Adapalene

ADAPALENE- adapalene cream
Perrigo New York Inc

Rx Only
For topical use only. Not for ophthalmic, oral, or intravaginal use.

adapalene_cream_carton_imageadapalene_cream_tube_image

DESCRIPTION

Adapalene Cream, 0.1%, contains adapalene 0.1% in an aqueous cream emulsion consisting of carbomer 934P, cyclomethicone, edetate disodium, glycerin, methyl glucose sesquistearate, methylparaben, PEG-20 methyl glucose sesquistearate, phenoxyethanol, propylparaben, purified water, squalane, and trolamine.

The chemical name of adapalene is 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid. It is a white to off-white powder which is soluble in tetrahydrofuran, sparingly soluble in ethanol, and practically insoluble in water. The molecular formula is C28 H28 O3 and molecular weight is 412.53. Adapalene is represented by the following structural formula.

structural formula imagestructural formula image

CLINICAL PHARMACOLOGY

Mechanism of Action

Adapalene acts on retinoid receptors. 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 normalizes the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.

Pharmacokinetics

Absorption of adapalene from Adapalene Cream, 0.1% through human skin is low. In a pharmacokinetic study with six acne patients treated once daily for 5 days with 2 grams of Adapalene Cream, 0.1% applied to 1000 cm2 of acne involved skin, there were no quantifiable amounts (limit of quantification = 0.35 ng/mL) of adapalene in the plasma samples from any patient. Excretion appears to be primarily by the biliary route.

INDICATIONS AND USAGE

Adapalene Cream, 0.1% is indicated for the topical treatment of acne vulgaris.

CLINICAL STUDIES

Two vehicle-controlled clinical studies were conducted in patients 12 to 30 years of age with mild to moderate acne vulgaris, in which Adapalene Cream, 0.1% was compared with its vehicle. Patients were instructed to apply their treatment medication once daily at bedtime for 12 weeks. In one study patients were provided with a soapless cleanser and were encouraged to refrain from using moisturizers. No other topical medications, other than Adapalene Cream, 0.1%, were to be applied to the face during the studies. Adapalene Cream, 0.1% was significantly more effective than its vehicle in the reduction of acne lesion counts. The mean percent reduction in lesion counts from baseline after treatment for 12 weeks are presented in the following table:

MEAN PERCENT REDUCTION IN LESION COUNTS FROM BASELINE TO WEEK 12
Efficacy Variable Study No. 1 Study No. 2

Adapalene
Cream, 0.1%
N=119

Cream
Vehicle
N=118
Adapalene
Cream, 0.1%
N=175
Cream
Vehicle
N=175
Non-inflammatory lesions 34% 18% 35% 15%
Inflammatory lesions 32% 17% 14% 6%
Total lesions 34% 18% 30% 15%

The trend in the Investigator’s global assessment of severity supported the efficacy of Adapalene Cream, 0.1% when compared to the cream vehicle.

CONTRAINDICATIONS

Adapalene Cream, 0.1% should not be administered to individuals who are hypersensitive to adapalene or any of the components in the cream vehicle.

PRECAUTIONS

General

Certain cutaneous signs and symptoms of treatment such as erythema, dryness, scaling, burning, or pruritus may be experienced with use of Adapalene Cream, 0.1%. These are most likely to occur during the first two to four weeks of treatment, are mostly mild to moderate in intensity, and usually lessen with continued use of the medication. Depending upon the severity of these side effects, patients should be instructed to reduce the frequency of application or discontinue use.

If a reaction suggesting sensitivity or chemical irritation occurs, use of the medication should be discontinued. Exposure to sunlight, including sunlamps, should be minimized during use of adapalene. Patients who normally experience high levels of sun exposure, and those with inherent sensitivity to sun, should be warned to exercise caution. Use of sunscreen products and protective clothing over treated areas is recommended when exposure cannot be avoided. Weather extremes, such as wind or cold, also may be irritating to patients under treatment with adapalene.

Avoid contact with the eyes, lips, angles of the nose, and mucous membranes. The product should not be applied to cuts, abrasions, eczematous or sunburned skin. As with other retinoids, use of “waxing” as a depilatory method should be avoided on skin treated with adapalene.

Information for Patients

Patients using Adapalene Cream, 0.1% should receive the following information and instructions:

1. This medication is to be used only as directed by the physician.

2. It is for external use only.

3. Avoid contact with the eyes, lips, angles of the nose, and mucous membranes.

4. Cleanse area with a mild or soapless cleanser before applying this medication.

5. Moisturizers may be used if necessary; however, products containing alpha hydroxy or glycolic acids should be avoided.

6. Exposure of the eye to this medication may result in reactions such as swelling, conjunctivitis, and eye irritation.

7. This medication should not be applied to cuts, abrasions, eczematous or sunburned skin.

8. Wax epilation should not be performed on treated skin due to the potential for skin erosions.

9. During the early weeks of therapy, an apparent exacerbation of acne may occur. This is due to the action of this medication on previously unseen lesions and should not be considered a reason to discontinue therapy. Overall clinical benefit may be noticed after two weeks of therapy, but at least eight weeks are required to obtain consistent beneficial effects.

Drug Interactions

As Adapalene Cream, 0.1% has the potential to produce local irritation in some patients, concomitant use of other potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect, and products with high concentrations of alcohol, astringents, spices or lime rind) should be approached with caution. Particular caution should be exercised in using preparations containing sulfur, resorcinol, or salicylic acid in combination with Adapalene Cream, 0.1%. If these preparations have been used, it is advisable not to start therapy with Adapalene Cream, 0.1% until the effects of such preparations in the skin have subsided.

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