Meinertz T, Gilfrich H J, Groth U, Jonen H G, Jähnchen E
Clin Pharmacol Ther. 1977 Jun;21(6):731-5. doi: 10.1002/cpt1977216731.
The effect of cholestyramine (12 gm/day divided into 3 doses) on the pharmacokinetics and pharmacodynamics of a single intravenouse dose (30 mg) of phenprocoumon was studied in 6 normal subjects. Cholestyramine treatment led to an increase in the rate of elimination of phenprocoumon in all. Total clearance increased 1.5- to 2-fold. The total anticoagulant effect per dose was considerably reduced during treatment with cholestyramine. Binding studies in vitro showed that phenprocoumon is strongly bound to cholestyramine and that at a given cholestyramine concentration the percentage of phenprocoumon bound remained constant over a large concentration range of phenprocoumon. The results suggest that phenprocoumon undergoes extensive enterohepatic recycling in man which can be effectively interrupted by cholestyramine.
在6名正常受试者中研究了消胆胺（每天12克，分3次服用）对单次静脉注射剂量（30毫克）苯丙香豆素的药代动力学和药效学的影响。消胆胺治疗导致所有受试者中苯丙香豆素的消除速率增加。总清除率增加了1.5至2倍。在消胆胺治疗期间，每剂的总抗凝作用显著降低。体外结合研究表明，苯丙香豆素与消胆胺紧密结合，并且在给定的消胆胺浓度下，在苯丙香豆素的较大浓度范围内，结合的苯丙香豆素百分比保持恒定。结果表明，苯丙香豆素在人体内经历广泛的肠肝循环，而消胆胺可有效中断这种循环。
