INACTIVATION OF DIGOXIN BY THE GUT FLORA - REVERSAL BY ANTIBIOTIC-THERAPY
INACTIVATION OF DIGOXIN BY THE GUT FLORA - REVERSAL BY ANTIBIOTIC-THERAPY
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DOI：
10.1056/nejm198110013051403
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发表时间：
1981-01-01
影响因子：
158.5
通讯作者：
SAHA, JR
中科院分区：
文献类型：
--
作者：
LINDENBAUM, J;RUND, DG;SAHA, JR
在.apprx. 10%给予地高辛的患者，发生药物实质性转化为无心脏活性的还原代谢产物（地高辛还原产物或DRP）。这种转化的部位和临床意义尚不清楚。在4名正常志愿者中，每天服用地高辛4周，摄入吸收不良片剂后尿中DRP排泄量最大，静脉给药后尿中DRP排泄量最少。已知在体内产生DRP的受试者（排泄物）的粪便培养物将地高辛转化为DRP;非排泄物的培养物则不会。三个排泄者服用地高辛片22-29天。在10-17天的基线期后给予5天的红霉素或四环素疗程，可显著减少或消除尿和粪便中的DRP排泄。给予抗生素后，血清地高辛浓度升高高达2倍。在某些人中，地高辛明显被胃肠道细菌灭活。肠道植物群的变化可显著改变数字化的状态。
In .apprx. 10% of patients given digoxin, substantial conversion of the drug to cardioinactive, reduced metabolites (digoxin reduction products or DRP) occurs. The site and clinical importance of this conversion are unknown. In 4 normal volunteers taking digoxin daily for 4 wk, urinary excretion of DRP was greatest after a poorly absorbed tablet was ingested, and least after i.v. administration. Stool cultures from subjects known to make DRP in vivo (excretors) converted digoxin to DRP; cultures from nonexcretors did not. Three excretors were given digoxin tablets for 22-29 days. A 5-day course of erythromycin or tetracycline, administered after a base-line period of 10-17 days, markedly reduced or eliminated DRP excretion in urine and stool. Serum digoxin concentrations rose as much as 2-fold after antibiotics were given. In some persons digoxin is evidently inactivated by gastrointestinal bacteria. Changes in the enteric flora may markedly alter the state of digitalization.