Drug information of Tazarotene

Tazarotene

فارسی

Tazarotene is a prescription topical retinoid sold as a cream or gel. This medication is approved for treatment of psoriasis, acne, and sun damaged skin (photodamage).

Mechanism of effect

Although the exact mechanism of tazarotene action is not known, studies have shown that the active form of the drug (tazarotenic acid) binds to all three members of the retinoic acid receptor (RAR) family: RARa, RARb, and RARg, but shows relative selectivity for RARb, and RARg and may modify gene expression. It also has affinity for RXR receptors.

Pharmacodynamic

Tazarotene is a prodrug and a member of the acetylenic class of retinoids. Following topical application, tazarotene undergoes esterase hydrolysis to form its active metabolite, tazarotenic acid. When treating acne tazarotene may be taken in conjunction with an oral antibiotic. Tazarotene has been shown in peer-reviewed double blinded studies to reduce: mottling and hyperpigmentation, sallowness, fine wrinkling and coarse wrinkling in sun damaged skin.

Histological studies have shown that long term (greater than 1 year) use of Tazarotene is associated with a significant reduction in atypical melanocytes and keratocytes - cells considered to be precursors of skin cancer. Some studies have shown long term use of Tazarotene to be associated with increased collagen production and better organization of skin collagen bundles.

Pharmacokinetics

  • Absorption: <1% systemically absorbed
  • Protein binding: The active form of the drug, tazarotenic acid, is highly bound to plasma proteins (>99%).
  • Metabolism: Undergoes esterase hydrolysis in skin to form its active metabolite, tazarotenic acid. Tazarotenic acid is further metabolized in skin and, after systemic absorption, hepatically metabolized to sulfoxides, sulfones, and other polar products for elimination.
  • Half-Life: 18 hr
  • Route of elimination: through urinary and fecal pathways.

Drug indications

Acne , Psoriasis

Dosage

Adult

Acne Vulgaris

  • Cream 0.1% indicated for acne vulgaris and gel 0.1% indicated for mild-to-moderate acne vulgaris; whereas, foam 0.1% indicated for moderate-to-severe acne
  • Cream/gel/foam 0.1%: Apply to affected area qDay

Psoriasis

Indicated for topical treatment of stable plaque psoriasis; gel indicated for up to 20% BSA

  • Cream/gel 0.05% or 0.1%: apply to affected area qDay

Wrinkles

Indicated to mitigate signs of chronic sunlight exposure (eg, coarse or deep wrinkling, tactile roughness, telangiectasia, skin laxity, keratinocytic atypia, melanocytic atypia, or dermal elastosis)

Cream 0.1%: Apply to affected areas qHS

Pediatric

Acne Vulgaris

Cream 0.1% indicated for acne vulgaris and gel 0.1% indicated for mild-to-moderate acne vulgaris; whereas, foam 0.1% indicated for moderate-to-severe acne

<12 years: Safety and efficacy not established

≥12 years: Apply to affected area qDay

Psoriasis

Cream indicated for topical treatment of stable plaque psoriasis; gel indicated for up to 20% BSA

<12 years: Safety and efficacy not established

≥12 years: Apply to affected area qDay

Alerts

Re-evaluate if not healed in 10 days

May cause fetal harm when administered to a pregnant woman; obtain a pregnancy test in females of reproductive potential within 2 weeks prior to initiating treatment; advise females of reproductive potential to use effective contraception

Some individuals may experience excessive pruritus, burning, skin redness, or peeling; if these reactions occur, discontinue therapy until integrity of skin has been restored or reduce dosing interval; avoid use on eczematous skin, as such use may cause severe irritation

Local tolerability reactions and hypersensitivity adverse reactions have been observed with topical tazarotene, including blistering, skin desquamation, and urticaria; if adverse reactions occur, discontinue medication until integrity of skin is restored, or reduce dosing to an interval the patient can tolerate

Avoid using cream if patient is also taking drugs known to be photosensitizers (e.g., thiazides, tetracyclines, fluoroquinolones, phenothiazines, sulfonamides) because of increased possibility of augmented photosensitivity

Use of sunscreens (minimum strength of SPF 15) & protective clothing recommended during use

Avoid exposure to sunlight, sunlamps, and weather extremes; in sunburn, do not use tazarotene until full recovery

Nof for use in lentigo maligna; carefully assess facial pigmented lesions of concern before application of cream

Points of recommendation

Some weather conditions may irritate the skin. Talk with the doctor.

Skin may look worse before it looks better.

Talk with your doctor before you use other drugs or products on your skin.

You may get sunburned more easily. Avoid sun, sunlamps, and tanning beds. Use sunscreen and wear clothing and eyewear that protects you from the sun.

If you are pregnant or you get pregnant while taking tazarotene cream, call your doctor right away.

Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Do not take tazarotene cream by mouth. Use on your skin only. Keep out of your mouth, nose, and eyes (may burn).

Do not put in the vagina.

If you get tazarotene cream in any of these areas, rinse well with water.

If you are able to get pregnant, start using tazarotene cream during your normal menstrual period.

Wash your hands before use.

Clean affected part before use. Make sure to dry well.

Put a thin layer on the affected skin and rub in gently.

Do not put on cuts, scrapes, eczema, or damaged skin.

Do not use coverings (bandages, dressings, make-up) unless told to do so by the doctor.

Avoid putting on healthy skin.

If you are not treating the skin on your hands, wash your hands after use.

Skip the missed dose and go back to your normal time.

Do not put on 2 doses or extra doses.

Drug contraindications

pregnancy , eczema , Hypersensitivity

Pregnancy level

D

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