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Antimicrob Agents Chemother. 1982 January; 21(1): 151–158.
PMCID: PMC181844

Disposition of ketoconazole, an oral antifungal, in humans.


The pharmacology of ketoconazole was studied in patients with fungal infections. After administration of 50-, 100-, and 200-mg doses of ketoconazole, there was a linear increase in the area under the curve of serum concentrations; this was not apparent when higher doses of ketoconazole were given. An increase in the area under the curve occurred in patients receiving 200 mg daily who were restudied after 1 to 12 months of therapy. However, normalized area under the curve appeared to decrease after higher doses were administered chronically. The half life ranged from 2.0 to 3.3 h. Peak serum concentrations up to 50 micrograms/ml were detected in this study, and potentially therapeutic concentrations were detectable up to 26 h after high doses. Ketoconazole penetrated the saliva and inflamed joint fluid and meninges, although variably, and could be demonstrated in some other tissue compartments. In the presence of renal failure, ketoconazole disposition was not altered, whereas in the presence of hepatic insufficiency, an alteration in disposition was suggested. The interactions of ketoconazole and other drugs were studied. Of note, antacids did not significantly affect ketoconazole pharmacokinetics (nor did meals), and ketoconazole and warfarin did not appear to affect the pharmacokinetics of the other.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.
  • Bennett JE. Clotrimazole: new drug for systemic mycoses? Ann Intern Med. 1970 Oct;73(4):653–654. [PubMed]
  • Borelli D, Bran JL, Fuentes J, Legendre R, Leiderman E, Levine HB, Restrepo A, Stevens DA. Ketoconazole, an oral antifungal: laboratory and clinical assessment of imidazole drugs. Postgrad Med J. 1979 Sep;55(647):657–661. [PMC free article] [PubMed]
  • Niemegeers CJ, Levron JC, Awouters F, Janssen PA. Inhibition and induction of microsomal enzymes in rat. A comparative study of four antimycotics: miconazole, econazole, clotrimazole and ketoconazole. Arch Int Pharmacodyn Ther. 1981 May;251(1):26–38. [PubMed]

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