Tomson T, Tybring G, Bertilsson L, Ekbom K, Rane A
Arch Neurol. 1980 Nov;37(11):699-703. doi: 10.1001/archneur.1980.00500600047009.
Seven patients with trigeminal neuralgia were treated with carbamazepine at three dose levels, each period lasting for six days. A single-blind technique was used, the patients being unaware of the dose changes. During the last three days of each dose treatment, the pain score was determined by the patients and the plasma concentrations of carbamazepine and its epoxide metabolite were measured. There was a correlation between the dose and plasma level of carbamazepine (r = .56; P < .01). At the carbamazepine doses studied (200 to 1,400 mg/day), no indication of saturation kinetics was seen. As the ratio between the plasma levels of the epoxide and carbamazepine was relatively low and constant, it was not possible to evaluate the potency of the epoxide. In six of the patients studied a plasma level-effect relationship was found. The best effect was seen at carbamazepine levels between 24 and 43 mu mole/L (5.7 and 10.1 microgram/mL). In one patient who was studied twice, the plasma level-response curve was different on the two occasions. Side effects were recorded in two patients, both with carbamazepine plasma levels above 33 mu mole/L (7.9 microgram/mL).
七名三叉神经痛患者接受了三种剂量水平的卡马西平治疗,每个阶段持续六天。采用单盲技术,患者不知道剂量变化。在每个剂量治疗的最后三天,由患者确定疼痛评分,并测量卡马西平及其环氧化物代谢物的血浆浓度。卡马西平的剂量与血浆水平之间存在相关性(r = 0.56;P < 0.01)。在所研究的卡马西平剂量(200至1400毫克/天)下,未观察到饱和动力学迹象。由于环氧化物与卡马西平的血浆水平之比相对较低且恒定,因此无法评估环氧化物的效力。在六名研究患者中发现了血浆水平-效应关系。在卡马西平水平为24至43微摩尔/升(5.7至10.1微克/毫升)时效果最佳。在一名接受两次研究的患者中,两次的血浆水平-反应曲线不同。两名患者出现了副作用,两人的卡马西平血浆水平均高于33微摩尔/升(7.9微克/毫升)。