Amfepramone is an indirect alpha-sympathomimetic and is used in Germany as an appetite suppressant. Because of a not inconsiderable potential for abuse, the active ingredient is prescribed only in urgent cases for a short time for the supportive treatment of obesity.
What is amfepramone?
Because of a not insignificant potential for abuse, the drug is prescribed for short periods only in urgent cases for the supportive treatment of obesity. Amfepramone is also known as 2-diethylamino-1-phenylpropan-1-one, 2-diethylaminopropiophenone, amfepramonum, or diethylpropion. It belongs to the group of phenylethylamine derivatives. These are chemical compounds derived from phenylethylamine. Phenylethylamines are widely distributed in nature (for example, the neurotransmitter dopamine or the amino acid-like substance tyramine) or are produced artificially (for example, certain amphetamines). Among the phenylethylamines, amfepramone belongs to the cathinone subgroup. Cathinones are named after the compound cathinone, which belongs to the amphetamines and has a stimulating effect. Amfepramone also acts as a stimulant and stimulates the sympathetic nervous system, a part of the autonomic (vegetative) nervous system. It is classified as an alpha-sympathomimetic. It is commercially available as a prescription drug under the trade names Regenon and Tenuate. In Germany, amfepramone falls under the Narcotics Act, but it is marketable and may be prescribed by a physician.
Pharmacologic action
Alpha-sympathomimetics (also known as alpha-adrenoceptor agonists) act on the autonomic nervous system. This is also called the involuntary or autonomic nervous system because it cannot be influenced voluntarily. The active ingredients stimulate a specific part of this nervous system, the sympathetic nervous system. Amfepramone acts as an indirect alpha sympathomimetic. While direct alpha-sympathomimetics mimic the action of adrenaline by binding to the same receptors, indirect alpha-sympathomimetics lead to a release of dopamine and norepinephrine These then stimulate the sympathetic nervous system. In this way, amfepramone stimulates the cardiovascular system and certain organs, but also has a central nervous effect by crossing the blood–brain barrier on brain activity. As a result, the active ingredient briefly boosts physical and mental performance and increases alertness. Blood flow to the lungs, blood pressure and heart rate increase. In addition, amfepramone suppresses feelings of fatigue, inhibits thirst, and (via a target localized in the hypothalamus) causes a decrease in food intake and appetite. Because of its multiple effects on the whole organism, a prescription for amfepramone will be weighed very carefully by the physician to avoid adverse effects.
Medicinal use and application
Alpha-sympathomimetics are used as anorectics (appetite suppressants), among other uses. Amfepramone is used for supportive treatment in patients with overweight (obesity) whose body mass index (BMI) is greater than 30. BMI is calculated using the following formula: BMI = body weight in kilograms / (height in meters)2. However, the agent should only be used if other appropriate weight reduction measures have not been successful. In patients who have been unable to achieve weight loss through dieting and exercise, but who urgently need to lose weight for medical reasons, the physician may opt for short-term treatment with amfepramone. Because it is a central nervous anorectic, side effects are common and there is a potential for abuse. In summer 2001, the German Federal Institute for Drugs and Medical Devices (BfArM) withdrew approval for appetite suppressants containing amfepramone due to side effects. The manufacturers successfully appealed against this decision. The preparations have been back on the market since 2004. However, their efficacy for actual, long-term weight reduction is disputed. Therefore, amfepramone is now prescribed only in individual cases and is generally used only for short-term treatment of obesity.
Risks and side effects
Amfepramone (like many alpha-sympathomimetics) has a not insignificant potential for abuse and dependence. For this reason, it was classified as a narcotic and included in Schedule 3 of the German Narcotics Act (narcotics that can be marketed and prescribed).The German BfArM and other EU drug authorities explicitly point out the low medical benefit in relation to the serious side effects. Side effects included psychosis, depression, hallucinations, agitation, sleep disturbances, palpitations, hypertension, dizziness, and lightheadedness. Amfepramone also appears to promote the development of pulmonary arterial hypertension. Some patients may experience dangerous cardiac arrhythmias, including myocardial infarction or cardiac arrest, during treatment with amfepramone. Prolonged use of amfepramone may cause dependence and withdrawal symptoms may occur after discontinuation of the drug.
