ArticleDrug metabolism and disposition: the biological fate of chemicals2009
Interaction of macrolide antibiotics with intestinally expressed human and rat organic anion-transporting polypeptides.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 43 citations in OpenAlex.
- A modified grapefruit juice eliminates two compound classes as major mediators of the grapefruit juice-fexofenadine interaction: an in vitro-in vivo "connect".Journal of clinical pharmacology · 2013Trial
- Effect of clarithromycin and fluconazole on the pharmacokinetics of montelukast in human volunteers.European journal of clinical pharmacology · 2012Trial
- Drug-Drug Interactions in Nosocomial Infections: An Updated Review for Clinicians.Pharmaceutics · 2024Review
- Conversion of Olmesartan to Olmesartan Medoxomil, A Prodrug that Improves Intestinal Absorption, Confers Substrate Recognition by OATP2B1.Pharmaceutical research · 2024Article
- Computational Studies on Selected Macrolides Active againstMolecules (Basel, Switzerland) · 2022Article
- 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
- Drug Interactions for Patients with Respiratory Diseases Receiving COVID-19 Emerged Treatments.International journal of environmental research and public health · 2021Review
- Digoxin absorption decreased independently of P-gp activity in rats with irinotecan-induced gastrointestinal damage.Journal of pharmaceutical health care and sciences · 2021Article
- Disease-drug and drug-drug interaction in COVID-19: Risk and assessment.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2021Review
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- Effects of Nigella sativa, Lepidium sativum and Trigonella foenum-graecum on sildenafil disposition in beagle dogs.European journal of drug metabolism and pharmacokinetics · 2015Article
- Effect of ABCC2 (MRP2) transport function on erythromycin metabolism.Clinical pharmacology and therapeutics · 2011Article
- Neuropsychiatric manifestations associated with azithromycin in two brothers.European journal of clinical pharmacology · 2010Article
- Reliability of inhibition models to correctly identify type of inhibition.Pharmaceutical research · 2010Article
- Azithromycin-induced Adolescent Manic Episode with Psychotic Features: A Case Report.Innovations in clinical neuroscienceArticle
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The macrolide antibiotics azithromycin and clarithromycin are large molecular weight compounds that exhibit moderate to excellent oral bioavailability in preclinical species and humans. Previous concomitant dosing studies in rats using rifamycin SV, a general organic anion-transporting polypeptide (OATP) inhibitor, suggested that the high oral absorption of azithromycin and clarithromycin may be caused by facilitative uptake by intestinal Oatps. In this study, we used OATP/Oatp-expressing cells to investigate the interaction of macrolides with rat Oatp1a5, human OATP1A2, and human/rat OATP2B1/Oatp2b1. These experiments showed that azithromycin and clarithromycin were potent inhibitors of rat Oatp1a5-mediated taurocholate uptake with apparent inhibitor constant (K(i)) values of 3.3 and 2.4 microM, respectively. The macrolides functioned as noncompetitive inhibitors but were not transport substrates for rat Oatp1a5, as assessed by direct uptake measurements of radiolabeled azithromycin and clarithromycin. cis-Inhibition and direct uptake studies further showed that azithromycin and clarithromycin were only very weak inhibitors and not substrates for human OATP1A2 and human/rat OATP2B1/Oatp2b1. In summary, these results indicate that the macrolides azithromycin and clarithromycin potently inhibit rat Oatp1a5 but do not significantly interact with OATP1A2 and OATP2B1/Oatp2b1. These intestinally expressed OATP/Oatp(s) are not responsible for the postulated facilitative uptake of azithromycin and clarithromycin, and alternative facilitative pathways must exist for their intestinal absorption.
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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.