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ketoconazole

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https://www.readbyqxmd.com/read/29155491/variation-in-the-response-of-clozapine-biotransformation-pathways-in-human-hepatic-microsomes-to-cyp1a2-and-cyp3a4-selective-inhibitors
#1
Michael Murray, Wei V Zhang, Robert J Edwards
The atypical antipsychotic agent clozapine (CLZ) is effective in many patients who are resistant to conventional antipsychotic drugs. Cytochromes P450 (CYPs) 1A2 and 3A4 oxidise CLZ to norCLZ and CLZ N-oxide in human liver. Concurrent treatment with inducers and inhibitors of CYP1A2 modulates CLZ elimination that disrupts therapy. Drug-drug interactions involving CYP3A4 are also significant but less predictable. To further characterise the factors underlying these interactions, we used samples from a cohort of human livers to assess variation in CLZ oxidation pathways in relation to intrinsic CYP3A4 and CYP1A2 activities and the effects of the corresponding selective inhibitors ketoconazole (0...
November 20, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29154400/a-chiral-enantioseparation-generic-strategy-for-anti-alzheimer-and-antifungal-drugs-by-short-end-injection-capillary-electrophoresis-using-an-experimental-design-approach
#2
Ahmed M Abdel-Megied, Rasha S Hanafi, Hassan Y Aboul-Enein
The present study describes a generic strategy using capillary electrophoretic (CE) method for chiral enantioseparation of anti-Alzheimer drugs, namely, donepezil (DON), rivastigmine (RIV), and antifungal drugs, namely, ketoconazole (KET), Itraconazole (ITR), fluconazole (FLU), and sertaconazole (SRT) in which these drugs have different basic and acidic properties. Several modified cyclodextrins (CDs) were applied for enantioseparation of racemates such as highly sulfated α, γ CDs, hydroxyl propyl-β-CD, and Sulfobutyl ether-β-CD...
November 20, 2017: Chirality
https://www.readbyqxmd.com/read/29143966/drug-interaction-at-herg-channel-in-vitro-assessment-of-the-electrophysiological-consequences-of-drug-combinations-and-comparison-against-theoretical-models
#3
Barbara Wiśniowska, Bartosz Lisowski, Magdalena Kulig, Sebastian Polak
Drugs carry a proarrhythmic risk, which gets even greater when they are used in combination. In vitro assessment of the proarrhythmic potential of drugs is limited to one compound and thus neglects the potential of drug-drug interactions, including those involving active metabolites. Here we present the results of an in vitro study of potential drug-drug interactions at the level of the hERG channel for the combination of up to three compounds: loratadine, desloratadine and ketoconazole. Experiments were performed at room temperature on an automated patch-clamp device CytoPatch 2, with the use of heterogeneously, stably transfected HEK cells...
November 16, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29138059/pityrosporum-folliculitis-a-retrospective-review-of-110-cases
#4
Brea Prindaville, Leah Belazarian, Nikki A Levin, Karen Wiss
BACKGROUND: Pityrosporum folliculitis is an under-recognized eruption of the face and upper trunk that may be confused with, or occur simultaneously with, acne vulgaris. OBJECTIVE: We sought to characterize risk factors for Pityrosporum folliculitis, its clinical presentation, and response to treatment. METHODS: A retrospective chart review was performed on all patients aged 0 to 21 years seen from 2010-2015 with Pityrosporum folliculitis confirmed by potassium hydroxide (KOH) preparation...
November 11, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29137864/synthesis-molecular-docking-and-qsar-study-of-sulfonamide-based-indoles-as-aromatase-inhibitors
#5
Ratchanok Pingaew, Prasit Mandi, Veda Prachayasittikul, Supaluk Prachayasittikul, Somsak Ruchirawat, Virapong Prachayasittikul
Thirty four of indoles bearing sulfonamides (11-44) were synthesized and evaluated for their anti-aromatase activities. Interestingly, all indole derivatives inhibited the aromatase with IC50 range of 0.7-15.3 μM. Indoles (27-36) exerted higher aromatase inhibitory activity than that of ketoconazole. The phenoxy analogs 28 and 34 with methoxy group were shown to be the most potent compounds with sub-micromolar IC50 values (i.e., 0.7 and 0.8 μM, respectively) without affecting to the normal cell line. Molecular docking demonstrated that the indoles 28, 30 and 34 could occupy the same binding site on the aromatase pocket and share several binding residues with those of the natural substrate (androstenedione), which suggested the competitive binding could be the mode of inhibition of the compounds...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29135059/effect-of-incorporation-of-antifungal-agents-on-the-ultimate-tensile-strength-of-temporary-soft-denture-liners
#6
Karin Hermana Neppelenbroek, Jozely Francisca Mello Lima, Juliana Hotta, Lucas Lulo Galitesi, Ana Lucia Pompéia Fraga Almeida, Vanessa Migliorini Urban
PURPOSE: To investigate the ultimate tensile strength of temporary soft denture liners modified by minimum inhibitory concentrations (MICs) of antifungal agents for Candida albicans biofilm (SC5314) determined in previous microbiological research. MATERIALS AND METHODS: Dumbbell-shaped specimens (n = 7) with a central cross-sectional area of 6 × 3 × 33 mm were produced by Softone and Trusoft, without (control) or with incorporation of drugs in powder form at MICs for C...
November 14, 2017: Journal of Prosthodontics: Official Journal of the American College of Prosthodontists
https://www.readbyqxmd.com/read/29129847/effects-of-ketoconazole-on-cyclophosphamide-metabolism-evaluation-of-cyp3a4-inhibition-effect-using-the-in-vitro-and-in-vivo-models
#7
Le Yang, Chenyang Yan, Feng Zhang, Bo Jiang, Shouhong Gao, Youtian Liang, Lifeng Huang, Wansheng Chen
Cyclophosphamide (CP) is widely used in anticancer therapy regimens and 2-dechloroethylcyclophosphamide (DECP) is its side-chain dechloroethylated metabolite. N-dechloroethylation of CP mediated by the enzyme CYP3A4 yields nephrotoxic and neurotoxic chloroacetaldehyde (CAA) in equimolar amount to DECP. This study aimed to evaluate the inhibitory effect of ketoconazole (KTZ) on CP metabolism through in vitro and in vivo drug-drug interaction (DDI) research. Long-term treatment of KTZ induces hepatic injury; thus single doses of KTZ at low, middle, and high levels (10, 20, and 40 mg/kg) were investigated for pharmacokinetic DDI with CP...
November 13, 2017: Experimental Animals
https://www.readbyqxmd.com/read/29117990/simultaneous-physiologically-based-pharmacokinetic-pbpk-modeling-of-parent-and-active-metabolites-to-investigate-complex-cyp3a4-drug-drug-interaction-potential-a-case-example-of-midostaurin
#8
Helen Gu, Catherine Dutreix, Sam Rebello, Taoufik Ouatas, Lai Wang, Dung Yu Chun, Heidi J Einolf, Handan He
Midostaurin (PKC412) is being investigated for the treatment of acute myeloid leukemia (AML) and advanced systemic mastocytosis (advSM). It is extensively metabolized by cytochrome P450 (CYP) 3A4 to form 2 major active metabolites, CGP52421 and CGP62221. In vitro and clinical drug-drug interaction (DDI) studies indicated that midostaurin and its metabolites are substrates, reversible and time-dependent inhibitors, and inducers of CYP3A4. A simultaneous pharmacokinetic model of parent and active metabolites was initially developed by incorporating data from in vitro, preclinical, and clinical pharmacokinetic studies in healthy volunteers and in patients with AML or advSM...
November 8, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29102550/a-physiologically-based-pharmacokinetic-modeling-approach-to-predict-drug-drug-interactions-of-buprenorphine-after-subcutaneous-administration-of-cam2038-with-perpetrators-of-cyp3a4
#9
Tao Liu, Jogarao V S Gobburu
CAM2038, FluidCrystral (FC) injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research is to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physiologically based pharmacokinetic (PBPK) modeling. A PBPK model was developed for CAM2038 based on the previously published buprenorphine PBPK model after intravenous (IV) and sublingual (SL) administration and the PK profiles after SC administration of CAM2038 from two Phase I clinical trials...
November 1, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29098603/development-of-guanfacine-extended-release-dosing-strategies-in-children-and-adolescents-with-adhd-using-a-physiologically-based-pharmacokinetic-model-to-predict-drug-drug-interactions-with-moderate-cyp3a4-inhibitors-or-inducers
#10
Aiqun Li, Karen Yeo, Devin Welty, Haojing Rong
BACKGROUND: Guanfacine extended-release (GXR) is an orally administered, non-stimulant treatment for children and adolescents with attention-deficit/hyperactivity disorder (ADHD) and is primarily metabolized by the 3A4 isozyme of cytochrome P450 (CYP3A4). The results of clinical pharmacokinetic (PK) studies indicate that guanfacine is sensitive to drug-drug interactions (DDIs) perpetrated by strong inhibitors and inducers of CYP3A4. OBJECTIVE: The aim was to provide guidance on the possible requirement for GXR dose adjustment in children and adolescents with ADHD by predicting DDIs following co-administration with moderate CYP3A4 inhibitors and inducers...
November 2, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/29097142/exploring-the-feasibility-of-the-use-of-biopolymers-as-a-carrier-in-the-formulation-of-amorphous-solid-dispersions-part-i-gelatin
#11
Timothy Pas, Bjorn Vergauwen, Guy Van den Mooter
Biopolymers have rarely been used so far as carriers in the formulation of amorphous solid dispersions (ASD) to overcome poor solubility of active pharmaceutical ingredients (APIs). In an attempt to enlarge our knowledge on this topic, gelatin, type 50PS was selected. A screening study was initiated in which twelve structurally different poorly soluble biopharmaceutical classification system (BCS) Class II drugs (carbamazepine, cinnarizine, diazepam, itraconazole, nifedipine, indomethacin, darunavir (ethanolate), ritonavir, fenofibrate, griseofulvin, ketoconazole and naproxen) were selected for evaluation...
October 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29080856/formulation-and-evaluation-of-selected-transmucosal-dosage-forms-containing-a-double-fixed-dose-of-acyclovir-and-ketoconazole
#12
Joe M Viljoen, Danélia Botes, Jan H Steenekamp
Viral and fungal dermatological manifestations are often the first and only sign of HIV/AIDS. They are cosmetically disfiguring and threaten the quality of life, but can be treated by acyclovir and ketoconazole, correspondingly. This study attempted the formulation of stable, double fixed-dose acyclovir and ketoconazole novel transmucosal dosage forms, which are able to provide an efficient flux for both compounds. A cream, gel and lip balm formulation containing both drugs were formulated that can be applied to mucosal tissue...
November 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29076676/adrenal-insufficiency-in-pakistani-hiv-infected-patients
#13
Bahjat Afreen, Khurshid Ahmed Khan, Amna Riaz
BACKGROUND: Adrenal insufficiency (AI) is the most common endocrine complication among patients with AIDS/HIV infection and there are number of causes of AI in HIV patients. Human immunodeficiency virus directly as well as indirectly destroys adrenal glands. The estimates of its prevalence and severity vary. AI is the most life threatening but readily correctable endocrine complication that occurs in persons with HIV infection. This study was carried out to determine the frequency of Adrenal Insufficiency in HIV patients and their clinical features as proper diagnosis and timely treatment have been shown to improve quality of life and long-term mortality in AIDS patients...
July 2017: Journal of Ayub Medical College, Abbottabad: JAMC
https://www.readbyqxmd.com/read/29076107/pharmacokinetic-evaluation-of-the-interactions-of-amenamevir-asp2151-with-ketoconazole-rifampicin-midazolam-and-warfarin-in-healthy-adults
#14
Tomohiro Kusawake, Martin den Adel, Dorien Groenendaal-van de Meent, Alberto Garcia-Hernandez, Akitsugu Takada, Kota Kato, Yoshiaki Ohtsu, Masataka Katashima
INTRODUCTION: Amenamevir is a nonnucleoside antiherpes virus compound available for treating herpes zoster infections. Four studies aimed to determine any potential interactions between amenamevir and ketoconazole, rifampicin, midazolam, or warfarin in healthy male participants. METHODS: Two studies were open-label studies that evaluated the effects of multiple doses of ketoconazole (400 mg) and rifampicin (600 mg) on the pharmacokinetics of a single oral dose of amenamevir...
October 26, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/29062248/evaluation-of-candida-species-and-antifungal-susceptibilities-among-children-with-invasive-candidiasis
#15
Murat Sütçü, Manolya Acar, Gonca Erköse Genç, İlknur Kökçü, Hacer Aktürk, Gürkan Atay, Selda Hançerli Törun, Nuran Salman, Zayre Erturan, Ayper Somer
AIM: Non-albicans Candida species and resistant microorganisms have been more commonly isolated in invasive candidiasis in recent years. The aim of this study was to evaluate the distrubution of Candida spp and antifungal resistance in our clinic. MATERIAL AND METHODS: Fifty-four Candida isolates and antifungal susceptibility results obtained from patients diagnosed as having invasive candidiasis between December 2012 and June 2016 were included. Clinical and laboratory data were retrospectively analyzed...
September 2017: Türk Pediatri Arşivi
https://www.readbyqxmd.com/read/29061761/antileishmanial-efficacy-and-pharmacokinetics-of-db766-azole-combinations
#16
April C Joice, Sihyung Yang, Abdelbasset A Farahat, Heidi Meeds, Mei Feng, Junan Li, David W Boykin, Michael Zhuo Wang, Karl A Werbovetz
Given the limitations of current antileishmanial drugs and the utility of oral combination therapy for other infections, developing an oral combination against visceral leishmaniasis should be a high priority. In vitro combination studies with DB766 and antifungal azoles against intracellular L. donovani showed that posaconazole and ketoconazole, but not fluconazole, enhanced DB766 potency. Pharmacokinetic analysis of DB766-azole combinations in uninfected Swiss Webster mice revealed that DB766 exposure was increased by higher posaconazole and ketoconazole doses, while DB766 decreased ketoconazole exposure...
October 23, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29050342/role-of-the-cyp3a4-mediated-11-12-epoxyeicosatrienoic-acid-pathway-in-the-development-of-tamoxifen-resistant-breast-cancer
#17
Nguyen Thi Thuy Phuong, Ji Won Kim, Jung-Ae Kim, Jang Su Jeon, Ji-Yoon Lee, Wen Jun Xu, Jin Won Yang, Sang Kyum Kim, Keon Wook Kang
Epoxyeicosatrienoic acid (EET) production via cytochrome P450 (CYP) epoxygenases closely correlates with the progression of breast cancer. However, its role in the development of chemoresistant breast cancers has yet to be elucidated. Here, we found that CYP3A4 expression and its epoxy-product, 11,12-epoxyeicosatrienoic acid (11,12-EET) was enhanced in tamoxifen (TAM)-resistant MCF-7 (TAMR-MCF-7) breast cancer cells compared to control MCF-7 cells. Treatment of TAMR-MCF-7 cells with ketoconazole and azamulin (selective CYP3A4 inhibitors) or 14,15-epoxyeicosa-5(Z)-enoic acid (14,15-EEZE, an EET antagonist) inhibited cellular proliferation and recovered the sensitivity to 4-hydroxytamoxifen...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29049452/hsd3b1-and-response-to-a-nonsteroidal-cyp17a1-inhibitor-in-castration-resistant-prostate-cancer
#18
Nima Almassi, Chad Reichard, Jianbo Li, Carly Russell, Jaselle Perry, Charles J Ryan, Terence Friedlander, Nima Sharifi
Importance: The HSD3B1 (1245C) germline variant encodes for a gain-of-function missense in 3β-hydroxysteroid dehydrogenase isoenzyme 1 (3βHSD1) that results in increased dihydrotestosterone synthesis from extragonadal precursors and is predictive of more rapid progression to castration-resistant prostate cancer (CRPC). Objective: To determine whether the HSD3B1 (1245C) genotype is predictive of clinical response to extragonadal androgen ablation with nonsteroidal 17α-hydroxylase/17,20-lyase (CYP17A1) inhibition in men with metastatic CRPC...
October 12, 2017: JAMA Oncology
https://www.readbyqxmd.com/read/29049321/determination-and-production-of-antimicrobial-compounds-by-aspergillus-clavatonanicus-strain-mj31-an-endophytic-fungus-from-mirabilis-jalapa-l-using-uplc-esi-ms-ms-and-td-gc-ms-analysis
#19
Vineet Kumar Mishra, Ajit Kumar Passari, Preeti Chandra, Vincent Vineeth Leo, Brijesh Kumar, Sivakumar Uthandi, Sugitha Thankappan, Vijai Kumar Gupta, Bhim Pratap Singh
Endophytic fungi associated with medicinal plants are reported as potent producers of diverse classes of secondary metabolites. In the present study, an endophytic fungi, Aspergillus clavatonanicus strain MJ31, exhibiting significant antimicrobial activity was isolated from roots of Mirabilis jalapa L., was identified by sequencing three nuclear genes i.e. internal transcribed spacers ribosomal RNA (ITS rRNA), 28S ribosomal RNA (28S rRNA) and translation elongation factor 1- alpha (EF 1α). Ethyl acetate extract of strain MJ31displayed significant antimicrobial potential against Bacillus subtilis, followed by Micrococccus luteus and Staphylococcus aureus with minimum inhibitory concentrations (MIC) of 0...
2017: PloS One
https://www.readbyqxmd.com/read/29046138/usefulness-of-simultaneous-measurement-of-plasma-steroids-including-precursors-for-the-evaluation-of-drug-effects-on-adrenal-steroidogenesis-in-rats
#20
Tomoaki Tochitani, Akihito Yamashita, Izumi Matsumoto, Mami Kouchi, Yuta Fujii, Izuru Miyawaki, Toru Yamada, Kiyoko Bando
The aim of this study was to evaluate the usefulness of simultaneous measurement of plasma steroids, including precursors, for the evaluation of drug effects on adrenal steroidogenesis in vivo. Plasma concentrations of corticosterone and its precursors were examined in rats dosed with compounds that affect adrenal steroidogenesis via different modes of action as well as the relationships of the changes with blood chemistry and adrenal histopathology. Male rats were dosed with tricresyl phosphate, aminoglutethimide, trilostane (TRL), metyrapone (MET), ketoconazole (KET), or mifepristone for 7 days...
August 2017: Toxicologic Pathology
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