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Aminolevulinic Acid (Monograph)

Brand name: Levulan
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
ATC class: L01XD04
VA class: DE350
Chemical name: 5-Aminolevulinic acid hydrochloride
Molecular formula: C5H9NO3•HCl
CAS number: 5451-09-2


Photosensitizer; hydrochloride salt of 5-aminolevulinic acid, an endogenous precursor of protoporphyrin IX.

Uses for Aminolevulinic Acid

Nonhyperkeratotic Actinic Keratoses of Face or Scalp

Treatment of minimally to moderately thick (nonhyperkeratotic) actinic keratoses of the face or scalp, in conjunction with blue light illumination using the BLU-U Blue Light Photodynamic Therapy Illuminator (BLU-U).

Aminolevulinic Acid Dosage and Administration



Topical Administration

Preparation of the Applicator

With the applicator cap pointing up, sequentially break the 2 glass ampuls within the plastic applicator by applying finger pressure to appropriate position on the bottom ampul (vehicle solution), then the top ampul (powdered drug).

With applicator cap pointed away from face, shake applicator gently for at least 3 minutes to completely dissolve the drug in the vehicle. Do not press on end cap while shaking.

Topical Application

Apply topically; use within 2 hours because of the instability of the activated product. If application of the solution is not completed within 2 hours of activation, discard applicator and use a new one.

Clean and dry lesions prior to application of solution.

Gently dab target lesions directly with wet applicator tip, uniformly wetting lesion surface, including the edges, without excess running or dripping.

Allow application to dry and then reapply one time in the same manner.

Illumination of Treated Lesions

14–18 hours after application, gently rinse target lesions with water, pat dry, and photoactivate with blue light illumination from the BLU-U Blue Light Photodynamic Therapy Illuminator.

Patients and medical personnel should use blue light-blocking protective eyewear during BLU-U illumination.

Solution is not intended for use with any device other than the BLU-U Blue Light Photodynamic Illuminator.



Actinic Keratoses

Apply solution to lesions as directed (See Topical Application under Dosage and Administration); allow to dry and reapply once. 14–18 hours later, expose affected areas to BLU-U illumination for 1000 seconds [16 minutes, 40 seconds].

After 8 weeks, apply solution a second time to lesions that have not completely resolved.

Cautions for Aminolevulinic Acid




Topical Application Only

Solution contains alcohol; for topical use only. Do not apply in or around the eyes or to mucous membranes. May cause excessive irritation if applied under occlusion.

General Precautions

Application by Health Professional

Only qualified medical personnel should apply solution; application to perilesional area of face or scalp may result in photosensitivity.

Photosensitivity Reactions

Sites will be photosensitive after topical application of solution; stinging and/or burning sensation, erythema, and/or edema of lesions may occur with exposure to bright light.

Avoid exposure of treated sites to sunlight or bright indoor light (e.g., examination lamps, operating room lamps, tanning beds, lights at close proximity) prior to blue light photoactivation.

Protect treated lesions from sun by wearing a wide-brimmed hat or similar head covering of light-opaque material, and keep lesions dry. Sunscreens will not protect against photosensitivity reactions caused by visible light.

Reduce exposure to light if stinging and/or burning occurs.

Dermatologic Reactions

Following photoactivation with blue light, reddening, swelling, and scaling of treated actinic keratoses and surrounding skin may occur.

Lesion changes usually resolve completely within 4 weeks after treatment.

Delay in Receiving Blue Light Treatment

Patients should contact clinician if they cannot return for blue light treatment 14–18 hours after application of solution.

Patients should continue to avoid exposure of photosensitized lesions to sunlight or prolonged or intense light for ≥40 hours after solution application.

Specific Populations


Category C.


Not known whether aminolevulinic acid is distributed into milk; use caution.

Common Adverse Effects

Transient local stinging and/or burning, itching, erythema, edema, scaling/crusting, itching, hypopigmentation/hyperpigmentaion, erosion, skin disorder (unspecified), wheal/flare, vesiculation.

Drug Interactions

No formal drug interaction studies performed. No drug-specific interactions noted during controlled clinical trials.

Other Known Photosensitizing Agents

Potential pharmacologic interaction (increased photosensitivity reaction) with other known photosensitizing agents (e.g., griseofulvin, thiazide diuretics, sulfonylureas, phenothiazines, sulfonamides, tetracyclines).

Aminolevulinic Acid Pharmacokinetics



50-60% after a 128-mg oral dose of aminolevulinic acid hydrochloride (equivalent to 100 mg of aminolevulinic acid).


Time to Peak Fluorescence

Peak fluorescence intensity for protoporphyrin IX (metabolite of aminolevulinic acid) reached at approximately 11 or 12 hours in actinic keratoses or perilesional skin, respectively.



0.83 or 0.7 hours with a 128-mg aminolevulinic acid hydrochloride IV or oral dose, respectively.

Mean fluorescence half-life of 30 or 28 hours in lesions or perilesional skin, respectively.





20–25°C; excursions permitted to 15–30°C. Discard reconstituted solution 2 hours after mixing.


Advice to Patients


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.

Aminolevulinic Acid Hydrochloride


Dosage Forms


Brand Names



For solution

354 mg (for preparation of a 20% solution)

Levulan Kerastick (1.5 mL alcohol 48% v/v and isopropyl alcohol diluent)


AHFS DI Essentials™. © Copyright 2024, Selected Revisions August 1, 2007. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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