPG) base have been compared in a double-blind trial of 76 patients with either eczema or psoriasis. The results show betamethasone valerate ointment to be significantly (P less than.05) superior to fluocinonide FAPG in the treatment of both these skin conditions. In the light of publications from other studies on betamethasone valerate cream this trial indicates that the ointment base considerably increases the efficacy of betamethasone valerate.

Betamethasone↗

Treatment of refractory psoriasis with fluocinonide gel.

Twenty patients with refractory psoriasis that had responded poorly to previous therapy were treated with fluocinonide gel (0.05 percent), unoccluded, for six weeks. Patients were evaluated weekly. By the sixth week, all patients had improved, and seventeen (85 percent) showed "excellent" improvement. One patient discontinued the trial after four weeks because the lesions had completely cleared. No other patient discontinued using the medication for any reason. Patient complaints were minimal and consisted of stinging (three patients), itching (two patients), and drying (two patients). The study suggests that fluocinonide gel (0.05 percent) is a cosmetically acceptable alternative for the treatment of refractory psoriasis.

Adolescent↗

[The topical treatment of atrophic-erosive oral lichen planus with fluocinonide in a bioadhesive gel, chlorhexidine and miconazole gel. A totally open trial].

To evaluate the efficacy and long-term course of topical steroids treatment in oral lichen planus (OLP), an open trial has been carried out in 30 patients with atrophic-erosive or symptomatic varieties of OLP confirmed histologically with relative contraindications for systemic steroid treatment (namely, liver disease, peptic ulcer, diabetes, blood hypertension or osteoporosis). The treatment was the following: Fluocinonide (Topsyn) 0.025% in 4% idrossiethylcellulose gel applied 3 times/daily for two months, 2 times/daily for the next 2 months and 1 times/daily for other 2 months. Moreover, chlorhexidine (Plakout) 0.12%, 3 mouthwashes/daily and miconazole gel (Micotef) applied 1 times/daily were used for the entire period of the steroid therapy as antimycotics. The clinical evaluation of signs and symptoms was assessed on a scale of 0 to 5 and of 0 to 3, respectively. Twenty patients concluded the entire therapeutical scheme, whereas 5 (17%) interrupted the treatment for the appearance of side-effects (namely, gastroesophageal disturbances, mucosal bleeding and pruritus), 1 interrupted voluntarily the treatment and 4 cases did not present at the controls. No cases of oral candidiasis were seen. Eighteen patients (90%) had improvements of oral lesions with significant statically reductions in the scores of signs (p < 0.002) and of symptoms (p < 0.02) (Wilcoxon test). We emphasize also that in 61% of the responders the oral conditions were stable after 6 months of follow-up. In conclusion our results suggest the following: a) fluocinonide is an effective and safe drug for the treatment of OLP, especially in addition with chlorehixidine and miconazole; b) the stability of our results demonstrates that probably an adequate steroid therapeutical scheme is more useful than continuous steroid administration in the treatment of OLP.

Administration, Topical↗

Multicenter trial analysis. Fluocinonide and betamethasone gel in psoriasis.

The relative efficacy of fluocinonide and betamethasone benzoate gels in treating the symptoms of psoriasis was evaluated in 335 patients, of whom 263 were analyzable. By means of a paired comparison design in which both drugs were examined simultaneously in the same patient, many potential sources of variation were eliminated. In addition, the analysis took into account the difficulties of pooling results in a multicenter trial. Imposing a rigorous grouping structure on the results from individual clinics minimized differences between clinics and demonstrated consistently high, statistically significant results in favor of fluocinodine gel even when several different statistical approaches were used. Local adverse reactions related to drugs were experienced by few patients.

Administration, Topical↗

Pyostomatitis vegetans associated with ulcerative colitis. Temporary clearance with fluocinonide gel and complete remission after colectomy.

Pyostomatitis vegetans is a rare condition characterized by pustules that affect the oral mucosa. It is consistently associated with inflammatory bowel disease and is usually resistant to treatment. We present the case of a 65-year-old white man with pyostomatitis vegetans that was associated with ulcerative colitis and adenocarcinoma of the colon. Fluocinonide gel resulted in a complete but temporary clearance of the lesions. Complete remission was achieved immediately after a total colectomy.

Adenocarcinoma↗

Preliminary clinical evaluation of a new topical corticosteroid, halopredone acetate, as compared to fluocinonide.

17,21-Bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-diene-3,20-dione (halopredone acetate; Topicon), a new corticosteroid for topical use, was compared with fluocinonide in a double blind sequential study. The tests were made on a total of 16 patients affected with psoriasis and exudative dermatitis. In each patient, the symmetrically distributed skin lesions were separately treated with either halopredone acetate or the reference compound. The two active substances were in the same concentration (0.05%) in the same carrier (cream), and both reduced the subjective and objective symptoms of these skin conditions. No statistically significant differences were observed between the two medicated areas. Haloperidone acetate, the excipients of the cream and the reference compound were all excellently tolerated.

Administration, Topical↗

Topically applied fluocinonide in an adhesive base in the treatment of oral vesiculoerosive diseases.

Patients with oral vesiculoerosive diseases frequently require corticosteroid treatment to induce healing and reduce pain. Because of the adverse effects associated with systemic use, topical application of 0.05% fluocinonide in an adhesive base was investigated. The study group was comprised of 89 patients with erythema multiforme, lichen planus, benign mucous membrane pemphigoid, or pemphigus. In the double-blind phase involving 15 patients, seven responded completely and eight partially to the topical ointment. In the open study that included 74 patients, 35 had complete disappearance of signs and symptoms, while 39 experienced partial benefit. There were no adverse side effects. All 89 patients were observed for three to 35 months and each patient's condition continued to respond to the treatment when its use was required.

Administration, Topical↗

Fluocinonide compared with betamethasone in the treatment of eczema and psoriasis.

Good results have been obtained with a single daily application of fluocinonide ('Metosyn') to one area as compared with a twic-daily application of betamethasone 17-valerate ('Betnovate') to a similar area on the opposite side in the treatment of eczema and psoriasis. These conditions are difficult to control even in favourable circumstances and have a tendency to relapse despite any form of treatment. Both creams were entirely acceptable to the patients involved and during the course of the trial no patient expressed dissatisfaction with either the mode of treatment or the preparation involved.

Betamethasone↗

Once-daily fluocinonide-bifonazole combination for the treatment of vulvar itching and vulvovaginal candidiasis. Preliminary study.

Vulvovaginitis presents a therapeutic challenge. Treatment of vulvovaginal candidiasis with topical imidazole preparations is well accepted. In our work we tested a new cream combining antifungal Bifonazole with a corticosteroid agent (Fluocinonide). The results suggest that most of the patients with vulvovaginitis can benefit from treatment with this new combination cream.

Adolescent↗

A complete proton and carbon-13 NMR analysis of fluocinonide, a fluorinated corticosteroid.

This paper presents a complete analysis of the proton and carbon-13 NMR spectra of 21-acetoxy-6 alpha,9-difluoro-11 beta-hydroxy-16 alpha,17-(1-methylethylidene) bis-(oxy) pregna-1,4-diene-3,20-dione, a potent anti-inflammatory fluorosteroid. The 300 MHz proton spectrum was analyzed using a combination of the two-dimensional homonuclear chemical shift correlation (COSY) technique and one-dimensional NOE difference spectra. Exact coupling constants and chemical shifts were obtained by spectral simulation and iteration. The carbon-13 spectrum was assigned from the proton spectrum via a two-dimensional heteronuclear chemical shift experiment, and long-range fluorine-proton couplings were confirmed by a fully coupled heteronuclear COSY-type experiment.

Chemical Phenomena↗