Drug Index

Folinic acid

Synonym :


Mechanism :

Leucovorin is a mixture of the diastereoisomers of the 5¬formyl derivative of tetrahydrofolic acid. The biologically active component of the mixture is the L isomer, known as Citrovorum factor, or folinic acid. Leucovorin does not require reduction by the enzyme dihydrofolate reductase in order to participate in reactions utilizing folates as a source of one carbon moieties.

Indication :

  • Dihydrobiopterin reductase (DHPR) deficiency
  • Uridine monophosphate synthase (UMPS) deficiency
  • Methylene synthase deficiency
  • Hereditary folate malabsorption
  • Methylene tetrahydrofolate reductase deficiency
  • Cobalamin metabolism
  • Folate rescue after methotrexate therapy

Contraindications :

Contraindicated in pernicious anemia and other megaloblastic anemias secondary to the lack of vitamin B12.

Dosing :

Usual Pediatric Dose for Methotrexate Rescue:

10 mg/m² PO/IM/IV every 6 hours x 10 doses. If the serum methotrexate levels are >50 or 5 micromolar at 24 and 48 hours, or if there is a 50% or more increase in serum creatinine within the first 24 hours after the beginning of the methotrexate infusion, the dosage of leucovorin should be increased 20-fold (twice the dose and frequency) to 100 mg/m² IV every 3 hours until the MTX level is <0.05 micromolar.

Usual Pediatric Dose for Megaloblastic Anemia:

1 mg IV or IM once a day. Vitamin B12 should be replenished prior to or during folate replacement lest neurologic symptoms persist or worsen during hematologic remission.

Usual Pediatric Dose for Folic Acid Antagonist (TMP-SMX) Overdose:

2 to 15 mg/day orally for 3 days or until blood counts are normal or 5 mg orally every 3 days. 6 mg/day orally is recommended for use in patients with platelet counts <100,000/mm3.

Adverse Effect :

Allergic sensitization (anaphylactoid reactions, urticaria), pyrexia

Interaction :

Phenobarbital, Phenytoin and Primidone: In large amounts may counteract the antiepileptic effect of phenobarbital, phenytoin and primidone, and increase the frequency of seizures in susceptible children.

Leucovorin: May enhance the toxicity of fluorouracil.

Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-50Dose as in normal renal function
10-20Dose as in normal renal function
<10Dose as in normal renal function

Dose in Patients undergoing Renal Replacement Therapies
CAPDSome removal likely. Dose as in normal renal function
HDSome removal likely. Dose as in normal renal function
HDF/High fluxDialysed. Dose as in normal renal function
CAV/VVHDSome removal likely. Dose as in normal renal function

Hepatic Dose :

No dosage adjustments are recommended.
03/13/2024 06:22:43 Folinic acid
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