Usage
- Tazarotene is prescribed for the topical treatment of acne vulgaris (in the foam, gel, cream, and lotion formulations) and plaque psoriasis (in the cream and gel formulations) in adults and children over a certain age, depending on the formulation and condition being treated. It is also used to reduce fine facial wrinkles and certain types of dark and light spots on the face (in the 0.1% cream formulation).
- Pharmacological Classification: retinoid, specifically an acetylenic retinoid.
- Mechanism of Action: Tazarotene is a prodrug that is converted to its active form, tazarotenic acid, in the skin. Tazarotenic acid binds to retinoic acid receptors (RARs), specifically RARβ and RARγ, which regulate gene expression related to cell proliferation, differentiation, and inflammation, ultimately normalizing the abnormal keratinization and differentiation processes in the skin linked to acne and psoriasis.
Alternate Names
- Tazarotenic acid (active form)
- Brand Names: Tazorac, Avage, Fabior, Arazlo
How It Works
- Pharmacodynamics: Tazarotenic acid, the active metabolite, modulates gene expression by binding to specific nuclear retinoic acid receptors (RARs). This action leads to normalization of keratinocyte proliferation and differentiation, resulting in reduced inflammation and improved skin lesions in acne and psoriasis.
- Pharmacokinetics: Tazarotene is applied topically and is metabolized in the skin to tazarotenic acid. Systemic absorption is minimal, especially with proper application to affected areas only.
- Mode of Action: Tazarotene exerts its therapeutic effects by binding to RARβ and RARγ receptors in the skin. This binding influences gene expression, reduces inflammation, and normalizes cellular processes in the skin affected by acne or psoriasis.
- Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Binds to retinoic acid receptors (RARs), particularly RARβ and RARγ. Does not significantly inhibit enzymes or modulate neurotransmitters.
- Elimination Pathways: Primarily metabolized in the skin; minimal systemic absorption occurs, after which it is conjugated and excreted in urine and feces.
Dosage
Standard Dosage
Adults:
- Acne:
- Cream/Gel (0.05% or 0.1%): Apply a thin film to the affected area(s) once daily, in the evening. Start with 0.05% and increase to 0.1% if tolerated and medically necessary.
- Foam (0.1%): Apply a small amount to the affected area(s) once daily, in the evening.
- Lotion (0.045%): Apply a thin layer to the affected area(s) once daily.
- Psoriasis:
- Cream/Gel (0.05% or 0.1%): Apply a thin film to the affected area(s) once daily, in the evening. Start with 0.05% and increase to 0.1% if tolerated and medically necessary. Do not apply to more than 20% of body surface area.
- Fine facial wrinkles/dark spots:
- Cream (0.1%): Apply a pea-sized amount to the entire face once daily at bedtime.
Children:
- Acne:
- Cream/Gel/Foam (0.1%): Apply a thin film to the affected area(s) once daily, in the evening (for children 12 years and older).
- Lotion (0.045%): Apply a thin layer to the affected area(s) once daily (for children 9 years and older).
- Psoriasis: Use and dose must be determined by the doctor.
- Pediatric Safety Considerations: Safety and efficacy in children younger than the specified ages have not been established. Use with caution in the pediatric population.
Special Cases:
- Elderly Patients: Use with caution; no dosage adjustment is specifically recommended, but monitor for increased sensitivity.
- Patients with Renal Impairment: No specific dosage adjustment is necessary due to minimal systemic absorption.
- Patients with Hepatic Dysfunction: No specific dosage adjustment is necessary due to minimal systemic absorption.
- Patients with Comorbid Conditions: Consider individual patient factors and monitor for any potential drug interactions.
Clinical Use Cases
Tazarotene is intended for topical dermatological use and is not indicated for:
- Intubation
- Surgical Procedures
- Mechanical Ventilation
- Intensive Care Unit (ICU) Use
- Emergency Situations
Dosage Adjustments
- Adjust dosage based on tolerability and clinical response. Reduce the frequency of application or concentration if irritation occurs.
Side Effects
Common Side Effects:
- Skin irritation (burning, stinging, itching, redness, dryness, peeling) at the application site.
Rare but Serious Side Effects:
- Severe allergic reactions (e.g., swelling of the face, lips, or tongue, difficulty breathing)
Long-Term Effects:
- Skin discoloration (hyperpigmentation or hypopigmentation) which is usually reversible upon discontinuation.
Adverse Drug Reactions (ADR)
- Severe skin reactions (e.g., blistering, severe burning/stinging).
Contraindications
- Pregnancy
- Hypersensitivity to tazarotene or any component of the formulation
Drug Interactions
- Concomitant use of other topical medications on the same area, especially those with drying or irritant effects, may increase the risk of skin irritation.
- Photosensitizing medications may exacerbate sun sensitivity.
- Use caution with products containing benzoyl peroxide, sulfur, resorcinol, or salicylic acid.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: X (Contraindicated)
- Fetal Risks: Tazarotene is teratogenic and should not be used during pregnancy.
- Breastfeeding: Not known if tazarotene is excreted in breast milk. Exercise caution and avoid applying to areas that may come in contact with the infant.
Drug Profile Summary
- Mechanism of Action: Retinoid; binds to RAR receptors, normalizing skin cell proliferation and differentiation.
- Side Effects: Skin irritation (burning, stinging, itching, redness, dryness), allergic reactions.
- Contraindications: Pregnancy, hypersensitivity.
- Drug Interactions: Other topical medications, photosensitizing drugs.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy; caution during breastfeeding.
- Dosage: Topical application, once daily; varies depending on the formulation and condition.
- Monitoring Parameters: Monitor skin for irritation and treatment efficacy.
Popular Combinations
- No specific popular drug combinations are recommended with topical tazarotene.
Precautions
- General Precautions: Avoid contact with eyes, lips, and mucous membranes. Wash hands thoroughly after application.
- Specific Populations:
- Pregnant Women: Contraindicated.
- Breastfeeding Mothers: Use with caution; avoid applying to areas that may come in contact with the infant.
- Children & Elderly: Use as directed and monitor for increased sensitivity.
- Lifestyle Considerations: Protect treated skin from sunlight. Use sunscreen and protective clothing.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Tazarotene?
A: Dosage depends on the formulation, the condition being treated, and the patient’s age. Consult the Dosage section above for specific information.
Q2: Can Tazarotene be used during pregnancy?
A: No, Tazarotene is contraindicated during pregnancy due to its teratogenic effects.
Q3: Is Tazarotene safe to use while breastfeeding?
A: It is unknown whether tazarotene is excreted in breast milk. Caution should be exercised. Avoid applying to areas that may come into contact with the nursing infant.
Q4: What are the most common side effects of Tazarotene?
A: The most common side effects are local skin reactions, including burning, stinging, itching, redness, dryness, and peeling.
Q5: How should Tazarotene be applied?
A: Apply a thin film to the affected areas once daily, usually in the evening, after cleansing the skin. Avoid application to unaffected skin or mucous membranes.
Q6: How long does it take to see results with Tazarotene?
A: Improvement is usually seen within 4-12 weeks of initiating treatment. However, optimal results may require longer-term therapy.
Q7: What should I do if I experience skin irritation with Tazarotene?
A: If skin irritation occurs, you may reduce the frequency of application, reduce the concentration used (e.g., from 0.1% to 0.05%), or temporarily discontinue use until the irritation subsides. Consult your physician for guidance.
Q8: Can Tazarotene be used with other topical acne medications?
A: Concomitant use of other topical medications on the same area, especially those with drying or irritant effects, may increase the risk of skin irritation. Use caution and consult your physician before combining tazarotene with other topical acne treatments.
Q9: Does Tazarotene make skin more sensitive to the sun?
A: Yes, tazarotene can increase photosensitivity. It’s essential to use sunscreen with an SPF of 30 or higher and wear protective clothing when exposed to sunlight while using tazarotene.
