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The Medical Journal of Australia Feb 1968
Topics: Central Nervous System; Chlorpromazine; Diethylpropion; Female; Humans; Paranoid Disorders; Schizophrenia; Substance-Related Disorders
PubMed: 5642840
DOI: 10.5694/j.1326-5377.1968.tb82658.x -
Gastroenterology Nov 2022Pharmacological management of obesity improves outcomes and decreases the risk of obesity-related complications. This American Gastroenterological Association guideline...
BACKGROUND & AIMS
Pharmacological management of obesity improves outcomes and decreases the risk of obesity-related complications. This American Gastroenterological Association guideline is intended to support practitioners in decisions about pharmacological interventions for overweight and obesity.
METHODS
A multidisciplinary panel of content experts and guideline methodologists used the Grading of Recommendations Assessment, Development and Evaluation framework to prioritize clinical questions, identify patient-centered outcomes, and conduct an evidence synthesis of the following agents: semaglutide 2.4 mg, liraglutide 3.0 mg, phentermine-topiramate extended-release (ER), naltrexone-bupropion ER, orlistat, phentermine, diethylpropion, and Gelesis100 oral superabsorbent hydrogel. The guideline panel used the evidence-to-decision framework to develop recommendations for the pharmacological management of obesity and provided implementation considerations for clinical practice.
RESULTS
The guideline panel made 9 recommendations. The panel strongly recommended the use of pharmacotherapy in addition to lifestyle intervention in adults with overweight and obesity (body mass index ≥30 kg/m, or ≥27 kg/m with weight-related complications) who have an inadequate response to lifestyle interventions. The panel suggested the use of semaglutide 2.4 mg, liraglutide 3.0 mg, phentermine-topiramate ER, and naltrexone-bupropion ER (based on moderate certainty evidence), and phentermine and diethylpropion (based on low certainty evidence), for long-term management of overweight and obesity. The guideline panel suggested against the use of orlistat. The panel identified the use of Gelesis100 oral superabsorbent hydrogel as a knowledge gap.
CONCLUSIONS
In adults with overweight and obesity who have an inadequate response to lifestyle interventions alone, long-term pharmacological therapy is recommended, with multiple effective and safe treatment options.
Topics: Adult; Humans; Orlistat; Anti-Obesity Agents; Overweight; Liraglutide; Bupropion; Naltrexone; Topiramate; Weight Loss; Diethylpropion; Phentermine; Obesity; Hydrogels
PubMed: 36273831
DOI: 10.1053/j.gastro.2022.08.045 -
Revista Da Associacao Medica Brasileira... Mar 2017Antiobesity pharmacotherapy remains the main point of disagreement among both scientists and regulators. This is probably due to small sample sizes, high levels of...
Antiobesity pharmacotherapy remains the main point of disagreement among both scientists and regulators. This is probably due to small sample sizes, high levels of heterogeneity, and low methodological quality. For many years, Brazil was one of the largest consumers of appetite suppressants worldwide, with evidence of irrational use of this drug class. Therefore, the country was the scene of a debate that divided the Brazilian Health Surveillance Agency (Anvisa - Agência Nacional de Vigilância Sanitária) and medical societies over the maintenance record of diethylpropion, mazindol and fenproporex. In this context, this commentary presents new arguments to contribute to the discussion, as well as recommendations for future studies.
Topics: Amphetamines; Appetite Depressants; Brazil; Cyclobutanes; Diethylpropion; Drug Approval; Humans; Mazindol; Obesity; Risk Assessment; Treatment Outcome
PubMed: 28489121
DOI: 10.1590/1806-9282.63.03.203 -
The Medical Journal of Australia Dec 1970
Topics: Adult; Diethylpropion; Female; Humans; Obesity; Psychoses, Substance-Induced; Substance-Related Disorders
PubMed: 5491072
DOI: 10.5694/j.1326-5377.1970.tb63346.x -
International Review of Neurobiology 2009The antiappetite agent diethylpropion (DEP), and the antidepressant and antismoking aid compound bupropion (BP), not only share the same structural motif but also... (Review)
Review
The antiappetite agent diethylpropion (DEP), and the antidepressant and antismoking aid compound bupropion (BP), not only share the same structural motif but also present similar mechanisms of action in the CNS. For example, both drugs induce the release as well as inhibit the reuptake of neurotransmitters such as a dopamine (DA) and norepinephrine (NE). In general, they produce mild side effects, including reversible psychomotor alterations mostly in geriatric patients (by BP), or moderate changes in neurotransmitter contents linked to oxidative damage (by DEP). Therefore, attention must be paid during any therapeutic use of these agents. Regarding the interaction of BP with the DA transporter, residues S359, located in the middle of TM7, and A279, located close to the extracellular end of TM5, contribute to the binding and blockade of translocation mediated by BP, respectively. Additional mechanisms of action have also been determined for each compound. For example, BP is a noncompetitive antagonist (NCA) of several nicotinic acetylcholine receptors (AChRs). Based on this evidence, the dual antidepressant and antinicotinic activity of BP is currently considered to be mediated by its stimulatory action on DA and NE systems as well as its inhibitory action on AChRs. Considering the results obtained in the archetypical mouse muscle AChR, a sequential mechanism can be hypothesized to explain the inhibitory action of BP on neuronal AChRs: (1) BP first binds to AChRs in the resting state, decreasing the probability of ion channel opening, (2) the remnant fraction of open ion channels is subsequently decreased by accelerating the desensitization process, and finally (3) BP interacts with a binding domain located between the serine (position 9') and valine (position 13') rings that is shared with the NCA phencyclidine and other tricyclic antidepressants. The homologous location in the alpha3beta4 AChR is between the serine and valine/phenylalanine rings. This new evidence opens a window for further investigation using AChRs as targets for the action of safer antidepressants and novel antiaddictive compounds.
Topics: Animals; Appetite Depressants; Brain; Bupropion; Diethylpropion; Dopamine Uptake Inhibitors; Humans
PubMed: 19897080
DOI: 10.1016/S0074-7742(09)88009-4 -
Clinical Neuropharmacology Apr 1988Five female patients who developed psychosis while taking diethylpropion hydrochloride are described, four with paranoid psychosis and one with manic psychosis. In all...
Five female patients who developed psychosis while taking diethylpropion hydrochloride are described, four with paranoid psychosis and one with manic psychosis. In all but one patient, these drugs were medically prescribed. Although relatively few cases of psychosis and psychosis-like illness were reported to the Committee for Safety of Medicines from 1963 until 1986, further cases may be anticipated. Patients on the drug should be carefully supervised and it should not be prescribed to those with personality disorder, previous evidence of amphetamine, alcohol, or other drug abuse, or those with a history of psychiatric breakdown.
Topics: Adult; Bipolar Disorder; Diethylpropion; Female; Humans; Middle Aged; Obesity; Paranoid Disorders; Psychoses, Substance-Induced
PubMed: 3378228
DOI: 10.1097/00002826-198804000-00011 -
The British Journal of Psychiatry : the... Jan 1988
Topics: Adult; Diethylpropion; Female; Humans; Psychoses, Substance-Induced
PubMed: 3167330
DOI: 10.1192/bjp.152.1.146 -
The British Journal of Psychiatry : the... Apr 1988
Topics: Adult; Diethylpropion; Female; Humans; Psychoses, Substance-Induced
PubMed: 3167418
DOI: 10.1192/s0007125000219752 -
The European Respiratory Journal Sep 2003Primary pulmonary hypertension (PPH) is characterised by sustained elevations of pulmonary arterial pressure without a demonstrable cause, leading to right ventricular... (Review)
Review
Primary pulmonary hypertension (PPH) is characterised by sustained elevations of pulmonary arterial pressure without a demonstrable cause, leading to right ventricular failure and death. Hereditary mutations in the bone morphogenetic protein receptor type II (BMPR2) gene result in familial PPH transmitted as an autosomal dominant trait, albeit with low penetrance. The causes in cases without a BMPR2 mutation are unknown, but a syndrome of pulmonary arterial hypertension (PAH) similar to hereditary PPH is associated with systemic connective tissue disease, congenital heart disease, portal hypertension, and human immunodeficiency virus infection, or with the use of appetite-suppressant drugs. The authors identified a BMPR2 gene mutation in a 27-yr-old female who developed PAH after a short course of the appetite-suppressant drug amfepramone (diethylpropion). This allowed molecular genetic counselling and prevention of potentially harmful drug exposure in the patient's son treated for attention deficit disorder with methylphenidate, an amphetamine-related drug. No BMPR2 mutation was found in four additional, unrelated patients with appetite suppressant-related PPH. The findings provide strong evidence that amfepramone can trigger primary pulmonary hypertension in a bone morphogenetic protein receptor type II gene mutation carrier, and indicate that other genes are probably implicated in genetic susceptibility to appetite suppressants.
Topics: Adult; Appetite Depressants; Attention Deficit Disorder with Hyperactivity; Bone Morphogenetic Protein Receptors, Type II; Diethylpropion; Female; Genetic Predisposition to Disease; Humans; Hypertension, Pulmonary; Methylphenidate; Mutation; Protein Serine-Threonine Kinases; Receptors, Cell Surface
PubMed: 14516151
DOI: 10.1183/09031936.03.00095303