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See detailLe medicament du mois. Le lixisenatide (Lyxumia): nouvel agoniste des recepteurs du glucagon-like peptide-1 a action preferentiellement post-prandiale.
Scheen, André ULg

in Revue medicale de Liege (2014), 69(2), 102-9

Lixisenatide (Lyxumia) is a new agonist of Glucagon-Like Peptide-1 (GLP-1) receptors that is indicated in the treatment of type 2 diabetes, in one single subcutaneous daily injection of 20 microg. It ... [more ▼]

Lixisenatide (Lyxumia) is a new agonist of Glucagon-Like Peptide-1 (GLP-1) receptors that is indicated in the treatment of type 2 diabetes, in one single subcutaneous daily injection of 20 microg. It exerts an incretin effect by stimulating insulin secretion after a meal while inhibiting glucagon secretion, both in a glucose-dependent manner, which limits the risk of hypoglycaemia. In addition, it slows down gastric emptying after a meal, which contributes to reduce postprandial hyperglycaemia, especially after breakfast. Lixisenatide is currently reimbursed in Belgium after failure of a dual therapy with metformin and a sulfonylurea but also in combination with a basal insulin (with or without oral antidiabetic drugs). The latter interesting combination should tackle fasting glycaemia with basal insulin (after appropriate dose titration) and postprandial hyperglycaemia with the GLP-1 receptor agonist in a complementary manner. The consequence is a further improvement of glycated haemoglobin (HbA(1c)) varying between 0.3 and 0.9% in various studies comparing lixisenatide versus placebo. As other compounds of the class, lixisenatide induces a small weight reduction, which contrasts with the weight gain commonly observed with other antidiabetic medications (including insulin). Further studies should demonstrate the effects of lixisenatide on vascular complications and overall prognosis of patients with type 2 diabetes. [less ▲]

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See detailLe médicament du mois. Le tacrolimus topique (Protopic).
Pierard, Gérald ULg; Pierard, Claudine ULg; Paquet, Philippe ULg

in Revue Médicale de Liège (2002), 57(8), 552-5

Tacrolimus is a potent inhibitor of immune mechanisms. It belongs to the macrolactam group. It inhibits the release of both Th1 and Th2 cytokines. It proves to be efficacious after topical application in ... [more ▼]

Tacrolimus is a potent inhibitor of immune mechanisms. It belongs to the macrolactam group. It inhibits the release of both Th1 and Th2 cytokines. It proves to be efficacious after topical application in the treatment of atopic dermatitis. In this indication, tacrolimus challenges topical corticosteroids. Irritation risks are present. The local immuno-depression can boost disseminated infections including herpes. The risk to promote photocarcinogenesis on the long term, and that bound to chronic resorption remain theoretical concerns that have not been assessed so far. [less ▲]

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See detailLe medicament du mois. Le tiotropium (SPIRIVA)
Corhay, Jean-Louis ULg; Louis, Renaud ULg

in Revue Médicale de Liège (2004), 59(9), 530-3

SPIRIVA (tiotropium) is a long-acting anticholinergic bronchodilatator, inhaled once a day, which produces relaxation of airway smooth muscle through antagonism of acetylcholine at M3-muscarinic receptors ... [more ▼]

SPIRIVA (tiotropium) is a long-acting anticholinergic bronchodilatator, inhaled once a day, which produces relaxation of airway smooth muscle through antagonism of acetylcholine at M3-muscarinic receptors. Its duration of action is at least 24h with once daily administration of tiotropium. Several studies have shown its efficacy and its good tolerance in the treatment of patients who are suffering from moderate to very severe chronic obstructive pulmonary disease (COPD). SPIRIVA improves spirometric measurements and quality of life, and reduces dyspnea and exacerbation rate in COPD patients. [less ▲]

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See detailLe medicament du mois. Le vardenafil (Levitra).
Scheen, André ULg

in Revue Médicale de Liège (2003), 58(9), 576-9

Vardenafil (Levitra), recently launched in Belgium by Bayer and Glaxo-SmithKline, is a new drug that potently and selectively inhibits phosphodiesterase type 5 (PDE5) in the cavernosum tissue of the penis ... [more ▼]

Vardenafil (Levitra), recently launched in Belgium by Bayer and Glaxo-SmithKline, is a new drug that potently and selectively inhibits phosphodiesterase type 5 (PDE5) in the cavernosum tissue of the penis. Inhibition of PDE5 blocks the hydrolysis of cyclic guanosine monophosphate (GMPc) and results in increased arterial blood flow leading to enlargement of the corpus cavernosum and resulting in erection. In controlled clinical trials, vardenafil at least doubled the rate of successful erections as compared to placebo, whatever the evaluation parameter considered and the subgroup of patients studied. Vardenafil is thus indicated in the treatment of patients with erectile dysfunction. It is presented as 5, 10 and 20 mg tablets and the usual dose is 10 mg to be ingested 25 to 60 minutes before sexual activity. Vardenafil has a more potent inhibitory activity of PDE5 in vitro than sildenafil or tadalafil while its pharmacokinetics in vivo is somewhat more rapid than that of the two other compounds. The dosage of vardenafil may be reduced to 5 mg (especially in older individuals) to improve tolerance or be increased up to 20 mg (especially in the presence of organic diseases aggravating erectile dysfunction) to improve efficacy. Contra-indications (co-administration with drugs increasing nitric oxide) and side-effects (headache and flushing due to vasodilatation) of vardenafil are similar to those of other PDE5 inhibitors. [less ▲]

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See detailLe medicament du mois. Liraglutide (Victoza): analogue du glucagon-like- peptide-1 humain en une injection par jour pour le traitement du diabete de type 2.
Scheen, André ULg; Van Gaal, L. F.

in Revue Médicale de Liège (2010), 65(7-8), 464-70

Liraglutide (Victoza) is a peptide produced by DNA recombinant technology, which presents 97% homology with human glucagon-like peptide-1 (GLP-1) but is resistant to dipeptidylpeptidase-4, the enzyme that ... [more ▼]

Liraglutide (Victoza) is a peptide produced by DNA recombinant technology, which presents 97% homology with human glucagon-like peptide-1 (GLP-1) but is resistant to dipeptidylpeptidase-4, the enzyme that degrades the natural hormone. It actives the GLP-1 receptor and exerts an incretin mimetic effect during at least 24 hours after a single subcutaneous injection. Besides a glucose-dependent stimulatory effect of insulin secretion, liraglutide inhibits glucagon secretion and retards gastric emptying. In patients with type 2 diabetes, it reduces glycated haemoglobin by at least 1%, without inducing hypoglycaemia. It also induces a moderate weight loss and a mild reduction in blood pressure. Gastrointestinal adverse events (nausea, vomiting) may occur during the initial phase of treatment, but rarely impose the interruption of the medication and usually diminish with time.Although indicated in combination with other glucose-lowering agents, liraglutide is currently reimbursed in Belgium only if administered in patients with type 2 diabetes not sufficiently controlled with a combination of metformin plus sulfonylurea or metformin plus a thiazolidinedione. Victoza is presented in prefilled pens and is injected subcutaneously once a day. Treatment will be initiated with 0.6 mg to improve digestive tolerance and the daily dose will be increased to 1.2 mg (usual dose) after at least one week, and up to 1.8 mg (maximal dose) if necessary. [less ▲]

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See detailLe medicament du mois. Lowette, un contraceptif pour traiter l'acne de la jeune femme.
Goffin, Véronique ULg; Pierard, Claudine ULg; Pierard, Gérald ULg

in Revue Médicale de Liège (2003), 58(4), 261-3

Acne is a multifactorial disorder affecting the vast majority of adolescents and young adults. Among the therapeutic armamentum, estroprogestative contraception can be offered to young women. The choice ... [more ▼]

Acne is a multifactorial disorder affecting the vast majority of adolescents and young adults. Among the therapeutic armamentum, estroprogestative contraception can be offered to young women. The choice must, however, be carefully targeted because the estroprogestative associations do not show similar anti-acne efficacy. A new contraceptive associating 20 micrograms of ethinyl estradiol and 100 micrograms of levonorgestrel (Lowette) has proven its clinical efficacy in this indication. [less ▲]

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See detailLe medicament du mois. Olmesartan medoxomil hydrochlorothiazide (Olmetec Plus ou Belsar Plus)
Lancellotti, Patrizio ULg

in Revue Médicale de Liège (2007), 62(3), 175-9

The therapeutic control of hypertension is still a global challenge and frequently requires combination therapy. Olmesartan medoxomil hydrochlorothiazide (Olmetec plus, Belsar plus) is a fixed-dose ... [more ▼]

The therapeutic control of hypertension is still a global challenge and frequently requires combination therapy. Olmesartan medoxomil hydrochlorothiazide (Olmetec plus, Belsar plus) is a fixed-dose combination of olmesartan 20 mg and hydrochlorothiazide 12.5 or 25 mg. Olmesartan is a well known angiotensin II AT1 receptor blocker characterized by a good efficacy, a fast and prolonged duration of action and a placebo-like tolerability. With the combination therapy, no significant change of pharmacokinetics of either component is observed. The fixed-dose combination results in a greater blood pressure reduction compared to monotherapy with either component. This is at least effective as or even more effective than the combination of atenolol or losartan with hydrochlorothiazide, respectively. The responder rate is about 90%. The safety and tolerability remain excellent. Beyond the antihypertensive effect, olmesartan significantly reduces vascular inflammation and the wall-to-lumen ration in arteries. The starting dose is 20/12.5 mg. [less ▲]

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See detailLe medicament du mois. Prasugrel (Efient): puissant inhibiteur de l'activation et de l'agregation plaquettaire de la classe des thienopyridines.
LANCELLOTTI, Patrizio ULg

in Revue Médicale de Liège (2010), 65(11), 642-7

Prasugrel (Efient), a thienopyridine of third generation, is a prodrug that, like clopidogrel, requires conversion to an active metabolite before binding to the platelet P2Y12 receptor to confer ... [more ▼]

Prasugrel (Efient), a thienopyridine of third generation, is a prodrug that, like clopidogrel, requires conversion to an active metabolite before binding to the platelet P2Y12 receptor to confer antiplatelet activity. At the currently studied doses, prasugrel inhibits adenosine diphosphate-induced platelet aggregation more rapidly, more consistently, and to a greater extent than do standard and higher doses of clopidogrel. The risk of myocardial ischemic events in patients with acute coronary syndromes has been shown to be reduced by means of platelet inhibition. Dual-antiplatelet therapy with aspirin and clopidogrel has become the cornerstone of treatment to prevent thrombotic complications of acute coronary syndromes and percutaneous coronary intervention. In patients with acute coronary syndromes (TRITON-TIMI 38 trial), prasugrel therapy was associated with significantly reduced rates of ischemic events, including stent thrombosis, but with an increased risk of major bleeding. Subjects with diabetes mellitus tended to even have a greater reduction in ischemic events with prasugrel. In Belgium, Efient is currently reimbursed for 1 year in patients with an acute coronary syndrome and scheduled for a percutaneous coronary intervention (PCI) who present at least one of the following criteria: primary PCI for ST-elevation myocardial infarction, stent thrombosis despite treatment with clopidogrel, or diabetes mellitus. [less ▲]

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See detailLe medicament du mois. Rimonabant (Acomplia): premier antagoniste des recepteurs CB1 du systeme endocannabinoide.
Scheen, André ULg; Van Gaal, L. F.

in Revue Médicale de Liège (2008), 63(1), 50-5

Rimonabant (Acomplia) is the first selective CB1 receptor blocker of the endocannabinoid system. Clinical trials showed that, compared to placebo, rimonabant 20 mg/ day consistently increases weight loss ... [more ▼]

Rimonabant (Acomplia) is the first selective CB1 receptor blocker of the endocannabinoid system. Clinical trials showed that, compared to placebo, rimonabant 20 mg/ day consistently increases weight loss, reduces waist circumference, improves atherogenic dyslipidaemia (low HDL cholesterol, high triglycerides, high small dense LDL), diminishes insulin resistance, reduces HbA1c levels, and contributes to lower blood pressure and C-reactive protein levels. Almost half of the most important metabolic effects occur beyond weight loss, suggesting direct peripheral effects of rimonabant, especially in visceral adipose tissue as suggested by the increase in adiponectin levels. Rimonabant at a daily dose of 20 mg is indicated as an adjunct to diet and exercise for the treatment of obese patients, or overweight patients with associated risk factor(s) such as type 2 diabetes or dyslipidaemia. Adverse effects concern digestive tract (nausea, mostly transient) and psychological disorders (depressed mood, anxiety), in relation to the mechanism of action of the drug. Therefore, rimonabant is contra-indicated in case of depression and/or in patients receiving antidepressants. [less ▲]

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See detailLe medicament du mois. Rosuvastatine (Crestor).
Scheen, André ULg

in Revue Médicale de Liège (2004), 59(1), 56-9

Rosuvastatin (Crestor) has been recently launched in Belgium by AstraZeneca. This new statin is indicated for the treatment of primary hypercholesterolaemia or combined dyslipidaemia, when changes in ... [more ▼]

Rosuvastatin (Crestor) has been recently launched in Belgium by AstraZeneca. This new statin is indicated for the treatment of primary hypercholesterolaemia or combined dyslipidaemia, when changes in dietary habits are insufficient. Direct comparative randomised clinical trials with other statins demonstrated that rosuvastatin exerts a more favourable impact on lipid profile. When compared on a mg basis to other statins, rosuvastatin is associated with a greater reduction in total and LDL cholesterol levels and a greater increase of HDL cholesterol concentration, with a similar decrease in triglyceride levels. At the usual dosage of 10 mg, rosuvastatin allowed to reduce LDL cholesterol below recommended target levels for at risk patients among almost 80% of treated individuals in phase III clinical trials. If necessary, the daily dosage may be increased to 20 mg, or up to 40 mg (maximal dose), mostly in case of severe familial hypercholesterolaemia. Safety profile is good and similar to that of other commercialised statins. Rosuvastatin is currently evaluated in an extensive programme of randomised clinical trials (Galaxy programme) in order to demonstrate its efficacy in both prevention of atherosclerosis and reduction of cardiovascular morbidity and mortality. [less ▲]

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See detailLe medicament du mois. Saxagliptine (ONGLYZA): nouvel inhibiteur de la dipeptidylpeptidase-4 pour le traitement oral du diabete de type 2.
Scheen, André ULg

in Revue Médicale de Liège (2010), 65(9), 527-32

Saxagliptin (Onglyza) is a specific and reversible inhibitor of dipeptidylpeptidase-4 (DPP-4), which inhibits the activity of the enzyme for at least 24 hours after one single oral administration. It ... [more ▼]

Saxagliptin (Onglyza) is a specific and reversible inhibitor of dipeptidylpeptidase-4 (DPP-4), which inhibits the activity of the enzyme for at least 24 hours after one single oral administration. It increases the circulating levels of incretin hormones (GLP-1, GIP), which contributes to amplify the insulin secretory response to meals and to reduce postprandial hyperglycaemia and, subsequently, fasting glycaemia. Saxagliptin, 5 mg once daily, has been shown to be effective in patients with type 2 diabetes treated with diet alone, metformin, sulfonylurea or glitazone, with a favourable tolerance profile. Reduction in glycated haemoglobin (HbA(1c)) averaged 0.6-0.8%, without increasing the risk of hypoglycaemia or promoting weight gain. The only indication of saxagliptin that is currently reimbursed in Belgium is the treatment of patients not controlled with metformin, the oral antidiabetic agent that is recommended as first line therapy in the management of type 2 diabetes. [less ▲]

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See detailLe medicament du mois. Sitagliptine (Januvia): incretinopotentiateur indique comme insulinosecretagogue dans le traitement du diabete de type 2.
Scheen, André ULg; Van Gaal, L. F.

in Revue Médicale de Liège (2008), 63(2), 105-9

Sitagliptin (Januvia) is the first selective antagonist of dipeptidylpeptidase-4, an enzyme that degrades glucagon-like peptide-1 (GLP-1). This hormone is mainly secreted by ileal L cells and this ... [more ▼]

Sitagliptin (Januvia) is the first selective antagonist of dipeptidylpeptidase-4, an enzyme that degrades glucagon-like peptide-1 (GLP-1). This hormone is mainly secreted by ileal L cells and this secretion is abnormally low in patients with type 2 diabetes. Sitagliptin increases post-meal insulin secretion ("incretin effect) by enhancing the postprandial GLP-1 response ("incretin enhancer"), in a glucose-dependent manner. It improves glycaemic control (HbA1c) in type 2 diabetic patients treated by diet alone, by metformin, by sulfonylurea, by glitazone or by a metformin-sufonylurea combined therapy. The glucose-lowering effect is similar to that of glipizide, but with the advantage of no weight gain and no hypoglycaemic episodes. The tolerance to sitagliptin is excellent. Treatment is simple, with 100 mg once daily, without need of titration or home blood glucose monitoring. In Belgium, sitagliptin is currently reimbursed in patients with type 2 diabetes not adequately controlled with diet and metformin monotherapy. [less ▲]

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See detailLe medicament du mois. Valdecoxib (Bextra)
Scheen, André ULg; Malaise, Michel ULg

in Revue Médicale de Liège (2004), 59(4), 251-254

Valdecoxib (Bextra tablets of 10 mg and 20 mg) is a new non steroidal antiinflammatory drug (NSAID) that selectively inhibits COX-2 isoform of cyclo-oxygenase. It is indicated for the symptomatic ... [more ▼]

Valdecoxib (Bextra tablets of 10 mg and 20 mg) is a new non steroidal antiinflammatory drug (NSAID) that selectively inhibits COX-2 isoform of cyclo-oxygenase. It is indicated for the symptomatic treatment of osteoarthritis or rheumatoid arthritis (10 to 20 mg once a day) and for the treatment of primary dysmenorrhea (40 mg once a day). Valdecoxib is as efficacious as conventional non-COX-2 selective NSAIDs, but offers the advantage of a much better gastrointestinal tolerance. Valdecoxib has a prodrug that can be administered intravenously or intramuscularly (parecoxib, Dynastat) and has been developed for the short-term treatment of postsurgical pain. [less ▲]

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See detailLe medicament du mois. Vildagliptine (Galvus) et combinaison fixe vildagliptine-metformine (Eucreas) dans le traitement du diabete de type 2.
Scheen, André ULg; Paquot, Nicolas ULg

in Revue Médicale de Liège (2009), 64(3), 161-7

Vildagliptin (Galvus) is a selective inhibitor of dipeptidylpeptidase-4, an enzyme involved in the metabolism of glucagon-like peptide-1 (GLP-1) secreted by L cells of the intestine. It potentiates the ... [more ▼]

Vildagliptin (Galvus) is a selective inhibitor of dipeptidylpeptidase-4, an enzyme involved in the metabolism of glucagon-like peptide-1 (GLP-1) secreted by L cells of the intestine. It potentiates the insulin secretory response (incretin effect) by enhancing the endogenous post-prandial response of GLP-1 (incretin enhancer) in a glucose-dependent manner. Vildagliptin is indicated in the treatment of type 2 diabetes. It improves blood glucose control (HbA1c) in patients treated by diet alone, metformin, sulfonylurea, glitazone or insulin. In patients not well controlled with metformin alone, the addition of vildagliptin is as effective in reducing HbA1c as the coadministration of glimepiride or pioglitazone. Tolerance of vildagliptin is excellent, with no weight gain and no hypoglycaemic episodes. Treatment is simple, with two doses of 50 mg per day, without need of titration or home blood glucose monitoring. In Belgium, vildagliptin is currently reimbursed for the treatment of type 2 diabetes after diet failure and monotherapy with metformin. Therapy can be administered separately or by using a fixed combination vildagliptin-metformin (Eucreas), which should improve drug compliance. [less ▲]

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See detailLe medicament du mois: Linagliptine (Trajenta): un inhibiteur selectif de la DPP-4 a elimination renale negligeable.
SCHEEN, André ULg; Van Gaal, L. F.

in Revue Médicale de Liège (2012), 67(2), 91-7

Linagliptin (Trajenta) is a selective inhibitor of dipeptidyl peptidase-4, an enzyme that degrades two incretin hormones, GLP-1 ("Glucagon-Like Peptide-1") and GIP ("Glucose-dependent Insulinotropic ... [more ▼]

Linagliptin (Trajenta) is a selective inhibitor of dipeptidyl peptidase-4, an enzyme that degrades two incretin hormones, GLP-1 ("Glucagon-Like Peptide-1") and GIP ("Glucose-dependent Insulinotropic Polypeptide"). As other molecules belonging to this pharmacological class, linagliptin improves blood glucose control of type 2 diabetic patients, without increasing hypoglycaemic risk, without promoting weight gain and with a good clinical and biological tolerance profile. Both efficacy and safety have been demonstrated in randomized controlled trials as monotherapy or in combination with other glucose-lowering agents, independent of demographic or clinical patient's characteristics. The pharmacokinetics specificity of linagliptin comprises its biliary excretion, with low hepatic metabolism (no drug-drug interactions) and, in contrast to other gliptins, its negligible renal elimination. Because of these favourable properties, linagliptin may be used without dose adjustment (5 mg once a day) in patients with renal impairment, as well as in elderly people. [less ▲]

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See detailLe medicament du mois: Olmesartan medoxomil (Belsar ou Olmetec)
Krzesinski, Jean-Marie ULg; Scheen, André ULg

in Revue Médicale de Liège (2004), 59(10), 607-611

Olmesartan medoxomil (Belsar, Olmetec) developed by Sankyo Pharma and proposed by Sankyo Pharma but also Menarini is a new angiotensin II ATI receptor blocker. Its indication is the treatment of ... [more ▼]

Olmesartan medoxomil (Belsar, Olmetec) developed by Sankyo Pharma and proposed by Sankyo Pharma but also Menarini is a new angiotensin II ATI receptor blocker. Its indication is the treatment of hypertension. Olmesartan is indeed an antihypertensive agent with an efficacy dependent on the dose from 10 to 40 mg. It is taken once a day, because of a long duration of action. This prodrug has a dual elimination pathway (biliary and renal). The contraindications are the same as for the other sartans. One of its main advantage, besides its rapidly observed efficacy to lower high blood pressure, is its relatively low cost within this family. It has also cardiovascular and renal protective effects. The recommended usual dosage is 20 mg/day. [less ▲]

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See detailLe médicament parmi les thérapies relationnelles : Enquête et réflexions.
David, Claire; WAUTHY, Jacques ULg; Vaulet, Véronique et al

in Revue des Hôpitaux de Jour Psychiatriques et des Thérapies Institutionnelles (2001)

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See detailLe médicament, la fourrure et le bâti. Le castor et ses modes d'existence
Strivay, Lucienne ULg

Article for general public (2011)

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See detailMédicaments anti-asthmatiques. De la pharmacologie à la clinique
Louis, Renaud ULg; Radermecker, Maurice ULg

in Revue Médicale de Liège (1991), 46(2), 58-81

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