Action And Clinical Pharmacology: Adapalene is a chemically stable, retinoid-like compound. Biochemical and pharmacological profile studies have demonstrated that adapalene is a potent modulator of cellular differentiation, keratinization and inflammatory processes all of which represent important features in the pathology of acne vulgaris. Although the exact mode of action of adapalene is unknown, current evidence suggests that topical adapalene normalizes the differentiation of follicular epithelial cells resulting in decreased microcomedone formation. Adapalene inhibits the chemotactic (directional) and chemokinetic (random) responses of human polymorphonuclear leucocytes and also inhibits the metabolism of arachidonic acid, by lipoxidation, to inflammatory mediators. tag_IndicationsIndications
Indications And Clinical Uses: For the topical treatment of acne vulgaris.
Contra-Indications: Patients who have demonstrated a hypersensitivity to the drug. Patients with eczema or seborrheic dermatitis.
Manufacturers’ Warnings In Clinical States: Pregnancy : Topical adapalene should be used by women of childbearing years only after contraceptive counselling. It is recommended that topical adapalene should not be used by pregnant women.
There have been rare reports of birth defects among babies born to women exposed to topical retinoids during pregnancy. However, there are no well controlled prospective studies of the use of topical retinoids, including adapalene, in pregnant women. A retrospective study of mothers exposed to topical tretinoin during the first trimester of pregnancy found no increase in the incidence of birth defects.
As with retinoids, adapalene administered orally at high doses (25 mg/kg/day) is teratogenic. In topical adapalene studies with doses of 50 to 200 times the likely clinical dose, no teratogenic effects were observed in rats or rabbits. However, topical retinoid teratology studies in rats and rabbits have been inconclusive.
General: For external use only. Avoid contact with the eyes, lips, angles of the nose, mucous membranes and open wounds. Certain cutaneous signs and symptoms such as erythema, dryness, scaling, burning or pruritus are associated with the topical application of retinoids and can also be expected with the use of adapalene. These treatment-related effects generally occur during the first 2 to 4 weeks of therapy and usually resolve as the skin undergoes adjustment with continued use. Depending on the degree of the side effects, patients can be directed to use the medication less frequently or temporarily discontinue use until the symptoms subside (see Dosage).
Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when adapalene is administered to a nursing mother.
Children: Safety and effectiveness in children below the age of 12 have not been established.
Precautions: General: For external use only. Patients should be advised to use noncomedogenic cosmetics. Color cosmetics such as blushers and powders are acceptable; however, make-up cosmetics should be water based only. Cosmetics must be removed by thorough cleansing before the area is treated. Exposure to excessive sunlight, including sunlamps, should be avoided while using the preparation, or a suitably effective sunscreen should be employed.
Drug Interactions: There are no known interactions with other medications which are likely to be used topically and concurrently with adapalene. Absorption of adapalene through human skin is low; therefore, interaction with systemic medications is unlikely. As adapalene has the potential for local irritation, it is possible that concomitant use of abrasive cleansers, strong drying agents or irritant products may produce additive irritant effects. Other cutaneous antiacne treatments (e.g., erythromycin topical solution, clindamycin phosphate topical solution 1% or benzoyl peroxide products in concentrations up to 10%) may be used in the morning when adapalene topical cream or gel is used at night.
Adverse Reactions: In clinical trials with adapalene topical cream, the total incidence of adverse reactions related to treatment was 5.5% (17 reports from 311 participants). The most frequently reported treatment-related events were skin irritation 1.6% (5/311) and sunburn 1% (3/311). Other dermatologic (treatment-related) events at an incidence rate less than 1% were acne flare 0.6% (2/311), contact dermatitis 0.6% (2/311), eyelid edema 0.6% (2/311), erythema 0.3% (1/311), skin discomfort 0.3% (1/311) and dry skin 0.3% (1/311).
In clinical trials with adapalene topical gel, the total incidence of adverse reactions related to treatment was 4.2% (28 reports from 661 participants). The most frequent adverse reactions reported were erythema (0.9%), dry skin (0.9%), skin irritation (0.6%), burning and stinging (0.6%) and acne flare (0.5%). Other adverse experiences which were attributed to treatment or were possibly related to treatment but occurred less frequently (in less than 0.5% of patients) were pruritus and one instance of sunburn.
Most of the reactions occurred within 2 to 4 weeks of initiation of therapy and were generally observed to resolve with continued use of the product or temporary adjustment of the treatment schedule. Contact allergy to topical adapalene was not reported during clinical trials. To date, all adverse effects of adapalene topical cream or gel, 0.1% have been reversible upon discontinuation of therapy.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: Adapalene topical cream and gel are intended for cutaneous use only. If the medication is applied excessively, no more rapid or better results will be obtained and marked redness, peeling or discomfort may occur. The acute oral toxicity of adapalene topical gel in mice and rats is greater than 10 mL/kg. Inadvertent oral ingestion of adapalene may lead to the same adverse effects as those associated with excessive oral intake of Vitamin A including teratogenesis in women of childbearing years. Therefore, in such cases, pregnancy testing should be carried out in women of childbearing years. In the event of accidental ingestion of the product, an appropriate method of gastric emptying might be considered.
Dosage And Administration: Apply to the affected areas of the face, chest and back once a day before retiring and after washing. A small amount should be applied to provide a thin film, avoiding eyes, lips and mucous membranes.
Discontinue treatment if a severe local inflammatory response is experienced. Reinstitute therapy when the reaction has subsided, initially applying the preparation less frequently. Once daily application may be resumed if it is judged that the patient is able to tolerate the treatment.
Clinical improvement is expected to be clearly evident after 4 to 8 weeks of treatment, with further improvement expected with continued use. Cutaneous safety of adapalene topical gel has been demonstrated over a 6-month period of treatment.
Availability And Storage: Cream: Each g of topical cream contains: adapalene 0.1% (1 mg). Nonmedicinal ingredients: carbomer 934P, cyclomethicone, edetate disodium, glycerin, methyl gluceth-20 sesquistearate, methyl glucose sesquistearate, methylparaben, phenoxyethanol, propylparaben, purified water, squalane and trolamine. Tubes of 15 and 45 g.
Gel: Each g of topical gel contains: adapalene 0.1% (1 mg). Nonmedicinal ingredients: carbomer 940, edetate disodium, methylparaben, poloxamer 182, propylene glycol, purified water and sodium hydroxide and/or hydrochloric acid for pH adjustment. Tubes of 15 and 45 g.
Store between 15 and 30°C. Keep container tightly closed.
DIFFERIN® Galderma Adapalene Acne Therapy
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