Nizoral
In vitro susceptibility of 245 yeast isolates to amphotericin B, 5-fluorocytosine, ketoconazole, fluconazole and itraconazole.

Martin E, Parras P, Lozano MC.

Microbiology Laboratory, Valme University Hospital, Seville, Spain.

The in vitro activity of amphotericin B, 5-fluorocytosine, ketoconazole, fluconazole and itraconazole was tested against 245 yeast strains isolated from clinical specimens (68 Candida albicans, 74 Candida tropicalis, 43 Candida krusei, 28 Candida glabrata, 19 Candida parapsilosis, 8 Candida lusitaniae and 5 Candida guilliermondii). An agar dilution method was employed to carry out testing. Minimal inhibitory concentrations to restrain 90% of isolate growth (MIC90) ranged from 0.12 to 2 mg/l for amphotericin B and for 5-fluorocytosine, from 0.03 to 8 mg/l for ketoconazole, from 0.05 to 50 mg/l for itraconazole and from 0.1 to > 100 mg/l for fluconazole. Among the azole derivatives, the most active was ketoconazole, followed by itraconazole. Only 1 strain of C. albicans was resistant to amphotericin B (MIC > 4 mg/l). Both C. tropicalis and C. krusei responded poorly to fluconazole and the former to itraconazole as well. The species most susceptible to the antifungal agents tested was C. glabrata and the most resistant were C. tropicalis and C. krusei.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1337508&dopt=Abstract ketoconazole Nizoral



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Susceptibility to ketoconazole of Candida albicans strains from sequentially followed HIV-1 patients with recurrent oral candidosis.

Bruatto M, Marinuzzi G, Raiteri R, Sinicco A.

Istituto di Malattie Infettive dell'Universita di Torino, Italy.

The MIC values of the antifungal drug ketoconazole were evaluated on 66 Candida albicans strains. These strains were isolated from 26 HIV-1 infected patients with oral recurrent candidosis. Each episode of oral candidosis observed in these patients was orally treated with ketoconazole (200 mg/day) until the clinical disappearance of the lesions. The most frequent MIC values were 20 micrograms/ml and 10 micrograms/ml, observed in 37 and 19 isolates respectively. Only strains from five patients showed changes in their susceptibility to ketoconazole. This fact could indicate that a different strain causes the subsequent reappearance of the oral lesions, rather than the drug selecting resistant fungal strains. Our results stress the role of host characteristics in the occurrence of candidal infections, pointing to the progressing failure of the immunological response as the most important factor responsible for the recurrence of oral candidosis during HIV-1 infection.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1406790&dopt=Abstract ketoconazole Nizoral



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Cyclosporine and low-dose ketoconazole in renal transplant recipients: a single-center experience.

Carbajal H, Soltero L, Rodriguez-Montalvo C, Valdes A.

Escuela de Medicina, Ignacio A. Santos del Instituto Tecnologicoy de Estudios Superiores de Monterrey and the State of Nuevo Leon Organ and Tissue Transplant Registry, Monterrey, Mexico. hcarba intercable.net

BACKGROUND: The high cost of cyclosporine A (CsA) is an impediment for low-income patients. Previous studies have used ketoconazole at doses between 200 and 400 mg/day to lower CsA consumption. METHODS: Ketoconazole and CsA were administered prospectively to renal transplant patients. Patients treated historically with CsA were used as a reference group. At different intervals posttransplant, clinical and laboratory data were recorded. RESULTS: The reference group (n=14) was treated with CsA from 1992 to 1997 and the CsA plus ketoconazole group (n=17) from 1998 to 2002. Follow-up was 76+/-22 and 29+/-14 months, respectively. CsA doses throughout the study were 4.0+/-1.3 and 1.6+/-0.6 mg/kg/day (a 60% reduction, P =0.00). Trough levels of CsA were 194+/-87 and 193+/-69 ng/mL, respectively. The ketoconazole dose was 54+/-17 mg/day. The monthly cost of CsA was reduced by 60%, including the cost of ketoconazole. CONCLUSIONS: CsA with ketoconazole resulted in a substantial dose and cost reduction that proved safe and effective.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15087768&dopt=Abstract ketoconazole Nizoral



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Ketoconazole for treatment of dermatophytosis in cats.

Medleau L, Chalmers SA.

Department of Small Animal Medicine, College of Veterinary Medicine, University of Georgia, Athens 30602.

Twelve cats with generalized dermatophytosis were treated with ketoconazole (10 mg/kg of body weight, PO, with food, q 24 h). This treatment was successful in 8 cats, with resolution of lesions and negative findings on mycologic evaluation after 2 to 10 weeks (median duration, 6 weeks). One additional cat failed to improve initially, but complete resolution was achieved after the dosage of ketoconazole was doubled. Adverse effects in 3 cats included anorexia, weight loss, vomiting, and diarrhea.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1537696&dopt=Abstract ketoconazole Nizoral



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Essential oil compounds from Agastache rugosa as antifungal agents against Trichophyton species.

Shin S.

College of Pharmacy, Duksung Women's University, Seoul 132-714, Korea. swshin duksung.ac.kr

The antifungal activities of the essential oil from Agastache rugosa and its main component, estragole, combined with ketoconazole, one of the azole antibiotics commonly used to treat infections caused by Trichophyton species, were evaluated in this study. The combined effects were measured by the checkerboard microtiter and the disk diffusion tests, against T. erinacei, T. mentagrophytes, T. rubrum, T. schoenleinii and T. soudanense. Susceptibility of the five Trichophyton species to the oil alone, or ketoconazole alone, differed distinctly. The fractional inhibitory concentration indices (FICI) of ketoconazole combined with estragole or A. rugosa essential oil, against the tested Trichophyton species, were between 0.05 and 0.27, indicating synergistic effects. These drug combinations exhibited the most significant synergism against T. mentagrophytes, with FICIs of 0.05 and 0.09 for estragole and the essential oil fraction from A. rugosa, respectively. Isobolograms based on the data from checkerboard titer tests also indicated significant synergism between ketoconazole and the Agastache oil fraction or estragole, against the Trichophyton species evaluated. Trichophyton susceptibility to ketoconazole was significantly improved by combination with the Agastache rugosa oil fraction or its main component, estragole.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15089034&dopt=Abstract ketoconazole Nizoral



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Comparison of SCH 39304, fluconazole, and ketoconazole for treatment of systemic infections in mice.

Cacciapuoti A, Loebenberg D, Parmegiani R, Antonacci B, Norris C, Moss EL Jr, Menzel F Jr, Yarosh-Tomaine T, Hare RS, Miller GH.

Schering-Plough Research, Bloomfield, New Jersey 07003.

SCH 39304 was compared with fluconazole and ketoconazole in a systemic Candida albicans infection in mice (10(6) CFU per mouse). Results were based on survival rates and CFU in kidneys following once-daily oral treatment of 2, 5, or 10 days duration. In normal mice, SCH 39304 (dose to reduce kidney counts by 4 log units, 0.5 mg/kg of body weight) was 3 and 200 times more active than fluconazole and ketoconazole, respectively. In immunocompromised mice (gamma irradiation, 600 rads), SCH 39304 (dose to reduce kidney counts by 4 log units, 1.3 mg/kg) was 35 and greater than 100 times more active than fluconazole and ketoconazole, respectively. In normal mice, when the infecting inoculum varied from 10(5) to 10(7) CFU, only a fivefold increase in the dose to reduce kidney counts by 4 log units was observed with SCH 39304. Excellent protection was also seen when mice were treated with a single oral dose of SCH 39304 up to 24 h prior to infection with C. albicans. Studies in a systemic C. albicans infection model indicated that SCH 39304 is equally efficacious following either oral or intravenous administration. In a systemic Aspergillus flavus infection, mice treated with SCH 39304 (5 mg/kg) survived twice as long (16 days) as those treated with fluconazole (50 mg/kg) or controls did.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1590702&dopt=Abstract ketoconazole Nizoral



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Evaluation of topical ketoconazole in cutaneous leishmaniasis.

Abahusein A, Larbi EB, al-Khawajah A, al-Gindan Y, Jain S.

Department of Dermatology, King Faisal University College of Medicine.

The efficacy of topical ketoconazole in cutaneous leishmaniasis (CL) caused by L. major was assessed in an open trial. Ten patients with twenty two lesions of CL, confirmed by smear/or biopsy, were recruited into the study. Of the twenty two lesions treated, three increased in size and lesion characteristics worsened, ten showed no change but in nine there was some improvement in lesion characteristics. No lesion healed completely. No side effects were reported in nine. Topically applied ketoconazole is safe but does not significantly alter the course of CL. The differences in the results of systematically administered and topically applied ketoconazole may be due to differences in the pharmacokinetics of the drug when it is administered by different routes.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1628541&dopt=Abstract ketoconazole Nizoral