Sabouraud A, Rochdi M, Urtizberea M, Christen M O, Achtert G, Scherrmann J M
INSERM U26, Hôpital Fernand Widal, Paris, France.
Z Gastroenterol. 1992 Mar;30 Suppl 1:35-9.
Thanks to the development of a sensitive and specific radioimmunoassay for colchicine, the pharmacokinetics of colchicine is now well-established after single oral doses. Absorption is characterized by a zero-order rate constant while disposition appears biexponential with a rapid distribution phase (t1/2 = 1.8 h) and a long elimination phase (t1/2 = 20 h). All studies confirm the large total body clearance (35 l/h) predominantly by the extrarenal route and the large distribution volume (700 l). Further studies need to be performed to investigate colchicine absorption and to describe the metabolic pathway of the drug. To date, relationships between colchicine plasma levels and pharmacological effects have not been defined. Monitoring of plasma levels in patients with familial Mediterranean fever should improve treatment with colchicine. However, the therapeutic range has not been precisely determined. The use of colchicine in the treatment of liver cirrhosis and primary biliary cirrhosis is a recent development; so, assuming that a large part of total body clearance depends on hepatic function, the influence of hepatic diseases on colchicine disposition needs to be investigated in order to define the most appropriate therapeutic dosing.
由于针对秋水仙碱开发出了一种灵敏且特异的放射免疫测定法，秋水仙碱单次口服给药后的药代动力学现已明确。吸收的特征是零级速率常数，而处置呈现双指数特征，具有快速分布相（t1/2 = 1.8小时）和长消除相（t1/2 = 20小时）。所有研究均证实主要通过肾外途径的全身清除率高（35升/小时）以及分布容积大（700升）。需要进行进一步研究以调查秋水仙碱的吸收情况并描述该药物的代谢途径。迄今为止，秋水仙碱血浆水平与药理作用之间的关系尚未明确。对家族性地中海热患者的血浆水平进行监测应能改善秋水仙碱的治疗效果。然而，治疗范围尚未精确确定。秋水仙碱用于治疗肝硬化和原发性胆汁性肝硬化是一项新进展；因此，假设全身清除率的很大一部分取决于肝功能，则需要研究肝脏疾病对秋水仙碱处置的影响，以便确定最合适的治疗剂量。
