DERIVA AQUEOUS GEL

Indications

• Acne vulgaris
• Facial acne vulgaris
• Infantile acne

Dosage

Children: Child 12–17 years: Apply once daily in the evening. For infants (1 month–1 year), consult specific guidelines or refer to BNF for Children.

Adults: Apply once daily to the affected area in the evening. Discontinue use if irritation occurs.

Mechanism of action

Adapalene acts by modulating the differentiation and proliferation of epithelial cells and has anti-inflammatory properties. It binds to specific retinoic acid receptors in the skin, influencing gene expression to promote normal skin cell turnover.

Pharmacodynamics

Adapalene demonstrates anti-acne activity by normalizing the process of keratinization and reducing the formation of comedones (blocked pores), while also exerting anti-inflammatory effects that help to reduce redness and swelling associated with acne.

Pharmacokinetics

Adapalene is minimally absorbed through the skin. Its systemic absorption is low, resulting in a reduced risk of systemic side effects. The pharmacokinetics profile indicates that it is metabolized in the liver, with a majority of the drug excreted in urine.

Contra-indications

• Hypersensitivity to adapalene or any excipients
• Eczematous, broken, or sunburned skin
• Use in patients with sensitive skin

Adverse effects

• Skin reactions
• Facial swelling
• Cheilitis
• Angioedema
• Eye swelling

Interactions

• Avoid contact with eyes, nostrils, mouth, and mucous membranes
• Caution with other retinoids

Precautions

• Avoid excessive exposure to sunlight
• Introduce at reduced frequency in sensitive areas
• Avoid accumulation in angles of the nose

Pregnancy

Avoid use during pregnancy due to potential risks.

Breast-feeding

Consult healthcare provider before use; safety not established.

Storage

Store at room temperature, protected from light and moisture.

Formulations

• Cream
• Gel

Mechanism of action

Adapalene is used for the treatment/maintenance of mild-to-severe acne (acne vulgaris). Acne is a multifactorial condition, and evidence exists to support multiple mechanisms of action for adapalene. Adapalene binds to retinoic acid receptor (RAR)-beta and RAR-gamma; this complex subsequently binds to one of three retinoid X receptors (RXRs), which as a complex is capable of binding DNA to modulate transcriptional activity. Although the full extent of transcriptional modulation is not described, retinoid activation is generally known to affect cellular proliferation and differentiation, and adapalene has been shown to inhibit HeLa cell proliferation and human keratinocyte differentiation. These effects primarily account for adapalene's comedolytic and anticomedogenic properties. In addition, adapalene modulates the immune response by down-regulating toll-like receptor 2 (TLR-2) expression and inhibiting the transcription factor activator protein 1 (AP-1). TLR-2 recognizes _Cutibacterium acnes_ (formerly _Propionibacterium acnes_), the bacterium primarily associated with acne. TLR-2 activation causes nuclear translocation of AP-1 and downstream pro-inflammatory gene regulation. Therefore, adapalene has a general anti-inflammatory effect, which reduces inflammation-mediated acne symptoms. When used with benzoyl peroxide, which possesses free radical-mediated bactericidal effects, the combination acts synergistically to reduced comedones and inflammatory lesions.

Pharmacodynamics

Adapalene is anticomedogenic, preventing the formation of new comedones and inflammatory lesions, and also acts to reduce inflammation by modulating the innate immune response. Like other retinoid compounds, adapalene is chemically stable but photosensitive; use with sunscreen is recommended. Minor skin irritations, including erythema, scaling, dryness, and stinging/burning, have been reported.