Wilner K D, Hansen R A, Folger C J, Geoffroy P
Department of Clinical Research, Pfizer Central Research, Groton, CT 06340, USA.
Br J Clin Pharmacol. 2000;49 Suppl 1(Suppl 1):57S-60S. doi: 10.1046/j.1365-2125.2000.00154.x.
To evaluate the effects of cimetidine and Maalox(R) (aluminium hydroxide 1.35 g and magnesium hydroxide 1.2 g) on the pharmacokinetics of ziprasidone.
Eleven healthy young subjects aged 18-45 years were given single oral doses of ziprasidone 40 mg on three occasions at least 7 days apart. On one occasion ziprasidone was administered alone, on another occasion ziprasidone was co-administered with oral cimetidine 800 mg and on a third occasion ziprasidone was co-administered with oral Maalox(R).
The administration of cimetidine increased the ziprasidone AUC(0,infinity) by 6% but there were no statistically significant differences in Cmax, tmax or lambda(z) between the ziprasidone+cimetidine group and the ziprasidone group. The administration of Maalox did not produce any statistically significant differences in AUC(0,infinity), Cmax, tmax or lambda(z) between the ziprasidone+Maalox group and the ziprasidone group.
The pharmacokinetics of ziprasidone are not affected by concurrent administration of cimetidine or Maalox. This suggests that other nonspecific inhibitors of cytochrome P450 and antacids are unlikely to alter the pharmacokinetics of ziprasidone.
评估西咪替丁和氢氧化铝镁(氢氧化铝1.35 g和氢氧化镁1.2 g)对齐拉西酮药代动力学的影响。
11名年龄在18至45岁之间的健康年轻受试者,在至少相隔7天的三个时间段分别单次口服40 mg齐拉西酮。一次单独服用齐拉西酮,另一次齐拉西酮与800 mg口服西咪替丁联合服用,第三次齐拉西酮与口服氢氧化铝镁联合服用。
西咪替丁的给药使齐拉西酮的AUC(0,∞)增加了6%,但齐拉西酮+西咪替丁组与齐拉西酮组之间的Cmax、tmax或λ(z)没有统计学上的显著差异。氢氧化铝镁的给药在齐拉西酮+氢氧化铝镁组与齐拉西酮组之间的AUC(0,∞)、Cmax、tmax或λ(z)方面未产生任何统计学上的显著差异。
齐拉西酮的药代动力学不受同时服用西咪替丁或氢氧化铝镁的影响。这表明细胞色素P450的其他非特异性抑制剂和抗酸剂不太可能改变齐拉西酮的药代动力学。