Ghose K, Fry D E, Christfides J A
Eur J Clin Pharmacol. 1983;24(3):375-81. doi: 10.1007/BF00610058.
The effect of dosage frequency of carbamazepine (CBZ) (brand name Tegretol) on pseudo-steady state drug serum levels were studied in 14 male (16-18 years) epileptics. They had already been receiving CBZ (mean dose 13.7 mg/kg) for an average period of 2.3 years in combination with other antiepileptic drugs. During this investigation, total daily CBZ dose was kept unaltered, but they received medication in thrice, twice and once daily dosage regimes. Each treatment period lasted for 4 weeks. The profiles of 24 h serum drug levels as assessed at the end of each treatment period, were observed to be within the therapeutic range during these 3 regimes. However, as expected, there were higher fluctuations of serum CBZ concentrations during once daily medication than during divided dosage regimes. Other concomitant antiepileptic drugs were continued in 2-3 divided daily doses during these 3 treatment periods, and the serum drug levels were measured at 8 h prior to the morning dosing. The concentrations of other drugs remained unchanged apart from a slight decrease in the serum sodium valproate levels during once daily medication. No clinical or electroencephalographic adverse effects were observed and there was no significant change in the fit frequency. In view of this observation, CBZ (Tegretol tablet) is probably effective as a single daily dose, but further long-term controlled clinical trial is necessary.
在14名年龄在16至18岁的男性癫痫患者中,研究了卡马西平(CBZ,商品名:得理多)的给药频率对伪稳态药物血清水平的影响。他们已经联合使用其他抗癫痫药物接受CBZ治疗(平均剂量13.7mg/kg),平均治疗时间为2.3年。在本次研究期间,每日CBZ的总剂量保持不变,但他们分别接受每日三次、两次和一次的给药方案。每个治疗期持续4周。在这三种给药方案下,每个治疗期结束时评估的24小时血清药物水平均在治疗范围内。然而,正如预期的那样,与分次给药方案相比,每日一次给药时血清CBZ浓度的波动更大。在这三个治疗期内,其他联合使用的抗癫痫药物继续每日分2至3次给药,并在早晨给药前8小时测量血清药物水平。除了每日一次给药时血清丙戊酸钠水平略有下降外,其他药物的浓度保持不变。未观察到临床或脑电图方面的不良反应,癫痫发作频率也无显著变化。鉴于这一观察结果,卡马西平(得理多片)每日单次给药可能有效,但仍需进一步进行长期对照临床试验。