Penicillin levels in blood and CSF achieved by treatment of syphilis

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Published on: December 27, 2016

E M Dunlop, S S Al-Egaily, E T Houang

    JAMA
    |June 8, 1979
    PubMed

    Insights

    Penicillin G procaine with aluminum monostearate did not achieve treponemicidal levels in CSF. Combining penicillin G with probenecid successfully reached therapeutic penicillin concentrations in cerebrospinal fluid for syphilis treatment.

    Area of Science:

    • Infectious Diseases
    • Pharmacology
    • Neurology

    Background:

    • Penicillin is the primary treatment for neurosyphilis.
    • Achieving adequate penicillin concentrations in cerebrospinal fluid (CSF) is crucial for effective treatment.
    • Penicillin G procaine with aluminum monostearate (PAM) has been used to prolong penicillin release.

    Purpose of the Study:

    • To evaluate if intramuscular injections of penicillin G procaine with aluminum monostearate can achieve treponemicidal penicillin levels in CSF.
    • To assess the efficacy of probenecid in combination with penicillin G or penicillin G procaine for achieving therapeutic CSF penicillin levels.

    Main Methods:

    • Patients received varying doses of intramuscular penicillin G procaine with aluminum monostearate.
    • In other patient groups, oral probenecid was administered concurrently with intramuscular penicillin G or penicillin G procaine.
    • CSF penicillin levels were measured to determine treponemicidal concentrations.

    Main Results:

    • Intramuscular injections of 600,000 IU penicillin G procaine with PAM did not yield treponemicidal CSF penicillin levels.
    • Concurrent administration of probenecid with penicillin G or penicillin G procaine successfully achieved treponemicidal CSF penicillin levels in a significant proportion of patients.
    • Higher doses of penicillin G procaine, when combined with probenecid, increased the likelihood of achieving therapeutic CSF concentrations.

    Conclusions:

    • Penicillin G procaine with aluminum monostearate alone is insufficient for achieving treponemicidal penicillin levels in CSF.
    • Probenecid significantly enhances CSF penetration of penicillin, making it a valuable adjunct for treating neurosyphilis.
    • Combination therapy with probenecid and penicillin G or penicillin G procaine is effective in reaching therapeutic CSF penicillin concentrations.

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