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：:The review emphasizes the role of NGF, the most representative member of the neurotrophins family, in cardiac physiopathology with a particular focus on healing and sprouting processes occurring after tissue damage. Cardiac and circulating NGF levels dramatically increase following myocardial injury (MI). A very early...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2010.12.017
更新日期：2011-04-01 00:00:00
abstract：:Erectile function is a widely accepted indicator of systemic endothelial activity since from a clinical standpoint erectile dysfunction (ED) often precedes cardiovascular events. Recently it has been described a potential role for β3 adrenoceptor in cardiovascular diseases emphasizing a possible development of new dru...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.07.025
更新日期：2017-10-01 00:00:00
abstract：:Novel therapeutic strategies are needed to address and to solve the emerging problem of hypoxia-induced resistance to anticancer drugs. N-(4-Hydroxyphenyl)retinamide (4-HPR) exhibits potent anticancer and chemopreventive activities, but its inefficiency under hypoxia, through undetermined mechanisms, may contribute to...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2010.07.002
更新日期：2010-11-01 00:00:00
abstract：:Skeletal muscle fitness is vital for human health and disease and is determined by the capacity for burning fuel, mitochondrial ATP production, and contraction. High quality mitochondria in skeletal muscle are essential for maintaining energy homeostasis in response to a myriad of physiologic or pathophysiological str...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.12.020
更新日期：2019-03-01 00:00:00
abstract：:Breast cancer, the most prevalent cancer in women, remains the second in the list of cancer mortality, the majority of these fatalities resulted from estrogen receptor alpha (ERα) positive disease. ERα is well known for its function on breast cancer initiation and development and has become the most successful biomark...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104294
更新日期：2019-08-01 00:00:00
abstract：UNLABELLED:The purpose of this study was an attempt to extrapolate favorable observations on the effects of magnesium on platelets and haemostasis from animal models to humans. Intravenous magnesium in the treatment of acute myocardial infarction has been tested in several large clinical trials and remains controversia...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0212
更新日期：1997-07-01 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：: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：:Apoptosis of tissues may contribute to ischaemia-reperfusion injury. The aim of the present study was to determine whether administration of a colloid solution would prevent apoptosis after liver ischaemia-reperfusion. New Zealand rabbits, weighing 1.5-2 kg, were randomized to receive either 4% SG (20 ml kg (-1)h(-1) ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2002.0984
更新日期：2002-06-01 00:00:00
abstract：:The Notch pathway represents a highly conserved signaling network with essential roles in regulation of key cellular processes and functions, many of which are critical for development. Accumulating evidence indicates that it is also essential for fibrosis and thus the pathogenesis of chronic fibroproliferative diseas...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.04.010
更新日期：2016-06-01 00:00:00
abstract：:It has demonstrated that carteolol can increase the endothelium-dependent vasodilation induced by alpha-2 adrenergic agonist. In order to evaluate the effect of carteolol, and to clarify the mechanism, we examined the effects of 10 microM carteolol on the vasodilation induced by increasing doses (10(-7)-10(-4) M) of c...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(95)80038-7
更新日期：1995-05-01 00:00:00
abstract：:Green tea and its major polyphenols constituents, tea catechins, have been shown to have many health benefits including cancer prevention. Tea catechins and tea catechin metabolites/catabolites are bioavailable in the systemic circulation after oral intake of green tea or green tea catechins. The metabolites/catabolit...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2011.05.007
更新日期：2011-08-01 00:00:00
abstract：:One of the most serious side effects of the immunosuppressive agent, cyclosporin A (CsA), is drug-related hypertension. As it is generally accepted, the sympathetic nervous system may play an important role in the development or maintenance of this abnormal pathophysiological situation. This study is aimed at assessin...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1999.0572
更新日期：2000-02-01 00:00:00
abstract：:The endocannabinoid signalling system includes: (1) at least two G-protein-coupled receptors, known as the cannabinoid CB(1) and CB(2) receptors and discovered following studies on the mechanism of action of Delta(9)-tetrahydrocannabinol, the major psychoactive principle of the hemp plant Cannabis sativa; (2) the endo...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2009.02.010
更新日期：2009-08-01 00:00:00
abstract：:The hepatoprotective effects of acetylbergenin were examined against D -galactosamine (GalN)-induced liver damage in rats, compared with that of bergenin reported previously. Acetylbergenin was synthesized from acetylation of bergenin, isolated from Mallotus japonicus, to increase lipophilic and physiological activiti...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2000.0730
更新日期：2000-11-01 00:00:00
abstract：:Extensive studies have reported the significant roles of numerous cellular features and processes in properly maintaining neuronal morphology and function throughout the lifespan of an animal. Any alterations in their homeostasis appear to be strongly associated with neuronal aging and the pathogenesis of various neur...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.003
更新日期：2017-05-01 00:00:00
abstract：:Folic acid-conjugated albumin nanospheres (FA-AN) have been developed to provide an actively targetable drug delivery system for improved drug targeting of cancer cells with reduced side effects. The nanospheres were prepared by conjugating folic acid onto the surface of albumin nanospheres using 1-ethyl-3-(3-dimethyl...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2010.10.012
更新日期：2011-01-01 00:00:00
abstract：:Short-chain fatty acids (SCFAs), mainly including acetate, propionate, and butyrate, are metabolites produced during the bacterial fermentation of dietary fiber in the intestinal tract. They are believed to be essential factors affecting host health. Most in vitro and ex vivo studies have shown that SCFAs affect the r...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2021.105420
更新日期：2021-01-09 00:00:00
abstract：:Nerve growth factor (NGF) is the prototype of the neurotrophin family and promotes the survival of specific populations of neurons, stimulates their morphological differentiation and regulates neuronal gene expression. Since its discovery, NGF attracted clinicians for its potential application in the treatment of neur...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1016/j.phrs.2007.03.007
更新日期：2007-07-01 00:00:00
abstract：:Prader-Willi syndrome (PWS), the leading genetic cause of obesity, is characterized by a striking hyperphagic behavior that can lead to obesity, type-2 diabetes, cardiovascular disease and death. The molecular mechanism underlying impaired satiety in PWS is unknown. Oleoylethanolamide (OEA) is a lipid mediator involve...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.12.024
更新日期：2017-03-01 00:00:00
abstract：:Lipid peroxidation increased both in the liver homogenates and in the hepatic mitochondrial fraction of bile duct ligated (BDL)-rats. Although mitochondrial superoxide dismutase (SOD) activity did not change in the liver, glutathione (GSH) levels and glutathione peroxidase (GSH-Px) activity decreased in hepatic mitoch...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0225
更新日期：1997-09-01 00:00:00
abstract：:The apelinergic system is an important player in the regulation of both vascular tone and cardiovascular function, making this physiological system an attractive target for drug development for hypertension, heart failure and ischemic heart disease. Indeed, apelin exerts a positive inotropic effect in humans whilst re...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.02.032
更新日期：2018-05-01 00:00:00
abstract：:The mitochondrial citrate carrier (CIC) is a nuclear-encoded protein located in the inner mitochondrial membrane. By mediating efflux of citrate from the mitochondria to the cytosol, CIC links mitochondrial central carbon metabolism and cytosolic lipogenesis together. Abnormal activity or expression of CIC was found i...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.105132
更新日期：2020-11-01 00:00:00
abstract：:Myocardial infarction (MI) is a major cause of morbidity and mortality in western countries and the formation of intracoronary thrombi is recognized as a critical determinant of this ischaemic event. Since streptokinase and urokinase cause in vitro lysis of clots, it was though that these drugs were also effective in ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/1043-6618(89)90233-8
更新日期：1989-03-01 00:00:00
abstract：:It is generally accepted that divalent cations are involved in the nociceptive pathway. The effect of systemic co-administration of magnesium sulfate and calcium channel blockers (nifedipine, verapamil) on the analgesic effect of opioid (mixed mu/kappa: butorphanol) and non-opioid drugs (paracetamol) was investigated....
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0811
更新日期：2001-06-01 00:00:00
abstract：:Dyslipidemia and hyperglycemia are associated with an increased risk of ischemic cardiovascular disease. Positive effects of a nutraceutical combination comprising red yeast rice, berberine, policosanol, astaxanthin, coenzyme Q10 and folic acid (NComb) on plasma lipid and glucose levels have been reported in some but ...
journal_title：Pharmacological research
pub_type： 杂志文章,meta分析,评审
doi：10.1016/j.phrs.2016.04.021
更新日期：2016-08-01 00:00:00
abstract：:Using cultured human keratinocytes, the present study investigates the role of nitric oxide (NO) in the mediation of the antiproliferative effects of ultraviolet light A (UVA). UVA treatment of cells (3-21 J cm (-2)) caused a time- and dose-dependent increase in nitrite formation in a micromolar range. This effect was...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0939
更新日期：2002-03-01 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：:In hypothermic rats with acute hypertension induced by intravenous injection of adrenalin, regional changes in blood-brain barrier permeability to macromolecules were investigated using Evans blue as indication. Evans blue albumin extravasation was determined as a macroscopic finding and a quantitative estimation with...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：
更新日期：1992-07-01 00:00:00
abstract：:Our goal was to establish the requirement of β3 adrenoceptor (β3Adr) for green tea (GT) effects on the energy metabolism of obese mice. This study was carried out in wild-type (WT) and β3Adr knockout (KO) male mice fed with a standard diet or a high-fat diet (HFD/16 weeks) treated or not with GT (0.5 g/kg of body weig...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.104956
更新日期：2020-09-01 00:00:00
