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Nitrofurantoin disposition

B Hoener, S E Patterson

    Clinical Pharmacology and Therapeutics
    |June 1, 1981
    PubMed
    Summary
    This summary is machine-generated.

    Nitrofurantoin absorption can be erratic, impacting urine concentrations. Oral bioavailability is high, but individual responses vary, affecting treatment efficacy.

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    Area of Science:

    • Pharmacokinetics and Drug Metabolism

    Background:

    • Nitrofurantoin is a widely used antibiotic for urinary tract infections.
    • Understanding its pharmacokinetic profile is crucial for optimizing therapeutic outcomes.

    Purpose of the Study:

    • To characterize the pharmacokinetic properties of nitrofurantoin in healthy male subjects.
    • To assess the oral bioavailability and absorption characteristics of nitrofurantoin tablets.
    • To evaluate urinary excretion and metabolite formation.

    Main Methods:

    • A three-way random crossover study involving six healthy men.
    • Intravenous infusion of nitrofurantoin (50 mg) followed by oral administration of tablets.
    • Plasma concentration monitoring and analysis using a two-compartment open-body model.
    • Assessment of urinary excretion of unchanged drug and its metabolite, aminofurantoin.

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    Main Results:

    • Nitrofurantoin exhibited a terminal half-life of 58.1 ± 15 min after intravenous administration.
    • Oral bioavailability was high, with values of 0.87 ± 0.13 (fasting) and 0.94 ± 0.13 (with food).
    • Absorption rate was complex and erratic; two subjects did not reach the minimum effective urine concentration (32 µg/ml).
    • Urinary excretion of unchanged nitrofurantoin was 47 ± 13%, with 1.2 ± 0.3% recovered as aminofurantoin.

    Conclusions:

    • Nitrofurantoin demonstrates good oral bioavailability, but absorption can be variable.
    • Erratic absorption may lead to sub-therapeutic urine concentrations in some individuals.
    • Further investigation into factors influencing nitrofurantoin absorption and achieving effective urine levels is warranted.