Fluocinolone acetonide
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| Clinical data | |
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| Trade names | Synalar, Iluvien, others |
| AHFS/Drugs.com | Monograph Monograph |
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| Routes of administration | Topical, ophthalmic intravitreal injection |
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| Pharmacokinetic data | |
| Metabolism | Liver, CYP3A4-mediated |
| Elimination half-life | 1.3 to 1.7 hours |
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| ECHA InfoCard | 100.000.607 |
| Chemical and physical data | |
| Formula | C24H30F2O6 |
| Molar mass | 452.495 g·mol−1 |
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Fluocinolone acetonide is a corticosteroid primarily used in dermatology to reduce skin inflammation and relieve itching.[citation needed] It is a synthetic hydrocortisone derivative. The fluorine substitution at position 9 in the steroid nucleus greatly enhances its activity. It was first synthesized in 1959 in the Research Department of Syntex Laboratories S.A. Mexico City.[2] Preparations containing it were first marketed under the name Synalar. A typical dosage strength used in dermatology is 0.01–0.025%. One such cream is sold under the brand name Flucort-N and includes the antibiotic neomycin.
Fluocinolone acetonide was also found to strongly potentiate TGF-β-associated chondrogenesis of bone marrow mesenchymal stem/progenitor cells, by increasing the levels of collagen type II by more than 100 fold compared to the widely used dexamethasone.[3]
Fluocinolone acetonide intravitreal implants have been used to treat non-infectious uveitis. A systematic review could not determine whether fluocinolone acetonide implants are superior to standard of care treatment for uveitis.[4] A fluocinolone acetonide intravitreal implant with the brand name Iluvien is sold by biopharmaceutical company Alimera Sciences to treat diabetic macular edema (DME).[5]
It was approved for medical use in 1961.[6]
Classification
Fluocinolone is a group V (0.025%) or group VI (0.01%) corticosteroid under US classification.
See also
References
- ^ "Regulatory Decision Summary for Iluvien". Drug and Health Product Portal. Health Canada. 23 October 2014.
- ^ Mills JS, Bowers A, Djerassi C, Ringold HJ (1960). "Steroids CXXXVII. Synthesis of a New Class of Potent Cortical Hormones. 6α,9α-Difluoro-16α-Hydroxyprednisolone and its Acetonide". Journal of the American Chemical Society. 80 (13): 3399–3404. doi:10.1021/ja01498a041.
- ^ Hara ES, Ono M, Pham HT, Sonoyama W, Kubota S, Takigawa M, et al. (September 2015). "Fluocinolone Acetonide Is a Potent Synergistic Factor of TGF-β3-Associated Chondrogenesis of Bone Marrow-Derived Mesenchymal Stem Cells for Articular Surface Regeneration". Journal of Bone and Mineral Research. 30 (9): 1585–1596. doi:10.1002/jbmr.2502. PMC 5569386. PMID 25753754.
- ^ Brady CJ, Villanti AC, Law HA, Rahimy E, Reddy R, Sieving PC, et al. (February 2016). "Corticosteroid implants for chronic non-infectious uveitis". The Cochrane Database of Systematic Reviews. 2016 (2): CD010469. doi:10.1002/14651858.CD010469.pub2. PMC 5038923. PMID 26866343.
- ^ "Real-world study shows long-term safety, efficacy of Iluvien in DME". Healio. 2020-07-02. Retrieved 2020-10-28.
- ^ Fischer J, Ganellin CR, eds. (2006). "Tables of Structural and Functional Analogues: Systemic Hormonal Preparations". Analogue-based Drug Discovery. John Wiley & Sons. p. 485. ISBN 9783527607495.
External links
- "Fluocinolone acetonide". Drug Information Portal. U.S. National Library of Medicine.
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