Ruen S J, Hesselfeldt P, Larsen N E
Scand J Gastroenterol. 1979;14(4):489-92.
The plasma concentration of cimetidine was measured in 40 patients with duodenal ulcer after an oral dose of 200 mg cimetidine. The peak plasma concentration was on average 1.33 mg x 1(-1) (S.D. = 0.53) and the area under the plasma concentration curve (AUC) between 60 and 120 min after cimetidine was 1.13 mg x h x 1(-1) (S.D. = 0.48). The percentage inhibition (I%) of maximal acid output (MAO) to pentagastrin during this 60-min period was 49% (S.D. = 19) with a very low, but statistically significant, correlation with the AUC, r = 0.35 (p less than 0.05), thus demonstrating a very great individual variation in sensitivity to cimetidine. In 37 of the patients the time from start of treatment with cimetidine, 1.0 g/day, to disappearance of ulcer symptoms could be assessed, and it was found that neither the individual sensitivity to cimetidine, I%/AUC, nor the gastric secretory capacity, MAO, correlated significantly with the clinical effectiveness of the cimetidine treatment, although 8 patients with a low sensitivity to cimetidine and a high MAO improved more slowly (28 days) than the other 29 patients (13 days) (p less than 0.1).
对40例十二指肠溃疡患者口服200mg西咪替丁后测定其血浆西咪替丁浓度。血浆峰值浓度平均为1.33mg·L⁻¹(标准差=0.53),西咪替丁给药后60至120分钟期间血浆浓度曲线下面积(AUC)为1.13mg·h·L⁻¹(标准差=0.48)。在此60分钟期间,五肽胃泌素刺激的最大酸排量(MAO)的抑制百分比(I%)为49%(标准差=19),与AUC呈非常低但具有统计学意义的相关性,r = 0.35(p<0.05),从而表明个体对西咪替丁的敏感性差异很大。在37例患者中,可以评估从开始使用西咪替丁治疗(1.0g/天)到溃疡症状消失的时间,发现个体对西咪替丁的敏感性(I%/AUC)或胃分泌能力(MAO)与西咪替丁治疗的临床疗效均无显著相关性,尽管8例对西咪替丁敏感性低且MAO高的患者比其他29例患者(13天)改善得更慢(28天)(p<0.1)。