Adapalene gel /Adapalene is a topical retinoid-like compound, chemically similar to vitamin A. Although the exact mechanism of action is unknown, adapalene binds to specific retinoic acid receptors in the nucleus, leading to specific gene expression. This agent stimulates skin growth through modulation of cellular differentiation, inflammatory processes, and keratinization of follicular epithelial cells. Adapalene may increase dermal sensitivity to ultraviolet radiation. (NCI04)
Adapalene is a naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether. It has a role as a dermatologic drug, a non-steroidal anti-inflammatory drug, and an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor. It is a monocarboxylic acid, a member of adamantanes and a naphthoic acid. It derives from a CD437.
Adapalene is a member of the retinoid drug class that is typically found in topical formulations used for the treatment of acne. It may be used to treat keratosis pilaris as well as other skin conditions as off-label use. It is marketed by Galderma under the trade names Differin and Adaferin.
Mechanism of Action of Adapalene
Mechanistically, adapalene binds to specific retinoic acid nuclear receptors (gamma and beta) and retinoid X receptors but does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, it is suggested that topical adapalene may normalize the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.
Indications of Adapalene gel
- For the topical treatment of comedo, papular and pustular acne (acne vulgaris) of the face, chest or back.
- Acne Vulgaris
- Acne vulgaris of the back
- Acne vulgaris of the chest
- Acne vulgaris of the face
- Per the recommendations – of the Global Alliance on Improving Outcomes of Acne, retinoids such as adapalene are considered first-line therapy in acne treatment and are to be used either independently or in conjunction with benzoyl peroxide and/or an antimicrobial agent for maximum efficacy.[rx][rx]
- Furthermore, adapalene – like other retinoids, increases the efficacy and penetration of other topical acne medications that are used in conjunction with topical retinoids as well as hastens the improvement of the post-inflammatory hyperpigmentation caused by acne.[rx] In the long term, it can be used as maintenance therapy.[rx]
- While adapalene – is often thought to be the least efficacious of the retinoid medications, two multicenter randomized double-blinded studies showed that the use of adapalene 0.1% lotion for 12 weeks improved inflammatory and noninflammatory acne as well as reduced the total lesion count from baseline in those patients in the treatment group.[rx]
- Other non-FDA approved – indications that have been reported in the literature include treatment of verruca Vulgaris, molluscum contagiosum, Darier disease, photoaging, pigmentary disorders, actinic keratoses, and alopecia areata.[rx]
- A study has concluded that adapalene gel 0.1% under occlusion is an effective, safe and easy to use treatment for plantar warts and may help clear lesions faster than cryo-therapy.[rx]
Contraindications of Adapalene gel
- Skin rash with sloughing
- Increased sensitivity of the skin to the sun
- Pregnancy
- Avoid eyes, lips, and mucous membranes.
- For external use only.
- Minimize UV light exposure; use sunscreen and protective clothing.
- Extreme weather (e.g., wind, cold) may cause skin irritation.
- Adverse reaction risk higher during the first month of treatment; generally subsides with use.
- Allergies to Benzoyl Peroxide
Dosage of Adapalene
Strengths: 0.1%; 0.3%
Acne
- Usual dose: Apply a thin layer to the affected area once a day at bedtime
Pediatric Dose for Acne
12 years and older
- Usual dose: Apply a thin layer to the affected area once a day at bedtime
Side Effects of Adapalene
More common
- Burning sensation or stinging of the skin
- Allergic dermatitis/allergic contact dermatitis, rash, eczema, skin discoloration
- Worsening of acne
- Dryness and peeling of skin
- Itching of skin
- Redness of skin
Common
- Skin irritation, sunburn
- burning or stinging
- discomfort
- dry skin
- itchiness
- peeling
- redness
- skin irritation
- sunburn
Rare
- Skin irritation, sunburn
- Contact dermatitis, eczema,
- dermatitis,
- skin discomfort pain,
- skin exfoliation,
- acne flares,
- skin swelling
- excessively dry, red, swollen, or blistered skin
Drug Interactions of Adapalene
- aminolevulinic acid
- aminolevulinic acid topical
- benzoyl peroxide topical
- isotretinoin
- methoxsalen
- methyl aminolevulinate topical
- resorcinol topical
- salicylic acid topical
- sulfur topical
- verteporfin
Pregnancy Category of Adapalene gel
FDA Pregnancy Category – C
Pregnancy
Women who are pregnant or considering pregnancy should not use adapalene. Women who use adapalene should ensure that they are using adequate birth control while they are using this medication.
Breast-feeding
It is not known if adapalene passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children under the age of 12.
Home Advice
- Patients should be counseled on using appropriate sun protection while on therapy.
- Patients should be instructed to wash the affected area with mild, non-medicated soap and pat the area dry before application. Patients should be told to avoid washing the area too frequently or scrubbing the skin too hard.
- Patients should be warned that benefits may not be seen for up to 12 weeks; initially, acne may look worse, but patients should not discontinue use during this time.
- Patients should be told to avoid contact with extremes in weather, other topical drugs, agents with strong drying effects, preparations with high alcohol concentrations, abrasive soaps, astringents, spices, and/or lime or lime peels to decrease the risk of skin irritation.
- Patients should be advised to speak to their healthcare provider if they are pregnant, intend to become pregnant, or are breastfeeding.
References
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