5-aminolevulinic acid hydrochloride: clinical use

Prescribing considerations

• Gliolan is restricted to trained, experienced neurosurgeons familiar with malignant glioma surgery and functional neuroanatomy.
• Gliolan fluorescence is an intraoperative aid, not a diagnostic test; false-positive and false-negative fluorescence can occur.
• Use Gliolan cautiously in clinically relevant renal or hepatic impairment and pre-existing cardiovascular disease.
• Ameluz should be used under guidance from a professional experienced in photodynamic therapy. Stop UV therapy beforehand and avoid treating bleeding lesions.
• Other skin disease or tattoos may compromise Ameluz efficacy and assessment.

Contraindications and cautions

• Gliolan: hypersensitivity to 5-ALA or porphyrins, acute or chronic porphyria, and pregnancy.
• Ameluz: hypersensitivity to 5-ALA, porphyrins, soya, peanuts or another excipient; porphyria; and known photodermatoses or diseases aggravated by sunlight.

Monitoring

• For Gliolan, preserve neurological function with appropriate localisation when tumour lies near eloquent brain structures; observe for hypotension and postoperative neurological complications.
• After Gliolan, apply strong-light precautions and consider clinically appropriate follow-up of blood counts and liver-related tests.
• During Ameluz illumination, monitor pain and local reactions; discontinue photodynamic therapy immediately if transient amnesia develops.
• Review treated skin for response, healing, persistent inflammation or infection.

Clinical pharmacology

5-ALA is a physiological haem precursor converted to protoporphyrin IX. Glioma fluorescence follows excitation by blue light. With Ameluz, activation in oxygenated tissue generates reactive oxygen species and phototoxic destruction of target cells; relevant systemic absorption after topical use is low.

Formulation and product differences

• Gliolan is an excipient-free powder reconstituted with drinking water as an oral solution for fluorescence-guided malignant glioma surgery.
• Ameluz is a white-to-yellowish cutaneous gel containing soybean phosphatidylcholine and sodium benzoate. It requires an appropriate red-light, natural-daylight or artificial-daylight method selected for the lesion and body site.
• Gliolan produces temporary general photosensitivity precautions, whereas Ameluz primarily photosensitises treated skin.

Gel

Route: Cutaneous

Strengths: 78 mg/g

Oral solution

Route: Oral

Strengths: 30 mg/mL