Synthèse et évaluation de l’activité pharmacologique de la 4-phényl-1,5- benzodiazépin-2-one et ses dérivés

La synthèse et l’étude de la réactivité de la 4-phényl-1,5-benzodiazépin-2-one nous a permis d’obtenir deux dérivés : la 4-phényl-1,3,4,5-tétrahydro-1,5-benzodiazépin-2-one et la 4-phényl-1,5-benzodiazépin-2-thiole. Ces produits ont fait l’objet d’une étude toxicologique et nous avons aussi exploré leur activité sur le système nerveux central, notamment l’action analgésique, grâce à un test spécifique. Après analyse de nos résultats, nous avons constaté que les composés testés s’avèrent atoxiques à des doses thérapeutiques, avec une DL50 supérieure à 1000 mg/kg par voie intrapéritonéale, et exercent une action analgésique modérée, surtout pour les composés 1 et 3 vis-à-vis de l’acide acétylsalicylique. Le produit 2 a une action analgésique moins importante.© 2010 International Formulae Group. All rights reserved.Mots clés : 1,5-benzodiazépine, synthèse, activités pharmacologiques, toxicité aiguë, activité analgésique

Pharmacological and chemical properties of some marine echinoderms

Echinoderms have attracted the attention of scientists over the past few years after identifying a variety of unique structures endowed by interesting biological properties. However, the Moroccan coast biodiversity is still uninvestigated. In our ongoing attempts to valorize the rich Moroccan marine environment, this study aimed at assessing the antimicrobial activity of extracts obtained from three echinoderms Astropecten irregularis, Luidia sarsi and Ophiura albida against the human pathogens: Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enterica and Bacillus subtilis. Moreover, their antioxidant activities were tested using standard methods in addition to the antidiabetic activity which has been evaluated in vitro against α-amylase and α-glucosidase enzymes. HPLC-DAD-QTOF-MS analysis revealed a significant content of some phenolic compounds such as pyrogallol, gallic, sinapic, ferulic, p-hydroxybenzoic and salicylic acids whose existence can be related to the endophytic fungi and/or dietary intake whereas GC-MS analysis exhibited diverse chemical structures such as cholesterol, oleic acid and glycerol 1-palmitate

The cost-utility of treating anemia with continuous erythropoietin receptor activator or Epoetin versus routine blood transfusions among chronic hemodialysis patients

Omar Maoujoud,1,2 Samir Ahid,1 Yahia Cherrah1 1Research Team of Pharmacoepidemiology and Pharmacoeconomics, Medical and Pharmacy School, Mohammed V University, Rabat, 2Department of Nephrology and Dialysis, Military Hospital, Agadir, Morocco Objective: The purpose of this study was to determine the cost-utility of treating anemic dialysis patients with continuous erythropoietin receptor activator (CERA) once monthly or Epoetin Beta (EpoB) thrice weekly compared with a reference strategy of managing anemia with red blood cell transfusion (RBCT).Methods: Cost-utility analysis study design. Decision analysis model, National health care payer, over 1 year with the publicly funded health care system. Chronic hemodialysis patients with renal anemia were included. The outcome marker of this study was the incremental cost per quality-adjusted life-year (QALY) gained (incremental cost-utility ratio [ICUR]) of CERA or EpoB relative to RBCT.Results: The total cost per patient (in US$) was estimated at$2,176.37, $4,107.01, and$4,356.69 for RBCT, CERA, and EpoB, respectively. The cost-utility ratio was calculated at 4,423.52, 6,955.50, and 7,406.38 $/QALY for RBCT, CERA, and EpoB, with an ICUR of CERA and EpoB in relation to RBCT at 19,606.40 and 22,466.09$/QALY, respectively. In sensitivity analysis, the model was most sensitive to hospitalization costs, hospital stay, and annual number of RBCT units. Also, assuming utility and survival improvement with erythropoiesis stimulating agents use resulted in a decrease in ICUR at 13,429 $/QALY for CERA and 15,331$/QALY for EpoB. In probabilistic sensitivity analysis, the main results of our model were unchanged; CERA and EpoB were more costly and more effective than RBCT below a threshold of 19,500 $/QALY. CERA was the best option for a willingness to pay over 19,500$/QALY.Limitations: Some model parameters were obtained from observational data, the comparator RBCT is not the standard of care.Conclusion: Our study suggests that managing anemia in dialysis patient with CERA or EpoB may results in better outcomes with higher overall costs. Considering different assumptions, we found substantial variability in the estimates of the cost-utility and incremental of using CERA or EpoB. Keywords: cost-utility, cost-effectiveness, anemia, dialysis, erythropoiesis stimulating agents, continuous erythropoietin receptor activator, epoeti