Bioavailability of drugs: the digoxin dilemma

DJ Greenblatt, TW Smith, J Koch-Weser - Clinical pharmacokinetics, 1976 - Springer
The absorption of oral digoxin preparations has been a topic of much concern during the last
5 yean. The completeness of digoxin absorption is proportional to the area under the serum …

P-gp inhibition potential in cell-based models: which “calculation” method is the most accurate?

PV Balimane, A Marino, S Chong - The AAPS journal, 2008 - Springer
The objective was to directly compare the four different “calculation” methods of assessing P-
gp inhibition potential using experimental data obtained from~ 60 structurally diverse …

Predicting inhibitory drug—drug interactions and evaluating drug interaction reports using inhibition constants

KA Bachmann, JD Lewis - Annals of Pharmacotherapy, 2005 - journals.sagepub.com
OBJECTIVE: To review the use of inhibitory constants (Ki) determined from in vitro
experiments in the prediction of the significance of inhibitory drug—drug interactions (DDIs) …

Role of P-Glycoprotein Inhibition for Drug Interactions: Evidence from In Vitro and Pharmacoepidemiological Studies

S Eberl, B Renner, A Neubert, M Reisig… - Clinical …, 2007 - Springer
Objectives We determined in vitro the potency of macrolides as P-glycoprotein inhibitors and
tested in hospitalised patients whether coadministration of P-glycoprotein inhibitors leads to …

Impact of cremophor-EL and polysorbate-80 on digoxin permeability across rat jejunum: delineation of thermodynamic and transporter related events using the …

K Katneni, SA Charman, CJH Porter - Journal of pharmaceutical sciences, 2007 - Elsevier
The effect of Cremophor-EL (Cr-EL) and polysorbate-80 (PS-80) on the transepithelial
permeability of digoxin (DIG) has been evaluated using the reciprocal permeability …

P‐glycoprotein‐mediated intestinal and biliary digoxin transport in humans

S Drescher, H Glaeser, T Mürdter… - Clinical …, 2003 - Wiley Online Library
Background and Aims Intestinal transport by P‐glycoprotein is a recently recognized
determinant of drug disposition. However, direct measurements of transporter‐mediated …

In vitro predictability of drug-drug interaction likelihood of P-glycoprotein-mediated efflux of dabigatran etexilate based on [I] 2/IC50 threshold

W Kishimoto, N Ishiguro, E Ludwig-Schwellinger… - Drug Metabolism and …, 2014 - ASPET
Dabigatran etexilate, an oral, reversible, competitive, and direct thrombin inhibitor, is an in
vitro and in vivo substrate of P-glycoprotein (P-gp). Dabigatran etexilate was proposed as an …

Comparison of species differences of P-glycoproteins in beagle dog, rhesus monkey, and human using Atpase activity assays

CQ Xia, G Xiao, N Liu, S Pimprale, L Fox… - Molecular …, 2006 - ACS Publications
P-glycoprotein (P-gp) is a transmembrane efflux transporter which possesses many
important functions in drug absorption, disposition, metabolism, and toxicity. The ultimate …

Ritonavir decreases the nonrenal clearance of digoxin in healthy volunteers with known MDR1 genotypes

SR Penzak, JM Shen, RM Alfaro… - Therapeutic drug …, 2004 - journals.lww.com
Our objective was to examine the influence of ritonavir on P-glycoprotein (P-gp) activity in
humans by characterizing the effect of ritonavir on the pharmacokinetics of the P-gp …

P-glycoprotein recognition of substrates and circumvention through rational drug design

TJ Raub - Molecular pharmaceutics, 2006 - ACS Publications
It is now well recognized that membrane efflux transporters, especially P-glycoprotein (P-gp;
ABCB1), play a role in determining the absorption, distribution, metabolism, excretion, and …