Actinic Keratosis Medication

  • Author: James M Spencer, MD; Chief Editor: Dirk M Elston, MD   more...
 
Updated: Mar 19, 2012
 

Medication Summary

The goals of pharmacotherapy are to reduce morbidity and to prevent complications.

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Antineoplastic Agent, Topical

Class Summary

DOC is topical 5-FU lotion or cream, which inhibits cell growth and proliferation.

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Fluorouracil topical (Fluoroplex, Carac, Efudex)

 

Used topically for management of actinic keratoses. Interferes with DNA synthesis by blocking methylation of deoxyuridylic acid via inhibition of thymidylate synthetase and, subsequently, cell proliferation. For lesions on bald scalp or extremities, longer treatment is often necessary.

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Ingenol mebutate topical (Picato)

 

The precise mechanism by which ingenol mebutate causes cell death in actinic keratosis is unknown, but may include a dual action of 1) rapid lesion necrosis by mitochondrial swelling and membrane disruption, and 2) specific neutrophil-mediated, antibody-dependent cellular cytotoxicity by antibodies produced from B cells that bind to antigens on dysplastic epidermal cells.

The dosage for actinic keratosis differs depending on the application site. The 0.015% gel is used for application to the face or scalp for 3 consecutive days, whereas the 0.05% gel is used for application to the trunk or extremities for 2 consecutive days.

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Immunomodulator, Topical

Class Summary

Investigation of imiquimod demonstrates it induces interferons alpha and gamma, TNF-alpha, and interleukin 12, among other cytokines. Studies using 5% cream in mice showed significant induction of interferon alpha at the site of application, occurring as early as 2 h after treatment. At 4 h after application, increases in interferon alpha mRNA levels were found, indicating an increase in transcription. Cytokine up-regulation is thought to be activated by imiquimod binding to toll-like receptor VII.

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Imiquimod (Aldara 5% cream, Zyclara 3.75% cream)

 

Immune response modifier thought to produce a nonspecific anti–actinic keratosis response; interferon, natural killer cells) and a specific immune response (cytotoxic T cells). Indicated for clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp.

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Photosensitizing Agent, Topical

Class Summary

Administered in combination with PDT.

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Aminolevulinic acid (Levulan), Methyl aminolevulinate cream (Metvixia)

 

Porphyrin precursor used in combination with narrow-band, red-light illumination for nonhyperkeratotic, nonpigmented actinic keratoses. When used with PDT, accumulation of photoactive porphyrins produce a photodynamic reaction that results in a cytotoxic process dependent upon the simultaneous presence of oxygen.

PDT with aminolevulinic acid is a 2-stage process involving application of the solution followed by illumination with blue light 14-18 h later; treatment may be repeated every 8 weeks.

Levulan: Topical solution 20% intended for direct application to individual lesions diagnosed as actinic keratosis and not to perilesional skin. Application should involve either scalp or face lesions, but not both simultaneously. Recommended treatment frequency is 1 application and 1 dose of illumination per treatment site per 8-wk treatment session. Each Levulan Kerastick should be used for only 1 patient.

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Nonsteroidal Anti-inflammatory Drug, Topical

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Diclofenac topical (Solaraze)

 

Designated chemically as 2-[(2,6-dichlorophenyl) amino] benzeneacetic acid, monosodium salt, with an empirical formula of C14 H10 Cl2 NO2 Na. One of a series of phenylacetic acids that has demonstrated anti-inflammatory and analgesic properties in pharmacological studies. Believed to inhibit the enzyme cyclooxygenase, which is essential in the biosynthesis of prostaglandins. Can cause hepatotoxicity; hence, liver enzyme levels should be monitored in first 8 wk of treatment.

Used topically as a keratolytic agent to treat actinic keratoses.

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Contributor Information and Disclosures
Author

James M Spencer, MD  Professor of Clinical Dermatology, Mount Sinai School of Medicine, New York; Private Practice, Spencer Dermatology, St Petersburg, Florida

James M Spencer, MD is a member of the following medical societies: American Academy of Cosmetic Surgery, American Academy of Dermatology, American College of Mohs Micrographic Surgery and Cutaneous Oncology, American Dermatological Association, American Medical Association, American Society for Dermatologic Surgery, American Society for Laser Medicine and Surgery, and International Society for Dermatologic Surgery

Disclosure: Graceway Pharmaceutical Honoraria Speaking and teaching; Sanofi Aventis Honoraria Consulting; Medicis Grant/research funds Independent contractor; Peplin Grant/research funds Independent contractor

Coauthor(s)

Michelle Henry, MD  Resident Physician, Department of Dermatology, Mount Sinai School of Medicine of New York University

Disclosure: Nothing to disclose.

Specialty Editor Board

Kelly M Cordoro, MD  Assistant Professor of Clinical Dermatology and Pediatrics, Department of Dermatology, University of California, San Francisco School of Medicine

Kelly M Cordoro, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Dermatology, American Medical Association, Association of Professors of Dermatology, Dermatology Foundation, Medical Society of Virginia, National Psoriasis Foundation, Society for Pediatric Dermatology, and Women's Dermatologic Society

Disclosure: Nothing to disclose.

Michael J Wells, MD  Associate Professor, Department of Dermatology, Texas Tech University Health Sciences Center, Paul L Foster School of Medicine

Michael J Wells, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Dermatology, American Medical Association, and Texas Medical Association

Disclosure: Nothing to disclose.

Mary Farley, MD  Dermatologic Surgeon/Mohs Surgeon, Anne Arundel Surgery Center

Disclosure: Nothing to disclose.

Catherine M Quirk, MD  Clinical Assistant Professor, Department of Dermatology, University of Pennsylvania

Catherine M Quirk, MD is a member of the following medical societies: Alpha Omega Alpha and American Academy of Dermatology

Disclosure: Nothing to disclose.

Chief Editor

Dirk M Elston, MD  Director, Ackerman Academy of Dermatopathology, New York

Dirk M Elston, MD is a member of the following medical societies: American Academy of Dermatology

Disclosure: Nothing to disclose.

Additional Contributors

The authors and editors of eMedicine gratefully acknowledge the contributions of previous authors, James Fulton Jr, MD, PhD, and Amy Lynn Basile, DO, MPH, to the development and writing of this article. The authors and editors of eMedicine also gratefully acknowledge the contributions of previous Chief Editor, William D. James, MD, to the development and writing of this article.

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Courtesy of Hon Pak, MD, and reviewed by Ross Levy, MD.
Actinic keratosis during treatment with topical 5-fluorouracil. Courtesy of Hon Pak, MD, and reviewed by Ross Levy, MD.
Actinic keratosis right after treatment with topical 5-fluorouracil. Courtesy of Hon Pak, MD, and reviewed by Ross Levy, MD.
Erythematous, scaly lesions on the temple area, typical of actinic keratosis.
 
 
 
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