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Adapalene (Topical) (Monograph)

Brand name: Differin
Drug class: Keratolytic Agents

Medically reviewed by Drugs.com on May 10, 2024. Written by ASHP.

Introduction

Retinoid; synthetic naphthoic acid-derivative.7 8 10 11 12 13 14 15 16 17 18 19 20 22

Uses for Adapalene (Topical)

Acne Vulgaris

Treatment of acne vulgaris.1 4 5 6 7 11 12 13 14 16 17 18 19 20 21 22 31 32

Adapalene (Topical) Dosage and Administration

Administration

Topical Administration

Apply a thin film to skin as a cream, gel, or solution.1 4 5 7 11 12 13 16 17 18 19 20 21 22 31 32

Cleanse and dry the affected areas prior to application.1 31 32

Do not apply to eye(s), lips, angles of nose, or mucous membranes.1 31 32

A transient feeling of pruritus or burning may occur immediately after application.1 12 31 32 If increased sensitivity or irritation occurs, reduce frequency of application or, depending on the severity, discontinue use.1 31 32

Apparent exacerbation of acne that may occur during early weeks of therapy is attributable to the drug’s action on previously unseen lesions; do not discontinue.1 31 32

Excessive use does not increase therapeutic effects and may produce marked erythema, peeling, and discomfort.1 31 32

Pledgets

Remove single-use pledget applicators from foil immediately before use, use once, and then discard; do not use if seal is broken.31

Dosage

Pediatric Patients

Acne Vulgaris
Topical

Children and adolescents ≥12 years of age: Apply once daily in the evening at bedtime.1 12 31 32

Improvement usually detectable within 8–12 weeks.1 31 32

Adults

Acne Vulgaris
Topical

Apply once daily in the evening at bedtime.1 12 31 32

Improvement usually detectable within 8–12 weeks.1 31 32

Prescribing Limits

Pediatric Patients

Acne Vulgaris
Topical

Children and adolescents ≥12 years of age: most reported experience to date has been for treatment periods that did not exceed 12 weeks.4 5 6 12 22

Adults

Acne Vulgaris
Topical

Most reported experience to date has been for treatment periods that did not exceed 12 weeks.4 5 6 12 22

Cautions for Adapalene (Topical)

Contraindications

Warnings/Precautions

Sensitivity Reactions

Photosensitivity

Increased risk for sunburn; minimize exposure to sunlight or artificial UV irradiation sources (e.g., sunlamps).1 31 32

Use caution in patients subjected to considerable occupational sun exposure or with inherent sun sensitivity; use of sunscreen products (SPF 15 or greater) and protective clothing over treated areas recommended when exposure cannot be avoided.1 31 32

Avoid concomitant use of photosensitizing agents.33 (See Interactions.)

Use not recommended in patients with sunburn until full recovery occurs.1 31

Other Sensitivity Reactions

Discontinue therapy if sensitivity reaction or chemical irritation occurs.1 31 32

General Precautions

Dermatologic Effects

Erythema, dryness, scaling, burning, or pruritus may occur.1 31 32 If increased sensitivity or irritation occurs, use less frequently or, depending on the severity of the reaction, discontinue.1 31 32

Do not apply to cuts, abrasions, or eczematous or sunburned skin.1 31 32 (See Photosensitivity under Cautions.)

Facial Cleansing

Use of mild or soapless cleanser is recommended; use medicated or drying soaps and abrasive soaps and cleansers with caution.1 31 32

Cosmetic Agents or Processes

Avoid use of irritating cosmetics, other preparations, or processes (e.g., electrolysis) that might dry or irritate the skin.33 (See Interactions.)

Environmental Stimuli

Possible increased skin irritation in patients exposed to environmental extremes (e.g., wind, cold).1 31 32

Dry Skin

Use moisturizers if necessary; avoid preparations containing alpha hydroxy or glycolic acids.32

Specific Populations

Pregnancy

Category C.1 31 32

Lactation

Not known whether adapalene is distributed into milk.1 31 32 Use caution.1 31 32

Pediatric Use

Safety and efficacy not established in children <12 years of age.1 31 32

Geriatric Use

Insufficient experience in controlled clinical studies in patients ≥65 years of age to determine whether geriatric patients respond differently to adapalene than younger adults.32 However, clinical experience generally has not revealed age-related differences.32

Common Adverse Effects

Erythema, scaling, dryness, pruritus, burning/stinging.1 31 32

Drug Interactions

Specific Drugs

Drug

Interaction

Comments

Keratolytic agents (e.g., resorcinol, salicylic acid, sulfur)

Possible additive effects1 31 32

Allow sufficient time for the effects of the keratolytic agent to subside before initiating adapalene1 31 32

Photosensitizing agents (e.g., fluoroquinolone anti-infectives, phenothiazines, sulfonamides, thiazide diuretics)

Possible increased phototoxicity33

Avoid concomitant use33

Other Topical Preparations

Potential pharmacodynamic interaction (increased skin irritation).1 31 32 Avoid concurrent use of topical preparations with high concentrations of alcohol, menthol, spices, or lime (e.g., lotions, astringents, perfume); irritating cosmetics (e.g., toners, peeling [desquamating] agents); permanent wave solutions; or hair depilatories or waxes.1 31 32 33

Adapalene (Topical) Pharmacokinetics

Absorption

Bioavailability

Minimally absorbed following topical application.1 31 32

Elimination

Elimination Route

Eliminated principally by biliary excretion.1 31 32

Stability

Storage

Topical

Cream, Gel, Solution

20–25°C.1 31 32

Protect cream from freezing.32

Store solution upright in tight container.31

Actions

Advice to Patients

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.

Preparations

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.

Adapalene

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

0.1%

Differin (with parabens)

Galderma

Gel

0.1%

Differin (with methylparaben and propylene glycol)

Galderma

Pledgets (saturated with solution)

0.1%

Differin (with SD alcohol 40-B 30% w/v)

Galderma

Solution

0.1%

Differin (with SD alcohol 40-B 30% w/v)

Galderma

AHFS DI Essentials™. © Copyright 2024, Selected Revisions May 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Galderma. Differin (adapalene) gel 0.1% prescribing information. Fort Worth, TX; 1996 May.

2. Hurwitz S. Acne vulgaris: current concepts of pathogenesis and treatment. Am J Dis Child. 1979; 133:536-44. http://www.ncbi.nlm.nih.gov/pubmed/155397?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/1827344?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/8609263?dopt=AbstractPlus

6. Bernard BA. Adapalene, a new chemical entity with retinoid activity. Skin Pharmacol. 1993; 6(Suppl 1):61-9. http://www.ncbi.nlm.nih.gov/pubmed/8142113?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/8396608?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/2139085?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/2109510?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/2069410?dopt=AbstractPlus

11. Leyden JJ. Therapy for acne vulgaris. N Engl J Med. 1997; 336:1156-62. http://www.ncbi.nlm.nih.gov/pubmed/9099661?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/9074847?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/9204085?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/9204087?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/9204090?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/9204091?dopt=AbstractPlus

22. Anon. Adapalene for acne. Med Lett Drugs Ther. 1997; 39:19-20. http://www.ncbi.nlm.nih.gov/pubmed/9057779?dopt=AbstractPlus

23. Thiboutot DM. Acne: an overview of clinical research findings. Dermatol Clin. 1997; 15:97-109. http://www.ncbi.nlm.nih.gov/pubmed/9001864?dopt=AbstractPlus

24. Gibson JR. Rationale for the development of new topical treatments for acne vulgaris. Cutis. 1996; 57:13-9. http://www.ncbi.nlm.nih.gov/pubmed/8654127?dopt=AbstractPlus

25. Anon. Update on birth defects with isotretinoin. FDA Drug Bull. 1984; 14:15-6. http://www.ncbi.nlm.nih.gov/pubmed/6592122?dopt=AbstractPlus

26. Benke PJ. The isotretinoin teratogen syndrome. JAMA. 1984; 251:3267-9. http://www.ncbi.nlm.nih.gov/pubmed/6587131?dopt=AbstractPlus

27. de la Cruz E, Sun S, Vangvanichyakorn K et al. Multiple congenital malformations associated with maternal isotretinoin therapy. Pediatrics. 1984; 74:428-30. http://www.ncbi.nlm.nih.gov/pubmed/6591112?dopt=AbstractPlus

28. Lammer EJ, Chen DT, Hoar RM et al. Retinoic acid embryopathy. N Engl J Med. 1985; 313:837-41. http://www.ncbi.nlm.nih.gov/pubmed/3162101?dopt=AbstractPlus

29. Rosa FW, Wilk AL, Kelsey FO. Teratogen update: vitamin A congeners. Teratology. 1986; 33:355-64. http://www.ncbi.nlm.nih.gov/pubmed/3461576?dopt=AbstractPlus

30. Cohen M, Rubenstein A, Li JK et al. Thymic hypoplasia associated with isotretinoin embryopathy. Am J Dis Child. 1987; 141:263-6. http://www.ncbi.nlm.nih.gov/pubmed/3492909?dopt=AbstractPlus

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.

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