Pharmacology. Leucovorin (folinic acid or citrovorum factor) is a metabolically functional form of folic acid. Unlike folic acid, leucovorin does not require reduction by dihydrofolate reductase, and therefore it can participate directly in the one-carbon transfer reactions necessary for purine biosynthesis and cellular DNA and RNA production. In animal models of methanol intoxication, replacement of a deficiency of leucovorin and folic acid can reduce morbidity and mortality because these agents catalyze the oxidation of the highly toxic metabolite formic acid to nontoxic products. However, there is no evidence that their administration in the absence of a deficiency is effective.

Indications

1. 
   

   Folic acid antagonists (eg, methotrexate, trimethoprim, and pyrimethamine). Note: Leucovorin treatment is essential because cells are incapable of using folic acid owing to inhibition of dihydrofolate reductase.

   
   
2. 
   

   Methanol poisoning. Leucovorin is an alternative to folic acid.

Contraindications. No known contraindications.

Adverse effects

1. 
   

   Allergic reactions as a result of prior sensitization have been reported.

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