ACNAL

Acne vulgaris is a multifactorial disorder of the pilosebaceous unit involving increased sebum production, inflammation, and hyperproliferation/hyperkeratinization of the follicular infundibulum.

It is also associated with

Cutibacterium acnes (also known as Propionibacterium acnes ).

Adapalene is a third-generation topical retinoid used for the treatment of acne vulgaris.

Adapalene has similar efficacy but a superior safety profile compared to tretinoin.

Tazarotene is more efficacious than adapalene but is designated as pregnancy category X and hence is contraindicated in pregnant women.

Adapalene can also be combined with benzoyl peroxide (BPO), which possesses bactericidal properties 6, and either adapalene alone, or adapalene BPO combination products, are commonly used to treat mild-to-severe acne.

Differin®, produced by Galderma Labs, was first granted FDA approval on May 31st, 1996, as a 0.1% adapalene topical solution.

Differin was later made available as 0.1% gel, cream, or lotion, or 0.3% gel products.

On December 8th, 2008, Galderma Labs gained FDA approval for Epiduo®, a 0.1% adapalene, 2.5% BPO combination gel.

Adapalene is indicated for the topical treatment of acne vulgaris in patients aged and over.

It is also indicated for acne vulgaris in combination with benzoyl peroxide and in a triple combination therapy with benzoyl peroxide and clindamycin.

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.

Retinoic acid receptor beta Agonist Retinoic acid receptor gamma Agonist Retinoic acid receptor RXR-beta Agonist + 4 more targets.

Adapalene is applied topically and absorbed through the skin.

In one clinical study treating patients once per day with 2 g of 0.3% gel applied to 2 mg/cm of skin, 15 patients had detectable blood plasma adapalene levels (0.1 ng/ml) resulting in a mean C max of 0.553 ± 0.466 ng/ml and a mean AUC of 8.37 ± 8.46 ng*h/ml on day 10.

Extensive information regarding adapalene metabolism in humans is unavailable, although it is known to accumulate in the liver and GI-tract.

In human, mouse, rat, rabbit, and dog cultured hepatocytes, metabolism appears to affect the methoxybenzene moiety but remains incompletely characterized.

The major products of metabolism are glucuronides.

Approximately 25% of the drug is metabolized; the rest is excreted as parent drug.

Adapalene is primarily excreted by the biliary route at about 30 ng/g of the topically applied amount.

In one clinical study, after ten days of treatment with 2 g of 0.3% cream or gel, the terminal half-life was between and 51 hours, with a mean of 17.2 ± 10.2.

Adapalene is rapidly cleared from blood plasma, typically undetectable after 72 hours following topical application.

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information regarding adapalene is not readily available.

Patients experiencing an overdose are at an increased risk of severe adverse effects such as redness, scaling, and skin discomfort.

Symptomatic and supportive measures are recommended.

Adapalene has an acute oral LD in S-D rats and CD-1 mice of over 5000 mg/kg. The LD of 0.3% applied topically to Credo OF1 mice is over 10 ml/kg (30 mg/kg).

No systemic or local toxicity was observed in rats treated topically with 6 mg/kg/day of 0.3% adapalene.

For topical use only; adapalene and benzoyl peroxide gel 0.1% / 2.5% is not for oral, ophthalmic, or intravaginal use.

Apply a thin film of adapalene and benzoyl peroxide gel 0.1% / 2.5% to affected areas of the face and/or trunk once daily after washing.

Use a pea-sized amount for each area of the face (e.g., forehead, chin, each cheek).

Avoid the eyes, lips and mucous membranes.

Adapalene and benzoyl peroxide gel 0.1% / 2.5% is not for oral, ophthalmic, or intravaginal use.

Adapalene and benzoyl peroxide gel 0.1% / 2.5% is white to very pale yellow in color and opaque in appearance.

NDC: 72162-2296-2: 45 g in a BOTTLE, PUMP Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) .

Repackaged/Relabeled by: Bryant Ranch Prepack, Inc.

Burbank, CA 91504.

There are no well-controlled trials in pregnant women treated with adapalene and benzoyl peroxide gel 0.1% / 2.5%.

Animal reproduction studies have not been conducted with the combination gel or benzoyl peroxide.

Furthermore, such studies are not always predictive of human response; therefore, adapalene and benzoyl peroxide gel 0.1% / 2.5% should be used during pregnancy only if the potential benefit justifies the risk to the fetus.

No teratogenic effects were observed in rats treated with oral doses of 0.15 to 5.0 mg adapalene/kg/day, up to 25 times (mg/m2/day) the maximum recommended human dose (MRHD) of 2 grams of adapalene and benzoyl peroxide gel 0.1% / 2.5%.

However, teratogenic changes were observed in rats and rabbits when treated with oral doses of ≥ 25 mg adapalene/kg/day representing and 246 times MRHD, respectively.

Findings included cleft palate, microphthalmia, encephalocele and skeletal abnormalities in rats; and umbilical hernia, exophthalmos and kidney and skeletal abnormalities in rabbits.

Dermal teratology studies conducted in rats and rabbits at doses of 0.6 to 6.0 mg adapalene/kg/day [25 to 59 times (mg/m2) the MRHD] exhibited no fetotoxicity and only minimal increases in supernumerary ribs in both species and delayed ossification in rabbits.

It is not known whether adapalene or benzoyl peroxide is excreted in human milk following use of adapalene and benzoyl peroxide gel 0.1% / 2.5%.

Because many drugs are excreted in human milk, caution should be exercised when adapalene and benzoyl peroxide gel 0.1% / 2.5% is administered to a nursing woman.

Safety and effectiveness of adapalene and benzoyl peroxide gel 0.1% / 2.5% in pediatric patients under the age of 9 have not been established.

Clinical studies of adapalene and benzoyl peroxide gel 0.1% / 2.5% did not include sufficient numbers of subjects aged and over to determine whether they respond differently from younger subjects.