Tazarotene

Allopathic
Indications

Approved Indications:

  • Acne Vulgaris: Topical treatment of acne vulgaris, particularly comedonal and inflammatory types, in patients ≥12 years old.
  • Plaque Psoriasis: Treatment of stable plaque psoriasis of up to 20% body surface area involvement in adults.
  • Facial Fine Wrinkling, Mottled Hyper/Hypopigmentation, and Tactile Roughness (Adjunctive Use): For patients seeking improvement in photodamaged skin (in cream form, U.S. FDA-approved).

Off-Label or Clinically Accepted Uses:

  • Keratotic Skin Disorders: Occasionally used for conditions like ichthyosis or Darier disease.
  • Other Psoriatic Variants: May be used under specialist supervision in palmoplantar psoriasis or guttate psoriasis, though not formally approved.
  • Photoaging: Topical application for cosmetic improvement of skin tone and texture, though this is primarily a cosmetic benefit.
Dosage & Administration

General Administration:

  • Formulations: Cream, gel, foam – available in 0.05%, 0.1%, and 0.045% (foam).
  • Route: Topical only. For external use.

Adults:

  • Psoriasis: Apply a thin film of 0.05% or 0.1% gel or cream once daily in the evening to affected areas.
  • Acne: Apply a thin layer of 0.1% or 0.045% foam once daily in the evening.
  • Photodamage: 0.1% cream once daily in the evening.

Pediatric Use (≥12 years):

  • Acne: Apply 0.1% foam or gel once daily. Not recommended for children <12 years.

Elderly:

  • Use with standard adult dosing unless significant dermal atrophy or fragility is present.

Renal/Hepatic Impairment:

  • No dose adjustment necessary due to minimal systemic absorption.

Administration Notes:

  • Apply to clean, dry skin.
  • Avoid eyes, mouth, mucous membranes, and broken skin.
  • Use moisturizer to minimize irritation.
  • Sunscreen (SPF 15 or higher) is essential during treatment.
Mechanism of Action (MOA)

Tazarotene is a third-generation topical retinoid and a prodrug that is rapidly converted to its active form, tazarotenic acid. It selectively binds to retinoic acid receptors (RAR-β and RAR-γ) within keratinocytes. By modulating gene expression, it normalizes keratinocyte differentiation, reduces hyperproliferation, and exhibits anti-inflammatory effects. This mechanism is key to its efficacy in acne (by decreasing comedogenesis and inflammation) and psoriasis (by reducing plaque formation and epidermal thickness).

Pharmacokinetics
  • Absorption: Minimal systemic absorption (~1–5%); increases if applied over large areas or broken skin.
  • Distribution: High local tissue concentration; limited systemic distribution.
  • Metabolism: Rapidly hydrolyzed in the skin to active tazarotenic acid; further metabolized by hepatic oxidative pathways.
  • Elimination: Excreted mainly via urine and feces as inactive metabolites.
  • Half-life: ~18 hours (tazarotenic acid).
Pregnancy Category & Lactation
  • Pregnancy: Category X (U.S. FDA). Contraindicated during pregnancy due to teratogenic effects observed in animal studies.
  • Lactation: Not recommended. Although systemic absorption is low, the potential for adverse effects on the infant cannot be excluded.
  • Recommendation: Use effective contraception in women of childbearing potential during and for some time after treatment. Do not use during pregnancy or while breastfeeding.
Therapeutic Class
  • Primary Class: Topical Retinoid
  • Subclass: Third-generation acetylenic retinoid
Contraindications
  • Known hypersensitivity to tazarotene or any formulation components
  • Pregnancy (Category X)
  • Eczema or skin abrasion at the application site
  • Concurrent use on sunburned skin
Warnings & Precautions
  • Photosensitivity: Increases risk of sunburn; strict photoprotection required.
  • Skin Irritation: Erythema, peeling, burning, and dryness may occur. Consider alternate-day dosing or moisturizer use.
  • Pregnancy: Absolute contraindication. Require negative pregnancy test before starting and effective contraception during use.
  • Avoid Occlusion: Do not apply under occlusive dressings to prevent enhanced absorption.
  • Concomitant Topicals: Avoid using with alcohol-based, astringent, or abrasive skin products.
Side Effects

Common (≥10%):

  • Skin irritation (burning, stinging, redness, peeling)
  • Dryness
  • Erythema
  • Pruritus

Less Common (1–10%):

  • Desquamation
  • Photosensitivity reactions
  • Rash
  • Worsening of psoriasis (initial flaring)

Rare but Serious (<1%):

  • Severe dermatitis
  • Contact allergy
  • Exacerbation of eczema
  • Systemic absorption-related side effects (extremely rare)
Drug Interactions
  • Photosensitizers (e.g., tetracyclines, sulfonamides): Additive risk of phototoxicity.
  • Keratolytics (e.g., benzoyl peroxide, salicylic acid): Increased irritation; use with caution or stagger applications.
  • Cosmetic products: Avoid harsh cleansers, alcohol-based products, or exfoliants concurrently.
  • Systemic Retinoids (e.g., isotretinoin): Not typically combined due to cumulative irritation risk.

Enzyme System Involvement: Minimal systemic interaction as tazarotenic acid metabolism does not significantly involve CYP450 enzymes.

Recent Updates or Guidelines
  • No major changes in 2024–2025 regulatory approvals.
  • Combination therapies with topical corticosteroids (e.g., tazarotene + halobetasol) are gaining use for psoriasis.
  • Updated pregnancy warnings emphasize absolute avoidance in women who are or may become pregnant.
Storage Conditions
  • Temperature: Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C.
  • Humidity: Keep tightly closed to protect from moisture.
  • Light: Protect from excessive light; store in original packaging.
  • Handling: Do not freeze. Shake well before use (if suspension).
  • Shelf Life: Check printed expiry date; avoid use beyond that.