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https://www.readbyqxmd.com/read/29679912/effects-of-ugt2b7-scn1a-and-cyp3a4-on-the-therapeutic-response-of-sodium-valproate-treatment-in-children-with-generalized-seizures
#1
Weixing Feng, Shenghui Mei, Leting Zhu, Yazhen Yu, Weili Yang, Baoqin Gao, Xiaojuan Wu, Zhigang Zhao, Fang Fang
PURPOSE: This study aims to evaluate the associations between genetic polymorphisms and the effect of sodium valproate (VPA) therapy in children with generalized seizures. METHODS: A total of 174 children with generalized seizures on VPA therapy were enrolled. Steady-state trough plasma concentrations of VPA were analyzed. Seventy-six single nucleotide polymorphisms involved in the absorption, metabolism, transport, and target receptor of VPA were identified, and their associations with the therapeutic effect (seizure reduction) were evaluated using logistic regression adjusted by various influence factors...
April 14, 2018: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/29678659/association-of-cyp3a4-1b-genotype-with-cyclosporin-a-pharmacokinetics-in-renal-transplant-recipients-a-meta-analysis
#2
Cai-E Wang, Ke-Peng Lu, Zhao Chang, Meng-Li Guo, Hai-Ling Qiao
OBJECTIVE: Cyclosporine (CsA) is a substrate of cytochrome P450 (CYP) 3A4 with a narrow therapeutic index and large individual difference. CYP3A4*1B is reported to be associated with CsA pharmacokinetics parameters, but the relevance is still in dispute. Therefore, a meta-analysis was employed to evaluate the influence of CYP3A4*1B on CsA pharmacokinetics at different post-transplantation times in adult renal transplant recipients. METHODS: Studies on evaluating the CYP3A4*1B genotype and CsA pharmacokinetics were retrieved through a systematical search of relevant database including PubMed, Emabase, Web of science, the Cochrane Library, Clinical Trials...
April 17, 2018: Gene
https://www.readbyqxmd.com/read/29668485/prolonged-activity-and-toxicity-of-sirolimus-in-a-patient-with-metastatic-renal-perivascular-epithelioid-cell-tumor-a-case-report-and-literature-review
#3
Alessandra Raimondi, Francesca Colombo, Giulia Pintarelli, Carlo Morosi, Salvatore L Renne, Anna M Frezza, Maristella Saponara, Angelo P Dei Tos, Arabella Mazzocchi, Salvatore Provenzano, Paolo G Casali, Silvia Stacchiotti
Perivascular epithelioid cell tumor (PEComa) is a family of mesenchymal tumors. Conventional chemotherapy has little activity in this disease, but case reports are available on the activity of mammalian target of rapamycin inhibitors (e.g. sirolimus and temsirolimus). Pharmacokinetic assays of sirolimus are available as this drug has a precise therapeutic window and blood levels might be influenced by CYP3A4 polymorphisms and drug interactions. We report on a case of a patient with metastatic, progressive PEComa who started sirolimus at a dose of 5 mg/day with evidence of grade (G) 3 mucositis, G2 thrombocytopenia, and G1 leucopenia 10 days after the treatment started, in absence of concomitant medications or prohibited food assumption...
April 17, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29659506/in-vitro-inhibitory-effects-of-synthetic-cannabinoid-eam-2201-on-cytochrome-p450-and-udp-glucuronosyltransferase-enzyme-activities-in-human-liver-microsomes
#4
Tae Yeon Kong, Soon-Sang Kwon, Jae Chul Cheong, Hee Seung Kim, Jin Young Kim, Hye Suk Lee
EAM-2201, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors that is widely abused as an illicit recreational drug in combination with other drugs. To evaluate the potential of EAM-2201 as a perpetrator of drug–drug interactions, the inhibitory effects of EAM-2201 on major drug-metabolizing enzymes, cytochrome P450s (CYPs) and uridine 5′-diphospho-glucuronosyltransferases (UGTs) were evaluated in pooled human liver microsomes using liquid chromatography–tandem mass spectrometry (LC-MS/MS)...
April 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29649093/comparison-of-cyp3a4-inducing-capacity-of-enzyme-inducing-antiepileptic-drugs-using-4%C3%AE-hydroxycholesterol-as-biomarker
#5
Kristine Hole, Birgit M Wollmann, Camilla Nguyen, Tore Haslemo, Espen Molden
BACKGROUND: Enzyme-inducing antiepileptic drugs (EIAEDs) are among the clinically most important inducers of cytochrome P450 (CYP) 3A4, but there is limited evidence regarding the comparative potency of each EIAED in raising CYP3A4 activity. The aim of this study was to estimate CYP3A4-inductive potency of EIAEDs by comparing CYP3A4 activity in patients treated with carbamazepine, phenobarbital, or phenytoin. METHODS: Residual serum samples from patients treated with EIAEDs or levetiracetam were collected from a therapeutic drug monitoring service for analysis of 4β-hydroxycholesterol (4βOHC), which is an indicator of CYP3A4 activity...
April 11, 2018: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29620050/pharmacokinetics-and-disposition-of-anlotinib-an-oral-tyrosine-kinase-inhibitor-in-experimental-animal-species
#6
Chen-Chun Zhong, Feng Chen, Jun-Ling Yang, Wei-Wei Jia, Li Li, Chen Cheng, Fei-Fei Du, Su-Ping Zhang, Cheng-Ying Xie, Na-Ting Zhang, Olajide E Olaleye, Feng-Qing Wang, Fang Xu, Li-Guang Lou, Dong-Ying Chen, Wei Niu, Chuan Li
Anlotinib is a new oral tyrosine kinase inhibitor; this study was designed to characterize its pharmacokinetics and disposition. Anlotinib was evaluated in rats, tumor-bearing mice, and dogs and also assessed in vitro to characterize its pharmacokinetics and disposition and drug interaction potential. Samples were analyzed by liquid chromatography/mass spectrometry. Anlotinib, having good membrane permeability, was rapidly absorbed with oral bioavailability of 28%-58% in rats and 41%-77% in dogs. Terminal half-life of anlotinib in dogs (22...
April 5, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29603629/cyp3a5-3-and-abcb1-61a-g-significantly-influence-dose-adjusted-trough-blood-tacrolimus-concentrations-in-the-first-three-months-post-kidney-transplantation
#7
Rong Hu, Daniel T Barratt, Janet K Coller, Benedetta C Sallustio, Andrew A Somogyi
Tacrolimus (TAC) is a first-line immunosuppressant used to prevent organ rejection after kidney transplantation. There is large inter-individual variability in its pharmacokinetics. Single nucleotide polymorphisms (SNPs) in genes encoding TAC metabolising enzymes cytochromes P450 3A4/5 (CYP3A4/5), P-glycoprotein efflux transporter (ABCB1), their expression regulator pregnane X receptor (NR1I2), and CYP3A co-factor cytochrome P450 reductase (POR), have been studied for their effects on tacrolimus disposition...
March 30, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29596975/role-of-cytochrome-p450-enzymes-in-fimasartan-metabolism-in-vitro
#8
Young Jae Choi, Ji-Yoon Lee, Chang Seon Ryu, Yong Ha Chi, Soo Heui Paik, Sang Kyum Kim
Fimasartan (FMS), an angiotensin II receptor antagonist, is metabolized to FMS S-oxide, FMS N-glucuronide, oxidative desulfurized FMS (BR-A-557), and hydroxy-n-butyl FMSs. The purpose of this study was to characterize enzymes involved in NADPH-dependent FMS metabolism using recombinant enzymes such as cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO), as well as selective chemical inhibitors. The results showed that CYP, but not FMO, plays a major role in FMS metabolism. CYP2C9, CYP3A4, and CYP3A5 were involved in the formation of FMS S-oxide, which was further metabolized to BR-A-557 by CYP3A4/5...
March 26, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29589331/population-pharmacokinetic-analysis-of-asunaprevir-in-subjects-with-hepatitis-c-virus-infection
#9
Li Zhu, Hanbin Li, Phyllis Chan, Timothy Eley, Yash Gandhi, Marc Bifano, Mayu Osawa, Takayo Ueno, Eric Hughes, Malaz AbuTarif, Richard Bertz, Tushar Garimella
INTRODUCTION: Asunaprevir (ASV) is a potent, pangenotypic, twice-daily hepatitis C virus (HCV) NS3 inhibitor indicated for the treatment of chronic HCV infection. METHODS: A population pharmacokinetic (PPK) model was developed using pooled ASV concentration data from 1239 HCV-infected subjects who received ASV either as part of the DUAL regimen with daclatasvir or as part of the QUAD regimen with daclatasvir and peg-interferon/ribavirin. RESULTS: A two-compartment model with first-order elimination from the central compartment, an induction effect on clearance, and an absorption model consisted of zero-order release followed by first-order absorption adequately described ASV PK after oral administration...
March 27, 2018: Infectious Diseases and Therapy
https://www.readbyqxmd.com/read/29572664/identification-of-cytochrome-p450-mediated-drug-drug-interactions-at-risk-in-cases-of-gene-polymorphisms-by-using-a-quantitative-prediction-model
#10
Nicolas Fermier, Laurent Bourguignon, Sylvain Goutelle, Nathalie Bleyzac, Michel Tod
BACKGROUND AND OBJECTIVE: The magnitude of drug-drug interactions mediated by cytochrome P450 (CYP) may depend on the genotype of polymorphic cytochromes. The objective of this study was to identify drug-drug interactions with greater magnitude in CYP variant groups than in extensive metabolizers. METHODS: The in-vivo mechanistic static model was used to predict the area under the curve ratio of drug-drug interactions. Five cytochromes (CYP3A4/5, 2D6, 2C9, 2C19, 1A2) and five groups of genotypes for each polymorphic cytochrome (CYP2D6, 2C9, 2C19) were considered...
March 23, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29570971/phenotypic-assessment-of-drug-metabolic-pathways-and-p-glycoprotein-in-patients-treated-with-antidepressants-in-an-ambulatory-setting
#11
Célia Lloret-Linares, Marija Bosilkovska, Youssef Daali, Marianne Gex-Fabry, Kyle Heron, Victor Bancila, Giorgio Michalopoulos, Nader Perroud, Hélène Richard-Lepouriel, Jean-Michel Aubry, Jules Desmeules, Marie Besson
OBJECTIVE: Drug-metabolizing enzymes (DMEs), such as cytochrome P450 (CYP) enzymes, and transporters have emerged as major determinants of variability in drug metabolism and response. This study investigated the association between CYP and P-glycoprotein activities and plasma antidepressant concentration in an outpatient clinical setting. Secondary outcomes were antidepressant efficacy and tolerance. We also describe phenotypes in patients treated with antidepressants and evaluate the tolerance of a minimally invasive phenotyping approach...
March 20, 2018: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/29557814/factors-affecting-time-to-reach-and-recover-from-gefitinib-induced-hepatotoxicity
#12
Yoon Hee Park, Soyeon Cho, Jeong Yee, Jae Youn Kim, Sandy Jeong Rhie, Hye Sun Gwak
Gefitinib is an oral tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR) for non-small-cell lung cancer with EGFR mutations. Although a few studies have analyzed the causes of gefitinib-induced hepatotoxicity, research focusing on the time intervals before and after hepatotoxicity has yet to be reported. Therefore, this study investigated two types of factors: the time to reach gefitinib-induced hepatotoxicity and the time for recovery. From January 2013 to December 2014, a retrospective study was carried out on 473 non-small-cell lung cancer patients who were treated with gefitinib...
March 19, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29557709/disposition-and-metabolism-of-the-g-protein-coupled-receptor-40-agonist-tak-875-fasiglifam-in-rats-dogs-and-humans
#13
Akifumi Kogame, Ronald Lee, Liping Pan, Miyako Sudo, Masami Nonaka, Yuu Moriya, Tomoaki Higuchi, Yoshihiko Tagawa
1. The absorption, distribution, metabolism and excretion of fasiglifam were investigated in rats, dogs, and humans. 2. The absolute oral bioavailability of fasiglifam was high in all species (> 76.0%). 3. After oral administration of [14 C]fasiglifam, the administered radioactivity was quantitatively recovered and the major route of excretion of radioactivity was via feces in all species. 4. Fasiglifam was a major component in the plasma and feces in all species. Its oxidative metabolite (M-I) was observed as a minor metabolite in rat and human plasma (< 10% of plasma radioactivity)...
March 20, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29547545/prediction-of-tacrolimus-exposure-by-cyp3a5-genotype-and-exposure-of-co-administered-everolimus-in-japanese-renal-transplant-recipients
#14
Hideaki Kagaya, Takenori Niioka, Mitsuru Saito, Takamitsu Inoue, Kazuyuki Numakura, Ryohei Yamamoto, Yumiko Akamine, Tomonori Habuchi, Shigeru Satoh, Masatomo Miura
While tacrolimus and everolimus have common metabolic pathways through CYP3A4/5, tacrolimus is metabolized solely by CYP3A4 in recipients with the CYP3A5*3 / *3 . The purpose of this study was to evaluate how the area under the blood concentration-time curves (AUC) of tacrolimus could be predicted based on CYP3A5 genotype and the AUC of everolimus in renal transplant patients taking both drugs. The dose-adjusted AUC (AUC/D) of tacrolimus and everolimus were calculated at one month and one year after transplantation...
March 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29526584/a-systematic-review-of-pharmacokinetic-studies-on-herbal-drug-fuzi-implications-for-fuzi-as-personalized-medicine
#15
Jin-Jun Wu, Zhen-Zhen Guo, Yuan-Feng Zhu, Zhi-Jian Huang, Xia Gong, Yu-Huan Li, Wen-Jie Son, Xiao-Yan Li, Yan-Mei Lou, Li-Jun Zhu, Lin-Lin Lu, Zhong-Qiu Liu, Liang Liu
BACKGROUND: Fuzi, which is the processed lateral roots of Aconitum carmichaeli Debx. (Ranunculaceae), is a traditional herbal medicine that is well known for its excellent pharmacological effects and acute toxicity. Aconitum alkaloids are responsible for its pharmacological activity and toxicity. Although a large number of studies on Fuzi have been reported, no comprehensive review on its pharmacokinetics has yet been published. PURPOSE: This paper seeks to present a comprehensive review regarding the phytochemistry, pharmacokinetic features and toxicity of Fuzi...
March 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29521134/effects-of-cyp3a4-1g-and-cyp3a5-3-polymorphisms-on-pharmacokinetics-of-tylerdipine-hydrochloride-in-healthy-chinese-subjects
#16
Sufeng Zhou, Mingxue Tao, Yuanyuan Wang, Lu Wang, Lijun Xie, Juan Chen, Yuqing Zhao, Yun Liu, Hongwen Zhang, Ning Ou, Guangji Wang, Feng Shao, Jiye Aa
1. The aim of this analysis was to explore the influence of CYP3A4*1G and CYP3A5*3 polymorphisms on the pharmacokinetics of tylerdipine in healthy Chinese subjects. 2. A total of 64 and 63 healthy Chinese subjects were included and identified as the genotypes of CYP3A4*1G and CYP3A5*3, respectively. Plasma samples were collected for up to 24 h post-dose to characterize the pharmacokinetic profile following single oral dose of the drug (5, 15, 20, 25, 30 mg). Plasma levels were measured by a high-performance liquid chromatography-mass spectrometry (LC-MS/MS)...
March 9, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29504673/inhibition-of-in-vitro-metabolism-of-opioids-by-skeletal-muscle-relaxants
#17
David E Moody, Yueqiao Fu, Wenfang B Fang
The purpose of this study was to test the hypothesis that skeletal muscle relaxants could inhibit the in vitro metabolism of common co-medications opioids buprenorphine, methadone and oxycodone. The compounds (solubility-limited concentration (μM) studied) were: baclofen (1000), carisoprodol (200), its metabolite meprobamate (1000), chlorzoxazone (200), cyclobenzaprine (1000), metaxalone (50), methocarbamol (1000), orphenadrine (1000) and tizanidine (1000). Compounds were first incubated with human liver microsomes (HLM) ± pre-incubation, screened with pathway-specific cDNA-expressed cytochrome P450s (rCYP), and then IC50 values determined using either 8-concentration tests for those where the rCYP screen suggested an IC50 was achievable, or a 3-concentration test with downward extrapolation if screen suggested 50% inhibition was not achievable...
March 5, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29498947/pharmacokinetic-properties-of-a-sufentanil-sublingual-tablet-intended-to-treat-acute-pain
#18
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
https://www.readbyqxmd.com/read/29498548/evaluation-of-multikinase-inhibitor-ldn193189-induced-hepatotoxicity-in-teleost-fish-poecilia-latipinna
#19
Isha Ranadive, Sonam Patel, Abhilasha Mhaske, Gowri Kumari Uggini, Isha Desai, Suresh Balakrishnan
Currently, scientists show keen interest in the drugs that inhibit multiple kinases, LDN193189, being an example. It combats certain cancers in vitro as well as in vivo, making it a prerequisite for researchers to study the toxic potential of this drug in animal models. As most of the drugs metabolized by liver cause hepatic injury, LDN193189-induced hepatotoxicity was examined using a teleost fish, Poecilia latipinna. As a prelude, calculation of LD50 showed a value of 95.22 mg/kg body weight and three doses were decided based on it for further evaluations...
March 2, 2018: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/29493154/-transcriptional-regulation-effect-of-thsg-and-anthraquinones-in-tubers-of-polygonum-multiflorum-based-on-human-progesterone-x-receptor-pxr-mediated-cyp3a4-rapid-screening-system
#20
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
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