Pharmacodynamics of liposomal amphotericin B and flucytosine for cryptococcal meningoencephalitis: safe and effective regimens for immunocompromised patients.

Background: Cryptococcal meningoencephalitis is a lethal infection with relatively few therapeutic options. The optimal dosage of liposomal amphotericin B (LAmB) alone or in combination with flucytosine is not known.Methods: A murine model of cryptococcal meningoencephalitis was used. The fungal den...

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Published in:Journal of Infectious Diseases Vol. 208; no. 2; pp. 351 - 362
Main Authors: O'Connor, Lucy, Livermore, Joanne, Sharp, Andrew D, Goodwin, Joanne, Gregson, Lea, Howard, Susan J, Felton, Timothy W, Schwartz, Julie A, Neely, Michael N, Harrison, Thomas S, Perfect, John R, Hope, William W
Format: research Journal Article
Published: Oxford University Press / USA Jul2013
Online Access:View this record in EBSCOhost
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      pub: Oxford University Press / USA
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        atl: Pharmacodynamics of liposomal amphotericin B and flucytosine for cryptococcal meningoencephalitis: safe and effective regimens for immunocompromised patients.
      aug:
        au:
          O'Connor, Lucy
          Livermore, Joanne
          Sharp, Andrew D
          Goodwin, Joanne
          Gregson, Lea
          Howard, Susan J
          Felton, Timothy W
          Schwartz, Julie A
          Neely, Michael N
          Harrison, Thomas S
          Perfect, John R
          Hope, William W
        affil: School of Translational Medicine, The University of Manchester, Manchester Academic Health Science Centre, National Institute for Health Research Translational Research Facility in Respiratory Medicine, University Hospital of South Manchester National Health Service, Foundation Trust.
      sug:
        subj:
          Amphotericin B Pharmacodynamics
          Antifungal Agents Pharmacodynamics
          Cryptococcus Drug Effects
          Heterocyclic Compounds Pharmacodynamics
          Meningitis, Cryptococcal Drug Therapy
          Meningoencephalitis Drug Therapy
          Amphotericin B Pharmacokinetics
          Animals
          Antifungal Agents Pharmacokinetics
          Brain Drug Effects
          Brain Microbiology
          Cryptococcus
          Drug Therapy, Combination
          Heterocyclic Compounds Pharmacokinetics
          Immunocompromised Host
          Male
          Meningitis, Cryptococcal Immunology
          Meningitis, Cryptococcal Metabolism
          Meningitis, Cryptococcal Microbiology
          Meningoencephalitis Microbiology
          Mice
          Microbial Culture and Sensitivity Tests
          Models, Biological
          Male
      ab: Background: Cryptococcal meningoencephalitis is a lethal infection with relatively few therapeutic options. The optimal dosage of liposomal amphotericin B (LAmB) alone or in combination with flucytosine is not known.Methods: A murine model of cryptococcal meningoencephalitis was used. The fungal density in the brain was determined using quantitative cultures. Pharmacokinetic-pharmacodynamic relationships were determined for LAmB and flucytosine administered alone. The effect of the combination was described using the Greco model and a mathematical model. The results were bridged to humans.Results: Inoculation resulted in hematogenous dissemination and logarithmic growth within the central nervous system. There was histological evidence of multifocal infection throughout the brain. Both LAmB and flucytosine produced a dose-dependent reduction in fungal burden. The effect of the combination of agents in the brain was additive. Bridging studies suggested that a human dosage of LAmB 3 mg/kg/d resulted in a submaximal antifungal effect. Regimens of LAmB 6 mg/kg/d alone, LAmB 3 mg/kg/d plus flucytosine 50 mg/kg/d, and LAmB 3 mg/kg/d plus flucytosine 100 mg/kg/d all resulted in near-maximal antifungal activity.Conclusions: Potential regimens for further study in clinical trials include LAmB 6 mg/kg/d alone, LAmB 3 mg/kg/d plus flucytosine 50 mg/kg/d, and LAmB 3 mg/kg/d plus flucytosine 100 mg/kg/d.
      pubtype: Academic Journal
      doctype:
        research
        Journal Article
      ougenre: Article
    language: English
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