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Peer Reviewed
See detailPharmacological treatment of obesity: present status.
Scheen, André ULg; Lefebvre, Pierre ULg

in International Journal of Obesity & Related Metabolic Disorders (1999), 23 Suppl 1

OBJECTIVE: Obesity poses a serious health hazard and its treatment is often disappointing. This review describes the present status of pharmacological treatment of obesity in man. DESIGN: Obesity ... [more ▼]

OBJECTIVE: Obesity poses a serious health hazard and its treatment is often disappointing. This review describes the present status of pharmacological treatment of obesity in man. DESIGN: Obesity treatment may include drugs that reduce food intake, drugs that increase energy expenditure and drugs that affect nutrient partitioning or metabolism. The mode of action, efficacy and safety of each approach will be briefly discussed. RESULTS: All of the pharmacological possibilities have potential activities, but also serious limitations. While current anti-obesity pharmacotherapy essentially uses centrally-acting anorectic drugs, severe side-effects (more particularly pulmonary hypertension and valvular heart disease) have been reported, leading to the withdrawal of licensed fenfluramine and d-fenfluramine. New approaches have been recently proposed, such as sibutramine, an amine reuptake inhibitor which decreases food intake, and orlistat, an intestinal lipase inhibitor which decreases fat absorption. Obesity is a chronic disease and should be treated as such with reasonable expectations. Large-scale one-year placebo-controlled studies demonstrated that d-fenfluramine, sibutramine and orlistat significantly increased body weight loss by an average of 2-4 kg when compared to placebo and, more interestingly, multiplied by 2-3 the number of patients who succeeded in obtaining and maintaining a reduction of more than 10% of initial body weight. Interestingly, some of these compounds may also exert favourable effects on other vascular risk factors, independently of weight loss. CONCLUSIONS: Even if all anti-obesity pharmacological approaches can be helpful, they also have important limitations so that other strategies including either combined therapies or new drugs (peptides) are currently under investigation. [less ▲]

Detailed reference viewed: 18 (1 ULg)
Peer Reviewed
See detailPharmacological treatment of the obese diabetic patient.
Scheen, André ULg; Lefebvre, Pierre ULg

in Diabète & Métabolisme (1993), 19(6), 547-59

Obesity is a well-known risk factor for non-insulin-dependent (or Type 2) diabetes mellitus. Consequently, reduction of weight excess comes to the front line in the prevention and management of NIDDM. It ... [more ▼]

Obesity is a well-known risk factor for non-insulin-dependent (or Type 2) diabetes mellitus. Consequently, reduction of weight excess comes to the front line in the prevention and management of NIDDM. It is only when diet and physical exercise fail that drug treatment should be considered. Pharmacological treatment of obesity should favour drugs which not only promote weight loss, by reducing caloric intake and/or increasing thermogenesis and energy expenditure, but also, and especially, improve insulin sensitivity. Serotoninergic anorectic compounds (dexfenfluramine, fluoxetine) appear to possess, to some extent, all these properties. Metformin significantly reduces insulin resistance and improves glycaemic control without inducing weight gain, and even favouring some weight loss. This biguanide is now considered as the first line drug for the obese diabetic patient. Alpha-glucosidase inhibitors may help to reduce post-prandial glucose excursions but do not promote weight loss per se. Sulfonylureas can be prescribed to an obese patient when hyperglycaemia persists despite diet and the above-mentioned oral agents, but their use should be associated with reinforcement of dietary advices in order to prevent further weight increase; it is also the case for insulin therapy. Finally, drugs specifically stimulating thermogenesis and energy expenditure, new agents sensitizing tissues to the action of insulin and various compounds interfering with lipid metabolism are currently under extensive investigation with promising preliminary results in the obese diabetic patient. In conclusion, obesity remains a major problem in the management of Type 2 diabetes mellitus and this justifies the search for new, safe and effective, pharmacological approaches. [less ▲]

Detailed reference viewed: 14 (0 ULg)
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See detailPharmacologie - Suivez la Flèche
Lambert, Philippe; Angenot, Luc ULg

Article for general public (1995)

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See detailPharmacologie - Suivre la Flèche
Lambert, Philippe; Angenot, Luc ULg

Article for general public (1996)

Detailed reference viewed: 10 (8 ULg)
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Peer Reviewed
See detailPharmacologie clinique des bisphosphonates : revue de littérature axée sur le tiludronate chez le cheval.
Delguste, Catherine ULg; Lepage, Olivier M; Amory, Hélène ULg et al

in Annales de Médecine Vétérinaire (2007), 151

Detailed reference viewed: 25 (3 ULg)
Peer Reviewed
See detailPharmacologie des canaux K+ATP-dépendants des cellules B pancréatiques: nouveaux développements
Lebrun, P.; Pirotte, Bernard ULg; Antoine, M. H.

Conference (1997, March 08)

Detailed reference viewed: 3 (0 ULg)
Peer Reviewed
See detailLa pharmacologie et le problème des résidus des agonistes 2 adrénergiques chez les bovins
Gustin, Pascal ULg; Ansay; Maghuin-Rogister, Guy ULg

in Annales de Médecine Vétérinaire (1989), 133

Detailed reference viewed: 15 (5 ULg)
Peer Reviewed
See detailPharmacology of a new sulfonylurea (BM 27) effective in brain edema
Masereel, B.; Schynts, M.; Pirotte, Bernard ULg et al

Conference (1994, March)

Peer Reviewed
See detailPharmacology of a new sulfonylurea (BM 27) effective in brain edema
Masereel, B.; Schynts, M.; Pirotte, Bernard ULg et al

in Journal de Pharmacie de Belgique (1994), 49

Detailed reference viewed: 8 (0 ULg)
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Peer Reviewed
See detailPharmacology Of The Hypoglycaemic Sulphonylurea Gliquidone .3. Conformational Analysis
Lins, Laurence ULg; Brasseur, Robert ULg; Malaisse, Wj.

in Pharmacological Research (1996), 34(1-2), 9-10

The hypoglycaemic sulphonylurea gliquidone was found, by conformation analysis, to display a U-shaped configuration, with hydrophobic cycles placed at the extremity of each branch and a peptidic bond ... [more ▼]

The hypoglycaemic sulphonylurea gliquidone was found, by conformation analysis, to display a U-shaped configuration, with hydrophobic cycles placed at the extremity of each branch and a peptidic bond placed at the bottom of the U. This configuration is similar to that recently observed with the hypoglycaemic sulphonylureas glimepiride and glibenclamide and non-sulphonylurea hypoglycaemic agents of the meglitinide family, such as S3075, repaglinide, A-4166 and KAD-1229. The identification of a conformation common to these various hypoglycaemic drugs may provide an imprint of their binding site at the level of the B-cell sulphonylurea receptor. [less ▲]

Detailed reference viewed: 24 (1 ULg)
Peer Reviewed
See detailPharmacology of the Thromboxane Receptor Antagonist and Thromboxane Synthase Inhibitor Bm-531
Dogné, J. M.; Rolin, S.; de Leval, X. et al

in Cardiovascular Drug Reviews (2001), 19(2, Summer), 87-96

BM-531 (N-tert-butyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative, is a novel noncarboxylic thromboxane receptor antagonist and thromboxane synthase inhibitor. Indeed, its ... [more ▼]

BM-531 (N-tert-butyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea), a torasemide derivative, is a novel noncarboxylic thromboxane receptor antagonist and thromboxane synthase inhibitor. Indeed, its affinity for human washed platelet TXA2 receptors labeled with [3H]SQ-29548 (IC50 = 0.0078 microM) is higher than sulotroban (IC50 = 0.93 microM) and SQ-29548 (IC50 = 0.021 microM). Moreover, BM-531 is characterized by a potent antiaggregatory property. Indeed, on one hand, in human citrated platelet-rich plasma BM-531 prevents platelet aggregation induced by arachidonic acid (600 microM) (ED100 = 0.125 microM), U-46619, a stable TXA2 agonist (1 microM) (ED50 = 0.482 microM) or collagen (1 microgram/mL) (percentage of inhibition: 42.9% at 10 microM) and inhibits the second wave of ADP (2 microM)-induced aggregation. On the other hand, when BM-531 is incubated in whole blood from healthy donors, the closure time measured by the recently developed platelet function analyser (PFA-100) is significantly prolonged. In addition, at the concentrations of 10 and 1 microM, BM-531 totally prevents the production of TXB2 by human platelets activated by arachidonic acid. Finally, at 10 microM, BM-531 significantly prevents rat fundus contractions induced by U-46619 but not by prostacyclin. These results suggest that BM-531, which is devoid of the diuretic property of torasemide, can be regarded as a promising antiplatelet agent. [less ▲]

Detailed reference viewed: 10 (0 ULg)
See detailPharmacology of tiludronate in horses
Delguste, Catherine ULg

Conference (2008, November 08)

Detailed reference viewed: 9 (1 ULg)
Peer Reviewed
See detailPharmacomodulation of torasemide led to original diuretic, neuroprotective, anticonvulsant and antithrombotic drugs
Masereel, B.; Dogne, J. M.; Damas, J. et al

Conference (1997, April)

Detailed reference viewed: 5 (0 ULg)
Peer Reviewed
See detailPharmacomodulation of torasemide led to original diuretic, neuroprotective, anticonvulsant and antithrombotic drugs
Masereel, B.; Dogne, J.-M.; Damas, J. et al

in Journal de Pharmacie de Belgique (1997), 52

Detailed reference viewed: 4 (0 ULg)
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See detailPHARMACOMODULATIONS DU WAY-100635 : DE NOUVELLES PISTES DANS LA CONCEPTION D’ANTAGONISTES SÉLECTIFS DES RÉCEPTEURS 5-HT1A
Dilly, Sébastien ULg; Mangin, Floriane; Joly, Benoît ULg et al

Poster (2012, May 24)

Le composé WAY-100635 est un outil pharmacologique abondamment utilisé dans l’exploration des récepteurs sérotoninergiques 5-HT1A. Dès lors, cette molécule de référence devrait présenter une sélectivité ... [more ▼]

Le composé WAY-100635 est un outil pharmacologique abondamment utilisé dans l’exploration des récepteurs sérotoninergiques 5-HT1A. Dès lors, cette molécule de référence devrait présenter une sélectivité importante pour sa cible. Cependant, des travaux récents ont démontré que, à côté de son activité antagoniste des récepteurs 5-HT1A, le WAY-100635 possédait également une affinité et activité conséquentes vis-à-vis des récepteurs dopaminergiques D4, ce qui pourrait limiter son utilisation comme outil pharmacologique. Dans ce contexte, nous avons entrepris diverses modulations structurales de cette molécule de manière à augmenter sa sélectivité vis-à-vis des récepteurs 5-HT1A. Cette sélectivité a été augmentée de manière significative lors du remplacement de la chaîne latérale basique par un groupement 4-phénylpipérazine ou 4-phényl-1,2,3,6-tétrahydropyridine. Une évaluation biologique plus approfondie des deux composés comprenant un profil d’affinité élargi à d’autres récepteurs a confirmé leur sélectivité vis-à-vis des récepteurs 5-HT1A. De plus, des expériences électrophysiologiques sur tranches de cerveau. [less ▲]

Detailed reference viewed: 23 (1 ULg)
Peer Reviewed
See detailPharmacophore generation to design new leads for selective cyclooxygenase-2 (COX-2) inhibition
Michaux, C.; De Leval, X.; Julemont, F. et al

Poster (2003, May)

Detailed reference viewed: 10 (0 ULg)
Peer Reviewed
See detailPharmacophore generation to design new leads for selective cyclooxygenase-2 inhibition
Michaux, C.; Julemont, F.; De Leval, X. et al

Poster (2004, October 07)

Detailed reference viewed: 8 (0 ULg)
See detailPharmacopoea Aegyptia et Graeco-Aegyptia : bibliographie générale
Marganne, Marie-Hélène ULg; Koemoth, Pierre ULg

Textual, factual or bibliographical database (2003)

Bibliographical references to identify animal, plant and mineral products used in the pharmacopoeias of Pharaonic, Greco-Roman and Byzantine Egypt

Detailed reference viewed: 41 (8 ULg)
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Peer Reviewed
See detailPharmacotherapy of onychomycosis
Baran, R.; Gupta, A. K.; Pierard, Gérald ULg

in Expert Opinion on Pharmacotherapy (2005), 6(4), 609-624

Fungal infections of the nails are frequent in some segments of the population. Dermatophytes, yeasts and moulds are potential pathogens. A series of antifungal treatments are available to the clinician ... [more ▼]

Fungal infections of the nails are frequent in some segments of the population. Dermatophytes, yeasts and moulds are potential pathogens. A series of antifungal treatments are available to the clinician, differing by both their mechanistic nature and mode of administration. The pharmacodynamic and pharmacokinetic properties of each antifungal agent are distinct. This review focuses on the characteristics of amorolfine, bifonazole, ciclopirox, fluconazole, griseofulvin, itraconazole, ketoconazole, ravuconazole, R126638 and terbinafine. Single drug treatments and combined therapies are presented. None of the current drug regimens have demonstrated reliable efficacy against all cases of onychomycosis. Treatment failures, relapses and reinfections remain stubborn problems in the management of onychomycosis. [less ▲]

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Peer Reviewed
See detailA phase 1-2, prospective, double blind, randomized study of the safety and efficacy of Sulfasalazine for the treatment of progressing malignant gliomas: study protocol of [ISRCTN45828668].
Robe, Pierre ULg; Martin, Didier ULg; Albert, Adelin ULg et al

in BMC Cancer (2006), 6

BACKGROUND: The prognosis of patients suffering from WHO grade 3 and 4 astrocytic glioma remains poor despite surgery, radiation therapy and the use of current chemotherapy regimen. Indeed, the median ... [more ▼]

BACKGROUND: The prognosis of patients suffering from WHO grade 3 and 4 astrocytic glioma remains poor despite surgery, radiation therapy and the use of current chemotherapy regimen. Indeed, the median survival of glioblastoma multiforme (WHO grade 4) patients is at best 14.6 month with only 26.5 percent of the patients still alive after 2 years and the median survival of anaplastic astrocytomas (WHO grade 3) is 19.2 month. Recent evidence suggests that the transcription factor NF-kappaB is constitutively expressed in malignant gliomas and that its inhibition by drugs like Sulfasalazine may block the growth of astrocytic tumors in vitro and in experimental models of malignant gliomas. DESIGN: ULg_GBM_04/1 is a prospective, randomized, double blind single-center phase 1-2 study. A total of twenty patients with progressive malignant glioma despite surgery, radiation therapy and a first line of chemotherapy will be recruited and assigned to four dosage regimen of Sulfasalazine. This medication will be taken orally t.i.d. at a daily dose of 1.5-3-4 or 6 g, continuously until complete remission, evidence of progression or drug intolerance. Primary endpoints are drug safety in the setting of malignant gliomas and tumor response as measured according to MacDonald's criteria. An interim analysis of drug safety will be conducted after the inclusion of ten patients. The complete evaluation of primary endpoints will be conducted two years after the enrollment of the last patient or after the death of the last patient should this occur prematurely. DISCUSSION: The aim of this study is to evaluate the safety and efficacy of Sulfasalazine as a treatment for recurring malignant gliomas. The safety and efficacy of this drug are analyzed as primary endpoints. Overall survival and progression-free survival are secondary endpoint. [less ▲]

Detailed reference viewed: 74 (19 ULg)