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Klin Wochenschr. 1982 Jun 1;60(11):541-9. doi: 10.1007/BF01724209.
Bile acid profiles from plasma and urine of six patients suffering from intrahepatic cholestasis were studied before and during treatment with phenobarbital. All patients responded to this treatment by decreasing their plasma bile acid levels. Using gas chromatographic and mass spectrometric methods for separation and identification of the bile acids, especially the occurrence of major atypical bile acids was quantitatively evaluated. The plasma bile acid lowering effect of phenobarbital in intrahepatic cholestasis can be partly explained by an increased formation of tetrahydroxylated bile acids, which are rapidly excreted by renal pathways. These tetrahydroxylated bile acids, present as nonsulfated compounds, have high renal excretory flow rates exceeding those of bile acid sulfates. Their enterohepatic circulation, however, seems to be low, since only small amounts of tetrahydroxylated bile acids can be found in bile. It is mainly the 1- and 6-hydroxylation that is stimulated by phenobarbital. The exact site of formation of tetrahydroxylated bile acids, however, is still unknown. These findings may provide a rationale for the institution of a phenobarbital treatment in cases of intrahepatic cholestasis.
对6例肝内胆汁淤积患者在使用苯巴比妥治疗前及治疗期间的血浆和尿液胆汁酸谱进行了研究。所有患者经此治疗后血浆胆汁酸水平均下降。采用气相色谱和质谱方法分离和鉴定胆汁酸，尤其对主要非典型胆汁酸的出现情况进行了定量评估。苯巴比妥对肝内胆汁淤积患者血浆胆汁酸的降低作用，部分可通过四羟基化胆汁酸生成增加来解释，这些胆汁酸可通过肾脏途径快速排泄。这些以非硫酸化化合物形式存在的四羟基化胆汁酸，其肾脏排泄流速高于胆汁酸硫酸盐。然而，它们的肠肝循环似乎较低，因为在胆汁中只能发现少量的四羟基化胆汁酸。主要是1-羟基化和6-羟基化受到苯巴比妥的刺激。然而，四羟基化胆汁酸的确切生成部位仍不清楚。这些发现可为肝内胆汁淤积病例采用苯巴比妥治疗提供理论依据。
