Branch R A, Herbert C M, Read A E
Gut. 1973 Jul;14(7):569-73. doi: 10.1136/gut.14.7.569.
Antipyrine has been used as a model drug to investigate the effects of liver disease on drug metabolism in man. A prolongation in antipyrine half-life (T(1/2)) was found in patients with liver disease, patients with chronic liver disease showing a greater increase than those with acute, reversible pathology. The most marked prolongation in T(1/2) was found in association with hypoalbuminaemia and hypoprothrombinaemia, suggesting that the cause for these changes was defective protein synthesis of microsomal enzyme protein. This hypothesis was supported by demonstrating that enzyme-inducing agents, which are known to increase the amount of microsomal enzyme protein, reduced the antipyrine half-life.
安替比林一直被用作模型药物来研究肝脏疾病对人体药物代谢的影响。在患有肝脏疾病的患者中发现安替比林半衰期(T(1/2))延长,慢性肝病患者的延长幅度大于急性可逆性病变患者。T(1/2)延长最明显的情况与低白蛋白血症和低凝血酶原血症相关,这表明这些变化的原因是微粒体酶蛋白的蛋白质合成存在缺陷。通过证明已知能增加微粒体酶蛋白量的酶诱导剂可缩短安替比林半衰期,这一假设得到了支持。