Fluocinolone/hydroquinone/tretinoin
| Combination of | |
|---|---|
| Fluocinolone acetonide | Corticosteroid |
| Hydroquinone | Bleaching agent |
| Tretinoin | Vitamin A derivative |
| Clinical data | |
| Trade names | Tri-Luma (US),Fumeida (CN) |
| Routes of administration | Topical (cream) |
| Legal status | |
| Legal status |
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| Identifiers | |
| CAS Number | |
| ChemSpider |
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| KEGG | |
The cream containing the drug combination fluocinolone acetonide/hydroquinone/tretinoin (trade name Tri-Luma) is used for the treatment of melasma (dark skin patches).It is marketed by Galderma.[1][2] In China, this generic drug with the same ingredients is sold under the trade name "Fumeida® （孚美达®乳膏）"[3] [4]and exclusively manufactured and marketed by Zhejiang Fonow Medicine Co., Ltd.（浙江孚诺药业股份有限公司）[5]
Medical uses
[edit]Fluocinolone acetonide (0.01%)/Hydroquinone (4%)/ Tretinoin (0.05%) Cream is indicated for the short-term (up to 8 weeks) treatment of moderate to severe melasma of the face in the presence of measures for sun avoidance, including the use of sunscreens. [6] Tri-Luma is the only FDA-approved drug containing hydroquinone,[7] a prescription product approved for the short-term treatment of dark spots associated with moderate-to-severe melasma of the face. FA+HQ+RA is effective in patients of all races/ethnicities and Fitzpatrick skin types.[8]
Side effects
[edit]Some patients may have very severe allergic reactions to Tri-Luma Cream due to the sulfites contained in the product. In some cases, these allergic reactions may result in severe asthma attacks, which can be life threatening. While you use Tri-Luma Cream, your skin may develop mild-to-moderate redness, peeling, burning, dryness, or itching.
Tri-Luma Cream contains a corticosteroid medicine as one of its active components. The following side effects have been reported with application of corticosteroid medicines to the skin: itching, irritation, dryness, infection of the hair follicle, acne, changes in skin color, inflammation around the mouth, allergic skin reaction, skin infection, skin thinning, stretch marks and sweat problems. In addition, Tri-Luma Cream contains a corticosteroid that may produce reversible effects on the adrenal gland called hypothalamic-pituitary-adrenal (HPA) axis suppression, so tell your doctor if you have any condition that may affect your adrenal function, such as Addison’s disease. Some patients using Tri-Luma Cream develop dark spots on their skin, tingling, increased skin sensitivity, rash, acne, skin redness caused by a condition called rosacea, skin bumps, blisters, or tiny red lines or blood vessels showing through the skin. Tri-Luma Cream may also cause a gradual blue-black darkening of your skin.[9]
The most common side effects ：[10]
• redness
• dryness
• peeling
• itching
• burning
• acne
Active ingredients
[edit]Hydroquinone
Several hypotheses exist to explain the action of hydroquinone in skin lightening.It may interrupt one or more steps in thetyrosine-tyrosinase pathway of melanin synthesis,thus inhibit-ing the conversion of tyrosine to melanin.It compromises the formation of melanosomes and destroys the membranous structures of melanocytes,which results in their degradation.It has also been shown that hydroquinone affects fundamental aspects of cellular metabolism and that melanocytes are partic-ularly vulnerable.Hydroquinone may be oxidized by tyrosi-nase to form toxic compounds.Even low concentrations can cause decreases in DNA and RNA synthesis in melanotic cells.
Tretinoin
Tretinoin (retinoic acid)causes dispersion of pigment granules in keratinocytes,interferes with pigment transfer,and acceler-ates epidermal transfer,thus causing pigment to be lost more rapidly.Tretinoin also accelerates epidermal turnover,shorten-ing the "transit time"from the basal layer and accelerating pig-ment loss.Retinoic acid reduces epidermal melanin,possibly by decreasing the rate of transfer of melanosomes to ker-atinocytes,secondary to an increase in epidermal proliferation and tyrosinase inhibition and a resultant reduction in melano-genesis.
Corticosteroid
Corticosteroids have anti-metabolic effects on many cell sys-tems.They are cytotoxic or cytostatic for the epidermis anddecrease epidermal turnover.[11]
History
[edit]Kligman formula consisting of 0.1% tretinoin, 5.0% hydroquinone, 0.1% dexamethasone, and hydrophilic ointment.[12] The dermatologist gold-standard formula for treating hyperpigmentation is the Kligman formula, a prescription named after its inventor, dermatologist Dr. Albert Kilgman. It was originally formulated in 1975 and has remained the most effective topical treatment formula for fading dark spots ever since. [13]
References
[edit]- ^ Drugs.com: Tri-Luma
- ^ Tri-Luma prescribing information
- ^ "Fumeida cream(孚美达乳膏)".
- ^ "Fluocinolone acetonide hydroquinone and tretinoin cream (氟轻松氢醌维A酸乳膏)". National Medical Products Administration, China.
- ^ "Zhejiang Fonow Medicine Co., Ltd. (浙江孚诺医药股份有限公司)".
- ^ "TRI-LUMA (fluocinolone acetonide 0.01%, hydroquinone 4%, tretinoin 0.05%) Cream [Prescribing Information]. Dallas, TX: Galderma Laboratories, L.P.; 2014".
- ^ "FDA works to protect consumers from potentially harmful OTC skin lightening products".
- ^ "R Balkrishnan, A P Kelly, A McMichael, H Torok. Improved quality of life with effective treatment of facial melasma: the pigment trial. J Drugs Dermatol. 2004 Jul-Aug;3(4):377-81.PMID: 15303781".
- ^ "Prescription Melasma Treatment".
- ^ "TRI-LUMA (fluocinolone acetonide 0.01%, hydroquinone 4%, tretinoin 0.05%) Cream [Prescribing Information]. Dallas, TX: Galderma Laboratories, L.P.; 2014" (PDF).
- ^ "Alan Menter Rationale for the use of topical corticosteroids in melasma J Drugs Dermatol. 2004 Mar-Apr;3(2):169-74".
- ^ "Kligman AM, Willis I. A new formula for depigmenting human skin. Arch Dermatol. 1975;111:40–8".
- ^ "What is the Kligman formula? Does it help fade dark spots?".
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