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See detailAntioxidant to treat osteoarthritis: dream or reality?
Henrotin, Yves ULg; Kurz, B.

in Current Drug Targets (2007), 8(2), 347-57

Osteoarthritis is one of the most common chronic diseases that causes pain and physical disability in patient. Although OA is considered as a global disease affecting all joint tissues, cartilage ... [more ▼]

Osteoarthritis is one of the most common chronic diseases that causes pain and physical disability in patient. Although OA is considered as a global disease affecting all joint tissues, cartilage degradation is the end point. The degradation of cartilage results of the combination of mechanical stress and biochemical factors, mainly metalloproteinases and reactive oxygen species (ROS). The activity of reactive oxygen species is balanced by enzymatic and non-enzymatic antioxidants, that act by inhibiting oxidative enzymes, scavenging free radicals or chelating ion metals. Until now, few information is available on the antioxidative status of chondrocytes. Further, the modification of the antioxidative system in osteoarthritis remains unknown. Some antioxidant supplements or drugs with antioxidant properties have been developed to reinforce the cellular antioxidant status. However, until now, there is no consistent evidence that additional antioxidant supply is efficient to relieve OA symptoms or to prevent structural changes in OA cartilage. [less ▲]

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See detailAntioxidant vitamin cocktail does not improve calves'lung function and airway inflammation in ozone-induced pulmonary disease
Kirschvink, Nathalie; Jacqmot, Olivier ULg; Fievez, Laurence ULg et al

in Pflügers Archiv : European Journal of Physiology (2001), 442(R42),

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See detailAntioxidants involvement in the Ageing of Non-Green Organs
Delaplace, Pierre ULg; Fauconnier, Marie-Laure ULg; du Jardin, Patrick ULg

in Gupta, S. Dutta (Ed.) Reactive oxygen species and antioxidants in higher plants (2010)

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See detailAntioxydant activity of β-carboline derivatives in the LDL oxidation model
Hadjaz, Fariza; Besret, Soizic; Martin-Nizard, Françoise et al

in European Journal of Medicinal Chemistry (2001), 46

A series of b-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the ... [more ▼]

A series of b-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO4 or 2,20-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective actions of these compounds against the cytotoxicity were evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Most of compounds showed an higher antioxidant activity than GWC22 derivative (R = 1.6 for 5 mM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R = 1.9 to 2.8 for 1 mM CuSO4. These substances have protective actions and increase significantly the cell viability. [less ▲]

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See detailAntioxydants et santé : conseils pratiques.
PINCEMAIL, Joël ULg

Conference (2015, January)

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See detailAntiparasitic activities of two sesquiterpenic lactones isolated from Acanthospermum hispidum D.C
Ganfon; Bero, Joanne; Tchinda Tiabou, Alembert ULg et al

in Journal of Ethnopharmacology (2012), 141(0), 411-417

Ethnopharmacological relevance : Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria Aim of the study : Identify ... [more ▼]

Ethnopharmacological relevance : Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria Aim of the study : Identify active compounds from extracts of Acanthospermum hispidum D.CV. leaves previously shown to possess antimalarial properties and analyse in vivo activity and toxicity of crude extracts. Materials and methods : Compounds were isolated from aerial part of A. hispidum D.C. and structurally elucidated using extensive spectroscopic analysis. Antiplasmodial activity was evaluated in vitro against a chloroquinosensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity and in vivo against P. berghei berghei by the 4-days suppressive test. Selectivity of extract and purified compounds on Plasmodium parasites were evaluated by using MTT test on J774 macrophage like murine cells and WI38 human normal fibroblasts and also against two other parasites: Trypanosoma brucei brucei and Leishmania mexicana mexicana. Acute and sub-acute toxicities of a crude extract were evaluated on mice. Results : Two known sesquiterpenic lactones were isolated: 1 (15-acetoxy-8β-[(2-methylbutyryloxy)]-14-oxo-4, 5-cis-acanthospermolide) and 2 (9α-acetoxy-15-hydroxy-8β-(2-methylbutyryloxy) -14-oxo-4, 5-trans-acanthospermolide). 1 and 2 showed in vitro antiplasmodial activity against the chloroquino-sensitive strain (3D7) with IC50 of 2.9 ± 0.5 and 2.23 ± 0.09 μM respectively. Only 2 showed a high selectivity index (SI: 18.4) on Plasmodium compared to cytotoxicity against human fibroblasts cell line (WI38). 1 and 2 also showed interesting antiparasitic activities in vitro against Trypanosoma brucei brucei (IC50 of 2.45 ± 0.49 and 6.36 ± 1.42 μM respectively) and Leishmania mexicana mexicana (IC50 of 0.94 ± 0.05 and 2.54 ± 0.19 μM respectively). Furthermore, crude acidic water extract and fractions containing one of the two isolated compounds displayed a weak in vivo antimalarial activity against P. berghei berghei with a long half-life causing a delayed effect. In vivo acute (2000 mg/kg) and sub-acute (1000 mg/kg) toxicity tests on the crude acidic water extract did not show toxicity. Conclusion : Crude acidic water extract, fractions and pure isolated compounds from A.hispidum showed promising in vitro antiplasmodial activity. Despite our study did not show in vivo acute and subacute toxicities of the crude acidic water extract, its weak in vivo antimalarial activity and the in vitro cytoxicity of pure compounds and enriched extracts containing 1 and 2 indicate that the aerial parts of A. hispidum should be used with caution for malaria treatments. [less ▲]

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See detailAntiparasitic hybrids of Cinchona alkaloids and bile acids.
Leverrier, Aurelie; Bero, Joanne; Frederich, Michel ULg et al

in European journal of medicinal chemistry (2013), 66

A series of 16 hybrids of Cinchona alkaloids and bile acids (4a-h, 5a-h) was prepared by means of a Barton-Zard decarboxylation reaction. Quinine, quinidine, cinchonine and cinchonidine were ... [more ▼]

A series of 16 hybrids of Cinchona alkaloids and bile acids (4a-h, 5a-h) was prepared by means of a Barton-Zard decarboxylation reaction. Quinine, quinidine, cinchonine and cinchonidine were functionalized at position C-2 of the quinoline nucleus by radical attack of a norcholane substituent. The newly synthesized hybrids were evaluated in vitro for their antitrypanosomal, antileishmanial and antiplasmodial activities, along with their cytotoxicity against WI38, a normal human fibroblast cell line. Seven compounds (4d, 4f, 4h, 5b, 5d, 5f, 5h) showed promising trypanocidal activity with IC(5)(0) values in the same range as the commercial drug suramine. Moreover all the 16 hybrids showed antiplasmodial activity (IC(5)(0) </= 6 mug/ml), particularly those containing a nor-chenodeoxycholane moiety (4b, 4d, 4f, 4h, 5b, 5d, 5f, 5h) with IC(5)(0) values comparable to those of the natural alkaloids, and selectivity indices in the range of 5.6-15.7. [less ▲]

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See detailAntiparasitic Properties of Diploceline, a Quaternary Alkaloid from Strychnos gossweileri
Gasquet, Monique; Quetin-Leclercq, Joëlle; Timon-David, Pierre et al

in Planta Medica (1992), 58

The activity of diploceline is relatively weak as compared to metronidazole on Entamoeba histolytica and Trichomonas vaginalis. The quaternary alkaloid does not produce any inhibition of Plasmodium ... [more ▼]

The activity of diploceline is relatively weak as compared to metronidazole on Entamoeba histolytica and Trichomonas vaginalis. The quaternary alkaloid does not produce any inhibition of Plasmodium falciparum growth at 25 micrograms/ml (maximum tested concentration). [less ▲]

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See detailAntipeptide antibody against the bovine IGF-BP-2 : application to the detection of BST-treated cows
Scippo, Marie-Louise ULg; Degand, Guy ULg; Duyckaerts, Anne et al

in Food & Agricultural Immunology (1996), 8

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See detailAntiphase synchronization of electrically shaken conducting beads
Mersch, Eric ULg; Vandewalle, Nicolas ULg

in Physical Review. E : Statistical, Nonlinear, and Soft Matter Physics (2011), 84

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See detailAntiplasmodial activity of alkaloids from various Strychnos species
Frederich, Michel ULg; Jacquier, M. J.; Thepenier, P. et al

in Journal of Natural Products (2002), 65(10), 1381-1386

The in vitro antiplasmodial activities of 69 alkaloids from various Strychnos species were evaluated against chloroquine-resistant and chloroquine-sensitive lines of Plasmodium falciparum. The compounds ... [more ▼]

The in vitro antiplasmodial activities of 69 alkaloids from various Strychnos species were evaluated against chloroquine-resistant and chloroquine-sensitive lines of Plasmodium falciparum. The compounds, comprising mainly indolomonoterpenoid alkaloids, exhibited a wide range of biological potencies in the antiplasmodial assays. The most active alkaloids were also tested for cytotoxicity against HCT-116 colon cancer cells to determine their antiplasmodial selectivity. As a result of these studies, structure-activity relationships for these alkaloids have begun to emerge. Alkaloids presenting four types of bisindole skeleton exhibited potent and selective activities against Plasmodium. They were sungucine-type (IC(50) values ranging from 80 nM to 10 microM), longicaudatine-type (IC(50) values ranging from 0.5 to 10 microM), matopensine-type (IC(50) values ranging from 150 nM to 10 microM), and usambarine-type alkaloids. Within the last structural type, isostrychnopentamine (49) and ochrolifuanine A (46) were found to be active against chloroquine-sensitive and -resistant strains (IC(50) values of 100-150 and 100-500 nM, respectively), and dihydrousambarensine (51) exhibited a 30-fold higher activity against the chloroquine-resistant strain (IC(50) = 32 nM) than against the chloroquine-sensitive one. [less ▲]

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See detailAntiplasmodial Alkaloids from the Stem Bark of Strychnos malacoclados.
Tchinda Tiabou, Alembert ULg; Ngono, A. R.; Tamze, V. et al

in Planta Medica (2012), 78

From the stem bark of STRYCHNOS MALACOCLADOS, one new bisindole alkaloid, 3-hydroxylongicaudatine Y ( 1), was isolated along with the known alkaloids vomicine ( 2), bisnordihydrotoxiferine ( 3), divarine ... [more ▼]

From the stem bark of STRYCHNOS MALACOCLADOS, one new bisindole alkaloid, 3-hydroxylongicaudatine Y ( 1), was isolated along with the known alkaloids vomicine ( 2), bisnordihydrotoxiferine ( 3), divarine ( 4), longicaudatine ( 5), longicaudatine Y ( 6), and longicaudatine F ( 7). All the compounds were tested for their antimalarial activity against the chloroquine-sensitive 3D7 and -resistant W2 strains of PLASMODIUM FALCIPARUM. Longicaudatine was the most active compound with IC (50) values of 0.682 and 0.573 microM, respectively. The activity of compounds 1, 3, 4, 6, and 7 against the two strains ranged from 1.191 to 6.220 microM and 0.573 to 21.848 microM, respectively. Vomicine ( 2), the only monomer isolated, was inactive. The alkaloids of the longicaudatine-type ( 1, 5- 7) were more active than those of the caracurine-type ( 3- 4). The presence of the ether bridge in the molecule seems to increase the antiplasmodial activity. Compounds 1, 5, and 7 were tested against the WI-38 human fibroblast cell line. Longicaudatine was the most cytotoxic compound with an IC (50) of 2.721 microM. Longicaudatine F was 40-46 times more active against the two strains of P. FALCIPARUM than against the human fibroblasts and was thus considered as the more selective alkaloid. The structures of the compounds were determined based on the analysis of their spectral data. [less ▲]

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See detailAntiplasmodial and antitrypanosomal activity of Triclisia sacleuxii (Pierre) Diels
Murebwayire, Sangabo; Frederich, Michel ULg; Hannaert, V. et al

in Phytomedicine : International Journal of Phytotherapy and Phytopharmacology (2008), 15(9), 728-733

The antiplasmodial and antitrypanosomal activities of Triclisia sacleuxii (Pierre) Diels were investigated on three Plasmodium falciparum strains [FcB1, 3D7 (chloroquine – sensitive) and W2 (chloroquine – ... [more ▼]

The antiplasmodial and antitrypanosomal activities of Triclisia sacleuxii (Pierre) Diels were investigated on three Plasmodium falciparum strains [FcB1, 3D7 (chloroquine – sensitive) and W2 (chloroquine – resistant) strains] and on Trypanosoma brucei Tbsf 221. Roots, stems and leaves ethanolic extracts as well as crude tertiary and quaternary alkaloids fractions were considered. Whereas the ethanolic extracts and quaternary crude alkaloids fractions exhibited no significant activity, the roots and stems tertiary alkaloid fractions revealed interesting growth inhibition against the Plasmodium FcB1 and Trypanosoma Tbsf 221 strains. The IC50 were 1.04 and 0.89 g/ml (roots), 2.50 and 0.91 g/ml (stems), respectively. The leaves tertiary alkaloids fraction also showed a promising antitrypanosomal activity (IC50 : 1.85 g/ml). Phytochemical analysis of the roots tertiary alkaloids fraction yielded four major compounds, phaeanthine, N-methylapateline, 1,2-dehydroapateline and 1,2-dehydrotelobine, which were identified on the basis of their spectroscopic data. The four compounds displayed (in vitro) antitrypanosomal activity with IC50 of 2.68, 1.19, 1.06 and 1.11 µM, respectively. They also demonstrated antiplasmodial activity on Plasmodium falciparum 3D7, with IC50 of 1.72, 0.93, 1.39 and 12.4 µM respectively and on the chloroquine – resistant W2 with IC50 of 0.35, 1.10, 1.63, 1.52 µM. [less ▲]

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See detailAntiplasmodial and cytotoxic activities of Rwandan medicinal plants used in the treatment of malaria.
Muganga, R.; Angenot, Luc ULg; Tits, Monique ULg et al

in Journal of Ethnopharmacology (2010), 128

AIM OF THE STUDY: In our study, methanol, dichloromethane and aqueous extracts of 13 Rwandan medicinal plants used in the treatment of malaria were tested for in vitro antiplasmodial activity. MATERIALS ... [more ▼]

AIM OF THE STUDY: In our study, methanol, dichloromethane and aqueous extracts of 13 Rwandan medicinal plants used in the treatment of malaria were tested for in vitro antiplasmodial activity. MATERIALS AND METHODS: The growth inhibition of chloroquine-sensitive Plasmodium falciparum strain (3D7) was evaluated using the measurement of lactate dehydrogenase activity. The active extracts were also tested against the chloroquine-resistant Plasmodium falciparum strain (W2) and for cytotoxicity assay using human normal foetal lung fibroblasts (WI-38). RESULTS: The majority of the plants tested showed an antiplasmodial activity and the best results were observed with dichloromethane leaf and flower extracts of Tithonia diversifolia, leaf extract of Microglossa pyrifolia and root extract of Rumex abyssinicus, methanol leaf extract of Fuerstia africana, root bark extracts of Zanthoxylum chalybeum and methanol bark extract of Terminalia mollis. Those extracts were active (IC(50)<15mug/ml) on both chloroquine-sensitive and resistant strains of Plasmodium falciparum. Zanthoxylum chalybeum, Solanecio mannii and Terminalia mollis presented the best selectivity index. CONCLUSIONS: The traditional use of most of the plant evaluated was confirmed by the antiplasmodial test. This study revealed for the first time the antiplasmodial activity of two plants: Terminalia mollis and Rumex abyssinicus. [less ▲]

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See detailAntiplasmodial and cytotoxic alkaloids from Strychnos species
Frederich, Michel ULg

Conference (2003, March 14)

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See detailAntiplasmodial anthraquinones and hemisynthetic derivatives from the leaves of Tectona grandis (Verbenaceae)
Kopa, T.K.; Tchinda Tiabou, Alembert ULg; Tala, M.F. et al

in Phytochemistry Letters (2014), 8

Chemical investigation of the methanol extract of the leaves of Tectona grandis led to the isolation of one new anthraquinone derivative, grandiquinone A (3-acetoxy-8-hydroxy-2-methylanthraquinone) (1 ... [more ▼]

Chemical investigation of the methanol extract of the leaves of Tectona grandis led to the isolation of one new anthraquinone derivative, grandiquinone A (3-acetoxy-8-hydroxy-2-methylanthraquinone) (1), along with nine known compounds: 5,8-dihydroxy-2-methylanthraquinone (2), hydroxysesamone (3), 3-hydroxy-2-methylanthraquinone (4), quinizarine (5), betulinic acid (6), ursolic acid (7), tectograndone (8), corosolic acid (9) and sitosterol 3-O-β-d-glucopyranoside (10). Compounds 2 and 3 were isolated for the first time from the leaves of this plant, while 5 has never been reported from the genus Tectona. Hydroxysesamone (3) and tectograndone (8) were subjected to cyclisation and acetylation reactions to afford two hemisynthetic derivatives, 6,9-dihydroxy-2,2-(dimethyldihydropyrano)-3,4-dihydro-2H-benzo[g]chromene-5,10-dione (11) and acetyltectograndone (12) respectively, which are reported here for the first time. The ethyl acetate-soluble portion, some of the isolated compounds and hemisynthetic derivatives were evaluated for their antiplasmodial activity against the multidrug-resistant Dd2 strain of Plasmodium falciparum. Compound 3 showed a prominent activity, while 2, 8, 9, 11 and 12 showed significant in vitro anti-malarial activity. Compound 1 was weakly active in this test. The structures of the compounds were elucidated by spectroscopic methods and comparison of the data with the literature. [less ▲]

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See detailAntiplasmodial, anti-inflammatory and cytotoxic activities of various plant extracts from the Mascarene Archipelago.
Jonville, Marie ULg; Kodja, H.; Strasberg, D. et al

in Journal of Ethnopharmacology (2011), 136

AIM OF THE STUDY: Antiplasmodial activity, inhibition of nitric oxide (NO) overproduction, and anti-proliferative activity were investigated in vitro to evaluate the bioactive potential of the traditional ... [more ▼]

AIM OF THE STUDY: Antiplasmodial activity, inhibition of nitric oxide (NO) overproduction, and anti-proliferative activity were investigated in vitro to evaluate the bioactive potential of the traditional pharmacopoeia of the Mascarene Archipelago, which is known for its biodiversity and for the richness of its endemic flora. MATERIALS AND METHODS: A total of 45 methanol (MeOH) and dichloromethane (DCM) extracts were prepared from 19 plant species collected on Reunion and Mauritius Islands. Ninety-six-well microplate assays were performed on chloroquine sensitive Plasmodium falciparum 3D7 strain, on LPS-stimulated Raw 264.7 murine macrophages and on A-549, DLD-1 and WS1 human cells. Activity was evaluated through spectrophotometric methods. RESULTS: Activity was attributed to plant extracts expressing IC(50)<50mug/ml for antiplasmodial response, IC(50)<100mug/ml for cytotoxicity, and IC(50)<130mug/ml for anti-inflammatory reaction. The majority of the extracts tested (69%) exhibited potency in at least one of these three types of activity. This is the first report describing promising antiplasmodial activity (IC(50)<15mug/ml) for Psiadia dentata DCM extract and Terminalia bentzoe MeOH bark extract. NO inhibition assay revealed seven interesting plants, described for the first time as anti-inflammatory: Aphloia theiformis, Buddleja salviifolia, Eupatorium riparium, Hiptage benghalensis, Psiadia arguta, Psiadia dentata, and Scutia commersonii. Finally, anti-proliferative activity was observed for two endemic species, Geniostoma borbonicum and Nuxia verticillata. CONCLUSION: Using the criterion of endemism as part of the criteria for traditional medicinal use raises the chances of finding original active principles. In our case, 86% of the endemic plants tested displayed pharmacological interest. [less ▲]

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See detailAntiplatelet Activity of Clopidogrel in Coronary Artery Bypass Graft Surgery Patients
David, Jean-Louis ULg; Limet, Raymond ULg

in Thrombosis and Haemostasis (1999), 82(5), 1417-21

Clopidogrel is a recently introduced platelet ADP receptor antagonist, belonging to the thienopyridine derivatives, like its analogue ticlopidine. Its potential advantage is to be safer than ticlopidine ... [more ▼]

Clopidogrel is a recently introduced platelet ADP receptor antagonist, belonging to the thienopyridine derivatives, like its analogue ticlopidine. Its potential advantage is to be safer than ticlopidine. At 75 mg/od clopidogrel significantly inhibits platelet aggregation in ambulatory patients with symptomatic atherosclerotic disease and it prevents the recurrence of ischemic events more efficiently than aspirin. Its adequate dose in more acute situations remained to be determined. Therefore, sixty two patients with coronary artery disease were randomly assigned in four groups treated, within 24 h after coronary artery bypass graft, by clopidogrel 50 mg/od, 75 mg/od or 100 mg/od or by ticlopidine 250 mg/bid which was considered as the reference. The tolerance of clopidogrel was fairly good during the whole period of the study. Bleeding time and ex-vivo platelet aggregation induced by ADP 2 microM and 5 microM were performed at day -1, +9 and +28 after surgery. Like ticlopidine, the three dose levels of clopidogrel significantly inhibited ex-vivo platelet activity and prolonged the bleeding time at day 28. However, unlike ticlopidine, the inhibitory effects of clopidogrel were not significant at day 9, especially with 75 mg/od, a dose which was found to significantly protect patients in a chronic situation. Hence, although the clinical outcome for patients included in this limited study was the same in the four groups, these results suggest that the dose regime of clopidogrel should be more extensively investigated during the early period following coronary artery bypass graft, facing an overproduction of young and hyperreactive platelets. By analogy, the dose regime should be also investigated in other situations with an acute risk of arterial thrombotic occlusion. [less ▲]

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See detailAntiplatelet therapy in the perioperative period.
Engelen, S.; Sinaeve, P.; Van Damme, Hendrik ULg et al

in Acta Anaesthesiologica Belgica (2010), 61

antiplatelet drugs are the cornerstone treatment in the secondary prevention of arterial thrombosis. Until recently, their intake was interrupted in the perioperative period because of fear for bleeding ... [more ▼]

antiplatelet drugs are the cornerstone treatment in the secondary prevention of arterial thrombosis. Until recently, their intake was interrupted in the perioperative period because of fear for bleeding, but new insights have challenged this old habit. in patients at high risk for atherothrombotic events who need to undergo surgery or an invasive procedure, the risk for bleeding complications because of a treatment with low-dose acetylsalicylic acid (lD aSa) needs to be balanced against the risk of atherothrombotic events after treatment discontinuation. for patients at high risk of atherothrombotic complications recent guidelines do no longer advocate to interrupt lD aSa routinely. However, the likelihood of bleeding versus atherothrombotic complications should be considered on a case-by-case basis. when continued perioperatively, the bleeding risk associated with thienopyridines (ticlopidine, clopidogrel and prasugrel) is higher than that of lD aSa. it is recommended to stop their intake 1 week before the surgical intervention, except in patients with (recent) coronary stenting [less ▲]

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See detailAntipodean Dialogue in the Novels of David Malouf
Delrez, Marc ULg

Conference (1988)

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