Jones D B, Ching M S, Morgan D J, Anderson J D, Smallwood R A
J Pharm Pharmacol. 1985 Mar;37(3):196-8. doi: 10.1111/j.2042-7158.1985.tb05039.x.
The effect of low (50 micrograms) and high (1 mg) doses of the histamine H2-receptor antagonists cimetidine and ranitidine on the first pass extraction of propranolol was studied in the rat isolated perfused liver. Both low and high dose cimetidine increased the area under the perfusate propranolol concentration time curve (AUC) 4 to 5-fold. Although low dose ranitidine did not alter propranolol AUC, high dose ranitidine increased it to the same extent as cimetidine. These results indicate that ranitidine has a clear propensity for microsomal inhibition, but one which is unlikely to be manifest at therapeutic dosage.
在大鼠离体灌注肝脏中研究了低剂量(50微克)和高剂量(1毫克)组胺H2受体拮抗剂西咪替丁和雷尼替丁对普萘洛尔首过提取率的影响。低剂量和高剂量的西咪替丁均使灌注液中普萘洛尔浓度-时间曲线下面积(AUC)增加了4至5倍。虽然低剂量雷尼替丁未改变普萘洛尔的AUC,但高剂量雷尼替丁使其增加到与西咪替丁相同的程度。这些结果表明,雷尼替丁有明显的微粒体抑制倾向,但在治疗剂量下不太可能表现出来。