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Hydroquinone inhibits tyrosinase — the rate-limiting enzyme in melanin synthesis — reducing melanin production in existing melanocytes. At prescription concentrations, it also mildly inhibits melanocyte proliferation and accelerates melanin degradation.
OTC hydroquinone is limited to 2%. Prescription 4% is available commercially but at $100+/month. Compounding allows concentrations from 4–10%, custom Kligman’s Formula (hydroquinone + tretinoin + corticosteroid), and novel combination formulas at substantially lower cost.
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Hydroquinone has been the FDA standard for prescription skin lightening for over 50 years. At 4–10%, it is more effective than any other single depigmenting agent available.
The most powerful application of compounded hydroquinone is Kligman’s Formula — a combination of hydroquinone (5%), tretinoin (0.1%), and a corticosteroid (dexamethasone 0.1% or fluocinolone 0.01%). This triple-combination addresses melanin synthesis, cell turnover, and inflammation simultaneously, producing faster results for melasma than any monotherapy.
Melasma (primary indication), post-inflammatory hyperpigmentation, solar lentigos (sun spots), freckles, café au lait spots
4% cream: Apply to affected area twice daily; avoid normal skin
Kligman’s Formula: Apply once nightly to affected area; always use SPF in AM
Continuous use limited to 5–6 months; follow with maintenance therapy
Irritation, dryness, mild erythema at application site. Ochronosis (rare, irreversible skin darkening) with prolonged high-dose use. Never use >6 months continuously.
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