Nader Ahmed M, Foster David R
Pharmaceutical Sciences Section, College of Pharmacy, Qatar University, Doha, Qatar.
J Clin Pharmacol. 2014 Jan;54(1):3-13. doi: 10.1002/jcph.200. Epub 2013 Oct 26.
The study of transporter-mediated drug-drug interactions (DDI) requires use of appropriate probes to reflect transporter function. Digoxin is often used as a probe in DDI studies involving P-glycoprotein (P-gp) and is recommended by FDA for this purpose, despite several lingering questions regarding suitability of digoxin as P-gp probe. This review aims to critically evaluate use of digoxin as a probe for P-gp-mediated clinical DDI studies, with focus on sensitivity and specificity of digoxin for P-gp. Although previous reviews have evaluated digoxin transport by P-gp, the purpose of the current review is to critically evaluate such literature in light of newly evolving literature suggesting digoxin transport by non-P-gp transporters.
对转运体介导的药物相互作用(DDI)的研究需要使用合适的探针来反映转运体功能。地高辛常被用作涉及P-糖蛋白(P-gp)的DDI研究中的探针,并且美国食品药品监督管理局(FDA)为此推荐使用地高辛,尽管关于地高辛作为P-gp探针的适用性仍存在一些悬而未决的问题。本综述旨在严格评估地高辛作为P-gp介导的临床DDI研究探针的使用情况,重点关注地高辛对P-gp的敏感性和特异性。尽管先前的综述已经评估了P-gp对地高辛的转运,但本综述的目的是根据新出现的表明非P-gp转运体也能转运地高辛的文献,严格评估此类文献。