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Ketoconazole

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4981. Enhancement of ketoconazole penetration across the blood-brain barrier of mice by dimethyl sulfoxide. (PubMed)

Enhancement of ketoconazole penetration across the blood-brain barrier of mice by dimethyl sulfoxide. Mice were treated with ketoconazole with and without dimethyl sulfoxide. Concentrations of ketoconazole at 3 and 5 h after treatment were significantly higher in serum (P less than 0.05) and brain tissue homogenate (P less than 0.01) of mice treated with dimethyl sulfoxide than in those of mice not treated with dimethyl sulfoxide.

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1986 Antimicrobial Agents and Chemotherapy

4982. Ketoconazole blocks bile acid synthesis in hepatocyte monolayer cultures and in vivo in rat by inhibiting cholesterol 7 alpha-hydroxylase. (PubMed)

Ketoconazole blocks bile acid synthesis in hepatocyte monolayer cultures and in vivo in rat by inhibiting cholesterol 7 alpha-hydroxylase. In cultured hepatocytes conversion of [4-14C]cholesterol into bile acids was dose dependently reduced by the antimycotic drug ketoconazole, giving half-maximal inhibition at 10 microM ketoconazole in rat hepatocytes and at 1 microM in human hepatocytes. No change was observed in the ratio of produced cholic, beta-muricholic, and chenodeoxycholic acid (...) with increasing amounts of the drug. Conversion of [4-14C]7 alpha-hydroxycholesterol, an intermediate of bile acid pathway, to bile acids was not affected by ketoconazole. These results together with kinetic studies with rat liver microsomes, demonstrating noncompetitive inhibition (Ki = 0.4 microM), indicate that cholesterol 7 alpha-hydroxylase is the main site of inhibition. In bile-diverted rats a single dose of ketoconazole (50 mg/kg) dramatically impaired bile flow and biliary bile acid output (92

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1986 Journal of Clinical Investigation

4983. In vitro activity of ketoconazole against herpes simplex virus. (PubMed)

In vitro activity of ketoconazole against herpes simplex virus. The effects of ketoconazole alone and in combination with acyclovir and adenine arabinoside upon the replication of herpes simplex virus types 1 and 2 (HSV-1 and -2) were investigated by using a yield reduction assay. Ketoconazole demonstrated antiviral activity against HSV-1 and -2 and synergistic antiviral activity when it was combined with acyclovir. Combinations of ketoconazole with adenine arabinoside resulted in either (...) interference or indifference. The effects of ketoconazole upon the protein synthesis of HSV-2-infected cells were also determined in an effort to define the mechanism of action for the antiviral activity of ketoconazole. There was no reduction of HSV proteins when compared with acyclovir. These findings suggest that further investigations of the use of ketoconazole for the treatment of HSV infections are warranted.

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1986 Antimicrobial Agents and Chemotherapy

4984. Pharmacokinetics and dose proportionality of ketoconazole in normal volunteers. (PubMed)

Pharmacokinetics and dose proportionality of ketoconazole in normal volunteers. Ketoconazole is an orally effective, broad-spectrum, systemic antifungal agent. The pharmacokinetics and bioavailability of ketoconazole given as a 200-mg single dose in a tablet, suspension, or solution were studied in 24 fasting healthy males by using a crossover design. Levels of ketoconazole in plasma were determined for up to 48 h by a sensitive reverse-phase high-performance liquid chromatography method (...) . The absorption of ketoconazole was rapid, with mean maximum concentrations of the drug in plasma of 4.2, 5.0, and 6.2 micrograms/ml attained at 1.7, 1.2, and 1.0 h, respectively, after administration of the tablet, suspension, and solution, respectively. The mean distribution and elimination half-life values were 1.5 to 1.7 and 7.5 to 7.9 h, respectively. The mean oral clearance of the solution dose was 209 (+/- 82.9 [standard deviation]) ml/min, and the mean apparent volume of distribution was 88.31

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1986 Antimicrobial Agents and Chemotherapy

4985. Broth dilution testing of Candida albicans susceptibility to ketoconazole. (PubMed)

Broth dilution testing of Candida albicans susceptibility to ketoconazole. We performed a detailed investigation of the kinetics of ketoconazole activity in the setting of broth dilution testing of Candida albicans susceptibility. Turbidimetric readings reflected parallel quantitative colony counts. The method of endpoint determination markedly affected the results. Determinations of 50% inhibitory concentrations clearly separated the ketoconazole-resistant strains from the susceptible strains.

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1987 Antimicrobial Agents and Chemotherapy

4986. Ketoconazole Use in Tinea Versicolor (PubMed)

Ketoconazole Use in Tinea Versicolor 18750333 2010 06 30 2018 11 13 0093-0415 147 4 1987 Oct The Western journal of medicine West. J. Med. Ketoconazole use in tinea versicolor. 457 Jacobs P H PH eng Journal Article United States West J Med 0410504 0093-0415 1987 10 1 0 0 1987 10 1 0 1 1987 10 1 0 0 ppublish 18750333 PMC1025909 Cutis. 1984 Nov;34(5):470-1 6094116 Int J Dermatol. 1982 Jan-Feb;21(1):8-11 7061193

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1987 Western Journal of Medicine

4987. Activity of ICI 195,739, a new oral triazole, compared with that of ketoconazole in the therapy of experimental murine blastomycosis. (PubMed)

Activity of ICI 195,739, a new oral triazole, compared with that of ketoconazole in the therapy of experimental murine blastomycosis. ICI 195,739, a novel orally active triazole, proved 50 times as potent as ketoconazole, produced a clinical cure, and completely eradicated residual infection in a murine model of pulmonary blastomycosis. No other previously tested azole has shown similar activity. Fungicidal activity against Blastomyces dermatitidis was seen in vitro at concentrations 1/40

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1989 Antimicrobial Agents and Chemotherapy

4988. Preoperative ketoconazole therapy for adrenocortical carcinoma. (PubMed)

Preoperative ketoconazole therapy for adrenocortical carcinoma. 2743227 1989 08 11 2018 11 13 0820-3946 141 2 1989 Jul 15 CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne CMAJ Preoperative ketoconazole therapy for adrenocortical carcinoma. 131-3 Sinnaeve L J LJ Department of Medicine, St. Joseph's Health Centre, Western Ontario, London. Becks G P GP eng Case Reports Journal Article Canada CMAJ 9711805 0820-3946 R9400W927I Ketoconazole AIM IM Adrenal (...) Cortex Neoplasms drug therapy surgery Carcinoma drug therapy surgery Combined Modality Therapy Drug Evaluation Female Humans Ketoconazole therapeutic use Middle Aged Neoplasm Recurrence, Local drug therapy Premedication 1989 7 15 1989 7 15 0 1 1989 7 15 0 0 ppublish 2743227 PMC1269337 JAMA. 1985 Apr 26;253(16):2413-4 3981770 Arch Intern Med. 1985 May;145(5):863-4 2986567 Lancet. 1985 Jul 20;2(8447):151-2 2410748 J Clin Endocrinol Metab. 1986 Sep;63(3):766-9 3755445 J Steroid Biochem. 1986 Jan;24(1

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1989 CMAJ: Canadian Medical Association Journal

4989. A randomized, phase II trial of ketoconazole plus alendronate versus ketoconazole alone in patients with androgen independent prostate cancer and bone metastases. (PubMed)

A randomized, phase II trial of ketoconazole plus alendronate versus ketoconazole alone in patients with androgen independent prostate cancer and bone metastases. Alendronate (AL), a potent oral bisphosphonate, blocks the secretion of matrix metalloproteinase-2 and the establishment of bone metastases in animal models. Ketoconazole (KT) has demonstrated activity in androgen independent prostate cancer (AIPC). In this study we determined whether KT plus AL produced acceptable disease responses

2005 The Journal of urology

4990. Response to low-dose ketoconazole and subsequent dose escalation to high-dose ketoconazole in patients with androgen-independent prostate cancer. (PubMed)

Response to low-dose ketoconazole and subsequent dose escalation to high-dose ketoconazole in patients with androgen-independent prostate cancer. High-dose ketoconazole (HDK) in combination with steroids has been recognized as an effective secondary hormonal therapy in androgen-independent prostate cancer (AIPC). However, HDK causes more severe adverse events than low-dose ketoconazole (LDK). To the authors' knowledge, relatively little is known regarding the efficacy of LDK in AIPC

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2006 Cancer

4991. Comparison of itraconazole and ketoconazole in HIV-positive patients with oropharyngeal or esophageal candidiasis. Human Immunodeficiency Virus Itraconazole Ketoconazole Project Group. (PubMed)

Comparison of itraconazole and ketoconazole in HIV-positive patients with oropharyngeal or esophageal candidiasis. Human Immunodeficiency Virus Itraconazole Ketoconazole Project Group. The efficacy of oral itraconazole and ketoconazole in the treatment of oropharyngeal and/or esophageal candidiasis, and the rate of post-treatment relapse, were compared in a multicenter, prospective, double-blind, double-dummy, randomized, parallel-group trial. A total of 143 adult HIV-positive patients (...) with oropharyngeal and/or esophageal candidiasis were assigned to receive either itraconazole or ketoconazole (200 mg/day). Patients with oropharyngeal and esophageal candidiasis were treated for 2 and 4 weeks, respectively. Patients were evaluated clinically and mycologically after 1, 2 and 4 (for esophageal patients) weeks of therapy, and relapses were compared in a 6-week post-treatment follow-up period. Of 129 evaluable patients, 98 had oropharyngeal candidiasis and 31 esophageal infection. CDC

1997 Chemotherapy

4992. Treatment of seborrhoeic dermatitis with ketoconazole: I. Response of seborrhoeic dermatitis of the scalp to topical ketoconazole. (PubMed)

Treatment of seborrhoeic dermatitis with ketoconazole: I. Response of seborrhoeic dermatitis of the scalp to topical ketoconazole. A randomized, double-blind, placebo-controlled cross-over study was made of ketoconazole shampoo in the treatment of 20 subjects with seborrhoeic dermatitis of the scalp. Responses were measured by clinicians using clinical gradings, and by the patients using a linear analogue scale. Scaling and itching of the scalp improved significantly with ketoconazole (...) and no response was seen with placebo. Topical ketoconazole appears to be an effective therapy for seborrhoeic dermatitis of the scalp, and more suitable for long-term treatment than the oral preparation.

1987 The British journal of dermatology

4993. Treatment of seborrhoeic dermatitis with ketoconazole: II. Response of seborrhoeic dermatitis of the face, scalp and trunk to topical ketoconazole. (PubMed)

Treatment of seborrhoeic dermatitis with ketoconazole: II. Response of seborrhoeic dermatitis of the face, scalp and trunk to topical ketoconazole. A randomized, double-blind, placebo-controlled study was made of 2% ketoconazole cream and shampoo in 20 patients with seborrhoeic dermatitis of the face. Sixteen also had seborrhoeic dermatitis of the scalp and five had seborrhoeic dermatitis of the chest or back. Responses were measured by clinicians and patients independently using a grading (...) system and linear analogue scales, respectively. Face and scalp lesions, assessed by both patient and clinician, showed a significant improvement or complete clearance in the group treated with ketoconazole. The patients who had seborrhoeic dermatitis of the chest or back and were treated with ketoconazole also improved. There was no improvement with placebo. This study provides further evidence for the aetiological role of pityrosporon yeasts in seborrhoeic dermatitis and of the efficacy of topical

1987 The British journal of dermatology

4994. Randomized phase 2 trial of ketoconazole and ketoconazole/doxorubicin in androgen independent prostate cancer. (PubMed)

Randomized phase 2 trial of ketoconazole and ketoconazole/doxorubicin in androgen independent prostate cancer. Eighty-nine patients with progressive prostate cancer despite suppression of testosterone and withdrawal of anti-androgens were studied. This was a relatively advanced population, with 63 of 89 having either osseous metastases (mets) beyond the axial skeleton or visceral mets. Patients were randomly assigned to receive either ketoconazole alone, or ketoconazole with weekly doxorubicin (...) . All patients received replacement hydrocortisone. The primary endpoints were response and survival. Based on PSA reduction criteria (>/= 80% maintained for at least 8 weeks), 14 of 45 patients (31%) in the single-agent ketoconazole arm responded. Sixteen of 44 patients (36%) in the combination ketoconazole/doxorubicin arm responded. There were no important differences between the two treatments in any outcome measure. The median overall survival for all patients was 12.5 months; median time

2001 Urologic oncology

4995. Activities of fluconazole (UK 49,858) and ketoconazole against ketoconazole-susceptible and -resistant Candida albicans. (PubMed)

Activities of fluconazole (UK 49,858) and ketoconazole against ketoconazole-susceptible and -resistant Candida albicans. We have compared the activities of fluconazole and ketoconazole against ketoconazole-susceptible and -resistant strains of Candida albicans in a neutropenic-site rabbit model. Oral treatment with fluconazole resulted in much higher serum and extravascular concentrations of this antifungal agent than did comparable doses of ketoconazole. Fluconazole had no additional in vivo (...) activity against the ketoconazole-susceptible strains; no fungicidal activity was observed with peak drug levels as high as approximately 75 micrograms/ml in the infection sites. Significant fungistatic activity against the ketoconazole-resistant strains was observed with fluconazole treatment (80 mg/kg), but not with less fluconazole (20 mg/kg) or with ketoconazole (approximately 67 mg/kg). In vitro susceptibility tests separated the ketoconazole-susceptible strains from the ketoconazole-resistant

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1988 Antimicrobial Agents and Chemotherapy

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