Adult: Short-term adjunct in the management of exogenous cases in patients with ≥30 kg/m2 initial BMI or those unresponsive to appropriate weight reducing regimen: As immediate-release tab: 25 mg tid, given 1 hour before meals. Additional 25 mg may be given midevening, if necessary, to overcome night hunger. As extended- or controlled-release tab: 75 mg once daily, given in midmorning. Discontinue treatment if tolerance develops. Elderly: Initiate at low doses.
Administration
Should be taken on an empty stomach. Take 1 hr before meals.
Contraindications
Advanced arteriosclerosis, hyperthyroidism, severe hypertension, pulmonary hypertension, glaucoma, agitated states; history of drug abuse. Concomitant use with other anorectic agents; during or within 14 days of discontinuing MAOI.
Special Precautions
Patient with hypertension or symptomatic CV disease, including arrhythmias; pre-existing psychosis or bipolar disorders, history of seizure disorders, Tourette’s syndrome, diabetes mellitus. Renal and hepatic impairment. Elderly. Pregnancy and lactation. Not recommended for use in patients who have used other anorectic agents within the prior year. Avoid abrupt withdrawal.
Adverse Reactions
Significant: Heart failure, valvular heart disease, new-onset psychosis or mania, toxic psychosis, induction of mixed/manic episodes, hallucinations (high doses), increased convulsions, CNS effects; drug abuse, tolerance, or dependence (prolonged use); withdrawal symptoms. Rarely, cardiac valvulopathy. Blood and lymphatic system disorders: Agranulocytosis, leucopenia. Cardiac disorders: Arrhythmia, tachycardia, palpitation, precordial pain, dyspnoea. Eye disorders: Blurred vision, mydriasis. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, constipation abdominal discomfort, dysgeusia, xerostomia. General disorders and administration site conditions: Malaise, jitteriness. Investigations: ECG changes. Musculoskeletal and connective tissue disorders: Myalgia. Nervous system disorders: Headache, drowsiness, dizziness, restlessness, dyskinesia, tremor, cerebrovascular accident. Psychiatric disorders: Insomnia, anxiety, euphoria, depression, nervousness, dysphoria. Renal and urinary disorders: Dysuria, polyuria. Reproductive system and breast disorders: Impotence, gynaecomastia, changes in libido, menstrual irregularity. Skin and subcutaneous tissue disorders: Rash, urticaria, erythema, ecchymoses, alopecia, increased sweating. Vascular disorders: Hypertension. Potentially Fatal: Primary pulmonary hypertension.
This drug may cause CNS effects that may impair your mental alertness or physical coordination; if affected, do not drive or operate machinery.
Monitoring Parameters
Perform baseline cardiac evaluation to detect pulmonary hypertension or pre-existing valvular heart disease before treatment initiation. Monitor echocardiogram during and after treatment; blood pressure, heart rate, weight, waist circumference, renal function (in elderly).
Overdosage
Symptoms: Restlessness, confusion, hallucinations, panic states, hyperreflexia, tremor, mydriasis, tachycardia, hyper- or hypotension, arrhythmia, circulatory collapse, nausea, vomiting, abdominal cramps, and diarrhoea. Management: Symptomatic treatment. May perform gastric lavage or give barbiturate to induce sedation. May consider IV phentolamine for acute severe hypertension.
Drug Interactions
Effects may be potentiated by sedatives. May cause arrhythmias with general anaesthetics. May alter the drug requirements of antidiabetics (e.g. insulin). May interfere with the effects of antihypertensives (e.g. guanethidine, α-methyldopa). Anorectic effects may be antagonised by phenothiazines.
Potentially Fatal: May increase risk of serious cardiac problems with other anorectic agents (e.g. sibutramine). Increased risk of hypertensive crises with MAOIs.
Food Interaction
Effects may be potentiated by alcohol.
Action
Description: Mechanism of Action: Amfepramone is a central stimulant and indirect-acting sympathomimetic amine with properties similar to amphetamines. Its anorexigenic activity is possibly secondary to CNS effects, including hypothalamus stimulation to release norepinephrine.
Synonym: diethylpropion. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Distribution: Crosses the blood-brain barrier and placenta, enters breast milk. Metabolism: Extensively metabolised in the liver via N-dealkylation and reduction into active metabolites. Excretion: Mainly via urine (>75%; 64-67% as metabolites, 3-6% as unchanged drug). Elimination half-life: Approx 4-6 hours (aminoketone metabolites).
Chemical Structure
Amfepramone Source: National Center for Biotechnology Information. PubChem Database. Diethylpropion, CID=7029, https://pubchem.ncbi.nlm.nih.gov/compound/7029 (accessed on June 25, 2020)
Anon. Diethylpropion. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/06/2020.Anon. Diethylpropion. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/06/2020.Buckingham R (ed). Diethylpropion Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/06/2020.Diethylpropion Hydrochloride Extended-Release Tablets (Lannett Company, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/06/2020.Diethylpropion Hydrochloride Immediate-Release Tablets (NuCare Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/06/2020.Diethylpropion. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com/. Accessed 05/06/2020.Tenuate Immediate-Release 25 mg Tablets and Tenuate Dospan Controlled-Release 75 mg Tablets (Merrell Pharmaceuticals Inc. An Aventis Pharmaceuticals Company). U.S. FDA. https://www.fda.gov/. Accessed 05/06/2020.
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