tazarotene (Rx)

>10%

Scaling (51%)

Erythema (34-49%)

Desquamation (40%)

Burning/stinging (22-30%)

Itching (29%)

Dry skin (15%)

1-10%

Skin irritation (10%)

Pruritus (10%)

Irritant contact dermatitis (8%)

Stinging (3%)

Rash (3%)

Cheilitis (1%)

Arazlo

• Application site pain (5%)
• Application site dryness (4%)
• Application site exfoliation (2%)
• Application site erythema (2%)
• Application site pruritus (1%)

Frequency Not Defined

Worsening of psoriasis

Eczema

Rash

Dry skin

Skin inflammation

Fissuring

Bleeding

Peripheral edema

Hypertriglyceridemia

Postmarketing Reports

Blister, rash, skin discoloration (including skin hyperpigmentation or skin hypopigmentation), and pain

Embryofetal toxicity

Photosensitivity and risk of sunburn

Contraindications

Pregnancy

Hypersensitivity

Cautions

Propellant in foam is flammable; avoid fire, flame, and/or smoking during and immediately following application

Local irritation

• Excessive irritation in skin of certain sensitive individuals; local reactions (including blistering and skin desquamation, pruritus, burning, erythema)and hypersensitivity adverse reactions (including urticaria) reported with topical application
• If adverse reactions occur, consider discontinuing the medication or reducing dosing frequency, as appropriate, until integrity of skin is restored; alternatively, patients withpsoriasis who are being treated with 0.1% concentration can be switched to lower concentration; frequency of application should be closely monitored by careful observation of clinical therapeutic response and skin tolerance; therapy can be resumed, or drug concentrationor frequency of application can be increased as patient becomes able to tolerate treatment
• Concomitant topical medications and cosmetics that have strong drying effect should be avoided; it is also advisable to "rest" a patient's skin until effects of such preparations subside before treatment is initiated
• Drug should not be used on eczematous skin, as it may cause severe irritation
• Weather extremes, such as wind or cold, may be more irritating to patients using the topical application

Photosensitivity and risk of sunburn

• Because of heightened burning susceptibility, exposure to sunlight (including sunlamps) should be avoided unless deemed medically necessary, and in such cases, exposure should be minimized during therapy
• Patients must be warned to use sunscreens and protective clothing when using this drug; patients with sunburn should be advised not to use the topical application until fully recovered; patients who may have considerable sun exposure due to their occupation and those patients with inherent sensitivity to sunlight should exercise particular caution when using this drug
• Administer with caution if patient is taking drugs known to be photosensitizers (eg, thiazides, tetracyclines, fluoroquinolones, phenothiazines, sulfonamides)because of increased possibility of augmented photosensitivity
• Use of sunscreens (minimum strength of SPF 15) and protective clothing recommended during use

Embryofetal toxicity

• This drug elicits malformations and developmental effects associated with retinoids after topical and oral administration to pregnant rats and rabbits during organogenesis; systemic exposure to tazarotenic acid is dependent upon extent of body surface area treated; in patients treated topically over sufficient body surface area, exposure could be in same order of magnitude as in orally treated animals
• Although there may be less systemic exposure in treatment of acne of the face alone due to less surface area for application, this drug is a teratogenic substance and causes fetal malformations in animals, and it is not known what level of exposure is required for teratogenicity in humans

Drug interaction overview

• Concomitant topical acne therapy should be used with caution because a cumulative irritant effect may occur; if irritancy or dermatitis occurs, reduce frequency of application or temporarily interrupt treatment and resume once the irritation subsides
• Avoid concomitant dermatologic medications and cosmetics that have a strong drying effect; postpone treatment until the effects of these products subside before initiating treatment
• Coadministration with oxidizing agents, such as benzoyl peroxide, may cause degradation of tazarotene and may reduce the clinical efficacy of tazarotene; if combination therapy is required, apply at different times of the day (eg, one in the morning and the other in the evening).

Pregnancy

There are no adequate and well-controlled studies with use in pregnant women

Contraindicated in females who are or may become pregnant

Based on data from animal reproduction studies, retinoid pharmacology, and the potential for systemic absorption, may cause fetal harm when administered to a pregnant female and is contraindicated during pregnancy; safety in pregnant females has not been established; the potential risk to the fetus outweighs the potential benefit to the mother during pregnancy; therefore, discontinue as soon as pregnancy is recognized

Females of childbearing potential

• Females of child-bearing potential should be warned of potential risk and use adequate birth- control measures when the drug is administered; the possibility that a female of child-bearing potential is pregnant at time of institution of therapy should be considered

• Pregnancy testing

  • Pregnancy testing is recommended within 2 weeks before initiating therapy, which should begin during a menstrual period

• Contraception

  • Based on animal studies, fetal harm may occur when administered to a pregnant woman
  • Advise to use effective contraception during treatment

Lactation

Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or from the underlying maternal condition

Clinical considerations

• To minimize potential exposure to the breastfed infant via breast milk, use for the shortest duration possible while breastfeeding
• Advise breastfeeding patients not to apply directly to the nipple and areola to prevent direct infant exposure

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Mechanism of Action

Retinoid: Appears to affect expression of genes that modulate cell (eg, epidermal) differentiation, proliferation, and inflammation, leading to normalization of keratinocyte differentiation and a reduction in cellular hyperproliferation and inflammation

Absorption

<1% systemically absorbed

Peak plasma concentration: 0.43 ng/mL (foam); 0.71 ng/ mL (gel); 0.236 ng/mL (0.1% cream)

Peak plasma time: 6 hr (foam); 9 hr (gel)

AUC: 6.98 ng⋅hr/mL (foam); 10.1 ng⋅hr/mL (gel); 1.38 ng⋅hr/mL (0.1% cream)

Steady-state within 22 days

Distribution

Protein bound: >99%

Metabolism

Hydrolyzed to its active metabolite, tazarotenic acid

Elimination

Half-Life: 8.1 hr (foam); ~18 hr (gel and cream)

Sulfoxides, sulfones, and other polar metabolites eliminated through urinary and fecal pathways

Topical Administration

Not for ophthalmic, oral, or intravaginal use

Avoid the eyes, mouth, paranasal creases, and mucous membranes

If contact with eyes occurs, rinse thoroughly with water

Use effective sunscreens and wear protective clothing during use

Foam

• Apply after washing with a mild cleanser and fully drying the affected area
• Dispense a small amount of foam into the palm of the hand
• Using fingertips, apply only enough foam to lightly cover the entire affected areas of the face and/or upper trunk with a thin layer; gently massage the foam into the skin until the foam disappears
• Avoid eyes, lips, and mucous membranes
• Wash hands after application
• Use moisturizer as needed
• If undue irritation (redness, peeling, or discomfort) occurs, reduce frequency of application or temporarily interrupt treatment
• Resume once irritation subsides; discontinue if irritation persists

Lotion

• Topical use only
• Apply a thin layer to the affected areas
• If lotion gets in or near eyes, rinse thoroughly with water
• Wash hands thoroughly after applying lotion

Gel

• Apply a thin film to cover only the psoriatic lesions on no more than 20% of BSA
• If a bath or shower is taken before application, skin should be dry before applying the gel
• If emollients are used, apply at least 1 hour before application
• Because unaffected skin may be more susceptible to irritation, carefully avoid application of tazarotene

Storage

Gel and foam: Store at 20-25ºC (68-77ºF); excursions permitted from 15-30ºC (59-86ºF)

Tazorac cream: Store at 20-25ºC (68-77ºF); excursions permitted from -5-30ºC (23-86ºF)