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Trade Names:
Diethylpropion Hydrochloride
- Tablets 25 mg
- Tablets, sustained-release 75 mg

Mechanism of Action

Pharmacology

Stimulates satiety center in brain, causing appetite suppression.

Pharmacokinetics

Absorption

Rapidly absorbed.

Distribution

Crosses the blood-brain barrier and the placenta.

Metabolism

Extensively metabolized, involving N-dealkylation and reduction, to many active metabolites.

Elimination

75% to 100% excreted in the urine. Plasma t _½ of aminoketone metabolites is 4 to 6 h.

Indications and Usage

Short-term (few weeks) adjunct to diet plan to reduce weight.

Contraindications

Advanced arteriosclerosis; symptomatic cardiovascular disease; moderate to severe hypertension; hyperthyroidism; hypersensitivity to sympathomimetic amines; glaucoma; agitated states; history of drug abuse; concurrent use with or within 14 days of MAOI; coadministration with other CNS stimulants.

Dosage and Administration

PO Immediate-release tablets 25 mg 3 times daily, 1 h before meals; Sustained-release tablets 75 mg once daily, in mid-morning. Do not crush or open sustained-release tablets.

Drug Interactions

May decrease hypotensive effect.

Hypertensive crisis and intracranial hemorrhage may occur.

Sympathomimetic effects of diethylpropion may be increased; increased risk of serotonin syndrome.

May decrease anorexiant effect.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations; tachycardia; arrhythmias; hypertension; hypotension.

CNS

Overstimulation; dizziness; insomnia; euphoria; tremor; headache.

Dermatologic

Excessive sweating; flushing.

EENT

Mydriasis; blurred vision.

GI

Dry mouth; unpleasant taste; nausea; diarrhea; constipation; stomach pain.

Genitourinary

Dysuria; urinary frequency; impotence; menstrual disturbances.

Hematologic

Bone marrow depression; agranulocytosis; leukopenia.

Miscellaneous

Hair loss; myalgia; gynecomastia; allergic reactions (eg, urticaria; rash; erythema).

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Not recommended in children younger than 16 yr of age.

CV effects

Diethylpropion may cause or aggravate hypertension or arrhythmias.

Convulsions

Diethylpropion may aggravate convulsions; dose titration or discontinuance may be necessary.

Drug dependence

Related to amphetamine; has abuse potential.

Tolerance

Tolerance may occur.

Overdosage

Symptoms

Restlessness, tremor, hyperreflexia, fever, tachypnea, dizziness, panic, aggression, hallucinations, seizure, coma, arrhythmias, hypotension, hypertension, death.

Patient Information

• Explain potential for increased agitation, palpitations, and dizziness, and identify precaution to take when performing tasks that require physical coordination or mental concentration.
• Tell patient to record weight weekly.
• Explain that drug will make patient feel less hungry and thus make it easier to adhere to diet but that weight loss will occur only with calorie reduction and increased physical activity.
• Instruct patient on missed medication procedure: if less than 2 h, take medication; if more than 2 h, wait until next scheduled dose. Do not double up on medication.
• Advise patient to limit intake of coffee, tea, cocoa, chocolate, and caffeinated soft drinks.
• Identify techniques to prevent or treat dry mouth.