Leucovorin

Administration

• Type: Antidote; Chemotherapy Modulating Agent; Rescue Agent (Chemotherapy)
• Dosage Forms: 5,10,15,25
• Routes of Administration: IV, IM
• Common Trade Names: Lederle Leucovorin

Adult Dosing

• Fluorouracil adjuvant tx, adv. colorectal CA
  • high dose: 200 mg/m^2 IV qd x5 days
  • low dose: 20 mg/m^2 IV qd x5 days

• Leucovorin rescue, high-dose methotrexate
  • normal methotrexate elimination: 15 mg PO/IM/IV q6h x10 doses
  • delayed late methotrexate elimination: 15 mg PO/IM/IV q6h; Max: 25 mg/dose PO, May give higher doses IM/IV

• Delayed early methotrexate elimination and/or acute renal injury: 150 mg IV q3h until methotrexate level <1 micromolar, then 15 mg IV q3h

• Leucovorin rescue, methotrexate overdose: 10 mg/m^2 PO/IM/IV q6h

• Folate antagonist overdose
  • pemetrexed: 50 mg/m^2 IV q6h x8 days; Start: 100 mg/m^2 IV x1
  • pyrimethamine, trimethoprim: 5-15 mg PO/IM/IV qd until hematopoiesis restored

• Megaloblastic anemia, folate-deficient: <1 mg IM/IV qd
  • Max: 1 mg/day

Pediatric Dosing

• Leucovorin rescue, high-dose methotrexate
  • normal methotrexate elimination: 10 mg/m^2 PO/IM/IV q6h x10 doses; Start: 24h after methotrexate start; Max: 25 mg/dose PO
  • delayed late methotrexate elimination: 10 mg/m^2 PO/IM/IV q6h; Max: 25 mg/dose PO
  • delayed early methotrexate elimination and/or acute renal injury: 100 mg/m^2 IV q3h until methotrexate level <1 micromolar, then 10 mg/m^2 IV q3

• Leucovorin rescue, methotrexate overdose: 10 mg/m^2 PO/IM/IV q6h

• Folate antagonist overdose: 5-15 mg PO/IM/IV qd until hematopoiesis restored

• Megaloblastic anemia, folate-deficient: <1 mg IM/IV qd
  • Max: 1 mg/day

Special Populations

• Pregnancy Risk Factor: C

Renal Dosing

• Not defined

Hepatic Dosing

• Not defined

Contraindications

• Allergy to class/drug
• intrathecal administration
• caution if pernicious anemia
• caution if megaloblastic anemia, vitamin B12 deficient
• caution if vitamin B-12 deficiency

Adverse Reactions

Serious

• anaphylactoid rxn
• seizures
• syncope

Common

• urticaria
• nausea/vomiting (IV use)

Pharmacology

• Half-life: 6hr
• Metabolism: liver, GI, CYP450
• Excretion: Urine

References

<Epocrates, UpToDate>