Neuenkirchen H, Wilkens J H, Oellerich M, Sybrecht G W
Eur J Respir Dis. 1985 Mar;66(3):196-204.
In a double-blind, multiple-dose, cross-over study the therapeutic effects of an S-R theophylline preparation given once each night (mean 11.2 mg/kg/day) were compared to standard treatment with an S-R aminophylline preparation every 12 h (mean 10.3 mg theophylline/kg/day) in 9 patients with nocturnal asthma. On Day 5 of each treatment period, serum theophylline concentrations and PEF were measured every 2 h over a 24 h period. With the twice-daily regimen peak theophylline concentrations were lower at night than during the day (mean 9.4 +/- 0.9 vs 11.3 +/- 1.0 mg/1). With the single administration, serum theophylline concentrations were considerably higher at night (mean C max 16.3 +/- 1.4 mg/1). In spite of the high theophylline peak to trough difference (mean 12.0 +/- 2.1 mg/1) during the once daily regimen, the circadian variations of PEF were significantly reduced. Thus, greater airways' stability can be obtained by appropriate timing of theophylline administration.
在一项双盲、多剂量、交叉研究中,对9例夜间哮喘患者比较了每晚服用一次(平均11.2毫克/千克/天)的S-R型茶碱制剂与每12小时服用一次标准治疗的S-R型氨茶碱制剂(平均10.3毫克茶碱/千克/天)的治疗效果。在每个治疗期的第5天,在24小时内每2小时测量一次血清茶碱浓度和呼气峰流速(PEF)。采用每日两次给药方案时,夜间茶碱浓度峰值低于白天(平均9.4±0.9对11.3±1.0毫克/升)。采用单次给药时,夜间血清茶碱浓度显著更高(平均Cmax 16.3±1.4毫克/升)。尽管每日一次给药方案期间茶碱峰谷差异较大(平均12.0±2.1毫克/升),但PEF的昼夜变化显著减小。因此,通过适当安排茶碱给药时间可获得更大的气道稳定性。