Glucuronidation of capsaicin by liver microsomes and expressed UGT enzymes: reaction kinetics, contribution of individual enzymes and marked species differences.

abstract：:Valproate (2-propylpentanoate) is available as valproic acid, sodium valproate and semisodium valproate. It has actions on dopamine, GABA and glutamate neurotransmission and intracellular signaling. Its main psychiatric use is to treat bipolar disorder. It has been used in other psychiatric disorders, including schizo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Haddad PM,Das A,Ashfaq M,Wieck A

更新日期：2009-05-01 00:00:00

abstract：:Rats are an important tool in pharmacology and toxicology. The authors focus on rat P450s in relation to diazepam metabolism. In particular, considerable attention is devoted to the CYP2D subfamily, which is a group of highly polymorphic enzymes. First, the metabolic profiles of diazepam of humans and other animals ar...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Sakai N,Ishizuka M

更新日期：2009-11-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The prevalence of acute renal allograft rejection has decreased substantially in past decades due to new and more specific immunosuppressive compounds but improvements in long-term graft function have not been achieved. There is a large need for new immunosuppressive agents that lack toxicity of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Matz M,Naik M,Mashreghi MF,Glander P,Neumayer HH,Budde K

更新日期：2011-01-01 00:00:00

abstract：INTRODUCTION:Enzalutamide is the first approved second-generation androgen receptor (AR) antagonist in the treatment of metastatic castration-resistant prostate cancer (mCRPC) with or without docetaxel-based chemotherapy. Over the past 5 years, a number of attempts were made to determine the efficacy of enzalutamide in...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hong JH

更新日期：2018-03-01 00:00:00

abstract：:Changes in mammalian diets alter the hepatic expression of CYP drug-metabolising enzymes and endobiotic oxidases. Thus, dietary constituents may significantly influence the duration of action of chemicals in tissues. Recent improvements in the mechanistic information on the regulation of constitutive and inducible exp...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Murray M

更新日期：2007-04-01 00:00:00

abstract：INTRODUCTION:Picoplatin was developed as platinum coordination complex to overcome development of resistance, through conjugation to thioles, by the introduction of a methyl-pyridine moiety into the cisplatin parent structure. Pharmacokinetic parameters of the drug, after intravenous and oral application, were studied ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hamilton G

更新日期：2013-10-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The use of the first generation non-nucleoside reverse transcriptase inhibitor efavirenz (EFV) as a component of first-line antiretroviral therapy has been accepted worldwide. EFV is the only antiretroviral agent currently on the market that has been combined with emtricitabine and tenofovir dis...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rakhmanina NY,van den Anker JN

更新日期：2010-01-01 00:00:00

abstract：:Toxicogenomics is the application of gene expression profiling technology to toxicology. This results in the generation of very large and complex gene expression data sets associated with the development of toxicities. It is widely assumed that this data can be deconvoluted to reveal novel insights into toxicological ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huby R,Tugwood JD

更新日期：2005-08-01 00:00:00

abstract：INTRODUCTION:Raltegravir was the first available integrase inhibitor for treating HIV-positive patients. This review aims to provide an overview of its role in the management of HIV-1 infection, highlighting its key pharmacokinetic and pharmacodynamic properties. AREAS COVERED:This review covers material searched and ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Calcagno A,D'Avolio A,Bonora S

更新日期：2015-07-01 00:00:00

abstract：:There is wide inter-individual variability in the pharmacokinetics, pharmacodynamics and tolerance of anticancer drugs. Recent evidence suggests that there is even greater variability between individuals of different ethnicity. Allelic variants of genes encoding drug metabolising enzymes are expressed with different i...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Phan VH,Moore MM,McLachlan AJ,Piquette-Miller M,Xu H,Clarke SJ

更新日期：2009-03-01 00:00:00

abstract：INTRODUCTION:Major depressive disorder (MDD), one of the most common disorders in medical practice and one of the leading causes of disability worldwide, is frequently comorbid with anxiety disorders. Vortioxetine (Lu AA21004) is a new antidepressant that combines a number of neurotransmitter reuptake and receptor effe...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Dubovsky SL

更新日期：2014-05-01 00:00:00

abstract：BACKGROUND:The aim of the study was to evaluate the bioequivalence of two itraconazole 100 mg capsule formulations. RESEARCH DESIGN AND METHODS:The single-center, open-label, randomized, three-period, three-sequence, reference-replicated, cross-over study included 38 healthy subjects under fed conditions. In each stud...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Dragojević-Simić V,Kovačević A,Jaćević V,Rančić N,Djordjević S,Kilibarda V,Mikov M,Bokonjić D

更新日期：2018-09-01 00:00:00

abstract：INTRODUCTION:Chronic low back pain (CLBP) is a common and difficult illness to manage. Some individuals with CLBP have pain processing disorders and are also at risk for opioid abuse, misuse; addiction and diversion. Guidelines have been published to guide management; neuromodulation, exercise, mindfulness-based stress...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Davis MP

更新日期：2016-07-01 00:00:00

abstract：INTRODUCTION:Chronic hepatitis C virus (HCV) infection has recently become a curable disease with antiviral therapy. The knowledge of drug interactions using direct-acting antivirals (DAA) may permit maximizing antiviral efficacy and avoiding drug-related toxicities. Ageing in the chronic hepatitis C population, along ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Soriano V,Labarga P,Barreiro P,Fernandez-Montero JV,de Mendoza C,Esposito I,Benítez-Gutiérrez L,Peña JM

更新日期：2015-03-01 00:00:00

abstract：INTRODUCTION:Emtricitabine/tenofovir disoproxil fumarate fixed-dose combination (FTC/TDF FDC) is the co-formulation of a nucleoside and a nucleotide, respectively. After oral administration, both drugs exhibit plasma and intracellular half-lives suitable for once-daily dosing. Within the host cells, active metabolites ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Uglietti A,Zanaboni D,Gnarini M,Maserati R

更新日期：2012-10-01 00:00:00

abstract：INTRODUCTION:Invasive fungal infections remain a leading cause of infectious morbidity and mortality in immunocompromised patients. There are relatively few effective antifungal agents, and currently available agents all have significant limitations. Isavuconazole is a novel second-generation triazole with broad-spectr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Livermore J,Hope W

更新日期：2012-06-01 00:00:00

abstract：INTRODUCTION:Sumatriptan was developed more than 20 years ago as a 5-HT1B/1D receptor agonist, the first drug in a new class of specific anti-migraine drugs, the triptans. A large amount of information and experience has been gained from the clinical trials undertaken as well the various formulations of sumatriptan use...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tfelt-Hansen P,Hougaard A

更新日期：2013-01-01 00:00:00

abstract：INTRODUCTION:It is widely accepted that current practice of polypharmacy inevitably increases the incidence of drug-drug interactions (DDIs). Serious DDIs are a major liability for new molecular entities entering the pharmaceutical market. Various strategies are employed to avoid problematic compounds for clinical deve...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Riley RJ,Wilson CE

更新日期：2015-04-01 00:00:00

abstract：:There is an increasing recognition within the pharmaceutical industry of the importance of the ADME studies in drug registration. Consequently, there has been a drive in recent times to conduct the ADME studies as early as possible in the development programme. There are, however, regulatory barriers, particularly in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lappin G,Garner RC

更新日期：2005-06-01 00:00:00

abstract：INTRODUCTION:Variations in the human genome sequence sometimes play an important role in pharmacokinetics and/or pharmacodynamics. Previous studies have demonstrated a high degree of variation both between and within different ethnic populations. Areas covered: This review sought to summarize key SNPs in CYP2B6, CYP3A ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Neary M,Owen A

更新日期：2017-11-01 00:00:00

abstract：INTRODUCTION:The elucidation of the toxicological mechanisms of herbal medicines is becoming more and more important with the increasing application of herbal medicines, for treatment of various diseases and the promotion of health. Furthermore, it is widely recognized that as herbal components undergo bioactivation, t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Fang ZZ,Zhang YY,Wang XL,Cao YF,Huo H,Yang L

更新日期：2011-08-01 00:00:00

abstract：:Knowledge of pharmacokinetics and the use of a mechanistic-based approach can improve our ability to predict the effects of pregnancy for medications when data are limited. Despite the many physiological changes that occur during pregnancy that could theoretically affect absorption, bioavailability does not appear to ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Anderson GD

更新日期：2006-12-01 00:00:00

abstract：:The onset, intensity and duration of therapeutic response to a compound depend on the intrinsic pharmacological activity of the drug and pharmacokinetic factors related to its absorption, distribution, metabolism and elimination that are inherent to the biological system. The process of drug transfer from the site of ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hurst S,Loi CM,Brodfuehrer J,El-Kattan A

更新日期：2007-08-01 00:00:00

abstract：INTRODUCTION:Pregabalin is an alternative compound to SSRIs and SNRIs for the first-line treatment of generalized anxiety disorder (GAD). Areas covered: We describe the pharmacokinetic properties of pregabalin and their implications for the treatment of GAD. A search in the main database sources (Medline, ISI, Web of K...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Buoli M,Caldiroli A,Serati M

更新日期：2017-03-01 00:00:00

abstract：INTRODUCTION:Pediatric critical illness and associated alterations in organ function can change drug pharmacokinetics (PK). Extracorporeal membrane oxygenation (ECMO), a life-saving therapy for severe cardiac and/or respiratory failure, causes additional PK alterations that affect drug disposition. AREAS COVERED:The p...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Himebauch AS,Kilbaugh TJ,Zuppa AF

更新日期：2016-10-01 00:00:00

abstract：INTRODUCTION:Golimumab is a human anti-TNF monoclonal antibody that was derived from human antibody-transgenic mice. Golimumab demonstrated meaningful clinical benefit and tolerable safety in patients with active rheumatoid arthritis (RA) who were methotrexate (MTX)-naïve, or who inadequately responded to MTX or who ha...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Tanaka Y,Senoo A,Fujii H,Baker D

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Cytochrome P450 2E1 (CYP2E1) plays a central role in the metabolism and metabolic activation of a large number of small, mostly xenobiotic compounds. These qualities distinguish CYP2E1 from traditional enzymes and pose significant challenges to understanding the role and consequences of CYP2E1-mediated metab...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Miller GP

更新日期：2008-08-01 00:00:00

abstract：BACKGROUND:Carboxylesterases (CEs) are ubiquitous enzymes responsible for the hydrolysis of numerous clinically useful drugs. As ester moieties are frequently included in molecules to improve their water solubility and bioavailability, de facto they become substrates for CEs. OBJECTIVE:In this review, we describe the ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Hatfield JM,Wierdl M,Wadkins RM,Potter PM

更新日期：2008-09-01 00:00:00

abstract：INTRODUCTION:The key feature of the newborn is its fast age-dependent maturation, resulting in extensive variability in pharmacokinetics and -dynamics, further aggravated by newly emerging covariates like treatment modalities, environmental issues or pharmacogenetics. This makes clinical research in neonates relevant a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Samardzic J,Turner MA,Bax R,Allegaert K

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:Recent advances in molecular biology have enabled personalized cancer therapies with molecularly targeted agents (MTAs), which offer a promising future for cancer therapy. Dynamic modeling and simulation (M&S) is a powerful mathematical approach linking drug exposures to pharmacological responses, providin...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yamazaki S,Spilker ME,Vicini P

更新日期：2016-01-01 00:00:00