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ketoconazole

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https://www.readbyqxmd.com/read/28805726/chemical-identity-of-interaction-of-protein-with-reactive-metabolite-of-diosbulbin-b-in-vitro-and-in-vivo
#1
Kai Wang, Dongju Lin, Xiucai Guo, Wenlin Huang, Ying Peng, Jiang Zheng
Diosbulbin B (DIOB), a hepatotoxic furan-containing compound, is a primary ingredient in Dioscorea bulbifera L., a common herbal medicine. Metabolic activation is required for DIOB-induced liver injury. Protein covalent binding of an electrophilic reactive intermediate of DIOB is considered to be one of the key mechanisms of cytotoxicity. A bromine-based analytical technique was developed to characterize the chemical identity of interaction of protein with reactive intermediate of DIOB. Cysteine (Cys) and lysine (Lys) residues were found to react with the reactive intermediate to form three types of protein modification, including Cys adduction, Schiff's base, and Cys/Lys crosslink...
August 14, 2017: Toxins
https://www.readbyqxmd.com/read/28802958/interaction-of-erythromycin-and-ketoconazole-on-the-neurological-biochemical-and-behavioral-responses-in-crucian-carp
#2
Jianchao Liu, Yuanfei Cai, Guanghua Lu, Xiaoxiang Dan, Donghai Wu, Zhenhua Yan
The presence of pharmaceuticals in the aquatic environment has received great attention due to their potential impacts on public health. The single, as well as the combined toxicities of erythromycin (ERY) and ketoconazole (KCZ) on the bioaccumulation, biochemical and behavioral responses, were examined in crucian carp. This study focused on the uptake of contaminants, acetylcholinesterase (AChE) activity in the brain, swimming and shoaling behavior of fish. After 14days of binary exposure, the addition of KCZ at nominal concentrations of 0...
August 7, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28800141/effects-of-strong-cyp3a-inhibition-and-induction-on-the-pharmacokinetics-of-ixazomib-an-oral-proteasome-inhibitor-results-of-drug-drug-interaction-studies-in-patients-with-advanced-solid-tumors-or-lymphoma-and-a-physiologically-based-pharmacokinetic-analysis
#3
Neeraj Gupta, Michael J Hanley, Karthik Venkatakrishnan, Alberto Bessudo, Drew W Rasco, Sunil Sharma, Bert H O'Neil, Bingxia Wang, Guohui Liu, Alice Ke, Chirag Patel, Karen Rowland Yeo, Cindy Xia, Xiaoquan Zhang, Dixie-Lee Esseltine, John Nemunaitis
At clinically relevant ixazomib concentrations, in vitro studies demonstrated that no specific cytochrome P450 (CYP) enzyme predominantly contributes to ixazomib metabolism. However, at higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms, with the estimated relative contribution being highest for CYP3A at 42%. This multiarm phase 1 study (Clinicaltrials.gov identifier: NCT01454076) investigated the effect of the strong CYP3A inhibitors ketoconazole and clarithromycin and the strong CYP3A inducer rifampin on the pharmacokinetics of ixazomib...
August 11, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28796631/endocrine-disruption-in-human-fetal-testis-explants-by-individual-and-combined-exposures-to-selected-pharmaceuticals-pesticides-and-environmental-pollutants
#4
Pierre Gaudriault, Séverine Mazaud-Guittot, Vincent Lavoué, Isabelle Coiffec, Laurianne Lesné, Nathalie Dejucq-Rainsford, Martin Scholze, Andreas Kortenkamp, Bernard Jégou
BACKGROUND: Numerous chemicals are capable of disrupting androgen production, but the possibility that they might act together to produce effects greater than those of the most effective component in the mixture has not been studied directly in human tissues. Suppression of androgen synthesis in fetal life has been associated with testis maldescent, malformations of the genitalia at birth, and poor semen quality later in life. OBJECTIVES: Our aim was to investigate whether chemicals can act together to disrupt androgen production in human fetal testis explants and to evaluate the importance of mixture effects when characterizing the hazard of individual chemicals...
August 4, 2017: Environmental Health Perspectives
https://www.readbyqxmd.com/read/28776447/analysis-of-imidazoles-and-triazoles-in-biological-samples-after-microextraction-by-packed-sorbent
#5
Cristina Campestre, Marcello Locatelli, Paolo Guglielmi, Elisa De Luca, Giuseppe Bellagamba, Sergio Menta, Gokhan Zengin, Christian Celia, Luisa Di Marzio, Simone Carradori
This paper reports the MEPS-HPLC-DAD method for the simultaneous determination of 12 azole drugs (bifonazole, butoconazole, clotrimazole, econazole, itraconazole, ketoconazole, miconazole, posaconazole, ravuconazole, terconazole, tioconazole and voriconazole) administered to treat different systemic and topical fungal infections, in biological samples. Azole drugs separation was performed in 36 min. The analytical method was validated in the ranges as follows: 0.02-5 μg mL(-1) for ravuconazole; 0.2-5 μg mL(-1) for terconazole; 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28771009/model-based-analysis-of-biopharmaceutical-experiments-to-improve-mechanistic-oral-absorption-modelling-an-integrated-in-vitro-in-vivo-extrapolation-iviv_e-perspective-using-ketoconazole-as-a-model-drug
#6
Shriram M Pathak, Aaron Ruff, Edmund Kostewicz, Nikunjkumar Patel, David B Turner, Masoud Jamei
Mechanistic modelling of in vitro data generated from metabolic enzyme systems (viz. liver microsomes, hepatocytes, rCYP enzymes etc.) facilitates in vitro-in vivo extrapolation (IVIV_E) of metabolic clearance which plays a key role in the successful prediction of clearance in vivo within Physiologically-Based Pharmacokinetic (PBPK) modelling. A similar concept can be applied to solubility and dissolution experiments whereby mechanistic modelling can be used to estimate intrinsic parameters required for mechanistic oral absorption simulation in vivo...
August 3, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28770093/the-clinical-practice-guideline-for-the-management-of-ards-in-japan
#7
Satoru Hashimoto, Masamitsu Sanui, Moritoki Egi, Shinichiro Ohshimo, Junji Shiotsuka, Ryutaro Seo, Ryoma Tanaka, Yu Tanaka, Yasuhiro Norisue, Yoshiro Hayashi, Eishu Nango
BACKGROUND: The Japanese Society of Respiratory Care Medicine and the Japanese Society of Intensive Care Medicine provide here a clinical practice guideline for the management of adult patients with ARDS in the ICU. METHOD: The guideline was developed applying the GRADE system for performing robust systematic reviews with plausible recommendations. The guideline consists of 13 clinical questions mainly regarding ventilator settings and drug therapies (the last question includes 11 medications that are not approved for clinical use in Japan)...
2017: Journal of Intensive Care
https://www.readbyqxmd.com/read/28754462/in-vitro-susceptibility-of-candida%C3%A2-albicans-clinical-isolates-to-eight-antifungal-agents-in-ouagadougou-burkina-faso
#8
A Zida, A Yacouba, S Bamba, I Sangare, M Sawadogo, T Guiguemde, S Kone, L K Traore, R Ouedraogo-Traore, R T Guiguemde
INTRODUCTION: In recent years, the infection Candida albicans infection worldwide has risen, and the incidence of resistance to traditional antifungal therapies is also increasing. The aim of this study was to evaluate in vitro susceptibility of C. albicans clinical isolates to eight antifungal agents in Ouagadougou. MATERIALS AND METHODS: A cross-sectional study was conducted from January 2013 to December 2015 at Yalgado Ouédraogo University Teaching Hospital...
July 25, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28749293/diagnosis-and-successful-treatment-of-a-potentially-zoonotic-dermatophytosis-caused-by-microsporum-gypseum-in-a-zoo-housed-north-american-porcupine-erethizon-dorsatum
#9
Christine E Hackworth, David Eshar, Melissa Nau, Mary Bagladi-Swanson, Gordon A Andrews, James W Carpenter
A female North American porcupine ( Erethizon dorsatum ) was evaluated for a unilateral pedal crusting and alopecic dermatopathy. Fungal culture and histopathology testing revealed Microsporum gypseum dermatophytosis. Treatment with topical miconazole was initiated and then discontinued after 9 days and changed to oral terbinafine. Twenty-eight days after initial examination, clinical signs were improving, and fungal cultures of the front foot, muzzle, and noninfected area along the dorsum were negative for M...
June 2017: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
https://www.readbyqxmd.com/read/28745287/copper-nanoflowers-as-effective-antifungal-agents-for-plant-pathogenic-fungi
#10
Avinash P Ingle, Mahendra Rai
Flower-shaped copper nanoparticles were synthesised by a green and ecofriendly chemical reduction approach using copper sulphate and cytyltrimethal ammonium bromide. The UV-vis spectrophotometer analysis showed maximum absorption at about 552 nm, which is specifically reported for copper nanoparticles. The crystal lattice structure of copper nanoflowers was confirmed by X-ray diffraction analysis. Further, the transmission electron microscopic studies revealed the flower shape copper nanoparticles in the size range of 100-500 nm...
August 2017: IET Nanobiotechnology
https://www.readbyqxmd.com/read/28740275/edible-wild-plant-heracleum-pyrenaicum-subsp-orsinii-as-a-potential-new-source-of-bioactive-essential-oils
#11
Ljuboš Ušjak, Silvana Petrović, Milica Drobac, Marina Soković, Tatjana Stanojković, Ana Ćirić, Marjan Niketić
Many Heracleum L. taxa (Apiaceae) are used as food and spices, and in traditional medicine. In this work, the chemical composition of Heracleum pyrenaicum subsp. orsinii (Guss.) F. Pedrotti and Pignatti root, leaf and fruit essential oils, their antimicrobial activity and cytotoxic effect on malignant and normal cells were investigated for the first time. The composition of the oils was analyzed by GC and GC-MS. Monoterpenes prevailed in the root oil, with β-pinene (38.6%) being dominant, while in the leaf oil, sesquiterpenes, mostly (E)-nerolidol (20...
July 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28739796/multicenter-and-international-study-of-mic-mec-distributions-for-definition-of-epidemiological-cutoff-values-ecvs-for-species-of-sporothrix-identified-by-molecular-methods
#12
A Espinel-Ingroff, D P B Abreu, R Almeida-Paes, R S N Brilhante, A Chakrabarti, A Chowdhary, F Hagen, S Córdoba, G M Gonzalez, N P Govender, J Guarro, E M Johnson, S E Kidd, S A Pereira, A M Rodrigues, S Rozental, M W Szeszs, R Ballesté Alaniz, A Bonifaz, L X Bonfietti, L P Borba-Santos, J Capilla, A L Colombo, M Dolande, M G Isla, M S C Melhem, A C Mesa-Arango, M M E Oliveira, M M Panizo, Z Pires de Camargo, R M Zancope-Oliveira, J F Meis, J Turnidge
Clinical and Laboratory Standards Institute (CLSI) conditions for testing the susceptibilities of pathogenic Sporothrix species to antifungal agents are based on a collaborative study that evaluated five clinically relevant isolates of Sporothrix schenckii sensu lato and some antifungal agents. With the advent of molecular identification, there are two basic needs: to confirm the suitability of these testing conditions for all agents and Sporothrix species and to establish species-specific epidemiologic cutoff values (ECVs) or breakpoints (BPs) for these species...
July 24, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28736794/tinea-capitis-by-microsporum-audouinii-case-reports-and-review-of-published-global-literature-2000-2016
#13
Fábio Brito-Santos, Maria Helena Galdino Figueiredo-Carvalho, Rowena Alves Coelho, Anna Sales, Rodrigo Almeida-Paes
Tinea capitis caused by Microsporum audouinii is reported herein from two Brazilian schoolchildren, which are brothers. Arthroconidia were evidenced on direct examination of scalp hair, and a fungus of the genus Microsporum was isolated from cultures of each patient. The isolated fungi were classified as M. audouinii by visualization of species-specific structures, including: pectinate hyphae, chlamydospores, and fusiform macroconidia, sterile growth with characteristic brown pigment in rice grains, and through DNA sequencing of the internal transcriber spacer region...
July 24, 2017: Mycopathologia
https://www.readbyqxmd.com/read/28734977/modulation-of-the-interaction-between-human-p450-3a4-and-b-megaterium-reductase-via-engineered-loops
#14
Silvia Castrignanò, Serena D'Avino, Giovanna Di Nardo, Gianluca Catucci, Sheila J Sadeghi, Gianfranco Gilardi
Chimerogenesis involving cytochromes P450 is a successful approach to generate catalytically self-sufficient enzymes. However, the connection between the different functional modules should allow a certain degree of flexibility in order to obtain functional and catalytically efficient proteins. We previously applied the molecular Lego approach to develop a chimeric P450 3A4 enzyme linked to the reductase domain of P450 BM3 (BMR). Three constructs were designed with the connecting loop containing no glycine, 3 glycine or 5 glycine residues and showed a different catalytic activity and coupling efficiency...
July 19, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28732711/study-of-rheology-and-polymer-adsorption-onto-drug-nanoparticles-in-pharmaceutical-suspensions-produced-by-nano-milling
#15
Renata Negrini, Simone Aleandri, Martin Kuentz
Nanosuspensions provide a drug delivery approach to cope with erratic absorption of poorly water-soluble compounds. Despite of extensive research over the last years, there are still open pharmaceutical challenges so it is often unclear how quality attributes such as viscosity and physical stability are generated, which requires a more thorough study of the colloidal structures and interactions in nanosuspensions. In this study, diffusing wave spectroscopy and microfluidics-based rheology were used for the first time to assess pharmaceutical nanosuspensions that were obtained by wet milling...
July 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28710189/use-of-cabergoline-for-the-management-of-persistent-cushing-s-disease-in-pregnancy
#16
Kathleen Su-Yen Sek, Doddabele Srinivasa Deepak, Kok Onn Lee
Cushing's disease (CD) is rare during pregnancy and is associated with significant maternal and fetal complications. It is important to control hypercortisolism during pregnancy, either surgically or medically, for a successful maternal and fetal outcome. We report a patient with recurrent CD who was treated with low-dose cabergoline (CAB) for persistent hypercortisolism throughout pregnancy. A 36-year-old woman was diagnosed with CD at the age of 23. She underwent trans-sphenoidal surgery with initial complete remission...
July 14, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28705617/drug-solubility-in-lipid-nanocarriers-influence-of-lipid-matrix-and-available-interfacial-area
#17
Katrin Göke, Heike Bunjes
Amongst other strategies for the formulation of poorly water-soluble drugs, solubilization of these drugs in lipid-based formulations is a promising option. Most screening methods for the identification of a suitable lipid-based formulation fail to elucidate the role interfacial effects play for drug solubility in disperse systems. In a novel screening approach called passive drug loading, different preformed lipid nanocarrier dispersions are incubated with drug powder. Afterwards, undissolved drug is filtered off and the amount of solubilized drug is determined...
July 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28685145/oral-candida-in-patients-with-fixed-orthodontic-appliance-in-vitro-combination-therapy
#18
Wisam Alhamadi, Rafal J Al-Saigh, Nebras N Al-Dabagh, Hussam W Al-Humadi
BACKGROUND: Fixed orthodontic appliance (FOA) increases the cariogenic microorganisms of mouth including candida. The aim was to evaluate the pharmacodynamic effects of some antibacterial drugs in combination with most applicable antifungal agents on candida isolated from patients with FOA. METHODS: Three antifungal agents (amphotericin B (AMB), ketoconazole (KET), and itraconazole (ITZ)) and three antibacterial drugs (ciprofloxacin (CIP), doxycycline (DOX), and metronidazole (MET)) with serial concentrations have been used and microdilution broth method has been done for single and combination therapy, then fungal growth was assessed spectrophotometrically, and the combinations were evaluated by bliss independent analysis...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28681884/condition-responsive-nanoparticles-for-managing-infection-and-inflammation-in-keratitis
#19
Saad M Ahsan, Ch Mohan Rao
Keratitis is a major cause of avoidable visual impairment. About 30% of patients with fungal keratitis eventually become permanently blind in the developing world. Proteases, secreted by the pathogen and the host, damage the cornea before the infection is resolved. Treating keratitis is a challenge because both infection and inflammation need to be addressed. An additional challenge is to maintain a therapeutic dose at the corneal surface as blinking and tear film wash away the drugs, administered as eye drops...
July 20, 2017: Nanoscale
https://www.readbyqxmd.com/read/28676004/evaluation-of-1-3-benzoxathiol-2-one-derivatives-as-potential-antifungal-agents
#20
Luciana Terra, Eliza de L Chazin, Paola de S Sanches, Max Saito, Marcus V N de Souza, Claudia R B Gomes, James L Wardell, Solange M S V Wardell, Plínio C Sathler, Gabriela C C Silva, Viviane O Lione, Marcos Kalil, Ana Joffily, Helena C Castro, Thatyana R A Vasconcelos
BACKGROUND: Over the last few years, fungal infections have emerged as a worrisome global public health problem. Candidiasis is a disease caused by Candida species and has been a problem worldwide mainly for immunosuppressed patients. Lately, the resistant strains and side effects have been reported as important issues for treating Candidiasis, which have to be solved by identifying new drugs. OBJECTIVE: The goal of this work was to synthesize a series of 1,3-benzoxathiol-2-one derivatives, XY-benzo[d][1,3]oxathiol-2-ones, and evaluate their antifungal activity against five Candida species...
July 3, 2017: Medicinal Chemistry
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