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At least 19 recordsLinked to original sources
PubMed1979

The roles of brain noradrenaline and dopamine in the anorectic activity of diethylpropion in rats: a comparison with d-amphetamine.

The anorectic activity of diethylpropion and d-amphetamine was studied in rats subjected to various treatments known to affect brain monoamines. The effect of diethylpropion, like that of d-amphetamine, was completely prevented by a lesion of the ventral noradrenergic bundle, which selectively decreases brain noradrenaline, but was not significantly modified in desipramine pretreated rats by an intraventricular injection of 6-hydroxydopamine, a condition decreasing only dopamine. Pretreatment with penfluridol significantly reduced the effect of d-amphetamine but not that of diethylpropion. A non-significant reduction of drug effect was found with alpha-methyl-p-tyrosine. Lesion of the nucleus medianus raphe, which destroys central serotonin neurons, or treatment with methergoline, a central serotonin antagonist, caused no changes in the effects of both compounds. The findings show that integrity of central noradrenergic neurons is an important condition for diethylpropion and d-amphetamine to exert their anorectic effect. Dopamine does not seem to play any role in the effect of diethylpropion but might contribute to that of d-amphetamine. The data are against any involvement of brain serotonin in diethylpropion anorexia.

Animals↗
PubMed1975

A comparison of mazindol (Teronac) with diethylpropion in the treatment of exogenous obesity.

Fifty obese patients were entered into a 12-week parallel group study of mazindol with diethylpropion in a general practice group. Both drugs produced weight loss, but patients on mazindol lost 19.9 lbs in 12 weeks, while those on diethylpropion lost 11.6 lbs, a statistically significant difference (p less than 0.01). At each visit during the trial, patients had lost more weight with mazindol, but this was only significant statistically in the period 8-12 weeks (p less than 0.01). Patients developed tolerance to the effect of diethylpropion in the last period (8-12 weeks) but this was not evident in those patients taking mazindol. The number of side-effects was less in the mazindol group and mainly of an adrenergic, peripheral type, while those in the diethylpropion group are mainly of the central stimulant type.

Adult↗
PubMed1979

Diethylpropion and paranoid psychosis.

The case of a 36-year old woman who developed a paranoid psychosis while abusing diethylpropion is reported. It is suggested that the newer appetite-suppressing drugs have a bigger abuse potential than eas previously thought and may therefore be a hazard for a minority of susceptible subjects. The need to test separately for diethylpropion in cases of suspected drug-induced psychosis is emphasized.

Adult↗
PubMed1978

Effects of intravenous cocaine, diethylpropion, d-amphetamine and perphenazine on responding maintained by food delivery and shock avoidance in rhesus monkeys.

The effects of perphenazine, cocaine, diethylpropion and d-amphetamine on responding maintained by both food delivery and electric shock avoidance were determined using a multiple schedule of reinforcement in rhesus monkeys. This schedule had three components, each separated by a timeout: a fixed-ratio schedule of food delivery, a schedule of spaced responding (differential reinforcement of low rates) maintained by food delivery and a fixed-ratio schedule of shock avoidance. Control rates of responding on both ratio schedules were similar and were high relative to the low rates generated by the schedule of spaced responding. Perphenazine decreased rates on all three schedules in a dose-dependent fashion. All three psychomotor stimulants decreased food-maintained ratio responding at doses which had little effect on or increased rates of shock avoidance. Except for diethylpropion and d-amphetamine in one animal in which rates were increased, low rates of spaced responding were also decreased.

Animals↗
PubMed1977

High-performance liquid chromatographic determination of diethylpropion hydrochloride in tablets: isolation and identification of two decomposition products.

A rapid assay was developed for diethylpropion hydrochloride tablets using high-performance liquid chromatography (HPLC) with UV detection. This technique provided separation of the drug from other UV-absorbing components present as the result of decomposition. A major decomposition product detected by HPLC in extracts of tablets and of the cotton filler from a tablet bottle was collected from the column effluents. This product was subsequently identified as 1-phenyl-1,2-propanedione, a highly volatile compound. A second decomposition product, isolated from decomposed drug by distillation from alkaline solution, was identified as diethylamine, apparently present as the hydrochloride salt, GLC, UV, IR, NMR, and mass spectrometry were used to confirm the identity of the decomposition products. HPLC assay results compared favorably with results of the NF assay; the latter procedure separated the drug from 1-phenyl-1,2-propanedione via liquid-liquid extraction.

Chromatography, Gas↗
PubMed1978

A double-blind controlled study of the use of diethylpropion hydrochloride (Tenuate) in obese patients in a rural practice.

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. TD was found to produce significantly more weight loss than placebo and side effects were not significantly greater. The need for the treatment of obese patients in general practice is discussed, as is the role of anorexiant therapy.

Diethylpropion↗
PubMed1979

[Weight reduction in obese diabetics: a double-blind study of diethylpropionate (author's transl)].

In a double-blind study 40 overweight maturity-onset diabetics on a weight-reducing diet were randomly assigned to treatment with either the appetite-suppressant diethylpropion hydrochloride (Tenuate), or placebo. After treatment for 8 weeks the mean weight loss achieved by each group was 4.9 and 3.3%, respectively. This approximately equal weight loss was too slight to exert any significant effect on glucose tolerance. Thus, an additional effect of this anorexiant in comparison with diet restriction alone, as described in obese non-diabetic subjects, is not evident in the case of obese diabetic patients.

Clinical Trials as Topic↗
PubMed1976

Self-administration of psychomotor stimulant drugs: the effects of unlimited access.

Rhesus monkeys surgically prepared with intravenous catheters were given 23 hr daily access to injection of either cocaine, d-amphetamine, 1-amphetamine, d-methamphetamine or diethylpropion on a fixed ratio 1 schedule of reinforcement for a maximum of 30 days. Responding was maintained by all these drugs but showed both day-to-day and hour-to-hour variability. The two animals self-administering 0.2 mg/kg/infusion cocaine died in less than 5 days. All 6 animals given access to 0.05 mg/kg/infusion d-amphetamine or 0.025 mg/kg/infusion d-methamphetamine also died, but tended to survive more days than animals exposed to cocaine. Three of the 5 animals whose responding was maintained by 0.5 mg/kg/infusion diethylpropion and one of the two animals whose responding was maintained by 0.05 mg/kg/infusion 1-amphetamine survived the entire 30 days despite high rates of intake. Food intake was initially decreased, but often returned to predrug levels and was not related to level of drug intake.

Amphetamine↗
PubMed1976

Anorectic drugs: use in general practice.

The treatment of obesity is one of the major measures available today in the field of preventive medicine. In particular, the coronary epidemic of Western civilisation would be halted, and most cases of maturity-onset diabetes prevented, if obesity were to be treated effectively. Anorectic drugs act mainly on the satiety centre in the hypothalamus to produce anorexia. They also have various metabolic effects involving fat and carbohydrate metabolism, but many of these may be secondary to loss of weight. Most of the drugs are related directly or indirectly to amphetamine and in addition act by increasing general physical activity. Anorectic drugs tend to lose their effect after some months, and part of this reduction in effect may be due to chemical alterations produced by the drugs in the brain. All the drugs, with the exception of fenfluramine, have a stimulant effect on the central nervous system in some individuals, resulting in restlessness and nervousness, irritability and insomnia. Fenfluramine commonly produces drowsiness in normal doses, but has stimulant effects with overdosage. Dexamphetamine, phenmetrazine and benzphetamine all tend to cause euphoria and the risk of addiction is therefore considerable. Euphoria occasionally occurs with diethylpropion, phentermine and chlorphentermine, but to a much lesser extent. Side-effects also occur due to sympathetic stimulation and gastro-intestinal irritation. These side-effects may cause some individuals to stop taking the drug, but are never serious or dangerous. Drug interactions may occur with monoamine oxidase inhibitors and to a clinically unimportant extent, with antihypertensive drugs. The anorectic drugs have a very definite part to play in the treatment of obesity, mainly for those individuals who have altered their eating habits but have come to a plateau of weight which they find difficult to get below. The drugs are best given in a long-acting form and can safely be continued as long as weight loss persists, provided that the clinician exercises careful supervision. Dexamphetamine, phenmetrazine and benzphetamine should rarely be used because of the danger of addiction, and chlorphentermine is potentially hazardous for long-term use. Diethylpropion emerges as the drug of first choice, as fenfluramine has a tendency to cause depression and has a higher incidence of side-effects. Fenfluramine is mainly useful for people who are especially tense and for obese maturity-onset diabetics who have been unable to lose weight with the biguanides. Mazindol and phentermine appear to be useful as alternative drugs.

Adipose Tissue↗
PubMed1976

Comparison of behavior maintained by infusions of eight phenylethylamines in baboons.

Doses of eight phenylethylamines were substituted for cocaine on a drug-maintained behavior baseline in baboons. Intravenous infusions of drug were contingent upon completion of 160 lever presses (a 160-response fixed-ratio schedule; FR 160). A 3-h time-out period followed each infusion, permitting a maximum of 8 infusions per day. Fenfluramine was the only drug that did not maintain self-infusion performance at any dose tested. d-Amphetamine was approximately 10 times more potent than phentermine, phenmetrazine or diethylpropion, and 20 to 30 times more potent than methylenedioxyamphetamine (MDA), clortermine or chlorphentermine, in maintaining self-infusion behavior. Some doses of d-amphetamine and phentermine produced a cyclic pattern of drug intake over days. Increasing self-infused doses of all drugs produced a substantial suppression of concurrent food-maintained behavior. There was no clear relation between the potency of the phenylethylamines in maintaining self-infusion performance and the potency in suppressing food-maintained behavior which indicates that different mechanisms may underlie the two effects. Examination of chemical structures indicates that substitution on the phenyl ring may decrease the potency of phenylethylamines in maintaining self-infusion behavior.

3,4-Methylenedioxyamphetamine↗
PubMed1979

The effect of propranolol phentolamine and pimozide on drug-induced anorexia in the mouse.

Pimozide was a potent antagonist of (+)amphetamine, diethylpropion, mazindol and phentermine anorexia in the mouse. Phentolamine and propranolol produced no such antagonism, but either potentiated or had no effect on the drug-induced anorexia. Although the mechanism of action of the four anorectic agents appears to involve dopamine receptor agonist activity, an antagonist or partial agonist effect at noradrenergic receptors may also be involved.

Animals↗
PubMed1978

Treatment of obesity: cost-benefit assessment of behavioral therapy, placebo, and two anorectic drugs.

Mazindol, diethylpropion, and a placebo were compared with behavioral therapy for effectiveness in producing weight reduction in an outpatient obesity clinic. Each method was also compared in cost and harmful side effects. The patients were recruited from the middle and lower socioeconomic groups. Of the 120 patients beginning treatment, only 33 completed the entire 14-week study. There was no statistically significant difference in the weight loss among the treatment groups. The program of behavioral therapy was administered by a dietitian who as experienced in the techniques of behavior modification; the drug treatment groups were seen by physicians. We conclude that behavioral therapy may be the treatment of choice in an outpatient obese population since it requires little physician time, is less expensive, and avoids the side effects of anorectic drugs.

Appetite Depressants↗