The P-glycoprotein transport system and cardiovascular drugs

JD Wessler, LT Grip, J Mendell, RP Giugliano - Journal of the American …, 2013 - jacc.org
Permeability glycoprotein (P-gp) mediates the export of drugs from cells located in the small
intestine, blood-brain barrier, hepatocytes, and kidney proximal tubule, serving a protective …

Pharmacokinetic interactions with rifampicin: clinical relevance

M Niemi, JT Backman, MF Fromm, PJ Neuvonen… - Clinical …, 2003 - Springer
The antituberculosis drug rifampicin (rifampin) induces a number of drug-metabolising
enzymes, having the greatest effects on the expression of cytochrome P450 (CYP) 3A4 in …

Polymorphisms in Human MDR1 (P‐glycoprotein): Recent Advances and Clinical Relevance

C Marzolini, E Paus, T Buclin… - Clinical Pharmacology & …, 2004 - Wiley Online Library
Drug transporters are increasingly recognized to be important to drug disposition and
response. P‐glycoprotein, the encoded product of the human MDR1 (ABCB1) gene, is of …

The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin

B Greiner, M Eichelbaum, P Fritz… - The Journal of …, 1999 - Am Soc Clin Investig
Recent data point to the contribution of P-glycoprotein (P-gp) to digoxin elimination. On the
basis of clinical observations of patients in whom digoxin levels decreased considerably …

Frequency of single nucleotide polymorphisms in the P‐glycoprotein drug transporter MDR1 gene in white subjects

I Cascorbi, T Gerloff, A Johne, C Meisel… - Clinical …, 2001 - Wiley Online Library
Background P‐glycoprotein, the gene product of MDR1, confers multidrug resistance
against antineoplastic agents but also plays an important role in the bioavailability of …

Drugs as P-glycoprotein substrates, inhibitors, and inducers

RB Kim - Drug metabolism reviews, 2002 - Taylor & Francis
In humans, there are two P-glycoprotein (P-gp) transporters encoded by MDR1 (PGY1) and
MDR3 (also named MDR2 and PGY3) adjacently located at the chromosomal region 7q21 …

Gut microbiota modulates drug pharmacokinetics

J Zhang, J Zhang, R Wang - Drug metabolism reviews, 2018 - Taylor & Francis
Gut microbiota, one of the determinants of pharmacokinetics, has long been underestimated.
It is now generally accepted that the gut microbiota plays an important role in drug …

MDR1 pharmacogenetics: frequency of the C3435T mutation in exon 26 is significantly influenced by ethnicity

MM Ameyaw, F Regateiro, T Li, X Liu… - Pharmacogenetics …, 2001 - journals.lww.com
Abstract P-glycoprotein (PGP), the product of the multidrug resistance gene (MDR1), acts as
an energy-dependent efflux pump that exports its substrates out of the cell. PGP expression …

Inhibition of P-glycoprotein–mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine

MF Fromm, RB Kim, CM Stein, GR Wilkinson… - Circulation, 1999 - Am Heart Assoc
Background—Although quinidine is known to elevate plasma digoxin concentrations, the
mechanism underlying this interaction is not fully understood. Digoxin is not extensively …

The barrier function of CYP3A4 and P-glycoprotein in the small bowel

PB Watkins - Advanced drug delivery reviews, 1997 - Elsevier
CYP3A4 present in small bowel enterocytes can catalyze substantial metabolism of some
orally administered drugs and, thus, exerts a first-pass effect. Recent data indicate that the P …