keyword
MENU ▼
Read by QxMD icon Read
search

ketoconazole

keyword
https://www.readbyqxmd.com/read/28443986/minimal-inhibitory-concentration-distributions-and-epidemiological-cutoff-values-of-five-antifungal-agents-against-sporothrix-brasiliensis
#1
Rodrigo Almeida-Paes, Fábio Brito-Santos, Maria Helena Galdino Figueiredo-Carvalho, Ana Caroline Sá Machado, Manoel Marques Evangelista Oliveira, Sandro Antonio Pereira, Maria Clara Gutierrez-Galhardo, Rosely Maria Zancopé-Oliveira
BACKGROUND: Sporothrix brasiliensis is the most virulent sporotrichosis agent. This species usually responds to antifungal drugs, but therapeutic failure can occur in some patients. Antifungal susceptibility tests have been performed on this species, but no clinical breakpoints (CBPs) are available. In this situation, minimal inhibitory concentration (MIC) distributions and epidemiological cutoff values (ECVs) support the detection of identification of resistant strains. OBJECTIVES: To study the MIC distributions of five antifungal drugs against S...
May 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28442602/molecular-basis-of-metabolism-mediated-conversion-of-pk11195-from-an-antagonist-to-an-agonist-of-the-constitutive-androstane-receptor
#2
Bryan Mackowiak, Linhao Li, Matthew A Welch, Daochuan Li, Jace W Jones, Scott Heyward, Maureen A Kane, Peter W Swaan, Hongbing Wang
The constitutive androstane receptor (CAR) plays an important role in xenobiotic metabolism, energy homeostasis, and cell proliferation. Antagonism of CAR represents a key strategy for studying its function and may have potential clinical applications. However, specific human CAR (hCAR) antagonists are limited and conflicting data on the activity of these compounds have been reported. PK11195, a typical peripheral benzodiazepine receptor ligand, has been established as a potent hCAR deactivator in immortalized cells; whether it inhibits hCAR activity under physiologically-relevant conditions remains unclear...
April 25, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28441497/development-of-a-biorelevant-material-sparing-membrane-flux-test-for-rapid-screening-of-bioavailability-enhancing-drug-product-formulations
#3
Aaron M Stewart, Michael E Grass, Deanna M Mudie, Michael M Morgen, Dwayne T Friesen, David T Vodak
Bioavailability-enhancing formulations are often used to overcome challenges of poor gastrointestinal solubility for drug substances developed for oral administration. Conventional in vitro dissolution tests often do not properly compare such formulations due to the many different drug species that may exist in solution. To overcome these limitations, we have designed a practical in vitro membrane flux test, requiring minimal active pharmaceutical ingredient (API) and capable of rapidly screening many drug product intermediates...
April 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28436281/terfenadine-t-butyl-hydroxylation-catalyzed-by-human-and-marmoset-cytochrome-p450-3a-and-4f-enzymes-in-livers-and-small-intestines
#4
Shotaro Uehara, Yukako Yuki, Yasuhiro Uno, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
1. Roles of human cytochrome P450 (P450) 3A4 in oxidation of an antihistaminic drug terfenadine have been previously investigated in association with terfenadine-ketoconazole interaction. Several antihistamine drugs have been recently identified as substrates for multiple P450 enzymes. In this study, overall roles of P450 3A4, 2J2, and 4F12 enzymes in terfenadine t-butyl hydroxylation were investigated in small intestines and livers from humans, marmosets, and/or cynomolgus monkeys. 2. Human liver microsomes and liver and small intestine microsomes from marmosets and cynomolgus monkeys effectively mediated terfenadine t-butyl hydroxylation...
April 22, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28432535/exploring-the-carbamazepine-interaction-with-human-pregnane-x-receptor-and-effect-on-abcc2-using-in-vitro-and-in-silico-approach
#5
Gurpreet K Grewal, Khuraijam D Singh, Neha Kanojia, Chitra Rawat, Samiksha Kukal, Ajay Jajodia, Anshika Singhal, Richa Misra, Selvaraman Nagamani, Karthikeyan Muthusamy, Ritushree Kukreti
PURPOSE: Over expression of ATP-binding cassette transporters is considered one of the major reasons for non-responsiveness to antiepileptic drugs. Carbamazepine (CBZ), one of first line antiepileptic drug is known to influence ABCC2 expression but its exact molecular mechanism is unknown. METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay...
April 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28418693/validating-the-predicted-effect-of-astemizole-and-ketoconazole-using-a-drosophila-model-of-parkinson-s-disease
#6
Katarzyna Styczyńska-Soczka, Luigi Zechini, Lysimachos Zografos
Parkinson's disease is a growing threat to an ever-ageing population. Despite progress in our understanding of the molecular and cellular mechanisms underlying the disease, all therapeutics currently available only act to improve symptoms and do not stop the disease process. It is therefore imperative that more effective drug discovery methods and approaches are developed, validated, and used for the discovery of disease-modifying treatments for Parkinson's. Drug repurposing has been recognized as being equally as promising as de novo drug discovery in the field of neurodegeneration and Parkinson's disease specifically...
April 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28407186/antimicrobial-activity-and-chemical-composition-of-brunfelsia-uniflora-flower-oleoresin-extracted-by-supercritical-carbon-dioxide
#7
L C T Thiesen, E Y Y Sugauara, V Tešević, J Glamočlija, M Soković, J E Gonçalves, Z C Gazim, G A Linde, N B Colauto
Brunfelsia genus is traditionally utilized in popular medicine due to its antibacterial and antifungal properties to name but a few. However, studies on the antimicrobial activity of Brunfelsia uniflora flower oleoresin have not been found yet. This study aimed to evaluate the chemical composition and antimicrobial activity of B. uniflora flower oleoresin obtained by supercritical carbon dioxide. Oleoresin from the plant dried flowers was obtained by carbon dioxide, and the chemical composition was analyzed by gas chromatographic-mass spectrometry...
April 13, 2017: Genetics and Molecular Research: GMR
https://www.readbyqxmd.com/read/28381607/antifungal-susceptibility-testing-of-malassezia-spp-with-an-optimized-colorimetric-broth-microdilution-method
#8
Cheryl Leong, Antonino Buttafuoco, Martin Glatz, Philipp P Bosshard
Malassezia is a genus of lipid dependent yeasts. It is associated with common skin diseases such as pityriasis versicolor or atopic dermatitis and can cause systemic infections in immunocompromised individuals. Owing to slow growth and lipid requirements of these fastidious yeasts, convenient and reliable antifungal drug susceptibility testing assays for Malassezia spp. are not widely available. We have therefore optimized a broth microdilution assay for the testing of Malassezia that is based on the assays from CLSI and EUCAST for Candida and other yeasts...
April 5, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28368521/regulation-of-pulsatile-and-entropic-acth-secretion-under-fixed-exogenous-secretagogue-clamps
#9
Ferdinand Roelfsema, Paul Aoun, Paul Y Takahashi, Dana Erickson, Rebecca Yang, Johannes D Veldhuis
Background: Studies of ACTH secretion are hampered by unobservable hypothalamic CRH and AVP pulses. Clamping one of the secretagogues could allow indirect quantification of the impact of the endogenous heterotypic hormone. Methods: Randomized, double-blind, placebo-controlled cross-over study in 28 healthy adults (16 men), mean age 55 yr. Volunteers received leuprolide, followed by placebo or sex-steroid addback. Eucortisolemia was accomplished by oral ketoconazole and continuous iv cortisol administration with 10 h of 10-min sampling...
March 28, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28365198/-how-to-act-when-an-alpha-blocker-is-associated-with-a-potent-inhibitor-of-cyp3a4
#10
N Bensalah, S Garcia, F X Rose, P Bedouch, O Conort, M Juste, R Roubille, B Allenet, M Tod, B Charpiat
OBJECTIVE: Combination of alpha-blockers with potent CYP3A4 inhibitors is either contra-indicated or not recommended. We searched data supporting this classification and guiding prescribers when such an interaction occurs. METHODS: We analyzed reports published by the French agency for drug safety, reference books and performed search in databases of pharmacokinetics studies and case or case series related with these interactions. RESULTS: The classification of the potential severity of these interactions defined by the French agency for drug safety evolved over time...
March 29, 2017: Progrès en Urologie
https://www.readbyqxmd.com/read/28361556/fungicide-xylaria-sp-bcc-1067-extract-induces-reactive-oxygen-species-and-activates-multidrug-resistance-system-in-saccharomyces-cerevisiae
#11
Pichayada Somboon, Attaporn Poonsawad, Songsak Wattanachaisaereekul, Laran T Jensen, Masakazu Niimi, Supapon Cheevadhanarak, Nitnipa Soontorngun
AIM: To investigate antifungal potential of Xylaria sp. BIOTEC culture collection (BCC) 1067 extract against the model yeast Saccharomyces cerevisiae. MATERIALS & METHODS: Antifungal property of extract, reactive oxygen species levels and cell survival were determined, using selected deletion strains. RESULTS: Extract showed promising antifungal effect with minimal inhibitory concentration100 and minimal fungicidal concentration of 500 and 1000 mg/l, respectively...
April 2017: Future Microbiology
https://www.readbyqxmd.com/read/28358331/absorption-metabolic-stability-and-pharmacokinetics-of-ginger-phytochemicals
#12
Rao Mukkavilli, Chunhua Yang, Reenu Singh Tanwar, Ahmed Ghareeb, Latika Luthra, Ritu Aneja
We have previously demonstrated promising anticancer efficacy of orally-fed whole ginger extract (GE) in preclinical prostate models emphasizing the importance of preservation of the natural "milieu". Essentially, GE primarily includes active ginger phenolics viz., 6-gingerol (6G), 8-gingerol (8G), 10-gingerol (10G), and 6-shogaol (6S). However, the druglikeness properties of active GE phenolics like solubility, stability, and metabolic characteristics are poorly understood. Herein, we determined the physicochemical and biochemical properties of GE phenolics by conducting in vitro assays and mouse pharmacokinetic studies with and without co-administration of ketoconazole (KTZ)...
March 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28346364/new-benzimidazole-1-2-4-triazole-hybrid-compounds-synthesis-anticandidal-activity-and-cytotoxicity-evaluation
#13
Hülya Karaca Gençer, Ulviye Acar Çevik, Serkan Levent, Begüm Nurpelin Sağlık, Büşra Korkut, Yusuf Özkay, Sinem Ilgın, Yusuf Öztürk
Owing to the growing need for antifungal agents, we synthesized a new series 2-((5-(4-(5-substituted-1H-benzimidazol-2-yl)phenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)-1-(substitutedphenyl)ethan-1-one derivatives, which were tested against Candida species. The synthesized compounds were characterized and elucidated by FT-IR, ¹H-NMR, (13)C-NMR and HR-MS spectroscopies. The synthesized compounds were screened in vitro anticandidal activity against Candida species by broth microdiluation methods. In vitro cytotoxic effects of the final compounds were determined by MTT assay...
March 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28345929/utility-of-cyp3a4-and-pxr-car-cyp3a4-3a7-transgenic-mouse-models-to-assess-the-magnitude-of-cyp3a4-mediated-drug-drug-interactions
#14
Justin Q Ly, Kirsten Messick, Ann Qin, Ryan H Takahashi, Edna F Choo
Species differences in the expression, activity, regulation, and substrate specificity of metabolizing enzymes preclude the use of animal models to predict clinical drug-drug interactions (DDIs). The objective of this work is to determine if the transgenic (Tg) Cyp3a(-/-)Tg-3A4Hep/Int and Nr1i2/Nr1i3(-/-)-Cyp3a(-/-)Tg-PXR-CAR-3A4/3A7Hep/Int (PXR-CAR-CYP3A4/3A7) mouse models could be used to predict in vivo DDI of 10 drugs; alprazolam, bosutinib, crizotinib, dasatinib, gefitinib, ibrutinib, regorafenib, sorafenib, triazolam, and vandetinib (as victims); with varying magnitudes of reported CYP3A4 clinical DDI...
April 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28340497/p450-inhibitor-ketoconazole-increased-the-intratumor-drug-levels-and-antitumor-activity-of-fenretinide-in-human-neuroblastoma-xenograft-models
#15
Lluis Lopez-Barcons, Barry J Maurer, Min H Kang, C Patrick Reynolds
We previously reported that concurrent ketoconazole, an oral anti-fungal agent and P450 enzyme inhibitor, increased plasma levels of the cytotoxic retinoid, fenretinide (4-HPR) in mice. We have now determined the effects of concurrent ketoconazole on 4-HPR cytotoxic dose-response in four neuroblastoma (NB) cell lines in vitro and on 4-HPR activity against two cell line-derived, subcutaneous NB xenografts (CDX) and three patient-derived NB xenografts (PDX). Cytotoxicity in vitro was assessed by DIMSCAN assay...
March 24, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28339378/stability-of-allopurinol-amitriptyline-hydrochloride-carbamazepine-domperidone-isoniazid-ketoconazole-lisinopril-naproxen-paracetamol-acetaminophen-and-sertraline-hydrochloride-in-syrspend-sf-ph4-oral-suspensions
#16
Hudson C Polonini, Sharlene Loures, Edson Peter de Araujo, Marcos Antônio F Brandão, Anderson O Ferreira
Oral liquids are safe alternatives to solid dosage forms, notably for elderly and pediatric patients that present dysphagia. The use of ready-to-use suspending vehicles such as SyrSpend SF PH4 is a suitable resource for pharmacists as they constitute a safe and timesaving option that has been studied often. The objective of this study was to evaluate the stability of 10 commonly used active pharmaceutical ingredients (allopurinol 20 mg/mL; amitriptyline hydrochloride 10 mg/mL; carbamazepine 25 mg/mL; domperidone 5 mg/mL; isoniazid 10 mg/mL; ketoconazole 20 mg/mL; lisinopril 1 mg/mL; naproxen 25 mg/mL; paracetamol [acetaminophen] 50 mg/mL; and sertraline hydrochloride 10 mg/mL) compounded in oral suspensions using SyrSpend SF PH4 as the vehicle throughout the study period and stored both at controlled refrigerated (2°C to 8°C) and room temperature (20°C to 25°C)...
September 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28335386/revisiting-the-metabolism-and-bioactivation-of-ketoconazole-in-human-and-mouse-using-liquid-chromatography-mass-spectrometry-based-metabolomics
#17
Ju-Hyun Kim, Won-Gu Choi, Sangkyu Lee, Hye Suk Lee
Although ketoconazole (KCZ) has been used worldwide for 30 years, its metabolic characteristics are poorly described. Moreover, the hepatotoxicity of KCZ limits its therapeutic use. In this study, we used liquid chromatography-mass spectrometry-based metabolomics to evaluate the metabolic profile of KCZ in mouse and human and identify the mechanisms underlying its hepatotoxicity. A total of 28 metabolites of KCZ, 11 of which were novel, were identified in this study. Newly identified metabolites were classified into three categories according to the metabolic positions of a piperazine ring, imidazole ring, and N-acetyl moiety...
March 13, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28332874/long-term-outcome-of-the-different-treatment-alternatives-for-recurrent-and-persistent-cushing-s-disease
#18
Ana Laura Espinosa-de-Los-Monteros, Ernesto Sosa-Eroza, Etual Espinosa, Victoria Mendoza, Rocio Arreola, Moises Mercado
BACKGROUND: Treatment alternatives for persistent and recurrent Cushing's disease (CD) include pituitary surgical reintervention, radiotherapy, pharmacotherapy and bilateral adrenalectomy (BA). The decision of which of these alternatives is better suited for the individual patient rests on clinical judgment and the availability of resources. OBJECTIVE: To evaluate the long-term efficacy of the different secondary interventions for persistent and recurrent Cushing's disease...
March 23, 2017: Endocrine Practice
https://www.readbyqxmd.com/read/28331311/a-potential-in-situ-gel-formulation-loaded-with-novel-fabricated-poly-lactide-co-glycolide-nanoparticles-for-enhancing-and-sustaining-the-ophthalmic-delivery-of-ketoconazole
#19
Tarek Abdelnapy Ahmed, Bader M Aljaeid
Oral ketoconazole therapy is commonly associated with serious hepatotoxicity. Improving ocular drug delivery could be sufficient to treat eye fungal infections. The purpose of this study was to develop optimized ketoconazole poly(lactide-co-glycolide) nanoparticles (NPs) with subsequent loading into in situ gel (ISG) formulation for ophthalmic drug delivery. Three formulation factors were optimized for their effect on particle size (Y1) and entrapment efficiency (Y2) utilizing central composite experimental design...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28329820/hepatocellular-toxicity-of-imidazole-and-triazole-antimycotic-agents
#20
Patrizia Haegler, Lorenz Joerin, Stephan Krähenbühl, Jamal Bouitbir
Hepatotoxicity has been described for all antimycotic azoles currently marketed. A possible mechanism involving mitochondrial dysfunction has been postulated for ketoconazole, but not for the other azoles. The aim of the current investigations was to study the toxicity of different azoles in human cell models and to find out mechanisms of their toxicity. In HepG2 cells, posaconazole and ketoconazole were cytotoxic starting at 20 and 50 µM and decreased the cellular ATP content starting at 5 and 10 µM, respectively...
January 27, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
keyword
keyword
40820
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"