glucarpidase (Rx)

Brand and Other Names:Voraxaze
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, as lyophilized powder for reconstitution

  • 1,000 units/vial
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Methotrexate Toxicity

Indicated for treatment of toxic plasma methotrexate concentrations (>1 micromole/L) in patients with delayed methotrexate clearance due to impaired renal function

50 units/kg as a single IV injection over 5 minutes

Renal & Hepatic Impairment

Renal impairment: No dose adjustment is recommended

Hepatic impairment: No specific studies have been conducted

Dosage Forms & Strengths

injection, as lyophilized powder for reconstitution

  • 1,000 units/vial
more...

Methotrexate Toxicity

Indicated for treatment of toxic plasma methotrexate concentrations (>1 micromole/L) in patients with delaye methotrexate clearance due to impaired renal function

50 units/kg as a single IV injection over 5 minutes

Clinical trials in children

  • Effectiveness in pediatric patients was established in 22 patients in the efficacy dataset; 12 were pediatric patients with ages ranging from 5-16 years
  • The pooled clinical safety database included data for 147 patients from 1 month up to 17 years; no overall differences in safety were observed between pediatrics and adult patients

Renal & Hepatic Impairment

Renal impairment: No dose adjustment is recommended

Hepatic impairment: No specific studies have been conducted

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Interactions

Interaction Checker

and glucarpidase

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Paresthesias (2%)

            Flushing (2%)

            Nausea/vomiting (2%)

            Headache (1%)

            Hypotension (1%)

            <1%

            Blurred vision

            Diarrhea

            Hypersensitivity

            Hypertension

            Rash

            Throat irritation/throat tightness

            Tremor

            Frequency Not Defined

            Antibody formation

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            Warnings

            Contraindications

            None

            Cautions

            Serious allergic reactions (occurred in <1% of patients)

            Leucovorin is a substrate for glucarpidase; other potential substrates of glucarpidase include reduced folates and folate antimetabolites (eg, folic acid, L-methylfolate, pemetrexed, pralatrexate, trimethoprim, pentamidine)

            Immunogenicity: 17% (n=16) of patients developed anti-glucarpidase antibodies; 12 of the 16 patients had received 1 dose and the other 4 patients had received 2 doses

            Monitoring methotrexate serum concentrations

            • Methotrexate concentrations within 48 hours following administration of glucarpidase can only be reliably measured by a chromatographic method
            • DAMPA (4-deoxy-4-amino-N10-methylpteroic acid) is an inactive metabolite of methotrexate resulting from treatment with glucarpidase that interferes with the measurement of methotrexate concentration using immunoassays (ie, immunoassays overestimates the methotrexate concentration)
            • Due to the long half-life of DAMPA (~9 hours), measurement of methotrexate using immunoassays is unreliable for samples collected within 48 hours following glucarpidase administration

            Continuation and timing of leucovorin rescue

            • Leucovorin is a substrate for glucarpidase
            • Do not administer leucovorin within 2 hr before or after glucarpidase
            • No dose adjustment is recommended for the continuing leucovorin regimen because the leucovorin dose is based on the patient’s pre-glucarpidase methotrexate concentration
            • For the first 48 hours after glucarpidase, administer the same leucovorin dose as given prior to glucarpidase
            • Beyond 48 hours after glucarpidase, administer leucovorin based on the measured methotrexate concentration
            • Do not discontinue therapy with leucovorin based on the determination of a single methotrexate concentration below the leucovorin treatment threshold
            • Therapy with leucovorin should be continued until the methotrexate concentration has been maintained below the leucovorin treatment threshold for a minimum of 3 days
            • Continue hydration and alkalinization of the urine as indicated
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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Unknown whether distributed in breast milk; caution advised

            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

            Recombinant bacterial enzyme that hydrolyzes the carboxyl-terminal glutamate residue from folic acid and classical antifolates such as methotrexate

            Converts methotrexate to its inactive metabolites 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA) and glutamate

            Provides an alternate nonrenal pathway for methotrexate elimination in patients with renal dysfunction during high-dose methotrexate treatment

            Absorption

            Peak Plasma Concentration: 3.3 mcg/mL

            AUC: 23.3 mcg•hr/mL

            Distribution

            Vd: 3.6 L

            Elimination

            Half-life (based on serum activity levels): 5.6 hr; 8.2 hr (renal impairment)

            Half-life (based on serum total concentrations): 9 hr

            Systemic clearance: 7.5 mL/min

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            Administration

            IV Preparation

            Reconstitute the lyophilized powder in the vial with 1 mL of sterile saline for injection, USP

            Do not shake

            Roll and tilt the vial gently to mix

            Inspect the vial and discard if the solution is not clear, colorless, and free of particulate matter

            Use reconstituted solution immediately or store under refrigeration at 36-46°F (2-8°C) for up to 4 hr if not used immediately

            Contains no preservative and is supplied as a single-use vial

            Discard any unused product

            IV Administration

            Administer IV as a bolus over 5 minutes

            Flush IV line before and after administration

            Storage

            Unopened vials are stable until date indicated on package when stored at refrigerated 36-46°F (2-8°C)

            Reconstituted solution: May store under refrigeration at 36-46°F (2-8°C) for up to 4 hr if not used immediately

            Do not freeze

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            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
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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