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Differin (Adapalene)
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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.
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.
Indications
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.
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.
Contraindications
In patients who have demonstrated a hypersensitivity to the drug. In patients with eczema or seborrheic dermatitis.
In patients who have demonstrated a hypersensitivity to the drug. In patients with eczema or seborrheic dermatitis.
Safety Information / Warning
Pregnancy : Topical adapalene should be used by women of childbearingyears 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 (25mg/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 2to 4weeks 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.
Pregnancy : Topical adapalene should be used by women of childbearingyears 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 (25mg/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 2to 4weeks 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, gel or solution is used at night.
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, gel or solution is used at night.
Side Effects / Adverse Effects
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% (28reports 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.
In clinical trials with adapalene topical solution, the total incidence of adverse reactions related to treatment was 12.7% (73 reports from 571 participants). The most frequent adverse reactions reported were burning and stinging (3.7%), skin irritation (2.4%), erythema (2.1%), dry skin (1.9%) and pruritus (1.4%). Other adverse experiences which were attributed to treatment or were possibly related to treatment but occurred less frequently (in less than 1% of patients) were dermatitis, sunburn, acne flare and one instance of impetigo flare.
Most of the reactions occurred within 2to 4weeks 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, gel or solution 0.1% have been reversible upon discontinuation of therapy.
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% (28reports 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.
In clinical trials with adapalene topical solution, the total incidence of adverse reactions related to treatment was 12.7% (73 reports from 571 participants). The most frequent adverse reactions reported were burning and stinging (3.7%), skin irritation (2.4%), erythema (2.1%), dry skin (1.9%) and pruritus (1.4%). Other adverse experiences which were attributed to treatment or were possibly related to treatment but occurred less frequently (in less than 1% of patients) were dermatitis, sunburn, acne flare and one instance of impetigo flare.
Most of the reactions occurred within 2to 4weeks 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, gel or solution 0.1% have been reversible upon discontinuation of therapy.
Overdose
Symptoms and Treatment: Adapalene topical cream, gel and solution 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 and solution in mice and rats is greater than 10mL/kg. Inadvertent oral ingestion of adapalene may lead to the same adverse effects as those associated with excessive oral intake of VitaminA 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.
Symptoms and Treatment: Adapalene topical cream, gel and solution 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 and solution in mice and rats is greater than 10mL/kg. Inadvertent oral ingestion of adapalene may lead to the same adverse effects as those associated with excessive oral intake of VitaminA 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.
Recommended Dosage
Apply to the affected areas of the face, chest and back once aday 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 4to 8weeks 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.
Information for the Patient: See Blue Section--Information for the Patient “Differin”.
Apply to the affected areas of the face, chest and back once aday 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 4to 8weeks 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.
Information for the Patient: See Blue Section--Information for the Patient “Differin”.
Supplied / Packaging
Cream: Each g of topical cream contains: adapalene 0.1% (1mg). 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 45g.
Gel: Each g of topical gel contains: adapalene 0.1% (1mg). 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 45g.
Solution: Each mL of topical solution contains: adapalene 0.1% (1mg). Nonmedicinal ingredients: ethanol and polyethylene glycol 400. Pledgets of 30´1mL.
Store between 15and 30°C. Keep container tightly closed.
Cream: Each g of topical cream contains: adapalene 0.1% (1mg). 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 45g.
Gel: Each g of topical gel contains: adapalene 0.1% (1mg). 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 45g.
Solution: Each mL of topical solution contains: adapalene 0.1% (1mg). Nonmedicinal ingredients: ethanol and polyethylene glycol 400. Pledgets of 30´1mL.
Store between 15and 30°C. Keep container tightly closed.
