Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablets

  • 5mg
  • 10mg
  • 15mg
  • 25mg

powder for injection

  • 50mg
  • 100mg
  • 200mg
  • 350mg
  • 500mg

injectable solution

  • 10mg/mL
more...

Methotrexate Overdose

1:1 ratio for leucovorin to inadvertent methotrexate overdose, within 1 hr

Initial IV, then may switch to IM q6hr and continue until methotrexate level has fallen below 0.05 micromolar and the renal failure has resolved

High Dose Methotrexate Rescue

10 mg/m² IV q6hr starting 24 hr after methotrexate 

May give PO after 1st IV dose

Coadministration with Trimetrexate (Discontinued)

20 mg/m² IV/PO q6hr (for PO, round dose up to next 25 mg increment) 

Dose adjustment for both trimetrexate & leucovorin may be necessary if hematologic toxicity occurs

Advanced Colorectal Carcinoma (with 5FU)

Recommended 20 mg/m² IV followed by 425 mg/m² fluorouracil 

Dose reduction treatment pause may be necessary based on hematologic toxicity

Methanol Poisoning

1 mg/kg (50-70 mg adults) IV q4-6hr

Trimethoprim Toxicity

10 mg/m² PO q6hr

Other Indications & Uses

Bone marrow suppression due to folic acid antagonism, megaloblastic anemia

Dosage Forms & Strengths

tablets

  • 5mg
  • 10mg
  • 15mg
  • 25mg

powder for injection

  • 50mg
  • 100mg
  • 200mg
  • 350mg
  • 500mg

injectable solution

  • 10mg/mL
more...

Methotrexate Overdose

1:1 ratio for leucovorin to inadvertent methotrexate overdose, within 1 hr

Initial IV, then may switch to IM q6hr and continue until methotrexate level has fallen below 0.05 micromolar and the renal failure has resolved

High Dose Methotrexate Rescue

10 mg/m² IV q6hr starting 24 hr after methotrexate

May give PO after 1st IV dose

Trimethoprim Toxicity

10 mg/m² PO q6hr

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Interactions

Interaction Checker

and leucovorin

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Diarrhea

            Nausea

            Vomiting

            Stomatitis

            Thrombocytosis

            Anaphylactoid reaction

            Wheezing

            Urticaria

            Anaphylactoid reactions

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            Warnings

            Contraindications

            Vitamin B12 deficiency anemia and pernicious anemia

            Cautions

            Hypersensitivity reactions including anaphylactoid reactions & urticaria

            Risk of severe neurological complications in patients with undiagnosed anemia

            Geriatric or debilitated patients receiving cotreatment with fluorouracil

            May increase tosicity of 5-fluorouracil

            May increase treatment failure of sulfamethoxazole-trimethoprim therapies

            Formulations containing benzyl alcohol not to be used in infants

            Thrombocytosis reported during intra-arterial infusion of methotrexate

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: not known whether distributed in breast milk; use caution

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Serves as a cofactor supplement to counteract folic acid antagonists such as methotrexate; leucovorin is an active metabolite of folic acid

            Displaces methotrexate from intracellular binding sites and restores the folate required for DNA/RNA synthesis

            In methanol toxicity it serves as a tetrahydrofolate source to help the body eliminate the formic acid resulting from methanol's toxicity

            Pharmacokinetics

            Distribution: all body tissues, predominantly in liver

            Metabolism: Rapidly converted to THF derivatives

            Excretion: Urine (primarily); feces

            Half-life elimination: 4-8hr

            Peak plasma time: 2 hr (PO); 10 min (as folate); 1 hr (as tetrahydrofolate)

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            Administration

            IV Incompatibilities

            Additive: fluorouracil, trimetrexate

            Syringe: droperidol, trimetrexate, fluorouracil

            Y-site: amphotericin B cholesteryl sulfate, droperidol, foscarnet, NaHCO3

            IV Compatibilities

            Solution: compatible w/ most common fluids

            Additive: cisplatin, cisplatin w/ floxuridine, floxuridine

            Syringe: bleomycin, cisplatin, cyclophosphamide, doxorubicin, droperidol, fluorouracil, furosemide, heparin, methotrexate, metoclopramide, mitomycin, vinblastine, vincristine

            Y-site (partial list): bleomycin, cisplatin, cyclophosphamide, fluorouracil(?), furosemide, heparin, linezolid, methotrexate, metoclopramide, mitomycin

            IV Preparation

            Reconstitute w/ BWI or SWI of 10 mg/mL or 20 mg/mL (for 350 mg vial)

            Available in 10 mg/mL preservative-free solutions

            Do not use benzyl alcohol-containing diluents for doses >10 mg/sq.meter

            Reconstituted solution is stable for 7 d

            Use immediately if reconstituted w/ preservative-free solution

            IV/IM Administration

            Infusion: not to exceed 160 mg/min

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            Images

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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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