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Biliary levels of ceforanide.

D E Kenady, M D Ram

    Antimicrobial Agents and Chemotherapy
    |May 1, 1983
    PubMed
    Summary

    Ceforanide achieves high concentrations in the biliary tract, including gallbladder bile and tissue, in patients with normal or diseased biliary systems. Drug levels were notably lower in gallbladder bile with an occluded cystic duct.

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    Area of Science:

    • Pharmacology
    • Hepatobiliary Medicine
    • Infectious Diseases

    Background:

    • Biliary tract infections pose significant clinical challenges.
    • Understanding antibiotic penetration into biliary tissues is crucial for effective treatment.
    • Ceforanide is a cephalosporin antibiotic with potential applications in treating infections.

    Purpose of the Study:

    • To quantify Ceforanide concentrations in plasma, gallbladder bile, gallbladder tissue, and common bile duct.
    • To evaluate Ceforanide's distribution in the biliary tract of patients with normal and diseased conditions.
    • To assess the impact of biliary tract pathology, specifically cystic duct patency, on drug levels.

    Main Methods:

    • Intravenous administration of 1g Ceforanide to 45 patients (10 normal, 35 with biliary disease).
    • Measurement of drug levels at various intervals post-injection in plasma, gallbladder bile, gallbladder tissue, and common bile duct.
    • Comparison of Ceforanide concentrations between patients with normal biliary tracts and those with chronic cholecystitis (patent vs. occluded cystic duct).

    Main Results:

    • Peak plasma Ceforanide levels (67 ± 15 µg/ml) were reached within 1 hour.
    • High gallbladder bile levels (76 ± 25 µg/ml at 2h, 182 ± 51 µg/ml at 4h) were observed in patients with normal biliary tracts and patent cystic ducts.
    • Significantly lower gallbladder bile concentrations (14 ± 7 µg/ml at 2h) occurred in patients with occluded cystic ducts.
    • Consistent gallbladder tissue levels (21 ± 3 µg/g at 1-3h) were achieved regardless of cystic duct status.
    • Common bile duct concentrations reached 149 ± 59 µg/ml at 2h, remaining above 60 µg/ml for 1-4 hours.

    Conclusions:

    • Ceforanide effectively penetrates the biliary tract, achieving substantial concentrations in bile and tissue.
    • Cystic duct patency is critical for optimal Ceforanide accumulation in gallbladder bile.
    • The drug's high biliary concentrations suggest potential efficacy for preventing and treating biliary infections.

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