Photosensitizing Agent, Topical; Topical Skin Product

Treatment of non-hyperkeratotic actinic keratoses of the face or scalp; to be used in conjunction with blue light illumination

C

No adequate or well-controlled studies in pregnant women. Should be used during pregnancy only if clearly needed; excretion in breast milk is unknown; use caution in breast-feeding.

Individuals with cutaneous photosensitivity at wavelengths of 400-450 nm; porphyria; allergy to porphyrins; hypersensitivity to any component

For external use only. Do not apply to eyes or mucous membranes. Treatment site will become photosensitive following application. Patients should be instructed to avoid exposure to sunlight, bright indoor lights, or tanning beds during the period prior to blue light treatment. Should be applied by a qualified health professional to avoid application to perilesional skin. Has not been tested in individuals with coagulation defects (acquired or inherited).

Transient stinging, burning, itching, erythema and edema result from the photosensitizing properties of this agent. Symptoms subside between 1 minute and 24 hours after turning off the blue light illuminator. Severe stinging or burning was reported in at least 50% of patients from at least 1 lesional site treatment.

>10%: Dermatologic: Severe stinging or burning (50%), scaling of the skin/crusted skin (64% to 71%), hyperpigmentation/hypopigmentation (22% to 36%), itching (14% to 25%), erosion (2% to 14%)

1% to 10%:

Central nervous system: Dysesthesia (0% to 2%)

Dermatologic: Skin ulceration (2% to 4%), vesiculation (4% to 5%), pustular drug eruption (0% to 4%), skin disorder (5% to 12%)

Hematologic: Bleeding/hemorrhage (2% to 4%)

Local: Wheal/flare (2% to 7%), local pain (1%), tenderness (1%), edema (1%), scabbing (0% to 2%)

Monitoring and supportive care are recommended. Patient should be advised to avoid incidental exposure to intense light sources for at least 40 hours. The consequences of exceeding the recommended topical dosage are not known.

Photosensitizing agent including griseofulvin, thiazide diuretics, sulfonamides, sulfonylureas, phenothiazines, and tetracyclines theoretically may increase the photosensitizing potential of aminolevulinic acid

Store at 25°C (77°F). Topical solution should be used immediately following solution preparation and must be completed within 2 hours of solution preparation.

Aminolevulinic acid is a metabolic precursor of protoporphyrin IX (PpIX), which is a photosensitizer. Photosensitization following application of aminolevulinic acid topical solution occurs through the metabolic conversion to PpIX. When exposed to light of appropriate wavelength and energy, accumulated PpIX produces a photodynamic reaction.

Aminolevulinic acid:

Bioavailability: Oral: 50% to 60%

Half-life, mean: 0.7 ± 0.18 hours after oral

PpIX:

Peak fluorescence intensity: 11 ± 1 hour

Half-life, mean clearance for lesions: 30 ± 10 hours

Adults: Topical: Apply to actinic keratoses ( not perilesional skin) followed 14-18 hours later by blue light illumination. Application/treatment may be repeated at a treatment site after 8 weeks.

Actinic keratoses targeted for treatment should be clean and dry prior to application. Follow instructions for solution preparation and application. Solution is applied directly to the lesion, but not the perilesional skin, using the supplied applicator. Should not be applied to periorbital area or allowed to contact ocular or mucous membranes. Blue light exposure should follow between 14 and 18 hours after the application.

No information available to require special precautions

No effects or complications reported

Avoid exposure to sunlight, bright indoor lights, or tanning beds during the period prior to blue light treatment. Wear a wide-brimmed hat to protect from exposure. Sunscreens do not protect against photosensitization by this agent.

Solution, topical: 20% (with applicator)

To be used in conjunction with the BLU-U™ Blue Light Photodynamic Therapy Illuminator