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甲氨蝶呤在人体内的代谢转化

Metabolic conversion of methotrexate in man.

作者信息

Donehower R C

出版信息

Recent Results Cancer Res. 1980;74:37-41. doi: 10.1007/978-3-642-81488-4_5.

DOI:10.1007/978-3-642-81488-4_5
PMID:7444148
Abstract

Metabolism of methotrexate (MTX) to closely related analogues has been increasingly recognized in recent years. 7-Hydroxymethotrexate, 2,4-diamino-N10-methylpteroic acid, and methotrexate poly-gamma-glutamates have been established as products of metabolic conversion in man. The significance of the formation of these metabolites has not been firmly established. Certain of these compounds may play a role in the development of the renal failure syndrome associated with high-dose infusions, contribute to the chronic toxicity of MTX administration, and cross-react to a significant degree in radioimmunoassay methods for measurement of MTX concentrations.

摘要

近年来,甲氨蝶呤(MTX)代谢为密切相关类似物的现象越来越受到关注。7-羟基甲氨蝶呤、2,4-二氨基-N10-甲基蝶酸和甲氨蝶呤多聚γ-谷氨酸已被确认为人体代谢转化的产物。这些代谢产物形成的意义尚未完全明确。其中某些化合物可能在与高剂量输注相关的肾衰竭综合征的发生中起作用,导致甲氨蝶呤给药的慢性毒性,并在用于测量甲氨蝶呤浓度的放射免疫分析方法中产生显著的交叉反应。

相似文献

1
Metabolic conversion of methotrexate in man.甲氨蝶呤在人体内的代谢转化
Recent Results Cancer Res. 1980;74:37-41. doi: 10.1007/978-3-642-81488-4_5.
2
Presence of 2,4-diamino-N10-methylpteroic acid after high-dose methotrexate.
Clin Pharmacol Ther. 1979 Jul;26(1):63-72. doi: 10.1002/cpt197926163.
3
A simple preparation of the methotrexate metabolites 7-hydroxymethotrexate and 4-deoxy-4-amino-N10-methylpteroic acid.甲氨蝶呤代谢物7-羟基甲氨蝶呤和4-脱氧-4-氨基-N10-甲基蝶酸的一种简易制备方法。
Ther Drug Monit. 1983;5(3):363-6. doi: 10.1097/00007691-198309000-00021.
4
Pharmacokinetics of methotrexate and 7-hydroxymethotrexate following infusions of high-dose methotrexate.大剂量甲氨蝶呤输注后甲氨蝶呤和7-羟基甲氨蝶呤的药代动力学
Cancer Treat Rep. 1982 Sep;66(9):1733-41.
5
Plasma methotrexate as determined by liquid chromatography, enzyme-inhibition assay, and radioimmunoassay after high-dose infusion.大剂量输注后通过液相色谱法、酶抑制测定法和放射免疫测定法测定的血浆甲氨蝶呤。
Clin Chem. 1980 May;26(6):734-7.
6
Radioimmunoassays of 7-hydroxymethotrexate and methotrexate.
Clin Chim Acta. 1984 Aug 31;141(2-3):135-49. doi: 10.1016/0009-8981(84)90006-8.
7
Determination of methotrexate and its metabolites 7-hydroxymethotrexate and 2,4-diamino-N10-methylpteroic acid in biological fluids by liquid chromatography with fluorimetric detection.采用液相色谱-荧光检测法测定生物流体中甲氨蝶呤及其代谢物7-羟基甲氨蝶呤和2,4-二氨基-N10-甲基蝶酸。
J Chromatogr. 1986 May 28;378(1):173-81.
8
Aldehyde oxidase-catalysed oxidation of methotrexate in the liver of guinea-pig, rabbit and man.醛氧化酶催化的甲氨蝶呤在豚鼠、兔和人肝脏中的氧化作用。
J Pharm Pharmacol. 1999 Apr;51(4):411-8. doi: 10.1211/0022357991772619.
9
Methotrexate analogues. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids.甲氨蝶呤类似物。34. 用长链2-氨基链烷二酸取代甲氨蝶呤和氨基蝶呤中的谷氨酸部分。
J Med Chem. 1988 Jul;31(7):1338-44. doi: 10.1021/jm00402a014.
10
Pharmacokinetics and metabolism of the methotrexate metabolite 2, 4-diamino-N(10)-methylpteroic acid.甲氨蝶呤代谢产物2,4-二氨基-N(10)-甲基蝶酸的药代动力学与代谢
J Pharmacol Exp Ther. 2000 Sep;294(3):894-901.

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5
Theoretically required urinary flow during high-dose methotrexate infusion.
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