Apalene

Uses

Apalene cream is used for the topical treatment of acne vulgaris of the face, chest or back.

Apalene is also used to associated treatment for these conditions: Acne Vulgaris

How Apalene works

Apalene 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. Apalene 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.

Dosage

Apalene dosage

A thin film topical cream should be applied to the affected areas once a day before bedtime, after washing. The affected areas should be dry before application.

Side Effects

Local reactions include burning, erythema, stinging, pruritus, dry or peeling skin. Increased sensitivity to UVB light or sunlight occurs.

Toxicity

Toxicity 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.

Apalene has an acute oral LD₅₀ in S-D rats and CD-1 mice of over 5000 mg/kg. The LD₅₀ 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.

Precaution

Apalene cream should not come into contact with the eyes, lips mouth and mucous membranes, angles of the nose or broken skin (cuts and abrasions). If product enters the eye, wash with warm water. Because of a potential for increased irritation Apalene cream should not be used by patients with eczema or seborrhoeic dermatitis. If a reaction suggesting severe irritation occurs, discontinue use of the medication. If the irritation is not severe, use the medication less frequently, discontinue use temporarily until symptoms subside, or discontinue use altogether.

Interaction

Concomitant use of other potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect, products with high concentrations of alcohol, astringents, spices or lime) should be approached with caution.

Exercise particular caution in using preparations containing sulfur, resorcinol or salicylic acid in combination with Apalene.

If any of these preparations have been used, it is advisable not to start therapy with Apalene until the effects of such preparations in skin have subsided. If combined use of both medications is important, it is better to use in two different times.

Food Interaction

Elimination Route

Apalene is applied topically and absorbed through the skin. In one clinical study treating patients once per day with 2g of 0.3% gel applied to 2 mg/cm² 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.

Half Life

In one clinical study, after ten days of treatment with 2g of 0.3% cream or gel, the terminal half-life was between 7 and 51 hours, with a mean of 17.2 ± 10.2.

Clearance

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

Elimination Route

Apalene is primarily excreted by the biliary route at about 30 ng/g of the topically applied amount. Approximately 75% of the drug remains unchanged.

Pregnancy & Breastfeeding use

Pregnancy: Category C. There are no well-controlled studies in pregnant women.

Nursing Mothers: It is not known whether Apalene is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Apalene 0.1% cream is administered to a lactating mother.

Contraindication

Apalene should not be administered to individuals who are hypersensitive to Apalene or any of its components.

Special Warning

Safety and effectiveness in children below 12 years of age have not been established.

Acute Overdose

If the medication is applied excessively, no more rapid or better results will be obtained and marked redness, peeling or discomfort may occur.

Interaction with other Medicine

There are no known interactions with other medications, which might be used topically and concurrently with adapalene topical cream. Other retinoids or drugs with a similar mode of action should not be used concurrently with adapalene. Absorption of adapalene through human skin is low and therefore no interaction with systemic medication.

Storage Condition

Store in a cool and dry place (below 25oC). Do not freeze.

Innovators Monograph

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