Trial reportBritish journal of clinical pharmacology2007
Effects of clarithromycin and grapefruit juice on the pharmacokinetics of glibenclamide.
Trial report in British journal of clinical pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
24 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Improving antibacterial prescribing safety in the management of COPD exacerbations: systematic review of observational and clinical studies on potential drug interactions associated with frequently prescribed antibacterials among COPD patients.The Journal of antimicrobial chemotherapy · 2019Pooled it
- Evaluation of the pharmacokinetics of glibenclamide tablet given, off label, orally to children suffering from neonatal syndromic hyperglycemia.European journal of clinical pharmacology · 2016Trial
- Population Pharmacokinetic Modeling Study of Glibenclamide in Chinese Healthy Volunteers.European journal of drug metabolism and pharmacokinetics · 2026Article
- Repeated Intake of Grapefruit Juice Inhibits CYP2B6, CYP2C9, CYP2C19, and CYP3A4 while Lingonberry Powder Does Not Induce Major CYP Enzymes in Humans.Clinical pharmacology and therapeutics · 2026Article
- Virtual Bioequivalence Assessment and Dissolution Safe Space Exploration for Fixed-Dose Metformin-Glyburide Tablet Using Physiologically Based Biopharmaceutics Modeling.Pharmaceutics · 2025Article
- Dietary Modulation of CYP3A4 and Its Impact on Statins and Antidiabetic Drugs: A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2025Review
- The Use of Microdosing for In vivo Phenotyping of Cytochrome P450 Enzymes: Where Do We Stand? A Narrative Review.European journal of drug metabolism and pharmacokinetics · 2024Review
- Article
- A regulatory science viewpoint on botanical-drug interactions.Journal of food and drug analysis · 2018Review
- Comprehensive PBPK Model of Rifampicin for Quantitative Prediction of Complex Drug-Drug Interactions: CYP3A/2C9 Induction and OATP Inhibition Effects.CPT: pharmacometrics & systems pharmacology · 2018Article
- Toxicological and Biochemical Analyses of an Autopsy Case Involving Oral Overdose of Multiple Antidiabetic and Antihypertensive Drugs.Case reports in medicine · 2018Article
- Review
- Hypoglycemia after antimicrobial drug prescription for older patients using sulfonylureas.JAMA internal medicine · 2014Article
- Mechanism-based pharmacokinetic modeling to evaluate transporter-enzyme interplay in drug interactions and pharmacogenetics of glyburide.The AAPS journal · 2014Article
- Sucralose, a synthetic organochlorine sweetener: overview of biological issues.Journal of toxicology and environmental health. Part B, Critical reviews · 2013Review
- Pharmacokinetic drug interactions of antimicrobial drugs: a systematic review on oxazolidinones, rifamycines, macrolides, fluoroquinolones, and Beta-lactams.Pharmaceutics · 2011Article
- Transporter-mediated drug-drug interactions with oral antidiabetic drugs.Pharmaceutics · 2011Article
- The effect of grapefruit juice on drug disposition.Expert opinion on drug metabolism & toxicology · 2011Review
- Grapefruit-drug interactions.Drugs · 2010Review
- Fruit juice inhibition of uptake transport: a new type of food-drug interaction.British journal of clinical pharmacology · 2010Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsCase reports suggest that clarithromycin can increase the glucose-lowering effect of glibenclamide which is metabolized mainly by CYP2C9 and is a substrate for P-glycoprotein and OATP2B1. Our objective was to evaluate whether the P-glycoprotein inhibitor, clarithromycin, increases and the putative OATP2B1 inhibitor, grapefruit juice, decreases plasma concentrations of glibenclamide.
methodsIn a randomized three-phase crossover study, 12 subjects ingested 250 mg clarithromycin or placebo twice daily or 200 ml grapefruit juice three times daily for 2 days. On day 3, they ingested 0.875 mg glibenclamide with sugar water or grapefruit juice. Concentrations of glibenclamide and clarithromycin in plasma, glucose in blood, and excretion of hydroxy-glibenclamide into urine were measured up to 12 h.
resultsClarithromycin increased the peak concentration (C(max)) of glibenclamide to 1.25-fold (95% confidence interval (CI) 1.12, 1.40; P < 0.01) and the area under the plasma concentration-time curve to 1.35-fold (95% CI 1.21, 1.50; P < 0.01) compared with the placebo phase. The time to C(max), the half-life of glibenclamide, and the amount of hydroxy-glibenclamide excreted into urine remained unaltered. Grapefruit juice did not change the pharmacokinetics of glibenclamide. Clarithromycin concentrations implied a good compliance. Blood glucose did not deviate between the phases.
conclusionsClarithromycin increased plasma concentrations of glibenclamide, possibly by inhibiting P-glycoprotein in the intestinal wall. Although not seen with the present study design, clarithromycin may enhance the effect of glibenclamide by increasing plasma glibenclamide concentrations, which warrants close monitoring of blood glucose during their co-administration. Grapefruit juice had no effect on glibenclamide pharmacokinetics.
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