Iser J H, Sali A
Drugs. 1981 Feb;21(2):90-119. doi: 10.2165/00003495-198121020-00002.
Chenodeoxycholic acid (chenic acid; CDCA) is 1 of the 3 major biliary bile acids in man. When administered in pharmacological doses it causes a decrease in cholesterol saturation of bile, which in turn may lead to gradual dissolution of cholesterol gallstones. The stone dissolution rate during CDCA therapy has varied considerably from about one-third of patients overall to 80 to 90% in a highly selected group of patients. Radiolucent gallstones in a functioning gallbladder are absolute requirements. CDCA is well tolerated; diarrhoea (sometimes requiring dosage reduction) is the only frequent side effect. Although hepatotoxicity has occurred in certain animal species, and slight hypertransaminasaemia has occurred in some patients, definite liver damage has not been observed in man. CDCA is considered contraindicated in pregnancy, and in those patients with the complications from gallstones which require immediate surgery. Care should be taken in patients with liver disease. The only other proven agent for dissolving gallstones is the 7 beta-epimer of CDCA, ursodeoxycholic acid (UDCA). Preliminary results show that UDCA is as effective as CDCA, but at one-half to two-thirds the dose, without causing diarrhoea. Further studies need to be done with both CDCA and UDCA to improve criteria for selection of patients most likely to respond, and to establish optimum schedules for dosage and duration of treatment.
鹅去氧胆酸(鹅胆酸;CDCA)是人体内三种主要的胆汁酸之一。以药理剂量给药时,它会降低胆汁的胆固醇饱和度,进而可能导致胆固醇结石逐渐溶解。在CDCA治疗期间,结石溶解率差异很大,总体约三分之一的患者出现溶解,而在一组经过严格挑选的患者中,溶解率可达80%至90%。胆囊功能正常且结石为透X线结石是绝对必要条件。CDCA耐受性良好;腹泻(有时需要减少剂量)是唯一常见的副作用。虽然在某些动物物种中发生过肝毒性,一些患者出现过轻微的转氨酶升高,但在人类中尚未观察到明确的肝损伤。CDCA被认为在妊娠期间以及患有需要立即手术的胆结石并发症的患者中禁用。肝病患者应谨慎使用。另一种经证实的溶石药物是CDCA的7β-差向异构体,熊去氧胆酸(UDCA)。初步结果表明,UDCA与CDCA效果相同,但剂量仅为其二分之一至三分之二,且不会引起腹泻。需要对CDCA和UDCA进行进一步研究,以完善最可能有反应患者的选择标准,并确定最佳的给药方案和治疗持续时间。