Brands, Medical Use, Clinical Data
Drug Category
- Appetite Depressants
- Anorexigenic Agents
- Stimulants
Dosage Forms
- 25 mg tablets and 75 mg controlled-release tablets.
Brands / Synonyms
Adiposon; alpha-Benzoyltriethylamine; alpha-Diethylaminopropiophenone
; Amfepramon; Amfepramone; Amfepramone HCL; Amfepramone Hydrochloride; Amfepramonum [INN-Latin]; Amphepramon; Amphepramone; Amphepramonum hydrochloride; Anfamon; Anfepramona [INN-Spanish]; Anorex; Cegramine; Danylen; DEA No. 1610; Derfon; Diethylpropion HCL; Diethylpropion Hydrochloride; Diethylpropione; Diethylpropione hydrochloride; Dobesin; Frekentine; Keramik; Keramin; Magrene; Moderatan; Modulor; Neobes; Nopropiophenone; Obesitex; Parabolin; Prefamone; Regenon; Regenon hydrochloride; Reginon; Silutin; Tenuate; Tenuate Dospan; Tenuate hydrochloride; Tepanil; Tepanil Ten-tab; Tylinal
Indications
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.
Pharmacology
Diethylpropion is a sympathomimetic stimulant drug marketed as an appetite suppressant. Chemically, it is the N,N-diethyl analog of cathinone. Its mechanism of action is similar to other appetite suppressants such as sibutramine, phentermine and dextroamphetamine.
Mechanism of Action
Diethylpropion 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. Diethylpropion (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.
Absorption
Diethylpropion is rapidly absorbed from the GI tract after oral administration.
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.
Biotrnasformation / Drug Metabolism
Extensively metabolized through a complex pathway of biotransformation involving N-dealkylation and reduction. Many of these metabolites are biologically active and may participate in the therapeutic action of diethylpropion.
Contraindications
Advanced arteriosclerosis, hyperthyroidism, known hypersensitivity or idiosyncrasy to the sympathomimetic amines,
glaucoma, severe hypertension.
Agitated states.
Patients with a history of drug abuse.
During or within 14 days following the administration of monoamine oxidase inhibitors, hypertensive crises may
result.
Drug Interactions
Antidiabetic drug requirements (i.e., insulin) may be altered. Concurrent use with general anesthetics may result
in arrhythmias. The pressor effects of diethylpropion and those of other drugs may be additive when the drugs are
used concomitantly; conversely, diethylpropion may interfere with antihypertensive drugs (i.e., guanethidine,
a-methyldopa). Concurrent use of phenothiazines may antagonize the anorectic effect of
diethylpropion.
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