Department of Pharmacology, Pomeranian Medical University, Powstancow Wlkp 72, 70-111, Szczecin, Poland.
Department of Pharmacology, Medicine University Greifswald, Friedrich-Ludwig-Jahn-Straße 17, 17489, Greifswald, Germany.
Pharmacol Rep. 2020 Oct;72(5):1173-1194. doi: 10.1007/s43440-020-00139-6. Epub 2020 Jul 27.
Emerging information suggests that gastrointestinal and systemic pathology states may affect expression and function of membrane transporters in the gastrointestinal tract. Altered status of the transporters could affect drug as well as endogenous compounds handling with subsequent clinical consequences. It seems that in some pathologies, e.g., liver or kidney failure, changes in the intestinal transporter function provide compensatory functions, eliminating substrates excreted by dysfunctional organs. A literature search was conducted on Ovid and Pubmed databases to select relevant in vitro, animal and human studies that have reported expression, protein abundance and function of intestinal drug transporters. The accumulated data suggest that gastrointestinal pathology (inflammatory bowel disease, celiac disease, cholestasis) as well as systemic pathologies (kidney failure, liver failure, hyperthyroidism, hyperparathyroidism, obesity, diabetes mellitus, systemic inflammation and Alzheimer disease) may affect drug transporter expression and function in the gastrointestinal tract. The altered status of drug transporters may provide compensatory activity in handling endogenous compounds, affect local drug actions in the gastrointestinal tract as well as impact drug bioavailability.
新出现的信息表明，胃肠道和全身病理状态可能会影响胃肠道中膜转运体的表达和功能。转运体的异常状态可能会影响药物以及内源性化合物的处理，从而产生后续的临床后果。在某些病理情况下，例如肝或肾衰竭，肠道转运体功能的变化提供了代偿功能，消除了功能失调器官排泄的底物。在 Ovid 和 Pubmed 数据库上进行了文献检索，以选择报告肠道药物转运体表达、蛋白丰度和功能的相关体外、动物和人体研究。累积的数据表明，胃肠道病理（炎症性肠病、乳糜泻、胆汁淤积）以及全身病理（肾衰竭、肝衰竭、甲状腺功能亢进、甲状旁腺功能亢进、肥胖、糖尿病、全身炎症和阿尔茨海默病）可能会影响胃肠道中药物转运体的表达和功能。药物转运体的异常状态可能会提供对内源性化合物的代偿活性，影响胃肠道局部药物作用，并影响药物生物利用度。
