Melasma Medication

Updated: Apr 27, 2020
  • Author: Willis Hughes Lyford, MD; Chief Editor: William D James, MD  more...
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Medication Summary

The goals of pharmacotherapy are to reduce morbidity and prevent complications.


Depigmenting agents

Class Summary

These agents inhibit key enzymes involved in melanin synthesis.

Hydroquinone (Claripel cream with sunscreens)

Hydroquinone produces reversible depigmentation of skin by inhibiting enzymatic oxidation of tyrosine to 3-(3,4-dihydroxyphenyl-alanine [dopa]) and suppression of other melanocyte metabolic processes. Exposure to sunlight or UV light causes repigmentation, which may be prevented by the broad-spectrum sunscreen agents contained in this product.


Brand names include Alphaquin HP, Alustra, Eldopaque, Eldopaque Forte, Eldoquin, Eldoquin Forte, Esoterica, Esoterica Sensitive Skin, Glyquin, Glyquin-XM, Lustra, Melanex, Melanol, Melpaque HP, Melquin HP, Melquin-3, Nuquin HP, Solaquin, Solaquin Forte, and Viquin Forte. Hydroquinone suppresses melanocyte metabolic processes, especially enzymatic oxidation of tyrosine to 3,4-dihydroxyphenylamine. Exposure to sun reverses effects and causes repigmentation. It lightens healthy and hyperpigmented skin.


Antibiotic agents

Class Summary

These agents inhibit DNA synthesis and mitochondrial enzymes to interrupt hyperactive melanocytes. Normally functioning melanocytes are not inhibited.

Azelaic acid (Azelex) Cream 20%

Azelaic acid may decrease microcomedo formation. It may have a bleaching effect on skin. It may also have an antimicrobial effect.



Class Summary

These agents regulate cell growth and proliferation.

Tretinoin topical (Avita, Retin-A)

Topical tretinoin inhibits microcomedo formation and eliminates lesions. It makes keratinocytes in sebaceous follicles less adherent and easier to remove. Dosage formulations include 0.025%, 0.05%, and 0.1% cream; 0.01%, 0.025%, and 0.1% gel; and 0.05% solution.

Adapalene (Differin)

Adapalene binds to specific retinoic-acid nuclear receptors and modulates cellular differentiation, keratinization, and inflammatory processes.


Antifibrinolytic Agents

Tranexamic acid oral (Lysteda)

Tranexamic acid oral is an antifibrinolytic; it is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure.