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


Hydroquinone, which is a hydroxyphenolic chemical, has been the gold standard for treatment of hyperpigmentation for over 50 years. It acts by inhibiting the enzyme tyrosinase, thereby reducing the conversion of DOPA to melanin. Some of the other possible mechanisms of action are the destruction of melanocytes, degradation of melanosomes, and the inhibition of the synthesis of DNA and RNA.[2]

Hydroquinone can be compounded into 5%-10% concentrations, but at these strengths, may be irritating and unstable. The 2% concentrations of hydroquinone available over the counter in the US and Canada are not as efficacious as the 3% and 4% prescription formulations, as their onset of action is later than with the higher concentrations. Antioxidants, such as vitamin C and retinoids, as well as alpha-hydroxy acids may be used as additives to increase penetration and enhance efficacy. Exogenous ochronosis with the use of hydroquinone has been reported in dark-skinned patients, in particular South African women who frequently use very high concentrations of hydroquinone over large surface areas.[3] Although hydroquinone is used extensively in North America, there have only been about 30 reported cases of exogenous ochronosis from hydroquinone use in North America.

Adverse reactions from hydroquinone use include irritant and allergic contact dermatitis, and nail discoloration. Postinflammatory hyperpigmentation may occur from the contact dermatitis. Hypopigmentation of the normal skin surrounding the treated areas may also occur. These usually resolve with the discontinuation of the hydroquinone treatment.[2]


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