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

Interaction Checker

and aminolevulinic acid oral

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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

            Postmarketing Reports

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

            Metabolism and nutrition disorders: Metabolic acidosis

            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

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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 24 hr postoperatively

            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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            Formulary

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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
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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