Postinflammatory Hyperpigmentation Medication

Updated: Jun 13, 2023
  • Author: Robert A Schwartz, MD, MPH; Chief Editor: Dirk M Elston, MD  more...
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Medication

Medication Summary

Topical treatments include hydroquinone, azelaic acid, corticosteroids, tretinoin cream, GA, and trichloroacetic acid. [38] Skin whitening products are used for clinical treatment of postinflammatory hyperpigmentation. [39] They act at various levels of melanin production in the skin, some being competitive inhibitors of tyrosinase, while others inhibit the maturation of this enzyme or the transport of melanosomes from melanocytes to surrounding keratinocytes. Soy products containing serine protease inhibitors appear to have potential as a therapeutic option for the treatment of hyperpigmentation. [40] Postinflammatory hyperpigmentation has also been treated using vitamin C with a full-face iontophoresis mask and a mandelic/malic acid skin care regimen. [41] Extracts of the tropical fern Polypodium leucotomos given orally may be beneficial as an adjunctive approach. [42] Wide-spectrum sunscreens are an integral part of any treatment regimen.

Some prefer topical retinoids unless contraindicated, recognizing that novel formulations or application of commonly recommended moisturizers may help reduce irritation, and that retinoids can be combined with other topical agents and procedures such as superficial chemical peels to improve hyperpigmentation. [43]

Winhoven et al reported successful therapy with oral isotretinoin in an Asian patient. [44] Combined therapy using Q-switched ruby laser and cutaneous bleaching with tretinoin and hydroquinone may be used for periorbital skin hyperpigmentation in selected patients. [45] The efficacy and safety retinoids and azelaic acid in individuals with a dark complexion has been demonstrated. [46]  Topical cysteamine 5% cream is also another option. [47]

The combination of treatment with a low-fluence Q-switched 1064-nm Nd:YAG laser and a topical mixture of tranexamic acid, niacinamide, and kojic acid would seem beneficial for melasma. [48]  Kojic acid has become a popular option for hyperpigmentation and melasma, available in over-the-counter skincare products. [49]  Other common cosmeceuticals similarly employed as primary, adjunctive, or maintenance treatment for pigmentary disorders include licorice extract, niacinamide, azelaic acid, and hydroxyacids such as lactic, glycolic, and salicylic acid. [50]

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Depigmenting Agents

Class Summary

These agents are used for gradual bleaching of hyperpigmented skin.

Hydroquinone (Alphaquin HP, Eldopaque Forte, Nuquin HP)

Hydroquinone is a 1,4-benzenediol that suppresses melanocyte metabolic processes, especially enzymatic oxidation of tyrosine to 3,4-dihydroxyphenylamine. Exposure to the sun reverses the effects and causes repigmentation.

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Acne Agents, Topical

Class Summary

Acne products are used for their antibacterial and comedolytic properties and some may have bleaching effects.

Azelaic acid (Azelex, Finacea)

Azelaic acid may have bleaching effects on the skin. Also, it may have an antimicrobial effect.

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Keratolytic Agents

Class Summary

These agents cause cornified epithelium to swell and soften and then become macerated and desquamated.

Trichloroacetic acid topical (Tri-Chlor)

Trichloroacetic acid cauterizes skin, keratin, and other tissues. Trichloroacetic acid is a highly corrosive desiccating agent that cauterizes skin, keratin, and other tissues and is used to burn lesions. Although it is caustic, it causes less local irritation and systemic toxicity than other agents in the same class.

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Retinoid-Like Agents

Class Summary

Retinoids decrease the cohesiveness of abnormal hyperproliferative keratinocytes and modulate keratinocyte differentiation.

Tretinoin topical (Avita, Renova, Retin-A)

Tretinoin inhibits microcomedo formation and eliminates lesions. It makes keratinocytes in sebaceous follicles less adherent and easier to remove. Tretinoin topical is available as 0.025%, 0.05%, and 0.1% creams and 0.01% and 0.025% gels.

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Corticosteroids

Class Summary

These drugs have anti-inflammatory properties and cause profound and varied metabolic effects. Corticosteroids modify the body's immune response to diverse stimuli.

Hydrocortisone topical (Cortaid, Cortizone, Westcort)

Hydrocortisone topical is an adrenocorticosteroid derivative suitable for application to skin or external mucous membranes. It has mineralocorticoid and glucocorticoid effects, resulting in anti-inflammatory activity.

Desonide (DesOwen, LoKara)

Desonide stimulates the synthesis of enzymes that decrease inflammation. It suppresses mitotic activity and causes vasoconstriction.

Betamethasone topical (Celestone Diprolene, Luxiq)

Betamethasone decreases inflammation by suppressing the migration of polymorphonuclear leukocytes and reversing increased capillary permeability.

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