Hydroquinone
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Hydroquinone
Lustra, EpiQuin Micro, Melquin, Tri-Luma (with tretinoin and fluocinolone)
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Summary
Common uses
Melasma0, Post-inflammatory hyperpigmentation0, Ephelides/lentigines (selected)0
Pharmacy
Starting dose
Apply thin layer to hyperpigmented areas BID; limit to 4-6 month courses to avoid ochronosis
Preparations
4% prescription cream/lotion; OTC 2% withdrawn in US (2020 CARES Act); compounded higher strengths available
US FDA Max
4% topical; limit duration of use
Pharmacology
Routes
Topical
Onset
Visible lightening at 4-12 weeks
Duration
Hours per application
Half-life
Not meaningfully described — topical local action with minimal systemic absorption[1]
Bioavailability
Topical with limited but measurable systemic absorption[1]
Pregnancy
Generally avoided in pregnancy.[citation needed]
Legal status
Rx-only in US since 2020 (OTC 2% formulations withdrawn under CARES Act due to safety concerns)
Purported mechanism
Hydroquinone inhibits tyrosinase, the rate-limiting enzyme converting tyrosine to melanin in melanocytes; reduced melanin synthesis lightens hyperpigmented skin over weeks.0 Exogenous ochronosis (paradoxical blue-black hyperpigmentation, irreversible) is the most-feared adverse effect of prolonged use and the basis for the typical 4-month course limit. Combination with tretinoin and a low-potency steroid (Kligman formula, marketed as Tri-Luma) is more effective than monotherapy for melasma[1].
References
edit- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Tri-Luma (fluocinolone, hydroquinone, tretinoin), Galderma, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021112s016lbl.pdf