Amfepramone

Should be taken on an empty stomach.

Known hypersensitivity or idiosyncrasy to amfepramone or other sympathomimetic amines. Advanced arteriosclerosis, severe hypertension, hyperthyroidism, pulmonary hypertension, glaucoma, agitated states, history of drug abuse. Concomitant use with other anorectic drugs. Concurrent use with or within 14 days of discontinuing MAOIs.

Patient with diabetes mellitus, hypertension, other CV conditions (e.g. arrhythmias); pre-existing psychosis, bipolar disorder, history of seizure disorders, Tourette's syndrome. Not recommended in patients with known heart murmur or valvular heart disease. Not recommended for use in patients who have used other anorectic agents within the prior year. Avoid abrupt withdrawal. Renal impairment. Elderly. Pregnancy and lactation.

Significant: May cause direct myocardial toxicity (e.g. heart failure), valvular heart disease; CNS effects, exacerbation of behaviour and thought disorder symptoms, induction of mixed/manic episodes, increased risk of seizures; drug dependence or abuse (prolonged use); withdrawal syndrome (following abrupt discontinuation).
Blood and lymphatic system disorders: Leucopenia, agranulocytosis.
Cardiac disorders: Cardiac arrhythmia, palpitation, tachycardia.
Eye disorders: Blurred vision, mydriasis.
Gastrointestinal disorders: Abdominal distress, nausea, vomiting, diarrhoea, constipation, dysgeusia, xerostomia.
General disorders and administration site conditions: Malaise, jitteriness.
Investigations: ECG changes.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Dizziness, drowsiness, headache, tremor, dyskinesia, restlessness.
Psychiatric disorders: Anxiety, depression, dysphoria, insomnia.
Renal and urinary disorders: Dysuria, polyuria.
Reproductive system and breast disorders: Changes in libido, gynaecomastia, menstrual irregularity, impotence.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Alopecia, erythema, rash, diaphoresis, urticaria.
Vascular disorders: Hypertension.
Potentially Fatal: Rarely, primary pulmonary hypertension.

PO: B

This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery.

Perform baseline cardiac evaluation for pre-existing valvular heart disease and pulmonary hypertension before treatment initiation. Monitor echocardiogram during therapy; weight, waist circumference, and blood pressure.

Symptoms: Restlessness, confusion, panic states, hallucinations, hyperreflexia, tremor, mydriasis, nausea, vomiting, abdominal cramps, diarrhoea, rapid respiration, tachycardia, hyper- or hypotension, arrhythmia, and circulatory collapse. Management: Symptomatic treatment. May perform gastric lavage or give a barbiturate to induce sedation. May consider IV phentolamine for acute severe hypertension.

May lead to arrhythmias when given with anaesthetics. May alter the drug requirement of antidiabetics (e.g. insulin). Anorectic effect may be antagonised by phenothiazines. May interfere with the effects of antihypertensive agents (e.g. guanethidine, methyldopa). Enhanced CNS effects with sedatives.
Potentially Fatal: Increased risk of hypertensive crisis with MAOIs. May increase the risk of serious cardiac problems with other anorectic agents (e.g. sibutramine).

Enhanced CNS effects with alcohol.

Description:
Mechanism of Action: Amfepramone, an amfetamine congener, is a central stimulant and indirect-acting sympathomimetic amine. Its anorectic effect appears to be secondary to CNS effects, including stimulation of the hypothalamus to release norepinephrine.
Synonym(s): Diethylpropion.
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract.
Distribution: Crosses the blood-brain barrier and placenta; enters breastmilk.
Metabolism: Extensively metabolised in the liver via N-dealkylation and reduction to form active metabolites.
Excretion: Via urine. Elimination half-life: Approx 4-6 hours (aminoketone metabolites).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 7029, Diethylpropion. https://pubchem.ncbi.nlm.nih.gov/compound/Diethylpropion. Accessed Jan. 30, 2025.

Store between 20-25°C. Protect from excessive heat.

Anti-Obesity Agents

A08AA03 - amfepramone ; Belongs to the class of centrally acting antiobesity products. Used in the treatment of obesity.

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Diethylpropion Hydrochloride Tablet (Chartwell RX, LLC.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/10/2024.

Diethylpropion Hydrochloride Tablet, Extended Release (Chartwell RX, LLC.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/10/2024.

Diethylpropion Hydrochloride Tablet, Extended Release (Lannett Company, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/10/2024.

Diethylpropion. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 08/10/2024.