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[Obesity: a review of currently used antiobesity drugs and new compounds in clinical development].

This review summarizes data on currently used antiobesity drugs and new compounds under clinical development. Three antiobesity drugs are currently accepted for long-term use. Sibutramine is a noradrenaline and serotonin reuptake inhibitor which reduces body weight by about 4-5 kg but increases heart rate and arterial blood pressure. Orlistat is a gastrointestinal lipase inhibitor which results in mean weight loss by about 3 kg and reduces the incidence of type 2 diabetes in patients with impaired glucose tolerance; however, adverse gastrointestinal effects have been observed. Rimonabant is an

Drugs in the treatment of obesity: sibutramine, orlistat and rimonabant.

BACKGROUND: Modification of lifestyle is the main therapeutical approach in the treatment of obesity, but use to fail on long terms of time. Addition of anti-obesity drugs allows keeping the weight loss during years and improving obesity-related comorbidities. METHODS: This review is an actualisation on efficacy, safety and tolerability of the approved drugs on the long-term treatment of obesity (orlistat and sibutramine). New indications and effects of their use far beyond the weight loss are as well commented. Finally, potential benefits of the administration of CB1 antagonist rimonabant on

Pharmacotherapy for obesity.

The current obesity pandemic imposes a major global disease burden. However, sustained weight loss of between 5 and 10% in the obese confers marked health benefits. Currently available pharmacotherapies, orlistat and sibutramine, can induce weight loss of between 5 and 10% over 2 years or more. However, in these trials, drug induced weight loss tends to be only 2-4 kg greater than that produced by placebo control. Despite this, in the XENDOS trial, the modest placebo-subtract weight loss produced by orlistat (2.8 kg) reduced the incidence of diabetes by over a third. Recent data on the potenti

Differential effects of naproxen and rofecoxib on the development of hypersensitivity following nerve injury in rats.

The present study was undertaken to determine the effects of cyclooxygenase (COX) inhibitors on the development of neuropathic pain in rats following chronic constriction injury (CCI). A single intraperitoneal administration of naproxen, a nonselective COX inhibitor (10 or 30 mg/kg), or rofecoxib, a selective COX-2 inhibitor (3 or 10 mg/kg) 2 h before nerve injury did not attenuate the development of neuropathic state for 28 days. However, the administration of naproxen [10 or 30 mg/kg, intraperitonelly (i.p.)], but not rofecoxib (3 or 10 mg/kg, i.p.), on day 7 attenuated hypersensitivity but

What role for weight-loss medication? Weighing the pros and cons for obese patients.

Obesity is a chronic medical disorder that is not going away anytime soon. Physicians need all the education, tools, and resources possible to successfully help their overweight and obese patients. Weight-loss medications alone are clearly not the answer. However, they are one tool physicians can use in combination with lifestyle changes to increase the success of long-term weight loss in selected patients.

Long-term pharmacotherapy for obesity and overweight.

BACKGROUND: Worldwide prevalence rates of obesity and overweight are rising and safe and effective treatment strategies are urgently needed. A number of anti-obesity agents have been studied in short-term clinical trials, but long-term efficacy and safety need to be established. OBJECTIVES: To assess/compare the effects and safety of approved anti-obesity medications in clinical trials of at least one-year duration. SEARCH STRATEGY: MEDLINE, EMBASE, the Cochrane Controlled Trials Register, the Current Science Meta-register of Controlled Trials, and reference lists of original studies and rev

[Pharmacotherapy of obesity].

Obesity is a chronic disease with a worldwide increasing incidence. The mainstay of therapy consists in modification of behaviour related to obesity such as overeating and physical inactivity. When these life-style modifying attempts fail, the use of anti-obesity drugs is warranted. The two available drugs, orlistat and sibutramine, are capable of reducing body weight by 10%. Failure of these medications in a subset of patients to achieve adequate weight loss and limited overall efficacy have led to an extensive research on novel anti-obesity agents. This review presents an overview on the cur

Long-term pharmacotherapy for obesity and overweight.

BACKGROUND: Worldwide prevalence rates of obesity and overweight are rising and safe and effective treatment strategies are urgently needed. A number of anti-obesity agents have been studied in short-term clinical trials, but long-term efficacy and safety need to be established. OBJECTIVES: To assess/compare the effects and safety of approved anti-obesity medications in clinical trials of at least one-year duration. SEARCH STRATEGY: MEDLINE, EMBASE, the Cochrane Controlled Trials Register, the Current Science Meta-register of Controlled Trials, and reference lists of original studies and rev

The cerebrospinal fluid/serum leptin ratio during pharmacological therapy for obesity.

The aim of the present study was to evaluate the cerebrospinal fluid (CSF)/serum leptin ratio during pharmacological therapy for obesity with centrally and peripherally acting drugs. Thirty-one obese women (mean age, 32.3 +/- 10 yr; body mass index, 38.2 +/- 5.2 kg/m(2); body fat, 43.3 +/- 5.4%) were studied before and 2 months after a weight loss program consisting of a balanced diet (1200 kcal/d) plus drug therapy. The patients were randomly assigned into three study groups: group I, fenproporex 25 mg/d (n = 10); group II, sibutramine 10 mg/d (n = 10); and group III, orlistat 120 mg tid (n =

N-Acetylcysteine enhances the action of anti-inflammatory drugs as suppressors of prostaglandin production in monocytes.

The anti-inflammatory effect of non-steroidal anti-inflammatory drugs (NSAIDs) is associated with inhibition of cyclooxygenase (COX), the rate-limiting enzyme responsible for the synthesis of prostaglandins. Since oxygen free radicals can act as second cellular messengers, especially to modulate the metabolism of arachidonic acid and the prostaglandin tract, it seems plausible that antioxidants might affect the production of prostaglandin by activated cells. This research is focused on the effect of the antioxidant N-acetylcysteine (NAC) on the inhibition of prostaglandin E(2) formation in act

LuxS-mediated quorum sensing in Borrelia burgdorferi, the lyme disease spirochete.

The establishment of Borrelia burgdorferi infection involves numerous interactions between the bacteria and a variety of vertebrate host and arthropod vector tissues. This complex process requires regulated synthesis of many bacterial proteins. We now demonstrate that these spirochetes utilize a LuxS/autoinducer-2 (AI-2)-based quorum-sensing mechanism to regulate protein expression, the first system of cell-cell communication to be described in a spirochete. The luxS gene of B. burgdorferi was identified and demonstrated to encode a functional enzyme by complementation of an Escherichia coli l

[Management in Senegal of the 1st efficacy and tolerability studies of ivermectin (MK 933) in human onchocerciasis].

In 1981, 32 adult Senegalese males infected with Onchocerca volvulus but without ocular involvement were treated by groups of 8 with single oral dosages of 5, 10, 30 or 50 micrograms/kg of ivermectin . As soon as the second day after treatment, we observed a marked decrease of the dermal microfilaremic charge after a posology of 30 micrograms/kg. However the decrease is most important in the group subjected to 50 micrograms/kg and 75% of them had no more microfilariae in the dermis 28 days following treatment.

Anthelmintic effect of levamisole, ivermectin, albendazole and fenbendazole on larval Toxocara canis infection in mice.

The anthelmintic effects of levamisole (100-50 mg kg-1 live bodyweight), ivermectin (2 mg kg-1 bodyweight), albendazole and fenbendazole (both 100 mg kg-1 bodyweight), were tested against second stage Toxocara canis larvae in mice. Anthelmintic treatment on days 2 to 7 after infection inclusive resulted in significant (P less than 0.05) retention of larvae in the liver, and fewer larvae migrated subsequently to the brain and the musculature of treated mice compared to untreated controls. Most of the larvae retained in the liver subsequently died there and were not recoverable by day 35 after i

Preparation and Properties of Gemini Glycosyl Organosilicon Quaternary Ammonium Salts with Excellent Sustained Foam-Associated Antibacterial Activity.

In this study, d-glucono delta-lactone was used as the raw material to sequentially conduct amidation, substitution, and quaternization reactions, through which a novel Gemini sugar-based amide organosilicon quaternary ammonium salt surfactant (2/3SiDDGMAPB) was designed and synthesized, and its molecular structures were confirmed by FT-IR and nuclear magnetic resonance. Notably, the results of physicochemical characterization and application performance investigation demonstrate that the surface tension of 2SiDDGMAPB is as low as 29.38 mN/m. Transmission electron microscopy, energy-dispersive

Irreversible Bilayer Thermochromic Label Integrated With 3D Printing for Wide‑Range Temperature Monitoring in Food Logistics.

Temperature abuse during logistics is a major cause of quality deterioration in food, pharmaceuticals, and biological products. Therefore, the development of low-cost, irreversible, and tamper‑proof temperature indicators is of great practical significance. Based on the acid-catalyzed irreversible ring-opening coloration of crystal violet lactone (CVL) under acidic conditions, a bilayer temperature monitoring label was prepared in this study, and the label structure was further optimized by introducing three-dimensional (3D) printing technology. Upon temperature excursions, the acidic componen

Covalent targeting of PSMD14 by Eupalinolide B induces oncoprotein degradation and apoptosis in acute promyelocytic leukemia cells.

Treatment of acute promyelocytic leukemia (APL) remains challenged by toxicities associated with current regimens, highlighting the need for novel and safer therapeutic agents. Here, we identify Eupalinolide B (EB), a natural sesquiterpene lactone isolated from Eupatorium lindleyanum DC., as a potent anti-leukemic compound targeting the human APL-derived HL-60 cell line. Through integrated chemoproteomic profiling and functional validation, we demonstrate that EB covalently binds and inhibits 26S proteasome non-ATPase regulatory subunit 14 (PSMD14), a deubiquitinase enzyme (DUB) within the 19S

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… In this study, we identify the natural sesquiterpene lactone EB as a potent anti-leukemic compound active against APL-derived HL-60 cells. … Featuring a reactive α-methylene-γ-lactone moiety, a characteristic structural motif of sesquiterpene lactones, EB represents a novel chemotype for selectively targeting PSMD14. …

Nanostructured Lipid Carriers Enable In Vivo Efficacy of Parthenolide in Schistosoma mansoni Infection.

Background: Schistosomiasis remains a major neglected tropical disease, with praziquantel (PZQ) as the only widely used treatment, despite its limitations. Parthenolide (PTL), a sesquiterpene lactone, exhibits potent in vitro antischistosomal activity; however, its poor aqueous solubility, low oral bioavailability, and chemical instability may limit its in vivo efficacy. Objective: This study investigated whether nanoencapsulation in nanostructured lipid carriers (NLC) could enable the in vivo antischistosomal activity of PTL. Methods: PTL was isolated from Tanacetum parthenium and incorporate

Patch Testing in Individuals With Diabetes Using Medical Devices. Part 1-Contact Allergy to Baseline Series Allergens.

BACKGROUND: The prevalence of contact allergy in individuals with diabetes and diabetes medical device (MD) users is unknown. OBJECTIVES: This study (Part 1 and 2) aims at describing contact allergy prevalences in diabetes MD users. METHODS: Adults with type 1 diabetes from two endocrinology departments were patch tested with the Swedish baseline series (SBS) and a MD series. Contact allergies to the baseline series were compared with consecutive dermatitis patients. Detailed results for the MD series are presented in another manuscript. RESULTS: Overall, similar contact allergy prevalences