Skip to main content
Article thumbnail
Location of Repository

Pharmacokinetics of 18F-labeled fluconazole in healthy human subjects by positron emission tomography.

By A J Fischman, N M Alpert, E Livni, S Ray, I Sinclair, R J Callahan, J A Correia, D Webb, H W Strauss and R H Rubin


The distribution of fluconazole in tissue of human volunteers was determined by positron emission tomographic scanning over a 2-h period following the infusion of a tracer dose of 18F-fluconazole (5 to 7 mCi) plus 400 mg of unlabeled drug (the standard daily dose of fluconazole). Previous studies have validated this approach for animals. From serial positron emission tomographic imaging and blood sampling, pharmacokinetics of fluconazole in tissue were determined. There was significant distribution of the radiolabeled drug in all organs studied, with nearly constant levels achieved by 1 h. Plateau concentrations of fluconazole in key organs (micrograms per gram) included the following: whole brain, 4.92 +/- 0.17; heart, 6.98 +/- 0.20; lung, 7.81 +/- 0.46; liver, 12.94 +/- 0.24; spleen, 22.96 +/- 2.5; kidney, 11.23 +/- 0.61; prostate, 8.24 +/- 0.58; and blood, 3.76 +/- 0.30. Since levels of fluconazole of > 6 micrograms/g are needed to treat infection with most strains of Candida and levels of > 10 micrograms/g are needed for Cryptococcus neoformans, Coccidioides immitis, and Histoplasma capsulatum, the following predictions can be made. The current standard dose of 400 mg/day should be more than adequate in the treatment of urinary tract and hepatosplenic candidiasis but problematic in the treatment of candidal osteomyelitis, even with the higher levels that develop after multiple doses. Similarly, higher doses should be considered, particularly in immunocompromised patients, with infection with C. neoformans, H. capsulatum, and C. immitis that involves the central nervous and musculoskeletal systems

Topics: Research Article
Year: 1993
OAI identifier:
Provided by: PubMed Central
Sorry, our data provider has not provided any external links therefore we are unable to provide a link to the full text.

Suggested articles

To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.