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https://www.readbyqxmd.com/read/27882219/cyp2d6-gene-polymorphisms-in-brazilian-patients-with-breast-cancer-treated-with-adjuvant-tamoxifen-and-its-association-with-disease-recurrence
#1
Mariella De Ameida Melo, Rodrigo José De Vasconcelos-Valença, Fidelis Manes Neto, Rafael Soares Borges, Danylo Rafhael Costa-Silva, Maria Da Conceição Barros-Oliveira, Umbelina Soares Borges, Airlane Pereira Alencar, Vladimir Costa Silva, Benedito Borges Da Silva
At present, there is controversy regarding the efficacy of tamoxifen in breast cancer patients who are carriers of cytochrome P450 2D6 (CYP2D6) gene polymorphisms, in terms of recurrence and overall survival. Thus, the aim of the present study was to investigate the association of the CYP2D6 *4, *10 and *17 gene polymorphisms with breast cancer recurrence in a Brazilian population. The cohort comprised 40 receptor-positive breast cancer patients without recurrence and 40 with distant recurrence. A 3-ml sample of peripheral blood was collected from each patient to determine the presence of the *4, *10 and *17 single nucleotide polymorphisms of the CYP2D6 gene by quantitative polymerase chain reaction analysis...
November 2016: Biomedical Reports
https://www.readbyqxmd.com/read/27875319/enhanced-oral-bioavailability-of-metoprolol-with-gallic-acid-and-ellagic-acid-in-male-wistar-rats-involvement-of-cyp2d6-inhibition
#2
Bhargavi Latha Athukuri, Prasad Neerati
BACKGROUND: Cytochrome P450-2D6 (CYP2D6), a member of the CYP450 mixed function oxidase system, is an important CYP isoform with regard to herbal-drug interactions and is responsible for the metabolism of nearly 25% of drugs. Until now, studies on the effects of various phytochemicals on CYP2D6 activity in vivo have been very rare. Gallic acid and ellagic acid are natural polyphenols which are widely distributed in fruits and medicinal plants. In the present study, the effects of gallic acid and ellagic acid pretreatment on intestinal transport and oral bioavailability of metoprolol were investigated...
December 1, 2016: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/27853934/evaluation-of-in-vitro-cytochrome-p450-inhibition-and-in-vitro-fate-of-structurally-diverse-n-oxide-metabolites-case-studies-with-clozapine-levofloxacin-roflumilast-voriconazole-and-zopiclone
#3
Poonam Giri, Sneha Naidu, Nirmal Patel, Harilal Patel, Nuggehally R Srinivas
BACKGROUND AND OBJECTIVES: The role of metabolite(s) to elicit potential clinical drug-drug interaction (DDI) via cytochrome P450 enzymes (CYP) is gaining momentum. In this context, the role of N-oxides for in vitro CYP inhibition has not been evaluated. The objectives of this study were: (a) to examine in vitro CYP inhibition of N-oxides of clozapine, levofloxacin, roflumilast, voriconazole and zopiclone in a tiered approach and (b) evaluate in vitro fate of aforementioned N-oxides examined in recombinant CYPs, human microsomes and hepatocytes...
November 16, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27819189/inhibitory-effects-of-curculigoside-on-human-liver-cytochrome-p450-enzymes
#4
Jixiao Lang, Wei Li, Jingming Zhao, Kaiyou Wang, Dexi Chen
1. Curculigoside possesses numerous pharmacological activities, and however, little data available for the effects of curculigoside on the activity of human liver cytochrome P450 (CYP) enzymes. 2. This study investigates the inhibitory effects of curculigoside on the main human liver CYP isoforms. In this study, the inhibitory effects of curculigoside on the eight human liver CYP isoforms 1A2, 2A6, 2E1, 2D6, 2C9, 2C19, 2C8, and 3A4 were investigated in human liver microsomes. 3. The results indicated that curculigoside could inhibit the activity of CYP1A2, CYP2C8, and CYP3A4, with IC50 values of 15...
November 5, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27813451/pharmacogenomics-of-heart-failure-a-systematic-review
#5
Fannie Mottet, Orly Vardeny, Simon de Denus
BACKGROUND: Heart failure (HF) and multiple HF-related phenotypes are heritable. Genes implicated in the HF pathophysiology would be expected to influence the response to treatment. METHODS: We conducted a series of systematic literature searches on the pharmacogenetics of HF therapy to assess the current knowledge on this field. RESULTS: Existing data related to HF pharmacogenomics are still limited. The ADRB1 gene is a likely candidate to predict response to β-blockers...
November 2016: Pharmacogenomics
https://www.readbyqxmd.com/read/27800629/the-combination-of-pharmacogenetic-and-pharmacokinetic-analyses-to-optimize-clomipramine-dosing-in-major-depression-a-case-report
#6
Stefania Antoniazzi, Alessandro Tatulli, Felicia S Falvella, Michela Cigliobianco, Riccardo A Paoli, Dario Cattaneo, Stefania Cheli, Francesca F Bernardi, Emilio Clementi, Carlo A Altamura
WHAT IS KNOWN AND OBJECTIVE: Polymorphisms in cytochrome P450 2D6 and 2C19 can lead to interindividual differences in drug plasma concentrations, affecting clomipramine efficacy. Pharmacokinetic and pharmacogenetic analyses may improve drug therapy. CASE SUMMARY: We report the case of a depressed woman requiring higher doses than standard of clomipramine. Identification of low plasma drug levels led to extensive pharmacogenetic analyses of all genes and major functional polymorphisms reported to affect clomipramine metabolism...
October 31, 2016: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/27785397/cyp2d6-allele-distribution-in-macedonians-albanians-and-romanies-in-the-republic-of-macedonia
#7
M Kuzmanovska, M Dimishkovska, I Maleva Kostovska, P Noveski, E Sukarova Stefanovska, D Plaseska-Karanfilska
Cytochrome P450 2D6 (CYP2D6) is an enzyme of great importance for the metabolism of clinically used drugs. More than 100 variants of the CYP2D6 gene have been identified so far. The aim of this study was to investigate the allele distribution of CYP2D6 gene variants in 100 individuals of each of the Macedonian, Albanian and Romany population, by genotyping using long range polymerase chain reaction (PCR) and a multiplex single base extension method. The most frequent variants and almost equally distributed in the three groups were the fully functional alleles *1 and *2...
December 1, 2015: Balkan Journal of Medical Genetics: BJMG
https://www.readbyqxmd.com/read/27783977/targeting-the-entry-region-of-hsp90-s-atp-binding-pocket-with-a-novel-6-7-dihydrothieno-3-2-c-pyridin-5-4h-yl-amide
#8
Ju Hui Jeong, Yong Jin Oh, Yunmee Lho, Sun You Park, Kwang-Hyeon Liu, Eunyoung Ha, Young Ho Seo
The molecular chaperone Hsp90 plays an important role in cancer cell survival and proliferation by regulating the maturation and stabilization of numerous oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 has emerged as an attractive therapeutic target for cancer treatment. In this study, the design, synthesis, and biological evaluation of a series of Hsp90 inhibitors are described. Among the synthetic compounds, 6,7-dihydrothieno [3,2-c]pyridin-5(4H)-yl amide 19 exhibits a remarkable binding affinity to the N-terminus of Hsp90 in a fluorescence polarization (FP) binding assay (IC50 = 50...
October 18, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27766562/a-physiologically-based-pharmacokinetic-model-to-predict-human-fetal-exposure-for-a-drug-metabolized-by-several-cyp450-pathways
#9
Maïlys De Sousa Mendes, Gabrielle Lui, Yi Zheng, Claire Pressiat, Deborah Hirt, Elodie Valade, Naïm Bouazza, Frantz Foissac, Stephane Blanche, Jean-Marc Treluyer, Saik Urien, Sihem Benaboud
BACKGROUND: Pregnant women and their fetuses are exposed to numerous drugs; however, they are orphan populations with respect to the safety and efficacy of drugs. Therefore, the prediction of maternal and fetal drug exposure prior to administration would be highly useful. METHODS: A physiologically-based pharmacokinetic (PBPK) model for nevirapine, which is metabolized by the cytochrome P450 (CYP) 3A4, 2B6 and 2D6 pathways, was developed to predict maternal and fetal pharmacokinetics (PK)...
October 21, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27761064/human-cytochrome-p450-enzyme-modulation-by-gymnema-sylvestre-a-predictive-safety-evaluation-by-lc-ms-ms
#10
Bera Rammohan, Karmakar Samit, Das Chinmoy, Saha Arup, Kundu Amit, Sarkar Ratul, Karmakar Sanmoy, Adhikari Dipan, Sen Tuhinadri
BACKGROUND: Traditionally GS is used to treat diabetes mellitus. Drug-herb interaction of GS via cytochrome P450 enzyme system by substrate cocktail method using HLM has not been reported. OBJECTIVE: To evaluate the in-vitro modulatory effects of GS extracts (aqueous, methanol, ethyl acetate, chloroform and n-hexane) and deacylgymnemic acid (DGA) on human CYP1A2, 2C8, 2C9, 2D6 and 3A4 activities in HLM. MATERIAL AND METHODS: Probe substrate-based LCMS/MS method was established for all CYPs...
July 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27758707/new-psychoactive-substances-3-methoxyphencyclidine-3-meo-pcp-and-3-methoxyrolicyclidine-3-meo-pcpy-metabolic-fate-elucidated-with-rat-urine-and-human-liver-preparations-and-their-detectability-in-urine-by-gc-ms-lc-high-resolution-msn-and-lc-high-resolution
#11
Julian A Michely, Sascha K Manier, Achim T Caspar, Simon D Brandt, Jason Wallach, Hans H Maurer
3-Methoxyphencyclidine (3-MeO-PCP) and 3-methoxyrolicyclidine (3-MeO-PCPy) are two new psychoactive substances (NPS). The aims of the present study were the elucidation of their metabolic fate in rat and pooled human liver microsomes (pHLM), the identification of the cytochrome P450 (CYP) isoenzymes involved, and the detectability using standard urine screening approaches (SUSA) after intake of common users' doses using gas chromatography-mass spectrometry (GC-MS), liquid chromatography-multi-stage mass spectrometry (LC-MSn), and liquid chromatography-high-resolution tandem mass spectrometry (LC-HR-MS/MS)...
October 18, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27754210/os-31-02-antihypertensive-response-to-bisoprolol-was-not-related-to-polymorphisms-in-adrb1-or-cyp2d6-in-chinese-hypertensive-patients
#12
Weiwei Zeng, Tanya Chu, Miao Hu, Alice Kong, Brian Tomlinson
OBJECTIVE: The blood pressure (BP) response to antihypertensive drugs varies considerably between different patients. The response to some beta-blockers has been associated with polymorphisms in the beta1-adrenergic receptor (ADRB1) or cytochrome P450 2D6 (CYP2D6) genes. We examined the effects of common polymorphisms in ADRB1 and CYP2D6 on the response to bisoprolol in 100 Chinese patients. DESIGN AND METHOD: Chinese patients with primary hypertension with sitting clinic systolic BP (SBP) 140-169 mmHg and/or diastolic BP (DBP) 90-109 mmHg after placebo run-in were treated with open-label bisoprolol 2...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27751854/evaluation-of-the-in%C3%A2-vitro-and-in%C3%A2-vivo-metabolic-pathway-and-cytochrome-p450-inhibition-induction-profile-of-huperzine-a
#13
Ping-Ping Lin, Xue-Ning Li, Fei Yuan, Wei-Li Chen, Meng-Jie Yang, Hong-Rong Xu
Huperzine A (HupA), one of the reversible and selective acetylcholinesterase inhibitors derived from Chinese herb Huperzia Serrata, possesses affirmative action of ameliorating cognitive dysfunction of Alzheimer's disease. Up to now, the effects of HupA on human cytochrome P450s (CYPs) have not been fully elucidated. The purpose of the present study was to clarify the metabolic pathway of HupA in vitro and in vivo, and to evaluate the CYPs inhibition/induction profile of HupA in vitro. The catalytic activity of CYP enzymes (CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A4) was measured by the quantification of specific enzyme substrates using validated liquid chromatography-tandem mass spectrometry (LC/MS/MS) methods...
November 11, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27738376/paroxetine-the-antidepressant-from-hell-probably-not-but-caution-required
#14
Robert M Nevels, Samuel T Gontkovsky, Bryman E Williams
Paroxetine, also known by the trade names Aropax, Paxil, Pexeva, Seroxat, Sereupin and Brisdelle, was first marketed in the U.S. in 1992. Effective for major depression and various anxiety disorders, it quickly gained a sizable share of the antidepressant prescription market. By the late 1990s, paroxetine frequently was being associated with serious drug interactions and medication side effects. Most significantly, in a major Canadian epidemiological study examining the relationship between antidepressants and diseases, paroxetine was associated with a 620 percent increase in the rate of breast cancer in women who had taken it over a four-year period...
March 1, 2016: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/27735849/construction-of-metabolism-prediction-models-for-cyp450-3a4-2d6-and-2c9-based-on-microsomal-metabolic-reaction-system
#15
Shuai-Bing He, Man-Man Li, Bai-Xia Zhang, Xiao-Tong Ye, Ran-Feng Du, Yun Wang, Yan-Jiang Qiao
During the past decades, there have been continuous attempts in the prediction of metabolism mediated by cytochrome P450s (CYP450s) 3A4, 2D6, and 2C9. However, it has indeed remained a huge challenge to accurately predict the metabolism of xenobiotics mediated by these enzymes. To address this issue, microsomal metabolic reaction system (MMRS)-a novel concept, which integrates information about site of metabolism (SOM) and enzyme-was introduced. By incorporating the use of multiple feature selection (FS) techniques (ChiSquared (CHI), InfoGain (IG), GainRatio (GR), Relief) and hybrid classification procedures (Kstar, Bayes (BN), K-nearest neighbours (IBK), C4...
October 9, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27725449/evaluation-of-the-effects-of-s-allyl-l-cysteine-s-methyl-l-cysteine-trans-s-1-propenyl-l-cysteine-and-their-n-acetylated-and-s-oxidized-metabolites-on-human-cyp-activities
#16
Hirotaka Amano, Daichi Kazamori, Kenji Itoh
Three major organosulfur compounds of aged garlic extract, S-allyl-L-cysteine (SAC), S-methyl-L-cysteine (SMC), and trans-S-1-propenyl-L-cysteine (S1PC), were examined for their effects on the activities of five major isoforms of human CYP enzymes: CYP1A2, 2C9, 2C19, 2D6, and 3A4. The metabolite formation from probe substrates for the CYP isoforms was examined in human liver microsomes in the presence of organosulfur compounds at 0.01-1 mM by using liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27721546/metabolism-mediated-interaction-potential-of-standardized-extract-of-tinospora-cordifolia-through-rat-and-human-liver-microsomes
#17
Shiv Bahadur, Pulok K Mukherjee, S K Milan Ahmmed, Amit Kar, Ranjit K Harwansh, Subrata Pandit
OBJECTIVE: Tinospora cordifolia is used for treatment of several diseases in Indian system of medicine. In the present study, the inhibition potential of T. cordifolia extracts and its constituent tinosporaside to cause herb-drug interactions through rat and human liver cytochrome enzymes was evaluated. MATERIALS AND METHODS: Bioactive compound was quantified through reverse phase high-performance liquid chromatography, to standardize the plant extracts and interaction potential of standardized extract...
September 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/27695293/application-of-physiologically-based-pharmacokinetic-modeling-in-predicting-drug-drug-interactions-for-sarpogrelate-hydrochloride-in-humans
#18
Jee Sun Min, Doyun Kim, Jung Bae Park, Hyunjin Heo, Soo Hyeon Bae, Jae Hong Seo, Euichaul Oh, Soo Kyung Bae
BACKGROUND: Evaluating the potential risk of metabolic drug-drug interactions (DDIs) is clinically important. OBJECTIVE: To develop a physiologically based pharmacokinetic (PBPK) model for sarpogrelate hydrochloride and its active metabolite, (R,S)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol (M-1), in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP) 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27694571/risk-of-mortality-with-concomitant-use-of-tamoxifen-and-selective-serotonin-reuptake-inhibitors-multi-database-cohort-study
#19
Macarius M Donneyong, Katsiaryna Bykov, Pauline Bosco-Levy, Yaa-Hui Dong, Raisa Levin, Joshua J Gagne
OBJECTIVE:  To compare differences in mortality between women concomitantly treated with tamoxifen and selective serotonin reuptake inhibitors (SSRIs) that are potent inhibitors of the cytochrome-P450 2D6 enzyme (CYP2D6) versus tamoxifen and other SSRIs. DESIGN:  Population based cohort study. SETTING:  Five US databases covering individuals enrolled in private and public health insurance programs from 1995 to 2013. PARTICIPANTS:  Two cohorts of women who started taking tamoxifen...
September 30, 2016: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/27665326/frequency-of-genetic-polymorphism-for-adrenergic-receptor-beta-and-cytochrome-p450-2d6-enzyme-and-effects-on-tolerability-of-beta-blocker-therapy-in-heart-failure-with-reduced-ejection-fraction-patients-the-beta-genturk-study
#20
Mehdi Zoghi, Hakkı Kaya, Yüksel Çavuşoğlu, Enbiya Aksakal, Şerafettin Demir, Ceyhun Yücel, Haşim Mutlu, Oktay Ergene, Mehmet Birhan Yılmaz
OBJECTIVE: The present objective was to determine frequency of Arginine389Glycine (Arg389Gly) and Cytochrome p450 2D6*10 (Cyp2D6*10) polymorphism in cases of heart failure-reduced ejection fraction (HFREF), and to evaluate the influence of the polymorphisms in response to beta-blocker (BB) therapy. METHODS: A total of 206 HFREF patients and 90 healthy controls were prospectively enrolled. Genotypes for Arg389Gly and Cyp2D6*10 polymorphisms of the healthy controls and 162 of the 206 heart failure (HF) patients were measured, identified by polymerase-chain-reaction- and restriction-fragment-length-polymorphism analysis...
September 2016: Türk Kardiyoloji Derneği Arşivi: Türk Kardiyoloji Derneğinin Yayın Organıdır
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