Kastberg H, Jansen J A, Cole G, Wesnes K
Clinical Development, Novo Nordisk A/S, Bagsvaerd, Denmark.
Drug Metabol Drug Interact. 1998;14(4):259-73. doi: 10.1515/dmdi.1998.14.4.259.
Tiagabine is a new antiepileptic drug that inhibits the uptake of gamma-aminobutyric acid into neurons and glia. This double-blind, placebo-controlled study investigated the effect of multiple doses of tiagabine on the adverse cognitive effects produced by a single dose of ethanol in 20 healthy volunteers. The effects of each drug on the pharmaco-kinetics of the other were also determined. Compared with placebo, tiagabine produced no statistically significant effects on digit vigilance speed (primary assessment variable) or accuracy, choice reaction time, immediate or delayed word recall, delayed word recognition speed or sensitivity, visual tracking, body sway, or subjective measures of alertness, calmness, and contentment. There was no evidence of a pharmacodynamic interaction between tiagabine and ethanol with respect to these variables. The pharmacokinetic parameters of tiagabine and ethanol (maximum plasma concentration [Cmax], time to Cmax and area under the plasma concentration-time curve) were unchanged during concomitant administration. Adverse events, which mainly affected the central nervous system, occurred with a similar incidence during tiagabine and placebo administration and were more common after the administration of ethanol. There appears to be no need for additional caution regarding driving or operating machinery when ethanol is administered to patients taking tiagabine.
噻加宾是一种新型抗癫痫药物，可抑制γ-氨基丁酸被神经元和神经胶质摄取。这项双盲、安慰剂对照研究调查了多剂量噻加宾对20名健康志愿者单次服用乙醇所产生的不良认知影响。还确定了每种药物对另一种药物药代动力学的影响。与安慰剂相比，噻加宾对数字警觉速度（主要评估变量）或准确性、选择反应时间、即时或延迟单词回忆、延迟单词识别速度或敏感性、视觉追踪、身体摆动或警觉性、平静度和满足感的主观测量均无统计学显著影响。就这些变量而言，没有证据表明噻加宾与乙醇之间存在药效学相互作用。在同时给药期间，噻加宾和乙醇的药代动力学参数（最大血浆浓度[Cmax]、达到Cmax的时间和血浆浓度-时间曲线下面积）未发生变化。不良事件主要影响中枢神经系统，在服用噻加宾和安慰剂期间发生率相似，且在服用乙醇后更为常见。当给服用噻加宾的患者使用乙醇时，似乎无需对驾驶或操作机器格外谨慎。
