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Tazarotene - Usage, Dosage, Side Effects, Drug Warnings, and Precautions

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Tazarotene is an acetylenic retinoid group of medications used to treat fine wrinkles, mottled skin pigmentation, acne vulgaris, and plaque psoriasis.

Medically reviewed by

Dr. Nagaraj

Published At January 3, 2023
Reviewed AtJune 15, 2023

Introduction.

Tazarotene in topical formulations like foam, gel, and lotion is used to treat acne. This medicine helps clear acne on the face by keeping the skin pores clear. Tazarotene, a 0.1 % cream, is used to reduce fine facial wrinkles and dark and light spots in patients with a total skin care program and prevent exposure to sunlight. In addition, Tazarotene topical cream and gel are used in treating Psoriasis. It treats plaque psoriasis. It does not make the skin red and reduces the number and size of lesions on the skin.

This product is available in the following dosage forms:

  • Foam.

  • Gel or Jelly.

  • Lotion.

  • Cream.

Why Is Tazarotene Prescribed?

Tazarotene is an acne medicine. Tazarotene treats Psoriasis, a skin disease that forms red scaly patches on specific body areas. In addition, Tazarotene decreases facial wrinkles and discoloration in people who use skin care and sunlight protection programs. Tazarotene is a medication group called retinoids. It is used to treat acne and Psoriasis. It slows skin cell growth and decreases skin inflammation, leading to acne and Psoriasis.

Pharmacodynamics of Tazarotene

After topical application, Tazarotene is esterase hydrolyzed to form an active metabolite, Tazarotene acid. While treating acne, Tazarotene is taken in conjunction with an oral antibiotic. Tazarotene reduces mottling and hyperpigmentation, sallowness, fine wrinkling, and coarse wrinkling in sun-damaged skin.

Long-term use of Tazarotene is associated with a comprehensive reduction in atypical melanocytes and keratinocytes cells. These cells are precursors of skin cancer. In addition, long-term use of Tazarotene is associated with increased collagen production and better organization of skin collagen bundles.

Mechanism of Action

An active form of the drug is Tazarotene acid which binds to three of the retinoic acid receptor (RAR) family: RARa, RARb, and RARg, and has relative selectivity for RARb, and RARg and can modify gene expression. In addition, it has an affinity for RXR receptors.

Absorption

Minimal systemic absorption of Tazarotene occurs because of rapid metabolism in the skin to the active metabolite, Tazarotene acid. This acid is systemically absorbed and again metabolized.

Protein Binding: The active form of the drug, Tazarotene acid, has high binding to plasma proteins.

Metabolism

Tazarotene undergoes esterase hydrolysis in the skin to form an active metabolite. Tazarotenic acid is metabolized in the skin and, after systemic absorption, metabolized in the liver to sulfoxides, sulfones, and products for elimination.

Route of Elimination

Tazarotene and tazarotenic acid is metabolized to sulfoxides and sulfones, eliminated through urinary and fecal pathways.

Half-life

The half-life of the active form of the drug, tazarotenic acid, is around 18 hours.

Toxicity

Excessive topical use can cause redness, peeling, or discomfort. In addition, oral ingestion of the drug can affect liver function and cause hypertriglyceridemia. Other symptoms include conjunctival irritation, hair loss, headache, edema, fatigue, dermatitis, nausea, and visual disturbances.

How Should Tazarotene Be Used?

  • Tazarotene is available as a cream, foam, or gel that can be applied to the skin. It is generally used one time a day, mainly in the evening. However, it is recommended to use Tazarotene around the same time of the day.

  • It is recommended to follow the directions on the prescription label and, if needed, seek help from the doctor or pharmacist and understand the procedure. The use of Tazarotene should be precise as directed by the physician. It should be used in the amount that the doctor prescribes.

  • Depending on the betterment of the condition and the side effects experienced, the strength of Tazarotene can be adjusted, or the frequency of administration of the dose can be changed. We can temporarily discontinue the treatment. Make sure that the doctor knows the response to the treatment.

  • If Tazarotene treats acne, symptoms improve in around four weeks. However, symptoms improve in 1 to 4 weeks when Tazarotene is used to treat Psoriasis. Therefore, Tazarotene foam should be well shaken before use.

  • Tazarotene foam is flammable and can catch fire. Therefore, it is recommended to stay away from open fire and flames and not smoke while applying Tazarotene foam.

  • Tazarotene should not be applied to sunburned, irritated, scraped, or covered with eczema, a skin disease. In such conditions, Tazarotene should not be applied to that area until the skin has healed completely. Moisturizers should be used and fully absorbed in the skin before applying Tazarotene.

The following steps should be followed to use the cream, foam, and gel.

  • If Tazarotene is used to treat acne or reduce wrinkles and discoloration on the face, wash the face with mild soap and water, and pat the face dry using a soft towel. If Tazarotene is used to treat Psoriasis, it is unnecessary to wash the affected skin first, but if washed, the skin should be dry before applying Tazarotene.

  • Apply a thin layer of formulation to the affected skin area. If Tazarotene is used to reduce facial wrinkling and discoloration, apply it to the eyelids. Massage it into the skin. Be careful about contact with Tazarotene.

  • Do not cover the area either with bandages or dressings. Instead, wash your hands with soap and water after handling the medication.

  • Ask for the manufacturer's information brochure.

What Special Precautions to Follow While Using Tazarotene?

Before taking Tazarotene,

  • Inform the doctor and pharmacist about allergies to Tazarotene or any ingredients in Tazarotene cream, foam, or gel.

  • Inform the doctor and pharmacist about prescription and nonprescription medications, vitamins, and nutritional supplements.

The following components are found in Tazarotene:

  • Chlorothiazide.

  • Chlorpromazine; Chlorthalidone.

  • Fluphenazine.

  • Fluoroquinolone antibiotics such as

  • Ciprofloxacin, Gemifloxacin, Levofloxacin, Moxifloxacin, and Ofloxacin; Hydrochlorothiazide, Indapamide; Methyclothiazide; Metolazone; Perphenazine; Prochlorperazine; Sulfonamide medications like Co-trimoxazole, and Sulfisoxazole like Erythromycin ethyl succinate and Sulfisoxazole acetyl; Tetracycline antibiotics, such as Doxycycline, Tetracycline, and Tigecycline; Thioridazine; Trifluoperazine; and vitamin A supplements.

  • The doses of medications may need to be altered, or careful monitoring has to be done to look for side effects.

  • If benzoyl peroxide is used, it should be applied at different times of day and should not clash with Tazarotene.

  • Inform the doctor about personal or family history of skin cancer, eczema, any other skin condition, or skin sensitivity to sunlight.

  • Inform the physician about pregnancy, plan to be pregnant, or breastfeeding. It is not advised to get pregnant while using Tazarotene. Know from the doctor about birth control methods to be used during the treatment.

  • If you need to start the treatment, a negative pregnancy test within two weeks before beginning the therapy is required. Tazarotene can be started during the menstrual period to avoid the risk of becoming pregnant.

  • If pregnancy occurs while using Tazarotene, discontinue using Tazarotene and call the doctor immediately. Tazarotene can harm the fetus.

  • Avoid prolonged exposure to sunlight, tan beds, and sunlamps. Wear protective clothing, sunglasses, and sunscreen with a higher SPF. Avoid prolonged exposure to cold or wind. Tazarotene causes skin sensitivity to sunlight or extreme weather.

  • Inform the doctor about all skin or hair care products, including soaps, shampoos, wave solutions, cleansers, moisturizers, and cosmetics. Many skin care products irritate the skin if such products are used with Tazarotene.

  • These products are already harsh; they dry the skin and contain alcohol, spices, or lime rind. If these products are used for a long time, it is recommended to wait before using Tazarotene. Instead, look for recommended products that will not irritate the skin.

  • Avoid Tazarotene contact with the eyes. If Tazarotene contacts the eyes, wash with plenty of water.

  • Avoid using hot wax or electrolysis to remove unwanted hair from the area of application of Tazarotene.

What Special Instructions Should Be Followed?

  • Unless recommended, continue with everyday dietary habits.

  • If using Tazarotene gel and a dose is missed, it is better to skip the missed dose and continue the regular dosing schedule.

  • If using Tazarotene cream or foam, apply the missed dose as soon as possible. However, if it is time for the next dose, skip the missed dose and continue with the regular dosing schedule.

  • Do not apply extra medicine to compensate for a missed dose.

What Are the Side Effects of Tazarotene?

Tazarotene may cause specific side effects.

The following symptoms affect the skin treated with Tazarotene. Inform the doctor in case the following symptoms are seen.

  • Itching.

  • Burning.

  • Redness.

  • Rash.

  • Peeling.

  • Stinging.

  • Pain.

  • Dryness.

  • Swelling.

  • Discoloration.

  • Swelling of the eyelid or eye.

  • Irritated eyes.

  • Chapped or inflamed lips.

  • Swelling in arms or legs.

  • Tazarotene can also cause other side effects. Inform the doctor in case of unusual problems with this medication. If a severe side effect is seen, send a report to the Food and Drug Administration's (FDA) - Adverse Event Reporting program.

How Is Tazarotene Stored and Disposed of?

  • Keep the medication in the container in which it was received, closed, and out of reach of the kids. Store it at room temperature, away from heat and moisture.

  • Do not freeze.

  • Tazarotene foam is flammable, so keep it away from flames and extreme heat. Don't try to puncture or incinerate the Tazarotene foam container.

  • Medications not in use should be disposed of to ensure that pets, children, and others cannot consume them. However, do not flush this medication down the toilet.

  • The best way to dispose of the medication is through a medicine take-back program. Knowing about the garbage or recycling department is good for learning about the community take-back programs.

  • It is necessary to keep all medication out of sight and reach of children in the form of weekly pill minders, and eye drops, creams, patches, and inhalers are not child-resistant, and children can open them easily.

  • To protect children from poisoning, always lock safety caps and place the medication safely away from sight and reach.

  • In case of emergency/overdose, call the local poison control center if someone swallows Tazarotene. Also, call local emergency services if the victim has collapsed or is not breathing.

Brand Names

  • Average.

  • Fabior.

  • Tazorac.

  • Duobrii is available as a combination product containing Halobetasol and Tazarotene.

Drug Interactions of Tazarotene

1. Carcinogenesis, Mutagenesis, Impairment of Fertility:

A long-term study of Tazarotene after oral administration of 0.025, 0.050, and 0.125 mg/kg/day to rats showed no increased carcinogenic risks.

2. Pregnancy:

Teratogenic Effects: Women of childbearing age should use proper birth-control measures

3. Nursing Mothers:

After single topical doses of 14C Tazarotene to the skin of lactating rats, radioactivity was detected in milk, suggesting that there would be a transfer of drug-related material to the offspring via milk.

4. Pediatric Use:

The safety and efficacy of Tazarotene are not apparent in pediatric patients under the age of 12 years.

5. Geriatric Use:

Subjects over 65 years show adverse effects and lower treatment success rates.

Review of the Literature

  • Tazarotene Revisited: Safety and efficacy in plaque Psoriasis and its emerging role in treatment strategy by Tanghetti E states Psoriasis is a chronic, immune-related disease having different clinical expressions. Treatment options are relieving symptoms, reducing inflammation and induration, and controlling the disease. Tazarotene has been used to treat Psoriasis in cases of acne. Tazarotene is very effective for plaque psoriasis and reduces plaque and scaling. However, the efficacy of the medication is dose and formulation-dependent, and erythema is not responsive. The common side effect is mild-to-moderate irritation. Effectiveness improves with topical corticosteroids. Tazarotene increases epidermal thickness and reduces steroid-induced atrophy. Tazarotene is an effective psoriasis treatment that improves with topical corticosteroids and a new combination of Tazarotene and Halobetasol.

  • Pharmacokinetics of Tazarotene and acitretin in Psoriasis, Michael S. Heath reviews Psoriasis as a cutaneous condition with physical and psychological outcomes. Tazarotene and acitretin are the only approved retinoids for treating Psoriasis. Topical Tazarotene and oral acitretin act on retinoic acid receptors and retinoid-X-receptors, producing an altered gene expression of inflammatory cytokines and inhibiting keratinocyte proliferation. Tazarotene and acitretin are effective for Psoriasis. It does not cause immunosuppression and helps treat inflammatory Psoriasis. Combined with topical and systemic agents, retinoids improve clinical outcomes and lower the treatment threshold. However, topical adherence and side effects limit the use of retinoids.

  • Review of Characteristics and Analytical Methods of Tazarotene: Tazarotene is the first topical receptor-selective retinoid prodrug derived from vitamin A and used for managing plaque psoriasis and is efficacious in acne vulgaris and photoaging. FDA approved 0.1 % strength of TZR for the treatment of acne. Therefore, TZR is required for alternative methods for routine quality control and to estimate TZR in pharmaceutical dosage form, especially in pharmacokinetic studies of topical preparation.
Dr. Nagaraj
Dr. Nagaraj

Diabetology

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