Tazarotene (Monograph)

Brand names: Tazorac, Avage
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
ATC class: D05AX05
VA class: DE752
Molecular formula: C₂₁H₂₁NO₂S
CAS number: 118292-40-3

Introduction

Synthetic acetylenic retinoid.

Uses for Tazarotene

Psoriasis

Treatment of stable plaque psoriasis with ≤20% body surface area involvement.

Combination therapy with a mid-or high-potency topical corticosteroid more effective than either agent alone.

0.1% cream or gel more effective in improving psoriasis manifestations; 0.05% cream or gel associated with less local irritation.

Acne

Treatment of mild to moderate acne vulgaris.

Efficacy in patients resistant to oral antibiotics or previously treated with other retinoids not established.

Photoaging

Palliative therapy to improve dermatologic changes (e.g., fine wrinkling, mottled hypo- or hyperpigmentation, benign lentigines) associated with photodamage.

Use as an adjunct to a comprehensive skin care plan and sun avoidance program. (See Administration under Dosage and Administration.)

Does not eliminate or prevent wrinkles, repair photodamaged skin, reverse photoaging, or restore youthful or younger dermal histologic pattern. No mitigating effects on severe manifestations of chronic sunlight exposure (e.g., coarse/deep wrinkling, tactile roughness, telangiectasia, skin laxity, keratinocytic atypia, melanocytic atypia, dermal elastosis) demonstrated.

Safety and efficacy not established for use in nonwhite (e.g., Asian, Hispanic) patients or Fitzpatrick skin types V and VI.

Related/similar drugs

Otezla, Sotyktu, doxycycline, methotrexate, clindamycin topical, Botox, Humira

Tazarotene Dosage and Administration

General

• Excessive use does not increase therapeutic effect and may produce marked inflammatory reactions (e.g., erythema, peeling, discomfort). (See Dermatologic Effects under Cautions.)

Administration

Topical Administration

Apply topically to the skin as a cream or gel.

For dermatologic use only; avoid contact with mouth, eyes, and other mucous membranes.

Wash hands after applying cream or gel (unless the hands are being treated for psoriasis).

Occlusive dressings or wrappings should not be used.

A transient feeling of pruritus, burning, or stinging may occur after application.

If irritation is excessive, temporarily discontinue therapy, reduce dosage strength (in patients with psoriasis), or decrease frequency of applications; reinitiate therapy or increase drug concentration or application frequency when patient is able to tolerate the drug. Closely monitor patient response and tolerance to changes in drug concentration or application frequency.

Psoriasis

Apply a sufficient amount (2 mg/cm²) of cream or gel to cover affected area lightly.

Apply cream or gel to dry skin. If required, apply moisturizer ≥1 hour prior to applying cream or gel; apply tazarotene only after ensuring that there is no more moisturizer on skin surface.

Avoid application of cream or gel to unaffected skin; these areas may be more susceptible to irritation. (See Dermatologic Effects under Cautions.)

Acne

Gently wash and dry affected area(s) prior to application.

Apply a sufficient amount of 0.1% cream or gel (2 mg/cm²) to cover all lesions with a thin film.

Photoaging

Apply 0.1% cream topically to the face; use the minimum amount necessary to cover the face (including eyelids if desired) lightly; avoid eyes and mouth.

Gently wash face with mild soap, pat and dry, and wait 20–30 minutes before applying tazarotene cream to face.

Moisturizers may be applied to skin before or after application of tazarotene; however, allow first topical preparation to absorb into the skin and dry completely before applying the second preparation.

Administer in conjunction with a comprehensive skin care plan and a sun avoidance program; apply a moisturizing sunscreen (≥15 SPF) every morning.

Dosage

Pediatric Patients

Acne

Topical

Children >12 years of age: Apply a sufficient amount (2 mg/cm²) of 0.1% cream or gel once daily in the evening.

Improvement usually is detectable within 4 weeks of initiating therapy.

Adults

Psoriasis

Topical

Initially, apply 0.05% cream or gel (2 mg/cm²) once daily in the evening.

If tolerated and clinically indicated, increase to 0.1% cream or gel once daily in the evening; if excessive skin irritation occurs, reduce concentration to 0.05%.

Improvement in psoriasis plaques and scales usually is detectable within 1–4 weeks of initiating therapy; improvement in erythema may take longer.

Acne

Topical

Apply a sufficient amount (2 mg/cm²) of 0.1% cream or gel once daily in the evening.

Therapeutic effects may require >4 weeks of therapy.

Photoaging

Topical

Apply a pea-sized amount (5-mm or ¼-inch diameter) of the 0.1% cream to the face once daily at bedtime.

Prescribing Limits

Efficacy of application less than once daily not established.

Pediatric Patients

Acne

Topical

Children ≥12 years of age: In clinical studies, therapy did not exceed 12 weeks.

Adults

Psoriasis

Topical

Safety and efficacy of therapy with 0.05% and 0.1% gel for >12 months not established.

Safety of application to >20% of body surface area not established.

Acne

Topical

Safety and efficacy of therapy with 0.1% cream or gel for >12 weeks not established.

Photoaging

Topical

Safety and efficacy of therapy with 0.1% cream for >52 weeks not established.

Cautions for Tazarotene

Contraindications

• Known or suspected pregnancy. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

• Known hypersensitivity to tazarotene or any ingredient in the formulation.

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity and embryotoxicity demonstrated in animals receiving topical and oral tazarotene.

Systemic exposure depends on amount of body surface area treated. Level of exposure to produce teratogenic effects in humans unknown.

Exclude pregnancy using a reliable blood pregnancy test with a sensitivity of ≥50 mIU/mL for human chorionic gonadotropin (HCG) within 2 weeks before initiating tazarotene; initiate therapy during next normal menstrual period.

Use adequate forms of contraception during tazarotene therapy.

If pregnancy occurs, immediately discontinue and apprise of potential fetal hazard.

Sensitivity Reactions

Photosensitivity

Increased risk of sunburn.

Cautious use recommended in patients subjected to considerable occupational sun exposure and those with inherent sensitivity to the sun; use of sunscreen products (≥SPF 15) and protective clothing over treated areas recommended when exposure cannot be avoided.

Caution recommended with concomitant use of photosensitizing agents. (See Specific Drugs under Interactions.)

Use not recommended for patients with sunburn until full recovery occurs.

Minimize exposure of treated area(s) to sunlight and avoid use of sunlamps.

General Precautions

Use in Patients with Eczema

Possible severe irritation of eczematous skin. Use not recommended in patients with eczema.

Dermatologic Effects

Possible severe erythema, pruritus, burning, or stinging. If irritation is excessive, discontinue therapy temporarily until skin integrity restored, or reduce dosing to a concentration (in patients with psoriasis) or interval patient can tolerate; however, efficacy of reduced dosing frequencies (i.e., < once daily) not established. (See Dosage under Dosage and Administration.)

Avoid contact of the drug with mouth, eyes, and other mucous membranes. If ocular contact occurs, affected eye(s) should be flushed with copious amounts of cool water; consult clinician if ocular irritation persists.

Environmental Stimuli

Possible increased skin irritation in patients exposed to environmental extremes (e.g., wind, cold).

Lentigo maligna

Facial pigmented lesions should be assessed by a clinician before application of tazarotene therapy for photoaging. Lentigo maligna should not be treated with tazarotene.

Specific Populations

Pregnancy

Category X. (See Fetal/Neonatal Morbidity and Mortality and also Contraindications under Cautions.)

Lactation

Not known whether topical tazarotene distributed into human milk; caution advised if topical tazarotene used.

Pediatric Use

Safety and efficacy not established for treatment of psoriasis in children <18 years of age, for treatment of acne in children <12 years of age, or for treatment of photoaging in children <17 years of age.

Geriatric Use

Safety and/or efficacy for treatment of psoriasis and photoaging in those >65 years of age similar to that in younger adults; possibility exists of greater sensitivity to the drug in geriatric individuals.

Safety and efficacy not evaluated for treatment of acne in patients >65 years of age.

Common Adverse Effects

In patients with psoriasis: Pruritus, erythema, burning/stinging, worsening of psoriasis, irritation, skin pain.

In patients with acne: Desquamation, burning/stinging, dry skin, erythema, pruritus.

In patients treated for photoaging: Desquamation, erythema, burning, dry skin, skin irritation, pruritus.

Drug Interactions

Specific Drugs

Other Topical Preparations

Potential pharmacodynamic interaction (increased skin irritation). Avoid concomitant use of topical preparations with high concentrations of alcohol, menthol, spices, or lime (e.g., lotions, astringents, perfume); irritating cosmetics (e.g., toners, peeling [desquamating] agents); permanent wave solutions; electrolysis; hair depilatories; or other preparations or processes that might dry or irritate the skin. Allow time for effects of skin-drying preparations to subside before initiating tazarotene therapy.

Tazarotene Pharmacokinetics

Absorption

Bioavailability

Minimally absorbed following topical application; however, systemic exposure depends on the extent of body surface area treated.

Distribution

Extent

Not known whether topical tazarotene distributed into human milk.

Plasma Protein Binding

>99%.

Elimination

Metabolism

Metabolized via esterase hydrolysis to active metabolite, tazarotenic acid. Other metabolites (i.e., sulfoxides, sulfones, and other polar metabolites) have been identified.

Elimination Route

Excreted principally in urine and feces.

Half-life

Tazarotenic acid: approximately 18 hours.

Stability

Storage

Topical

Cream

25°C (may be exposed to -5–30°C).

Gel

25°C (may be exposed to 15–30°C).

Actions

• Pharmacologic actions similar to other retinoids (e.g., vitamin A, tretinoin, isotretinoin); however, tazarotene shows selective affinity for specific nuclear retinoic acid receptor (RAR) proteins RARβ and RARγ and may modify gene expression.

• Exact mechanism(s) of action for treatment of psoriasis not determined. May affect expression of genes that modulate cell (e.g., epidermal) differentiation, proliferation, and inflammation, leading to normalization of keratinocyte differentiation and reduced cellular hyperproliferation and inflammation.

• Exact mechanism(s) of action for treatment of acne not fully understood. Appears to modulate follicular keratinization, cell proliferation, and inflammation resulting in inhibition of corneocyte accumulation and cohesion and decreased inflammatory and noninflammatory acne lesions.

• Exact mechanism(s) of action in the treatment of photoaging not determined. May increase the number of granular cell layers and increase the incidence of epidermal edema.

Advice to Patients

• Importance of clinicians instructing patients about proper use of the drug, including associated precautions. Provide copy of the manufacturer's patient instructions.

• Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed. Necessity for clinicians to describe risk of birth defects and to advise women to avoid pregnancy by using adequate methods of contraception during therapy. (See Fetal/Neonatal Morbidity and Mortality under Warnings.)

• Importance of avoiding excessive use of topical tazarotene.

• Importance of contacting clinician if dermatologic condition worsens with tazarotene therapy.

• Importance of avoiding use of shaving lotions, astringents, perfume, toners, peeling (desquamating) agents, permanent wave solutions, electrolysis, hair depilatories, or other preparations or processes that might irritate the skin.

• Importance of consulting clinician regarding specific instructions for routine skin care, use of cosmetics, moisturizers, and sunscreens.

• Importance of adhering to prescribed directions for use; avoid contact with eyes, mouth, or mucous membranes.

• Importance of informing patients that treated areas of the skin should not be bandaged or otherwise covered or wrapped so as to be occlusive unless directed by their clinician.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and cosmetic products or procedures.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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