journal
https://read.qxmd.com/read/38523539/the-metabolism-of-the-new-benzodiazepine-remimazolam
#1
JOURNAL ARTICLE
Wolfgang Schmalix, Karl-Uwe Petersen, Marija Pesic, Thomas Stöhr
BACKGROUND: Remimazolam (RMZ) is a novel ultrashort-acting benzodiazepine used for sedation by intravenous administration. The pharmacophore of RMZ includes a carboxyl ester group sensitive to esterase- mediated hydrolysis, which is the primary path of metabolic elimination. However, for the sake of drug safety, a deeper and broader knowledge of the involved metabolic pathways and the evolving metabolites is required. Information is needed on both humans and experimental animals to evaluate the possibility that humans form harmful metabolites not encountered in animal toxicity studies...
March 21, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38523538/effects-of-clarithromycin-and-ketoconazole-on-fk506-metabolism-in-different-cyp3a4-genotype-recombinant-metabolic-enzyme-systems
#2
JOURNAL ARTICLE
Jinhua Wen, Yuwei Xiao, Menghua Zhao, Chen Yang, Weiqiang Hu
OBJECTIVE: This study aimed to investigate the effects of clarithromycin and ketoconazole on the pharmacokinetic properties of tacrolimus in different CYP3A4 genotype recombinant metabolic enzyme systems, so as to understand the drug interactions and their mechanisms further. METHOD: The experiment was divided into three groups: a blank control group, CYP3A4*1 group and CYP3A4*18 recombinant enzyme group. Each group was added with tacrolimus (FK506) of a series of concentrations...
March 20, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38509678/unraveling-the-role-of-comt-polymorphism-in-dopamine-mediated-vasopressor-effects-an-observational-cross-sectional-study
#3
JOURNAL ARTICLE
Kannan Sridharan, Anfal Jassim, Ali Mohammed Qader, Sheikh Abdul Azeez Pasha
AIMS: To evaluate the association between rs4680 polymorphism in the COMT gene and the vasoconstrictive effects of commonly used vasopressors. BACKGROUND: Dopamine is a medication that is given intravenously to critically ill patients to help increase blood pressure. Catechol O-Methyl Transferase (COMT) breaks down dopamine and other catecholamines. There is a genetic variation in the COMT gene called rs4680 that can affect how well the enzyme works. Studies have shown that people with this genetic variation may have different blood pressure levels...
March 20, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38509677/association-of-ugt1a-gene-polymorphisms-with-bkv-infection-in-renal-transplantation-recipients
#4
JOURNAL ARTICLE
Jingwen Yuan, Shuang Fei, Zeping Gui, Zijie Wang, Hao Chen, Li Sun, Jun Tao, Zhijian Han, Xiaobin Ju, Ruoyun Tan, Min Gu, Zhengkai Huang
BK virus (BKV) infection is an opportunistic infectious complication and constitutes a risk factor for premature graft failure in kidney transplantation. Our research aimed to identify associations and assess the impact of single-nucleotide polymorphisms (SNPs) on metabolism-related genes in patients who have undergone kidney transplantation with BKV infection. <p> Material/Methods: The DNA samples of 200 eligible kidney transplant recipients from our center, meeting the inclusion criteria, have been collected and extracted...
March 19, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38504562/fluoropyrimidine-toxicity-the-hidden-secrets-of-dpyd
#5
JOURNAL ARTICLE
Vangelis G Manolopoulos, Georgia Ragia
BACKGROUND: Fluoropyrimidine-induced toxicity is a main limitation of therapy. Currently, polymorphisms in the DPYD gene, which encodes the 5-FU activation enzyme dihydropyrimidine dehydrogenase (DPD), are used to adjust the dosage and prevent toxicity. Despite the predictive value of DPYD genotyping, a great proportion of fluoropyrimidine toxicity cannot be solely explained by DPYD variations. OBJECTIVE: We herein summarize additional sources of DPD enzyme activity variability, spanning from epigenetic regulation of DPYD expression, factors potentially inducing protein modifications, as well as drug-enzyme interactions that contribute to fluoropyrimidine toxicity...
March 19, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38482621/safety-aspects-of-herb-interactions-current-understanding-and-future-prospects
#6
JOURNAL ARTICLE
Subhajit Hazra, Preet Amol Singh
BACKGROUND: The use of herbal medicines is on the rise throughout the world due to their perceived safety profile. However, incidences of herb-drug, herb-herb and herb-food interactions considering safety aspects have opened new arenas for discussion. OBJECTIVE: The current study aims to provide comprehensive insights into the various types of herb interactions, the mechanisms involved, their assessment, and historical developments, keeping herbal safety at the central point of discussion...
March 12, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38468514/altitude-effect-on-propofol-pharmacokinetics-in-rats
#7
JOURNAL ARTICLE
Lijun Li, Xuejun Wang, Sheng Wang, Li Wen, Haopeng Zhang
BACKGROUND: Propofol is an intravenous agent for clinical anesthesia. As the influence of the hypobaric- hypoxic environment (Qinghai-Tibetan region, altitude: 2800-4300 m, PaO2: 15.1-12.4 kPa) on the metabolism of Propofol is complex, the research results on the metabolic characteristics of Propofol in high-altitude areas remain unclear. This study aimed to investigate the pharmacokinetic characteristics of Propofol in a high-altitude hypoxic environment using animal experiments. METHODS: Rats were randomly divided into three groups: high-altitude, medium-altitude, and plain groups...
March 11, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38465436/safety-issues-of-herb-warfarin-interactions
#8
JOURNAL ARTICLE
Subhajit Hazra, Preet Amol Singh, Neha Bajwa
Warfarin is a popular anticoagulant with high global demand. However, studies have underlined serious safety issues when warfarin is consumed concomitantly with herbs or its formulations. This review aimed to highlight the mechanisms behind herb-warfarin interactions while laying special emphasis on its PKPD interactions and evidence on Herb-Warfarin Interaction (HWI) with regards to three different scenarios, such as when warfarin is consumed with herbs taken as foods or prescribed as medicine, or when used in special situations...
March 8, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38454771/a-phase-i-clinical-study-of-the-pharmacokinetics-and-safety-of-prusogliptin-tablets-in-subjects-with-mild-to-moderate-hepatic-insufficiency-and-normal-liver-function
#9
JOURNAL ARTICLE
Huiting Zhang, Yicong Bian, Weifeng Zhao, Liyan Miao, Hua Zhang, Juanjuan Cui, Xiaofang Zhang, Xueyuan Zhang, Wen Cai
BACKGROUND: Prusogliptin is a potent and selective DPP-4 inhibitor. In different animal models, Prusogliptin showed potential efficacy in the treatment of type 2 diabetes. However, the knowledge of its pharmacokinetics and safety in patients with liver dysfunction is limited. OBJECTIVES: The present study evaluated the pharmacokinetics and safety of Prusogliptin in subjects with mild or moderate hepatic impairment compared with healthy subjects. METHODS: According to the liver function of the subjects, we divided them into a mild liver dysfunction group, a moderate liver dysfunction group and a normal liver function group...
March 5, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38445694/comparative-analysis-of-machine-learning-algorithms-evaluating-the-single-nucleotide-polymorphisms-of-metabolizing-enzymes-with-clinical-outcomes-following-intravenous-paracetamol-in-preterm-neonates-with-patent-ductus-arteriosus
#10
JOURNAL ARTICLE
Kannan Sridharan, George Priya Doss C, Hephzibah Cathryn R, Thirumal Kumar D, Muna Al Jufairi
AIMS: Pharmacogenomics has been identified to play a crucial role in determining drug response. The present study aimed to identify significant genetic predictor variables influencing the therapeutic effect of paracetamol for new indications in preterm neonates. BACKGROUND: Paracetamol has recently been preferred as a first-line drug for managing Patent Ductus Arteriosus (PDA) in preterm neonates. Single Nucleotide Polymorphisms (SNPs) in CYP1A2, CYP2A6, CYP2D6, CYP2E1, and CYP3A4 have been observed to influence the therapeutic concentrations of paracetamol...
March 5, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38441017/the-role-of-cyps-and-transporters-in-the-biotransformation-and-transport-of-the-anti-hepatitis-c-antiviral-agents-asunaprevir-daclatasvir-and-beclabuvir-impact-of-liver-disease-race-and-drug-drug-interactions-on-safety-and-efficacy
#11
JOURNAL ARTICLE
Michael Murray
Asunaprevir, daclatasvir, and beclabuvir are direct-acting antiviral agents used in the treatment of patients infected with hepatitis C genotype 1b. This article reviews the biotransformation and disposition of these drugs in relation to the safety and efficacy of therapy. CYP3A4 and 3A5 catalyze the oxidative biotransformation of the drugs, while P-glycoprotein mediates their efflux from tissues. Asunaprevir is also a substrate for the influx transporters OATP1B1 and OATP2B1 and the efflux transporter MRP2, while beclabuvir is also a substrate for the efflux transporter BCRP...
March 1, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38415474/a-combination-of-magnoflorine-and-spinosin-improves-the-antidepressant-effects-on-cums-mouse-model
#12
JOURNAL ARTICLE
Fenghe Bi, Zhihui Wang, Yijing Guo, Menglin Xia, Xuehui Zhu, Wei Qiao
BACKGROUND: Depression is a common neuropsychiatric disease. As a famous traditional Chinese medicine with significant anti-depressive and sleep-promoting effects, Ziziphi Spinosae Semen (ZSS) has attracted the attention of many researchers. Although it is well known that Magnoflorine (MAG) and Spinosin (SPI) were the main active components isolated from ZSS, there is a lack of research on the combined treatment of depression with these two ingredients. METHODS: The shaking bottle method was used to simulate the human environment for detecting the changes in oil-water partition coefficient before and after the drug combination...
February 23, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38409697/effect-of-high-altitude-environment-on-pharmacokinetic-and-pharmacodynamic-of-warfarin-in-rats
#13
JOURNAL ARTICLE
Xiaojing Zhang, Hongfang Mu, Yan Zhong, Rong Wang, Wenbin Li
BACKGROUND: High altitude environment affects the pharmacokinetic (PK) parameters of drugs and the PK parameters are an important theoretical basis for guiding the rational clinical use of drugs. Warfarin is an oral anticoagulant of the coumarin class commonly used in clinical practice, but it has a narrow therapeutic window and wide individual variation. However, the effect of high altitude environment on PK and pharmacodynamic (PD) of warfarin is unclear. OBJECTIVE: The objective of this study is to investigate the effect of a high altitude environment on PK and PD of warfarin in rats...
February 21, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38409696/recent-advances-in-hepatic-metabolic-regulation-by-the-nuclear-factor-rev-erb%C3%A9
#14
JOURNAL ARTICLE
Qi Zhang, Yutong Chen, Jingqi Li, Haishan Xia, Yongbin Tong, Yuyu Liu
Rev-erbɑ (NR1D1) is a nuclear receptor superfamily member that plays a vital role in mammalian molecular clocks and metabolism. Rev-erbɑ can regulate the metabolism of drugs and the body's glucose metabolism, lipid metabolism, and adipogenesis. It is even one of the important regulatory factors regulating the occurrence of metabolic diseases (e.g., diabetes, fatty liver). Metabolic enzymes mediate most drug metabolic reactions in the body. Rev-erbɑ has been recognized to regulate drug metabolic enzymes (such as Cyp2b10 and Ugt1a9)...
February 21, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38258775/effect-of-dexketoprofen-on-the-disposition-kinetics-of-moxifloxacin-in-plasma-and-lung-in-male-and-female-rats
#15
JOURNAL ARTICLE
Teslime Erdogan, Halis Oguz, Orhan Corum
BACKGROUND: The simultaneous use of NSAIDs and antibiotics is recommended for bacterial dis-eases in human and veterinary medicine. Moxifloxacin (MFX) and dexketoprofen (DEX) can be used simul-taneously in bacterial infections. However, there are no studies on how the simultaneous use of DEX affects the pharmacokinetics of MFX in rats. OBJECTIVES: The aim of this study was to determine the effect of DEX on plasma and lung pharmacokinetics of MFX in male and female rats...
January 22, 2024: Current Drug Metabolism
https://read.qxmd.com/read/38141188/the-impacts-and-changes-related-to-the-cancer-drug-resistance-mechanism
#16
JOURNAL ARTICLE
Prachi Varshney, Vishal Sharma, Devdhar Yadav, Yogesh Kumar, Amit Singh, Naga Rani Kagithala, Pramod Kumar Sharma, Omji Porwal, Neeraj Kumar Fuloria, Pradeep Kumar Sharma, Ashok Kumar Gupta, Koteswara Rao Gsn
BACKGROUND: Cancer drug resistance remains a difficult barrier to effective treatment, necessitating a thorough understanding of its multi-layered mechanism. OBJECTIVE: This study aims to comprehensively explore the diverse mechanisms of cancer drug resistance, assess the evolution of resistance detection methods, and identify strategies for overcoming this challenge. The evolution of resistance detection methods and identification strategies for overcoming the challenge...
December 20, 2023: Current Drug Metabolism
https://read.qxmd.com/read/38141187/comparative-pharmacokinetics-of-%C3%A4-ntravenous-enrofloxacin-in-one-six-and-twelve-month-old-sheep
#17
JOURNAL ARTICLE
Devran Coskun, Orhan Corum, Duygu Durna Corum, Kamil Uney
BACKGROUND: Enrofloxacin (ENR) is a fluoroquinolone antibiotic approved for use in sheep of all ages. The body composition and metabolic capability change with age. These changes may alter the pharmacokinetics of drugs and thus their effect. Therefore, the pharmacokinetics of drugs need to be established in target-age animals. OBJECTIVE: To determine the pharmacokinetics of ENR and its active metabolite, ciprofloxacin (CIP), following a single intravenous administration of ENR at a dose of 10 mg/kg in different ages of sheep...
December 20, 2023: Current Drug Metabolism
https://read.qxmd.com/read/38141186/reassessment-of-radiation-exposure-from-bone-scintigraphy
#18
JOURNAL ARTICLE
Handan Tanyildizi-Kökkülünk, Ahmet Murat Şenişik, Mahmut Yüksel
AIM: This study was aimed to re-determine the radiation dose rate emitted from the patients who underwent bone scintigraphy. MATERIAL AND METHODS: A mean of 20.87±2.54 mCi 99mTc-MDP was injected into patients. A GM counter was used to measure dose rates in 3 different periods, at intervals of 25, 50, 100, 150, and 200 cm from the patient's anterior for head, thorax, abdomen, and pelvis levels. Measurements were used to determine patient-induced environmental doses and radiation doses to personnel/patient relatives...
December 20, 2023: Current Drug Metabolism
https://read.qxmd.com/read/38099536/theoretical-evaluation-of-oleocanthal-reactive-centers
#19
JOURNAL ARTICLE
Mohammad Hossein Asgarshamsi, Mehrdad Mohammadpour Dehkordi, Seyed Mohamad Reza Nazifi Reza Nazifi, Krzysztof K Zborowski
BACKGROUND: Decarboxymethyl ligstroside aglycone (oleocanthal) is an essential component of olive oil. It is therefore interesting to study its metabolism in the human body. In order to find the best possible starting point for this metabolism, a theoretical study was carried out using DFT calculations and docking studies. METHODS: The DFT, B3LYP/6-311++G** and the PCM solvation model calculations were used to study the initial process of oleocanthal metabolism by the CYP1A2 enzyme...
December 11, 2023: Current Drug Metabolism
https://read.qxmd.com/read/38073103/pharmacokinetics-mass-balance-tissue-distribution-and-metabolism-of-14c-101bhg-d01-a-novel-muscarinic-receptor-antagonist-in-rats
#20
JOURNAL ARTICLE
Huaye Gao, Cheng Yang, Wenhui Hu, Juefang Ding, Xingxing Diao, Yuandong Zheng, Chang Shu, Li Ding
BACKGROUND: 101BHG-D01, a novel long-acting and selective muscarinic receptor antagonist for the treatment of chronic obstructive pulmonary disease (COPD), is undergoing Phase Ib clinical trial in patients and has shown its potential efficacy. Its preparation method and medical use thereof have been patented in the United States (Patent No.US9751875B2). OBJECTIVE: In this study, the pharmacokinetics, mass balance, tissue distribution and metabolism of radioactive 101BHG-D01 were investigated in rats after an intravenous dose of 1 mg/kg [14C]101BHG-D01 (100 μCi/kg)...
December 8, 2023: Current Drug Metabolism
journal
journal
35112
1
2
Fetch more papers »
Fetching more papers... Fetching...
Remove bar
Read by QxMD icon Read
×

Save your favorite articles in one place with a free QxMD account.

×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"

We want to hear from doctors like you!

Take a second to answer a survey question.