McKauge L, Tyrer J H, Eadie M J
Ther Drug Monit. 1981;3(1):63-70.
Simultaneous steady-state plasma concentrations of carbamazepine and carbamazepine-10, 11-epoxide were measured by high performance liquid chromatography in 295 patients. Plasma carbamazepine epoxide correlated more closely with carbamazepine dose than did plasma levels of the drug itself. Plasma carbamazepine epoxide levels tended to the higher, relative to drug dose, in children than in adults, whereas age did not seem to influence the relationship between plasma carbamazepine level and drug dose. Simultaneous phenytoin intake lowered the plasma carbamazepine levels relative to drug dose but left plasma carbamazepine epoxide levels largely unaltered. However, simultaneous valproate intake was associated with raised plasma carbamazepine epoxide levels relative to carbamazepine dose, whereas plasma carbamazepine epoxide levels were unaltered. The amount of conversion of carbamazepine to its epoxide thus appears to vary in different circumstances in human.
采用高效液相色谱法测定了295例患者同时期卡马西平和卡马西平-10,11-环氧化物的稳态血浆浓度。与药物本身的血浆水平相比，血浆卡马西平环氧化物与卡马西平剂量的相关性更密切。相对于药物剂量，儿童的血浆卡马西平环氧化物水平往往高于成人，而年龄似乎并未影响血浆卡马西平水平与药物剂量之间的关系。同时服用苯妥英会使相对于药物剂量的血浆卡马西平水平降低，但血浆卡马西平环氧化物水平基本未变。然而，同时服用丙戊酸盐会使相对于卡马西平剂量的血浆卡马西平环氧化物水平升高，而血浆卡马西平环氧化物水平未变。因此，卡马西平向其环氧化物的转化量在人类的不同情况下似乎有所不同。
