肝素给药对苯二氮䓬类药物血浆结合的影响。
Effect of heparin administration on plasma binding of benzodiazepines.
作者信息
Desmond P V, Roberts R K, Wood A J, Dunn G D, Wilkinson G R, Schenker S
出版信息
Br J Clin Pharmacol. 1980 Feb;9(2):171-5. doi: 10.1111/j.1365-2125.1980.tb05829.x.
Abstract
1 The effect of intravenous administration of 100 units of heparin on plasma of diazepam, chlordiazepoxide, oxazepam and lorazepam was examined in fourteen normal subjects and five patients with cirrhosis. 2 In normal non-fasted subjects heparin caused a rapid 150--250% rise in the free fraction of diazepam, chlordiazepoxide and oxazepam but no change of lorazepam. The changes in free fraction were slightly smaller, but still significant, when the subjects were fasted. 3 These change in free fraction occurred within 90 s of administration of heparin and binding had returned to baseline by 30 to 45 min. 4 In the cirrhotic subjects the response to heparin was variable. 5 The use of heparin during drug disposition studies may affect the estimation of pharmacokinetic parameters and possibly pharmacological effects which are dependent on the circulating unbound drug level.
摘要
- 在14名正常受试者和5名肝硬化患者中，研究了静脉注射100单位肝素对血浆中地西泮、氯氮䓬、奥沙西泮和劳拉西泮的影响。2. 在正常非空腹受试者中，肝素使地西泮、氯氮䓬和奥沙西泮的游离分数迅速升高150%-250%，但劳拉西泮无变化。当受试者禁食时，游离分数的变化略小，但仍显著。3. 这些游离分数的变化在注射肝素后90秒内出现，结合在30至45分钟时恢复到基线水平。4. 在肝硬化受试者中，对肝素的反应各不相同。5. 在药物处置研究中使用肝素可能会影响药代动力学参数的估计，以及可能依赖于循环中未结合药物水平的药理作用。
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本文引用的文献
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