Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2016 Publisher: Pfizer Ltd, Ramsgate Road, Sandwich, Kent, CT13 9NJ
Pharmacotherapeutic group: Detoxifying agents for antineoplastic treatment
ATC Code: V03AF03
Leucovorin (5-formyltetrahydrofolinate) acts partly by providing a fresh supply of tetrahydrofolate and also by competitively displacing methotrexate from dihydrofolate reductase so that its excretion is accelerated (methotrexate binds to the enzyme dihydrofolate reductase which is responsible for reducing dietary folic acid to dihydrofolate and tetrahydrofolate thus inhibiting its action.
Leucovorin is an active folic acid derivative and it can therefore relieve pathological conditions associated with folic acid deficiency e.g. megaloblastic anaemia.
The bioavailability of leucovorin following administration of both tablet and parenteral formulations is comparable. After 30 minutes approximately 90% of the total reduced folates were assayed as 5-methyltetrahydrofolate following oral administration compared with only 72% following i.m. administration. The half-life of leucovorin after reaching peak plasma levels was 35-45 minutes by both routes. Peak serum tetrahydrofolate levels were reached 2 hours after oral administration and approximately 40 minutes after i.m administration.
None stated.
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