Disease relevance of Amfepramone

• Mazindol, diethylpropion, and a placebo were compared with behavioral therapy for effectiveness in producing weight reduction in an outpatient obesity clinic [1].
• The effect of diethylpropion on energy intake was evaluated by the platter-service method in 2 overweight adult male subjects hospitalized on a metabolic unit for 41 days [2].
• Activity of anorectic drugs (Amphetamine), amfepramone and UP 507-O4) on two models of obesity in animals [proceedings] [3].
• Higher cumulative doses of Chinese herbs, (dex)fenfluramine and diethylpropion were observed in patients with Chinese herb nephropathy with, when compared to those without, aortic regurgitation [4].
• The effects of diethylpropion (DEP), an amphetamine derivative and a well-known anorectic agent, on different neurochemical and behavioral markers of toxicity in rats were evaluated [5].

Psychiatry related information on Amfepramone

• The effects of intramuscular amphetamine (AMPH), dexfenfluramine (DFEN), diethylpropion (DEP), phencyclidine (PCP), diazepam (DZP), as well as caloric prefeeding and acute food deprivation were determined [6].
• In the sensitive animals (type A) diethylpropion increased locomotor activity and anxiogenic-like behavior, but decreased bodycare activities [7].
• The study compares: (a) conventional 1000 kcal (4.19 MJ) diet with diethylpropion permitted: (b) isocaloric partial meal replacement with protein powder, and diethylpropion permitted; and (c) pre-meal satiation with protein powder [8].
• There were no differences between placebo and medication groups on any test, indicating that, within the time frame studied, diethylpropion does not produce neurotoxic effects that can be detected with standardized neuropsychological tests [9].

High impact information on Amfepramone

• In contrast, the structurally related anorectic agent mazindol and the amphetamine-based anorectic compounds diethylpropion, fenfluramine, and phentermine had no effect on K(ATP) channel activity in this cell line [10].
• The study investigated whether changes in body composition of normal and genetically obese C57BL/6J (ob/ob) mice caused by the anorectic drugs phentermine, diethylpropion, fenfluramine, and mazindol are entirely due to reduced food intake [11].
• In support of this conclusion, phentermine and mazindol increased energy expenditure in normal mice by 35% compared to untreated controls in the 6 h after dosing but diethylpropion and fenfluramine had little or no effect [11].
• Patients exposed to fenfluramines continue to be monitored, with some follow-up studies indicating no overall worsening in valvulopathy over time.There are limited efficacy and safety data for amfepramone (diethylpropion) and phentermine and their approval for the management of obesity is limited to short-term use [12].
• Effects of intravenous cocaine, diethylpropion, d-amphetamine and perphenazine on responding maintained by food delivery and shock avoidance in rhesus monkeys [13].

Chemical compound and disease context of Amfepramone

• In a double-blind, placebo-controlled evaluation in obese adults given comparable dietary and exercise recommendations, controlled-release diethylpropion hydrochloride promoted significantly more weight loss than matching placebo [14].
• In the insensitive monkeys, WAY 100635 had no effect on locomotor activity after diethylpropion, but blocked diethylpropion effects on some anxiogenic-like behavioral responses [7].
• Interestingly, despite the addition of fenfluramine and diethylpropion, two drugs incriminated in the development of valvular heart disease, no cardiac abnormalities were observed [15].
• We describe a case of torsade de pointes occurring in a patient with a prolonged QT interval while taking a 1000 calorie diet, diethylpropion hydrochloride (Tenuate Dospan) and bendrofluazide [16].

Biological context of Amfepramone

• On diethylpropion administration both subjects had an average decrease in energy intake of 11% and 15% (p less than 0.005) [2].
• The influence of pH on the hydrolysis of diethylpropion hydrochloride was investigated [17].
• 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 [18].
• Double blind evaluation of long acting diethylpropion hydrochloride in obese patients from a general practice [19].
• Effect of (3',4'-dichloro-2(2-imidazolin-2-yl-thio)-acetophenone hydrobromide) (DITA) on pulmonary and systemic arterial blood pressure: a comparison with diethylpropion [20].

Anatomical context of Amfepramone

• The objective and timing of drug disposition studies, appendix III. Diethylpropion and its metabolites in the blood plasma of the human after subcutaneous and oral administration [21].
• Following 11 days of treatment with diethylpropion, amphetamine or mazindol, there was a significant increase in purine nucleotide (GDP) binding to mitochondria only in the amphetamine-treated animals [22].
• Toxicological analysis of these droplets revealed the presence of thyroid extract and diethylpropione, an amphetamine-like noradrenergic anorectic agent banned in Belgium [23].

Associations of Amfepramone with other chemical compounds

• The adsorption of phenethylamines (dextroamphetamine, phentermine, mephentermine, diethylpropion), choline, and phenylimidazoles (levamisole and imazalil) was examined in vitro in aqueous solutions on bentonite and on lewatite at 25 degrees C. An ion-exchange mechanism prevails for lewatite and for bentonite up to 0.8 mEq X g-1 [24].
• Effect of mazindol, d-amphetamine and diethylpropion on purine nucleotide binding to brown adipose tissue [22].
• A double-blind, placebo-controlled, cross-over study has been carried out to compare long-acting diethylpropion hydrochloride (Tenuate Dospan, Wm. S. Merrell Company, hereafter referred to as TD) in a rural general practice [25].
• The excretion of amphepramone, amphetamine, ephedrine and prolintane was estimated qualitatively from saliva and urine using thin-layer chromatography (TLC) 1, 2, 4, 8, 12 and 24 h after a single intake of therapeutic doses by healthy volunteers [26].
• Part of the obese patients were subjected to a low carbohydrate, low calorie diet and also to short-term (9-14 days) courses of diethylpropion (DEP) 50 mg/day, meclofenoxate (MEC) 100 mg/day and thyroid extract (THE) 1-2 mg/kg/day [27].

Gene context of Amfepramone

• Primary pulmonary hypertension after amfepramone (diethylpropion) with BMPR2 mutation [18].
• Selective 5-HT1A-receptor antagonism modulated the acute diethylpropion effects responder type specifically [7].
• Amfepramone does not cause primary pulmonary hypertension [28].

Analytical, diagnostic and therapeutic context of Amfepramone

• A rapid assay was developed for diethylpropion hydrochloride tablets using high-performance liquid chromatography (HPLC) with UV detection [29].
• The enantiomers of the anorectic drug amfepramone [rac-diethylpropion, rac-2-(diethylamino)-1-phenyl-1-propanone; rac-DEP] were separated in the preparative scale by crystallization [30].
• The absorption of diethylpropion (DEP I), dimethylpropion (DMP I) and some of their basic metabolites into and passage through the skin was investigated and a comparison of their metabolism following oral and percutaneous administration made [31].
• Simultaneous determination of amfepramon and its two major metabolites in biological fluids by gas liquid chromatography [32].
• The respiratory movements as well as the EEG tracings were depressed by larger doses of amphepramone [33].

References