This review summarizes the results of pharmacokinetic and pharmacodynamic drug interaction studies in man with pantoprazole, a new, selective proton pump inhibitor. Various mechanisms have to be considered as causes for potential drug-drug interactions. Proton pump inhibitors (PPIs) in general may alter the absorption of drugs by increasing the intragastric pH. Due to the presence of an imidazole ring, the PPIs of the class of substituted benzimidazole sulfoxides may interfere with the metabolism of other drugs by altering the activity of drug metabolizing enzymes of the cytochrome P450 system, via either induction or inhibition. With the increasing use of PPIs, their interaction potential gains therapeutic importance as was the case with the first and second generation of H2-blockers (cimetidine and ranitidine, respectively). The enhanced selectivity of pantoprazole to the gastric H+/K(+)-ATPase characterizes the new PPI generation. In contrast to omeprazole, pantoprazole has a low potential to interact with the cytochrome P450 system in man. In the drug interaction studies conducted so far, substrates for all relevant cytochrome P450 families involved in the metabolism of drugs in man were investigated. Pantoprazole did not affect the pharmacokinetics or pharmacodynamics of antipyrine, caffeine, carbamazepine, diazepam, diclofenac, digoxin, ethanol, glibenclamide, a hormonal contraceptive (combination of levonorgestrel and ethinylestradiol), metoprolol, nifedipine, phenprocoumon, phenytoin, theophylline and warfarin in man. Pantoprazole also neither induced the metabolism of antipyrine or caffeine, nor increased urinary excretion of the induction markers D-glucaric acid and 6 beta-hydroxycortisol. Vice versa, the investigated drugs had no relevant influence on the pharmacokinetics of pantoprazole.

译文

这篇综述总结了一种新型选择性质子泵抑制剂泮托拉唑在人体内的药代动力学和药效学药物相互作用研究的结果。必须考虑各种机制作为潜在药物-药物相互作用的原因。质子泵抑制剂 (ppi) 通常可以通过增加胃内ph值来改变药物的吸收。由于存在咪唑环,取代的苯并咪唑亚砜类的ppi可能通过诱导或抑制来改变细胞色素P450系统的药物代谢酶的活性,从而干扰其他药物的代谢。随着ppi的使用增加,它们的相互作用潜力与第一代和第二代H2-blockers (分别为西咪替丁和雷尼替丁) 一样具有治疗重要性。泮托拉唑对胃H/K ()-ATPase的选择性增强是新的PPI世代的特征。与奥美拉唑相反,泮托拉唑与人体细胞色素P450系统相互作用的潜力较低。在迄今为止进行的药物相互作用研究中,研究了参与人体药物代谢的所有相关细胞色素P450家族的底物。泮托拉唑不影响安替比林,咖啡因,卡马西平,地西泮,双氯芬酸,地高辛,乙醇,格列本脲,激素避孕药 (左炔诺孕酮和乙炔雌二醇的组合),美托洛尔,硝苯地平,苯丙酚,苯妥英,茶碱和华法林人的药代动力学或药效学。泮托拉唑既不诱导安替比林或咖啡因的代谢,也不增加诱导标志物D-葡萄糖酸和6β-羟基皮质醇的尿排泄。反之亦然,所研究的药物对泮托拉唑的药代动力学没有相关影响。

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