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See detailLe medicament du mois : Preterax, la premiere association fixe faiblement dosee contenant un inhibiteur d'enzyme de conversion et un diuretique thiazide
Krzesinski, Jean-Marie ULg

in Revue Médicale de Liège (2004), 59(10), 601-606

Preterax is the first fixed very- low - dose combination of an angiotensin--converting enzyme inhibitor and a diuretic for first line treatment of hypertension. Its antihypertensive efficacy is remarkable ... [more ▼]

Preterax is the first fixed very- low - dose combination of an angiotensin--converting enzyme inhibitor and a diuretic for first line treatment of hypertension. Its antihypertensive efficacy is remarkable due to the presence of 2 drugs with additional effects. The tolerance is also excellent, with adverse effects similar to placebo. The 24 h blood pressure control is maintained. If necessary, the dose can be doubled (BiPreterax). The medical practitioner must keep in mind that it is an association of perindopril 2 mg and indapamide 0.625 mg with their own contra-indications. These low dose associations are now recommended as one of the 2 options to initiate an antihypertensive drug treatment, with the hope of an improvement in the percentage of well controlled blood pressure in the hypertensive population. Let us remember that the blood pressure target to be reached is at least < 140/90 mmHg. Up till now, no antihypertensive class has demonstrated a superiority over the others. Only the blood pressure fall magnitude is important to prevent cardiovascular complications. [less ▲]

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See detailLe Medicament du mois empagliflozine (Jardiance): nouvel inhibiteur des cotransporteurs rnaux SGLT2 comme traitement du diabete de type 2.
Scheen, Andre ULg

in Revue medicale de Liege (2015), 70(9), 472-9

Empagliflozin is a new inhibitor of sodiumglucose cotransporters type 2 (SGLT2) for the treatment of type 2 diabetes mellitus (T2DM). Its specific action inhibits glucose reabsorption in renal tubules and ... [more ▼]

Empagliflozin is a new inhibitor of sodiumglucose cotransporters type 2 (SGLT2) for the treatment of type 2 diabetes mellitus (T2DM). Its specific action inhibits glucose reabsorption in renal tubules and thus promotes glucosuria. This effect results in a reduction in fasting and postprandial glycaemia and a decrease of glycated haemoglobin (HbA(Ic)), independently of insulin. Furthermore, calorie urinary loss promotes weight reduction and osmotic diuresis lowers arterial blood pressure. The efficacy of empagliflozin increases according to the level of hyperglycaemia but decreases in patients with renal insufficiency. In 24 to 104-week controlled trials versus placebo, empagliflozin reduces HbA(1c) (approximately 0.8%), without hypoglycaemia (except in patients already treated with insulin or sulphonylureas). This improvement in glucose control is rather similar to that observed with active comparators (metformin, glimepiride or sitagliptin), with the advantage for empagliflozin of reducing body weight (approximately 2 kg) and blood pressure (systolic approximately 4 mm Hg and diastolic approximately 2 mm Hg). Empagliflozin has shown a cardiovascular protection in the EMPA-REG OUTCOME trial. Mycotic genital infections occur more frequently, especially in women, while a negligible increase in mild urinary tract infections may be observed. The risk of hypotension and volume depletion is low, although it should be carefully checked in more fragile and at risk patients. Empagliflozin (Jardiance), which is commercialized at the doses of 10 mg and 25 mg once daily, is indicated for the treatment of T2DM and reimbursed in Belgium with conditions as add-on to a background glucose-lowering therapy. [less ▲]

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See detailLE MÉDICAMENT DU MOIS La dapoxétine (Priligy®) : médicament à la demande pour le traitement de l’éjaculation prématurée
Andrianne, Robert ULg

in Revue Médicale de Liège (2013), 68(12), 663-668

L’éjaculation précoce (EP) est le dysfonctionnement sexuel masculin le plus fréquent; elle affecte environ 20-24 % des hommes. La prise en charge de l’EP est un défi pour les médecins et psycho-sexologues ... [more ▼]

L’éjaculation précoce (EP) est le dysfonctionnement sexuel masculin le plus fréquent; elle affecte environ 20-24 % des hommes. La prise en charge de l’EP est un défi pour les médecins et psycho-sexologues car aucun médicament n’est approuvé par les agences du médicament européenne (EMA) ou américaine (FDA). Au cours de la dernière décennie, des preuves cliniques indiquent un effet bénéfique des inhibiteurs sélectifs de la recapture de la sérotonine (ISRS), du tramadol, de l’anesthésie du pénis et, dans certains cas, des inhibiteurs de la phosphodiestérase (type 5) pour le traitement des hommes souffrant d’EP. Une prise en charge psycho-sexologique aide à la guérison. En dépit de leur efficacité, les effets indésirables sont la préoccupation majeure pour l’utilisation chronique des ISRS chez les patients avec EP et ils peuvent inciter l’arrêt de la thérapie. La dapoxétine, commercialisée sous le nom de Priligy®, est le premier médicament spécialement développé pour le traitement de l’EP, avec prise à la demande avant les rapports sexuels. La dapoxétine agit en inhibant le transporteur de la sérotonine, ce qui augmente l’action de la sérotonine au sein de la fente synaptique et, par conséquent, induit le retard de l’éjaculation. La dapoxétine est vite absorbée et éliminée rapidement de l’organisme. Grâce à son action rapide, le Priligy® convient pour le traitement de l’EP à la demande. [less ▲]

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See detailLe médicament du mois Le voriconazole (Vfend).
Pierard, Gérald ULg; Arrese Estrada, Jorge ULg; Quatresooz, Pascale ULg et al

in Revue Médicale de Liège (2003), 58(5), 351-5

Invasive fungal infections are a rare but important cause of morbidity and mortality among patients with severely compromised host defenses. Despite considerable advances in antifungal therapies over the ... [more ▼]

Invasive fungal infections are a rare but important cause of morbidity and mortality among patients with severely compromised host defenses. Despite considerable advances in antifungal therapies over the past years, invasive mycoses remain a stubborn and dramatic problem. Voriconazole is a new triazole antifungal agent which confers a relative survival benefit in fluconazole-resistant invasive candidiasis, and in invasive aspergillosis, fusariosis and Scedosporium infections as well. [less ▲]

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See detailLe médicament du mois, EXFORGE® : première association d'un antagoniste calcique (bésylate d’amlodipine) et d'un inhibiteur des récepteurs de l'angiotensine II (valsartan)
Krzesinski, Jean-Marie ULg; Scheen, André ULg

in Revue Médicale de Liège (2007), 62

Hypertension is a common treatable risk factor for cardiovascular disease. Even when identified and treated, most patients with hypertension do not get to blood pressure goal and they often need at least ... [more ▼]

Hypertension is a common treatable risk factor for cardiovascular disease. Even when identified and treated, most patients with hypertension do not get to blood pressure goal and they often need at least two antihypertensive agents to achieve blood pressure control. Although various combination therapies are currently available for the treatment of hypertension, development of more powerful therapies is necessary to help implement guideline recommendations that call for more aggressive treatment options and early blood pressure control. Amlodipine/valsartan (Exforge®) is a new combination of antihypertensive agents that lower blood pressure via calcium channel blockade and angiotensin receptor antagonism. This potent dual mechanism of action is also likely to attenuate compound-specific adverse events, such as amlodipine-related peripheral oedema. Currently available data show that such a combination is a well-tolerated treatment that gets different kinds of patients with all grades of hypertension to their blood pressure goal. [less ▲]

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See detailLe médicament du mois, SEVIKAR/HCT° : association d'un antagoniste calcique (bésylate d'amlodipine), d'un inhibiteur des récepteurs de l'angiotensine II (olmésartan médoxomil) et d'un diurétique thiazide (hydrochlorothiazide)
Krzesinski, Jean-Marie ULg

in Revue Médicale de Liège (2011), 66(12), 636-642

Hypertension is a common treatable risk factor for cardiovascular disease. Even when identified and treated, most patients with hypertension do not reach the blood pressure goal and they often need in ... [more ▼]

Hypertension is a common treatable risk factor for cardiovascular disease. Even when identified and treated, most patients with hypertension do not reach the blood pressure goal and they often need in fact three antihypertensive agents to achieve blood pressure control. Although various combinations of two therapies are currently available for the treatment of hypertension, development of more powerful therapies with 3 molecules is necessary to control more hypertensive patients. Amlodipine/Olmesartan/hydrochlorothiazide (Sevikar/HCT°) is a new triple combination of antihypertensive agents that lower blood pressure via calcium channel blockade, angiotensin receptor blockade and diuretic action. Its potent triple mechanism of action is also likely to attenuate compound-specific adverse events, such as amlodipine-related peripheral oedema or sartan-induced hyperkalemia. Moreover, by reducing the number of pills to be taken every day, the compliance should be better. Currently available data show that such a combination is very powerful and well-tolerated allowing more patients with all grades of hypertension (especially those with the most severe forms) to reach the blood pressure target. The contraindications are those of each compound. [less ▲]

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See detailLe medicament du mois. Bydureon: premier agoniste des recepteurs du GLP-1 en une injection hebdomadaire (exenatide a liberation prolongee).
Scheen, André ULg

in Revue medicale de Liege (2014), 69(4), 214-9

Bydureon is a new galenic formulation (long-acting release) of exenatide, the first agonist of Glucagon-Like Peptide-1 (GLP-1) receptors having been commercialized for the management of type 2 diabetes ... [more ▼]

Bydureon is a new galenic formulation (long-acting release) of exenatide, the first agonist of Glucagon-Like Peptide-1 (GLP-1) receptors having been commercialized for the management of type 2 diabetes. The microsphere technology permits a prolonged absorption of exenatide from the subcutaneous depot, which allows one injection per week instead of two injections per day with the initial formulation of exenatide (Byetta). The clinical development programme DURATION showed that exenatide 2 mg once weekly more markedly reduces glycated haemoglobin (HbA(1c)), with a similar weight loss but a better digestive tolerance profile (less nausea and vomiting after treatment initiation), compared with the twice daily 10 microg exenatide. When compared to other glucose-lowering agents, once weekly exenatide is more efficacious than sitagliptin, pioglitazone or basal insulin (glargine or detemir), with the advantage of producing weight loss and lowering arterial blood pressure. It does not induce hypoglycaemia and does not necessarily require home blood glucose monitoring, two advantages compared with insulin therapy. Bydureon is currently only reimbursed in Belgium after failure of and in addition to metformin-sulfonylurea combination. [less ▲]

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See detailLe medicament du mois. Combinaison fixe ezetimibe/simvastatine (Inegy).
Scheen, André ULg; Radermecker, Régis ULg

in Revue Médicale de Liège (2007), 62(9), 585-90

Inegy, recently launched by Merck Sharp & Dohme and Schering Plough, is a fixed combination of simvastatin, which inhibits hepatic cholesterol synthesis, and ezetimibe, which selectively inhibits the ... [more ▼]

Inegy, recently launched by Merck Sharp & Dohme and Schering Plough, is a fixed combination of simvastatin, which inhibits hepatic cholesterol synthesis, and ezetimibe, which selectively inhibits the intestinal absorption of cholesterol and phytosterols. The two mechanisms of action are complementary and result in a synergistic cholesterol-lowering effect. Three formulations of Inegy are commercialized and reimbursed in Belgium, ezetimibe 10 mg/simvastatin 20 mg, ezetimibe 10 mg/simvastatin 40 mg and ezetimibe 10 mg/ simvastatin 80 mg. By blocking both synthesis and absorption of cholesterol, the fixed combination exerts a cholesterol-lowering effect as important as, or even greater than, that observed with the highest dosage of simvastatin and other statins, with a good tolerance profile. Inegy is indicated, as adjuvant treatment to diet, in patients with primary hypercholesterolaemia (homozygote or heterozygote familial form and non-familial polygenic form) not well controlled with a statin alone. Ongoing trials aim at proving the efficacy of such a fixed combination in reducing cardiovascular morbidity and mortality. [less ▲]

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See detailLe medicament du mois. Etoricoxib (Arcoxia)
Leclercq, P.; Malaise, Michel ULg

in Revue Médicale de Liège (2004), 59(5), 345-349

Etoricoxib (Arcoxia) is a novel non steroidal anti-inflammatory drug (NSAID) that selectively inhibits the inducible form of cyclo-oxygenase (COX), COX-2. Etoricoxib has a higher COX-1/COX-2 selectivity ... [more ▼]

Etoricoxib (Arcoxia) is a novel non steroidal anti-inflammatory drug (NSAID) that selectively inhibits the inducible form of cyclo-oxygenase (COX), COX-2. Etoricoxib has a higher COX-1/COX-2 selectivity ratio than the other COX-2-selective NSAIDs as rofecoxib, valdecoxib or celecoxib. Tablets of 60, 90 and 120 mg are available. The recommended dosage of etoricoxib is 60 mg/day for osteoarthritis, 90 mg/day for rheumatoid arthritis and 120 mg/day for acute gouty arthritis. Etoricoxib's efficacy has been widely studied in comparative studies, showing the same efficacy as non-COX-2 selective NSAID, with fewer gastro-intestinal adverse effects. [less ▲]

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See detailLe medicament du mois. Everolimus (RAD001/Afinitor) dans le traitement du cancer du rein métastatique.
Gennigens, Christine ULg; Sautois, Brieuc ULg; Jerusalem, Guy ULg

in Revue Médicale de Liège (2010), 65(4), 212-6

Renal cell carcinoma accounts for 3% of all malignant tumours. Until a few years ago, immunotherapy (interferon and/or interleukin-2) was the only approved option in the metastatic setting. Better ... [more ▼]

Renal cell carcinoma accounts for 3% of all malignant tumours. Until a few years ago, immunotherapy (interferon and/or interleukin-2) was the only approved option in the metastatic setting. Better knowledge of renal cell cancer biology drew attention on the fundamental role of angiogenesis. Several strategies targeting angiogenesis have been developed including VEGF ("Vascular Endothelial Growth Factor") and VEGFR inhibitors. They are now the usual treatment in first line. Until recently, no standard treatment was available after failure under or after these inhibitors. Everolimus (Afinitor), a mTOR ("mammalian Target Of Rapamycin") inhibitor, has just been validated and reimbursed in this setting. In this paper, we will review the mechanism of action and the clinical results of everolimus. [less ▲]

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See detailLe medicament du mois. Exenatide (Byetta). Incretinomimetique indique dans le traitement du diabete de type 2 apres echec et en complement des antidiabetiques oraux.
Scheen, André ULg; Van Gaal, L. F.

in Revue Médicale de Liège (2008), 63(3), 158-65

Exenatide (Byetta) is a synthetic derivative of exendin-4 and an agonist of receptors of glucagon-like peptide-1 (GLP-1). It is resistant to the rapid inactivation by dipeptidylpeptidase-4 and acts as an ... [more ▼]

Exenatide (Byetta) is a synthetic derivative of exendin-4 and an agonist of receptors of glucagon-like peptide-1 (GLP-1). It is resistant to the rapid inactivation by dipeptidylpeptidase-4 and acts as an incretin mimetic. It stimulates insulin secretion by the B cell in a glucose-dependent manner whereas it inhibits glucagon secretion. Exenatide improves mainly postprandial glucose concentrations and lowers glycated haemoglobin (HbA(1c)) levels, without being directly responsible for hypoglycaemia or requiring mandatory home blood glucose monitoring. Furthermore, it slows down gastric emptying and promotes sustained body weight reduction, even in absence of frequently reported nausea following treatment initiation. Exenatide is recommended and reimbursed in Belgium for the treatment of type 2 diabetes, in combination with metformin and a sulfonylurea, in patients not adequately controlled with maximal tolerated doses of these oral glucose-lowering agents. Exenatide is presented as pre-filled pens for subcutaneous injection. The recommended initial dose is 5 microg before morning and evening meals, to be up titrated to 10 microg twice daily. Exenatide may represent a valuable alternative to insulin therapy, especially in overweight or obese patients with type 2 diabetes and not ready to perform home blood glucose monitoring. [less ▲]

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See detailLe medicament du mois. Exforge HCT: premiere association fixe d'un antagoniste calcique (besylate d'amlodipine), d'un inhibiteur des recepteurs de l'angiotensine II (valsartan) et d'un diuretique (hydrochlorothiazide).
LANCELLOTTI, Patrizio ULg

in Revue Médicale de Liège (2010), 65(7-8), 471-5

Because of the multifactorial nature of hypertension, most patients require combination therapy to achieve blood pressure control. Very often the antihypertensive regimen includes a renin-angiotensin ... [more ▼]

Because of the multifactorial nature of hypertension, most patients require combination therapy to achieve blood pressure control. Very often the antihypertensive regimen includes a renin-angiotensin system blocker, a calcium channel blocker, and a diuretic. Currently, several associations combining two antihypertensive agents with complementary mechanisms of action are available. These combination therapies are more efficient to control blood pressure through synergistic and additive effects, can reach target blood pressure more quickly, are likely to attenuate the side effects of each molecule, and could improve patient adherence. Exforge HCT is the first fixed-dose combination of three antihypertensive drugs including amlodipine besylate, valsartan and hydrochlorothiazide (HCTZ) in a single pill. The association of these three drugs improves, with an equal tolerance, blood pressure control compared to dual therapies (valsartan/HCTZ, amlodipine/valsartan, or HCTZ/amlodipine). This triple therapy attenuates the diuretic-induced hypokalemia. The benefits of triple therapy over dual therapy are observed regardless of age, sex, race, ethnicity, or baseline mean sitting systolic blood pressure. Exforge HCT is currently indicated for the treatment of essential hypertension, as replacement therapy for adult patients whose blood pressure is adequately controlled by the combination of amlodipine, valsartan and HCTZ. [less ▲]

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See detailLe medicament du mois. Ezetimibe (Ezetrol).
Scheen, André ULg

in Revue Médicale de Liège (2004), 59(4), 246-50

Ezetimibe (Ezetrol), recently launched in Belgium by Merck Sharp& Dohme and Schering Plough, is presented as 10 mg tablets. It belongs to a new class of lipid-lowering agents that selectively inhibit the ... [more ▼]

Ezetimibe (Ezetrol), recently launched in Belgium by Merck Sharp& Dohme and Schering Plough, is presented as 10 mg tablets. It belongs to a new class of lipid-lowering agents that selectively inhibit the intestinal absorption of cholesterol and phytosterols. Its mechanism of action results in a synergistic cholesterol-lowering effect together with a statin that inhibits cholesterol synthesis by the liver. Ezetimibe, at a daily dose of 10 mg, is indicated, in combination with a statin, as adjuvant treatment to diet in patients with primary hypercholesterolaemia (homozygote or heterozygote familial form and non-familial polygenic form) not well controlled with a statin alone. In case of statin contra-indication or intolerance, ezetimibe can be used in monotherapy. Its tolerance profile is excellent. Statin-ezetimibe combination allows to significantly reduce total and LDL cholesterol levels and increases the percentage of hypercholesterolaemic patients who will reach the target levels recommended in the international guidelines against atherosclerosis. However, such a combination should still prove its efficacy in reducing cardiovascular morbidity and mortality in large prospective clinical trials. [less ▲]

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See detailLe medicament du mois. Femoston Low (0,5 mg d'estradiol plus 2,5 mg de dydrogesterone) comme traitement hormonal de substitution a la menopause.
SCHEEN, André ULg; Gaspard, Ulysse ULg

in Revue Médicale de Liège (2011), 66(4), 209-14

Femoston Low is a hormone replacement therapy that combines low dosages of steroids, i.e. 0.5 mg of estradiol and 2.5 mg of dydrogesterone. This oral preparation should be taken continuously to treat ... [more ▼]

Femoston Low is a hormone replacement therapy that combines low dosages of steroids, i.e. 0.5 mg of estradiol and 2.5 mg of dydrogesterone. This oral preparation should be taken continuously to treat climacteric symptoms in menopausal women. Femoston Low is in agreement with the recent recommendations for menopausal hormone replacement therapy, which give the preference to low dosage therapy whenever possible. The goals are to potentially minimize the risk of breast cancer, the danger of venous or arterial thrombosis and the glucose and lipid metabolic disturbances. Nevertheless, the preparation should efficaciously oppose to endometrial hyperplasia and yield a high degree of amenorrhea. [less ▲]

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See detailLe medicament du mois. Gliclazide a liberation modifiee (Uni Diamicron).
Scheen, André ULg

in Revue Médicale de Liège (2003), 58(10), 641-5

Gliclazide modified release that has been recently launched by Servier (Uni Diamicron 30 mg) is a new formulation of gliclazide to be given once daily. The original hydrophilic matrix improves the ... [more ▼]

Gliclazide modified release that has been recently launched by Servier (Uni Diamicron 30 mg) is a new formulation of gliclazide to be given once daily. The original hydrophilic matrix improves the biodisponsibility of gliclazide and allows a progressive release of the drug that better parallels the 24-hour glycaemic profile of patients with type 2 diabetes mellitus. Such characteristics may explain the rather low risk of hypoglycaemic episodes and the morning administration should contribute to improve patient's compliance. As the common formulation of gliclazide, the modified release formulation is indicated in the treatment of type 2 diabetes, in adult subjects, when diet, exercise and weight loss are insufficient to restore an adequate metabolic control. It may be used alone or in combination with metformin, glitazones, acarbose or insulin, with the same general principles of use as for the classical formulation of gliclazide. [less ▲]

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See detailLe medicament du mois. Glucovance dans le diabete de type 2, une association fixe metformine-glibenclamide pour faciliter le traitement d'une maladie bipolaire.
Scheen, André ULg

in Revue Médicale de Liège (2003), 58(6), 448-52

Glucovance, recently launched by Merck-Lipha (Glucovance 500 mg/2.5 mg and Glucovance 500 mg/5 mg), is a fixed combined therapy of a sulphonylurea (glibenclamide 2.5 or 5 mg) and a biguanide (metformin ... [more ▼]

Glucovance, recently launched by Merck-Lipha (Glucovance 500 mg/2.5 mg and Glucovance 500 mg/5 mg), is a fixed combined therapy of a sulphonylurea (glibenclamide 2.5 or 5 mg) and a biguanide (metformin 500 mg), indicated for the treatment of type 2 diabetes in adult patients. The only current official indication in Belgium is the substitution of a dual therapy with metformin and glibenclamide in patients with a stable and adequate metabolic control. The fixed combination aims at simplifying patient's treatment in order to improve compliance despite polymedication. In addition, it allows targeting synergistically the two main abnormalities of type 2 diabetes, i.e. the insulin secretory defect and the insulin resistance. [less ▲]

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See detailLe médicament du mois. Humalog® 200 U/ml KwikPenTM
SCHEEN, André ULg

in Revue Médicale de Liège (2015), 70

Summary : Insulin lispro (Humalog®) was the first short-acting insulin analogue to be indicated for the treatment of diabetes mellitus requiring insulin therapy. After subcutaneous injection, insulin ... [more ▼]

Summary : Insulin lispro (Humalog®) was the first short-acting insulin analogue to be indicated for the treatment of diabetes mellitus requiring insulin therapy. After subcutaneous injection, insulin lispro has a more favourable pharmacokinetics/pharmacodynamics profile than human insulin, characterized by a faster resorption and a more rapid and less prolonged glucose-lowering activity. These properties allow a better control of postprandial hyperglycaemia and a reduction of the risk of delayed hypoglycaemia, especially at night. The patient’s quality of life is also improved because insulin lispro can be injected within the 15 minutes before meal and even possibly after meal when the amount of food intake is unpredictable. Already commercialized as Humalog® 100 U/ml, insulin lispro is now also available as Humalog® 200 U/ml. A pharmacokinetics/pharmacodynamics study confirmed the bioequivalence of the two formulations, based upon the analysis of both plasma free insulin concentrations and glucose infusion rates to maintain normoglycaemia. Humalog® 200 U/ml is available in a novel disposable 3 ml pen (KwikPenTM), with lower glide force and injection volume; thus this new pen is more convenient for the patient compared with the current pen used to inject Humalog® 100 U/ml. The new formulation Humalog® 200 U/ml is indicated in Europe for adult patients with type 1 or type 2 diabetes who require more than 20 units of prandial insulin per day to cover their meals. [less ▲]

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See detailLe medicament du mois. Insuline glargine (Lantus).
Scheen, André ULg

in Revue Médicale de Liège (2004), 59(2), 110-4

Insulin glargine (Lantus) is a human insulin analogue produced by recombinant DNA technology and recently launched by Aventis. Modification of the human insulin molecule at position A21 and at the C ... [more ▼]

Insulin glargine (Lantus) is a human insulin analogue produced by recombinant DNA technology and recently launched by Aventis. Modification of the human insulin molecule at position A21 and at the C-terminus of the B-chain results in the formation of a stable compound that is soluble at pH 4.0, but forms amorphous microprecipitates in subcutaneous tissue (pH > 7,4) from which small amounts of insulin glargine are gradually released. The plasma concentration versus time profile of insulin glargine is therefore relatively constant over 24 hours as compared to conventional human insulins, especially NPH. This allows once-daily injection as basal insulin therapy, at any moment of the clock time (but if possible at the same time from day to day). Reproducibility of plasma insulin levels is also improved with insulin glargine as compared to human NPH insulin. Insulin glargine administration should be combined to rapid insulin injections, before each meal in order to control postprandial hyperglycaemia, or with oral antidiabetic agents in type 2 diabetes. The pharmacokinetic properties of insulin glargine allow an easier titration of basal insulin dose, which should facilitate adequate blood glucose control while decreasing the risk of hypoglycaemia, especially during night time. Insulin glargine use is safe with no increased antigenicity, immunogenicity or mitogenicity reactions as compared to human insulin. Optimal use of this new insulin analogue should be integrated in a global management of the diabetic patient as well as in a new culture of insulin therapy. [less ▲]

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See detailLe médicament du mois. Insuline glargine 300 U/mL (Toujeo®)
SCHEEN, André ULg

in Revue Médicale de Liège (2016), 71

Summary : This article presents a new formulation of insulin glargine concentrated at 300 U/mL (Gla-300). It is commercialized under the trade name of Toujeo® in an optimized pre-filled SoloStar™ pen for ... [more ▼]

Summary : This article presents a new formulation of insulin glargine concentrated at 300 U/mL (Gla-300). It is commercialized under the trade name of Toujeo® in an optimized pre-filled SoloStar™ pen for the treatment of type 1 and type 2 diabetes in adults. Besides a threefold higher concentration compared to the classical insulin Lantus® (100 U/mL or Gla-100), both pharmacokinetic and pharmacodynamic profiles of Gla-300 are flatter and longer (more than 24 hours) and have a lesser intra-/inter-variability, which makes them more reproducible. Overall, Toujeo® offers the same hypoglycaemic efficacy and the same safety profile when compared with Lantus®. However, a lower risk of hypoglycaemia, especially at night, a slightly smaller weight gain and a better flexibility in the time of injection have been reported. The two insulin formulations are not bioequivalent and the daily insulin requirement is slightly higher with insulin Gla-300 than with insulin Gla-100. The shift from an already available basal insulin towards Toujeo® may require a dose adjustment and a reinforcement of blood glucose monitoring. [less ▲]

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