METABOLISM OF METHOTREXATE IN MAN AFTER HIGH AND CONVENTIONAL DOSES

  • 1 January 1980
    • journal article
    • research article
    • Vol. 28  (3) , 551-561
Abstract
Methotrexate, an antineoplastic drug, was extensively metabolized to 7-hydroxymethotrexate in patients receiving conventional doses (< 10 mg/kg) and high doses (> 10 mg/kg). At 12 h after administration, plasma levels of the metabolite in several patients treated with low doses exceeded those of methotrexate. No 7-hydroxymethotrexate was found in CSF after CNS administration of methotrexate, but small amounts of the metabolite were found in the CSF after i.v. high dose infusion. Methotrexate is significantly metabolized in man at all doses used clinically.