Central Hospital Pharmacy and Haga Teaching Hospital, Den Haag, The Netherlands.
Aliment Pharmacol Ther. 2010 Jan;31(1):150-9. doi: 10.1111/j.1365-2036.2009.04150.x.
Esomeprazole and pantoprazole are metabolized in the liver and the polymorphic CYP2C19 enzyme is involved in that process. This genetic polymorphism determines fast (70% of Caucasians), intermediate (25-30% of Caucasians) and slow (2-5% of Caucasians) metabolism of PPIs.
To compare the acid-inhibitory effects of esomeprazole 40 mg and pantoprazole 40 mg at 4, 24 and 120 h after oral administration in relation to CYP2C19 genotype and pharmacokinetics.
CYP2C19*2, *3, *4, *5 and *17 genotypes were determined in healthy Helicobacter pylori-negative Caucasian subjects. 7 wt/wt, 7 wt/*2, 2 wt/*17, 2 *2/*17 and 1 *2/*2 were included in a randomized investigator-blinded cross-over study with esomeprazole 40 mg and pantoprazole 40 mg. Intragastric 24-h pH-monitoring was performed on days 0, 1 and 5 of oral dosing.
A total of 19 subjects (mean age 24 years, 7 male) completed the study. At day 1 and 5, acid-inhibition with esomeprazole was significantly greater and faster than with pantoprazole. Differences in acid-inhibition and pharmacokinetics between wt/wt and wt/*2 genotype were significant for pantoprazole at day 1 and 5.
Esomeprazole provides acid-inhibition faster than and superior to pantoprazole after single and repeated administration. The acid-inhibitory effect and the kinetics of pantoprazole are influenced by CYP2C19 genotype.
埃索美拉唑和泮托拉唑在肝脏中代谢，多态性 CYP2C19 酶参与该过程。这种遗传多态性决定了质子泵抑制剂（PPIs）的快速（70%的白种人）、中间（25-30%的白种人）和缓慢（2-5%的白种人）代谢。
比较埃索美拉唑 40mg 和泮托拉唑 40mg 在口服后 4、24 和 120 小时的抑酸作用与 CYP2C19 基因型和药代动力学的关系。
在健康的幽门螺杆菌阴性白种人受试者中确定 CYP2C19*2、*3、*4、5 和17 基因型。7 名 wt/wt、7 名 wt/*2、2 名 wt/17、2 名2/17 和 1 名2/*2 被纳入一项随机、研究者设盲的交叉研究，分别给予埃索美拉唑 40mg 和泮托拉唑 40mg。在口服给药的第 0、1 和 5 天进行胃内 24 小时 pH 监测。
共有 19 名受试者（平均年龄 24 岁，7 名男性）完成了这项研究。在第 1 天和第 5 天，埃索美拉唑的抑酸作用明显大于泮托拉唑，且起效更快。在第 1 天和第 5 天，wt/wt 和 wt/*2 基因型之间的抑酸作用和药代动力学差异在泮托拉唑中具有统计学意义。
埃索美拉唑单次和重复给药后的抑酸作用快于并优于泮托拉唑。泮托拉唑的抑酸作用和动力学受 CYP2C19 基因型的影响。
