Tazorac

Tazorac (marketed as Tazorac®, Avage® and Zorac®) 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). .
[Wikipedia].

Tazorac - Pharmacology:

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.

Tazorac mini report

Tazorac NDA
NDA - A product marketed under an approved New Drug Application
Tazorac CUTANEOUS
CUTANEOUS
Tazorac ORAL
ORAL
Tazorac HUMAN PRESCRIPTION DRUG
HUMAN PRESCRIPTION DRUG
Tazorac global name
tazarotene
Tazorac global name
Tazarotene
Start - Stop data
START DATA:
2000-Nov-13
Start - Stop data
STOP DATA
not occurred

Tazorac for patients

AVAGE (TAZAROTENE) Cream 0.1%

Use only on the face.

Read this leaflet carefully before you start to use your medicine. Read the information you get every time you get more medicine. There may be new information about the drug. This leaflet does not take the place of talks with your doctor. If you have any questions or are not sure about something, ask your doctor or pharmacist.

What is the most important information I should know about AVAGE™ Cream?

AVAGE™ Cream can cause birth defects in unborn children of women who are pregnant when they use the product.If you are a woman who can become pregnant,you must not be pregnant when you start using AVAGE™ Cream,and you must avoid pregnancy while you use it. See the sections "Who should not use AVAGE™ Cream?" "How should I use AVAGE™ Cream?" and "What should I avoid while using AVAGE™ Cream?" for more information.

• Avoid sunlight and other medicines that may increase your sensitivity to sunlight

• AVAGE™ Cream does not remove wrinkles or repair sun-damaged skin.

What is AVAGE™ Cream?

AVAGE™ Cream is a prescription medicine that may reduce fine facial wrinkles and certain types of dark and light spots on your face.

• AVAGE™ is for patients who are using a total skin care program and avoiding sunlight. AVAGE™Cream does not remove wrinkles, repair sun-damaged skin, reverse skin aging from the sun (photoaging), or bring back more youthful or younger skin. AVAGE™ does not work for everyone who uses it. It may work better for some patients than for others.

• The active ingredient in AVAGE™ Cream is tazarotene.

Who should not use AVAGE™ Cream? Do not use AVAGE™ Cream if

you are pregnant,plan to become pregnant,or may become pregnant. AVAGE™ Cream may harm your unborn child. Women who can become pregnant must have proof they are not pregnant from a reliable pregnancy test, done within 2 weeks before starting AVAGE™ Cream. Talk with your doctor about effective birth control if you are a woman who is able to become pregnant.

you have sunburn or eczema. If you have sunburn, wait until full recovery before using AVAGE™ Cream. AVAGE™ Cream may cause severe irritation if used on eczema. Wait until your doctor tells you your eczema has cleared up before starting AVAGE™ treatment.

you are allergic to the ingredients in AVAGE™ Cream. The active ingredient is tazarotene. See the end of this information for a list of inactive ingredients.

Tell your doctor before using AVAGE™ if

• you are breast feeding. We do not know if AVAGE™ Cream can pass through your milk and harm the baby.

• you are sensitive to sunlight. AVAGE™ may not be right for you or you may need extra protection from sunlight.

• you take certain other medicines, vitamins, and supplements that increase your sensitivity to sunlight. These include Vitamin A and medicines that are called thiazides, tertracyclines, fluoroquinolones, phenothiazines, and sulfonamides. Therefore, tell your doctor if you take any prescription or non-prescription medicines, vitamins, or supplements. This will help your doctor decide if you can take AVAGE™ Cream.

• you take any other prescription or non-prescription medicines, supplements or vitamins. Some of them may make you more sensitive to sunlight.

How should I use AVAGE™ Cream?

• If you are able to become pregnant, take a reliable pregnancy test within 2 weeks before beginning to use AVAGE™ Cream to be sure you are not pregnant. If you have menstrual periods, start taking AVAGE™ Cream during a normal menstrual period. These actions help assure you are not pregnant when you begin use.

• If you get pregnant while using AVAGE™ Cream, stop use and contact your doctor right away.

• Use AVAGE™ Cream only under the guidance of your doctor as part of a total skin care program in which you avoid sunlight. This program should include avoiding sunlight as much as possible, using clothing to protect you from sunlight, using sunscreens with an SPF of 15 or higher, and using face creams that add moisture to your skin.

• Follow these directions:

1. Use AVAGE™ Cream once a day in the evening.

2. In the evening, gently wash your face with mild soap. Pat your skin dry and wait 20-30 minutes before applying AVAGE™ Cream. 3. Be sure your skin is dry before you use AVAGE™ Cream.

4. Apply only a pea-sized amount (about .197 inch or 5 mm wide) to your face at one time. This should be enough to cover the wrinkled or discolored areas lightly. You can include your eyelids, if desired.

5. Wash your hands after applying the medicine. If the cream gets on areas you do not need to treat, wash it off. 6. In the morning, apply a moisturizing sunscreen of SPF 15 or greater.

• You can use a cream or lotion to soften or moisten your skin before or after you apply AVAGE™ Cream. Just be sure there is no more of the first cream or lotion on your skin and your skin is dry before you apply the second product.

• Keep AVAGE™ Cream out of your eyes and mouth. If it gets in your eyes, wash them off with large amounts of cool water. Contact your doctor if irritation continues.

• If you miss a dose, do not try to make it up. Continue with your normal schedule.

• In general, you can use facial moisturizers, such as lotions, oils, and creams, as often as you want. However, follow your doctors advice for routine skin care and for using makeup, moisturizers, and sunscreens.

• Do not use more AVAGE™ Cream than instructed or more often than instructed. Using larger amounts of medicine than recommended will not lead to faster or better results and may cause more side effects.

• Wear clothing that protects your skin from the sun, and use non-prescription creams to help keep your skin soft.

• Watch your reaction to AVAGE™ Cream carefully if you are also using other skin products or processes with strong drying or irritating effects. These include products with high amounts of alcohol, astringents, spices, lime peel, medicated or abrasive soaps, medicated shampoos, and permanent wave solution. Avoid electrolysis, hair depilatories, waxes, and other products or processes that may dry or irritate your skin.

• If AVAGE™ Cream is swallowed, contact your doctor or call your poison control center right away.

What should I avoid while using AVAGE™ Cream?

• Do not become pregnant while using AVAGE® Cream. See the section "How should I use AVAGE™ Cream?" for more information. Use effective birth control while using AVAGE™ Cream, and be sure you are not pregnant before you start using AVAGE™ Cream.

• If you become pregnant while using AVAGE™ Cream, stop use and contact your doctor right away.

• AVAGE™ Cream makes you more sensitive to sunlight. It works only in patients who follow a sun avoidance program. Therefore, avoid sunlight as much as possible. Use cover-up clothing and sunscreens of at least SPF 15 during the day when using AVAGE™ Cream. Also, do not use sunlamps, unless your doctor tells you to.

• If you are sensitive to sunlight or in the sun a lot on your job, be especially careful to protect your skin. Use sunscreens and protective clothing. Stay out of the sun as much as possible.

• Avoid cosmetics, medicines and supplements that may make you more sensitive to sunlight, including Vitamin A.

What are the possible side effects of AVAGE™ Cream?

AVAGE™ can cause increased skin irritation and increased chance of sunburn.

While you use AVAGE™ Cream, strong wind or cold may irritate your skin more than usual.

The most common side effects of AVAGE™ (TAZAROTENE) Cream 0.1% are peeling, redness, burning, dryness, and irritated and itching skin. These are not all the side effects possible with AVAGE™ Cream. For more information, ask your doctor or pharmacist.

Tell your doctor if side effects become problems.Your doctor may adjust your dose of AVAGE™ Cream.However,the effectiveness of AVAGE™ Cream when used less often than once a day has not been proven.

What are the ingredients of AVAGE™ Cream? The active ingredient is tazarotene. The inactive ingredients are benzyl alcohol, carbomer 934P, carbomer l342, edetate disodium, medium chain triglycerides, mineral oil, purified water, sodium hydroxide, sodium thiosulfate, and sorbitan monooleate.

General advice about prescription medicines

This medicine is for your use only. Never give it to other people. It may harm them even if their skin problem appears to be the same as yours. Medicines are sometimes prescribed for conditions not mentioned in patient information leaflets. Do not use AVAGE™ Cream for a condition for which it was not prescribed. Do not use AVAGE™ Cream after the expiration date on the bottom seal of the tube.

Where can I get more information about AVAGE™ Cream?

You can contact Allergan by calling 800-433-8871. You can ask your doctor or pharmacist for the information about AVAGE™ Cream that is written for health professionals.

Tazorac Interactions

Concomitant dermatologic medications and cosmetics that have a strong drying effect should be avoided. It is also advisable to "rest" a patients skin until the effects of such preparations subside before use of AVAGE™ Cream is begun.

Carcinogenesis,Mutagenesis,Impairment of Fertility:

A long term study of tazarotene following oral administration of 0.025, 0.050, and 0.125 mg/kg/day to rats showed no indications of increased carcinogenic risks. Based on pharmacokinetic data from a shorter term study in rats, the highest dose of 0.125 mg/kg/day was anticipated to give systemic exposure in the rat equivalent to 1.4 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation.

In evaluation of photo co-carcinogenicity, median time to onset of tumors was decreased, and the number of tumors increased in hairless mice following chronic topical dosing with intercurrent exposure to ultraviolet radiation at tazarotene concentrations of 0.001%, 0.005%, and 0.01% in a gel formulation for up to 40 weeks. A long-term topical application study of up to 0.1% tazarotene in a gel formulation in mice terminated at 88 weeks showed that dose levels of 0.05, 0.125, 0.25, and 1.0 mg/kg/day (reduced to 0.5 mg/kg/day for males after 41 weeks due to severe dermal irritation) revealed no apparent carcinogenic effects when compared to vehicle control animals; untreated control animals were not completely evaluated. Systemic exposure (AUC0-12h) at the highest dose was 7.8 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation.

Tazorac was found to be non-mutagenic in the Ames assays using Salmonella and E. coli and did not produce structural chromosomal aberrations in a human lymphocyte assay. Tazorac was also non-mutagenic in the CHO/HGPRT mammalian cell forward gene mutation assay and was non-clastogenic in the in vivo mouse micronucleus test.

No impairment of fertility occurred in rats when male animals were treated for 70 days prior to mating and female animals were treated for 14 days prior to mating and continuing through gestation and lactation with topical doses of tazarotene gel up to 0.125 mg/kg/day. Based on data from another study, the systemic drug exposure in the rat would be equivalent to 1.2 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation.

No impairment of mating performance or fertility was observed in male rats treated for 70 days prior to mating with oral doses of up to 1.0 mg/kg/day tazarotene. That dose produced an AUC0-24h that was 3.7 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation.

No effect on parameters of mating performance or fertility was observed in female rats treated for 15 days prior to mating and continuing through day 7 of gestation with oral doses of tazarotene up to 2.0 mg/kg/day. However, there was a significant decrease in the number of estrous stages and an increase in developmental effects at that dose. That dose produced an AUC0-24h that was 6.7 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for signs of fine wrinkling and mottled hyperpigmentation.

Reproductive capabilities of F1 animals, including F2 survival and development, were not affected by topical administration of tazarotene gel to female F0 parental rats from gestation day 16 through lactation day 20 at the maximum tolerated dose of 0.125 mg/kg/day. Based on data from another study, the systemic drug exposure in the rat would be equivalent to 1.2 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation.

Pregnancy: Teratogenic Effects: Pregnancy Category X:

See CONTRAINDICATIONS section. Women of child-bearing potential should use adequate birth-control measures when AVAGE™ Cream is used. The possibility that a woman of childbearing potential is pregnant at the time of institution of therapy should be considered. A negative result for pregnancy test having a sensitivity down to at least 50 mIU/mL for hCG should be obtained within 2 weeks prior to AVAGE™ Cream therapy, which should begin during a normal menstrual period. There are no adequate and well-controlled studies in pregnant women. As a retinoid, tazarotene is a teratogenic substance, and it is not known what level of exposure is required for teratogenicity in humans. However, there may be less systemic exposure in the treatment of the face alone, due to less surface area for application (see CLINICAL PHARMACOLOGY: Pharmacokinetics).

Nursing mothers

After single topical doses of 14C-tazarotene gel to the skin of lactating rats, radioactivity was detected in milk, suggesting that there would be transfer of drug-related material to the offspring via milk. It is not known whether this drug is excreted in human milk. Caution should be exercised when tazarotene is administered to a nursing woman.

Pediatric Use

The safety and efficacy of tazarotene cream have not been established in patients under the age of 17 years with facial fine wrinkling, facial mottled hypo-and hyperpigmentation, and benign facial lentigines.

Geriatric Use

In the studies of facial fine wrinkling, facial mottled hypo- and hyperpigmentation, and benign facial lentigines , 44 male patients and 180 female patients out of the total population of 1131 patients were older than 65 years of age. No overall differences in safety or effectiveness were observed between these patients and younger patients, and other clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Tazorac Contraindications

Retinoids may cause fetal harm when administered to a pregnant woman.

In rats, tazarotene 0.05% gel administered topically during gestation days 6 through 17 at 0.25 mg/kg/day resulted in reduced fetal body weights and reduced skeletal ossification. Rabbits dosed topically with 0.25 mg/kg/day tazarotene gel during gestation days 6 through 18 were noted with single incidences of known retinoid malformations, including spina bifida, hydrocephaly, and heart anomalies.

Systemic exposure (AUC0-24h) to tazarotenic acid at topical doses of 0.25 mg/kg/day tazarotene in a gel formulation in rats and rabbits represented 2.4 and 26 times, respectively, the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation. As with other retinoids, when tazarotene was given orally to experimental animals, developmental delays were seen in rats, and teratogenic effects and post-implantation loss were observed in rats and rabbits at doses producing 2.1 and 52 times, respectively, the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for fine wrinkling and mottled hyperpigmentation. In a study of the effect of oral tazarotene on fertility and early embryonic development in rats, decreased number of implantation sites, decreased litter size, decreased number of live fetuses, and decreased fetal body weights, all classic developmental effects of retinoids, were observed when female rats were administered 2 mg/kg/day from 15 days before mating through gestation day 7. A low incidence of retinoid-related malformations at that dose were reported to be related to treatment. That dose produced an AUC0-24h that was 6.7 times the maximum AUC0-24h in patients treated with 2 mg/cm2 of tazarotene cream 0.1% over 15% body surface area for signs of fine wrinkling and mottled hyperpigmentation.

Systemic exposure to tazarotenic acid is dependent upon the extent of the body surface area treated. IN PATIENTS TREATED TOPICALLY OVER SUFFICIENT BODY SURFACE AREA, EXPOSURE COULD BE IN THE SAME ORDER OF MAGNITUDE AS IN THESE ORALLY TREATED ANIMALS. As a retinoid, tazarotene is a teratogenic substance, and it is not known what level of exposure is required for teratogenicity in humans. However, there may be less systemic exposure in the treatment of the face alone, due to less surface area for application.

There were thirteen reported pregnancies in patients who participated in clinical trials for topical tazarotene. Nine of the patients were found to have been treated with topical tazarotene, and the other four had been treated with vehicle. One of the patients who was treated with tazarotene cream elected to terminate the pregnancy for non-medical reasons unrelated to treatment. The other eight pregnant women who were inadvertently exposed to topical tazarotene during clinical trials subsequently delivered apparently healthy babies. As the exact timing and extent of exposure in relation to the gestation times are not certain, the significance of these findings is unknown. AVAGE™ Cream is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, treatment should be discontinued and the patient apprised of the potential hazard to the fetus. Women of child-bearing potential should be warned of the potential risk and use adequate birth-control measures when AVAGE™ Cream is used. The possibility that a woman of childbearing potential is pregnant at the time of institution of therapy should be considered. A negative result for pregnancy test having a sensitivity down to at least 50 mIU/mL for human chorionic gonadotropin (hCG) should be obtained within 2 weeks prior to AVAGE™ Cream therapy, which should begin during a normal menstrual period.

AVAGE™ Cream is contraindicated in individuals who have shown hypersensitivity to any of its components.

Generic name, Overdose, Half Life Tazorac, Food Interactions, Chemical, etc..

Tazorac see also FDA report

Brand Names containing Tazarotene

Chemical structure:
O O S N H H H H H H H H H H H H H H H H H H H H H C21H21NO2S 2D chemical structure C21H21NO2S SVG | 2D structure chemical names, chemical properties, classification C21H21NO2S