Leucovorin

Name: Leucovorin

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)

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

An overdose of leucovorin is not likely to cause life-threatening symptoms. However, leucovorin overdose can make other medications less effective.

What should I avoid while taking leucovorin?

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

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