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柳氮磺胺吡啶对地高辛生物利用度的影响。

Effect of sulfasalazine on digoxin bioavailability.

作者信息

Juhl R P, Summers R W, Guillory J K, Blaug S M, Cheng F H, Brown D D

出版信息

Clin Pharmacol Ther. 1976 Oct;20(4):387-94. doi: 10.1002/cpt1976204387.

Abstract

Low levels of digoxin were noted in a patient receiving digoxin and sulfasalazine (SSA). Discontinuation of SSA resulted in a significant increase in serum digoxin levels. To determine whether or not SSA consistently interfered with the therapeutic effect of digoxin, both drugs were administered to 10 normal subjects in a crossover study. Each received 2 doses of digoxin (0.5 mg, elixir): one dose given alone, and a second dose after 6 days of treatment with SSA. When digoxin was given with SSA, the average area under the serum digoxin curve fell from the control value of 8.79 ng-hr-ml(-1) to 6.66 ng-hr-ml(-1) (p less than 0.05), fell and total urinary excretion decreased from 278 mcg/10 days to 228 mcg/10 days (p less than 0.025). These changes suggest interference with the bioavailability of digoxin by SSA. Studies were conducted to determine whether SSA inhibited digoxin absorption by physically absorbing the glycoside from solution. In vitro tests failed to reveal any significant adsorptive properties for SSA.

摘要

在一名接受地高辛和柳氮磺胺吡啶(SSA)治疗的患者中发现地高辛水平较低。停用SSA后,血清地高辛水平显著升高。为了确定SSA是否持续干扰地高辛的治疗效果,在一项交叉研究中,将这两种药物给予10名正常受试者。每人接受2剂地高辛(0.5毫克,酏剂):一剂单独给药,另一剂在接受6天SSA治疗后给药。当与SSA合用时,血清地高辛曲线下的平均面积从对照值8.79纳克·小时·毫升⁻¹降至6.66纳克·小时·毫升⁻¹(p<0.05),并且总尿排泄量从278微克/10天降至228微克/10天(p<0.025)。这些变化表明SSA干扰了地高辛的生物利用度。进行了研究以确定SSA是否通过从溶液中物理吸附糖苷来抑制地高辛的吸收。体外试验未发现SSA有任何显著的吸附特性。

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