血浆酯酶导致临床样本中的磷酸奥司他韦迅速降解。
Rapid degradation of oseltamivir phosphate in clinical samples by plasma esterases.
作者信息
Lindegardh Niklas, Davies Geraint R, Tran Tinh Hien, Farrar Jeremy, Singhasivanon Pratap, Day Nicholas P J, White Nicholas J
机构信息
Faculty of Tropical Medicine, Mahidol University, 420/6 Rajvithi Road, Bangkok 10400, Thailand.
出版信息
Antimicrob Agents Chemother. 2006 Sep;50(9):3197-9. doi: 10.1128/AAC.00500-06.
Abstract
The anti-influenza drug oseltamivir is an ester prodrug activated by hepatic carboxylesterases. Plasma esterases also convert up to 31.8% of the parent compound to the active metabolite after 4 h ex vivo, with wide interindividual variation. This source of error is removed by adding the esterase inhibitor dichlorvos to blood collection tubes.
摘要
抗流感药物奥司他韦是一种由肝脏羧酸酯酶激活的酯前药。血浆酯酶在离体4小时后也可将高达31.8%的母体化合物转化为活性代谢物，个体间差异很大。通过在采血管中加入酯酶抑制剂敌敌畏可消除这种误差来源。
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