Synalar
Effects of topically potent glucocorticoids on human diploid fibroblasts in vitro.

Kirk D, Mittwoch U.

A wide range of concentrations of both cortisol and a topically more potent synthetic derivative, fluocinolone acetonide, was found not to inhibit the growth of cultured human skin fibroblasts; fluocinolone acetonide produced a slight increase in the growth rate. Both steroids had a transient stimulatory effect on fibroblasts, promoting an earlier entry into the period DNA synthesis (S) which was also accompanied by a substantial increase in the length of S.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=889702&dopt=Abstract fluocinolone Synalar



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Rationale for the use of topical corticosteroids in melasma.

Menter A.

Division of Dermatology, Baylor University Medical Center, Dallas, Texas, USA.

Corticosteroids have been combined with other agents in the treatment of melasma for years. In early studies by Kligman and Willis, topical dexamethasone as monotherapy produced little depigmentation even after 3 months of therapy. A significant concern is that topical corticosteroids used alone in this setting, especially on the face, may result in epidermal atrophy, telangiectasia, rosacea-like erythemas, acne, and perioral dermatitis. Topical corticosteroids, however, including low-potency fluocinolone acetonide, also exert an anti-metabolic effect, resulting in decreased epidermal turnover, and, thus, may produce a mild depigmenting effect. When used in combination with tretinoin and hydroquinone in the treatment of melasma, fluocinolone acetonide 0.01% suppresses biosynthetic and secretory functions of melanocytes, and thus melanin production, leading to early response in melasma, synergy among the three agents, and no significant side effects over an 8-week period.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15098972&dopt=Abstract fluocinolone Synalar



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Ocular pharmacokinetics of fluocinolone acetonide after Retisert intravitreal implantation in rabbits over a 1-year period.

Driot JY, Novack GD, Rittenhouse KD, Milazzo C, Pearson PA.

Bausch & Lomb, Montpellier, France. jean-yves.driot bausch.com

PURPOSE: The present study was designed to examine the pharmacokinetics of a fluocinolone acetonide (FA) intravitreal implant in pigmented rabbits. METHODS: Pigmented rabbits were randomly assigned to receive either a 0.5 mg or 2.0 mg FA intravitreal implant (Retisert). Four animals were sacrificed per time point (2 hours; 2 weeks; and 3, 6, 9, and 12 months after implantation) for FA intraocular levels determination. RESULTS: In the vitreous, concentration of FA was relatively constant from the first time point, 2 hours, through 1 year, and dose-related, approximately seven- to eight-fold greater in the 2-mg implant. Concentrations of FA were generally higher in the vitreous (11-18 and 75-146 ng/g) and retina (42-87 and 224-489 ng/g) than in the aqueous humor (0.21-1.1 and 2.6-13.0 ng/g) for the 0.5- and 2-mg implants, respectively. Urine and plasma values were below the lower limit of quantitation (200 pg/mL) for all observations, indicating no evidence of systemic absorption. CONCLUSIONS: In this rabbit study, the Retisert provides relatively constant levels of FA in the posterior pole, which is consistent with previous reports of its clinical utility.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15279731&dopt=Abstract fluocinolone Synalar



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Comparative evaluation of skin atrophy in man induced by topical corticoids.

Jablonska S, Groniowska M, Dabroswki J.

In this in-patient study, mild skin atrophy was observed clinically in 6 out of a total of 22 patients after fluocinolone acetonide and in one patient after flumethasone pivalate ointment applications (P less than 0,05). Investigations were discontinued prematurely on days 14 and 17 in 2 patients because they developed early atrophy due to fluocinolone acetonide applications. Histological findings indicating either moderate or marked skin atrophy were evident in 15 patients after flucinolone acetonide as against one patient after flumethasone pivalate ointment applications (P less than 0.001). In comparison with the controls the mean decrease in epidermal thickness was more marked after fluocinolone acetonide applications, namely 30.5% vs 21.3% after flumethasone pivalate applications. The ultrastructural tissue changes were less marked at the sites to which flumethasone pivalate was applied. In comparison with controls, the percentages of mean decrease in diameters of collagen fibrils measured in six volunteer patients ranged from 5.1% to 27.6% after fluocinolone acetonide and from 0% to 12.3% following flumethasone pivalate ointment applications, This difference was statistically significant (range P less than 0,01 to less than 0.001). This experimental study has demonstrated that flumethasone pivalate displays only a mild atrophogenic effect and it is clinically and histologically significantly less atrophogenic than fluocinolone acetonide. Flumethasone pivalate can therefore be reckoned as a suitable topical corticosteroid especially for the long-term treatment of corticoid-responsive dermatoses.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=154921&dopt=Abstract fluocinolone Synalar



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Photochemistry and Phototoxicity of Fluocinolone 16,17-Acetonide.

Miolo G, Caffieri S, Dalzoppo D, Ricci A, Fasani E, Albini A.

University of Padova.

Fluocinolone 16,17-acetonide is a corticosteroid used topically to treat various inflammatory skin diseases. Its photoreactivity was studied under UVA and UVB light in aqueous buffer in the presence of oxygen. This drug is photolabile under UVB light and, to a lesser extent, under UVA light, which is absorbed far less. In phosphate buffer, about 80% of fluocinolone acetonide decomposes after 5 J/cm(2) of UVB irradiation, whereas under 30 J/cm(2) of UVA light only about 20% decomposes. Both the drug and its photoproducts have been evaluated through a battery of in vitro studies and found to cause photohemolysis and induce photodamage to proteins (erytrocyte ghosts, BSA) and linoleic acid. In addition, one of the photoproducts (the 17-hydroperoxy derivative) is highly toxic in the dark. Therefore, both loss of therapeutic activity and light-induced adverse effects may be expected when patients expose themselves to sunlight after drug administration. A major mechanism for phototoxicity involves radicals forming from drug breakdown, at least under UVB, although ROS may play a role, particularly under UVA.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15535735&dopt=Abstract fluocinolone Synalar