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See detailPharmacodynamie
Lekeux, Pierre ULg

in Delannoy, I. (Ed.) Le Grand Livre des AINS (1991)

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See detailPharmacodynamie des aminoglycosides et optimisation de leur pharmacocinétque en néonatologie
Battisti, Oreste ULg; Langhendries, J. P.; Bertrand, J. M. et al

Conference (1997)

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See detailPharmacogenetics of infliximab in Crohn's disease
Dideberg, Vinciane ULg; Louis, Edouard ULg; Bours, Vincent ULg

in Acta Endoscopica (2007), 37(4), 521-530

Pharmacogenetic studies will certainly contribute to a better management of medication in inflammatory bowel diseases. Infliximab is the most efficient drug in refractory and fistulising Crohn's disease ... [more ▼]

Pharmacogenetic studies will certainly contribute to a better management of medication in inflammatory bowel diseases. Infliximab is the most efficient drug in refractory and fistulising Crohn's disease. However, about one third of the patients do not respond to this treatment. Several studies have been performed to identify predictive factors of the response to infliximab in CD. We attempt to summarize the current knowledge on the use of infliximab in CD and focus on the result of these studies and more particularly on pharmacogenetic aspects. [less ▲]

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See detailPharmacognosie - Volume 2
Angenot, Luc ULg; Tits, Monique ULg; Frederich, Michel ULg

Learning material (2010)

Le volume 2 est consacré aux grands classiques de la pharmacognosie dont ont été isolés de très nombreux principes actifs (souvent des alcaloïdes) qui ont marqué l'histoire de la pharmacie et de la ... [more ▼]

Le volume 2 est consacré aux grands classiques de la pharmacognosie dont ont été isolés de très nombreux principes actifs (souvent des alcaloïdes) qui ont marqué l'histoire de la pharmacie et de la pharmacologie.Les chapitres suivants seront abordés: analgésiques (pavot,opium, colchique...); Solanacées à activité parasympatholytiques ( belladone, stramoine, jusquiames...); dérivés de l'ergot de seigle; médicaments des troubles cérébraux de la sénescence ( ginkgo, amaryllidacées à galanthamine...); drogues alcaloïdiques psychoactives ( coca, éphédra, khat, psilocybes, peyotl, harmel, yagé, iboga...); hallucinogènes non alcaloïdiques ( cannabis, sauge des devins..); poisons agissant sur la neurotransmission :cholinergiques ( jaborandi, éséré...), paralysants neuro-musculaires (curares) et antagonistes de la glycine ( noix-vomique); antiparasitaires (malaria et amibiase): quinquinas, armoises, ipécas; anticancéreux : lignanes ( Podophyllum), diterpènes des ifs (Taxus sp), alcaloïdes indoliques ( Catharanthus roseus, Camptotheca ...), divers ( origine marine, épices...); plantes toxiques de l'environnement ( toxicité par contact ou par ingestion) [less ▲]

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See detailPharmacognosie Volume 1
Angenot, Luc ULg; Tits, Monique ULg

Learning material (2009)

Le volume 1 est principalement consacré à la phytochimie. Le cours est subdivisé suivant les différentes classes chimiques des métabolites primaires et secondaires impliqués soit dans l'activité des ... [more ▼]

Le volume 1 est principalement consacré à la phytochimie. Le cours est subdivisé suivant les différentes classes chimiques des métabolites primaires et secondaires impliqués soit dans l'activité des plantes soit dans leur toxicité ou encore présentant des applications en pharmacotechnie ou dans l'alimentation. La connaissance des structures ( basée sur leur origine biosynthétique) est très importante pour évaluer leur solubilité, leur stabilité et ainsi mieux comprendre les processus d'extraction et les méthodes spécifiques de contrôle ( plantes entières ou pulvérisées, , extraits, huiles essentielles, huiles grasses, exsudats...). dans de nombreux cas, une relation structure-activité pharmacologique ou physiologique est établie. [less ▲]

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See detailPharmacognosie Volume 3
Angenot, Luc ULg; Tits, Monique ULg; Frederich, Michel ULg

Learning material (2010)

Le volume 3 est principalement consacré à la phytothérapie (intérêt et limites) avec des notions concernant aussi bien la médecine traditionnelle que les développements les plus récents ( y compris pour ... [more ▼]

Le volume 3 est principalement consacré à la phytothérapie (intérêt et limites) avec des notions concernant aussi bien la médecine traditionnelle que les développements les plus récents ( y compris pour certains s'appuyant sur des études cliniques) en matière de phytomédicaments. La classification se fait suivant les activités pharmacologiques de ces plantes. Au terme de ce cours, les étudiants doivent pouvoir faire la distinction entre les différentes formes pharmaceutiques à base de produits d'origine naturelle ( poudres, extraits sec et autres), les concentrations en principes actifs et traceurs y étant bien différentes. Les différences entre les médicaments enregistrés et les compléments alimentaires sont également bien mises en évidence car les exigences relatives au contrôle de qualité et à la stabilité des produits finis sont très différentes. A ce sujet l'annexe du volume 3 est consacrée au contrôle de qualité des plantes en insistant sur les méthodes et monographies de la pharmacopée européenne qui joue un rôle essentiel dans ce domaine. [less ▲]

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See detailPharmacognosie volume I
Frederich, Michel ULg; Tits, Monique ULg; Angenot, Luc ULg

Learning material (2010)

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See detailPharmacognosie volume II
Frederich, Michel ULg; Tits, Monique ULg; Angenot, Luc ULg

Learning material (2011)

Detailed reference viewed: 26 (2 ULg)
See detailPharmacognosie volume III
Frederich, Michel ULg; Tits, Monique ULg; Angenot, Luc ULg

Learning material (2011)

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See detailPharmacokinetic and pharmacodynamic evaluation of sitagliptin plus metformin.
Scheen, André ULg

in Expert Opinion on Drug Metabolism & Toxicology (2010), 6(10), 1265-76

IMPORTANCE OF THE FIELD: Type 2 diabetes is an increasingly prevalent disease resulting from various complex combinations of defects in insulin secretion and insulin action. Adequate blood glucose control ... [more ▼]

IMPORTANCE OF THE FIELD: Type 2 diabetes is an increasingly prevalent disease resulting from various complex combinations of defects in insulin secretion and insulin action. Adequate blood glucose control is necessary to minimize complications. DPP IV inhibitors (sitagliptin, vildagliptin, saxagliptin) offer new options for combined pharmacological therapy. AREAS COVERED IN THIS REVIEW: An extensive literature search was performed to analyze the potential pharmacokinetic (PK) and pharmacodynamic (PD) interactions between metformin (first-line drug for the management of type 2 diabetes) and sitagliptin (first commercialized DPP IV inhibitor). Metformin and sitagliptin may be administered together, either separately or in fixed-dose combination. WHAT THE READER WILL GAIN: Updated information about PK/PD data on metformin alone, sitagliptin alone and sitagliptin plus metformin. Metformin and sitagliptin are not prone to PK drug-drug interactions. Their co-administration, either separately or in a fixed-dose combination, improves blood glucose control more potently than either compound separately, without hypoglycemia and without increasing metformin-related gastrointestinal side effects. TAKE HOME MESSAGE: The combination sitagliptin plus metformin may be used as a first- or second-line therapy in the management of type 2 diabetes. [less ▲]

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See detailPharmacokinetic and pharmacodynamic profile of empagliflozin, a sodium glucose co-transporter 2 inhibitor.
Scheen, André ULg

in Clinical pharmacokinetics (2014), 53(3), 213-25

Empagliflozin is an orally active, potent and selective inhibitor of sodium glucose co-transporter 2 (SGLT2), currently in clinical development to improve glycaemic control in adults with type 2 diabetes ... [more ▼]

Empagliflozin is an orally active, potent and selective inhibitor of sodium glucose co-transporter 2 (SGLT2), currently in clinical development to improve glycaemic control in adults with type 2 diabetes mellitus (T2DM). SGLT2 inhibitors, including empagliflozin, are the first pharmacological class of antidiabetes agents to target the kidney in order to remove excess glucose from the body and, thus, offer new options for T2DM management. SGLT2 inhibitors exert their effects independently of insulin. Following single and multiple oral doses (0.5-800 mg), empagliflozin was rapidly absorbed and reached peak plasma concentrations after approximately 1.33-3.0 h, before showing a biphasic decline. The mean terminal half-life ranged from 5.6 to 13.1 h in single rising-dose studies, and from 10.3 to 18.8 h in multiple-dose studies. Following multiple oral doses, increases in exposure were dose-proportional and trough concentrations remained constant after day 6, indicating a steady state had been reached. Oral clearance at steady state was similar to corresponding single-dose values, suggesting linear pharmacokinetics with respect to time. No clinically relevant alterations in pharmacokinetics were observed in mild to severe hepatic impairment, or in mild to severe renal impairment and end-stage renal disease. Clinical studies did not reveal any relevant drug-drug interactions with several other drugs commonly prescribed to patients with T2DM, including warfarin. Urinary glucose excretion (UGE) rates were higher with empagliflozin versus placebo and increased with dose, but no relevant impact on 24-h urine volume was observed. Increased UGE resulted in proportional reductions in fasting plasma glucose and mean daily glucose concentrations. [less ▲]

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See detailPharmacokinetic and toxicological considerations for the treatment of diabetes in patients with liver disease.
Scheen, André ULg

in Expert opinion on drug metabolism & toxicology (2014)

Introduction: Patients with type 2 diabetes have an increased risk of chronic liver disease (CLD) such as non-alcoholic fatty liver disease and steatohepatitis and about one-third of cirrhotic patients ... [more ▼]

Introduction: Patients with type 2 diabetes have an increased risk of chronic liver disease (CLD) such as non-alcoholic fatty liver disease and steatohepatitis and about one-third of cirrhotic patients have diabetes. However, the use of several antidiabetic agents may be a cause for concern in the case of hepatic impairment (HI). Areas covered: An extensive literature search was performed to analyze the influence of HI on the pharmacokinetics (PK) of glucose-lowering agents and the potential consequences for clinical practice as far as the efficacy/safety balance of their use in diabetic patients with CLD is concerned. Expert opinion: Almost no PK studies have been published regarding metformin, sulfonylureas, thiazolidinediones and alpha-glucosidase inhibitors in patients with HI. Only mild changes in PK of glinides, dipeptidyl peptidase-4 inhibitors and sodium glucose cotransporters type 2 inhibitors were observed in dedicated PK studies in patients with various degrees of HI, presumably without major clinical relevance although large clinical experience is lacking. Glucagon-like peptide-1 receptor agonists have a renal excretion rather than liver metabolism. Rare anecdotal case reports of hepatotoxicity have been described with various glucose-lowering agents contrasting with numerous reassuring data. Nevertheless, caution should be recommended, especially in patients with advanced cirrhosis, including with the use of metformin. [less ▲]

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See detailPharmacokinetic considerations for the treatment of diabetes in patients with chronic kidney disease.
SCHEEN, André ULg

in Expert Opinion on Drug Metabolism & Toxicology (2013)

Introduction: People with chronic kidney disease (CKD) of stages 3 - 5 (creatinine clearance < 60 ml/min) represent approximately 25% of patients with type 2 diabetes mellitus (T2DM), but the problem is ... [more ▼]

Introduction: People with chronic kidney disease (CKD) of stages 3 - 5 (creatinine clearance < 60 ml/min) represent approximately 25% of patients with type 2 diabetes mellitus (T2DM), but the problem is underrecognized or neglected in clinical practice. However, most oral antidiabetic agents have limitations in case of renal impairment (RI), either because they require a dose adjustment or because they are contraindicated for safety reasons. Areas covered: The author performed an extensive literature search to analyze the influence of RI on the pharmacokinetics (PK) of glucose-lowering agents and the potential consequences for clinical practice. Expert opinion: As a result of PK interferences and for safety reasons, the daily dose should be reduced according to glomerular filtration rate (GFR) or even the drug is contraindicated in presence of severe CKD. This is the case for metformin (risk of lactic acidosis) and for many sulfonylureas (risk of hypoglycemia). At present, however, the exact GFR cutoff for metformin use is controversial. New antidiabetic agents are better tolerated in case of CKD, although clinical experience remains quite limited for most of them. The dose of DPP-4 inhibitors should be reduced (except for linagliptin), whereas both the efficacy and safety of SGLT2 inhibitors are questionable in presence of CKD. [less ▲]

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See detailPharmacokinetic evaluation of a long-acting sulfamethazine bolus for lambs
Evrard, Brigitte ULg; Delahaut, Philippe; Delattre, Luc ULg

in Proceedings of 21th International Symposium on controlled release of Bioactive Materials (1994)

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See detailPharmacokinetic evaluation of atorvastatin and sitagliptin in combination for the treatment of type 2 diabetes.
SCHEEN, André ULg

in Expert Opinion on Drug Metabolism & Toxicology (2012), 8(6), 745-58

INTRODUCTION: Patients with type 2 diabetes (T2DM) are exposed to a high risk of cardiovascular disease (CVD) requiring a global therapeutic approach. Statin therapy has proven its efficacy in reducing ... [more ▼]

INTRODUCTION: Patients with type 2 diabetes (T2DM) are exposed to a high risk of cardiovascular disease (CVD) requiring a global therapeutic approach. Statin therapy has proven its efficacy in reducing CVD events in T2DM patients. Dipeptidylpeptidase-4 inhibitors (gliptins), which are increasingly used to target hyperglycemia, also offer promising preliminary results regarding a possible reduction in CVD events. As most patients with T2DM may be treated with both a statin and a gliptin, dual pharmacological therapy, possibly as a fixed-dose combination (FDC), deserves further consideration. AREAS COVERED: The reader is provided with an update of information on the pharmacokinetics (PK) and pharmacodynamics (PD) of atorvastatin and sitagliptin . The article provides an analysis of the potential PK/PD interactions between the two compounds and puts into perspective the potential cardiovascular protection that such a dual therapy may offer in patients with T2DM. EXPERT OPINION: Atorvastatin and sitagliptin are not prone to PK drug-drug interactions. Their coadministration, either separately or in an FDC, improves both blood glucose levels and cholesterol concentrations, without clinically relevant adverse events. The atorvastatin plus sitagliptin combination may be used to reduce LDL cholesterol and hyperglycemia in patients with T2DM, with the aim to improve CVD prognosis and adherence to therapy. [less ▲]

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See detailPharmacokinetic parameters estimation using adaptive Bayesian P-splines models
Jullion, Astrid; Lambert, Philippe ULg; Beck, Benoit et al

in Pharmaceutical Statistics (2009), 8

In preclinical and clinical experiments, pharmacokinetic (PK) studies are designed to analyse the evolution of drug concentration in plasma over time i.e. the PK profile. Some PK parameters are estimated ... [more ▼]

In preclinical and clinical experiments, pharmacokinetic (PK) studies are designed to analyse the evolution of drug concentration in plasma over time i.e. the PK profile. Some PK parameters are estimated in order to summarize the complete drug’s kinetic profile: area under the curve (AUC), maximal concentration (Cmax), time at which the maximal concentration occurs (tmax) and half-life time (t1/2). Several methods have been proposed to estimate these PK parameters. A first method relies on interpolating between observed concentrations. The interpolation method is often chosen linear. This method is simple and fast. Another method relies on compartmental modelling. In this case, nonlinear methods are used to estimate parameters of a chosen compartmental model. This method provides generally good results. However, if the data are sparse and noisy, two difficulties can arise with this method. The first one is related to the choice of the suitable compartmental model given the small number of data available in preclinical experiment for instance. Second, nonlinear methods can fail to converge. Much work has been done recently to circumvent these problems (J. Pharmacokinet. Pharmacodyn. 2007; 34:229–249, Stat. Comput., to appear, Biometrical J., to appear, ESAIM P&S 2004; 8:115–131). In this paper, we propose a Bayesian nonparametric model based on P-splines. This method provides good PK parameters estimation, whatever be the number of available observations and the level of noise in the data. Simulations show that the proposed method provides better PK parameters estimations than the interpolation method, both in terms of bias and precision. The Bayesian nonparametric method provides also better AUC and t1/2 estimations than a correctly specified compartmental model, whereas this last method performs better in tmax and Cmax estimations. We extend the basic model to a hierarchical one that treats the case where we have concentrations from different subjects. We are then able to get individual PK parameter estimations. Finally, with Bayesian methods, we can get easily some uncertainty measures by obtaining credibility sets for each PK parameter. [less ▲]

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See detailPharmacokinetic study of a new synthetic MMP inhibitor (Ro 28-2653) after IV and oral administration of cyclodextrin solutions
Piette, Marie ULg; Evrard, Brigitte ULg; Frankenne, Francis et al

in European Journal of Pharmaceutical Sciences (2006), 28(3), 189-195

Ro 28-2653 (5-biphenyl-4-yl-5-[4-(4-nitro-phenyl)-piperazin-1-yl]-pyrimidine-2,4,6-trione) is a new synthetic inhibitor of matrix metalloproteinases (MMPs) with a high selectivity towards MMP2, MMP9 and ... [more ▼]

Ro 28-2653 (5-biphenyl-4-yl-5-[4-(4-nitro-phenyl)-piperazin-1-yl]-pyrimidine-2,4,6-trione) is a new synthetic inhibitor of matrix metalloproteinases (MMPs) with a high selectivity towards MMP2, MMP9 and membrane type 1-MMP. It has been shown that cyclodextrins (CDs) are able to form inclusion complexes with Ro 28-2653 and to increase its aqueous solubility. The aim of this study is to demonstrate that an increase in Ro 28-2653 solubility, via ternary complex formation, can lead to an increase in the oral bioavailability of this drug. This study shows that a synergistic effect exists between hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and L-lysine. The use of this multicomponent system enabled the preparation of oral and intravenous solutions of Ro 28-2653. In vivo evaluation of the oral solution of the inclusion complex of Ro 28-2653 in comparison with a suspension of the same uncomplexed drug showed a significant (p < 0.05) increase in absolute bioavailability. The area under curve (AUC) and the peak serum concentration (C-max) were approximately 10 times higher than those obtained with the suspension, while the time (T-max) to reach C-max was reduced. Moreover, in vivo administration of Ro 28-2653 solutions highlighted some information about the pharmacokinetic behavior of Ro 28-2653: a long biologic half-life (about 15.5 h) and a small overall volume of distribution (81). (c) 2006 Elsevier B.V. All rights reserved. [less ▲]

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See detailPharmacokinetic study of a new testosteron in-Adhesive Matrix patch applied every two days to hypogonadal men
Raynaud, J. P.; Aumonier, C.; Gualano, V. et al

in The Endocrine society ENDO 2005 - Abstract book (2005)

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See detailPharmacokinetic study of a new testosterone-in-adhesive matrix patch applied every 2 days to hypogonadal men.
Raynaud, J. P.; Aumonier, C.; Gualano, V. et al

in Journal of Steroid Biochemistry & Molecular Biology (2008), 109(1-2), 177-184

The present study assessed pharmacokinetic testosterone time profile and dose proportionality after application of a new matrix testosterone patch (30, 45, and 60 cm2 containing 0.5mg of testosterone per ... [more ▼]

The present study assessed pharmacokinetic testosterone time profile and dose proportionality after application of a new matrix testosterone patch (30, 45, and 60 cm2 containing 0.5mg of testosterone per cm2). This open study was a single dose, three-period, crossover trial with a randomised treatment sequence in 24 hypogonadal men, consisting in a single 48-h application of two patches of 2x 30 cm2, 2x 45 cm2, 2x 60 cm2, separated by a 5-day wash-out. Testosterone concentrations were determined during patch application and after patch removal. Dose proportionality was assessed on baseline corrected, dose normalised parameters for C av,corr/D, C max,corr/D and AUC(0-48),corr/D. Testosterone concentrations rose during the first 9h following patch application, remained relatively sustained until 48 h and then decreased abruptly after patch removal, with a half-life of 1.3h. Testosterone levels were maintained above 3 ng/mL for 42-45 h with all patches. C av were 3.39, 4.03 and 4.58 ng/mL and Cmax were 4.33, 5.29 and 6.18 ng/mL according to the doses. AUC 0-48), C av and Cmax were dose dependent with mean ratios within the acceptance range (0.70-1.43). In conclusion, dose linearity was demonstrated between the different strengths of testosterone patches. Application resulted in dose proportional increases in serum T levels in hypogonadal men into the low to mid-normal range within the first hours and achieved steady state for 48 h. During this short term study with three consecutive patch applications, this patch was shown to be efficient, convenient and safe with excellent adhesiveness and skin tolerability, and with no cross-contamination to partner or to environment. [less ▲]

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