aminolevulinic acid oral (Rx)

Brand and Other Names:Gleolan
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

lyophilized powder for oral solution

  • 30mg/mL (after reconstitution)

Glioma Imaging

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

20 mg/kg PO ~3 hr (range 2-4 hr) 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 Modifications

Renal impairment: Not studied; ~one-third of aminolevulinic acid (ALA) dose excreted in urine as parent drug; unknown if dose adjustments are needed

Hepatic impairment: Not studied; unknown if dose adjustments are needed

Dosing Considerations

Should only be used by neurosurgeons who have completed a training program on use of fluorescence in surgery (provided by the manufacturer)

Safety and efficacy not established

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Interactions

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              • acitretin

                aminolevulinic acid oral, acitretin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • adapalene

                aminolevulinic acid oral, adapalene. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • afatinib

                aminolevulinic acid oral, afatinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • alitretinoin topical

                aminolevulinic acid oral, alitretinoin topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • aminolevulinic acid topical

                aminolevulinic acid oral, aminolevulinic acid topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • amiodarone

                aminolevulinic acid oral, amiodarone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • bendroflumethiazide

                aminolevulinic acid oral, bendroflumethiazide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • bexarotene

                aminolevulinic acid oral, bexarotene. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • bicalutamide

                aminolevulinic acid oral, bicalutamide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • calcitriol topical

                aminolevulinic acid oral, calcitriol topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • celecoxib

                aminolevulinic acid oral, celecoxib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • chlorothiazide

                aminolevulinic acid oral, chlorothiazide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • chlorpromazine

                aminolevulinic acid oral, chlorpromazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • chlorpropamide

                aminolevulinic acid oral, chlorpropamide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • chlorthalidone

                aminolevulinic acid oral, chlorthalidone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ciprofloxacin

                aminolevulinic acid oral, ciprofloxacin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • cobimetinib

                aminolevulinic acid oral, cobimetinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • demeclocycline

                aminolevulinic acid oral, demeclocycline. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • diclofenac

                aminolevulinic acid oral, diclofenac. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • diclofenac topical

                aminolevulinic acid oral, diclofenac topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • diflunisal

                aminolevulinic acid oral, diflunisal. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • dong quai

                aminolevulinic acid oral, dong quai. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • doxycycline

                aminolevulinic acid oral, doxycycline. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • etodolac

                aminolevulinic acid oral, etodolac. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • fenoprofen

                aminolevulinic acid oral, fenoprofen. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • fluphenazine

                aminolevulinic acid oral, fluphenazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • flurbiprofen

                aminolevulinic acid oral, flurbiprofen. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • gemifloxacin

                aminolevulinic acid oral, gemifloxacin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • glimepiride

                aminolevulinic acid oral, glimepiride. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • glipizide

                aminolevulinic acid oral, glipizide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • glyburide

                aminolevulinic acid oral, glyburide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • griseofulvin

                aminolevulinic acid oral, griseofulvin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • hydrochlorothiazide

                aminolevulinic acid oral, hydrochlorothiazide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ibuprofen

                aminolevulinic acid oral, ibuprofen. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ibuprofen IV

                aminolevulinic acid oral, ibuprofen IV. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • indapamide

                aminolevulinic acid oral, indapamide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • indomethacin

                aminolevulinic acid oral, indomethacin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • isotretinoin

                aminolevulinic acid oral, isotretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ketoprofen

                aminolevulinic acid oral, ketoprofen. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ketorolac

                aminolevulinic acid oral, ketorolac. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ketorolac intranasal

                aminolevulinic acid oral, ketorolac intranasal. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • levofloxacin

                aminolevulinic acid oral, levofloxacin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • meclofenamate

                aminolevulinic acid oral, meclofenamate. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • mefenamic acid

                aminolevulinic acid oral, mefenamic acid. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • meloxicam

                aminolevulinic acid oral, meloxicam. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • methyclothiazide

                aminolevulinic acid oral, methyclothiazide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • methyl aminolevulinate

                aminolevulinic acid oral, methyl aminolevulinate. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • metolazone

                aminolevulinic acid oral, metolazone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • minocycline

                aminolevulinic acid oral, minocycline. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • moxifloxacin

                aminolevulinic acid oral, moxifloxacin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • nabumetone

                aminolevulinic acid oral, nabumetone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • naproxen

                aminolevulinic acid oral, naproxen. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • ofloxacin

                aminolevulinic acid oral, ofloxacin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • oxaprozin

                aminolevulinic acid oral, oxaprozin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • oxytetracycline

                aminolevulinic acid oral, oxytetracycline. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • panitumumab

                aminolevulinic acid oral, panitumumab. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • perphenazine

                aminolevulinic acid oral, perphenazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • pirfenidone

                aminolevulinic acid oral, pirfenidone. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • piroxicam

                aminolevulinic acid oral, piroxicam. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • porfimer

                aminolevulinic acid oral, porfimer. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • prochlorperazine

                aminolevulinic acid oral, prochlorperazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • St John's Wort

                aminolevulinic acid oral, St John's Wort. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • sulfadiazine

                aminolevulinic acid oral, sulfadiazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • sulfamethoxazole

                aminolevulinic acid oral, sulfamethoxazole. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • sulfisoxazole

                aminolevulinic acid oral, sulfisoxazole. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • sulindac

                aminolevulinic acid oral, sulindac. Either increases levels of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • tetracycline

                aminolevulinic acid oral, tetracycline. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • thioridazine

                aminolevulinic acid oral, thioridazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • tolazamide

                aminolevulinic acid oral, tolazamide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • tolbutamide

                aminolevulinic acid oral, tolbutamide. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • tolmetin

                aminolevulinic acid oral, tolmetin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • tretinoin

                aminolevulinic acid oral, tretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • tretinoin topical

                aminolevulinic acid oral, tretinoin topical. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • trifluoperazine

                aminolevulinic acid oral, trifluoperazine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • vemurafenib

                aminolevulinic acid oral, vemurafenib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • verteporfin

                aminolevulinic acid oral, verteporfin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              • voriconazole

                aminolevulinic acid oral, voriconazole. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid administering other phototoxic drugs with aminolevulinic acid oral for 24 hr during perioperative period.

              Monitor Closely (0)

                Minor (0)

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                  Adverse Effects

                  1-10%

                  Note: An imbalance was notable for the adverse events of aphasia, ataxia, convulsion, and hemianopsia, and is likely related to the higher amount of brain resection performed in the ALA arm

                  Aphasia (8%)

                  Hemiparesis (7.8%)

                  Hemianopsia (3.2%)

                  Headache (2.7%)

                  Seizure (1.9%)

                  Hemiplegia (1.9%)

                  Monoparesis (1.3%)

                  Hypoesthesia (1.1%)

                  <1%

                  Cerebral edema

                  Frequency Not Defined

                  Transient amnestic episodes

                  Risk of BF-RhodoLED Lamp

                  Induced eye injury

                  Increased photosensitivity

                  Bleeding in patients with coagulation disorders

                  Ophthalmic adverse reactions

                  Mucous membrane irritation

                  Nausea (following surgery)

                  Vomiting (following surgery)

                  Hypotension (following surgery)

                  Postmarketing Reports

                  Immune disorders: Anaphylactic shock, angioedema, drug eruption, urticaria, erythema

                  Metabolism and nutrition disorders: Metabolic acidosis, pyrexia

                  Skin and subcutaneous tissue disorders: Application site inflammation and/or discoloration

                  Eye disorders: Eye irritation, diplopia, ocular hyperemia, photophobia, and blurred vision

                  General disorders and administration site conditions: Fatigue

                  Nervous system disorders: Dysaesthesia, transient amnestic episodes

                  Cardiovascular: Hypertension

                  Gastrointestinal disorders: Nausea, vomiting

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                  Warnings

                  Contraindications

                  Hypersensitivity to ALA or porphyrins

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

                  Cautions

                  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
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                  Pregnancy & Lactation

                  Pregnancy

                  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 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.

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                  Pharmacology

                  Mechanism of Action

                  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

                  Absorption

                  Absolute bioavailability: 100%

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

                  Distribution

                  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

                  Elimination

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

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

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                  Administration

                  Oral Preparation

                  Powder must be reconstituted before administration by healthcare personnel

                  Determine total number of vials needed to achieve intended dose as follows: Number of vials = body weight (kg) divided by 75 kg/vial

                  Completely remove the white cap and aluminum crimp seal from each vial

                  Remove and retain the rubber stopper from the vial

                  Using an appropriate volumetric measuring device (eg, flask, graduated cylinder, dosing syringe), measure 50 mL of drinking water and add to each vial (1500 mg/vial)

                  Gently swirl vial to completely dissolve powder

                  Resulting reconstituted solution is 30 mg/mL

                  Solution should appear clear and colorless to slightly yellowish

                  If required, replace the stopper and store reconstituted solution for up to 24 hr at room temperature prior to administration

                  Oral Administration

                  For oral use only

                  Calculate administration volume according the following equation: mL = (body weight (kg) x 20 mg/kg) divided by 30 mg/mL

                  Transfer entire contents of prepared vial(s) into an appropriate dosing container (eg, oral medicine bottle); ensure the entire contents of the vials are transferred

                  After transfer, discard the empty vial(s)

                  Using a disposable volumetric syringe, remove the administration volume of reconstituted solution from the dosing container and transfer to a separate oral dosing container

                  Discard unneeded solution

                  Administer PO 3 hr (range 2-4 hr) before anesthesia induction

                  Storage

                  Unopened vials: Store at room temperature (25°C [77°F]); excursions permitted to 15-30°C (59-86°F)

                  Reconstituted solution: May be stored for up to 24 hr at room temperature

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                  Images

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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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                  Formulary

                  FormularyPatient Discounts

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                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
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                  ST Step Therapy
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                  OR Other Restrictions
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.