Alpha-Diethylaminopropiophenone

Uses

Alpha-Diethylaminopropiophenone is an appetite suppressant used for the short term treatment of exogenous obesity in addition to calorie restriction.

Used in the management of exogenous obesity as a short-term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction.

Alpha-Diethylaminopropiophenone is also used to associated treatment for these conditions: Exogenous Obesity

How Alpha-Diethylaminopropiophenone works

Alpha-Diethylaminopropiophenone is an amphetamine that stimulates neurons to release or maintain high levels of a particular group of neurotransmitters known as catecholamines; these include dopamine and norepinephrine. High levels of these catecholamines tend to suppress hunger signals and appetite. Alpha-Diethylaminopropiophenone (through catecholamine elevation) may also indirectly affect leptin levels in the brain. It is theorized that diethylpropion can raise levels of leptin which signal satiety. It is also theorized that increased levels of the catecholamines are partially responsible for halting another chemical messenger known as neuropeptide Y. This peptide initiates eating, decreases energy expenditure, and increases fat storage.

Toxicity

The reported oral LD₅₀ for mice is 600 mg/kg, for rats is 250 mg/kg and for dogs is 225 mg/kg. Manifestation of acute overdosage include restlessness, tremor, hyperreflexia, rapid respiration, confusion, assaultiveness, hallucinations, and panic states.

Food Interaction

• Take with or without food. The absorption is unaffected by food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate the central nervous system and cardiovascular effects of centrally-acting appetite suppressants.

In one study, concurrent administration of methamphetamine (30 mg intravenously) and ethanol (1 gm

This increases cardiac work and myocardial oxygen consumption, which may lead to more adverse cardiovascular effects than either agent alone.

Subjective effects of ethanol were diminished in the eight study subjects, but those of methamphetamine were not affected.

The pharmacokinetics of methamphetamine were also unaffected except for a decrease in the apparent volume of distribution at steady state.

MANAGEMENT: Concomitant use of centrally-acting appetite suppressants and alcohol should be avoided if possible, especially in patients with a history of cardiovascular disease.

Patients should be counselled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Alpha-Diethylaminopropiophenone Hypertension interaction

[Major] The use of CNS stimulants is contraindicated in patients with significant cardiovascular impairment such as uncompensated heart failure, severe coronary disease, severe hypertension (including that associated with hyperthyroidism or pheochromocytoma), cardiac structural abnormalities, serious arrhythmias, etc.

Sudden death has been reported in adults and children taking CNS stimulant treatment.

Additionally, stroke, myocardial infarction, chest pain, syncope, arrhythmias and other symptoms have been reported in adults under treatment.

A careful assessment of the cardiovascular status should be done in patients being considered for treatment.

This includes family history, physical exam and further cardiac evaluation (EKG and echocardiogram).

Patients who develop symptoms should have a detailed cardiac evaluation and if needed, treatment should be suspended.

[Major] CNS stimulant medications have shown to increase blood pressure, and their use might be contraindicated in patients with severe hypertension.

Caution should be used when administering to patients with preexisting high blood pressure and other cardiovascular conditions.

All patients under treatment should be regularly monitored for changes in blood pressure and heart rate.

Alpha-Diethylaminopropiophenone Drug Interaction

Major: escitalopram, escitalopramModerate: levothyroxine, levothyroxineUnknown: diphenhydramine, diphenhydramine, pregabalin, pregabalin, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, ergocalciferol, ergocalciferol, cholecalciferol, cholecalciferol, alprazolam, alprazolam, cetirizine, cetirizine

Alpha-Diethylaminopropiophenone Disease Interaction

Major: cardiovascular, glaucoma, agitation, cardiac disease, hypertension, liver disease, psychiatric disorders, pulmonary hypertension, substance abuse, ticsModerate: bipolar disorders, psychotic disorders, renal dysfunction, seizure disorders, diabetics

Elimination Route

Alpha-Diethylaminopropiophenone is rapidly absorbed from the GI tract after oral administration.

Half Life

Using a phosphorescence assay that is specific for basic compounds containing benzoyl group, the plasma half-life of the aminoketone metabolites is estimated to be between 4 to 6 hours.

Elimination Route

Alpha-Diethylaminopropiophenone is rapidly absorbed from the GI tract after oral administration and is extensively metabolized through a complex pathway of biotransformation involving N-dealkylation and reduction. Alpha-Diethylaminopropiophenone and/or its active metabolites are believed to cross the blood-brain barrier and the placenta. Alpha-Diethylaminopropiophenone and its metabolites are excreted mainly by the kidney.

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