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Newsweek Sep 1997
Topics: Antidepressive Agents, Second-Generation; Appetite Depressants; Consumer Product Safety; Fenfluramine; Fluoxetine; Heart Valve Diseases; Humans; Obesity; Phentermine; Risk Factors; United States; Weight Loss
PubMed: 10173270
DOI: No ID Found -
Expert Opinion on Pharmacotherapy Feb 2018Type 2 diabetes (T2DM) is associated with significant morbidity and mortality. Obesity is one of the main risk factors for T2DM and its management requires a... (Review)
Review
INTRODUCTION
Type 2 diabetes (T2DM) is associated with significant morbidity and mortality. Obesity is one of the main risk factors for T2DM and its management requires a multidisciplinary approach, which may include pharmacotherapy.
AREAS COVERED
In this paper, data on efficacy, tolerability and safety of FDA-approved pharmacotherapies for obesity (orlistat, phentermine/topiramate extended-release, lorcaserin, bupropion sustained release/naltrexone sustained release and liraglutide) are reviewed, focusing on individuals with type 2 diabetes.
EXPERT OPINION
Obesity is the major pathophysiologic driver of T2DM; conversely 5-10% weight loss leads to significant improvement in glycemic control, lipids and blood pressure. Weight loss maintenance is difficult with lifestyle interventions alone and may require adjunctive therapies. There is good evidence for the efficacy and tolerability of approved anti-obesity pharmacotherapies in individuals with T2DM, with current cardiovascular safety data being most favorable for liraglutide, orlistat and lorcaserin. Given the link between obesity and T2DM, a weight-centric therapeutic approach including use of weight reducing anti-diabetic therapies, and anti-obesity pharmacotherapies is both intuitive and rational to improve glycemic and other metabolic outcomes in patients with T2DM.
Topics: Anti-Obesity Agents; Benzazepines; Clinical Trials as Topic; Diabetes Mellitus, Type 2; Drug Compounding; Humans; Lactones; Liraglutide; Obesity; Orlistat; Phentermine; Weight Loss
PubMed: 29376439
DOI: 10.1080/14656566.2018.1428558 -
Journal of Chromatography. B,... Sep 2016Nonmedical use of prescription stimulants such as phentermine (PT) has been regulated by law enforcement authorities due to its euphorigenic and relaxing effects. Due to...
Nonmedical use of prescription stimulants such as phentermine (PT) has been regulated by law enforcement authorities due to its euphorigenic and relaxing effects. Due to high potential for its abuse, reliable analytical methods were required to detect and identify PT and its metabolite in biological samples. Thus a dilute and shoot liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for simultaneous determination of PT, N-hydroxyphentermine (NHOPT) and mephentermine (MPT) in urine. A 5μL aliquot of diluted urine was injected into the LC-MS/MS system. Chromatographic separation was performed by reversed-phase C18 column with gradient elution for all analytes within 5min. Identification and quantification were based on multiple reaction monitoring (MRM) detection. Linear least-squares regression with a 1/x(2) weighting factor was used to generate a calibration curve and the assay was linear from 50 to 15000ng/mL (PT and MPT) and 5 to 750ng/mL (NHOPT). The intra- and inter-day precisions were within 8.9% while the intra- and inter-day accuracies ranged from -6.2% to 11.2%. The limits of quantification were 3.5ng/mL (PT), 1.5ng/mL (NHOPT) and 1.0ng/mL (MPT). Method validation requirements for selectivity, dilution integrity, matrix effect and stability were satisfied. The applicability of the developed method was examined by analyzing urine samples from drug abusers.
Topics: Central Nervous System Stimulants; Chromatography, High Pressure Liquid; Humans; Limit of Detection; Mephentermine; Phentermine; Substance Abuse Detection; Sympathomimetics; Tandem Mass Spectrometry
PubMed: 27398632
DOI: 10.1016/j.jchromb.2016.06.045 -
Nature Reviews. Endocrinology Aug 2013Obesity, which results from an imbalance between calorie intake and expenditure, now affects over 500 million individuals worldwide. Lifestyle and behavioural... (Review)
Review
Obesity, which results from an imbalance between calorie intake and expenditure, now affects over 500 million individuals worldwide. Lifestyle and behavioural interventions aimed at reducing calorie intake and/or increasing energy expenditure have limited long-term effectiveness due to complex and persistent hormonal, metabolic and neurochemical adaptations that defend against weight loss and promote weight regain. Surgical treatments for obesity, although highly effective, are unavailable or unsuitable for the majority of individuals with excess adiposity. Accordingly, few effective treatment options are available to most individuals with obesity. In the past, the use of antiobesity drugs, seemingly the logical choice to fill this therapeutic gap, has been limited because of a lack of efficacy, poor long-term adherence rates and serious adverse effects. In 2012, the FDA approved two new medications-lorcaserin and phentermine-topiramate controlled release-and is currently reviewing the resubmission of naltrexone sustained release-bupropion sustained release. This Review presents the available data on the efficacy and safety of these three medications and discusses future perspectives and challenges related to pharmacological weight management.
Topics: Appetite Depressants; Benzazepines; Drug Combinations; Fructose; Humans; Life Style; Obesity; Phentermine; Topiramate
PubMed: 23752772
DOI: 10.1038/nrendo.2013.113 -
Yonsei Medical Journal Sep 2011
Topics: Female; Humans; Hypertension, Pulmonary; Phentermine
PubMed: 21786457
DOI: 10.3349/ymj.2011.52.5.869 -
Obesity (Silver Spring, Md.) Jan 2016Phentermine is thought to cause weight loss through a reduction in hunger. It was hypothesized that higher hunger ratings would predict greater weight loss with... (Clinical Trial)
Clinical Trial Observational Study
OBJECTIVE
Phentermine is thought to cause weight loss through a reduction in hunger. It was hypothesized that higher hunger ratings would predict greater weight loss with phentermine.
METHODS
This is an observational pilot study in which all subjects were treated with phentermine for 8 weeks and appetite and eating behaviors were measured at baseline and week 8. Outcomes were compared in subjects with ≥5% vs. <5% weight loss, and linear regression was used to identify predictors of percent weight loss.
RESULTS
Twenty-seven subjects (37 ± 4.5 years, 93.8 ± 12.1 kg, BMI 33.8 ± 3.1 kg m(-2) ) completed the study, with mean weight loss of -5.4 ± 3.3 kg (-5.7% ± 3.2%). Subjects with ≥5% weight loss had higher baseline pre-breakfast hunger (P = 0.017), desire to eat (P =0.003), and prospective food consumption (0.006) and lower baseline cognitive restraint (P = 0.01). In addition, higher baseline home prospective food consumption (P = 0.002) and lower baseline cognitive restraint (P < 0.001) were found to be predictors of weight loss.
CONCLUSIONS
These results suggest that individuals reporting greater hunger and less restraint are more likely to achieve significant weight loss with phentermine. This information can be used clinically to determine who might benefit most from phentermine treatment.
Topics: Adult; Appetite; Breakfast; Feeding Behavior; Female; Humans; Hunger; Male; Middle Aged; Obesity; Phentermine; Pilot Projects; Treatment Outcome; Weight Loss
PubMed: 26584649
DOI: 10.1002/oby.21244 -
Xenobiotica; the Fate of Foreign... Jun 19931. Urinary metabolites of the male Wistar rat dosed i.p. and orally with phentermine (Ph), N-hydroxyphentermine (N-hydroxy-Ph) and p-hydroxyphentermine (p-hydroxy-Ph)...
1. Urinary metabolites of the male Wistar rat dosed i.p. and orally with phentermine (Ph), N-hydroxyphentermine (N-hydroxy-Ph) and p-hydroxyphentermine (p-hydroxy-Ph) were examined by g.l.c. and g.l.c.-mass spectroscopy. 2. N-hydroxy-Ph which accounted for about 3% dose was identified in the urine of rat dosed i.p. and orally with Ph. The major urinary metabolite of Ph dosed i.p. and orally was a p-hydroxy-Ph conjugate (51% dose). 3. The major urinary metabolite of N-hydroxy-Ph dosed i.p. and orally was a p-hydroxy-Ph conjugate (40% dose). A N-hydroxy-Ph conjugate (12% dose) was identified following i.p. administration of N-hydroxy-Ph, but was not detected following oral administration. Small amounts of Ph (< 10% dose) and p-hydroxy-Ph (3% dose) were also identified after i.p. and oral administration of N-hydroxy-Ph. 4. The only urinary metabolite of p-hydroxy-Ph after either i.p. or oral dosing was a p-hydroxy-Ph conjugate (65% dose). 5. These results indicate that N-hydroxy-Ph is a urinary metabolite of Ph in rat; p-hydroxy-Ph is produced by the hydroxylation of Ph itself and partly by the hydroxylation of Ph formed from N-hydroxy-Ph; the p-hydroxy-Ph conjugate is the major and final metabolite of Ph dosed i.p. and orally.
Topics: Animals; Chromatography, Gas; Gas Chromatography-Mass Spectrometry; Hydroxylation; Male; Phentermine; Rats; Rats, Wistar
PubMed: 8212744
DOI: 10.3109/00498259309059408 -
Current Obesity Reports Sep 2022Obesity is closely associated with nonalcoholic fatty liver disease (NAFLD), a highly prevalent disease without any approved medication. The aim of this review was to... (Review)
Review
PURPOSE OF REVIEW
Obesity is closely associated with nonalcoholic fatty liver disease (NAFLD), a highly prevalent disease without any approved medication. The aim of this review was to summarize the evidence on the effect of anti-obesity medications on NAFLD, especially focusing on hepatic histology.
RECENT FINDINGS
Orlistat and some glucagon-like peptide-1 receptor analogs, including liraglutide and semaglutide, have beneficial effects on hepatic steatosis and inflammation, but not fibrosis. Other anti-obesity medications, including lorcaserin, setmelanotide, phentermine hydrochloric, phentermine/topiramate, and naltrexone/bupropion, have been minimally investigated in NAFLD. Furthermore, medications like sodium-glucose cotransporter-2 inhibitors and farnesoid X receptor have shown beneficial effects in both NAFLD and obesity, but they have not been licensed for either disease. Liraglutide, semaglutide, and orlistat may be currently used in selected patients with obesity and NAFLD. Further research is warranted, since targeting obesity may provide additional benefits on its comorbidities, including NAFLD.
Topics: Humans; Anti-Obesity Agents; Liraglutide; Non-alcoholic Fatty Liver Disease; Obesity; Orlistat; Phentermine; Sodium-Glucose Transporter 2 Inhibitors
PubMed: 35501557
DOI: 10.1007/s13679-022-00474-0 -
Nuclear Medicine Communications Jun 1987p-Iodo-phentermine (IP) and two of its derivatives, N,N,-dimethyl-p-iodo-phentermine (IDMP) and N-isopropyl-p-iodo-phentermine (IIP) were synthesized and radiolabelled...
p-Iodo-phentermine (IP) and two of its derivatives, N,N,-dimethyl-p-iodo-phentermine (IDMP) and N-isopropyl-p-iodo-phentermine (IIP) were synthesized and radiolabelled with iodine by isotopic exchange. They were evaluated as potential brain imaging agents and compared to IAMP biodistribution in rats did not show any superiority to IAMP.
Topics: Animals; Brain; Iodine Radioisotopes; Male; Phentermine; Radionuclide Imaging; Rats; Rats, Inbred Strains; Tissue Distribution
PubMed: 3696629
DOI: 10.1097/00006231-198706000-00007 -
Endocrine, Metabolic & Immune Disorders... 2024Obesity is a chronic lifestyle issue with devastating results. Behavioral changes are one of the initial lines of management strategies for obesity, but they are not... (Review)
Review
Obesity is a chronic lifestyle issue with devastating results. Behavioral changes are one of the initial lines of management strategies for obesity, but they are not very efficient management strategies. Many people also use surgical intervention to maintain a healthy weight, now considered to be the most common and effective obesity management. Chemically synthesized medicines fill the gap between lifestyle interventions and minimally invasive surgical management of obesity. The most common issue associated with monotherapy without side effects is its moderate effectiveness and higher dose requirement. Combination therapy is already used for many serious and complicated disease treatments and management and has shown efficacy as well. Generally, we use two or more medicines with different mechanisms of action for a better effect. The commonly used combination therapy for obesity management includes low-dose phentermine and prolonged and slow-releasing mechanism topiramate; naltrexone, and bupropion. Phentermine with inhibitors of Na-glucose cotransporter-2 or glucagon-like peptide-1 (GLP-1) agonists with gastric hormone or Na-glucose cotransporter-2 are two more viable combo therapy. This combination strategy aims to achieve success in bariatric surgery and the scientific community is working in this direction.
Topics: Humans; Obesity; Anti-Obesity Agents; Drug Therapy, Combination; Phentermine; Treatment Outcome; Animals
PubMed: 37641995
DOI: 10.2174/1871530323666230825140808