Tazarotene Gel

Shalita AR et al Tazarotene gel is safe and effective in the treatment of acne vulgaris. A multicenter, double-blind, vehicle-controlled study. Cutis 1999 63 349. [PMID 10388959]... 

The pharmacokinetics and metabolism of tazarotene (2) is especially worth noting. Topical gel application provides the direct delivery of tazarotene into the skin. Ten hours after a topical application of 0.1% tazarotene gel to the skin, approximately 4-6% of the dose resides in the stratum comeum and 2% of the dose is distributed to the viable epidermis and dermis. As depicted in Scheme 3, both tazarotene (2) and tazarotenic acid (11) undergo further metabolism to their corresponding sulfoxides 12 and 13, respectively. Sulfoxides 12 and 13, in turn, are even further oxidized to sulfones 14 and 15, respectively. These very polar metabolites do not accumulate in adipose tissue, but are rapidly eliminated via both urinary and fecal pathways with a terminal half-life of approximately 18 h. A lesson learned here is that installation of a sulfide moiety promotes clearance because it is oxidized to polar metabolites that are rapidly cleared. As the consequence, the systemic exposure is minimized. Percutaneous absorption of tazarotene (2) led to a plasma concentration below 1 gg/L. The systemic... 

Tanghetti, E.A., An observation study evaluating the treatment of plaque psoriasis with tazarotene gels, alone and with an emollient and/or corticosteroid. Cutis, 2000, 66 (Suppl. 6) 4—11. 

Once-daily tazarotene gel may be more effective than once-daily tretinoin in redncing papnles and open comedones, with eqnal efficacy against closed comedones. " Efficacy is comparable to adapalene, bnt its local tolerance by daily application is similar to tretinoin. In addition, tazarotene was stndied for its efficacy with short contact application. Once-daily short contact applications signiflcantly rednced irritation potential, yet maintained therapeutic equivalency to standard application regimens. ... 

Weinstein GD, Krueger GG, Lowe NJ, et al. Tazarotene gel, a new retinoid, for topical therapy of psoriasis vehicle-controlled study of safety, efficacy, and duration of therapeutic effect. J Am Acad Dermatol 1997 37 85-92. 

Tazarotene gel, applied once daily to dry skin, may be used as monotherapy or in combination with other medications, such as topical corticosteroids, for the treatment of localized plaque psoriasis. This is the first topical retinoid approved by the Food and Drug Administration (FDA) for the treatment of psoriasis. Side effects of burning, itching, and skin irritation are relatively common, and patients should avoid sun exposure. 

Kraemer KH, Di Giovanna JJ, Moshell AN, Tarone RE, Peck GL (1988) Prevention of skin cancer in xeroderma pigmentosum with the use of oral isotretinoin. N Engl J Med 318 1633-1637 Krueger GG, Drake LA, Elias PM, Lowe NJ, Guzzo C, Weinstein GD, Lew-Kaya DA, Lue JC, Sefton J, Chandraratna RA (1998) The safety and efficacy of tazarotene gel, a topical acetylenic retinoid, in the treatment of psoriasis. Arch Dermatol 134 57-60... 

Sefton J, Kligman AM, Kopper SC, Lue JC, Gibson JR (2004) Photodamage pilot study a double-blind, vehicle-controlled study to assess the efficacy and safety of tazarotene 0.1% gel. J Am Acad Dermatol 43 656-663... 

Tazarotene Tazorac 0.05% and 0.1 % cream 0.05% and 0.1% gel Apply a small amount once daily before bedtime Same as tretinoin but may be more severe... 

Tazarotene (Tazorac) is a synthetic retinoid that is hydrolyzed to its active metabolite, tazarotenic acid, which modulates keratinocyte proliferation and differentiation. It is available as a 0.05% or 0.1% gel and cream and is applied once daily (usually in the evening) for mild to moderate plaque psoriasis. Adverse effects are dose- and frequency related and include mild to moderate pruritus, burning, stinging, and erythema. Application of the gel to eczematous skin or to more than 20% of body surface area is not recommended because this may lead to extensive systemic absorption. Tazarotene is often used with topical corticosteroids to decrease local adverse effects and increase efficacy. 

Tazarotene (Tazorac) is an acetylenic retinoid that is available as a 0.1% gel and cream for the treatment of mild to moderately severe facial acne. Topical tazarotene should be used by women of childbearing age only after contraceptive counseling. It is recommended that tazarotene should not be used by pregnant women. 

Tazarotene is used in the treatment of mild to moderate acne vulgaris and has comedolytic, keratolytic, and anti-inflammatory action. Tazarotene 0.1% and 0.05% gel and cream have been shown to be more effective than vehicle in the treatment of acne vulgaris." " The 0.1% gel was slightly more effective than the 0.05% gel in decreasing lesion counts, with treatment snccess rates of 68% and 51% of patients, respectively. ... 

Treatment with 0.1% gel, apphed once daily, results in substantial reduction in the severity of scahng and plaque thickness during 12-week treatments. The 0.1% gel is somewhat more efficacious, but the 0.05% formulation is associated with less irritation." " Based on the results of clinical trials, tazarotene is effective for the treatment of mild to moderate plaque psoriasis." " ... 

Tazarotene 0.1% gel plus corticosteroid cream in the treatment of plaque psoriasis. Journal of the American Academy of Dermatology, 39 (4 Pt 1), 590-596. 

Comparative studies Topical tazarotene has been compared with crude coal tar in the topical treatment of stable plaque psoriasis in a non-blinded study, in which 27 patients applied tazarotene 0.1% gel on the right side... 

A beneficial response of stationary, plaque-type psoriasis by third generation retinoids for topical use such as tazarotene (0.05-0.1% gel) has recently been reported [12,25,47]. However, topical retinoids are more potent in combination with phototherapy or with mild topical corticosteroids in order to avoid retinoid-induced irritation [60, 43]. 

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