Local Tolerance of a New Ciclopirox Olamine Vaginal Preparation in Rats and Rabbits

Manzardo, S; Pinzetta, A.; Coppi, G

doi:10.1080/1120009x.1993.11739250

Cited by 3 publications

(1 citation statement)

References 6 publications

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“…Its use in treating vaginal candidiasis has also been studied, with limited success (9,17,21), and it has shown clinical promise against azole-resistant Candida species, including C. glabrata. It has demonstrated good topical and systemic tolerance in rats and rabbits when vaginal tissue was examined (5,15) and has been studied in settings with a lower pH (9,10). However, in this study, a 4-fold rise in MIC 90 from 0.5 to 2 g/ml with a decrease in pH was seen.…”

Section: Discussionmentioning

confidence: 99%

Effect of pH on In Vitro Susceptibility of Candida glabrata and Candida albicans to 11 Antifungal Agents and Implications for Clinical Use

Danby

Boikov

Rautemaa‐Richardson

et al. 2012

Antimicrob Agents Chemother

100

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The treatment of vulvovaginal candidiasis (VVC) due to Candida glabrata is challenging, with limited therapeutic options. Unexplained disappointing clinical efficacy has been reported with systemic and topical azole antifungal agents in spite of in vitro susceptibility. Given that the vaginal pH of patients with VVC is unchanged at 4 to 4.5, we studied the effect of pH on the in vitro activity of 11 antifungal agents against 40 C. glabrata isolates and compared activity against 15 fluconazole-sensitive and 10 reduced-fluconazole-susceptibility C. albicans strains. In vitro susceptibility to flucytosine, fluconazole, voriconazole, posaconazole, itraconazole, ketoconazole, clotrimazole, miconazole, ciclopirox olamine, amphotericin B, and caspofungin was determined using the CLSI method for yeast susceptibility testing. Test media were buffered to pHs of 7, 6, 5, and 4. Under conditions of reduced pH, C. glabrata isolates remained susceptible to caspofungin and flucytosine; however, there was a dramatic increase in the MIC 90 for amphotericin B and every azole drug tested. Although susceptible to other azole drugs tested at pH 7, C. albicans strains with reduced fluconazole susceptibility also demonstrated reduced susceptibility to amphotericin B and all azoles at pH 4. In contrast, fluconazole-sensitive C. albicans isolates remained susceptible at low pH to azoles, in keeping with clinical observations. In selecting agents for treatment of recurrent C. glabrata vaginitis, clinicians should recognize the limitations of in vitro susceptibility testing utilizing pH 7.0.

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Section: Discussionmentioning

confidence: 99%

Effect of pH on In Vitro Susceptibility of Candida glabrata and Candida albicans to 11 Antifungal Agents and Implications for Clinical Use

Danby

Boikov

Rautemaa‐Richardson

et al. 2012

Antimicrob Agents Chemother

100

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Pharmacokinetics of Ciclopirox Olamine after Vaginal Application to Rabbits and Patients

Coppi

Silingardi

Girardello

et al. 1993

Journal of Chemotherapy

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The authors reported the plasma levels and pharmacokinetic parameters of ciclopirox olamine in rabbits after i.v. and intravaginal administrations and in female patients after vaginal administration. Plasma levels of total and free ciclopirox were determined by a HPLC method. In rabbit ciclopirox showed a half-life of 2.22 h and an intravaginal bioavailability of about 2%. In female patients ciclopirox showed low intravaginal absorption; this value might explain the good local and systemic tolerability and also the penetration of drug in deep tissue.

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The hydroxypyridones: a class of antimycotics of its own

Körting

Grundmann-Kollmann

1997

Mycoses

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The hydroxypyridones chemically form a class of antimycotics not related to others. For a long time ciclopirox olamine has been the only compound to be used clinically. Recently, ciclopirox as a free acid and rilopirox have also been considered. The congeners are active against a broad spectrum of medically relevant fungi including dermatophytes, yeasts and moulds in vitro. According to investigations based on animal and in vivo models for fungal disease, this also applies in vivo. Low toxicity in the experimental animal has made topical applications in man possible. Clinical experience relates, in particular, to dermatophytosis and vaginal candidosis, but rarer conditions have also been investigated. High tolerability corresponds to efficacy in major dermatomycological conditions. Today, interest mainly focuses on ciclopirox lacquer for onychomycosis. Here as in general, the relative role of hydroxypyridones will have to be finally established in comparative trials.

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Local Tolerance of a New Ciclopirox Olamine Vaginal Preparation in Rats and Rabbits

Cited by 3 publications

References 6 publications

Effect of pH on In Vitro Susceptibility of Candida glabrata and Candida albicans to 11 Antifungal Agents and Implications for Clinical Use

Effect of pH on In Vitro Susceptibility of Candida glabrata and Candida albicans to 11 Antifungal Agents and Implications for Clinical Use

Pharmacokinetics of Ciclopirox Olamine after Vaginal Application to Rabbits and Patients

The hydroxypyridones: a class of antimycotics of its own

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