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药物代谢活化的一般概念药物和外源性化合物进入体内后,一般经两相代谢转化。第一相包括氧化、还原和水解;第二相主要为结合反应,包括葡萄糖醛酸甙化、硫酸酯化、酰化、甲基化及与氨基酸结合等。大多数药物经代谢后,活性降低,极性变大,水溶性增强,从而迅速排出体外,通常称之为生物解毒。部分药物则转化为更具有治疗作用的代谢物;但也有相当一部分药物经代谢后能形成高度反应性的中间体,即所谓代谢活化。不少药
The general concept of drug metabolism activation of drugs and exogenous compounds into the body, the general two-phase metabolic transformation. The first phase includes oxidation, reduction and hydrolysis; the second phase is mainly the binding reaction, including glucuronidation, sulfation, acylation, methylation and amino acid binding. Most drugs after metabolism, activity decreased, the polarity becomes larger, water-soluble enhancements, which quickly excreted, commonly referred to as biological detoxification. Some drugs are converted to more therapeutic metabolites; but there are a considerable number of drugs metabolized to form highly reactive intermediates, the so-called metabolic activation. Many drugs