两性霉素B与氟胞嘧啶的药代动力学
Pharmacokinetics of amphotericin B and flucytosine.
作者信息
Polak A
出版信息
Postgrad Med J. 1979 Sep;55(647):667-70. doi: 10.1136/pgmj.55.647.667.
Abstract
The absorption of flucytosine from the digestive tract is very good but minimal with amphotericin B. For this reason, amphotericin B has to be injected intravenously. Fungistatic levels are achieved rapidly with flucytosine and slowly with amphotericin B, since the dose has to be increased slowly. Distribution of flucytosine in other body fluids is high, whereas with amphotericin B it is poor. Flucytosine is excreted mainly via the kidney without metabolism, whereas amphotericin B is eliminated mainly by metabolism. Therefore, amphotericin B dosage does not have to be adapted to kidney function, which is the case for flucytosine. The half-life of flucytosine is short (hours), that of amphotericin B is long (days); flucytosine is haemodialysable, whereas amphotericin B, probably owing to the high protein binding, is not.
摘要
氟胞嘧啶从消化道的吸收非常好，但两性霉素B的吸收极少。因此，两性霉素B必须静脉注射。氟胞嘧啶能迅速达到抑菌水平，而两性霉素B则较慢，因为剂量必须缓慢增加。氟胞嘧啶在其他体液中的分布较高，而两性霉素B的分布较差。氟胞嘧啶主要通过肾脏排泄而不经过代谢，而两性霉素B主要通过代谢消除。因此，两性霉素B的剂量不必根据肾功能进行调整，而氟胞嘧啶则需要。氟胞嘧啶的半衰期短（数小时），两性霉素B的半衰期长（数天）；氟胞嘧啶可通过血液透析清除，而两性霉素B可能由于高蛋白结合率而不能。
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