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https://www.readbyqxmd.com/read/29343612/structural-and-functional-characterisation-of-the-cytochrome-p450-enzyme-cyp268a2-from-mycobacterium-marinum
#1
Stella A Child, Elise F Naumann, John B Bruning, Stephen G Bell
Members of the cytochrome P450 monooxygenase family CYP268 are found across a broad range of Mycobacterium species including the pathogens Mycobacterium avium, M. colombiense,M. kansasii and Mmarinum CYP268A2, from M. marinum , which is the first member of this family to be studied, was purified and characterised. CYP268A2 was found to bind a variety of substrates with high affinity, including branched and straight-chain fatty acids (C10-C12), acetate esters, and aromatic compounds. The enzyme was also found to bind phenylimidazole inhibitors but not larger azoles, such as ketoconazole...
January 17, 2018: Biochemical Journal
https://www.readbyqxmd.com/read/29341946/microemulgel-of-voriconazole-an-unfathomable-protection-to-counter-fungal-contagiousness
#2
Kalpesh C Ashara, Jalpa S Paun, Moinuddin M Soniwala, Jayant R Chavda
BACKGROUND: Fluconazole and ketoconazole both have poor minimum inhibitory concentration than voriconazole. Voriconazole had serious side effects in oral and intravenous doses. It has poor water solubility. The objective of the study was to prepare and optimize microemulgel of voriconazole for topical delivery. AIM: Formulation, development, and evaluation of voriconazole microemulgel for topical delivery. METHODS: Oil and emulsifi ers selected were on the basis of equilibrium solubility study and emulsification property respectively...
December 20, 2017: Folia Medica
https://www.readbyqxmd.com/read/29338933/physiological-based-pharmacokinetic-modeling-to-estimate-in%C3%A2-vivo-ki-of-ketoconazole-on-renal-p-gp-using-human-drug-drug-interaction-study-result-of-fesoterodine-and-ketoconazole
#3
Masayo Oishi, Yuma Takano, Yutaka Torita, Bimal Malhotra, Koji Chiba
This study was conducted to estimate in vivo inhibition constant (Ki) of ketoconazole on renal P-glycoprotein (P-gp) using human drug-drug interaction (DDI) study result of fesoterodine and ketoconazole. Fesoterodine is a prodrug which is extensively hydrolyzed by non-specific esterases to the active metabolite 5-hydroxymethyl tolterodine (5-HMT). 5-HMT is then further metabolized via Cytochrome P450 (CYP) 2D6 and CYP3A4. It is reported that 5-HMT is a substrate of P-gp whereas fesoterodine is not. Renal clearance of 5-HMT is approximately two-times greater than renal glomerular filtration rate...
November 15, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29315246/recent-advances-in-electrochemical-biosensors-based-on-enzyme-inhibition-for-clinical-and-pharmaceutical-applications
#4
REVIEW
Loubna El Harrad, Ilhame Bourais, Hasna Mohammadi, Aziz Amine
A large number of enzyme inhibitors are used as drugs to treat several diseases such as gout, diabetes, AIDS, depression, Parkinson's and Alzheimer's diseases. Electrochemical biosensors based on enzyme inhibition are useful devices for an easy, fast and environment friendly monitoring of inhibitors like drugs. In the last decades, electrochemical biosensors have shown great potentials in the detection of different drugs like neostigmine, ketoconazole, donepezil, allopurinol and many others. They attracted increasing attention due to the advantage of being high sensitive and accurate analytical tools, able to reach low detection limits and the possibility to be performed on real samples...
January 9, 2018: Sensors
https://www.readbyqxmd.com/read/29302149/epidemiological-trends-of-cutaneous-leishmaniasis-in-al-madinah-al-munawarah-province-western-region-of-saudi-arabia
#5
Miskelyemen Abdelatti Elmekki, Mogahid M Elhassan, Hani A Ozbak, Ilham T Qattan, Satti M Saleh, Ali H Alharbi
Objective: To investigate the epidemiological trends of cutaneous leishmaniasis (CL) in Al-Madinah Al-Munawarah, western region of KSA. Materials and Methods: Four hundred and sixty-seven parasitologically confirmed CL cases attending Al-Meeqat Hospital, Al-Madinah, during 2012-2015, were included in this study. Results: Both Saudi and non-Saudi nationals were infected, with the highest infection rate being among Saudis (68.7%). Males were more affected than females as 86...
October 2017: Journal of Global Infectious Diseases
https://www.readbyqxmd.com/read/29297772/assessment-of-drug-drug-interaction-potential-and-pbpk-modeling-of-cc-223-a-potent-inhibitor-of-the-mammalian-target-of-rapamycin-kinase
#6
Zeen Tong, Rangaraj Narayanan, Christian Atsriku, Jim Nissel, Yan Li, Hong Liu, Xiaomin Wang, Sekhar Surapaneni
1. CC-223 was studied in vitro for metabolism and drug-drug interactions (DDI), and in clinic for interaction with ketoconazole. 2. In vitro, human metabolites of CC-223 included O-desmethyl CC-223 (M1), keto (M2), N-oxide (M3), and imine (M13), with M1 being the most prominent metabolite. 3. CC-223 was metabolized by CYP2C9 and CYP3A, while metabolism of M1 was mediated by CYP2C8 and CYP3A. Ketoconazole increased CC-223 and M1 exposure by 60-70% in healthy volunteers. 4. CC-223 (IC50 ≥ 27 µM) and M1 (IC50 ≥ 46 µM) were inhibitors of CYP2C9 and CYP2C19 in human liver microsomes...
January 3, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29274212/drug-susceptibility-of-fungi-isolated-from-icu-patients
#7
Barbara D Modrzewska, Anna J Kurnatowska,, Katarzyna Khalid
Candida species can be a reason of infections associated with high morbidity and mortality. The risk of invasive candidosis for patients admitted to intensive care units (ICUs) is increased due to immunosuppressive states, prolonged length of stay, broad-spectrum antibiotics and Candida colonization. The aim of the study was to determine selected properties of fungi isolated from patients treated in the ICUs of hospitals in Lodz. The materials were collected from the oral cavity, the tracheostomy or endotracheal tube and urine from 16 children and 35 adult...
2017: Annals of Parasitology
https://www.readbyqxmd.com/read/29239000/minimal-physiologically-based-pharmacokinetic-and-drug-drug-disease-interaction-model-of-rivaroxaban-and-verapamil-in-healthy-and-renally-impaired-subjects
#8
Mohamed Ismail, Vincent H Lee, Christina R Chow, Christopher M Rubino
Current dosing recommendations for rivaroxaban advocate dosage reduction in patients with moderate to severe renal impairment and avoidance of concomitant strong inhibitors of CYP3A or P-glycoprotein. However, rivaroxaban dosing in patients with mild renal impairment taking concomitant moderate inhibitors of CYP3A and P-glycoprotein is not addressed. To quantify the impacts of concomitant verapamil administration and renal impairment on rivaroxaban pharmacokinetics, a minimal physiologically based pharmacokinetic model system was developed and used to evaluate potential increases in rivaroxaban exposure and the consequent increase in risk of major bleeding...
December 14, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29238706/angular-phenozaxine-ethers-as-potent-multi-microbial-targets-inhibitors-design-synthesis-and-molecular-docking-studies
#9
Mercy A Ezeokonkwo, Onyinyechi N Ogbonna, Sunday N Okafor, Evelyn U Godwin-Nwakwasi, Fidelia N Ibeanu, Uchechukwu C Okoro
The reaction of diaza-5H-benzo[a]phenoxazin-5-one and 5H-benzo[a]phenoxazin-5-one with various phenols catalyzed by Pd/t-BuXPhos/K3PO4 system gave previously unknown ether derivatives (7a-f and 8a-f) in good yields. UV-visible, FTIR, and 1H NMR data were used to confirm structures of the synthesized compounds. The parent compounds and the derivatives were screened in-silico for their drug-likeness and binding affinities to the microbial targets through molecular docking. Molinspiration software and AutoDock were used for the drug-likeness and docking studies, respectively...
2017: Frontiers in Chemistry
https://www.readbyqxmd.com/read/29237391/utility-of-pooled-cryopreserved-human-enterocytes-as-an-in-vitro-model-for-assessing-intestinal-clearance-and-drug-drug-interactions
#10
Zhengyin Yan, Susan Wong, Jane Kelly, Hoa Le, Ning Liu, Mika Kosaka, Suzanne Tey, Peter Vuong, Albert Li
A recent advancement in isolation and cryopreservation has resulted in commercially available primary human enterocytes that express various drug metabolizing enzymes (DMEs) and transporters. The main objective of this study was to further evaluate the utility of pooled cryopreserved enterocytes, specifically MetMax™ cryopreserved human enterocytes (In Vitro ADMET Laboratories), as an in vitro model for assessing intestinal clearance in comparison to hepatocytes. It was found that, for CYP3A4 substrates such as midazolam, amprenavir and loperamide, in vitro metabolic clearance is generally lower in enterocytes compared to that of hepatocytes, which is consistent with the relative abundance of the enzyme between the intestine and liver...
December 12, 2017: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29199561/antifungal-antioxidative-and-genoprotective-properties-of-extracts-from-the-blushing-bracket-mushroom-daedaleopsis-confragosa-agaricomycetes
#11
Aleksandar Knežević, Mirjana Stajić, Lada Živković, Ivan Milovanović, Biljana Spremo-Potparević, Jelena Vukojević
This study aimed to evaluate the antifungal, antioxidative, and genoprotective potentials of various extracts of Daedaleopsis confragosa fruiting bodies and mycelia. The extracts exhibited weak fungistatic and an absence of any fungicidal activities against 7 important animal and human pathogens. Although mycelial extracts, especially the hot water extract, were more effective antifungal agents than basidiocarp extracts, they were significantly weaker than the commercial antimycotic ketoconazole. The tested extracts reduced DPPH radicals to various extents, depending on the material used for extraction and the solvent...
2017: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/29191265/dapaconazole-versus-ketoconazole-in-the-treatment-of-interdigital-tinea-pedis
#12
André Alves Moraes Gobbato, Cintia Aparecida Rodrigues Santiago Gobbato, Ronilson A Moreno, Natalícia de Jesus Antunes, Gilberto De Nucci
No abstract text is available yet for this article.
November 30, 2017: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29189730/a-new-series-of-pyrrole-based-chalcones-synthesis-and-evaluation-of-antimicrobial-activity-cytotoxicity-and-genotoxicity
#13
Ahmet Özdemir, Mehlika Dilek Altıntop, Belgin Sever, Hülya Karaca Gençer, Handan Açelya Kapkaç, Özlem Atlı, Merve Baysal
In an effort to develop new potent antimicrobial and anticancer agents, new pyrrole-based chalcones were designed and synthesized via the base-catalyzed Claisen-Schmidt condensation of 2-acetyl-1-methylpyrrole with 5-(aryl)furfural derivatives. The compounds were evaluated for their in vitro antimicrobial effects on pathogenic bacteria and Candida species using microdilution and ATP luminescence microbial cell viability assays. MTT assay was performed to determine the cytotoxic effects of the compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, C6 rat glioma, and NIH/3T3 mouse embryonic fibroblast cell lines...
November 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29185916/drug-drug-interactions-in-cocaine-users-and-their-clinical-implications
#14
Luca Gallelli, Santo Gratteri, Antonio Siniscalchi, Erika Cione, Sabrina Sirico, Paolo Seminara, Giovambattista De Sarro, Maria Cristina Caroleo
Drug-drug interactions (DDIs) are a common problem in clinical practice during drug treatments. DDIs can induce development of adverse drug reactions or reduce clinical efficacy of the drugs. In this review, using PubMed, Embase and Cochrane library we searched articles published until January 10, 2017, and described both pharmacokinetic and pharmacodynamic DDIs in cocaine consumers, focusing the interest on their clinical implications. In this review, the nodal points treated focused on: i) cocaine biochemical metabolism described for both, inactive benzoylecgonine and ecgonine methyl esters and norcocaine active metabolites...
September 20, 2017: Current Drug Abuse Reviews
https://www.readbyqxmd.com/read/29181205/basidiobolomycosis-simulating-a-mycobacterium-ulcerans-infection-in-a-togolese-rural-child
#15
Bayaki Saka, Waguena Gnassingbe, Garba Mahamadou, Sefako Akakpo, Julienne Teclessou, Aurel Abilogun-Chokki, Abas Mouhari-Toure, Koussake Kombate, Palokinam Pitché
Background: Basidiobolomycosis is a deep mycosis which preferentially affects rural young people in tropical countries. We report an atypical case, with multiple ulcers, simulating a Buruli ulcer. Case Report: A 5-year-old boy, living in a rural area, was seen for ulcers on the buttocks and at the back and right flank that had been in progress for 4 months. On examination, we found an infiltrated plaque with sharp edges, little painful, located on the buttocks, back, and the right flank...
2017: Case Reports in Dermatological Medicine
https://www.readbyqxmd.com/read/29178772/antimicrobial-action-and-long-term-effect-of-overnight-denture-cleansers
#16
Amanda Peracini, Ingrid Machado Andrade, Viviane Cássia Oliveira, Ana Paula Macedo, Claudia Helena Silva-Lovato, Valéria Oliveira Pagnano, Evandro Watanabe, Helena de Freitas Oliveira Paranhos
PURPOSE: To evaluate two denture cleansers for overnight soaking (0.5% sodium hypochlorite and peroxide alkaline) regarding efficacy against Candida spp. biofilms (randomized clinical trial) and their effects on the physical properties of a denture base acrylic resin simulating a period of 5 years of use (laboratory study). The Candida spp. were identified and their resistance to main antifungal agents was evaluated. METHODS: 32 complete denture wearers were instructed to brush their dentures three times a day and to soak them (≥8 hours) in: control - water (C); alkaline peroxide (AP); or 0...
April 2017: American Journal of Dentistry
https://www.readbyqxmd.com/read/29177532/-a-different-kind-of-wrestler-s-ear
#17
H Gärtner, C S L Müller, S L Becker, A Bozzato
We report the case of a 19-year-old patient who presented with recurrent circular and scaly skin changes. The patient reported wrestling as his main leisure activity. After an unsuccessful attempt at local antibiotic treatment, detailed dermatological work-up revealed the skin changes to be tinea corporis gladiatorum. According to dermatological guidelines for dermatophytosis, systemic treatment with fluconazole and local ointments containing ciclopirox olamine and ketoconazole were administered, which rapidly led to significant improvement...
November 24, 2017: HNO
https://www.readbyqxmd.com/read/29175644/active-freeze-drying-for-production-of-nanocrystal-based-powder-a-pilot-study
#18
Antoine Touzet, François Pfefferlé, Peter van der Wel, Alf Lamprecht, Yann Pellequer
Active Freeze Drying allows for producing lyophilised powders by progressive agitation of frozen blocks undergoing sublimation. One potential application of this process is the formulation design of unstable nanosuspensions for oral drug delivery, as here shown for nanocrystal-based ketoconazole powder. With this technique, a critical vapour flow needs to be achieved in order to obtain reasonable process yields (>78%). The size distribution of powder particles (median size between 21 and 44 µm) was affected by the nanocrystals concentration and the drug-to-stabilizer ratio...
November 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29172026/effect-of-non-prohibited-drugs-on-the-phase-ii-metabolic-profile-of-morphine-an-in-vitro-investigation-for-doping-control-purposes
#19
Gabriella Ambrosio, Xavier de la Torre, Monica Mazzarino, Maria K Parr, Francesco Botrè
The potential consequences of drug-drug interaction on the strategies adopted by the anti-doping laboratories to report an adverse analytical finding for morphine were investigated. We have evaluated in vitro the effects of fourteen drugs on the principal metabolic pathways of morphine. The selected drugs are among those most commonly used by the athletes, none of them presently included in the World Anti-Doping Agency Prohibited List. The non-prohibited drugs included four antifungals (fluconazole, itraconazole, ketoconazole and miconazole), six benzodiazepines (alprazolam, bromazepam, clonazepam, lorazepam, lormetazepam and triazolam), and four non-steroidal anti-inflammatory drugs (diclofenac, ibuprofen, ketoprofen and nimesulide)...
November 24, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29167312/inhibition-of-o-glcnacase-sensitizes-apoptosis-and-reverses-bortezomib-resistance-in-mantle-cell-lymphoma-through-modification-of-truncated-bid
#20
Sudjit Luanpitpong, Nawin Chanthra, Montira Janan, Jirarat Poohadsuan, Parinya Samart, Yaowalak U-Pratya, Yon Rojanasakul, Surapol Issaragrisil
Aberrant energy metabolism represents a hallmark of cancer and contributes to numerous aggressive behaviors of cancer cells, including cell death and survival. Despite the poor prognosis of mantle cell lymphoma (MCL), due to the inevitable development of drug resistance, metabolic reprograming of MCL cells remains an unexplored area. Post-translational modification of proteins via O-GlcNAcylation is an ideal sensor for nutritional changes mediated by O-GlcNAc transferase (OGT) and is removed by O-GlcNAcase (OGA)...
November 22, 2017: Molecular Cancer Therapeutics
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