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M Cunha-Silva, V N Brito, D B Macedo, D S Bessa, C O Ramos, L G Lima, P S Barroso, I J P Arnhold, D L Segaloff, B B Mendonca, A C Latronico
Testotoxicosis is a rare cause of peripheral precocious puberty in boys caused by constitutively activating mutations of the LHCG receptor. Affected males usually have normal gonadotropin profiles and fertility in their adult life. Here, we described the long-term follow-up of a 24-year-old young man with severe testotoxicosis due to a de novo activating mutation in the third transmembrane helix of the LHCGR (p.Leu457Arg). This patient was treated with different medications, including medroxyprogesterone acetate, ketoconazole, cyproterone acetate and aromatase inhibitor from age 2...
March 12, 2018: Human Reproduction
Shivaprakash M Rudramurthy, Shamanth A Shankarnarayan, Sunil Dogra, Dipika Shaw, Khurram Mushtaq, Raees A Paul, Tarun Narang, Arunaloke Chakrabarti
Dermatophytosis, the commonest superficial fungal infection, has gained recent attention due to its change of epidemiology and treatment failures. Despite availability of several effective antifungal agents against dermatophytes, the incidence of chronic infection, re-infection and treatment failures are on the rise. Trichophyton rubrum and Trichophyton interdigitale are the two frequent clinical isolates in India. Consecutive patients (n=195) with suspected dermatophytosis during second half of 2014 were included in this study...
March 12, 2018: Antimicrobial Agents and Chemotherapy
Michelle H Fung, Kārlis Bērziņš, Raj Suryanarayanan
In an earlier investigation, coamorphous systems of ketoconazole (KTZ) prepared with each oxalic (OXA), tartaric (TAR), citric (CIT) and succinic (SUC) acid, revealed drug-acid ionic and/or hydrogen bonding interactions in the solid-state (Fung et al, Mol Pharmaceutics, 2018, 15(x), xxxx-yyyy). We showed that the drug-acid interactions in KTZ-TAR were the strongest, followed by KTZ-OXA, KTZ-CIT and KTZ-SUC. In this study, we investigated the crystallization propensity and dissolution behavior of the KTZ-acid coamorphous systems...
March 12, 2018: Molecular Pharmaceutics
Ju-Hyun Kim, Won-Gu Choi, Ju-Yeon Moon, Joo Young Lee, Sangkyu Lee, Hye Suk Lee
Itraconazole (ITZ) is a first-generation triazole-containing antifungal agent that effectively treats various fungal infections. As ITZ has a better safety profile than that of ketoconazole (KCZ), ITZ has been used worldwide for over 25 years. However, few reports have explored the metabolic profile of ITZ, and the underlying mechanism of ITZ-induced liver injury is not clearly understood. In the present study, we revisited ITZ metabolism in humans, using a non-targeted metabolomics approach, and identified several novel metabolic pathways including O-dearylation, piperazine oxidation, and piperazine-N,N'-deethylation...
March 7, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Omar Gómez-García, Dulce Andrade-Pavón, Elena Campos-Aldrete, Ricardo Ballinas-Indilí, Alfonso Méndez-Tenorio, Lourdes Villa-Tanaca, Cecilio Álvarez-Toledano
A series of 3-benzoyl imidazo[1,2- a ]pyrimidines, obtained from N -heteroarylformamidines in good yields, was tested in silico and in vitro for binding and inhibition of seven Candida species ( Candida albicans (ATCC 10231), Candida dubliniensis (CD36), Candida glabrata (CBS138), Candida guilliermondii (ATCC 6260), Candida kefyr , Candida krusei (ATCC 6358) and Candida tropicalis (MYA-3404)). To predict binding mode and energy, each compound was docked in the active site of the lanosterol 14α-demethylase enzyme (CYP51), essential for fungal growth of Candida species...
March 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Susana Córdoba, Guillermina Isla, Wanda Szusz, Walter Vivot, Alejandra Hevia, Graciela Davel, Cristina E Canteros
We studied 23 clinical and environmental strains of Sporothrix schenckii sensu lato collected from 1984 to 2017 in Argentina. The molecular identification (partial sequencing of a fragment of the calmodulin gene) of the strains was performed. For the yeast and mycelial phases, the in vitro susceptibility testing by a microdilution reference method was determined against eight antifungal drugs. Strains studied were identified as S. schenckii sensu stricto 13 (56.5%), S. brasiliensis 8 (34.7%) and S. globosa 2 (8...
March 3, 2018: Mycoses
Doreen Luedtke, Kristell Marzin, Arvid Jungnik, Ute von Wangenheim, Claudia Dallinger
BACKGROUND: Nintedanib is a substrate for p-glycoprotein which can impact bioavailability. We investigated the effects of ketoconazole, a p-glycoprotein inhibitor, and rifampicin, a p-glycoprotein inducer, on the pharmacokinetics of nintedanib. METHODS: In the ketoconazole study, 34 healthy subjects received nintedanib 50 mg orally alone and 1 h after the last dose of ketoconazole given orally at a dose of 400 mg once daily for 3 days in 1 of 2 randomized sequences...
March 2, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Dennis M Fisher, Peter Chang, D Russell Wada, Albert Dahan, Pamela P Palmer
BACKGROUND: Desirable product attributes for treatment of moderate-to-severe acute pain in many medically supervised settings are rapid onset and a route of administration not requiring intravenous access. The pharmacokinetic characteristics of sublingually administered tablets containing 15 or 30 µg of sufentanil are described. METHODS: Blood was sampled from healthy subjects (four studies, 122 subjects) and patients (seven studies, 944 patients). Studies in healthy subjects determined bioavailability, effect of inhibition of cytochrome P450 3A4, and the plasma concentration profile with single and hourly sublingual doses...
March 2, 2018: Anesthesiology
Zhao-Yan Zhang, Liang Yang, Xiao-Yan Huang, Mei-Xi Wang, Zeng-Chun Ma, Xiang-Lin Tang, Yu-Guang Wang, Yue Gao
The rapid screening technology was used to investigate the transcriptional regulation effect of main chemical constituents in tubers of Polygonum multiflorum, including 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside(THSG) and anthraquinones (such as rhein, chrysophanol, aloe-emodin, emodin) on CYP3A4 drug inducers induced by human pregnancy X receptor (PXR).The effect of chemical composition on the cell activity was detected by MTS cell viability assay. IC₅₀ was calculated. The expression vector and the reporter vector were co-transfected into HepG2 cells, with 10 μmol•L⁻¹ rifampicin (RIF) as a positive control, and 10 μmol•L⁻¹ ketoconazole (TKZ) as a negative control...
December 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Fawzy Elbarbry, Aimy Ung, Khaled Abdelkawy
Background: Quercetin (QR) and thymoquinone (TQ) are herbal remedies that are currently extensively used by the general population to prevent and treat various chronic conditions. Therefore, investigating the potential of pharmacokinetic interactions caused by the concomitant use of these herbal remedies and conventional medicine is warranted to ensure patient safety. Purpose of the Study: This study was conducted to determine the inhibitory effect of QR and TQ, two commonly used remedies, on the activities of selected cytochrome P450 (CYP) enzymes that play an important role in drug metabolism and/or toxicology...
January 2018: Pharmacognosy Magazine
Jianchao Liu, Xiaoxiang Dan, Guanghua Lu, Jie Shen, Donghai Wu, Zhenhua Yan
Pharmaceutically active compounds (PhACs) recently have been recognized to constitute a health risk for aquatic ecosystems. The major pathways of PhACs to enter the aquatic environment are excretion and discharge of effluents through sewage treatment plants (STPs). The occurrence, bioaccumulation and risk assessment of lipophilic PhACs, including erythromycin, ketoconazole, indomethacin, diclofenac, gemfibrozil, bezafibrate, propranolol, carbamazepine, sertraline and 17α-ethinylestradiol were investigated in a river that receives effluents from STP...
February 21, 2018: Ecotoxicology and Environmental Safety
Jacques Young, Jerome Bertherat, Marie Christine Vantyghem, Olivier Chabre, Salima Senoussi, Rita Chadarevian, Frédéric Castinetti
OBJECTIVE: Ketoconazole (KTZ) is one of few available treatments for Cushing's syndrome (CS). Although KTZ has been associated with severe hepatotoxicity, little information is available about hepatic safety in CS. The aim of this study was to document changes in liver function in patients with CS treated with KTZ. DESIGN: An observational prospective French cohort study (compassionate use programme). METHODS: Enrolled patients were stratified into a KTZ-naive cohort and a cohort already treated by another formulation of ketoconazole (KTZ-switch cohort)...
February 22, 2018: European Journal of Endocrinology
Lauren K Hoffman, Isabelle Raymond, Leon Kircik
BACKGROUND: Tinea pedis is the most common dermatophyte infection. Treatment is critical to alleviate pruritic symptoms, to reduce the risk for secondary bacterial infection, and to limit the spread of infection to other body sites or other individuals. The objective of this study was to compare the abilities of econazole nitrate topical foam, 1% and ketoconazole cream (2%) to reduce pruritus, thus improving quality of life, and to determine patient preference for the foam product versus the cream product in patients with interdigital tinea pedis...
February 1, 2018: Journal of Drugs in Dermatology: JDD
Emma Davidson Peiris, Raghav Wusirika
CYP24A1 is an enzyme that inactivates vitamin D. Loss-of-function mutations in this enzyme are rare but have been linked with idiopathic infantile hypercalcemia as well as adult-onset nephrocalcinosis and nephrolithiasis. Genetic testing for this mutation should be considered in the presence of calciuria, elevated serum calcium, elevated 1,25-dihydroxyvitamin D, and suppressed parathyroid hormone. We present a case with these lab findings as well as an elevated 25-hydroxyvitamin D/24,25-dihydroxyvitamin D ratio in whom compound heterozygous CYP24A1 mutations were found...
September 2017: Case Reports in Nephrology and Dialysis
Ruijuan Xu, Weihong Ge, Qing Jiang
PURPOSE: Rivaroxaban is a direct oral anticoagulant with a large inter-individual variability. The present study is to develop a physiologically based pharmacokinetic (PBPK) model to predict several scenarios in clinical practice. METHODS: A whole-body PBPK model for rivaroxaban, which is metabolized by the cytochrome P450 (CYP) 3A4/5, 2J2 pathways and excreted via kidneys, was developed to predict the pharmacokinetics at different doses in healthy subjects and patients with hepatic or renal dysfunction...
February 17, 2018: European Journal of Clinical Pharmacology
Ken-Ichi Umehara, Felix Huth, Christina S Won, Tycho Heimbach, Handan He
Ritonavir is one of several ketoconazole alternatives used to evaluate strong CYP3A4 inhibition potential in clinical drug-drug interaction (DDI) studies. In this study, four physiologically-based pharmacokinetic (PBPK) models of ritonavir as an in vivo time-dependent inhibitor of CYP3A4 were created and verified for the oral doses of 20, 50, 100 and 200 mg using fraction absorbed (Fa) and oral clearance (CLoral) values reported in the literature, as transporter and CYP enzyme reaction phenotyping data were not available...
February 16, 2018: Biopharmaceutics & Drug Disposition
Elena Valassi, Holger Franz, Thierry Brue, Richard A Feelders, Romana T Netea-Maier, Stylianos Tsagarakis, Susan M Webb, Maria Kostadinova Yaneva, Martin Reincke, Michael Droste, Irina Komerdus, Dominique Maiter, Darko Kastelan, Philippe Chanson, Marija Pfeifer, Christian J Strasburger, Miklos Toth, Olivier Chabre, Michal Krsek, Carmen Fajardo Montañana, Marek Bolanowski, Alicia Santos, Peter J Trainer, John A H Wass, Antoine Tabarin
BACKGROUND: Surgery is the definitive treatment of Cushing's syndrome (CS) but medications may also be used as a first-line therapy. Whether preoperative medical treatment (PMT) affects postoperative outcome remains controversial. OBJECTIVE: 1) Evaluate how frequently PMT is given to CS patients across Europe 2) examine differences in preoperative characteristics of patients who receive PMT and those who undergo primary surgery; 3) determine if PMT influences postoperative outcome in pituitary-dependent CS (PIT-CS)...
February 12, 2018: European Journal of Endocrinology
Rosana Lazzarini, Mariana F S Hafner, Barbara A F Miguel, Nathalia T Kawakami, Beatriz H Y Nakagome
No abstract text is available yet for this article.
March 2018: Contact Dermatitis
Magdalena Wypij, Magdalena Świecimska, Joanna Czarnecka, Hanna Dahm, Mahendra Rai, Patrycja Golinska
AIMS: Presently, the effective antimicrobial agents have been limited by emergence of microbial strains with multi-drug resistance and biofilm formation potential. In the present study, we report remarkable antimicrobial activity of silver nanoparticles (AgNPs) synthesized from Streptomyces calidiresistens IF11 and IF17 strains, including inhibition of biofilm formation and synergistic effect of AgNPs and antibiotics against selected bacteria and yeasts. Cytotoxic effect of AgNPs on mammalian cell lines was also evaluated...
February 10, 2018: Journal of Applied Microbiology
Masahiro Iwaki, Toshiro Niwa, Yukiko Nakamura, Atsushi Kawase, Hiroshi Komura
The relative contribution of cytochrome P450 (CYP) isoforms responsible for carvedilol (CAR) oxidation in rats were evaluated in order to compare with that of reported human CYPs responsible for the metabolism of CAR enantiomers. The depletion of CAR enantiomers by recombinant CYPs and the effects of CYP-selective inhibitors on the depletion catalyzed by rat liver microsomes (RLM) was determined. Quinine (rat CYP2D inhibitor) markedly inhibited the metabolism of both R- and S-CAR by RLM. The metabolism of S-CAR was inhibited more than that of R-CAR by furafylline, (a CYP1A2 inhibitor, 53...
2018: Journal of Toxicological Sciences
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