ArticleBritish journal of clinical pharmacology2006
Induction of P-glycoprotein in lymphocytes by carbamazepine and rifampicin: the role of nuclear hormone response elements.
Article in British journal of clinical pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 45 citations in OpenAlex.
- Carbamazepine differentially affects the pharmacokinetics of fexofenadine enantiomers.British journal of clinical pharmacology · 2012Trial
- Impact of rifampicin on P-glycoprotein (ABCB1) expression in M1 and M2 macrophages derived from the THP-1 monocytic cell line or peripheral blood mononuclear cells.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- THP-1-derived polarized macrophages differ by drug transporter transcriptomics, P-glycoprotein activity and rifampicin uptake kinetics.Archives of toxicology · 2026Article
- Intracellular Penetration of Atazanavir, Ritonavir and Dolutegravir With Concomitant Rifampicin: A Dose Escalation Study.Clinical pharmacology and therapeutics · 2025Article
- Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug-Drug Interaction between Rivaroxaban and Carbamazepine in Humans.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Application of physiologically-based pharmacokinetic model approach to predict pharmacokinetics and drug-drug interaction of rivaroxaban: A case study of rivaroxaban and carbamazepine.CPT: pharmacometrics & systems pharmacology · 2022Article
- Effects of Carbamazepine and Phenytoin on Pharmacokinetics and Pharmacodynamics of Rivaroxaban.Pharmaceutics · 2020Article
- Metabolome Analysis Reveals Dermal Histamine Accumulation in Murine Dermatitis Provoked by Genetic Deletion of P-Glycoprotein and Breast Cancer Resistance Protein.Pharmaceutical research · 2019Article
- In Vitro Assessment of the Effect of Antiepileptic Drugs on Expression and Function of ABC Transporters and Their Interactions with ABCC2.Molecules (Basel, Switzerland) · 2017Article
- Pregnane X Receptor Not Nuclear Factor-kappa B Up-regulates P-glycoprotein Expression in the Brain of Chronic Epileptic Rats Induced by Kainic Acid.Neurochemical research · 2017Article
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- The influence ofBalkan journal of medical genetics : BJMG · 2016Article
- P-glycoprotein Expression and Pharmacoresistant Epilepsy: Cause or Consequence?Epilepsy currents · 2014Article
- Article
- Psychotropic drug-drug interactions involving P-glycoprotein.CNS drugs · 2012Review
- Metabolism considerations for kinase inhibitors in cancer treatment.Expert opinion on drug metabolism & toxicology · 2010Review
- Comparison of the induction profile for drug disposition proteins by typical nuclear receptor activators in human hepatic and intestinal cells.British journal of pharmacology · 2008Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsCarbamazepine (CBZ) is an inducer of cytochrome P450 enzymes, which have been implicated in many drug interactions. However, for immunosuppressant and anti-HIV drugs, whose main site of action is the lymphocyte, induction of P-glycoprotein (Pgp) may also be important. In this study, we have investigated whether CBZ acts as an inducer of Pgp in lymphocytes.
methodsPgp expression was assessed by flow cytometry and real-time reverse transcriptase-polymerase chain reaction using lymphocytes from four healthy subjects after incubation with therapeutic concentrations of CBZ, using rifampicin as a positive control. Binding to DR-4 elements in the MDR1 promoter was assessed by electrophoretic mobility shift assay (EMSA) and a luciferase-reporter construct.
resultsCBZ increased MDR1 mRNA expression at 6 h by 3.7-fold [95% confidence interval (CI) 0, 7.6) when compared with controls. CBZ increased lymphocyte Pgp expression at 72 h by 7.6-fold (95% CI 2.1, 13.2) over control values. EMSA revealed a 2.1-fold (95% CI 1.5, 2.7) increased binding to the DR-4 element of CBZ when compared with control values. Activation of the DR-4 element was confirmed using reporter constructs. Rifampicin also had similar effects in all experiments.
conclusionsCarbamazepine induces Pgp in a manner comparable to rifampicin, by increasing binding to the DR4 element. This has implications for interactions involving drugs whose site of action is the lymphocyte.
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