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Appropriate nitroxoline dosage regimen design.

R Karba, A Mrhar, F Kozjek

    International Journal of Clinical Pharmacology and Biopharmacy
    |December 1, 1979
    PubMed
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    The standard nitroxoline dosage is ineffective for urinary tract infections. This study identifies optimal nitroxoline dosage forms and regimens for improved antibacterial activity and treatment success.

    Area of Science:

    • Pharmacology
    • Microbiology
    • Drug Delivery

    Background:

    • The current clinical dosage of nitroxoline (100 mg three times daily) is insufficient for effective treatment of urinary tract infections.
    • Nitroxoline requires concentrations above 6 mg/l for significant antibacterial activity, as confirmed by in vitro studies.

    Purpose of the Study:

    • To determine the most appropriate dosage form for nitroxoline.
    • To design an optimal dosage regimen for nitroxoline to ensure therapeutic efficacy.

    Main Methods:

    • Utilized a pharmacokinetic model to analyze drug behavior.
    • Employed multiple dosing simulations on an analog-hybrid computer (EAI 580).
    • Evaluated various dosage form alternatives.

    Main Results:

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    • Identified two viable nitroxoline dosage forms.
    • Determined the necessary dose and appropriate dosage interval for these forms.
    • Established regimens that achieve effective antibacterial concentrations.

    Conclusions:

    • The standard nitroxoline regimen is suboptimal for achieving therapeutic concentrations.
    • New dosage forms and regimens are proposed to enhance nitroxoline's effectiveness as a urinary antiseptic.