Tomson T, Bertilsson L
Arch Neurol. 1984 Jun;41(6):598-601. doi: 10.1001/archneur.1984.04210080006004.
The clinical effects of carbamazepine-10,11-epoxide were assessed in six patients with trigeminal neuralgia. The patients were first given an optimal therapeutic dose of carbamazepine. Part of or the entire carbamazepine dose was then exchanged for the metabolite carbamazepine-10,11-epoxide for three to six days. The patients were unaware of changes in the therapeutic regimen (single-blind). Carbamazepine dosages ranged from 400 to 1,400 mg/day and carbamazepine-10,11-epoxide dosages ranged from 300 to 1,000 mg/day. The clinical effects were assessed by the patients' recordings of pain attacks. When carbamazepine-10,11-epoxide and carbamazepine were given in similar doses, the pain control was comparable. On a plasma concentration basis, carbamazepine-10,11-epoxide had a considerably higher pain-relieving potency than carbamazepine. During carbamazepine treatment, the epoxide metabolite contributes to the antineuralgic effect to an extent that might be comparable to that of the parent drug. No side effects were seen during carbamazepine-10,11-epoxide therapy.
对6例三叉神经痛患者评估了卡马西平 - 10,11 - 环氧化物的临床效果。患者首先接受卡马西平的最佳治疗剂量。然后将部分或全部卡马西平剂量换成其代谢产物卡马西平 - 10,11 - 环氧化物，持续三至六天。患者未意识到治疗方案的变化（单盲）。卡马西平剂量范围为400至1400毫克/天，卡马西平 - 10,11 - 环氧化物剂量范围为300至1000毫克/天。通过患者记录的疼痛发作情况评估临床效果。当卡马西平 - 10,11 - 环氧化物和卡马西平以相似剂量给药时，疼痛控制效果相当。基于血浆浓度，卡马西平 - 10,11 - 环氧化物的止痛效力比卡马西平高得多。在卡马西平治疗期间，环氧化物代谢产物对止痛效果的贡献程度可能与母体药物相当。在卡马西平 - 10,11 - 环氧化物治疗期间未观察到副作用。
