Zonyra 0.005%15 gm

Zonyra 0.005% is a topical retinoid indicated for the treatment of acne vulgaris in patients 9 years of age and older.

• Established/FDA-approved use: Topical treatment of acne vulgaris of the face and/or trunk (back, chest, and shoulders) — Zonyra 0.005% is one of the few topical retinoids specifically studied and approved for truncal acne.

Use of Zonyra 0.005% for dermatologic conditions other than acne vulgaris has not been established and is not recommended.

Each gram of Trifarotene cream contains Trifarotene 0.005% (50 mcg/g) in a cream base intended for external topical application.

Zonyra 0.005% is a fourth-generation synthetic topical retinoid that selectively targets the retinoic acid receptor gamma (RAR-γ), the predominant retinoic acid receptor subtype found in human skin. It is formulated as a once-daily topical cream for the treatment of acne vulgaris affecting the face and trunk.

Zonyra 0.005% belongs to the topical retinoid class of medications, specifically a fourth-generation retinoid selective for the RAR-gamma receptor. It is classified as a topical anti-acne agent.

Mechanism of Action

Trifarotene is a retinoic acid receptor (RAR) agonist with selective, high-affinity activity at the RAR-gamma subtype, the most abundant RAR in the epidermis. By binding RAR-gamma (which heterodimerizes with retinoid X receptors), Trifarotene modulates gene transcription involved in keratinocyte differentiation and proliferation, and exerts anti-inflammatory effects on pathways implicated in acne pathogenesis.

Pharmacokinetics

• Absorption: Low systemic absorption with topical use; plasma concentrations reach steady state within about 2 weeks of once-daily application, with peak levels typically in the low picogram/mL range.
• Metabolism: Primarily hepatic, via CYP2C9, CYP3A4, and CYP2C8.
• Elimination half-life: Approximately 2-9 hours.
• Excretion: Predominantly fecal.

Zonyra 0.005% is for external, topical use only.

• Wash and gently dry the skin before application.
• Apply only once daily, in the evening.
• Use the recommended amount per pump; do not exceed the recommended amount or frequency.
• Avoid contact with the eyes, lips, corners of the nose, and mucous membranes; rinse thoroughly with water if accidental contact occurs.
• Wash hands after applying Zonyra 0.005%.
• Do not apply to cut, abraded, eczematous, or sunburned skin.

Zonyra 0.005% is applied topically with minimal systemic absorption, so clinically significant systemic drug interactions are not expected. Zonyra 0.005% has not been shown to alter circulating levels of oral hormonal contraceptives.

• Other topical retinoids, strong exfoliants, or high-concentration benzoyl peroxide: Concomitant use of other potentially irritating topical products with Zonyra 0.005% may increase skin irritation and is not recommended unless specifically directed by a physician.
• Photosensitizing agents: Concurrent use of other drugs that increase photosensitivity may add to the sun-sensitivity risk associated with Zonyra 0.005% (see Precautions and Warnings).

The most commonly reported adverse reactions with Zonyra 0.005% are local skin reactions, generally most pronounced during the first 4 weeks of treatment and decreasing thereafter:

• Application-site irritation (erythema/redness)
• Scaling and dryness
• Stinging or burning sensation
• Pruritus (itching) at the application site
• Sunburn or increased sun sensitivity

Severe or persistent irritation, blistering, or signs of an allergic reaction (rash, swelling, difficulty breathing) with Zonyra 0.005% should prompt discontinuation and medical evaluation.

Pregnancy

Zonyra 0.005% should not be used during pregnancy. Although systemic absorption from topical use is low, retinoids as a class carry a risk of fetal harm, and human data on Zonyra 0.005% use in pregnant women are limited. Use only if clearly needed and after consulting a physician; women of reproductive potential should use effective contraception while using Zonyra 0.005%.

Lactation

It is not known whether topical Zonyra 0.005% passes into breast milk in clinically relevant amounts. If used while breastfeeding, apply Zonyra 0.005% to the smallest area of skin needed and for the shortest duration, and avoid application to the nipple/areola area. Consult a physician before using Zonyra 0.005% while breastfeeding.

Skin Irritation

Erythema, scaling, dryness, and stinging/burning are common with Zonyra 0.005%, especially in the first few weeks of use. If irritation is significant, reduce application frequency, use a moisturizer, or temporarily suspend treatment, then resume as tolerated.

Photosensitivity

Zonyra 0.005% may increase skin sensitivity to sunlight. Minimize sun exposure and use of sunlamps/tanning beds during treatment; use sunscreen and protective clothing over treated areas when sun exposure cannot be avoided.

Avoid Irritated or Damaged Skin

Do not apply Zonyra 0.005% to eczematous, sunburned, windburned, or broken/abraded skin.

Concomitant Topical Products

Avoid concurrent use of other potentially irritating topical products (other retinoids, strong exfoliants, high-concentration benzoyl peroxide, astringents) with Zonyra 0.005% unless directed by a physician (see Interactions).

Application Area and Frequency

Do not exceed the labeled application area or frequency; applying more Zonyra 0.005% than directed increases irritation without added benefit.

Not for Oral, Ophthalmic, or Mucosal Use

Zonyra 0.005% is for external skin use only; avoid contact with the eyes, lips, and mucous membranes.

Zonyra 0.005% is intended for topical use only. Excessive application does not speed improvement and instead increases the risk of local skin irritation, redness, and peeling. Accidental ingestion of Zonyra 0.005% cream is unlikely to cause serious systemic toxicity given its minimal systemic absorption; however, if a large amount is swallowed or a severe reaction occurs, seek immediate medical attention or contact a poison control center/emergency services. Do not attempt home treatment of a suspected overdose.

Store Zonyra 0.005% cream at room temperature, between 20°C and 25°C (68°F-77°F); brief exposure to 15°C-30°C during travel is permitted. Keep the tube/pump tightly closed and away from excessive heat and direct light. Keep out of reach of children.

Pediatric

Safety and efficacy of Zonyra 0.005% are established in patients 9 to 17 years of age for acne vulgaris. Safety and efficacy in children under 9 years have not been established.

Geriatric

Clinical studies of Zonyra 0.005% did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger adults.

Renal/Hepatic Impairment

No specific dose-adjustment data are available for Zonyra 0.005% in renal or hepatic impairment; given minimal systemic absorption with topical use, clinically significant effects are not expected, but physician guidance is advised.

Improvement with Zonyra 0.005% is typically evaluated after approximately 12 weeks of consistent, once-daily use; benefit may continue to accrue with longer-term treatment (studied for up to 52 weeks). Treatment duration should be individualized by the prescribing physician based on response and tolerability. Do not stop or restart Zonyra 0.005% without medical advice.

Topical retinoid; fourth-generation retinoic acid receptor (RAR) agonist selective for RAR-gamma.

Trifarotene selectively binds and activates the retinoic acid receptor gamma (RAR-γ), the dominant RAR subtype in skin, modulating expression of genes that regulate keratinocyte differentiation, proliferation, and inflammatory pathways involved in the formation of acne comedones and lesions.

Zonyra 0.005% is approved for use in patients 9 years of age and older for acne vulgaris of the face and/or trunk. Safety and efficacy in children younger than 9 years have not been established, and Zonyra 0.005% should not be used in this age group.