Dosing and uses of Ameluz (aminolevulinic acid)
Adult dosage forms and strengths
topical gel (Ameluz)
- 10%
topical solution (Levulan Kerastick)
- 20%
Actinic Keratosis
Ameluz: Used in combination with photodynamic therapy (PDT) using BF-RhodoLED lamp, a narrowband, red light illumination source, is indicated for lesion-directed and field-directed treatment of actinic keratoses (AKs) of mild-to-moderate severity on the face and scalp
Levulan Kerastick: Indicated for treatment of minimally to moderately thick actinic keratoses of the face or scalp with blue light illumination using the BLU-U Blue Light Photodynamic Therapy (PDT) Illuminator
See Administration
Pediatric dosage forms and strengths
Safety and efficacy not established
Ameluz (aminolevulinic acid) adverse (side) effects
>10%
Erythema (92%)
Pain/burning (92%)
Irritation (72%)
Edema (35%)
Pruritus (34%)
Exfoliation (19%)
Scab (19%)
Induration (12%)
Vesicles (12%)
1-10%
Paresthesia (9%)
Hyperalgesia (5%)
Discomfort (3%)
Erosion (3%)
Discharge (2%)
Bleeding (1%)
Pustules (1%)
Postmarketing Reports
Skin and subcutaneous tissue disorders: Erythema, swelling, application site inflammation, skin discoloration
Eye disorders: Eye irritation, diplopia, ocular hyperemia, photophobia, and blurred vision
Warnings
Contraindications
Hypersensitivity to porphyrins
Hypersensitivity to any gel components, which includes soybean phosphatidylcholine
Porphyria; drug may cause uncontrolled phototoxic effects
Known photodermatoses of varying pathology and frequency (eg, metabolic disorders [aminoaciduria], idiopathic or immunological disorders [polymorphic light reaction], genetic disorders [xeroderma pigmentosum], and diseases precipitated or aggravated by exposure to sun light [lupus erythematoides or pemphigus erythematoides])
Cautions
For topical use only on the face and scalp; applied by physician or qualified medical personneL
BF-RhodoLED lamp may cause eye irritation, glare, or injury; protective eye equipment must be used by patient, healthcare providers and any person present during the illumination period
Has not been tested on patients with inherited or acquired coagulation disorders; special care should be taken to avoid bleeding during lesion preparation
Eyelid edema and mucous membrane irritation reported; rinse eyes with water in case of accidental contact
Pregnancy
Pregnancy
No available data
Lactation
Unknown if distributed in human breast milk
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Ameluz (aminolevulinic acid)
Mechanism of action
Aminolevulinic acid is a precursor of photoactive porphyrins, which accumulate in the skin lesions where the product has been applied and are subsequently illuminated with a photodynamic lamp
When exposed to the light, the accumulated photoactive porphyrins produce a photodynamic reaction, resulting in a cytotoxic process dependent on the simultaneous presence of oxygen, which as a result generates a singlet oxygen; the singlet oxygen can then react to form superoxide and hydroxyl radicals
Absorption
Plasma concentration: After occlusion for 3 hr, up to 2.5-fold increase of aminolevulinic acid plasma concentrations observed
Peak plasma time: 3 hr
Peak plasma concentration: 27.19 ng/mL
AUC: 142.83 mg·h/mL
Administration
Topical Administration
Topical product should be only applied by physician or qualified medical personneL
For topical use only; not for ophthalmic, oral, or intravaginal use
Photodynamic therapy is a multistep process
Ameluz
- One session of photodynamic therapy should be administered for single lesions or an entire field affected by multiple lesions
- Evaluate 3 months after treatment
- Non- or partially responding lesions should be retreated in a second session
- Step 1: Lesion preparation
- Before applying gel, carefully wipe all lesions with an ethanol or isopropanol-soaked cotton pad to ensure degreasing of the skin
- Thereafter, gently roughen all lesion surfaces; take care to avoid bleeding
- Step 2: Gel application
- Using gloved protected fingertips or spatula, apply gel ~1 mm thick to lesion(s) and include ~5 mm of the surrounding skin; if multiple lesions, cover the entire area (not to exceed 20 cm² and no more than 2 g (ie, 1 tube) for a session
- The gel can be administered to healthy skin around the lesions, whereas application near the eyes, nostrils, mouth, ears or mucosa should be avoided (keep a distance of 1 cm)
- Avoid direct contact of gel with the eyes or mucous membrane; if accidentally exposed, rinse with water
- Step 3: Occlude for 3 hours
- Allow gel to dry for ~10 minutes, before an occlusive light-tight dressing is placed over the treatment site
- Following 3 hr of incubation, the dressing should be removed and the remnant gel wiped off
- Illumination with red light
- Immediately after cleaning the lesions, the entire treatment area will be illuminated with a red light source with a narrow spectrum around 635 nm that delivers a light dose of approximately 37 J/cm² within 10 minutes
- During illumination the lamp should be fixed at the distance from the skin surface that is indicated in the user manual
- Position the lamp head 5-8 cm from the skin’s surface; when an area of 8 x 18 cm is illuminated, the effective treatment area is 6 x16 cm
- Larger areas can be illuminated in several steps
- If for any reason, the lesions cannot be illuminated within 3 hr after application, rinse off the gel with saline and water
- For 2 days, protect the lesion sites and surrounding skin from sunlight or prolonged or intense light
Levulan Kerastick
- Prepare Kerastick solution by crushing the bottom ampule (diluent) and then the top ampule (powder) of the stick to; shake gently for 30 sec
- 1 application per site per 8 week session
- Apply to affected area; allow to dry
- Follow application with blue light (400-450 nm) photodynamic blue light treatment 14-18 hr later
- May treat a second time lesions that did not completely healed after 8 hr
Storage
Store refrigerated between 2-8°C (36-46˚F); excursions permitted to 15-30°C (59-86°F)
Ameluz: After opening, can be stored for up to 12 wk in a refrigerator at 2-8°C (36-46˚F) if the tube is tightly closed
Levulan Kerastick: Solution must be used within 2 hr of dissolution
