Adapalene

Name: Adapalene

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Reviewed on 12/22/2015 References Reference: FDA Prescribing Information

Adapalene Dosage and Administration

Administration

Topical Administration

Apply a thin film to skin as a cream, gel, or solution.1 4 5 7 11 12 13 16 17 18 19 20 21 22 31 32

Cleanse and dry the affected areas prior to application.1 31 32

Do not apply to eye(s), lips, angles of nose, or mucous membranes.1 31 32

A transient feeling of pruritus or burning may occur immediately after application.1 12 31 32 If increased sensitivity or irritation occurs, reduce frequency of application or, depending on the severity, discontinue use.1 31 32

Apparent exacerbation of acne that may occur during early weeks of therapy is attributable to the drug’s action on previously unseen lesions; do not discontinue.1 31 32

Excessive use does not increase therapeutic effects and may produce marked erythema, peeling, and discomfort.1 31 32

Pledgets

Remove single-use pledget applicators from foil immediately before use, use once, and then discard; do not use if seal is broken.31

Dosage

Pediatric Patients

Acne Vulgaris Topical

Children and adolescents ≥12 years of age: Apply once daily in the evening at bedtime.1 12 31 32

Improvement usually detectable within 8–12 weeks.1 31 32

Adults

Acne Vulgaris Topical

Apply once daily in the evening at bedtime.1 12 31 32

Improvement usually detectable within 8–12 weeks.1 31 32

Prescribing Limits

Pediatric Patients

Acne Vulgaris Topical

Children and adolescents ≥12 years of age: most reported experience to date has been for treatment periods that did not exceed 12 weeks.4 5 6 12 22

Adults

Acne Vulgaris Topical

Most reported experience to date has been for treatment periods that did not exceed 12 weeks.4 5 6 12 22

Cautions for Adapalene

Contraindications

  • Known hypersensitivity to adapalene or any ingredient in the formulation.1 31 32

Warnings/Precautions

Sensitivity Reactions

Photosensitivity

Increased risk for sunburn; minimize exposure to sunlight or artificial UV irradiation sources (e.g., sunlamps).1 31 32

Use caution in patients subjected to considerable occupational sun exposure or with inherent sun sensitivity; use of sunscreen products (SPF 15 or greater) and protective clothing over treated areas recommended when exposure cannot be avoided.1 31 32

Avoid concomitant use of photosensitizing agents.33 (See Interactions.)

Use not recommended in patients with sunburn until full recovery occurs.1 31

Other Sensitivity Reactions

Discontinue therapy if sensitivity reaction or chemical irritation occurs.1 31 32

General Precautions

Dermatologic Effects

Erythema, dryness, scaling, burning, or pruritus may occur.1 31 32 If increased sensitivity or irritation occurs, use less frequently or, depending on the severity of the reaction, discontinue.1 31 32

Do not apply to cuts, abrasions, or eczematous or sunburned skin.1 31 32 (See Photosensitivity under Cautions.)

Facial Cleansing

Use of mild or soapless cleanser is recommended; use medicated or drying soaps and abrasive soaps and cleansers with caution.1 31 32

Cosmetic Agents or Processes

Avoid use of irritating cosmetics, other preparations, or processes (e.g., electrolysis) that might dry or irritate the skin.33 (See Interactions.)

Environmental Stimuli

Possible increased skin irritation in patients exposed to environmental extremes (e.g., wind, cold).1 31 32

Dry Skin

Use moisturizers if necessary; avoid preparations containing alpha hydroxy or glycolic acids.32

Specific Populations

Pregnancy

Category C.1 31 32

Lactation

Not known whether adapalene is distributed into milk.1 31 32 Use caution.1 31 32

Pediatric Use

Safety and efficacy not established in children <12 years of age.1 31 32

Geriatric Use

Insufficient experience in controlled clinical studies in patients ≥65 years of age to determine whether geriatric patients respond differently to adapalene than younger adults.32 However, clinical experience generally has not revealed age-related differences.32

Common Adverse Effects

Erythema, scaling, dryness, pruritus, burning/stinging.1 31 32

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Adapalene

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

0.1%

Differin (with parabens)

Galderma

Gel

0.1%

Differin (with methylparaben and propylene glycol)

Galderma

Pledgets (saturated with solution)

0.1%

Differin (with SD alcohol 40-B 30% w/v)

Galderma

Solution

0.1%

Differin (with SD alcohol 40-B 30% w/v)

Galderma

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Adapalene - Clinical Pharmacology

Adapalene is a chemically stable, retinoid-like compound. Biochemical and pharmacological profile studies have demonstrated that Adapalene is a modulator of cellular differentiation, keratinization, and inflammatory processes all of which represent important features in the pathology of acne vulgaris.

Mechanistically, Adapalene binds to specific retinoic acid nuclear 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.

Pharmacokinetics

Absorption of Adapalene through human skin is low. Only trace amounts (<0.25 ng/mL) of parent substance have been found in the plasma of acne patients following chronic topical application of Adapalene in controlled clinical trials. Excretion appears to be primarily by the biliary route.

Adverse Reactions

Some adverse effects such as erythema, scaling, dryness, pruritus, and burning will occur in 10-40% of patients. Pruritus or burning immediately after application also occurs in approximately 20% of patients. The following additional adverse experiences were reported in approximately 1% or less of patients: skin irritation, burning/stinging, erythema, sunburn, and acne flares. These are most commonly seen during the first month of therapy and decrease in frequency and severity thereafter. All adverse effects with use of Adapalene gel during clinical trials were reversible upon discontinuation of therapy.

Off Label Uses

Rosacea

Topical adapalene for the management of rosacea has been studied in a limited number of patients, with data suggesting it may be a useful alternative to topical metronidazole. An international consensus statement on the treatment of rosacea recognizes that evidence is limited to support the use of topical retinoids, which may aggravate underlying vascular disease and have irritant properties, but that some retinoids such as adapalene may be more tolerable. Data from larger, controlled trials are needed to establish adapalene's role in the management of rosacea.

Administration

For topical use only; not for oral, ophthalmic, or intravaginal use. Avoid contact with abraded, broken, eczematous, or sunburned skin, mucous membranes, eyes, lips, and angles of the nose. Moisturizers may be used if necessary; avoid alpha hydroxy or glycolic acid-containing products. A mild transitory sensation of warmth or slight stinging may occur shortly after application.

Cream/gel: Apply a thin film to clean/dry skin in the evening before bedtime; apply enough to cover entire affected area

Lotion: Apply after washing gently with a mild or soapless cleanser and then pat dry; dispense a nickel size amount (3 to 4 pump actuations) to cover entire face

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity reactions: Reactions such as pruritus, face edema, eyelid edema, and swelling have been reported. Discontinue use immediately if allergic or anaphylactoid/anaphylactic reactions occur.

• Photosensitivity: Use is associated with increased susceptibility/sensitivity to UV light; avoid sunlamps or excessive sunlight exposure. Daily sunscreen use and other protective measures are recommended. Patients with sunburn should discontinue use until sunburn has healed.

• Skin irritation: Certain cutaneous signs and symptoms such as erythema, dryness, scaling, stinging/burning, or pruritus may occur during treatment; these are most likely to occur during the first 2 to 4 weeks and will usually lessen with continued use. Treatment can increase skin sensitivity to weather extremes of wind or cold. Concomitant topical medications (eg, medicated or abrasive soaps and cleansers, or cosmetics with a strong drying effect, products with high concentrations of alcohol, astringents, spices or limes) should be avoided due to increased skin irritation. Depending on the severity of irritation, use moisturizer, reduce the frequency of application, or discontinue use.

Other warnings/precautions:

• Appropriate use: For external use only; avoid contact with abraded, broken, eczematous, or sunburned skin, mucous membranes, eyes, lips, and angles of the nose. Wax depilation is not recommended.

Pregnancy Risk Factor C Pregnancy Considerations

Adverse effects were observed in animal reproduction studies. Retinoids may cause harm when administered during pregnancy. A case report described maternal use of adapalene 1 month prior to pregnancy and through 13 weeks gestation; cerebral and ocular malformations were reported in the exposed fetus which resulted in termination of pregnancy (Autret, 1997). In clinical trials, women of childbearing potential were required to have a negative pregnancy test prior to therapy.

Adverse Effects

>10%

Dryness (1-45%)

Scaling (1-44%)

Burning/stinging (4-29%)

Erythema (0.5-26%)

1-10%

Skin discomfort (6%)

Pruritus (2%)

Desquamation (2%)

Sunburn (1%)

<1%

Acne flare

Conjunctivitis

Contact dermatitis

Eczema

Erythema

Eyelid edema

Rash

Skin discoloration

  • Acne (Pimples)

For the Consumer

Applies to adapalene topical: topical cream, topical gel/jelly, topical lotion, topical solution, topical swab

Along with its needed effects, adapalene topical may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur while taking adapalene topical:

More common - especially during the first month of use
  • Burning sensation or stinging of skin
  • dryness and peeling of skin
  • itching of skin
  • redness of skin

Some side effects of adapalene topical may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Rare - more common during the first month of use
  • Worsening of acne

Dose Adjustments

Data not available

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