Drug information of aminolevulinic acid oral

aminolevulinic acid oral

Drug group:

Aminolevulinic acid is given before surgery to remove a glioma (a type of brain or spinal cord tumor).

Mechanism of effect

ALA occurs endogenously as a metabolite that is formed in the mitochondria from succinyl-CoA and glycine; exogenous administration leads to accumulation of the ALA metabolite PpIX in tumor cells

The reason for the accumulation of PpIX in neoplastic brain tissue is not known

During glioma surgery, an operating microscope adapted with a blue-emitting light source and filters for excitation light of wavelength 375-440 nm, and observation at wavelengths of 620-710 nm is used; this allows tumor tissue to be visualized as red fluorescence; tissue lacking sufficient PpIX concentrations appears blue


Not available


Absolute bioavailability: 100%

Peak concentration time: 0.8 hr (ALA); 4 hr (PpIX)

Protein bound: 12%

Metabolism: Metabolized to PpIX, but the fraction of administered ALA that is metabolized to PpIX is unknown

Average plasma AUC of PpIX is <6% of ALA’s AUC

Half-life: 0.9 hr (ALA); 3.6 hr (PpIX)

Excretion: 34% (range 27-57%) in urine



Glioma Imaging

20 mg/kg PO ~3 hr (range 2-4 hr) before anesthesia induction


Safety and efficacy not established


Risk of phototoxic reactions; do not administer phototoxic drugs for 24 hr during perioperative period; reduce exposure to sunlight or room lights for 48 hours after administration of therapy

Errors may occur, including false negatives and false positives; nonfluorescing tissue in the surgical field does not rule out the presence of tumor in patients with glioma; fluorescence may be seen in areas of inflammation or metastases from other tumor types

Transient amnestic episodes reported during postmarketing use in combination with photodynamic therapy; inform patients and caregivers that combination with photodynamic therapy may cause transient amnestic episodes; advise them to contact healthcare provider if amnesia occurs after treatment

Hypersensitivity reactions, including serious reactions reported; these reactions include anaphylactic shock, swelling, and urticaria; cardiopulmonary resuscitation personnel and equipment must be readily available and monitor all patients for hypersensitivity reactions

Drug interaction overview

  • Not an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A
  • Avoid administering phototoxic drugs (eg, St. John’s wort, griseofulvin, thiazide diuretics, sulfonylureas, phenothiazines, sulfonamides, quinolones, tetracyclines) and topical ALA preparations for 24 hr before and after administering oral ALA
  • In vitro studies suggest that phenytoin and other anticonvulsants may decrease cellular PpIX (ALA metabolite) accumulation

Points of recommendation

For 24 hours before and after taking aminolevulinic acid, you will need to protect your skin from light, both sunlight and bright indoor light.

You should not breast-feed within 24 hours after taking aminolevulinic acid. If you use a breast pump during this time, throw out any milk you collect. Do not feed it to your baby.

Ask a Pharmacist

User's questions
    No comments yet.