Adapalene is a synthetic, naphthoic acid-derivative retinoid.7, 8, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 22
Adapalene is used topically for the treatment of acne vulgaris.1, 4, 5, 6, 7, 11, 12, 13, 14, 16, 17, 18, 19, 20, 21, 22, 31, 32 Therapy for acne vulgaris must be individualized and frequently modified depending on the types of acne lesions that predominate and the patient's response to therapy.2, 11
Adapalene has been shown to be more effective than placebo in reducing acne lesion counts in patients with mild to moderate acne vulgaris.32 In 2 placebo-controlled clinical studies, once-daily application of adapalene 0.1% topical cream for 12 weeks resulted in a 30-34% reduction in the total number of lesions compared with a 15-18% reduction achieved with vehicle placebo.32 In comparative studies in patients with mild to moderate facial acne,4, 5, 12, 17, 19, 21, 22 adapalene 0.1% topical gel was at least as effective as tretinoin 0.025% topical gel4, 6, 11, 14, 22 in reducing the number of comedonal,4, 11 inflammatory,5, 6, 12, 21, 22 and noninflammatory lesions,5, 6, 11, 12, 21, 22 as well as the total number of acne lesions4, 5, 6, 12, 13, 15, 20, 21, 23, 24 and generally was better tolerated (less local irritation).5, 6, 11, 12, 17, 19, 21, 22, 23, 24
A decrease in the number and severity of lesions generally occurs within 8-12 weeks following initiation of topical adapalene therapy.1, 4, 5, 6, 21, 22, 31
Adapalene is applied topically to the skin as a 0.1% cream or 0.1% gel.1, 4, 5, 7, 11, 12, 13, 16, 17, 18, 19, 20, 21, 22, 31, 32
Prior to application of the cream or gel, the affected areas should be cleansed and dried.1, 31, 32 A transient feeling of pruritus or burning may occur immediately after application of adapalene cream or gel.1, 12, 31, 32 If increased sensitivity or irritation occurs, patients should be instructed to reduce the frequency of application or, depending on the severity of the reaction, discontinue use of the drug.1, 31, 32
Patients should be advised not to use adapalene cream or gel in amounts larger than instructed or more often than instructed, since such use of the drug will not lead to more rapid or better results but may result in marked erythema, peeling, or discomfort.1, 31, 32
Care should be taken not to get adapalene cream or gel into the eyes.1, 31, 32 In addition, contact of the drug with the lips, mouth, angles of the nose, and mucous membranes should be avoided.1, 31, 32 If contact with the eye(s) occurs, the eye(s) should be washed with large amounts of water; patients should consult a clinician if ocular irritation persists.1
Patients receiving topical adapalene therapy should be cautioned to minimize exposure to sunlight or other UV rays, including sunlamps, unless deemed medically necessary; in such cases, exposure should be minimized during the use of adapalene.1, 12, 31, 32 Patients with sunburn should not use adapalene until full recovery occurs.1, 31 In addition, patients should be cautioned to inform their clinician if they are using other drugs that potentially could increase the sensitivity of their skin to sunlight (e.g., fluoroquinolone anti-infectives, thiazide diuretics, sulfonamides, phenothiazines).33 Patients who may be subjected to considerable sun exposure because of their occupation and those with inherent sensitivity to the sun should be especially cautious; when exposure cannot be avoided, use of sunscreens and protective clothing over treated areas may be prudent.1, 31, 32 Weather extremes (e.g., wind, cold) may be irritating to patients receiving topical adapalene therapy.1, 31, 32 Moisturizers may be used if necessary; however, products containing alpha-hydroxy or glycolic acids should be avoided.32 The manufacturer states that adapalene cream, gel, or solution should not be applied to abraded, eczematous, or sunburned skin.1, 31, 32
Patients should be advised that use of adapalene with other topical medications that have a strong skin-drying effect should be undertaken with caution.1, 12, 31, 32 In patients who have used such agents, sufficient time should elapse for the effects of these drugs to subside before initiating adapalene therapy.1, 31, 32 Use of topical preparations with high concentrations of alcohol, menthol, spices, or lime rind, such as shaving lotions, astringents, and perfume, also should be used with caution or avoided if possible.1, 31, 32 Particular caution should be exercised in using preparations containing sulfur, resorcinol, or salicylic acid in combination with adapalene cream, gel, or solution.1, 31, 32 Patients also should avoid the use of irritating cosmetics (e.g., toners, peeling [desquamating] agents), permanent wave solutions, electrolysis, hair depilatories, or other preparations or processes that might dry or irritate the skin during topical therapy with adapalene.33
The manufacturer states that safety and efficacy of adapalene in children younger than 12 years of age have not been established.1, 31, 32
For the topical treatment of acne vulgaris, a thin film of adapalene 0.1% cream or 0.1% gel should be applied to the cleansed affected area once daily in the evening at bedtime.1, 12, 31, 32 During the early weeks of therapy with adapalene, an apparent exacerbation of acne may occur.1, 31, 32 This effect is attributable to the action of the drug on previously unseen lesions and should not be considered a reason to discontinue therapy.1, 31, 32 Improvement usually is detectable within 8-12 weeks of initiating topical therapy with the drug.1, 31, 32 Most reported experience to date has been for treatment periods that did not exceed 12 weeks.4, 5, 6, 12, 22
Adapalene is a synthetic, naphthoic acid-derivative retinoid analog.7, 8, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 22 Adapalene has pharmacologic actions similar to those of other retinoids (e.g., tretinoin, isotretinoin) but has demonstrated more potent anti-inflammatory activity in vitro and in vivo.1, 4, 5, 6, 9, 13, 15, 16, 17, 19, 23, 24, 31 Unlike tretinoin and isotretinoin but like tazarotene, adapalene has relatively selective affinity for specific nuclear retinoic acid receptor (RAR) proteins (e.g., RARβ, RARγ) that appear to enhance gene transcription.5, 6, 7, 23, 24 RARγ is the predominant RAR species expressed in human epidermis and therefore may be the primary molecular target of retinoid action in adult human skin.6, 23 Adapalene does not interact with retinoid X receptors (RXRs),23, 24 which work in conjunction with RARs but appear to affect a variety of hormonal pathways and therefore may be involved in producing adverse effects of retinoid therapy.3 In addition, adapalene does not bind to cytosolic retinoic acid-binding proteins (CRABP).1, 5, 6, 7, 12, 13, 15, 16, 21, 23, 31
The exact mechanism of action of topically applied adapalene in the treatment of acne vulgaris has not been fully elucidated.1, 4, 5, 6, 9, 13, 15, 16, 17, 19, 31 Adapalene appears to affect expression of genes that modulate follicular keratinization,5, 19, 22 and cell (e.g., epithelial) differentiation,1, 4, 5, 6, 9, 10, 13, 15, 19, 22, 23, 31 which result in inhibition of corneocyte accumulation and cohesion and a reduction in inflammatory and noninflammatory acne lesions.1, 6, 11, 12, 22, 23, 24, 31
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
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.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Topical | Cream | 0.1% | Differin® | Galderma |
Gel | 0.1% | Differin® | Galderma |
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions May 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
1. Galderma. Differin® (adapalene) gel 0.1% prescribing information. Fort Worth, TX; 1996 May.
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3. Chandraratna RAS. Tazarotene—first of a new generation of receptor-selective retinoids. Br J Dermatol . 1996; 135:18-25.
4. Verschoore M, Langner A, Wolska H et al. Efficacy and safety of CD 271 alcoholic gels in the topical treatment of acne vulgaris. Br J Dermatol . 1991; 124:368-71. [PubMed 1827344]
5. Shalita A, Weiss JS, Chalker DK et al. A comparison of the efficacy and safety of adapalene gel 0.1% and tretinoin gel 0.025% in the treatment of acne vulgaris: a multicenter trial. J Am Acad Dermatol . 1996; 34:482-5. [PubMed 8609263]
6. Bernard BA. Adapalene, a new chemical entity with retinoid activity. Skin Pharmacol . 1993; 6(Suppl 1):61-9. [PubMed 8142113]
7. Griffiths CEM, Elder JT, Bernard BA et al. Comparison of CD271 (Adapalene) and all- trans retinoic acid in human skin: dissociation of epidermal effects and CRABP-II mRNA expression. J Invest Dermatol . 1993; 101:325-28. [PubMed 8396608]
8. Jamoulle JC, Grandjean L, Lamaud E et al. Follicular penetration and distribution of topically applied CD 271, a new naphthoic acid derivative intended for topical acne treatment. J Invest Dermatol . 1990; 94:731-2. [PubMed 2139085]
9. Hensby C, Cavey D, Bouclier M et al. The in vivo and in vitro anti- inflammatory activity of CD271: a new retinoid-like modulator of cell differentiation. Agents Actions . 1990; 29:56-8. [PubMed 2109510]
10. Bernerd F, Ortonne JP, Bouclier M et al. The rhino mouse model: the effects of topically applied all- trans retinoic acid and CD271 on the fine structure of the epidermis and utricle wall of pseudocomedones. Arch Dermatol Res . 1991; 283:100-7. [PubMed 2069410]
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12. Brogden RN, Goa KL. Adapalene: a review of its pharmacological properties and clinical potential in the management of mild to moderate acne. Drugs . 1997; 53:511-9. [PubMed 9074847]
13. Verschoore M. Adapalene: a novel topical retinoid receptor agonist for acne—overview. J Am Acad Dermatol . 1997; 36:S91.
14. Kligman AM. The treatment of acne with topical retinoids: one man's opinions. J Am Acad Dermatol . 1997; 36:S92-5.
15. Shroot B, Michel S. Pharmacology and chemistry of adapalene. J Am Acad Dermatol . 1997; 36:S96-103. [PubMed 9204085]
16. Verschoore M, Poncet M, Czernielewski J et al. Adapalene 0.1% gel has low skin- irritation potential. J Am Acad Dermatol . 1997; 36:S104-9.
17. Caron D, Sorba V, Kerrouche N et al. Split-face comparison of adapalene 0.1% gel and tretinoin 0.025% gel in acne patients. J Am Acad Dermatol . 1997; 36:S110-12. [PubMed 9204087]
18. Caron D, Sorba V, Clucas A et al. Skin tolerance of adapalene 0.1% gel in combination with other topical antiacne treatments. J Am Acad Dermatol . 1997; 36:S113-5.
19. Clucas A, Verschoore M, Sorba V et al. Adapalene 0.1% gel is better tolerated than tretinoin 0.025% gel in acne patients. J Am Acad Dermatol . 1997; 36:S116-8.
20. Allec J, Chatelus A, Wagner N. Skin distribution and pharmaceutical aspects of adapalene gel. J Am Acad Dermatol . 1997; 36:S119-25. [PubMed 9204090]
21. Cunliffe WJ, Caputo R, Dreno B et al. Clinical efficacy and safety comparison of adapalene gel and tretinoin gel in the treatment of acne vulgaris: Europe and U.S. multicenter trials. J Am Acad Dermatol . 1997; 36:S126-34. [PubMed 9204091]
22. Anon. Adapalene for acne. Med Lett Drugs Ther . 1997; 39:19-20. [PubMed 9057779]
23. Thiboutot DM. Acne: an overview of clinical research findings. Dermatol Clin . 1997; 15:97-109. [PubMed 9001864]
24. Gibson JR. Rationale for the development of new topical treatments for acne vulgaris. Cutis . 1996; 57:13-9. [PubMed 8654127]
25. Anon. Update on birth defects with isotretinoin. FDA Drug Bull . 1984; 14:15-6. [PubMed 6592122]
26. Benke PJ. The isotretinoin teratogen syndrome. JAMA . 1984; 251:3267-9. [PubMed 6587131]
27. de la Cruz E, Sun S, Vangvanichyakorn K et al. Multiple congenital malformations associated with maternal isotretinoin therapy. Pediatrics . 1984; 74:428-30. [PubMed 6591112]
28. Lammer EJ, Chen DT, Hoar RM et al. Retinoic acid embryopathy. N Engl J Med . 1985; 313:837-41. [PubMed 3162101]
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30. Cohen M, Rubenstein A, Li JK et al. Thymic hypoplasia associated with isotretinoin embryopathy. Am J Dis Child . 1987; 141:263-6. [PubMed 3492909]
31. Galderma. Differin® (adapalene) solution 0.1% prescribing information. Fort Worth, TX; 1997 Jul.
32. Galderma Laboratories. Differin® cream 0.1% (adapalene) prescribing information. Fort Worth, TX; 2000 May.
33. Galderma Laboratories, Fort Worth, TX: Personal communication.