Abstract:
:The purpose of the present work was to study the change in morphine metabolic ratio in obese subjects before and after Roux-en-Y Gastric Bypass (RYGB) and to identify clinical and/or biological factors associated with this change. The pharmacokinetics (PK) of oral morphine (30mg), morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) was performed in patients before (n=25; mean BMI=43.2 (35.4-61.9)kg/m2), 7-15days (n=16) and 6 months after RYGB (n=19; mean BMI=32.3 (25.4-46.0)kg/m2). Morphine Cmax and AUC0-inf were significantly increased and morphine Tmax significantly shortened at 6 months after RYGB compared with preoperative data, indicating an important increase in the rate and extent of morphine absorption. The morphine metabolic ratio 0-inf M3G+M6G/Morphine, decreased significantly from the preoperative to 6 months postoperative period with an average of -26% (range -74%; +21%; p=0.004), but not in the immediate post-operative period. The change in morphine metabolic ratio was associated with a change in BMI, fat mass in kg, and triglyceride levels (rho=0.5, p≤0.04). The degree of change in several markers of low-grade inflammation, or the level of liver steatosis and fibrosis before surgery, was not associated with the change in morphine metabolic ratios. Our findings indicate that RYGB-induced weight loss significantly decreases morphine metabolic ratio, arguing for an effect of morbid obesity on glucuronidation. With glucuronide exposure at 6 months similar to preoperative values, a higher morphine AUC0-inf should encourage reducing morphine dosage in patients undergoing RYGB and chronically receiving immediate-release oral morphine.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Lloret-Linares C,Luo H,Rouquette A,Labat L,Poitou C,Tordjman J,Bouillot JL,Mouly S,Scherrmann JM,Bergmann JF,Declèves Xdoi
10.1016/j.phrs.2016.08.031subject
Has Abstractpub_date
2017-04-01 00:00:00pages
64-70eissn
1043-6618issn
1096-1186pii
S1043-6618(16)30855-6journal_volume
118pub_type
杂志文章abstract::Flibanserin has been reported to be an agonist at 5-HT1A-receptors and an antagonist at 5-HT2A receptors, with higher affinity for 5-HT1A receptors. Despite the fact that less receptor occupation is required by full agonists than by antagonists to exert their effects, flibanserin was shown to exert 5-HT2A antagonism a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0762
更新日期:2001-02-01 00:00:00
abstract::Photodynamic therapy (PDT) using 5-aminolevulinic acid (ALA)-induced protoporphyrin IX may play a role in the treatment of dysplastic Barrett's oesophagus. An ALA thermosetting gel Pluronic F-127) was developed and evaluated in an in vivo mouse model for potential use in PDT of Barrett's mucosa. In vitro studies of th...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2001.0934
更新日期:2002-02-01 00:00:00
abstract::Pre-eclampsia (PE) is a complication of pregnancy that is associated with mortality and morbidity in mothers and fetuses worldwide. Oxygen dysregulation in the placenta, abnormal remodeling of the spiral artery, defective placentation, oxidative stress at the fetal-maternal border, inflammation and angiogenic impairme...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104692
更新日期:2020-05-01 00:00:00
abstract::We studied here the effect of a wide range of adenosine concentration and time of preincubation, on the histamine release induced in the guinea pig mast cells by different stimulus. Adenosine (10(-5)-10(-3)m) potentiated the histamine release induced by antigen in the guinea pig heart (isolated and dispersed tissue) a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0589
更新日期:2000-03-01 00:00:00
abstract::T lymphocytes produced by the thymus are essential mediators of immunity. Accelerated thymic atrophy appears in the patients with administration of glucocorticoids (GCs) which are commonly-used drugs to treat autoimmune and infectious diseases, leading to dysregulation of immunity with manifestation of progressive dim...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.09.011
更新日期:2018-11-01 00:00:00
abstract::The potential for modulating gene expression by the use of antisense oligonucleotides has become increasingly interesting in recent years. Antisense oligonucleotides are complementary nucleic acid fragments that hybridize to target sequences within RNA to form a DNA-RNA duplex, resulting in the block of translation of...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.1997.0227
更新日期:1997-09-01 00:00:00
abstract::Given the high and increasing prevalence of obesity, the safe and effective treatment of obesity would be beneficial. Here, we examined whether oral hydroxysafflor yellow A (HSYA), an active compound from the dried florets of Carthamus tinctorius L., can reduce high-fat (HF) diet-induced obesity in C57BL/6 J mice. Our...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.05.012
更新日期:2018-08-01 00:00:00
abstract::The effect of different L-histidine concentrations on human mammary tumour cell (CG5) proliferation was studied to test the hypothesis of a role of histidine in modulating sex steroid-regulated cell proliferation. Cell growth was only possible in the 10(-5) M and 10(-2) M range, while its inhibition by medroxyprogeste...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0126
更新日期:1997-02-01 00:00:00
abstract::The modification in the composition of bile acids in hamster by the administration of high dose of ursodeoxycholic acid (UDCA) was investigated. Male Golden Syrian hamsters were divided into five groups: a control group, two groups that received 0.5 g of UDCA per 100 g of standard diet during 30 and 60 days and anothe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(90)90727-u
更新日期:1990-05-01 00:00:00
abstract::The effects of betel leaf extract (0.10, 0.40, 0.80 and 2.0 g kg-1 day-1 for 15 days) on the alterations in thyroid hormone concentrations. lipid peroxidation (LPO) and on the activities of superoxide dismutase (SOD) and catalase (CAT) were investigated in male Swiss mice. Administration of betel leaf extract exhibite...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1998.0398
更新日期:1998-12-01 00:00:00
abstract::Carbon-based nanomaterials have unique physicochemical properties relevant to the diagnosis and treatment of various diseases. There have been many reports indicating that carbon nanomaterials (CNMs) can interact and perturb biomolecules such as proteins and amyloid structures. This review is an attempt to reflect the...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.03.023
更新日期:2019-05-01 00:00:00
abstract::Perinatal encounter of a hormone and its developing target receptor sets the receptor-hormone-signal transduction complex for life (hormonal imprinting). In this critical period excess of the appropriate hormone or foreign molecules able to bind the receptor can cause faulty imprinting with life-long consequences. At ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(03)00217-2
更新日期:2003-11-01 00:00:00
abstract::The insulinotropic action of several new esters of succinic acid was assessed in isolated rat islets incubated in the presence of 7 mM D-glucose. An efficient secretory response was observed with the monobenzyl, monoisopropyl, monoallyl, monopropyl, monoethyl, monobutyl, dibutyl, dipropyl and diallyl esters of succini...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0038
更新日期:1996-04-01 00:00:00
abstract:BACKGROUND AND PURPOSE:The enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) hydrolyze endogenous cannabinoids (eCBs), N-arachidonoyl ethanolamine (AEA) and 2-arachidonoyl glycerol (2-AG), respectively. These enzymes also metabolize eCB analogs such as lipoamines and 2-acyl glycerols, most of...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.04.020
更新日期:2016-08-01 00:00:00
abstract::As Traditional Chinese Medicine (TCM) transcends its cultural boundaries and becomes widely used in many countries around the world, one of the major risks to the growing use of TCM internationally is the damage caused to its reputation and to community safety when TCM practitioners are not adequately trained. Ensurin...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105217
更新日期:2020-11-01 00:00:00
abstract::Diabetic erectile dysfunction (DED) hugely affected the patients' sexual life quality. However, there are no satisfactory therapeutic methods and intervention targets for this subtype of erectile dysfunction (ED). Inspired by the clinical practice of traditional Chinese medicine (TCM), we found that hirudin, the main ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105244
更新日期:2021-01-01 00:00:00
abstract::Severely obese patients undergoing bariatric surgery (BS) are at increased risk for venous thromboembolism (VTE). How standard low molecular weight heparin (LMWH) regimen should be adapted to provide both sufficient efficacy and safety in this setting is unclear. We aimed to compare the influence of four body size des...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.02.012
更新日期:2018-05-01 00:00:00
abstract::Since the regenerative capacity of the adult mammalian heart is limited, cardiac injury leads to the formation of scar tissue and thereby increases the risk of developing compensatory heart failure. Stem cell therapy is a promising therapeutic approach but is facing problems with engraftment and clinical feasibility. ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.07.020
更新日期:2018-01-01 00:00:00
abstract::The clear importance of mutated KRAS as a therapeutic target has driven the investigation of multiple approaches to inhibit oncogenic KRAS signaling at different molecular levels. However, no KRAS-targeted therapy has reached the clinic to date, which underlies the intrinsic difficulty in developing effective, direct ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.01.006
更新日期:2017-03-01 00:00:00
abstract::Osteoporosis caused by aging and menopause had become an emerging threat to human health. The reduction of osteoblast differentiation has been considered to be an essential cause of osteoporosis. Osteoblast differentiation could be regulated by LncRNAs, and increasing evidences have proved that LncRNAs may be adopted ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105230
更新日期:2021-01-01 00:00:00
abstract::In 1996, Dr. Costa was invited by Prof. Boris Astrachan, Chairman of the Department of Psychiatry at the University of Illinois at Chicago, to direct the research of the "Psychiatric Institute, Department of Psychiatry, School of Medicine, at the University of Illinois at Chicago." He was asked to develop a seminal re...
journal_title:Pharmacological research
pub_type: 历史文章,杂志文章,评审
doi:10.1016/j.phrs.2011.05.026
更新日期:2011-10-01 00:00:00
abstract::Alzheimer's is the neurodegenerative disease affecting the largest number of patients in the world. In spite of the intense research of the last decades, progress about its knowledge and therapy was limited. In particular, various cytotoxic processes remained debated, while the few drugs approved for therapy were of o...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.104316
更新日期:2019-08-01 00:00:00
abstract::Drug-drug interactions (DDI) potentially occurring between medications used in the course of COVID-19 infection and medications prescribed for the management of underlying comorbidities may cause adverse drug reactions (ADRs) contributing to worsening of the clinical outcome in affected patients. First, we conducted a...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析
doi:10.1016/j.phrs.2020.105250
更新日期:2020-11-01 00:00:00
abstract::In the present study, we have investigated the effects of centrally administered ginsenoside Rc and Rg1 on the modulation of the NMDA receptor and GABA(A)receptor binding in rat brain. The NMDA receptor binding was analysed by quantitative autoradiography using [(3)H]MK-801 binding, and the GABA(A)receptor bindings we...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2001.0809
更新日期:2001-05-01 00:00:00
abstract:AIM:Acute myocardial infarction and subsequent post-infarction heart failure are among the leading causes of mortality worldwide. The endocannabinoid system has emerged as an important modulator of cardiovascular disease, however the role of endocannabinoid metabolic enzymes in heart failure is still elusive. Herein, w...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.104578
更新日期:2020-01-01 00:00:00
abstract::Tablets containing the inclusion complex of ursodeoxycholic acid (UDCA) with 2-hydroxypropyl-beta-cyclodextrin were prepared by direct compression. Plasma concentrations of UDCA were determined in six healthy volunteers after oral administration of tablets containing the inclusion complex or UDCA alone (Ursacol). Foll...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(95)80019-0
更新日期:1995-03-01 00:00:00
abstract::Biosimilars started receiving the marketing authorization by European Medicine Agency since 2006. The development of biosimilars follows a well-defined step-wise approach, the so-called comparability exercise, which aims to compare non-clinical (mainly quality features and biological activity) and clinical (efficacy a...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.11.002
更新日期:2017-12-01 00:00:00
abstract::The polyphenol resveratrol is considered to exert many beneficial actions, such as antioxidant, anti-inflammatory, insulin-sensitizer and anticancer effects. Its benefits in patients with type 2 diabetes mellitus (T2DM) are controversial. Our aims were to determine whether resveratrol supplementation at two different ...
journal_title:Pharmacological research
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.phrs.2016.08.010
更新日期:2016-09-01 00:00:00
abstract::We aimed to examine the effects of KTO-7924 (beta3-adrenoceptor agonist) on lipid metabolism and mRNA expressions in retroperitoneal white adipose tissue (RP WAT) in obese (fa/fa) Zucker rats using DNA microarray. Oral KTO-7924 for 28 days significantly decreased RP WAT weight, plasma triglyceride, free fatty acid, an...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.05.014
更新日期:2005-11-01 00:00:00
abstract::TNF-related apoptosis-inducing ligand (TRAIL) selectively induces the apoptosis pathway in tumor cells leading to tumor cell death. Because TRAIL induction can kill tumor cells, cancer researchers have developed many agents to target TRAIL and some of these agents have entered clinical trials in oncology. Unfortunatel...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104716
更新日期:2020-05-01 00:00:00