Pullar T, Edwards D, Haigh J R, Peaker S, Feely M P
Br J Clin Pharmacol. 1987 Mar;23(3):317-21. doi: 10.1111/j.1365-2125.1987.tb03051.x.
The effect of cimetidine on the single dose pharmacokinetics of orally administered clobazam and N-desmethylclobazam (NDMC) was studied in volunteers. Cimetidine inhibited the elimination of both clobazam and NDMC and inhibited the rate of formation of NDMC from clobazam. The increase in the AUC for NDMC generated from clobazam was relatively greater than that for clobazam itself. This suggests that NDMC elimination is inhibited to a relatively greater extent than clobazam elimination. The increase in AUC for NDMC generated from clobazam was also relatively greater than that for NDMC administered orally. This would suggest that cimetidine either increases the bioavailability of clobazam or reduces that of NDMC. The increases in the AUC for NDMC and for clobazam in some individuals was of a magnitude which is likely to be clinically significant.
在志愿者中研究了西咪替丁对口服氯巴占和N -去甲基氯巴占（NDMC）单剂量药代动力学的影响。西咪替丁抑制氯巴占和NDMC的消除，并抑制氯巴占生成NDMC的速率。由氯巴占生成的NDMC的AUC增加相对大于氯巴占本身的AUC增加。这表明NDMC的消除比氯巴占的消除受到相对更大程度的抑制。由氯巴占生成的NDMC的AUC增加也相对大于口服NDMC的AUC增加。这表明西咪替丁要么增加氯巴占的生物利用度，要么降低NDMC的生物利用度。在一些个体中，NDMC和氯巴占的AUC增加幅度可能具有临床意义。
