TAZORAC- tazarotene gel
Allergan, Inc.
FOR DERMATOLOGIC USE ONLY NOT FOR OPHTHALMIC, ORAL, OR INTRAVAGINAL USE.
DESCRIPTION
TAZORAC � Gel is a translucent, aqueous gel and contains the compound tazarotene, a member of the acetylenic class of retinoids. It is for topical dermatologic use only
Formula: C21 H21 NO2 S
Molecular Weight: 351.46
Chemical Name: Ethyl 6-[(4,4-dimethylthiochroman-6-yl)ethynyl]nicotinate
Contains:
Active: Tazarotene 0.05% or 0.1% (w/w)
Preservative: Benzyl alcohol 1% (w/w)
Inactives: Ascorbic acid; butylated hydroxyanisole; butylated hydroxytoluene; carbomer homopolymer type B; edetate disodium; hexylene glycol; poloxamer 407; polyethylene glycol 400; polysorbate 40; purified water; and tromethamine.
CLINICAL PHARMACOLOGY
Tazarotene is a retinoid prodrug which is converted to its active form, the cognate carboxylic acid of tazarotene (AGN 190299), by rapid deesterification in animals and man. AGN 190299 (�tazarotenic acid") binds to all three members of the retinoic acid receptor (RAR) family: RAR?, RAR?, and RAR? but shows relative selectivity for RAR?, and RAR? and may modify gene expression. The clinical significance of these findings is unknown.
Psoriasis: The mechanism of tazarotene action in psoriasis is not defined. Topical tazarotene blocks induction of mouse epidermal ornithine decarboxylase (ODC) activity, which is associated with cell proliferation and hyperplasia. In cell culture and in vitro models of skin, tazarotene suppresses expression of MRP8, a marker of inflammation present in the epidermis of psoriasis patients at high levels. In human keratinocyte cultures, it inhibits cornified envelope formation, whose build-up is an element of the psoriatic scale. Tazarotene also induces the expression of a gene which may be a growth suppressor in human keratinocytes and which may inhibit epidermal hyperproliferation in treated plaques. However, the clinical significance of these findings is unknown.
Acne: The mechanism of tazarotene action in acne vulgaris is not defined. However, the basis of tazarotene�s therapeutic effect in acne may be due to its anti-hyperproliferative, normalizing-of-differentiation and anti-inflammatory effects. Tazarotene inhibited corneocyte accumulation in rhino mouse skin and cross-linked envelope formation in cultured human keratinocytes. The clinical significance of these findings is unknown.
INDICATIONS AND USAGE
TAZORAC � (tazarotene) Gel 0.05% and 0.1% are indicated for the topical treatment of patients with stable plaque psoriasis of up to 20% body surface area involvement.
TAZORAC � (tazarotene) Gel 0.1% is also indicated for the topical treatment of patients with facial acne vulgaris of mild to moderate severity.
The efficacy of TAZORAC � Gel in the treatment of acne previously treated with other retinoids or resistant to oral antibiotics has not been established.
CONTRAINDICATIONS
Retinoids may cause fetal harm when administered to a pregnant woman.
DOSAGE AND ADMINISTRATION
General: Application may cause excessive irritation in the skin of certain sensitive individuals. In cases where it has been necessary to temporarily discontinue therapy, or the dosing has been reduced to a lower concentration (in patients with psoriasis) or to an interval the patient can tolerate, therapy can be resumed, or the drug concentration or frequency of application can be increased as the patient becomes able to tolerate the treatment. Frequency of application should be closely monitored by careful observation of the clinical therapeutic response and skin tolerance. Efficacy has not been established for less than once daily dosing frequencies.
For Psoriasis: It is recommended that treatment start with TAZORAC � 0.05% Gel, with strength increased to 0.1% if tolerated and medically indicated. Apply TAZORAC � Gel once a day, in the evening, to psoriatic lesions, using enough (2 mg/cm2) to cover only the lesion with a thin film to no more than 20% of body surface area. If a bath or shower is taken prior to application, the skin should be dry before applying the gel. If emollients are used, they should be applied at least an hour before application of TAZORAC � Gel. Because unaffected skin may be more susceptible to irritation, application of tazarotene to these areas should be carefully avoided. TAZORAC � Gel was investigated for up to 12 months during clinical trials for psoriasis.
For Acne: Cleanse the face gently. After the skin is dry, apply a thin film of TAZORAC � Gel 0.1% (2 mg/cm2) once a day, in the evening, to the skin where acne lesions appear. Use enough to cover the entire affected area. TAZORAC � Gel was investigated for up to 12 weeks during clinical trials for acne.
HOW SUPPLIED
TAZORAC � (tazarotene) Gel is available in concentrations of 0.05% and 0.1%. It is available in a collapsible aluminum tube with a tamper-evident aluminum membrane over the opening and a white propylene screw cap, in 30 g and 100 g sizes.