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ketoconazole

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https://www.readbyqxmd.com/read/28335386/revisiting-the-metabolism-and-bioactivation-of-ketoconazole-in-human-and-mouse-using-liquid-chromatography-mass-spectrometry-based-metabolomics
#1
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
#2
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
#3
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
#4
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
https://www.readbyqxmd.com/read/28328532/cushing-s-syndrome-in-infancy-due-to-ectopic-acth-secretion-by-a-sacro-coccygeal-teratoma
#5
Marta Rydzewska, Maryna Krawczuk-Rybak, Adrianna Zajkowska, Natalia Jurczuk, Dariusz Polnik, Mieczysław Szalecki, Elżbieta Moszczyńska, Martin O Savage, Artur Bossowski
BACKGROUND: Adenocorticotropic hormone (ACTH)-dependent Cushing's syndrome in infancy is extremely rare. We describe the case of a sacro-coccygeal ectopic ACTH-secreting immature teratoma in an infant who also presented the triad of defects characteristic of Currarino syndrome. CASE PRESENTATION: A girl was born with a large immature teratoma in the sacro-coccygeal region associated with anal atresia. At the age of 7 days, the concentration of α-fetoprotein (AFP) was above the age-specific normal range...
March 22, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
https://www.readbyqxmd.com/read/28325334/citric-acid-crosslinked-%C3%AE-cyclodextrin-carboxymethylcellulose-hydrogel-films-for-controlled-delivery-of-poorly-soluble-drugs
#6
Vishwajeet Sampatrao Ghorpade, Adhikrao Vyankatrao Yadav, Remeth Jacky Dias
Citric acid crosslinked β-cyclodextrin-carboxymethylcellulose (βCD-CMC) hydrogel films were prepared by esterification-crosslinking method for the controlled release of ketoconazole (model drug). The hydrogel films were evaluated for active βCD content, carboxyl content, swelling ratio, drug loading and release, and hemolytic activity. The structural characterization was carried out using solid state (13)C NMR, ATR-FTIR, TGA and DSC analysis. The βCD-CMC hydrogel films showed increase in active βCD content swelling ratio and drug loading with increase in the concentration of βCD in the feed...
May 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28277127/a-successful-case-of-pregnancy-in-a-woman-with-acth-independent-cushing-s-syndrome-treated-with-ketoconazole-and-metyrapone
#7
Wojciech Zieleniewski, Renata Michalak
Cushing's syndrome (CS) is a rare disease caused by a chronic excess of cortisol. Hypercortisolaemia may affect reproductive system leading to infertility in women. However, some of the patients remain fertile, although pregnancy is uncommon. In our report, we describe the case of a 31-years old woman suffering from hypertension, oligomenorrhea, easy bruising, muscle weakness and elevated levels of cortisol. During hospitalization, high level of serum cortisol with stiff diurnal rhythm and undetectable plasma ACTH concentration were found...
February 26, 2017: Gynecological Endocrinology
https://www.readbyqxmd.com/read/28275201/physiologically-based-pharmacokinetic-model-of-all-trans-retinoic-acid-with-application-to-cancer-populations-and-drug-interactions
#8
Jing Jing, Cara Nelson, Jisun Paik, Yoshiyuki Shirasaka, John K Amory, Nina Isoherranen
All-trans retinoic acid (atRA) is a front-line treatment for acute promyelocytic leukemia (APL). Due to its activity in regulating the cell cycle, it has also been evaluated for the treatment of other cancers. However, the efficacy of atRA has been limited by atRA inducing its own metabolism during therapy, resulting in a decrease of atRA exposure during continuous dosing. Frequent relapse occurs in patients receiving atRA monotherapy. In an attempt to combat therapy resistance, inhibitors of atRA metabolism have been developed...
March 8, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28270768/extracts-of-immature-orange-aurantii-fructus-immaturus-and-citrus-unshiu-peel-citri-unshiu-pericarpium-induce-p-glycoprotein-and-cytochrome-p450-3a4-expression-via-upregulation-of-pregnane-x-receptor
#9
Naoto Okada, Aki Murakami, Shiori Urushizaki, Misa Matsuda, Kazuyoshi Kawazoe, Keisuke Ishizawa
P-glycoprotein (P-gp) and cytochrome P450 3A4 (CYP3A4) are expressed in the intestine and are associated with drug absorption and metabolism. Pregnane X receptor (PXR) is the key molecule that regulates the expression of P-gp and CYP3A4. Given that PXR activity is regulated by a variety of compounds, it is possible that unknown PXR activators exist among known medicines. Kampo is a Japanese traditional medicine composed of various natural compounds. In particular, immature orange [Aurantii fructus immaturus (IO)] and citrus unshiu peel [Citri unshiu pericarpium (CP)] are common ingredients of kampo...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28263914/the-impact-of-supersaturation-level-for-oral-absorption-of-bcs-class-iib-drugs-dipyridamole-and-ketoconazole-using-in-vivo-predictive-dissolution-system-gastrointestinal-simulator-gis
#10
Yasuhiro Tsume, Kazuki Matsui, Amanda L Searls, Susumu Takeuchi, Gregory E Amidon, Duxin Sun, Gordon L Amidon
The development of formulations and the assessment of oral drug absorption for Biopharmaceutical Classification System (BCS) class IIb drugs is often a difficult issue due to the potential for supersaturation and precipitation in the gastrointestinal (GI) tract. The physiological environment in the GI tract largely influences in vivo drug dissolution rates of those drugs. Thus, those physiological factors should be incorporated into the in vitro system to better assess in vivo performance of BCS class IIb drugs...
March 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28263823/embryotoxic-and-pharmacologic-potency-ranking-of-six-azoles-in-the-rat-whole-embryo-culture-by-morphological-and-transcriptomic-analysis
#11
Myrto Dimopoulou, Aart Verhoef, Jeroen L A Pennings, Bennard van Ravenzwaay, Ivonne M C M Rietjens, Aldert H Piersma
Differential gene expression analysis in the rat whole embryo culture (WEC) assay provides mechanistic insight into the embryotoxicity of test compounds. In our study, we hypothesized that comparative analysis of the transcriptomes of rat embryos exposed to six azoles (flusilazole, triadimefon, ketoconazole, miconazole, difenoconazole and prothioconazole) could lead to a better mechanism-based understanding of their embryotoxicity and pharmacological action. For evaluating embryotoxicity, we applied the total morphological scoring system (TMS) in embryos exposed for 48h...
March 3, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28262031/antifungal-and-antioxidant-activities-of-coleonema-album-and-c-pulchellum-against-skin-diseases
#12
Olufunke O Fajinmi, Jiří Grúz, Petr Tarkowski, Manoj G Kulkarni, Jeffrey F Finnie, Johannes Van Staden
CONTEXT: Coleonema album (Thunb) Bart. & H. L. Wendl (Rutaceae) has been used in the formulation of skincare products, and the Khoisan people rub it on their skin to add luster. Coleonema pulchellum I. Williams has received less attention in the South African traditional medicine. OBJECTIVE: This study investigates the antifungal and antioxidant activities of C. album and C. pulchellum essential oil (EO) and leaf extracts; and analyzes the chemical components of their EOs...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28261269/comparative-hepatotoxicity-of-fluconazole-ketoconazole-itraconazole-terbinafine-and-griseofulvin-in-rats
#13
Star Khoza, Ishmael Moyo, Denver Ncube
Oral ketoconazole was recently the subject of regulatory safety warnings because of its association with increased risk of inducing hepatic injury. However, the relative hepatotoxicity of antifungal agents has not been clearly established. The aim of this study was to compare the hepatotoxicity induced by five commonly prescribed oral antifungal agents. Rats were treated with therapeutic oral doses of griseofulvin, fluconazole, itraconazole, ketoconazole, and terbinafine. After 14 days, only ketoconazole had significantly higher ALT levels (p = 0...
2017: Journal of Toxicology
https://www.readbyqxmd.com/read/28260511/clinically-relevant-drug-interactions-with-anti-alzheimer-s-drugs
#14
Filippo Caraci, Janet Sultana, Filippo Drago, Edoardo Spina
The aging world population had led to an increase in the prevalence of Alzheimer's disease (AD). The drugs used to slow down the onset of AD, galantamine, donepezil, rivastigmine and memantine, are generally well-tolerated. However, drug interactions between these drugs and other drugs are an important aspect of patient safety that should be borne in mind, particularly given the high burden of polypharmacy in the elderly. The aim of this review is to provide an updated review of clinically significant drug-drug interactions concerning drugs approved for AD...
March 3, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28260425/optimizing-immunosuppressive-regimens-among-living-donor-renal-transplant-recipients
#15
Mohamed Adel Bakr, Ayman Maher Nagib, Osama Ashry Gheith, Ahmed Farouk Hamdy, Ayman Fathi Refaie, Ahmed Farouk Donia, Ahmed Hassan Neamatalla, Khaled Farouk Eldahshan, Ahmed Abdelfattah Denewar, Mohamed Hamed Abbas, Amany Ismail Mostafa, Mohamed Ahmed Ghoneim
OBJECTIVES: We review different immunosuppressant protocols used for living-donor kidney transplant recipients at our center. MATERIALS AND METHODS: Many prospective randomized studies from our center have been reported between March 1976 and 2016, with more than 2700 renal transplant procedures conducted. The first study was a prospective randomized trial of azathioprine versus cyclosporine. The second study compared triple therapy (prednisolone + azathioprine + cyclosporine) versus conventional therapy (prednisolone + azathioprine)...
February 2017: Experimental and Clinical Transplantation
https://www.readbyqxmd.com/read/28258218/structural-analyses-of-candida-albicans-sterol-14%C3%AE-demethylase-complexed-with-azole-drugs-address-the-molecular-basis-of-azole-mediated-inhibition-of-fungal-sterol-biosynthesis
#16
Tatiana Y Hargrove, Laura Friggeri, Zdzislaw Wawrzak, Aidong Qi, William J Hoekstra, Robert J Schotzinger, John D York, F Peter Guengerich, Galina I Lepesheva
With some advances in modern medicine (such as cancer chemotherapy, broad exposure to antibiotics, and immunosuppression) the incidence of opportunistic fungal pathogens such as Candida albicans has increased. Cases of drug resistance among these pathogens have become more frequent, requiring the development of new drugs and a better understanding of the targeted enzymes. Sterol 14α-demethylase (CYP51) is a cytochrome P450 enzyme required for biosynthesis of sterols in eukaryotic cells and the major target of clinical drugs for managing fungal pathogens, but some of the CYP51 key features important for rational drug design have remained obscure...
March 3, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28254952/effects-of-microrna-34a-on-the-pharmacokinetics-of-cytochrome-p450-probe-drugs-in-mice
#17
Joseph L Jilek, Ye Tian, Ai-Ming Yu
MicroRNAs (miR) including miR-34a have been shown to regulate nuclear receptor, drug-metabolizing enzyme and transporter gene expression in various cell model systems. However, to what degree miRNAs would affect pharmacokinetics (PK) at the systemic level remains unknown. Additionally, miR-34a replacement therapy represents a new cancer treatment strategy, whereas it is undefined if miR-34a therapeutics would causes any drug-drug interactions (DDI). To address the questions, we developed a practical single-mouse PK approach and investigated the effects of a bioengineered miR-34a agent on the PK of multiple Cytochrome P450 (CYP) probe drugs (midazolam, dextromethorphan, phenacetin, diclofenac, and chlorzoxazone) administered as a cocktail to mouse models...
March 2, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28249055/weakness-and-pain-in-arms-and-legs-%C3%A2-dark-urine-%C3%A2-history-of-vertebral-osteomyelitis-%C3%A2-dx
#18
Antonios Charokopos, Tariq Muhammad, Sidana Surbhi, Andrei Brateanu
Rhabdomyolysis is a serious complication of statin treatment. Both higher statin doses and pharmacokinetic factors can raise statin levels, leading to this serious usclerelated syndrome. Co-administration of statins with drugs that are strong inhibitors of cytochrome P450 (CYP) 3A4 (the main cytochrome P450 isoform that metabolizes most statins) can increase statin levels several fold. The trigger for our patient's statin-induced rhabdomyolysis was fluconazole, a known moderate inhibitor of CYP3A4, which is comparatively weaker than certain potent azoles like itraconazole or ketoconazole...
March 2017: Journal of Family Practice
https://www.readbyqxmd.com/read/28242097/cutaneous-basidiobolomycosis-seven-cases-in-southern-benin
#19
F Atadokpédé, J Gnossikè, H Adégbidi, B Dégboé, Y Sissinto-Savi de Tovè, A Adéyé, C Koudoukpo, A Chauty, D Chabasse, J-P Saint-André, M-T Dieng, M-C Koeppel, H-G Yedomon, F do-Ango-Padonou
BACKGROUND: Cutaneous basidiobolomycosis is the most common form of entomophthoramycosis. Herein we report seven cases of cutaneous basidiobolomycosis. PATIENTS AND METHODS: A retrospective observational study was conducted at the Buruli ulcer treatment centre in Pobè and at the national teaching hospital in Cotonou from 2010 to 2015. RESULTS: Seven cases of cutaneous basidiobolomycosis were diagnosed. The mean patient age was 9.53 years...
February 24, 2017: Annales de Dermatologie et de Vénéréologie
https://www.readbyqxmd.com/read/28238899/estimation-of-the-contribution-of-cyp2c8-and-cyp3a4-in-repaglinide-metabolism-by-human-liver-microsomes-under-various-buffer-conditions
#20
Toshiyuki Kudo, Hitomi Goda, Yuki Yokosuka, Ryo Tanaka, Seina Komatsu, Kiyomi Ito
We have previously reported that the microsomal activities of CYP2C8 and CYP3A4 largely depend on the buffer condition used in in vitro metabolic studies, with different patterns observed between the two isozymes. In the present study, therefore, the possibility of buffer condition dependence of the fraction metabolized by CYP2C8 (fm2C8) for repaglinide, a dual substrate of CYP2C8 and CYP3A4, was estimated using human liver microsomes under various buffer conditions. Montelukast and ketoconazole showed a potent and concentration-dependent inhibition of CYP2C8-mediated paclitaxel 6α-hydroxylation and CYP3A4-mediated triazolam α-hydroxylation, respectively, without dependence on the buffer condition...
February 23, 2017: Journal of Pharmaceutical Sciences
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