Drug-induced Cholestasis: Mechanisms, Models, and Markers.

abstract：:This review provides an overview of the in vitro methods currently used in studies of intestinal drug metabolism and active efflux with a special emphasis on the efflux- metabolism interplay. These methods include e.g. expressed enzymes or efflux transporters, fractionated intestinal cells, cell lines, primary cells, ...

journal_title：Current drug metabolism

authors： Siissalo S,Heikkinen AT

更新日期：2013-01-01 00:00:00

abstract：:Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important role in drug discovery and development and several reliable in vitro ADME models are available. Recently higher throughput in vitro ADME screening facilities have been established in order to be able to evaluate an appreciable f...

journal_title：Current drug metabolism

authors： Hop CE,Cole MJ,Davidson RE,Duignan DB,Federico J,Janiszewski JS,Jenkins K,Krueger S,Lebowitz R,Liston TE,Mitchell W,Snyder M,Steyn SJ,Soglia JR,Taylor C,Troutman MD,Umland J,West M,Whalen KM,Zelesky V,Zhao SX

更新日期：2008-11-01 00:00:00

abstract：:Thiopurines such as azathioprine, 6-mercaptopurine and 6-thioguanine are antimetabolites that have been used for several decades in the treatment of several diseases including inflammatory bowel diseases. Additional anti-inflammatory properties of these thiopurines have been discovered in recent years. Thiopurine meta...

journal_title：Current drug metabolism

authors： Van Asseldonk DP,de Boer NK,Peters GJ,Veldkamp AI,Mulder CJ,Van Bodegraven AA

更新日期：2009-11-01 00:00:00

abstract：BACKGROUND:The prolonged circulation time of nanoparticles in the blood is a prerequisite to realize a controlled and targeted (passive or active targeting) release of the encapsulated gene/drug at the desired site of action. The most popular method to mask or camouflage nanoparticles is the adsorbed, grafted or conjug...

journal_title：Current drug metabolism

authors： Hu J,Sheng Y,Shi J,Yu B,Yu Z,Liao G

更新日期：2018-01-01 00:00:00

abstract：:There are several clinically useful endoperoxides, mainly artemisinin derivatives available in market for the treatment of malaria. These are highly potent drugs, with fastest parasite reduction ratio, broadest parasite stage specificity and effectiveness against all species of plasmodium in human. Endoperoxides are c...

journal_title：Current drug metabolism

authors： Gautam A,Ahmed T,Batra V,Paliwal J

更新日期：2009-03-01 00:00:00

abstract：BACKGROUND:In recent times, herbals or phytomedicines have become very popular due to their global acceptance as a complementary and alternative remedy. While modern drugs are commercially available only after laboratory validations, clinical trials, as well as approval from drug regulatory authorities, majority of the...

journal_title：Current drug metabolism

authors： Parvez MK,Rishi V

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Wound healing is a composite and vital process in which devitalized tissue layers and cellular structures repair themselves. Bronchiolitis is generally prompted by respiratory syncytial virus or human metapneumovirus; this condition is an acute inflammatory injury of bronchioles. Heart problems that develop ...

journal_title：Current drug metabolism

authors： AlMatar M,Batool T,Makky EA

更新日期：2016-01-01 00:00:00

abstract：:A number of studies have appeared recently on the underlying mechanisms of liposome-cell interactions under in vitro conditions, in which isolated cell populations or cell lines were used. However, our knowledge of how liposomes interact with cells and the parameters that influence this in vivo is limited. We will sum...

journal_title：Current drug metabolism

authors： Ishida T,Harashima H,Kiwada H

更新日期：2001-12-01 00:00:00

abstract：BACKGROUND:Nobel laureate Sir James Black's molecule, propranolol, still has broad potential in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of prop...

journal_title：Current drug metabolism

authors： Kalam MN,Rasool MF,Rehman AU,Ahmed N

更新日期：2020-01-01 00:00:00

abstract：:Human genome sequencing highlights the involvement of genetic variation towards differential risk of human diseases, presence of different phenotypes, and response to pharmacological elements. This brings the field of personalized medicine to forefront in the era of modern health care. Numerous recent approaches have ...

journal_title：Current drug metabolism

authors： Prakash S,Agrawal S

更新日期：2016-01-01 00:00:00

abstract：:With the recent advancement in nanoscience and nanotechnology, there is a growing demand for assessment of the toxicological effects of nano materials to humans and other biological systems. And a predictive toxicology approach that uses in vitro screening assays in conjunction with in vivo study results are widely em...

journal_title：Current drug metabolism

authors： Suma RN,Mohanan PV

更新日期：2015-01-01 00:00:00

abstract：:The aim of the present study was to develop and improve methods for phenotyping of CYP2E1, an important enzyme in the biotransformation of many industrial chemicals, therapeutic drugs and endogenous substances. The possibility to measure CYP2E1 activity in lymphocytes by using p-nitrophenol as a substrate and CYP2E1 p...

journal_title：Current drug metabolism

authors： Ernstgård L,Johanson G,Karlsson AS,Warholm M

更新日期：2007-06-01 00:00:00

abstract：:For the pharmaceutical industry, one of the challenges in evaluating the risk of future compound attrition at the discovery stage is the successful prediction of the major routes of clearance in humans. For compounds cleared by metabolism, such information will help to avoid the development of compounds that will exhi...

journal_title：Current drug metabolism

authors： Williams JA,Hurst SI,Bauman J,Jones BC,Hyland R,Gibbs JP,Obach RS,Ball SE

更新日期：2003-12-01 00:00:00

abstract：:Diabetes is associated with an increase risk for cardiovascular disease (CVD). Recently, macrovascular complications of diabetes have been shown to start before the development of diabetes. Indeed, several clinical studies have confirmed the increased risk of CVD in patients with impaired glucose tolerance (IGT). Sinc...

journal_title：Current drug metabolism

authors： Yamagishi S,Matsui T,Ueda S,Fukami K,Okuda S

更新日期：2009-02-01 00:00:00

abstract：:The present study was designed to investigate the hepatic disposition of the prodrug AM365 and the generated antiviral guanosine analogue, AM188 in the isolated perfused rat liver (IPL). The livers of rats (n=12) were isolated and perfused with Krebs-Henseleit pH 7.4 buffer to which AM365 was added as a bolus to achie...

journal_title：Current drug metabolism

authors： Wang J,Nation RL,Evans AM,Cox S,Shackleford D

更新日期：2005-10-01 00:00:00

abstract：:Recently, it was found that mutations in the binding cavity of drug-metabolizing Cytochrome P450 BM3 mutants can result in major changes in regioselectivity in testosterone (TES) hydroxylation. In the current work, we report the intrinsic reactivity of TES' C-H bonds and our attempts to rationalize experimentally obse...

journal_title：Current drug metabolism

authors： de Beer SB,van Bergen LA,Keijzer K,Rea V,Venkataraman H,Guerra CF,Bickelhaupt FM,Vermeulen NP,Commandeur JN,Geerke DP

更新日期：2012-02-01 00:00:00

abstract：:Transplantation has become an established and successful therapy. Rejections and infections are the principal immune-related complications in the post-transplant course. A reliable and early diagnosis is necessary to prevent graft failure and patient morbidity. Despite the immunologic nature of these complications the...

journal_title：Current drug metabolism

authors： Grebe SO,Mueller TF

更新日期：2002-04-01 00:00:00

abstract：:Cytochrome P450s (P450 or CYPs) comprise a superfamily of enzymes that catalyze the oxidation of a wide variety of xenobiotic chemicals. Although most of P450 inhibitors decrease the metabolic activities mediated by the corresponding P450 forms, unexpected phenomena, which are called as activation or heterotropic coop...

journal_title：Current drug metabolism

authors： Niwa T,Murayama N,Yamazaki H

更新日期：2008-06-01 00:00:00

abstract：:Ageing is characterized by a progressive decline in the functional reserve of multiple organs and systems, which can influence drug disposition. In addition, comorbidity and polypharmacy are highly prevalent in the elderly. As ageing is associated with some reduction in first-pass metabolism, bioavailability of a few ...

journal_title：Current drug metabolism

authors： Shi S,Klotz U

更新日期：2011-09-01 00:00:00

abstract：:Fluoropyrimidines and oxaliplatin continued to be the mainstay of therapeutic regimens in the treatment of colorectal cancer (CRC). For this reason, pharmacokinetic and metabolism of these drugs were analyzed and the identification of accurate and validated predictive, prognostic and toxicity markers became necessary ...

journal_title：Current drug metabolism

authors： Gnoni A,Russo A,Silvestris N,Maiello E,Vacca A,Marech I,Numico G,Paradiso A,Lorusso V,Azzariti A

更新日期：2011-12-01 00:00:00

abstract：:P-glycoprotein (P-gp) is involved in MDR and in neurodegenerative disorders such as Parkinson disease (PD), Alzheimer disease (AD) and epilepsy. Cytochrome P450 enzymes (CYP450s) catalyze the metabolism of a wide variety of endogenous and exogenous compounds including xenobiotics, drugs, environmental toxins, steroids...

journal_title：Current drug metabolism

authors： Inglese C,Perrone MG,Berardi F,Perrone R,Colabufo NA

更新日期：2011-10-01 00:00:00

abstract：:This paper reviews the metabolism of new designer drugs of abuse that have emerged on the black market during the last years and is an update of a review published in 2005. The presented review contains data concerning the so-called 2C compounds (phenethylamine type) such as 4-bromo-2,5-dimethoxy-beta-phenethylamine (...

journal_title：Current drug metabolism

authors： Meyer MR,Maurer HH

更新日期：2010-06-01 00:00:00

abstract：:Chronic heart failure (CHF) is now recognized as a multisystem disorder with increased sympathetic tone, hormonal derangements, an anabolic/catabolic imbalance, endothelial dysfunction, and systemic low-grade inflammation affecting various organ systems. Pro-inflammatory cytokines appear to play important roles in tha...

journal_title：Current drug metabolism

authors： Sandek A,Anker SD,von Haehling S

更新日期：2009-01-01 00:00:00

abstract：OBJECTIVES:Induction or inhibition of cytochrome P450 (CYP) enzyme activities, enzymes that activate or detoxify xenobiotics, is one mechanism by which vegetables may alter cancer risk. As the effect of food on CYP enzyme activities have not been studied in the Jordanian population, we examined the effect of supplement...

journal_title：Current drug metabolism

authors： Hakooz N,Hamdan I

更新日期：2007-01-01 00:00:00

abstract：:In recent years several arylpiperazine derivatives have reached the stage of clinical application, mainly for the treatment of depression, psychosis or anxiety. Examples are the pyrimidinylpiperazine buspirone, the chlorophenylpiperazine derivatives nefazodone and trazodone, the dichlorophenylpiperazine aripiprazole a...

journal_title：Current drug metabolism

authors： Caccia S

更新日期：2007-08-01 00:00:00

abstract：:The nature and level of systemic exposure to the active herbal constituents will profoundly affect their effects at action sites, which is fundamental in understanding their roles in the overall beneficial effects of a herbal medicine. The objective of this study is to gain a full picture of the systemic exposure to v...

journal_title：Current drug metabolism

authors： Li L,Zhao Y,Du F,Yang J,Xu F,Niu W,Ren Y,Li C

更新日期：2012-06-01 00:00:00

abstract：:Understanding the mechanism of action of organophosphates (OP)/nerve agents -- irreversible acetylcholinesterase (AChE, EC 3.1.1.7) inhibition at the cholinergic synapses followed by metabolic dysbalance of the organism -- two therapeutic principles for antidotal treatment are derived. The main drugs are anticholinerg...

journal_title：Current drug metabolism

authors： Bajgar J,Kuca K,Jun D,Bartosova L,Fusek J

更新日期：2007-12-01 00:00:00

abstract：:Several epidemiological studies throughout the years have suggested that polyphenols from fruits and vegetables promote health and reduce the risk of certain chronic and neurodegenerative diseases. Yet, it has been proved to be extremely difficult to quantitatively establish the benefit afforded by polyphenols, princi...

journal_title：Current drug metabolism

authors： Rubió L,Macià A,Motilva MJ

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Various transporters, including efflux transporters and uptake transporters, play an important role in the pharmacokinetics of drugs. Currently, studies suggest that several antibiotics also serve as substrates for transporters. In addition, these antibiotics are usually combined with other drugs to treat di...

journal_title：Current drug metabolism

authors： Hua WJ,Hua WX,Jian Z,Wei PH,Ni LY,Hua LY,Wen CD,Ying Z,Li C

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Despite recent therapeutic advances, osteoarthritis continues to be a challenging health problem, especially in the elderly population. Opioids, which are potent analgesics, have shown an extraordinary ability to reduce intense pain in many osteoarthritic clinical trials; however, there is an increased need ...

journal_title：Current drug metabolism

authors： Alhaj-Suliman SO,Milavetz G,Salem AK

更新日期：2020-01-01 00:00:00