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PMID: 2831809 Published · ppublish English Journal Article Research Support, U.S. Gov't, P.H.S. Review

Azole antifungal agents: emphasis on new triazoles.

Antimicrobial agents and chemotherapy ·Vol. 32 ·No. 1 ·1988-01-00 ·Pages 1-8

Saag MS, Dismukes WE

Abstract

Many advances have been made in antifungal therapy over the last three decades. Itraconazole and fluconazole, two investigational triazole agents, are the most recent additions to the list of antifungal drugs. This review has focused primarily on their mechanisms of action, favorable pharmacologic properties, and spectra of activity against a broad range of systemic pathogens. Itraconazole and fluconazole show much promise as orally active agents, with less potential for toxicity than the currently available azoles. Fluconazole and, to a lesser degree, itraconazole are especially promising therapies for cryptococcal meningitis. In addition, fluconazole may prove to be highly effective in urinary tract infections caused by Candida species and other fungi. Ongoing and future clinical trials will more clearly define the specific roles of itraconazole and fluconazole in the treatment of systemic mycoses.

MeSH Terms
Animals Antifungal Agents/pharmacology,therapeutic use Chemical Phenomena Chemistry Fluconazole Humans Itraconazole Ketoconazole/analogs & derivatives,pharmacology,therapeutic use Mycoses/drug therapy Triazoles/pharmacology,therapeutic use
Chemicals
Antifungal Agents Triazoles Itraconazole Fluconazole Ketoconazole
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Saag M S
Department of Medicine, University of Alabama School of Medicine, Birmingham 35294.
Dismukes W E
References (54)
54 references, click to expand
  1. Antimycotic properties of clotrimazole.
    Postgrad Med J. 1974 Jul;50 Suppl 1:11-2 PMID: 4467159
  2. Hepatic injury associated with ketoconazole therapy. Analysis of 33 cases.
    Gastroenterology. 1984 Mar;86(3):503-13 PMID: 6319220
  3. Effect of free fatty acids on liposome susceptibility to imidazole antifungals.
    Antimicrob Agents Chemother. 1979 Nov;16(5):660-3 PMID: 393166
  4. In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis.
    Antimicrob Agents Chemother. 1980 Jun;17(6):922-8 PMID: 6250469
  5. The activity of ketoconazole in mixed cultures of leukocytes and Candida albicans.
    Sabouraudia. 1980 Sep;18(3):197-210 PMID: 6254187
  6. Treatment of chronic mucocutaneous candidiasis with ketoconazole: a controlled clinical trial.
    Ann Intern Med. 1980 Dec;93(6):791-5 PMID: 6255844
  7. Gynecomastia with ketoconazole.
    Antimicrob Agents Chemother. 1981 Jun;19(6):1073-4 PMID: 6267997
  8. Ketoconazole: a review of its therapeutic efficacy in superficial and systemic fungal infections.
    Drugs. 1982 Jan-Feb;23(1-2):1-36 PMID: 6276122
  9. Disposition of ketoconazole, an oral antifungal, in humans.
    Antimicrob Agents Chemother. 1982 Jan;21(1):151-8 PMID: 6282204
  10. Ketoconazole blocks adrenal steroid synthesis.
    Ann Intern Med. 1982 Sep;97(3):370-2 PMID: 6287893
  11. Primary site of action of ketoconazole on Candida albicans.
    Antimicrob Agents Chemother. 1982 Jun;21(6):912-8 PMID: 6287929
  12. Effect of ketoconazole on isolated mitochondria from Candida albicans.
    Antimicrob Agents Chemother. 1982 Jun;21(6):919-24 PMID: 6287930
  13. Ketoconazole blocks testosterone synthesis.
    Arch Intern Med. 1982 Nov;142(12):2137-40 PMID: 6291475
  14. Long-term therapy of chronic mucocutaneous candidiasis with ketoconazole: experience with twenty-one patients.
    Am J Med. 1983 Jan 24;74(1B):23-9 PMID: 6295149
  15. Laboratory and clinical assessment of ketoconazole in deep-seated mycoses.
    Am J Med. 1983 Jan 24;74(1B):30-47 PMID: 6295150
  16. Treatment of paracoccidioidomycosis with ketoconazole: a three-year experience.
    Am J Med. 1983 Jan 24;74(1B):48-52 PMID: 6295151
  17. Post-therapy status of paracoccidioidomycosis treated with ketoconazole.
    Am J Med. 1983 Jan 24;74(1B):53-7 PMID: 6295152
  18. Experience with ketoconazole in three major manifestations of progressive coccidioidomycosis.
    Am J Med. 1983 Jan 24;74(1B):58-63 PMID: 6295153
  19. Hepatic reactions during ketoconazole treatment.
    Am J Med. 1983 Jan 24;74(1B):80-5 PMID: 6129799
  20. Effect of imidazole antifungals on the development of germ tubes by strains of Candida albicans.
    J Antimicrob Chemother. 1983 Oct;12(4):303-16 PMID: 6315670
  21. Hypothesis on the molecular basis of the antifungal activity of N-substituted imidazoles and triazoles.
    Biochem Soc Trans. 1983 Dec;11(6):665-7 PMID: 6667774
  22. Influence of food on the pharmacokinetics of ketoconazole.
    Antimicrob Agents Chemother. 1984 Jan;25(1):1-3 PMID: 6322675
  23. In vitro studies with R 51,211 (itraconazole).
    Antimicrob Agents Chemother. 1984 Jul;26(1):5-9 PMID: 6089654
  24. High-dose ketoconazole therapy and adrenal and testicular function in humans.
    Arch Intern Med. 1984 Nov;144(11):2150-3 PMID: 6093722
  25. Antifungal relative inhibition factors: BAY l-9139, bifonazole, butoconazole, isoconazole, itraconazole (R 51211), oxiconazole, Ro 14-4767/002, sulconazole, terconazole and vibunazole (BAY n-7133) compared in vitro with nine established antifungal agents.
    J Antimicrob Chemother. 1984 Aug;14(2):105-14 PMID: 6094418
  26. Interaction of ketoconazole with rifampin and isoniazid.
    N Engl J Med. 1984 Dec 27;311(26):1681-3 PMID: 6095080
  27. Itraconazole, a new triazole that is orally active in aspergillosis.
    Antimicrob Agents Chemother. 1984 Oct;26(4):527-34 PMID: 6097167
  28. R 51211 (itraconazole) therapy of murine cryptococcosis.
    Sabouraudia. 1984;22(6):445-53 PMID: 6098031
  29. Reversible adrenal insufficiency induced by ketoconazole.
    JAMA. 1985 Apr 26;253(16):2413-4 PMID: 3981770
  30. Activity of UK-49,858, a bis-triazole derivative, against experimental infections with Candida albicans and Trichophyton mentagrophytes.
    Antimicrob Agents Chemother. 1985 May;27(5):832-5 PMID: 2990328
  31. Itraconazole treatment of murine aspergillosis.
    Sabouraudia. 1985 Jun;23(3):219-23 PMID: 2992106
  32. Penetration of imidazoles and triazoles into cerebrospinal fluid of rabbits.
    J Antimicrob Chemother. 1985 Jul;16(1):81-6 PMID: 2995303
  33. Treatment of blastomycosis and histoplasmosis with ketoconazole. Results of a prospective randomized clinical trial. National Institute of Allergy and Infectious Diseases Mycoses Study Group.
    Ann Intern Med. 1985 Dec;103(6 ( Pt 1)):861-72 PMID: 2865921
  34. Treatment of systemic mycoses with ketoconazole: in vitro susceptibilities of clinical isolates of systemic and pathogenic fungi to ketoconazole.
    J Infect Dis. 1985 Dec;152(6):1249-56 PMID: 3905985
  35. Efficacy of UK-49,858 (fluconazole) against Candida albicans experimental infections in mice.
    Antimicrob Agents Chemother. 1985 Dec;28(6):815-8 PMID: 3002246
  36. Pharmacokinetic evaluation of UK-49,858, a metabolically stable triazole antifungal drug, in animals and humans.
    Antimicrob Agents Chemother. 1985 Nov;28(5):648-53 PMID: 3004323
  37. Comparison of itraconazole and fluconazole in treatment of cryptococcal meningitis and candida pyelonephritis in rabbits.
    Antimicrob Agents Chemother. 1986 Apr;29(4):579-83 PMID: 3010846
  38. Comparison of the in vitro and in vivo activity of the bis-triazole derivative UK 49,858 with that of amphotericin B against Histoplasma capsulatum.
    Antimicrob Agents Chemother. 1986 Apr;29(4):660-2 PMID: 3010852
  39. Treatment of paracoccidioidomycosis with itraconazole in a murine model.
    J Trop Med Hyg. 1985 Oct;88(5):295-9 PMID: 3014164
  40. Comparative activities of UK-49,858 and amphotericin B against Blastomyces dermatitidis infections in mice.
    Antimicrob Agents Chemother. 1986 Jan;29(1):161-2 PMID: 3015001
  41. Treatment of cryptococcal meningitis in mice with fluconazole.
    J Antimicrob Chemother. 1986 Aug;18(2):261-70 PMID: 3019986
  42. Treatment of murine histoplasmosis with UK 49,858 (fluconazole).
    Am Rev Respir Dis. 1986 Oct;134(4):768-70 PMID: 3021035
  43. Activity of fluconazole (UK 49,858) and ketoconazole against Candida albicans in vitro and in vivo.
    Antimicrob Agents Chemother. 1986 Sep;30(3):418-22 PMID: 3022641
  44. Activity of orally, topically, and parenterally administered itraconazole in the treatment of superficial and deep mycoses: animal models.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S15-32 PMID: 3027843
  45. Evolution of antifungal agents: past, present, and future.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S4-14 PMID: 3544144
  46. Itraconazole: pharmacologic studies in animals and humans.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S43-6 PMID: 3027845
  47. Oral treatment of paracoccidioidomycosis and histoplasmosis with itraconazole in humans.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S47-50 PMID: 3027846
  48. Itraconazole in the treatment of paracoccidioidomycosis: a preliminary report.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S51-6 PMID: 3027847
  49. A clinical trial of itraconazole in the treatment of deep mycoses and leishmaniasis.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S57-63 PMID: 3027848
  50. Early experience with itraconazole in vitro and in patients: pharmacokinetic studies and clinical results.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S71-6 PMID: 3027850
  51. Initial experience in therapy for progressive mycoses with itraconazole, the first clinically studied triazole.
    Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S77-86 PMID: 3027851
  52. Efficacy of fluconazole (UK-49,858) against experimental aspergillosis and cryptococcosis in mice.
    J Antimicrob Chemother. 1987 May;19(5):663-70 PMID: 3038824
  53. Biochemical targets for antifungal azole derivatives: hypothesis on the mode of action.
    Curr Top Med Mycol. 1985;1:313-51 PMID: 3916772
  54. Cytochemical and biochemical studies of yeasts after in vitro exposure to miconazole.
    Antimicrob Agents Chemother. 1977 Mar;11(3):500-13 PMID: 193437
Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
Published
1988-01-00
Pages
1-8
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC172087
Subset
IM
Grants
PHS HHS · N01 A1 52562 · United States
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