Tazarotene
Tazarotene
Generic Name
Tazarotene
Mechanism
Tazarotene selectively binds to retinaldehyde‑responsive nuclear receptors:
• RAR‑α & RAR‑β → up‑regulation of genes involved in keratinocyte differentiation and down‑regulation of genes promoting proliferation.
• Reduced keratinocyte hyperproliferation → normalization of epidermal turnover.
• Anti‑inflammatory effects via inhibition of pro‑inflammatory cytokines (TNF‑α, IL‑1β).
• Modulation of lipid metabolism → restoration of barrier function and reduction of comedogenesis in acne.
The net result is a decrease in follicular plugging, inflammation, and plaque formation.
Pharmacokinetics
- Absorption: Primarily dermal; systemic absorption is minimal (< 0.1 % of applied dose).
- Distribution: Retained in epidermal layers; negligible plasma levels.
- Metabolism: Hepatic oxidation primarily via CYP2C9 and CYP2C19; minor metabolites with reduced potency.
- Elimination: Excreted mainly in feces; half‑life in plasma ~3–4 h (if measurable).
- Drug interactions: Co‑administration with strong CYP2C9 inhibitors/inducers (e.g., fluconazole, rifampin) may alter local metabolism but generally has no clinically significant effect due to limited systemic exposure.
Indications
- Acne vulgaris: Mild‑to‑moderate lesions in adolescents and adults.
- Plaque psoriasis: Hand, foot, and body plaques; commonly used as monotherapy or Additive second‑line to topical corticosteroids.
- Actinic keratosis: Long‑term therapy (up to 1 yr) to minimize recurrence.
- Chronic plaque psoriasis: Maintenance doses after initial improvement.
Contraindications
- Pregnancy/Lactation: Category X; contraindicated.
- Children under 12: Limited data; use with caution.
- Known hypersensitivity: to retinoids or any component.
- Concurrent use of other retinoids: Avoid overlapping applications to reduce irritation.
- Photosensitivity: Patients must practice strict sun avoidance and use broad‑spectrum sunscreen daily.
- Skin trauma or burns: Do not apply to sites of dermatitis, eczema, or dermabrasion.
Warnings
• Severe dermatitis, ocular irritation (especially near eye margins).
• Potential for abnormal lipid profile if systemic absorption occurs (rare).
• Discontinue if severe irritation develops; may require short course of topical corticosteroid.
Dosing
| Indication | Product | Typical Dose | Frequency | Notes |
| Acne vulgaris | 0.05 % gel | Apply 2–3 cm² of gel to affected areas nightly | Once daily | May start with every other night to reduce irritation; increase to nightly once tolerated. |
| Plaque psoriasis | 0.1 % gel | Apply 2–3 cm² to lesions | 2× daily for first 4 weeks, then once daily as maintenance | Avoid hair follicles or nail beds to prevent irritation. |
| Actinic keratosis | 0.05 % cream | Apply 2–3 cm² to lesions | Twice every other week (Or 1 × per week) | Ensure drying time before covering; use protective clothing. |
• Application: Wash hands after application; allow absorbance (30–60 min) before covering or adding other topical agents.
• Micropore ABC: Do not apply under occlusive dressings unless prescribed.
Adverse Effects
Common (≥10 % incidence)
• Dryness, peeling, scaling (most pronounced with 0.1 % gel).
• Irritant dermatitis (erythema, pruritus).
• Photosensitivity (rash, sunburn).
• Turbid or brown discoloration of eyelids when applied near eye area.
Serious (≤1 % incidence)
• Severe dermatitis or contact allergy.
• Eyelid pruritus leading to ocular irritation; requires immediate ophthalmology review.
• Rare systemic retinoid toxicity (gastrointestinal, hepatic) although unlikely with topical use.
Monitoring
| Parameter | Frequency | Reason |
| Skin tolerance | At each visit (0–4 wk, then every 3 mo) | Adjust dose or schedule. |
| Pregnancy test | Prior to initiation if female of childbearing potential | Avoid teratogenic exposure. |
| Lipid panel | Baseline and >3 mo if systemic exposure suspected | Monitor for hyperlipidemia. |
| Visual assessment | If topical application near eyelids | Detect early ocular irritation. |
No routine laboratory monitoring required for most patients.
Clinical Pearls
1. Start low, go slow – titrate from every‑other‑night to nightly dosing to minimize irritation, especially for 0.1 % gel.
2. Combine with topical corticosteroids only for short bursts (≤7 days) to cover acute flare; avoid chronic steroid‑retinoid combination to prevent skin atrophy.
3. Photoprotection is critical – prescribe broad‑spectrum SPF ≥30 sunscreen and advise avoidance of peak UV hours.
4. Avoid application to alopecia or shaved areas unless supervision – itching and bleaching of hair pigment may occur.
5. Use fragrance‑free, para‑phenylenediamine‑free formulations for patients with sensitive skin to reduce dermatitis.
6. For actinic keratosis, schedule follow‑up after 3–6 months to assess lesion clearance and reduce cumulative exposure.
7. Counsel patients on the potential for temporary darkening of stratum corneum – it does not indicate worsening disease.
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• Tazarotene remains a cornerstone of topical dermatologic therapy when applied with judicious dosing, patient education, and vigilance for irritation or photosensitivity.