Amfepramone - General Information:

A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290)

Pharmacology:

Amfepramone 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.

Amfepramone for patients

The patient should be cautioned about concomitant use of alcohol or other CNS-active drugs and TENUATE or TENUATE DOSPAN.

The patient should be advised to observe caution when driving or engaging in any potentially hazardous activity.

Amfepramone 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.

Amfepramone 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.

Additional information about Amfepramone

Amfepramone Indication: 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.
Mechanism Of Action: Amfepramone 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. Amfepramone (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.
Drug Interactions: Acetophenazine Decreased anorexic effect, may increase psychotic symptoms
Chlorpromazine Decreased anorexic effect, may increase psychotic symptoms
Ethopropazine Decreased anorexic effect, may increase psychotic symptoms
Fluoxetine Risk of serotoninergic syndrome
Fluphenazine Decreased anorexic effect, may increase psychotic symptoms
Fluvoxamine Risk of serotoninergic syndrome
Guanethidine The agent decreases the effect of guanethidine
Isocarboxazid Possible hypertensive crisis
Mesoridazine Decreased anorexic effect, may increase psychotic symptoms
Methdilazine Decreased anorexic effect, may increase psychotic symptoms
Paroxetine Risk of serotoninergic syndrome
Perphenazine Decreased anorexic effect, may increase psychotic symptoms
Phenelzine Possible hypertensive crisis
Prochlorperazine Decreased anorexic effect, may increase psychotic symptoms
Promazine Decreased anorexic effect, may increase psychotic symptoms
Promethazine Decreased anorexic effect, may increase psychotic symptoms
Propiomazine Decreased anorexic effect, may increase psychotic symptoms
Rasagiline Possible hypertensive crisis
Thiethylperazine Decreased anorexic effect, may increase psychotic symptoms
Thioridazine Decreased anorexic effect, may increase psychotic symptoms
Tranylcypromine Possible hypertensive crisis
Trifluoperazine Decreased anorexic effect, may increase psychotic symptoms
Triflupromazine Decreased anorexic effect, may increase psychotic symptoms
Trimeprazine Decreased anorexic effect, may increase psychotic symptoms
Venlafaxine Risk of serotoninergic syndrome
Methotrimeprazine Decreased anorexic effect, may increase psychotic symptoms
Propericiazine Decreased anorexic effect, may increase psychotic symptoms
Food Interactions: Take without regard to meals.
Generic Name: Diethylpropion
Synonyms: Amfepramonum [INN-Latin]; Amfepramone Hydrochloride; Amfepramone HCL; alpha-Diethylaminopropiophenone; alpha-Benzoyltriethylamine; Amphepramonum hydrochloride; Anfepramona [INN-Spanish]; DEA No. 1610; Diethylcathinone; Diethylpropion HCL; Diethylpropione hydrochloride; Diethylpropione; Diethylpropion Hydrochloride
Drug Category: Appetite Depressants; Anorexigenic Agents; Stimulants
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Diethylpropion: Adiposon; Amfepramon; Amfepramone; Amphepramon; Amphepramone; Anfamon; Anorex; Cegramine; Danylen; Derfon; 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;
Absorption: Diethylpropion is rapidly absorbed from the GI tract after oral administration.
Toxicity (Overdose): 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.
Protein Binding: Not Available
Biotransformation: 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.
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.
Dosage Forms of Amfepramone: Tablet Oral
Tablet, extended release Oral
Chemical IUPAC Name: 2-diethylamino-1-phenylpropan-1-one
Chemical Formula: C13H19NO
Diethylpropion on Wikipedia: http://en.wikipedia.org/wiki/Diethylpropion
Organisms Affected: Humans and other mammals

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