Comparison of in vitro antifungal activities of topical antimycotics launched in 1990s in Japan

Nimura, Kazuhiro; Niwano, Yoshimi; Ishiduka, Seiji; Fukumoto, Ryoichi

doi:10.1016/s0924-8579(01)00365-x

Cited by 28 publications

(20 citation statements)

References 23 publications

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“…There is no report about the use of MVM medium in MIC determination for dermatophytic fungi. There is a scarcity of reports about the use of SDB for MIC determination for any fungi, including dermatophytes (17). We tested SDB medium because its cost is considerably lower than that of other tested media mentioned above and it is used in all mycology laboratories; however, SDB presented lower MICs and had high discrepancy compared to MVM and RPMI (P Ͻ 0.05).…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Broth Microdilution Antifungal Susceptibility Testing Conditions for Trichophyton rubrum

Santos

Hamdan

2005

J Clin Microbiol

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Fifty clinical isolates ofwere included as quality controls. All isolates produced clearly detectable growth only after 7 days of incubation. MICs were significantly independent of the incubation temperature (28 or 35°C) (P < 0.05). Different incubation periods resulted in MICs which were consistently different for each medium when azoles and griseofulvin were tested (P < 0.05). MICs obtained from different media at the same incubation time for the same isolate were significantly different when azoles and griseofulvin were tested (P < 0.05). MICs were consistently higher (usually 1 to 2 dilutions) with RPMI than with MVM or SDB (P < 0.05). When terbinafine was tested, no parameter had any influence on MICs (P < 0.05). RPMI standard medium appears to be a suitable testing medium for determining the MICs for T. rubrum. MICs obtained at different incubation times need to be correlated with clinical outcome to demonstrate which time has better reliability.

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Section: Discussionmentioning

confidence: 99%

Evaluation of Broth Microdilution Antifungal Susceptibility Testing Conditions for Trichophyton rubrum

Santos

Hamdan

2005

J Clin Microbiol

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“…However, two common dermatophytoses, tinea capitis and tinea unguium, do not respond well to such treatment and require the use of systemic antimycotics to be cured (2,8,23). Numerous topical agents and several systemic ones are available, but comparison of their in vitro activity against dermatophytes has been hampered by the lack of a well accepted MIC assay for these fungi (1,5,9,10,13,14,(18)(19)(20)25). Recently, several groups have adapted the proposed reference method for broth dilution antifungal susceptibility testing of conidium-forming filamentous fungi (17) for developing a more specific assay for dermatophytes (6).…”

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confidence: 99%

Comparison of In Vitro Activities of 17 Antifungal Drugs against a Panel of 20 Dermatophytes by Using a Microdilution Assay

et al. 2003

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The in vitro activities of 17 antifungal drugs against a panel of 20 dermatophytes comprising 6 different species were determined using a microdilution assay according to the NCCLS M38-P method with some modifications. Terbinafine was the most potent systemic drug while tolnaftate and amorolfine were the most active topical agents.Most superficial infections caused by dermatophytes can be rapidly eradicated with topical antifungals. However, two common dermatophytoses, tinea capitis and tinea unguium, do not respond well to such treatment and require the use of systemic antimycotics to be cured (2,8,23). Numerous topical agents and several systemic ones are available, but comparison of their in vitro activity against dermatophytes has been hampered by the lack of a well accepted MIC assay for these fungi (1,5,9,10,13,14,(18)(19)(20)25). Recently, several groups have adapted the proposed reference method for broth dilution antifungal susceptibility testing of conidium-forming filamentous fungi (17) for developing a more specific assay for dermatophytes (6). Since the preparation of conidia inoculum is sometimes a challenge with dermatophytes, a microdilution assay appears to be the ideal format (5,6,13,20). However, assay parameters, such as the temperature, duration, or growth inhibition endpoint, are still the subject of debate (11,12,21).The NCCLS guidelines are primarily aimed toward susceptibility testing of clinical isolates. The aim of the present study was to establish an NCCLS-compatible assay, which was optimized for our primary purpose of evaluating investigative antifungal agents.Twenty strains of dermatophytes, Trichophyton rubrum (n ϭ 5), Trichophyton tonsurans (n ϭ 5), Trichophyton mentagrophytes (n ϭ 4), Microsporum canis (n ϭ 4), Microsporum gypseum (n ϭ 1), and Epidermophyton floccosum (n ϭ 1), were employed. Five strains were obtained from either the fungal biodiversity center (Centralbureau voor Schimmelcultures RPMI 1640 medium (Invitrogen) with L-glutamine and without bicarbonate was buffered at pH 7.0 with 0.165 M morpholinepropanesulfonic acid (Sigma). Terbinafine, naftifine, butenafine, voriconazole, and itraconazole were synthesized at Novartis. Fluconazole was extracted and purified from Diflucan tablets (Pfizer). Miconazole, amorolfine, and tolciclate were obtained from Janssen, Roche, and Montedison, respectively. Clotrimazole, econazole, ketoconazole, ciclopiroxolamine, tolnaftate, griseofulvine, and undecylenic acid were purchased from Sigma, while tioconazole was bought from U.S. Pharmacopeia. All drugs were dissolved and twofold serially diluted in dimethyl sulfoxide (DMSO).All standard media were purchased from Merck. T. mentagrophytes, T. tonsurans, and E. floccosum were grown on Kimmig agar, T. rubrum was grown on potato dextrose agar, and M. canis and M. gypseum were grown on malt extract agar at 26°C for 2 to 3 weeks. Mycelium and spores were scraped from the plates and dispersed in a small volume of Sabouraud 2% dextrose broth (usually 20 ml for 25 plates) using a sterile gl...

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“…Ketoconazole (KTZ) was the first orally active azole introduced in clinical practice and has been an important and widely used drug. 2,3 KTZ is chiral and there are two stereogenic centers in the molecule. The drug is defined as the racemic mixture of the two cis enantiomers and their absolute configuration has been determined via synthesis by Rotstein et al 4 as (+)-(2R,4S) and ( -)-(2S,4R) (Fig.…”

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Enantioselectivity of inhibition of cytochrome P450 3A4 (CYP3A4) by ketoconazole: Testosterone and methadone as substrates

et al. 2003

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Racemic ketoconazole (KTZ) was the first orally active azole antifungal agent used in clinical practice and has become widely used in the treatment of mucosal fungal infections associated with AIDS immunosuppression and cancer chemotherapy. However, the use of KTZ has been limited because of adverse drug-drug interactions. KTZ blocks ergosterol biosynthesis by inhibiting the fungal cytochrome P450 (CYP51). KTZ is also a potent inhibitor of human cytochrome P450 3A4 (CYP3A4) enzyme, the major drug-metabolizing CYP isozyme in the human liver. We examined the enantioselective differences of KTZ in the inhibition of human CYP3A4 and in antifungal action. Dextro- and levo-KTZ exhibited modest enantioselective differences with respect to CYP3A4 inhibition of testosterone and methadone metabolism. For both substrates levo-KTZ was approximately a 2-fold more potent inhibitor. We examined the enantioselective differences in the in vitro activity of KTZ against medically relevant species of Candida and Aspergillus, as well as Cryptococcus neoformans. Overall, levo-KTZ was 2-4-fold more active than dextro-KTZ. Therefore, levo-KTZ is a more potent inhibitor of CYP3A4 and has stronger in vitro antifungal activity. Chirality 16:79-85, 2004.

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Comparison of in vitro antifungal activities of topical antimycotics launched in 1990s in Japan

Cited by 28 publications

References 23 publications

Evaluation of Broth Microdilution Antifungal Susceptibility Testing Conditions for Trichophyton rubrum

Evaluation of Broth Microdilution Antifungal Susceptibility Testing Conditions for Trichophyton rubrum

Comparison of In Vitro Activities of 17 Antifungal Drugs against a Panel of 20 Dermatophytes by Using a Microdilution Assay

Enantioselectivity of inhibition of cytochrome P450 3A4 (CYP3A4) by ketoconazole: Testosterone and methadone as substrates

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