ArticleAntimicrobial agents and chemotherapy2004
Possible involvement of the drug transporters P glycoprotein and multidrug resistance-associated protein Mrp2 in disposition of azithromycin.
Article in Antimicrobial agents and chemotherapy, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers, 3 of them syntheses that pooled it.
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Who cites it
44 citing papers in PubMed, 3 syntheses or guidelines pooled it, 107 citations in OpenAlex.
- Influential predictors of azithromycin pharmacokinetics: a systematic review of population pharmacokinetics.Annals of medicine · 2025Pooled it
- Significant Predictors of Azithromycin in Population Pharmacokinetic Analysis: A Systematic Review.Drug design, development and therapy · 2025Pooled it
- Interethnic differences in pharmacokinetics of antibacterials.Clinical pharmacokinetics · 2015Pooled it
- Influence of body weight, ethnicity, oral contraceptives, and pregnancy on the pharmacokinetics of azithromycin in women of childbearing age.Antimicrobial agents and chemotherapy · 2012Trial
- Pharmacogenomics of antibacterial and antiviral therapies: Clinical actionability, evidence gaps, and future directions.Pharmacological reviews · 2026Review
- Exposure to azithromycin and the effect of co-administration of rifampicin in patients with non-tuberculous mycobacterial disease.The Journal of antimicrobial chemotherapy · 2026Article
- Biopharmaceutic Assessment of Post-Approval Changes for Azithromycin Immediate Release Tablets Using Predictive In Vitro Dissolution and a Model-Informed Approach.Pharmaceutical research · 2026Article
- Drug-Drug Interactions in Nosocomial Infections: An Updated Review for Clinicians.Pharmaceutics · 2024Review
- Low azithromycin maximal concentrations in patients concomitantly taking rifampicin: time to move away from rifampicin in the treatment of non-tuberculous mycobacteria?Antimicrobial agents and chemotherapy · 2024Article
- Genetics ofCancers · 2023Review
- Review
- Developmental Pharmacokinetics of Antibiotics Used in Neonatal ICU: Focus on Preterm Infants.Biomedicines · 2023Review
- Impacts of COVID-19 in Breast Cancer: From Molecular Mechanism to the Treatment Approach.Current pharmaceutical biotechnology · 2023Review
- Article
- Core shell stationary phase for a novel separation of some COVID-19 used drugs by UPLC-MS/MS Method: Study of grapefruit consumption impact on their pharmacokinetics in rats.Microchemical journal : devoted to the application of microtechniques in all branches of science · 2022Article
- Plasma Protein Binding Rate and Pharmacokinetics of Lekethromycin in Rats.Antibiotics (Basel, Switzerland) · 2022Article
- P-glycoprotein: new insights into structure, physiological function, regulation and alterations in disease.Heliyon · 2022Review
- Elevation of alkaline phosphatase and long-term drug therapy for cystic fibrosis.European journal of clinical pharmacology · 2022Article
- Macrolide Treatment Failure due to Drug-Drug Interactions: Real-World Evidence to Evaluate a Pharmacological Hypothesis.Pharmaceutics · 2022Article
- ADME and Pharmacokinetic Properties of Remdesivir: Its Drug Interaction Potential.Pharmaceuticals (Basel, Switzerland) · 2021Review
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
P glycoprotein and multidrug resistance-associated protein 2 (Mrp2), ATP-dependent membrane transporters, exist in a variety of normal tissues and play important roles in the disposition of various drugs. The present study seeks to clarify the contribution of P glycoprotein and/or Mrp2 to the disposition of azithromycin in rats. The disappearance of azithromycin from plasma after intravenous administration was significantly delayed in rats treated with intravenous injection of cyclosporine, a P-glycoprotein inhibitor, but was normal in rats pretreated with intraperitoneal injection erythromycin, a CYP3A4 inhibitor. When rats received an infusion of azithromycin, cyclosporine and probenecid, a validated Mrp2 inhibitor, significantly decreased the steady-state biliary clearance of azithromycin to 5 and 40% of the corresponding control values, respectively. However, both inhibitors did not alter the renal clearance of azithromycin, suggesting the lack of renal tubular secretion of azithromycin. Tissue distribution experiments showed that azithromycin is distributed largely into the liver, kidney, and lung, whereas both inhibitors did not alter the tissue-to-plasma concentration ratio of azithromycin. Significant reduction in the biliary excretion of azithromycin was observed in Eisai hyperbilirubinemic rats, which have a hereditary deficiency in Mrp2. An in situ closed-loop experiment showed that azithromycin was excreted from the blood into the gut lumen, and the intestinal clearance of azithromycin was significantly decreased by the presence of cyclosporine in the loop. These results suggest that azithromycin is a substrate for both P glycoprotein and Mrp2 and that the biliary and intestinal excretion of azithromycin is mediated via these two drug transporters.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.