Hyperpigmentation: From Dark Spots to Even Tone

Hyperpigmentation is one of the most common skin concerns, but effective treatment requires understanding the different types and their unique mechanisms.

Melasma

Causes

Hormonal trigger: Estrogen → MSH → tyrosinase activation

UV-induced: VEGF, stem cell factor, Wnt signaling → melanocyte hyperactivity

Key Facts

No cure: Requires continuous management

More common in women and darker skin tones

Often appears during pregnancy or with hormonal contraceptives

Treatment Approach

Strict photoprotection (SPF 50+, reapply frequently)

Tyrosinase inhibitors

Anti-inflammatory agents

Traditional triple therapy: hydroquinone + tretinoin + corticosteroid

Tranexamic acid emerging as equally effective with better safety profile

Post-Inflammatory Hyperpigmentation (PIH)

Mechanism

Inflammation → cytokines/prostaglandins/ROS → melanocyte stimulation

Two Types

Prevention

Treat inflammation early

Minimize picking or trauma

Sunscreen is essential

Evidence-Based Brightening Agents

Hydroquinone (98.4% dermatologist agreement—highest rated)

Most effective but controversial

2-4% concentration

Prescription typically limited to 3-6 months (ochronosis risk)

Tranexamic Acid (87.1% dermatologist agreement)

Mechanism: Blocks plasminogen-keratinocyte bonding → inhibits tyrosinase

Forms: 3% topical, oral (250-500mg)

Evidence: Equal efficacy to hydroquinone for melasma with fewer side effects

Additional benefits: barrier strengthening, UV protection enhancement

Kojic Acid (93.6% dermatologist agreement)

Fungal metabolite

Most potent tyrosinase inhibitor tested: IC₅₀ = 70 µM

Mixed-type inhibitor (chelates copper in tyrosinase active site)

Alpha Arbutin

Natural hydroquinone derivative from bearberry

More stable, gentler mechanism

Safe for long-term use

Works well with niacinamide, vitamin C, AHAs

Azelaic Acid (88.7% dermatologist agreement)

Unique advantage: Doesn't affect normal melanocytes, only hyperactive ones

Won't lighten normal skin around lesions

Safe for pregnancy

Vitamin C (87.1% dermatologist agreement)

Tyrosinase inhibitor and antioxidant

Multiple mechanisms for brightening

Best at 10-20% concentration

Niacinamide (79% dermatologist agreement)

Inhibits melanosome transfer

2-5% concentration

Excellent for combination therapy

Licorice Extract (Glycyrrhiza glabra)

Key active: Glabridin

Multi-benefit: brightening + anti-inflammatory + antioxidant

Gentle enough for sensitive skin

Treatment Algorithm

First-line: Combination topical therapy + broad-spectrum SPF 50+

Second-line: Superficial chemical peels, low-fluence lasers

Third-line: Fractional RF, Q-switched/picosecond lasers (caution: can worsen)

Critical: Any inflammation or irritation can worsen hyperpigmentation in darker skin tones—a gentle, consistent approach is essential.

Sample Hyperpigmentation Routine

Morning

Gentle cleanser

Vitamin C serum

Tranexamic acid

Sunscreen SPF 50+

Evening

Gentle cleanser

Alpha arbutin serum

Niacinamide

Retinoid (2-3x/week)

Moisturizer

The Bottom Line

Treating hyperpigmentation requires patience, consistency, and rigorous sun protection. Multiple mechanisms work better than single agents, and realistic timelines (months to years) help set appropriate expectations.