ArticleAntimicrobial agents and chemotherapy2012
Comparison of fluconazole renal penetration levels in healthy and Candida albicans-infected Wistar rats.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- DoesFuture microbiology · 2025Article
- Prediction of higher ceftazidime-avibactam concentrations in the human renal interstitium compared with unbound plasma using a minimal physiologically based pharmacokinetic model developed in rats and pigs through microdialysis.Antimicrobial agents and chemotherapy · 2025Article
- Amphotericin B tissue penetration and pharmacokinetics in healthy andFrontiers in pharmacology · 2024Article
- Population Pharmacokinetic Modeling of Free Plasma and Free Brain Concentrations of Ceftaroline in Healthy and Methicillin-Resistant Staphylococcus aureus-Infected Wistar Rats.Antimicrobial agents and chemotherapy · 2023Article
- Population Pharmacokinetic Modeling to Describe the Total Plasma and Free Brain Levels of Fluconazole in Healthy and Cryptococcus neoformans Infected Rats: How Does the Infection Impact the Drug's Levels on Biophase?Pharmaceutical research · 2018Article
- Effect of Efflux Transporter Inhibition on the Distribution of Fluconazole in the Rat Brain.Neurochemical research · 2017Article
- Utility of Microdialysis in Infectious Disease Drug Development and Dose Optimization.The AAPS journal · 2017Review
- Simultaneous Semimechanistic Population Analyses of Levofloxacin in Plasma, Lung, and Prostate To Describe the Influence of Efflux Transporters on Drug Distribution following Intravenous and Intratracheal Administration.Antimicrobial agents and chemotherapy · 2016Article
- In Vivo Microdialysis To Determine Subcutaneous Interstitial Fluid Penetration and Pharmacokinetics of Fluconazole in Intensive Care Unit Patients with Sepsis.Antimicrobial agents and chemotherapy · 2016Observational
- Population pharmacokinetic modeling of the unbound levofloxacin concentrations in rat plasma and prostate tissue measured by microdialysis.Antimicrobial agents and chemotherapy · 2014Article
- Importance of relating efficacy measures to unbound drug concentrations for anti-infective agents.Clinical microbiology reviews · 2013Review
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Authors and funding
7 authors.
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Abstract
The aims of this study were to evaluate free levels of fluconazole (FCZ) in the kidneys of healthy and Candida albicans-infected Wistar rats using microdialysis and to establish the relationship between free renal and total plasma levels under both conditions. Microdialysis recovery rates were determined in vitro by dialysis, and retrodialysis recovery rates were determined in vivo by retrodialysis. The recovery rate was around 50%, independent of the method, drug concentration, or condition (in vitro or in vivo) used. FCZ kidney penetration in healthy and infected rats was investigated after the administration of 10 mg/kg of body weight intravenously (i.v.) or 50 mg/kg orally (n = 6/group) and blood and microdialysate sample harvesting at predetermined time points up to 24 and 18 h, respectively. There were no statistical differences between the area under the free concentration-time curve (AUC(0-∞)) values in plasma and in tissue for either healthy or infected groups for the same dose regimen investigated. The antifungal tissue penetrations were similar for both doses and under all conditions investigated (ranging from 0.77 to 0.84). The unbound fraction of FCZ was concentration independent (86.0% ± 2.0%), allowing the prediction of free renal levels using pharmacokinetic parameters obtained from total plasma fitting. The results showed that free renal and free plasma levels are similar in healthy and systemically C. albicans-infected rats. Therefore, free plasma levels are a good surrogate to estimate free FCZ renal concentrations in systemic candidiasis and can be used to optimize dosing regimens for this drug.
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