Diethylpropion Hydrochloride

DIETHYLPROPION HYDROCHLORIDE- diethylpropion hydrochloride tablet
PD-Rx Pharmaceuticals, Inc.

CIV Rx only

DESCRIPTION

Diethylpropion Hydrochloride Tablets USP, 25 mg are available for oral administration as tablets containing 25 mg diethylpropion hydrochloride, USP. The inactive ingredients in each tablet are: microcrystalline cellulose, lactose monohydrate, mannitol, tartaric acid, povidone, talc, and zinc stearate.

Diethylpropion hydrochloride is a sympathomimetic agent. The chemical name for diethylpropion hydrochloride is 1-phenyl-2-diethyl-amino-1-propanone hydrochloride.

Its chemical structure is:

diethylpropion-molec-structure
(click image for full-size original)

CLINICAL PHARMACOLOGY

Diethylpropion hydrochloride is a sympathomimetic amine with some pharmacologic activity similar to that of the prototype drugs of this class used in obesity, the amphetamines. Actions include some central nervous system stimulation and elevation of blood pressure. Tolerance has been demonstrated with all drugs of this class in which these phenomena have been looked for.

Drugs of this class used in obesity are commonly known as “anorectics” or “anorexigenics”. It has not been established, however, that the action of such drugs in treating obesity is primarily one of appetite suppression. For example, other central nervous system actions or metabolic effects may be involved.

Adult obese subjects instructed in dietary management and treated with “anorectic” drugs lose more weight on the average than those treated with placebo and diet, as determined in relatively short-term clinical trials.

The magnitude of increased weight loss of drug-treated patients over placebo-treated patients averages some fraction of a pound a week. However, individual weight loss may vary substantially from patient to patient. The rate of weight loss is greatest in the first weeks of therapy for both drug and placebo subjects and tends to decrease in succeeding weeks. The possible origins of the increased weight loss due to the various drug effects are not established. The amount of weight loss associated with the use of an “anorectic” drug varies from trial to trial, and the increased weight loss appears to be related in part to variables other than the drug prescribed, such as the physician/investigator relationship, the population treated, and the diet prescribed. Studies do not permit conclusions as to the relative importance of the drug and non-drug factors on weight loss.

The natural history of obesity is measured in years, whereas most studies cited are restricted to a few weeks duration; thus, the total impact of drug-induced weight loss over that of diet alone is unknown.

Diethylpropion 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. Many of these metabolites are biologically active and may participate in the therapeutic action of diethylpropion hydrochloride tablets USP, 25 mg. Due to the varying lipid solubilities of these metabolites, their circulating levels are affected by urinary pH. Diethylpropion and/or its active metabolites are believed to cross the blood-brain barrier and the placenta.

Diethylpropion and its metabolites are excreted mainly by the kidney. It has been reported that between 75-106% of the dose is recovered in the urine within 48 hours after dosing. 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.

INDICATIONS AND USAGE

Diethylpropion hydrochloride tablets USP, 25 mg are indicated in the management of exogenous obesity as a short-term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction in patients with an initial body mass index (BMI) of 30 kg/m 2 or higher and who have not responded to appropriate weight reducing regimen (diet and/or exercise) alone. Below is a chart of BMI based on various heights and weights. BMI is calculated by taking the patient’s weight, in kilograms (kg), divided by the patient’s height, in meters (m), squared. Metric conversions are as follows: pounds divided by 2.2 = kg; inches × 0.0254 = meters.

Body Mass Index (BMI), kg/m 2
Weight (pounds) Height (feet, inches)
5’0″ 5’3″ 5’6″ 5’9″ 6’0″ 6’3″
140 27 25 23 21 19 18
150 29 27 24 22 20 19
160 31 28 26 24 22 20
170 33 30 28 25 23 21
180 35 32 29 27 25 23
190 37 34 31 28 26 24
200 39 36 32 30 27 25
210 41 37 34 31 29 26
220 43 39 36 33 30 28
230 45 41 37 34 31 29
240 47 43 39 36 33 30
250 49 44 40 37 34 31

The usefulness of agents of this class (See CLINICAL PHARMACOLOGY) should be measured against possible risk factors inherent in their use such as those described below. Diethylpropion hydrochloride tablets USP, 25 mg are indicated for use as monotherapy only.

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