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Thirty-seven women with no tumoral hyperandrogenism treated with ketoconazole for 9 months (400 mg/day) were studied during treatment and one month after suppression of the medication. The study included the evaluation of total cholesterol, HDL cholesterol, triglycerides, LDL cholesterol and hormonal determinations of estradiol, androstenedione, testosterone, dehydroepiandrosterone, sulphate and sex hormone binding globulin.
Many prostate cancer patients with rising prostate-specific antigen (PSA) levels following radical prostatectomy or radiotherapy receive "early" hormonal therapy, despite its uncertain benefit. When these patients ultimately progress to androgen independence, their management remains controversial, with many receiving second-line hormonal therapy. Chemotherapy for the treatment of advanced prostate cancer has a defined palliative benefit; studies to establish its potential impact on survival are ongoing. E-1899 is an intergroup phase III trial comparing second-line hormonal therapy with ketoconazole plus hydrocortisone with docetaxel plus estramustine in patients with androgen-independent prostate cancer with rising PSA levels who have no evidence of metastases.
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The findings of this study reveal that mitragynine might inhibit cytochrome P450 enzyme activities, specifically CYP2D6. Therefore, administration of mitragynine together with herbal or modern drugs which follow the same metabolic pathway may contribute to herb-drug interactions.
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Ten cases of sporotrichosis associated with armadillo hunting detected in the State of Rio Grande do Sul were diagnosed by mycological methods. The susceptibility tests of Sporothrix schenckii isolates to antifungal agents itraconazole, ketoconazole and terbinafine showed that all the isolates were susceptible.
Risperidone is a relatively new antipsychotic drug that has been reported to improve both the positive and the negative symptoms of schizophrenia and produces relatively few extrapyramidal side effects at low doses. Formation of 9-hydroxyrisperidone, an active metabolite, is the most important metabolic pathway of risperidone in human. In the present study, in vitro metabolism of risperidone (100 microM) was investigated using the recombinant human cytochrome P450 (CYP) enzymes CYP1A1, CYP1A2, CYP2C8, CYP2C9-arg144, CYP2C9-cys144, CYP2C19, CYP2D6, CYP3A4 and CYP3A5 supplemented with an NADPH-generating system. 9-Hydroxyrisperidone was determined by a new HPLC method with an Hypersil CN column and a UV detector. Of these enzymes, CYPs 2D6, 3A4 and 3A5 were found to be the ones capable of metabolising risperidone to 9-hydroxyrisperidone, with activities of 7.5, 0.4 and 0.2 pmol pmol(-1) CYP min(-1), respectively. A correlation study using a panel of human liver microsomes showed that the formation of 9-hydroxyrisperidone is highly correlated with CYP2D6 and 3A activities. Thus, both CYP2D6 and 3A4 are involved in the 9-hydroxylation of risperidone at the concentration of risperidone used in this study. This observation is confirmed by the findings that both quinidine (inhibitor of CYP2D6) and ketoconazole (inhibitor of CYP3A4) can inhibit the formation of 9-hydroxyrisperidone. Furthermore, inducers of CYP can significantly increase the formation of 9-hydroxyrisperidone in rat. The formation of 9-hydroxyrisperidone is highly correlated with testosterone 6beta-hydroxylase activities, suggesting that inducible CYP3A contributes significantly to the metabolism of risperidone in rat.
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Complete cure of mycetoma is difficult to achieve and recurrence is common. The study objective was to determine the predictors of cure, amputation and follow-up dropout among the studied individuals with mycetoma. This prospective study included 1544 patients with confirmed mycetoma, of whom 1242 had eumycetoma and 302 actinomycetoma. They were treated and followed up regularly. Data were collected and analysed using logistic regression models to determine the predictors. In the eumycetoma group, longer treatment duration (OR=1.9; 95% CI 1.2-3.1) and absence of history of disease recurrence (OR=24.2; 95% CI 7.7-76.3) were significant predictors of increased odds of cure from mycetoma. A lesion size of 5-10 cm (OR=0.5; 95% CI 0.3-0.8) or >10 cm (OR=0.7; 95% CI 0.4-1.0) and combined medical treatment and surgery (OR=0.004; 95% CI 0.001-0.011) were each significant predictors of reduced odds of cure. Follow-up dropout among this group was high (54%). Large lesions (5-10 cm, OR=0.5, 95% CI 0.4-0.7; >10 cm, OR=0.6; 95% CI 0.5-0.9), amputations (OR=0.3; 95% CI 0.1-0.6) and longer treatment duration (OR=0.5; 95% CI 0.4-0.7) were significant predictors of reduced odds of follow-up dropout. In the actinomycetoma group, medical treatment was the only significant predictor of cure. Follow-up dropout among this group was also high (55.6%). Long treatment duration was a significant predictor of reduced odds of dropout (OR=0.5; 95% CI 0.3-0.8). There is a great demand for effective and efficient mycetoma treatment. Counselling and health education of patients is badly needed to encourage early reporting and treatment to reduce mycetoma's medical, social and economic impacts.
Advancement of in silico tools would be enabled by the availability of data for metabolic reaction rates and intrinsic clearance (CLint) of a diverse compound structure data set by specific metabolic enzymes. Our goal is to measure CLint for a large set of compounds with each major human cytochrome P450 (P450) isozyme. To achieve our goal, it is of utmost importance to develop an automated, robust, sensitive, high-throughput metabolic stability assay that can efficiently handle a large volume of compound sets. The substrate depletion method [in vitro half-life (t1/2) method] was chosen to determine CLint The assay (384-well format) consisted of three parts: 1) a robotic system for incubation and sample cleanup; 2) two different integrated, ultraperformance liquid chromatography/mass spectrometry (UPLC/MS) platforms to determine the percent remaining of parent compound, and 3) an automated data analysis system. The CYP3A4 assay was evaluated using two long t1/2 compounds, carbamazepine and antipyrine (t1/2 > 30 minutes); one moderate t1/2 compound, ketoconazole (10 < t1/2 < 30 minutes); and two short t1/2 compounds, loperamide and buspirone (t½ < 10 minutes). Interday and intraday precision and accuracy of the assay were within acceptable range (∼12%) for the linear range observed. Using this assay, CYP3A4 CLint and t1/2 values for more than 3000 compounds were measured. This high-throughput, automated, and robust assay allows for rapid metabolic stability screening of large compound sets and enables advanced computational modeling for individual human P450 isozymes.
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Multifocal fungal (Aspergillus terreus) discospondylitis was diagnosed in 2 German shepherd dogs. In one dog, the aetiology was established by means of fluoroscopic-guided disc aspiration, cytology and culture of disc material and urine. Disseminated aspergillosis was confirmed at necropsy and A. terreus cultured from numerous organs in this dog. The aetiology in the other dog was not established until therapeutic failure forced surgical curettage of disc material from which the fungus was cultured. Ketoconazole therapy failed to effect an improvement, and at necropsy, disease was localised to the spinal column, with A. terreus cultured from the affected discs and associated vertebrae. Immunodeficiency was suspected in both cases. In the case of disseminated disease a reduced lymphocyte blastogenic response was demonstrated. Reduced IgA was shown in both cases. The German shepherd breed seems to be predisposed to Aspergillus infections and IgA deficiency.
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Itraconazole, a systemically active antifungal, was tested for its effects on microscopically assessed phagocytosis and killing of Candida glabrata 233 in vitro. Yeast cells were exposed to itraconazole in culture and guinea-pig peritoneal polymorphonuclear leucocytes were exposed to the drug injected intraperitoneally in vivo. At a concentration of 10(-7) M and with exposure times of 1 h, itraconazole pre-treatment of the leucocytes had no effect on the ability of PMNL to ingest or kill C. glabrata. However, pre-treatment of the growing C. glabrata cells under the same conditions significantly increased their vulnerability to both phagocytosis and intracellular killing. Longer exposures of the yeasts to itraconazole further increased their susceptibility to leucocyte phagocytosis, and it also rendered the cells vulnerable to killing merely by immersion in sodium deoxycholate solution. These findings indicate that short exposures of C. glabrata to low itraconazole concentrations damages the cells sublethally and renders them highly susceptible to leucocyte killing. Itraconazole had no direct effects on leucocyte function itself.
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The diagnosis of acute lymphatic non-T-non-B leukaemia of common ALL type was confirmed in a 22-year-old woman. Cytostatic treatment brought full remission for 21/2 years. Renewed cytostatic treatment for recurrence brought about a mucormycosis in the mid-face region during a period of protracted agranulocytosis, despite antibiotic prophylaxis with ketoconazole and cotrimoxazole. The causative mucor organism was demonstrated in smears and biopsy material. The infection was successfully treated with i.v. amphotericin B and débridement of the affected tissue. There remained large tissue defects in the region of gum, nose, upper lip and right oral cavity. Previously the mortality rate of mucormycosis in the course of leukaemia was 100%.
Ketoconazole (KT) is a broad-spectrum antifungal agent whose pharmacological activity is based on the capability to interfere with steroid biosynthesis through an interaction with fungal cytochrome P-450 enzymes and thereby avoiding the formation of fungal walls. As the inhibition of fungal cytochrome P-450 by KT is not specific, the mammalian cytochrome P-450 species, which play an important role in the biosynthesis of steroidogenesis, are also affected. The reproductive and developmental toxicity of KT have been assessed. This antimycotic agent has been reported as embryotoxic and teratogenic when administered in high doses (80 mg/kg) to pregnant rats. The mechanisms by which KT exert teratogenic effects remains to be elucidated. When considering the potential inhibitory effect of KT on mammalian steroid biosynthesis as a possible responsible for the skeletal anomalies induced by this drug, this study aimed at determining whether steroid maternal supplementation may prevent the skeletal anomalies induced by KT. To test this hypothesis, maternal supplementation with prednisone (PRED) (0.1, 0.2 or 0.4 mg/kg) and 80 mg/kg of KT were administered to pregnant Wistar rats (n = 10) during organogenesis period. On gestational day 21, the dams were euthanized and examined for standard parameters of reproductive outcome. In summary, the results showed that PRED supplementation therapy may cause reductions in the incidence of KT-induced cranial and appendicular skeletal anomalies as well as cleft palate in the rat, being these results more consistent with 0.4 mg/kg of this drug. These results suggest an important role for glucocorticoids in KT-induced teratogenesis.
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Acanthamoeba keratitis is a rare cause of corneal infection in Taiwan, which can result in devastating visual outcomes. A 37-year-old woman, who wore soft contact lenses, suffered from severe pain in her left eye. Biomicroscopy revealed dendritic keratitis, radial keratoneuritis, and fine keratic precipitates on her cornea. Culture, using non-nutrient agar plate seeded with Escherichia coli, resulted in heavy growth of Acanthamoeba. The inpatient treatment, including topical neomycin-polymyxin B and metronidazole (0.5%) eyedrops, oral ketoconazole, and then oral prednisolone, successfully controlled the corneal infection. The best-corrected visual acuity was 0.9 without any evidence of recurrence of infection after 21 months of follow up. Acanthamoeba keratitis can present as dendritic keratitis, which mimics herpes simplex infection, thus, delays appropriate treatment. Early diagnosis and judicious treatment are essential for restoring the vision and avoiding the subsequent need of penetrating keratoplasty.
The model described here may present more similar conditions to clinical fungal infections; therefore the results such as MIC may be more helpful for hiring the most effective antifungal agent.
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Molecular phylogeny positioned S. purpuratus CYP51 at the base of the deuterostome clade. In zebrafish, CYP51 is expressed in all organs examined, most strongly in intestine. The recombinant protein bound lanosterol and catalyzed 14α-demethylase activity, at 3.2nmol/min/nmol CYP51. The binding of azoles to zebrafish CYP51 gave KS (dissociation constant) values of 0.26μM for ketoconazole and 0.64μM for propiconazole. Displacement of carbon monoxide also indicated zebrafish CYP51 has greater affinity for ketoconazole. Docking to homology models showed that lanosterol docks in fish and sea urchin CYP51s with an orientation essentially the same as in mammalian CYP51s. Docking of ketoconazole indicates it would inhibit fish and sea urchin CYP51s.
The polyenes, amphotericin B and mepartricin and the imidazoles, miconazole, ketoconazole, itraconazole and fluconazole, were studied either alone or in paired polyene-imidazole combinations to determine their activity in vitro against clinical yeast isolates. The methods included shaken and standing liquid cultures, continuous cultures and chequerboard titrations, with or without the incorporation of pooled human plasma. The polyenes were found to exert an immediate cidal action even with high cell populations whereas the imidazoles demonstrated a time-dependent fungistatic activity which increased very slowly with increase in drug concentration. The interactions observed with the paired combinations were consistent and were found to be anomalous with all methods used. The activity of the imidazoles was enhanced by the presence of the polyenes; by contrast the polyenes were strongly antagonized by the imidazoles.
This is the second case report of a temporal bone osteomyelitis caused by Blastomyces dermatitidis, which presented as a chronic serous otitis media. The presenting serous otitis media was refractory to conventional medical and surgical management and progressed to a temporal bone osteomyelitis prior to diagnosis. B. dermatitidis is a rare fungal pathogen that causes a systemic pyogranulomatous disease that primarily manifests itself in the skin, bones, pulmonary, and genitourinary systems. If left untreated it is associated with a high rate of mortality. The otologic presentation of this rare disease is emphasized, while the clinical and therapeutic features are reviewed.
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A PPK model was constructed using pooled ospemifene concentrations. Covariates considered before start of the analysis were: age, race, body weight, BMI, albumin, alanine amino-transferase, bilirubin, and creatinine clearance. The expected distribution of ospemifene concentration was derived for the 4 cases in phase-1 studies that increased ospemifene exposure: administration to severe renal impairment subjects (case 1), administration to moderate hepatic impairment subjects (case 2), coadministration with ketoconazole (case 3), or coadministration with fluconazole (case 4). Safety information in a long-term safety trial was used to assess the potential changes in risk of adverse events with ospemifene-exposure increase.
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The efficacy was analyzed in 66 out of the 79 patients included in the study (36 patients treated with oxiconazole, 30 with ketoconazole). At Day 14, a first assessment was made and 77.1 p. 100 of the patients treated with oxiconazole had been cured; this result was significantly better (p < 0.05) than that obtained with ketoconazole (51.7 p. 100 of cured patients). At Day 21, after a further week of treatment, both treatments were efficient with statistically non-different results between the two groups: 97.2 p. 100 of the patients treated with oxiconazole, versus 86.7 p. 100 with ketoconazole. Thus, a greater rapidity of action of oxiconazole was observed. No correlation was detected between the ratio of cured patients and the duration of the mycosis. The safety was assessed in 74 patients. No adverse effects were reported for the patients treated with oxiconazole, whereas 9 patients treated with ketoconazole experienced contact sensitization reactions and irritant skin reactions due to the application of the product. The difference between the two groups of treatment was statistically greatly significant (p < 0.001). Furthermore, acceptance of the drug on the part of the patient was better (p < 0.05) with oxiconazole.
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Twenty-four subjects were enrolled. Compared with neratinib administered alone, co-administration of ketoconazole increased neratinib C(max) by 3.2-fold (90% CI: 2.4, 4.3) and AUC by 4.8-fold (3.6, 6.5). Median t(max) was 6.0 h with both regimens. Ketoconazole decreased mean apparent oral clearance of neratinib from 346 lh(-1) to 87.1 lh(-1) and increased mean elimination half-life from 11.7 h to 18.0 h. The incidence of adverse events was comparable between the two regimens (50% neratinib alone, 65% co-administration with ketoconazole).
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Low-dose ritonavir produces extensive CYP3A inhibition exceeding that of ketoconazole (typically 10- to 15-fold midazolam AUC enhancement), and is a suitable positive control index inhibitor for drug-drug interaction studies. ALT-2074 inhibits CYP3A metabolism to a small degree that is of uncertain clinical importance.
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Mammalian cells, cultured in the presence of serum lipoproteins, acquire cholesterol necessary for growth from the uptake and lysosomal hydrolysis of low-density lipoproteins (LDL). The mechanism(s) of intracellular transport of LDL-derived cholesterol from lysosomes to other cellular sites is unknown. In this study, various pharmacological agents were assessed for their ability to inhibit the movement of LDL-cholesterol from lysosomes to the plasma membrane. The only pharmacological agent tested in these experiments that specifically inhibited LDL-cholesterol movement was U18666A. Ketoconazole impaired the intracellular transport of LDL-cholesterol; however, ketoconazole also had a general effect on cholesterol movement, since it impeded the desorption of endogenously synthesized cholesterol into the medium. Other drugs that affected cholesterol movement appeared to be nonspecific. Cholesterol transport from lysosomes to plasma membranes was not significantly altered by agents that affect lysosomal function or cytoskeletal organization, as well as energy poisons and cycloheximide.
The electrochemical reactions of the antifungal drugs itraconazole, ketoconazole, fluconazole and voriconazole have been investigated by differential pulse polarography (DPP) using a dropping mercury electrode (DME). All investigations were carried out in Britton-Robinson buffer solutions and methanol with varying pH values. Ketoconazole and itraconazole both showed a reduction peak with a potential between -1.5V and -1.6 V. Stable and reproducible conditions for the determination of itraconazole (c = 1 x 10(-7) M) were found within the pH range of 6.0 to 8.0 and for the determination of ketoconazole (c = 5 x 10(-8) M) within pH 6.0 to 7.0. Voriconazole showed a reduction peak with a peak potential of -1.7 V (c = 1 x 10(-5) M) within the pH range of 8.0 to 10.0. In the case of fluconazole no electrochemical activity was found.
In vitro anti-dermatophyte, anti-Candida albicans and anti-Malassezia furfur activities of amorolfine hydrochloride (AMF), terbinafine hydrochloride (TBF), butenafine hydrochloride (BTF), neticonazole hydrochloride (NCZ) and ketoconazole (KCZ), all of which were introduced for the treatment of dermatomycoses in the 1990s in Japan, were compared. Although all of the test drugs are classified as an ergosterol biosynthesis inhibitor, the antifungal properties were found to be different. TBF and BTF exerted extremely potent antifungal activity against Trichophyton spp. but not against C. albicans and M. furfur, whilst KCZ and NCZ showed potent antifungal activity against C. albicans and M. furfur rather than Trichophyton spp. AMF exhibited potent antifungal activity against all of the fungal species tested. Fungicidal activities of these antifungal agents against T. rubrum were determined by using neutral red staining. The fungicidal potentialities correlated with those obtained in the in vitro susceptibility test as determined by MICs against dermatophytes. TBF, BTF and AMF exerted more potent fungicidal action than NCZ and KCZ.
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Drug-target interaction (DTI) is the basis of drug discovery and design. It is time consuming and costly to determine DTI experimentally. Hence, it is necessary to develop computational methods for the prediction of potential DTI. Based on complex network theory, three supervised inference methods were developed here to predict DTI and used for drug repositioning, namely drug-based similarity inference (DBSI), target-based similarity inference (TBSI) and network-based inference (NBI). Among them, NBI performed best on four benchmark data sets. Then a drug-target network was created with NBI based on 12,483 FDA-approved and experimental drug-target binary links, and some new DTIs were further predicted. In vitro assays confirmed that five old drugs, namely montelukast, diclofenac, simvastatin, ketoconazole, and itraconazole, showed polypharmacological features on estrogen receptors or dipeptidyl peptidase-IV with half maximal inhibitory or effective concentration ranged from 0.2 to 10 µM. Moreover, simvastatin and ketoconazole showed potent antiproliferative activities on human MDA-MB-231 breast cancer cell line in MTT assays. The results indicated that these methods could be powerful tools in prediction of DTIs and drug repositioning.
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An HPLC method to determine simultaneously ketoconazole and formaldehyde in an anti-dandruff shampoo, originally developed on a long column, was transferred to two short columns with similar stationary phase properties, but with a length of at the most 30% of the initial one. Using the conventional column as reference, the fast HPLC methods on the short columns were validated. The validation characteristics consisted of selectivity, linearity range, precision (repeatability and time-different intermediate precision), bias and robustness. For the ketoconazole assay, linearity for peak area was found in the concentration range up to 0.20 mg/ml. For formaldehyde, two calibration ranges (0-10 x 10(-5) and 0-10 x 10(-4)%) were linear, both for peak area and height. The assays for both ketoconazole and formaldehyde in these ranges showed no bias and an acceptable precision, although the precision found with the short columns was slightly worse than with the long one. The robustness tests were performed applying a Plackett-Burman design. For the ketoconazole assay, 6 factors were examined in a 12 experiments design and for formaldehyde, 11 factors in 16 experiments. The methods were found to be robust. Despite the somewhat less good precision the transfer seems to be successful and the obtained assays on the short columns are applicable for fast routine analysis.