Skip to main content
Postgraduate Medical Journal logoLink to Postgraduate Medical Journal
. 1979 Sep;55(647):657–661. doi: 10.1136/pgmj.55.647.657

Ketoconazole, an oral antifungal: laboratory and clinical assessment of imidazole drugs.

D Borelli, J L Bran, J Fuentes, R Legendre, E Leiderman, H B Levine, A Restrepo, D A Stevens
PMCID: PMC2425651  PMID: 523356

Abstract

Miconazole, a parenterally administered imidazole antifungal agent has been shown to produce responses in systemic fungal infections in man. Ketoconazole, an analogue, can be given by mouth. It is inhibitory in vitro at low concentrations to most fungi. Blood levels after oral administration to animals and man greatly exceed these inhibitory concentrations for several hours. The efficacy of this drug has been demonstrated in animal models. Initial clinical evaluation has produced responses to therapy with 200-400 mg/day in 13 of 16 evaluable patients with systemic and superficial fungal infections, involving 10 fungal pathogens. No toxicity has been noted to date in these human studies. Ketoconazole is a promising agent needing further extensive evaluation.

Full text

PDF
657

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Brincker H. Miconazole in oral candidiasis. Proc R Soc Med. 1977;70 (Suppl 1):29–31. doi: 10.1177/00359157770700S109. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Fischer T. J., Klein R. B., Kershnar H. E., Borut T. C., Stiehm E. R. Miconazole in the treatment of chronic mucocutaneous candidiasis: a preliminary report. J Pediatr. 1977 Nov;91(5):815–819. doi: 10.1016/s0022-3476(77)81050-0. [DOI] [PubMed] [Google Scholar]
  3. Galgiani J. N., Stevens D. A. Antimicrobial susceptibility testing of yeasts: a turbidimetric technique independent of inoculum size. Antimicrob Agents Chemother. 1976 Oct;10(4):721–728. doi: 10.1128/aac.10.4.721. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Harvey R. P., Schmid E. S., Carrington C. C., Stevens D. A. Mouse model of pulmonary blastomycosis: utility, simplicity, and quantitative parameters. Am Rev Respir Dis. 1978 Apr;117(4):695–703. doi: 10.1164/arrd.1978.117.4.695. [DOI] [PubMed] [Google Scholar]
  5. Levine H. B. R34000, a dioxolane imidazole in the therapy for experimental coccidioidomycosis. Comparison with miconazole and econazole. Chest. 1976 Dec;70(6):755–759. doi: 10.1378/chest.70.6.755. [DOI] [PubMed] [Google Scholar]
  6. Levine H. B., Stevens D. A., Cobb J. M., Gebhardt A. E. Miconazole in coccidioidomycosis. I. Assays of activity in mice and in vitro. J Infect Dis. 1975 Oct;132(4):407–414. doi: 10.1093/infdis/132.4.407. [DOI] [PubMed] [Google Scholar]
  7. Lutwick L. I., Rytel M. W., Yañez J. P., Galgiani J. N., Stevens D. A. Deep infections from Petriellidium boydii treated with miconazole. JAMA. 1979 Jan 19;241(3):272–273. [PubMed] [Google Scholar]
  8. Sawyer P. R., Brogden R. N., Pinder R. M., Speight T. M., Avery G. S. Miconazole: a review of its antifungal activity and therapeutic efficacy. Drugs. 1975;9(6):406–423. doi: 10.2165/00003495-197509060-00002. [DOI] [PubMed] [Google Scholar]
  9. Stevens D. A., Levine H. B., Deresinski S. C. Miconazole in coccidiodomycosis. II. Therapeutic and pharmacologic studies in man. Am J Med. 1976 Feb;60(2):191–202. doi: 10.1016/0002-9343(76)90428-9. [DOI] [PubMed] [Google Scholar]
  10. Stevens D. A., Restrepo-M A., Cortés A., Betancourt J., Galgiani J. N., Gómez I. Paracoccidioidomycosis (South American blastomycosis): treatment with miconazole. Am J Trop Med Hyg. 1978 Jul;27(4):801–807. doi: 10.4269/ajtmh.1978.27.801. [DOI] [PubMed] [Google Scholar]
  11. Stevens D. Miconazole in the treatment of systemic fungal infections. Am Rev Respir Dis. 1977 Nov;116(5):801–806. doi: 10.1164/arrd.1977.116.5.801. [DOI] [PubMed] [Google Scholar]
  12. Van Cutsem J. M., Thienpont D. Miconazole, a broad-spectrum antimycotic agent with antibacterial activity. Chemotherapy. 1972;17(6):392–404. doi: 10.1159/000220875. [DOI] [PubMed] [Google Scholar]
  13. Verhaegen H. Miconazole treatment in candidal oesophagitis. Proc R Soc Med. 1977;70 (Suppl 1):47–50. doi: 10.1177/00359157770700S114. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from Postgraduate Medical Journal are provided here courtesy of BMJ Publishing Group

RESOURCES