Aminolevulinic Acid Oral

Aminolevulinic Acid Oral is a prescription medication indicated in patients with glioma (suspected WHO grades III or IV on preoperative imaging) as an adjunct for the visualization of malignant tissue during surgery.

• Aminolevulinic Acid Oral is available under the following different brand names: Gleolan.

Common side effects of Aminolevulinic Acid Oral include:

• fever
• low blood pressure (hypotension)
• nausea
• vomiting
• chills
• photosensitivity reaction
• skin rash from sun exposure
• abnormal liver function test
• diarrhea

Serious side effects of Aminolevulinic Acid Oral include:

• hypersensitivity reactions

Rare side effects of Aminolevulinic Acid Oral include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Lyophilized powder for oral solution

• 30 mg/mL (after reconstitution)

Glioma Imaging

Adult dosage

• 20 mg/kg orally approximately 3 hours (range 2-4 hours) before anesthesia induction
• Imaging instructions
  • Must be used with a standard surgical operating microscope adapted with a blue light-emitting light source (power density 40-80 mW/cm²) and ancillary excitation and emission filters to visualize fluorescence excitation in the wavelength of 375-440 nm and for observation from 620-710 nm
  • Filters transmit porphyrin fluorescence as red violet, as well as a fraction of backscattered blue excitation light necessary for distinguishing nonfluorescing tissue

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Aminolevulinic Acid Oral has severe interactions with no other drugs
• Aminolevulinic Acid Oral has serious interactions with at least 78 other drugs
• Aminolevulinic Acid Oral has moderate interactions with no other drugs
• Aminolevulinic Acid Oral has minor interactions with no other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity to ALA or porphyrins
• Acute or chronic types of porphyria, owing to the potential ineffectiveness of the drug in these patients

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Aminolevulinic Acid Oral?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Aminolevulinic Acid Oral?”

Cautions

• Risk of phototoxic reactions; do not administer phototoxic drugs for 24 hours during the 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 tumors 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 a 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 hours before and after administering oral ALA
  • In vitro studies suggest that phenytoin and other anticonvulsants may decrease cellular PpIX (ALA metabolite) accumulation

Pregnancy and Lactation

• No available human data in pregnant women to inform a drug-associated risk of adverse developmental outcomes
• In animal reproduction studies, no adverse developmental effects were observed with oral ALA administration to pregnant rabbits during organogenesis at doses 3 times the maximum recommended human oral dose
• Lactation
  • Unknown if distributed in human breast milk
  • To decrease exposure to the breastfed infant, advise a lactating woman to pump and discard breast milk after ALA administration for 24 hours (ie, 5-6 half-lives)
  • 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 the underlying maternal condition