作者: Ulrich Klotz , Matthias Schwab , Gerhard Treiber
DOI: 10.1111/J.1600-0773.2004.PTO950102.X
关键词: Rabeprazole 、 Proton-pump inhibitor 、 Pharmacology 、 Omeprazole 、 Esomeprazole 、 Lansoprazole 、 CYP2C19 、 Pharmacodynamics 、 Chemistry 、 Pantoprazole
摘要: Proton pump inhibitors such as omeprazole (esomeprazole), lansoprazole, pantoprazole and rabeprazole are eliminated by the hepatic route polymorphic CYP2C19 is mainly involved in their metabolism. In different populations three phenotypes have been identified: extensive metabolizers, poor metabolizers individuals carrying one wild type mutant allele (het metabolizers). Systemic exposure to proton expressed AUC (area under plasma level time profiles) 5-12-times higher than metabolizers. As pharmacodynamic response (elevation of intragastric pH) related directly AUC, a much pH can be monitored over 24 hr Furthermore, clinical efficacy all depend on maintaining above certain threshold levels significantly eradication rates Helicobacter pylori observed patients het phenotype if compared Likewise, limited data suggest that inhibitors-induced healing gastro-oesophageal reflux disease apparently metabolizers/het CYP2C19. Therefore initial genotyping for this enzyme dosage likely improve inhibitors.