Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0028754 (obesity)
 124,988 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Three medications with approval for long-term use in the treatment of obesity are currently available in the United States. Sibutramine (U.S. Food and Drug Administration [FDA] approved in 1997), orlistat (FDA approved in 1999), and rimonabant (available in Europe and given FDA approvable status in 2006 and expected to be marketed in 2007) represent modern approaches to medications used adjunctively for weight management. As demonstrated in large clinical trials of 2 to 4 years' duration, these medications significantly increase weight loss compared with placebo; weight loss with these drugs reaches a nadir between 20 and 28 weeks; weight loss, averaged 8%-10%, with the placebo contributing 4%-6% of that. Weight maintenance is demonstrated as long as adherence to medication continues. All medications have side effects that need to be considered. For sibutramine, there is a rise in blood pressure and heart rate that may require discontinuation of the drug in a small percent of patients. For orlistat, steatorrhea produces the principal gastrointestinal side effects. Rimonabant appears to have a favorable safety and tolerability profile. Nausea and gastrointestinal symptoms are the chief tolerability issue, but they are usually self-limited. In addition there are several drugs and drug combinations in phase 2 or phase 2 trials that will be reported on in the coming years.
 ...
PMID:Drug treatment of the overweight patient. 1749 15

The aim of this study was to evaluate the effects of sibutramine on gastric emptying, small-bowel contractions, rectal tone and compliance, and gastrointestinal myoelectrical activity. The study was performed in 14 dogs. It was composed of three separate experiments: gastric emptying of liquids and gastrointestinal slow waves; small-bowel contractions; and rectal tone and rectal compliance. Each experiment included two sessions: a control session and a treatment session with sibutramine (5 mg/kg orally) administrated 2 h before the study. Sibutramine significantly accelerated liquid gastric emptying at 75 and 90 min after the meal but did not alter gastrointestinal slow waves. Gastric emptying at 75 and 90 min was 61.42 +/- 7.71 and 66.32 +/- 7.67% in the control session, and increased to 71.27 +/- 5.14 and 75.93 +/- 5.29% in the session with sibutramine (p < 0.05, vs. control). Sibutramine significantly inhibited postprandial small-bowel contractions. Sibutramine did not alter the rectal tone, but significantly increased rectal compliance. Sibutramine accelerates gastric emptying of liquids but inhibits small-bowel contractions. These findings suggest the peripheral mechanisms of sibutramine in reducing food intake and causing weight loss in obesity patients.
 ...
PMID:Effects of sibutramine on gastric emptying, intestinal motility and rectal tone in dogs. 1751 Aug 1

Obesity is a multifactorial chronic disorder which comprises a serious health problem nowadays. The effective management of obesity is difficult in contemporary societies where abundance of hypercaloric food and sedentary lifestyle is the rule. Apart from lifestyle interventions, which include diet, exercise and behavioural treatment, weight-loss medications can also be used for the management of obesity. Sibutramine, a selective monoamine reuptake inhibitor, is a drug with established efficacy in sustained weight reduction and an overall favourable safety profile. However, its action on the sympathetic nervous system has linked sibutramine to blood pressure and heart rate elevations. These potentially adverse effects as well as other sibutramine-associated side effects and their possible underlying mechanisms are reviewed in the present article. Compelling evidence from the majority of data in the literature shows that sibutramine can be effectively used in conjunction with caloric restriction and exercise in obese patients. Hypertension, if adequately treated and frequently monitored, is not an absolute contraindication for the prescription of sibutramine.
 ...
PMID:Sibutramine-associated adverse effects: a practical guide for its safe use. 1803 90

Sibutramine is a serotonin and norepinephrine reuptake intake inhibitor approved for the management of obesity. It has various CNS adverse effects and a few case reports of psychiatric manifestations. Here, we report a case of severe catatonic and psychotic symptoms associated with sibutramine overuse in the patient who had no prior psychiatric history. The symptoms subsequently resolved completely with cessation. Given the widespread use of sibutramine, this case would be of interest to practitioners of internal medicine and psychiatry. Moreover, as sibutramine may be used for weight management in patients on antipsychotic medications, the implications on psychotic symptoms need to be explored further. We also discuss possible pathophysiologic underpinnings.
 ...
PMID:Catatonia and psychosis associated with sibutramine: a case report and pathophysiologic correlation. 1815 6

Sibutramine is one of the very few drugs that are approved for long-term treatment of obesity. Sibutramine is a racemic mixture (RS) containing two equal forms of the R(+) and S(-) enantiomers. In this paper, we have investigated comparative anorexic effect of sibutramine enantiomers and their recemate form in rats. After obtaining two days of baseline results, rats were administered orally either with (RS)-sibutramine or its enantiomers (R)- or (S)-sibutramine at dose levels of 5, 10, 20 mg/kg each for 4 days and body weight, food intake and water intake were measured daily. Locomotor activity score of each rat was also recorded on each day. R-Sibutramine and (RS)-sibutramine produced dose dependant decrease in the body weight and food intake. On the other hand, (S)-sibutramine was shown to increase in these parameters. Neither sibutramine nor it's enantiomers showed any consistent effects on spontaneous motor activity (SMA) scores. In conclusion, (R)-sibutramine is better anorexic than or (RS)-sibutramine or it's (S)-enantiomers.
 ...
PMID:Anorexic effect of (R)-sibutramine: comparison with (RS)-sibutramine [corrected] and (S)-sibutramine. 1817 63

Monohydrated sibutramine hydrochloride is a widely used active ingredient for the treatment of obesity. An anhydrous form of sibutramine hydrochloride was prepared starting from its monohydrate form upon heating it at 140 degrees C for 15 min. This dehydration process was monitored using conventional TG/DSC methods. Heated above 190 degrees C, sibutramine hydrochloride sublimes and recrystallizes on the cold walls of the test tube, giving platelet shaped crystals suitable for single crystal X-ray diffraction analysis: monoclinic, P2(1)/n, a = 7.321(2) A, b = 25.456(5) A, c = 9.750(3) A, beta = 101.60(2) degrees , V = 1779.9(8) A(3), Z = 4. At variance, sibutramine free base was typically recovered as a viscous oily material, upon treatment of its hydrochloride salt in ethyl acetate solution. Recrystallization from hexane yielded a white polycrystalline powder, the structure of which was determined by unconventional ab initio X-ray powder diffraction analysis: triclinic, P-1, a = 8.6578(3) A, b = 9.3318(3) A, c = 11.1224(4) A, alpha = 110.434(3) degrees , beta = 100.159(3) degrees , gamma = 89.201(2) degrees , V = 827.76(5) A(3), Z = 2. Sibutramine, in its different crystalline environments, was also fully characterized by solid state (13)C NMR analyses. Additional spectral information was obtained by collecting spectra of a metastable, oily sample, before it slowly recrystallizes (within hours).
 ...
PMID:Crystal chemistry of sibutramine: thermal, diffractometric and spectroscopic characterization. 1839 2

Sibutramine, a serotonin reuptake inhibitor, currently is used in treatment of obesity. The known side effects of sibutramine, ie, hypertension and tachycardia, depend on its adrenergic and serotoninergic effects. We describe a case of life-threatening hyponatremia associated with sibutramine use in an obese woman. We hypothesize that sibutramine, through its effect on neurotransmitters, may induce antidiuretic hormone secretion and lead to a syndrome of inappropriate antidiuretic hormone secretion. We advise careful monitoring of water-electrolytic balance during sibutramine therapy.
 ...
PMID:Severe symptomatic hyponatremia during sibutramine therapy: a case report. 1902 58

Sibutramine is an anti-obesity drug, which acts by inhibiting neuronal re-uptake of noradrenaline and serotonin. Although the most frequently seen effect of sibutramine on cardiovascular system is an increase in blood pressure and pulse rate, rare but severe side effects such as sibutramine-induced ventricular arrhythmias, heart failure and cardiovascular disease-related death are also reported. We describe a 24 year-old man with low atherosclerotic risk profile who had acute myocardial infarction possibly associated with sibutramine use.
 ...
PMID:Acute myocardial infarction in a 24 year-old man possibly associated with sibutramine use. 1868 92

Obesity is becoming one of the most common health problems in the world. Many other disorders, such as hypertension and diabetes are considered as the consequences of obesity. Since effective remedies are rare (only two drugs, Orlistat and Sibutramine, were officially approved by the US Food and Drug Administration for long-term obesity treatment so far), researchers are trying to discover new therapies for obesity, and acupuncture is among the most popular alternative approaches. To facilitate weight reduction, one can use manual acupuncture, electroacupuncture (EA) or transcutaneous electrical acupoint stimulation (TEAS). As the parameters of the EA or TEAS can be precisely characterized and the results are more or less reproducible, this review will focus on EA as a treatment modality for obesity. Results obtained in this laboratory in recent five years will be summarized in some detail.
 ...
PMID:Electroacupuncture in the treatment of obesity. 1871 95

Given the suggestion that many potential anti-obesity drugs may enhance within-meal satiation, few studies have directly measured the effects of any drug on the microstructure of human eating behaviour. The effects of 7 days dosing with sibutramine 10 mg and 15 mg a day on appetite and energy balance were determined in 30 obese women (BMI 34.6 +/- 3.3 kg/m2, age 46.0 +/- 12.9 years) using a Universal Eating Monitor (UEM) and indirect calorimetry, in a double-blind, placebo-controlled crossover study. At day 7, sibutramine 10 mg and 15 mg reduced food intake by 16.6% and 22.3%, respectively (p < 0.001), compared with placebo. Sibutramine reduced eating rate compared with placebo rather than meal length (10 mg p < 0.05; 15 mg p < 0.001). In addition, sibutramine 10 mg significantly reduced hunger later in the meal (p < 0.05) and sibutramine 15 mg increased fullness early in the meal (p < 0.01), both of which are consistent with enhanced within-meal satiation. Sibutramine had little effect on resting metabolic rate, although 15 mg did significantly reduce respiratory quotient at several time points during the test day. These results provide novel evidence that decreased consumption of a test meal induced by sibutramine is primarily because of reduced eating rate, enhancing the deceleration in cumulative food intake within a meal associated with the development of satiety. Changes in within-meal appetite ratings appear particularly sensitive to drug-induced enhancement of satiation, and may provide key indices for assessing the therapeutic potential of novel anti-obesity drugs.
 ...
PMID:The effects of sibutramine on the microstructure of eating behaviour and energy expenditure in obese women. 1875 18


<< Previous 1 2 3 4 5 6 7 8 9 10 Next >>