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Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/28587746/corrigendum-to-quantitative-prediction-of-histamine-h1-receptor-occupancy-by-the-sedative-and-non-sedative-antagonists-in-the-human-central-nervous-system-based-on-systemic-exposure-and-preclinical-data-drug-metab-pharmacokinet-32-2017-135-144
#1
Kayoko Kanamitsu, Yoshitane Nozaki, Yoko Nagaya, Yuichi Sugiyama, Hiroyuki Kusuhara
No abstract text is available yet for this article.
May 22, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28522025/corrigendum-to-genetic-polymorphism-of-cynomolgus-and-rhesus-macaque-cyp2c9-drug-metab-pharmacokinet-30-2015-130-132
#2
Yasuhiro Uno, Akinori Matsushita, Norie Murayama, Hiroshi Yamazaki
No abstract text is available yet for this article.
June 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28427759/polymorphisms-in-cyp2c8-and-cyp3a5-genes-in-the-nigerian-population
#3
Ayorinde Adehin, Oluseye Oladotun Bolaji, Martin A Kennedy
Polymorphisms in CYP2C8 and CYP3A5 genes have implications for responses elicited by the ingestion of some xenobiotics, the metabolism of which are mediated by these enzymes. CYP2C8*2, CYP2C8*3, CYP3A5*3, CYP3A5*6 and CYP3A5*7 are a few functionally-relevant variants of these genes which this study provides data for, in the Nigerian population. Blood samples were processed for genomic DNA from 178 unrelated subjects spread across Nigerian ethnicities and screened for these polymorphism through the Sequenom iPLEX MassARRAY platform...
June 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28412023/precise-prediction-of-activators-for-the-human-constitutive-androstane-receptor-using-structure-based-three-dimensional-quantitative-structure-activity-relationship-methods
#4
Harutoshi Kato, Noriyuki Yamaotsu, Norihiko Iwazaki, Shigeaki Okamura, Toshiyuki Kume, Shuichi Hirono
The constitutive androstane receptor (CAR, NR1I3) regulates the expression of numerous drug-metabolizing enzymes and transporters. The upregulation of various enzymes, including CYP2B6, by CAR activators is a critical problem leading to clinically severe drug-drug interactions (DDIs). To date, however, few effective computational approaches for identifying CAR activators exist. In this study, we aimed to develop three-dimensional quantitative structure-activity relationship (3D-QSAR) models to predict the CAR activating potency of compounds emerging in the drug-discovery process...
June 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28366619/development-of-pharmacophore-based-classification-model%C3%A2-for%C3%A2-activators-of-constitutive-androstane-receptor
#5
Kyungro Lee, Hwan You, Jiwon Choi, Kyoung Tai No
Constitutive androstane receptor (CAR) is predominantly expressed in the liver and is important for regulating drug metabolism and transport. Despite its biological importance, there have been few attempts to develop in silico models to predict the activity of CAR modulated by chemical compounds. The number of in silico studies of CAR may be limited because of CAR's constitutive activity under normal conditions, which makes it difficult to elucidate the key structural features of the interaction between CAR and its ligands...
June 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28365301/species-specificity-profiling-of-rat-and-human-organic-cation-carnitine-transporter-slc22a5-slc22a5-octn2-octn2
#6
Kitti Szabó, Zoltán Nagy, Viktória Juhász, Joseph K Zolnerciks, Attila Csorba, Zoltán Tímár, Éva Molnár, Petra Pádár, William Johnson, Erzsébet Beéry, Péter Krajcsi
The purpose of this study was to characterize the uptake of carnitine, the physiological substrate, and the uptake of 3-(2,2,2-trimethylhydrazinium)propionate, a consensus substrate by rat Octn2 and human OCTN2 transporters as well as to characterize drug-mediated inhibition of l-carnitine uptake by the rat and human orthologs overexpressed in CHO-K1 cells. l-carnitine and 3-(2,2,2-trimethylhydrazinium)propionate were found to be a lower affinity substrate for rat Octn2 (KM = 32.66 ± 5.11 μM and 23.62 ± 4...
June 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28318879/evidences-for-salbutamol-metabolism-by-respiratory-and-liver-cell-lines
#7
Titpawan Nakpheng, Supreedee Songkarak, Tan Suwandecha, Rutthapol Sritharadol, Charisopon Chunhachaichana, Teerapol Srichana
This study aimed to investigate the enantiomeric biotransformation of salbutamol in the human respiratory and liver cells. The cells from the different cell growth cycles were treated with various concentrations of salbutamol sulfate. Salbutamol and its metabolites were analyzed using chiral liquid chromatography and mass spectrometry. There were no metabolites of salbutamol found in the extracellular medium, intracellular, and cell lysate of respiratory cell lines. The S/R ratios of salbutamol were found to be 0...
April 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28318878/insulin-stimulates-transport-of-organic-anion-compounds-mediated-by-organic-anion-transporting-polypeptide-2b1-in-the-human-intestinal-cell-line-caco-2
#8
Taku Kobayashi, Takahiro Koizumi, Masaki Kobayashi, Jiro Ogura, Yuichi Horiuchi, Yuki Kimura, Ayuko Kondo, Ayako Furugen, Katsuya Narumi, Natsuko Takahashi, Ken Iseki
Organic anion transporting polypeptide 2B1 (OATP2B1) is the major uptake transporter in the intestine, and transports various clinically used therapeutic agents. Insulin acts through the insulin receptor in targeted cells, and Rab8A is one of the insulin signaling pathways. The small intestine in humans also expresses insulin receptor and Rab8A. It has been reported that insulin stimulates peptide transporter 1 (PEPT1) expression at the apical membrane and increases uptake of PEPT1 substrates in small intestine epithelial model cells (Caco-2 cells)...
April 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28209435/contribution-of-equilibrative-nucleoside-transporter-ent-2-to-fluorouracil-transport-in-rat-placental-trophoblast-cells
#9
Akinori Takagi, Tomohiro Nishimura, Tomoya Akashi, Masatoshi Tomi, Emi Nakashima
Fluorouracil is used for treatment of breast cancer even in pregnant women, except during fetal organogenesis. The purpose of this study was to clarify the transport mechanism of fluorouracil at the rat placental barrier. Maternal-to-fetal transfer of [(3)H]fluorouracil in rats at gestational day 19.5 was saturable and much higher than that of [(14)C]sucrose. The uptake of [(3)H]fluorouracil was also saturable in rat placental trophoblast TR-TBT 18d-1 cells, which express both equilibrative nucleoside transporter (ENT) 1 and ENT2...
April 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28190756/organic-anion-transporting-polypeptide-oatp-2b1-contributes-to-the-cellular-uptake-of-theaflavin
#10
Ayuko Kondo, Katsuya Narumi, Jiro Ogura, Ai Sasaki, Keisuke Yabe, Taku Kobayashi, Ayako Furugen, Masaki Kobayashi, Ken Iseki
Organic anion-transporting polypeptide (OATP) 2B1 has been reported in the apical membranes of the human small intestinal epithelium, where it contributes to the intestinal absorption of pharmacologically active drugs. To investigate the potential for OATP2B1-mediated drug-food interactions, the effects of several polyphenolic compounds on OATP2B1-mediated estrone-3-sulfate (E3S) transport were studied by using OATP2B1-expressing HEK293 cells. Our results showed that some compounds, especially theaflavin, were strong inhibitors of OATP2B1-mediated E3S uptake...
April 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28190755/quantitative-prediction-of-histamine-h1-receptor-occupancy-by-the-sedative-and-non-sedative-antagonists-in-the-human-central-nervous-system-based-on-systemic-exposure-and-preclinical-data
#11
Kayoko Kanamitsu, Yoshitane Nozaki, Yoko Nagaya, Yuichi Sugiyama, Hiroyuki Kusuhara
Significant histamine H1 receptor occupation in the central nervous system (CNS) is associated with sedation. Here we examined the time profiles of the H1 receptor occupancy (RO) in the CNS using sedative (diphenhydramine and ketotifen) and non-sedative (bepotastine and olopatadine) antagonists at their therapeutic doses by integrating in vitro and animal data. A pharmacokinetic model was constructed to associate plasma concentrations and receptor binding in the brain. Dissociation and association rate constants with the H1 receptor and plasma and brain unbound fractions were determined in vitro...
April 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28139372/in%C3%A2-vitro-ocular-metabolism-and-bioactivation-of-ketoconazole-in-rat-rabbit-and-human
#12
Amanda L Cirello, Jennifer L Dumouchel, Mithat Gunduz, Christine E Dunne, Upendra A Argikar
Oral ketoconazole is clinically administered for treatment of severe cases for fungal keratitis. Pharmacodynamics and efficacy of oral and topical (ocular) ketoconazole have been explored in rabbit. However, metabolism of ketoconazole in the eye in any species is not well explored in any preclinical species or human. An understanding of ocular drug metabolism in the eye is crucial for ocular therapeutics to facilitate the risk assessment and development of potential drug candidates for the clinic. We aimed to investigate the metabolism of ketoconazole in rat, rabbit and human ocular S9 fractions...
April 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28619281/metabolism-of-ko143-an-abcg2-inhibitor
#13
Ke Liu, Junjie Zhu, Yixian Huang, Chaoyue Li, Jie Lu, Madhav Sachar, Song Li, Xiaochao Ma
The ATP-binding cassette sub-family G member 2 (ABCG2) plays an important role in modulating drug disposition and endobiotic homeostasis. KO143 is a potent and relatively selective ABCG2 inhibitor. We found that the metabolic stability of KO143 was very poor in human liver microsomes (HLM). Our further studies illustrated that the tert-butyl ester group in KO143 can be rapidly hydrolyzed and removed by carboxylesterase 1. This metabolic pathway was confirmed as a major pathway of KO143 metabolism in both HLM and mice...
March 6, 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28153492/sex-and-age-dependent-gene-expression-in-human-liver-an-implication-for-drug-metabolizing-enzymes
#14
Yasuhiro Uno, Ryo Takata, Go Kito, Hiroshi Yamazaki, Kazuko Nakagawa, Yusuke Nakamura, Tetsuya Kamataki, Toyomasa Katagiri
Sex and age differences in hepatic expression of drug-metabolizing enzyme genes could cause variations in drug metabolism, but has not been fully elucidated, especially in Asian population. In this study, the global expression of human hepatic genes was analyzed by microarrays in 40 Japanese subjects (27 males and 13 females). Thirty-five sex-biased genes were identified (P < 0.005). Whereas, 60 age-biased genes in two age groups, <60 years and ≥70 years (P < 0.001), were identified in males...
February 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28017537/human-leukocyte-antigen-and-idiosyncratic-adverse-drug-reactions
#15
REVIEW
Toru Usui, Dean J Naisbitt
A clinical association between a specific human leukocyte antigen (HLA) allele and idiosyncratic adverse drug reactions (IADRs) is a strong indication that IADRs are mediated by the adaptive immune system. For example, it is well-established that HLA-B*15:02 and HLA-B*57:01 are associated with carbamazepine-induced Stevens-Johnson syndrome (SJS)/toxic epidermal necrolysis (TEN) and abacavir-induced hypersensitivity/flucloxacillin-induced liver injury, respectively. Drug-specific T-cells whose response is restricted by specific HLA risk alleles have been detected from IADR patients, also suggesting an adaptive immune pathogenesis...
February 2017: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28129974/prediction-of-the-potential-risk-of-idiosyncratic-drug-toxicity
#16
EDITORIAL
Kousei Ito, Kaoru Kobayashi
No abstract text is available yet for this article.
December 21, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28111103/potentiation-of-the-anticoagulation-effect-of-warfarin-by-the-herbal-remedy-shu-jing-hwo-shiee-tang-in-rats-the-dosing-regimen-and-pharmacokinetic-interaction
#17
Yune-Fang Ueng, Chung-Kuang Lu, Sien-Hung Yang, Hong-Jaan Wang, Chiung-Chiao Huang
The herbal remedy Shu-Jing-Hwo-Shiee-Tang (SJHST) has been used in traditional Chinese medical care for the treatment of osteoarthritis. This study aims to examine the influence of SJHST on the oxidation and anticoagulation effect of warfarin in male rats. In three SJHST preparations (S1-S3), hesperidin, gentiopicrin, and paeoniflorin were identified as chemical marker ingredients. The inhibition of liver microsomal warfarin 7-hydroxylation (WOH) activity by 50% methanolic extracts of SJHST was potentiated by β-glucosidase pretreatment, but not by NADPH-fortified microsomal preincubation...
December 8, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28340950/pharmacokinetics-and-bioavailability-of-oral-single-dose-maleic-acid-in-biofluids-of-sprague-dawley-rats
#18
Charlene Wu, Hsin-Chang Chen, Yu-Syuan Luo, Su-Yin Chiang, Kuen-Yuh Wu
Maleic acid (MA) was purposefully adulterated in an array of starch-based foods in Taiwan, inciting a food safety incident. Due to limited data on the pharmacokinetics and bioavailability of ingested MA, we studied pharmacokinetic (PK) parameters in serum and urine of Sprague Dawley rats. Three groups of male and female rats were given three doses of MA by oral gavage; biofluid samples were collected accordingly. Data demonstrated that a non-compartment model best described MA's linear kinetic behavior upon ingestion...
December 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27876352/quantitative-analysis-of-pharmacokinetic-profiles-of-verapamil-and-drug-drug-interactions-induced-by-a-cyp-inhibitor-using-a-stable-isotope-labeled-compound
#19
Makoto Kataoka, Chie Kojima, Kazuki Ueda, Keiko Minami, Haruki Higashino, Shinji Sakuma, Kazutaka Togashi, Kuninori Mutaguchi, Shinji Yamashita
The purpose of the present study is to demonstrate a useful approach (isotope-IV method) for analyzing drug-drug interactions (DDIs) following the oral administration of drugs using stable isotope-labeled compounds. Verapamil hydrochloride (VER) was used as a drug model. Deuterium-labeled VER (VER-d6, 0.005 mg/kg) was intravenously administered to rats with or without a pre-treatment with 1-aminobenzotriazole (ABT, 100 mg/kg), a potent CYP inhibitor, 1.5 h after the oral administration of VER (1 mg/kg)...
December 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27839692/a-possible-role-for-hla-drb1-04-06-in-statin-related-myopathy-in-japanese-patients
#20
Kimie Sai, Kouji Kajinami, Hironobu Akao, Mizuho Iwadare, Ryoko Sato-Ishida, Yasuyuki Kawai, Kenji Takeda, Takashi Tanimoto, Takashi Yamano, Takashi Akasaka, Tatsuro Ishida, Ken-Ichi Hirata, Keijiro Saku, Shusuke Yagi, Takeshi Soeki, Masataka Sata, Masafumi Ueno, Shunichi Miyazaki, Aya Shiraki, Jun-Ichi Oyama, Koichi Node, Koichi Sugamura, Hisao Ogawa, Kouichi Kurose, Keiko Maekawa, Yumiko Matsuzawa, Takuya Imatoh, Ryuichi Hasegawa, Yoshiro Saito
Statin-related myopathy (SRM) is a clinically important adverse reaction. Recent pharmacogenetic research, mainly in non-Asian populations, have indicated clinical relevance of some of genetic biomarkers to SRM, but predictive markers for SRM in Asian populations including Japanese has not yet been established. This study was aimed to identify clinically important genetic markers associated with SRM in Japanese patients. Allele frequencies of the three reported candidate markers - SLCO1B1 rs4149056, RYR2 rs2819742, and GATM rs9806699 - and carrier frequencies of HLA types were compared between patients with SRM patients (n = 52) and healthy Japanese subjects (n = 2878 or 86 (for rs9806699) as controls)...
December 2016: Drug Metabolism and Pharmacokinetics
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