Tazorac - Drug Monograph

Introduction

Tazorac (tazarotene) is a third-generation topical retinoid approved by the FDA for the treatment of plaque psoriasis and acne vulgaris. It belongs to the acetylenic class of retinoids and is available as a gel (0.05%, 0.1%) and cream (0.05%, 0.1%) formulation. Tazorac represents an important therapeutic option in dermatology due to its ability to modulate keratinocyte differentiation and proliferation.

Mechanism of Action

Tazarotene is a prodrug that is rapidly converted to its active form, tazarotenic acid, in the skin. The active metabolite binds to retinoic acid receptors (RARs), particularly RAR-β and RAR-γ subtypes. This binding modulates gene expression, resulting in:

• Normalization of keratinocyte differentiation
• Reduction of hyperproliferation in psoriatic plaques
• Inhibition of comedogenesis in acne
• Anti-inflammatory effects through modulation of inflammatory mediators
• Reduction of microcomedone formation

Indications

• Treatment of plaque psoriasis affecting up to 20% of body surface area (0.05% and 0.1% gel/cream)
• Treatment of facial acne vulgaris (0.1% gel)
• Treatment of mild to moderate facial acne (0.1% cream)

• Photoaging and photodamage
• Melasma
• Certain forms of ichthyosis
• Keratosis pilaris
• Stretch marks

Dosage and Administration

• Apply once daily in the evening to affected areas
• Use the smallest amount needed to cover lesions
• Start with 0.05% strength, may increase to 0.1% if tolerated

• Cleanse face gently and dry before application
• Apply thin film to affected areas once daily in evening
• 0.1% strength typically used

• Geriatric patients: Use with caution due to increased skin fragility
• Renal impairment: No dosage adjustment necessary
• Hepatic impairment: Use with caution; limited data available
• Pediatric patients: Safety and efficacy not established under age 12

Pharmacokinetics

Contraindications

• Hypersensitivity to tazarotene or any component of the formulation
• Pregnancy (Category X - contraindicated)
• Women attempting to conceive
• Breastfeeding (relative contraindication)

Warnings and Precautions

• Photosensitivity: Increased risk of sunburn; sun avoidance recommended
• Skin irritation: Erythema, pruritus, and burning common, especially during initial treatment
• Weather extremes: Use with caution in windy or cold weather
• Eczema: May cause severe irritation in patients with this condition
• Avoid contact with eyes, eyelids, mouth, angles of the nose, and mucous membranes

Drug Interactions

• Photosensitizing agents (tetracyclines, fluoroquinolones, sulfonamides): Enhanced photosensitivity
• Other topical products (especially drying agents, astringents): Increased risk of irritation
• Topical corticosteroids: May alter efficacy; sequential therapy often used
• Benzoyl peroxide: May oxidize tazarotene; apply at different times of day

Adverse Effects

• Application site reactions: pruritus (10-30%), burning/stinging (10-20%), erythema (10-20%)
• Dry skin (10-20%)
• Skin peeling/desquamation (5-15%)
• Irritation (5-10%)

• Skin discoloration
• Photosensitivity
• Contact dermatitis
• Worsening of psoriasis (rare)

• Severe skin irritation requiring discontinuation
• Hypersensitivity reactions
• Blistering and crusting

Monitoring Parameters

• Efficacy: Psoriasis: reduction in scaling, erythema, plaque elevation; Acne: lesion count reduction
• Skin tolerance: Degree of erythema, peeling, dryness, and irritation
• Pregnancy status: Monthly monitoring in women of childbearing potential
• Sun exposure: Education regarding sun protection measures
• Liver function: Periodically in long-term use, though rarely affected

Patient Education

• Use exactly as prescribed; more frequent application increases irritation without improving efficacy
• Apply to clean, dry skin only
• Use pea-sized amount for entire face
• Avoid sun exposure and use sunscreen (SPF ≥30) daily
• May cause initial worsening before improvement (4-8 weeks for acne, 2-4 weeks for psoriasis)
• Notify provider if excessive irritation, blistering, or crusting occurs
• Use effective contraception during treatment and for one month after discontinuation
• Do not apply to broken, sunburned, or eczematous skin
• Wait 20-30 minutes after washing before application
• May bleach hair or colored fabrics

References

1. FDA Prescribing Information: Tazorac (tazarotene) Gel and Cream 2. Lebwohl M, et al. J Am Acad Dermatol. 1998;39(4):S123-S127 3. Bershad S, et al. Arch Dermatol. 2002;138(4):481-489 4. Webster GF, et al. Cutis. 2001;68(4 Suppl):2-11 5. Chandraratna RA. J Am Acad Dermatol. 1997;36(6 Pt 3):S96-S103 6. Weinstein GD, et al. J Am Acad Dermatol. 1997;37(1):85-92 7. Drug Facts and Comparisons. Wolters Kluwer Health, 2023 8. Clinical Dermatology: A Color Guide to Diagnosis and Therapy. Elsevier, 2021