METHOTREXATE METABOLISM ANALYSIS IN BLOOD AND LIVER OF RHEUMATOID-ARTHRITIS PATIENTS - ASSOCIATION WITH HEPATIC FOLATE-DEFICIENCY AND FORMATION OF POLYGLUTAMATES

METHOTREXATE METABOLISM ANALYSIS IN BLOOD AND LIVER OF RHEUMATOID-ARTHRITIS PATIENTS - ASSOCIATION WITH HEPATIC FOLATE-DEFICIENCY AND FORMATION OF POLYGLUTAMATES
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DOI:
10.1002/art.1780290703
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发表时间:
1986-07-01
影响因子:
--
通讯作者:
KAMEN, B
KAMEN, B
中科院分区:
其他
文献类型:
--
作者:
KREMER, JM;GALIVAN, J;KAMEN, B

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对24例每周服用长期口服MTX治疗类风湿关节炎的患者进行了血清和红细胞甲氨蝶呤(MTX)水平以及肝脏MTX和叶酸水平的分析。血清MTX水平迅速达到峰值,24小时后无明显变化。红细胞MTX水平与末次注射MTX的间隔时间无关。在肝活检获得的肝组织中,与基线标本相比,MTX主要以多谷氨酸形式存在,肝脏叶酸储备耗尽。口服叶酸重复肝脏叶酸的短期治疗。MTX的肝毒性可能与肝脏叶酸水平降低和MTX多谷氨酸的形成有关。
Serum and red blood cell methotrexate (MTX) levels, as well as hepatic levels of MTX and folate, were analyzed in 24 patients who had received long-term oral MTX weekly for the treatment of rheumatoid arthritis. The serum MTX level peaked rapidly and was insignificant after 24 hours. The red blood cell MTX level was not related to the interval from the last MTX dose. In hepatic tissue obtained by liver biopsy, MTX was found in a predominantly polyglutamated form with depleted hepatic folate stores when compared with baseline specimens. A brief period of therapy with oral folinic acid repleted hepatic folate. It is possible that MTX hepatotoxicity is related to reduced hepatic folate levels and formation of MTX polyglutamates.