Treatment of vaginal candidiasis with ketoconazole, a new, orally active, antimycotic

Bisschop, M.P.J.M.; Merkus, J.M.W.M.; Scheygrond, H.; Cutsem, J. Van; Kuy, A. van de

doi:10.1016/0028-2243(79)90065-0

Cited by 48 publications

(13 citation statements)

References 10 publications

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“…6 In animal models, fluconazole has been shown to be more potent than ketoconazole against Candida infections. [7][8][9] Clotrimazole, which is effective against dermatophyte and other fungal infections, 10 …”

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Comparative Study of the Effectiveness of Oral Fluconazole and Intravaginal Clotrimazole in theTreatment of Vaginal Candidiasis

Mikamo

Izumi

Ito

et al. 1995

Infectious Diseases in Obstetrics and Gynecology

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Objective: A study was carried out to compare 3 treatment regimens for vaginal candidiasis.Methods: A total of 150 women with clinical and mycological evidence of vaginal candidiasis were randomized to receive 50 mg of oral fluconazole daily for 6 days (50 women), a single oral 150 mg dose of fluconazole (50 women), or 100 mg ofintravaginal clotrimazole daily for 6 days (50 women).They were assessed at 5-15 days (short-term assessment) and again at 30-60 days (long-term assessment) after the completion of treatment.Results: Candida species were completely eradicated from the vagina in 88% or 80% in the 6-day

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confidence: 99%

Comparative Study of the Effectiveness of Oral Fluconazole and Intravaginal Clotrimazole in theTreatment of Vaginal Candidiasis

Mikamo

Izumi

Ito

et al. 1995

Infectious Diseases in Obstetrics and Gynecology

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“…The imidazole derivatives miconazole, clotrimazole, and econazole administered topically and oral ketoconazole are highly effective in the treatment of vulvovaginal candidiasis (1,2). Itraconazole (R51,211) is a new oral imidazole ( Fig.…”

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Comparison of itraconazole and ketoconazole in the treatment of experimental candidal vaginitis

Jd¹,

Muller²

1984

Antimicrob Agents Chemother

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Comparison of itraconazole (R51,211) and ketoconazole in the treatment of experimental candidal vaginitis in rats on schedules of 3 and 5 days revealed significantly superior results with itraconazole at all dosages (1.0 to 7.5 mg/kg) studied, but was particularly evident at 1.0 and 2.5 mg/kg. A single 25-mg/kg dose of itraconazole was as effective as 5 daily 5-mg/kg doses of itraconazole.The imidazole derivatives miconazole, clotrimazole, and econazole administered topically and oral ketoconazole are highly effective in the treatment of vulvovaginal candidiasis (1, 2). Itraconazole (R51,211) is a new oral imidazole ( Fig. 1) which, like ketoconazole, is thought to inhibit cell membrane ergosterol synthesis. Preliminary in vitro data suggest that this agent has considerably more activity against Candida albicans in addition to a broader spectrum of activity, which includes Aspergillus sp. (J. Van Cutsem, F. Van Gerven, R. Zamon, J. Heeres, and P. A. J. Janssen, Proc. Int. Congr. Chemother. 13th, Vienna, Austria, p. 40/32-40/39, 1983). This report relates the results of a comparison of the activities of itraconazole and ketoconazole against 58 clinical isolates of C. albicans in vitro and against experimental vaginal infections with this fungus in rats.MICs of ketoconazole and itraconazole against 58 clinical vaginal isolates of C. albicans obtained from women with candida vaginitis were measured by agar dilution with an inoculum of 5 x 104 organisms as previously described (3). All isolates were maintained on agar slants at 4°C. The 50% MICs for itraconazole and ketoconazole were 0.16 and 0.2 pg/ml, respectively, and the 90% MICs for itraconazole and ketoconazole were 2.0 and 4.8 ,ug/ml, respectively.Pseudoestrous was induced in 170 oophorectomized female Sprague-Dawley rats (175 to 200 g) by subcutaneous injection of estradiol valerate in sesame oil (0.5 mg/0.1 ml) (E. R. Squibb & Sons, Princeton, N.J.) and was maintained by similar weekly injections. At 48 h after the initial estrogen injection, rats were inoculated vaginally with 104 C. albicans GMO2 blastospores (MICs of ketoconazole and itraconazole were each 0.2 ,ug/ml) suspended in 0.1 ml of sterile phosphate-buffered saline, pH 7.2. C. albicans cells used for infection were obtained by inoculating 10 ml of sterile 1% phytone-peptone glucose broth with 100 RI of a stock blastospore suspension and then incubating the preparation for 22 h at 26°C in a shaking water bath. The resulting culture suspension was centrifuged for 10 min at 2,000 rpm at 4°C and resuspended in 1 to 2 ml of sterile phosphate-buffered saline. The number of blastospores in this suspension was counted in a hemacytometer. Thereafter, the yeast suspension was administered (0.1 ml per animal) via a short segment of butterfly tubing (1.5 in. or ca. 3.8 cm) affixed to a 1-ml tuberculin syringe. * Corresponding author.Treatment with ketoconazole or itraconazole (Janssen Pharmaceutica, Piscataway, N.J.) at dosages of 1.0, 2.5, 5.0, and 7.5 mg/kg, administered by daily gavage for either 3 or 5...

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“…dichlorophenyl)-2-( lH-imidazol-1-ylmethyl) -1, 3-dioxalan-4-yl]methoxy]phenyl} piperazine) orally active agent with broad-spectrum activity against a variety of yeasts, dermatophytes, and dimorphous fungi (1,4,11,13,14).…”

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In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis

Bossche¹,

Willemsens²,

Cools³

et al. 1980

Antimicrob Agents Chemother

263

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Ketoconazole, an orally active antimycotic drug, is a potent inhibitor of ergosterol biosynthesis in Candida albicans when added to culture media which support yeast or mycelial growth or to cultures containing outgrown mycelium. This inhibition coincides with accumulation of sterols with a methyl group at C-14 and can thus be attributed to an interference with one of the reactions involved in the removal of the 14 alpha-methyl group of lanosterol. When administered to rats infected with C. albicans, ketocanazole also inhibits fungal synthesis of ergosterol. A six-times-higher dose is required to effect cholesterol synthesis by rat liver.

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Treatment of vaginal candidiasis with ketoconazole, a new, orally active, antimycotic

Cited by 48 publications

References 10 publications

Comparative Study of the Effectiveness of Oral Fluconazole and Intravaginal Clotrimazole in theTreatment of Vaginal Candidiasis

Comparative Study of the Effectiveness of Oral Fluconazole and Intravaginal Clotrimazole in theTreatment of Vaginal Candidiasis

Comparison of itraconazole and ketoconazole in the treatment of experimental candidal vaginitis

In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis

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