Topical Agents Used in the Management of Hyperpigmentation

R. M. Halder, MD; G. M. Richards, MD


Skin Therapy Letter. 2004;9(6) 

In This Article

Topical Retinoids

The efficacy of topical tretinoin 0.05-0.1% as monotherapy for postinflammatory hyperpigmentation has been reported.[16] Tretinoin was also used as monotherapy in a study on 38 African-American patients with melasma and 68%-73% of patients improved. In 88% of the patients, moderate side-effects of desquamation and erythema were observed.[17,18] Darker skinned patients who develop a dermatitis from tretinoin may develop postinflammatory hyperpigmentation secondary to the dermatitis.

The mechanism of action of tretinoin in the treatment of melasma is poorly understood. Clinical improvement has been found to be associated with a reduction in epidermal melanin, possibly as a result of the inhibition of tyrosinase by the action of tretinoin.[19]

Although tretinoin can be effective as monotherapy for hyperpigmentation and melasma, it requires 20 to 40-week treatment periods. Tretinoin can also be used in conjunction with hydroquinone or other depigmenting agents to improve efficacy. The first published study of combination therapy used tretinoin 0.1%, hydroquinone 5%, and dexamethasone 0.1% for postinflammatory hyperpigmentation.[20] Tretinoin was shown to reduce the atrophy of the corticosteroid and facilitated the epidermal penetration of the hydroquinone. The tretinoin-induced irritation was reduced by the corticosteroid. The first triple combination topical therapy approved by the US FDA for melasma is a modified formulation comprising fluocinolone acetonide, hydroquinone 4% and tretinoin 0.05%. In studies of patients with melasma, 78% had complete or near clearing after 8 weeks of therapy. Similar results and favorable safety profile were seen in a 12-month study.[21]

In a randomized clinical trial, the efficacy of adapalene 0.1% was found to be comparable to that of tretrinoin 0.05% cream in the treatment of melasma (mainly epidermal type). The results showed fewer side-effects and greater acceptability among patients using adapalene.[19]

The treatment of hyperpigmentation disorders can be a long process. The psychosocial impact of these disorders should be taken into consideration. There are several topical treatment options available, the most common of which is hydroquinone. The use of combination therapy and monotherapy with non-phenolic agents is increasingly common. These treatment options are primarily for epidermal disorders of hyperpigmentation. Dermal disorders of hyperpigmentation are difficult to treat, and have not been effectively managed using currently available therapy.


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