A randomized double-blind study comparing the efficacy and safety of orlistat versus placebo in obese patients with mild to moderate hypercholesterolemia.

INTRODUCTION: Obesity is a chronic disease and a serious health problem that leads to increased prevalence of diabetes, hypertension, dyslipidemia and gallbladder disease. OBJECTIVE: To evaluate the efficacy of orlistat for weight loss and improved lipid profile compared to placebo in obese patients with hypercholesterolemia, treated over a period of 6 months. METHODOLOGY: In a 6-month, multicenter (10 centers in Portugal), double-blind, parallel, placebo-controlled study, 166 patients, aged 18-65 years, body mass index (BMI) > or = 27 kg/m2, LDL cholesterol > 155 mg/dl, were randomized to a reduced calorie diet (600 kcal/day deficit) plus orlistat three times a day or placebo. Exclusion criteria included triglycerides > 400 mg/dl, severe cardiovascular disease, uncontrolled hypertension, type 1 or 2 diabetes under pharmacological treatment, and gastrointestinal or pancreatic disease. RESULTS: The mean difference in weight from baseline was 5.9% (5.6 kg) in the orlistat group vs. 2.3% (2.2 kg) in the placebo group. In the orlistat group 49% of patients achieved 5-10% weight loss and 8.8% achieved > 10%. The orlistat group showed a significant reduction in total and LDL cholesterol, with similar changes for HDL in both treatment groups. The frequency of gastrointestinal adverse events was slightly higher in the orlistat group than in the placebo group, leading to discontinuation in 7 patients. CONCLUSION: Treatment with orlistat plus a reduced calorie diet for 6 months achieved significant reductions in weight, BMI and lipid parameters.

Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials.

Imidazolidin-4-one derivatives of primaquine were synthesized as potential double prodrugs of the parent drug. The title compounds inhibit the development of the sporogonic cycle of Plasmodium berghei, affecting the appearance of oocysts in the midguts of the mosquitoes. The imidazolidin-4-ones are very stable, both in human plasma and in pH 7.4 buffer, indicating that they are active per se. Thus, imidazolidin-4-ones derived from 8-aminoquinolines represent a new entry in antimalarial structure-activity relationships.

[Characterization of patients with type 2 diabetes treated with vildagliptin]. / Caracterização de doentes com diabetes mellitus tipo 2 medicados com vildagliptina.

INTRODUCTION: Diabetes mellitus is a progressive disease and the rapid growth of this global prevalence has been a worldwide concern. About a third of Portuguese population has type 2 diabetes or pre-diabetes. 2 DM is associated with significant morbidity and mortality, although the treatment so far available it is a high percentage of patients who do not achieve the proposed objectives. Vildagliptin is an inhibitor of oral DPP-4, the most studied of this new class. Inhibiting the rapid degradation of incretins, the vildagliptin increases levels of GLP-1, getting this hormone available to modulate the function of a and ß cells. AIMS: This study aims to characterize the first patients with DM2 treated with vildagliptin in the Department of Endocrinology, Diabetes and Metabolism at the Military Hospital. METHODS: Retrospective study with the first 70 patients treated with vildagliptin, between October and December 2008. The information collected was demographic data, disease duration, associated diseases and their medication, metabolic control in the beginning of the disease (values HbA1c) and criteria for use of vildagliptin. RESULTS: Among the patients included in the study, 55, 7% were male, with the average age of 63, 3 years. These patients had a average duration of diabetes of 11, 7 years. Hypertension was the most frequent associated pathology (85.7% of patients), although dyslipidemia and obesity have a high percentage, 80% and 51% respectively. All patients were overweight (BMI =25 Kg/m(2)). More than half of the patients (55,7%) were on monotherapy until the introduction of vildagliptin, having been associated with other oral antidiabetic agents in all patients. CONCLUSIONS: Most of patients showed risk factors, for witch they were medicated. Vildagliptin has been added mostly in patients medicated with metformin. It is suggested that the therapeutic approach in type 2 diabetes is more and more early, effective and secure.

[Quality of care in diabetic outpatient clinics]. / Avaliação da qualidade de cuidados numa consulta de diabetes.

UNLABELLED: Type 2 Diabetes Mellitus affects an increasing number of people throughout the world. Several studies have shown that it is possible to prevent and minimize type 2 diabetes complications, be it treated appropriately over time. This study aimed to determine the quality of care provided to type 2 diabetic patients in our institution, through metabolic control and risk factors evaluation. SUBJECTS AND METHODS: We reviewed the medical records of 776 type 2 diabetic patients, followed at our outpatient clinic between 1998-2004. RESULTS: A total of 588 patients were included in the study, with a mean age of 66,8 ± 27,2 years. 58% were men. HbA1c levels averaged 7,2 ± 1,6. 57% had HbA1c = 7%. 25,3% met the target blood pressure of 130/80 mmHg; 48% met the goal LDL cholesterol level < 100 and 80% < 130 mg/dl. 6,8% of patients met the combined ADA goal for BP, LDL and HbA1c. Concerning therapeutic regimens: 71,5% used oral hypoglycaemic agents (OAD) alone (52,1% of these were using 2 or more agents); 28,5% were treated with insulin (16,2% in combination with OAD). 52,1% of the patients were anti-aggregated with aspirin. CONCLUSIONS: The metabolic control (HbA1c) and LDL values were favourable in our patients sample, comparing to other studies. The percentage of patients treated to the recommended BP of 130/80 mmHg is consistent with the literature. Only 6,8% of patients met the combined ADA goal for BP, LDL and HbA1c. Despite our comparable results to published data, we would like to highlight the difficulty to accomplish international recommendations to metabolic and risk factors control in clinical practice and the necessity of an aggressive approach to diabetes treatment.