Actinic Keratosis Medication

Updated: Jun 03, 2021
  • Author: James M Spencer, MD; Chief Editor: William D James, MD  more...
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Medication Summary

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


Antineoplastic Agent, Topical

Class Summary

The drug of choice is topical 5-FU lotion or cream, which inhibits cell growth and proliferation.

Fluorouracil topical (Fluoroplex, Carac, Efudex, Tolak)

Fluorouracil topical is used topically for the management of actinic keratoses. It 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.

Ingenol mebutate topical (Picato)

The precise mechanism by which ingenol mebutate causes cell death in actinic keratosis is unknown, but it 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.


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 hours after treatment. At 4 hours 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.

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

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


Photosensitizing Agent, Topical

Class Summary

Topical photosensitizing agents are administered in combination with PDT.

Aminolevulinic acid (Levulan Kerastick, Ameluz)

This agent is a porphyrin precursor used in combination with narrow-band, red-light illumination for nonhyperkeratotic, nonpigmented actinic keratoses. When used with PDT, accumulation of photoactive porphyrins produces 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 hours later; treatment may be repeated every 8 weeks.

Topical solution 20% is 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-week treatment session. Each Levulan Kerastick should be used for only one patient.

Topical solution 10% is to be applied 1 mm thick to actinic keratosis and to approximately 5 mm of surrounding skin. Application area should not exceed 20 cm2 and 2 g at one time. After covering with a light-blocking occlusive dressing for 3 hours, remove the dressing, wipe off the remaining gel, and follow with red light illumination.


Nonsteroidal Anti-inflammatory Drug, Topical

Diclofenac transdermal gel (3%)

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

It is used topically as a keratolytic agent to treat actinic keratoses.


Microtubule inhibitor

Tirbanibulin topical (Klisyri)

Tirbanibulin topical is a novel, first-in-class microtubule inhibitor that inhibits tubulin polymerization and Src kinase signalling. It is indicated for the topical treatment of actinic keratosis of the face or scalp.