DIETHYLPROPION

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.

Originator

Tenuate,Merrell National ,US,1959

The Uses of DIETHYLPROPION

appetite depressant;stimulating secretion of norepinephrine

Background

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)

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.

Definition

ChEBI: An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity.

Manufacturing Process

1,145 g of α-bromopropiophenone and 850 g of diethylamine are combined under stirring and heated on a water bath to boiling. The precipitate is filtered off under suction and washed with benzol. The filtrate is shaken up with aqueous hydrogen chloride, the aqueous solution made alkaline and etherified. The solution freed of the ether is fractionated. The boiling point (6 mm) is 140°C and the yield 800 g. The base is dissolved in acetic ester and precipitated with isopropanolic hydrogen chloride. After suction filtration and washing with ether the yield is found to be 750 g (80%)and the melting point 168°C.

brand name

Adiposan;Adipyn;Alipid;Amfepromone;Apisate;Bonumin;Brenalalit;Brendalit;Controlgras;D.i.p.n;Delgamer;Deramix;Dietec;Dietil retard;Dietil-retard;Lineal-plus;Lineal-rivo;Lineal-valeas;Linea-valeas;Lipomin;Liposlim;Menutil;Moderatan diffucap;Nobensin-75;Nobensine;Nobesine-25;Nulobes;Perfamone;Prefamone;Redicres;Regenon retard;Regibon;Sinapet;Slim-plus;Super emegrin;T-712;Tenuate dospan;Tenucap.

Therapeutic Function

Anorexic

World Health Organization (WHO)

Amfepramone, a phenethylamine derivative introduced in 1957, is controlled under Schedule IV of the 1971 Convention on Psychotropic Substances. It remains available in many other countries with highly evolved drug regulatory authorities as an aid to weight reduction.(Reference: (UNCPS4) United Nations Convention on Psychotropic Substances (IV), , , 1971)

Pharmacokinetics

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.

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.