ADAPALENE USES SIDE EFFECTS AND MORE

 

ADAPALENE CREAM/GEL/FORTE GEL

COMPOSITION

Adapco Cream

Each gram contains:

1mg (0.1%w/w)

Adapalene BP.....

Adapco Gel

Each gram contains:

1 mg (0.1%w/w)

Adapalene BP......

Adapco Forte Gel

Each gram contains:

Adapalone BP..

..,3mg (0.3%w/w)

DESCRIPTION

Adapco Cream / Gel, containing adapalene is a naphthoic acid derivative with retinoid-like properties. The chemical name for adapalene is (6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid).

The molecular formula is C28H280 and molecular weight is 412.53.

PHARMACOLOGICAL PROPERTIES

Mechanism of Action

Adapalene acts on retinoid receptors. 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 through human skin is low. No quantifiable amounts (limit of quantification = 0.35 ng/mL) is

found in the plasma samples of acne patients following chronic topical application of adapalene. Excretion appears to be primarily by the biliary route.

Systemic exposure of adapalene following a topical application was studied in one clinical study. Fourteen subjects at

18-29 years of age with severe acne were treated with 2 g of Adapalene once daily for 30 days to approximately 1000 cm2 of acne involved skin.

Serial plasma samples were collected for 24 or 72 hours following application on days 1, 15 and 30. All plasma: concentrations for 12 out of 14 patients were below the limit of quantification (LOQ=0.1 ng/mL). One patient had one sample above LOQ at day 30 and the other patient had four plasma samples above LOQ on both days 1 and 15, which ranged from 0.102 and 0.131 ng/mL. Due to the limited number of available data points, PK analysis was not undertaken.

Pharmacodynamics

Pharmacodynamics of Adapelene is unknown.

INDICATIONS

Adapco Cream / Gel is indicated for the topical treatment of acne vulgaris in patients 12 years and older.

DOSAGE & ADMINISTRATION

Adapco Cream / Gel should be applied to affected areas of the skin, once daily at night time, after washing gently with a mild soapless cleanser. A thin film of the Adapco Cream / Gel should be applied to the skin areas where acne lesions appear, using enough to cover the entire affected areas lightly. A mild transitory sensation of warmth or slight stinging may occur shortly after the application of Adapco Cream / Gel.

Patients should be instructed to minimize sun exposure. Patients may be instructed to use moisturizers for relief of dry skin or irritation.

Avoid application to the areas of skin around eyes, lips and mucous membranes.

Adapco Cream / Gel is for topical use only and not for oral, ophthalmic, or intravaginal use. If therapeutic results are not noticed after 12 weeks of treatment, therapy should be re-evaluated.

ADVERSE EFFECTS

Local cutaneous adverse events in patients using Adapco Cream / Gel once daily include: erythema, scaling, dryness, pruritus (persistent) and burning/stinging (persistent). Other local cutaneous adverse events may include: sunbum, skin discomfort-burning and stinging and skin irritation. Events occurring in less than 1% of patients treated with adapalene Cream / Gel include: acne flare, dermatitis and contact dermatitis, eyelid edema, conjunctivitis, erythema, pruritus, skin discoloration, rash, and eczema.

WARNING & PRECAUTIONS

Ultraviolet Light and Environmental Exposure

Exposure to sunlight, including sunlamps, should be avoided during the use of Adapco Cream / Gel. Patients with high levels of sun exposure and those with inherent sensitivity to sun should be warned to exercise caution.

Use of sunscreen products and protective apparel (e.g. hat) are recommended when exposure cannot be avoided.

Weather extremes, such as wind or cold, may be irritating to patients under treatment with Adapco Cream / Gel .

Local Cutaneous Reactions

Signs and symptoms of local skin irritation (such as erythema, scaling, dryness, stinging/burning) may be experienced with use of Adapco Cream / Gel.

These are most likely to occur during the first 2 weeks of treatment, are mostly mild to moderate in severity, and usually lessen with continued use of Adapco Cream / Gel. Depending upon the severity of these side effects, patients should be instructed to use a moisturizer, reduce the frequency of the application of Adapco Gream / Gel, or discontinue use.

Adapco Cream / Gel should not be applied to cuts, abrasions, eczematous or sunburned skin. As with other retinoid, use of "waxing" as a depilatory method should be avoided on skin treated with Adapco Cream / Gel.