Description

Simple

Clinical

Overview

Fenproporex is an orally active stimulant drug, which was developed in the 1960s. It is used as an appetite suppressant and a treatment for obesity. It is listed as an illicit substance in many countries due to addiction issues and listed as a prohibited substance by the World Anti-Doping Agency. Structurally, fenproporex (N-2-cyanoethylamphetamine) falls within the phenylethamine and amphetamine chemical class of drugs. The N-2-cyanoethyl substituent was once believed to be resistant to cleavage, because fenproporex -- once recommended as an obesity treatment for patients with cardiovascular disease -- was originally claimed to lack stimulant properties. Contrary to the claim, research has demonstrated easy in vivo cleavage of the N-2-cyanothyl substituent to yield amphetamine as a metabolite. [5] However, in clinical practice, central nervous system stimulative effects are less notorious than with some other agents such as diethylpropion and mazindol. [7]

In the United States fenproporex was never approved by the FDA for clinical use due to a lack of efficacy and safety data, and is listed as a drug in Schedule IV of the Controlled Substances Act. In 2006 and 2009, the FDA issued warnings that it had been detected in diet pills sold online, and imported from foreign manufacturers.

Despite being banned in the United States, fenproporex has been described as the second most commonly consumed appetite suppressant worldwide, [6] with fenproporex containing anorectics stil... Read more

Pharmacology

Indication

Fenproporex is used as an appetite suppressant, and anti-obesity agent [2]; however, due to substance abuse potential, it is an illicit substance in many countries. In some countries, such as Brazil, it is still prescribed -- often in the form of diet pills (ie. Brazilian Diet Pills) which combine a... Read more

Pharmacodynamic

Fenproporex was first claimed to not exert a stimulant effect on the body, however research into its metabolism has shown that it is converted into a considerable amount of amphetamine in the body, which leads to stimulant effects. [9]

Mechanism of action

Fenproporex is an amphetamine based anorectic which is rapidly metabolized into amphetamine in the body. Both acute and chronic fenproporex administration has been shown to increase brain energy metabolism in young rats, by increasing the activity of citrate synthase, malate dehydrogenase, succinate... Read more

Absorption

Information currently not available.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

The amphetamine metabolite can be detected for several days after the administration of forproporex (up to 119h, in one study). [2]

Half life

Information currently not available.

Route of elimination

Renally eliminated in the urine, mainly as amphetamine, but 5-9% as unchanged drug.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Fenproporex
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Abacavir
Abacavir may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Fenproporex which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Aclidinium
Fenproporex may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Fenproporex may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Albutrepenonacog alfa
Fenproporex may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Aldesleukin
Aldesleukin may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Allopurinol
Allopurinol may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Allylestrenol
Allylestrenol may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Almasilate
Fenproporex may decrease the excretion rate of Almasilate which could result in a higher serum level.
Alminoprofen
Alminoprofen may decrease the excretion rate of Fenproporex which could result in a higher serum level.
Almotriptan
Almotriptan may decrease the excretion rate of Fenproporex which could result in a higher serum level.
9 References
  1. 1 . Bray GA: A concise review on the therapeutics of obesity. Nutrition. 2000 Oct;16(10):953-60.PubMed: 11054601
  2. 2 . Cody JT, Valtier S: Detection of amphetamine following administration of fenproporex. J Anal Toxicol. 1996 Oct;20(6):425-31.PubMed: 8889679
  3. 3 . Cohen PA, McCormick D, Casey C, Dawson GF, Hacker KA: Imported compounded diet pill use among Brazilian women immigrants in the United States. J Immigr Minor Health. 2009 Jun;11(3):229-36. Epub 2007 Dec 9.PubMed: 18066718
  4. 4 . Cohen PA: Imported fenproporex-based diet pills from Brazil: a report of two cases. J Gen Intern Med. 2009 Mar;24(3):430-3. doi: 10.1007/s11606-008-0878-4.PubMed: 19096898
  5. 5 . Coutts RT, Nazarali AJ, Baker GB, Pasutto FM: Metabolism and disposition of N-(2-cyanoethyl)amphetamine (fenproporex) and amphetamine: study in the rat brain. Can J Physiol Pharmacol. 1986 Jun;64(6):724-8.PubMed: 3756624
  6. 6 . Kraemer T, Theis GA, Weber AA, Maurer HH: Studies on the metabolism and toxicological detection of the amphetamine-like anorectic fenproporex in human urine by gas chromatography-mass spectrometry and fluorescence polarization immunoassay. J Chromatogr B Biomed Sci Appl. 2000 Jan 28;738(1):107-18.PubMed: 10778932
  7. 7 . Rezin GT, Jeremias IC, Ferreira GK, Cardoso MR, Morais MO, Gomes LM, Martinello OB, Valvassori SS, Quevedo J, Streck EL: Brain energy metabolism is activated after acute and chronic administration of fenproporex in young rats. Int J Dev Neurosci. 2011 Dec;29(8):937-42. doi: 10.1016/j.ijdevneu.2011.06.007. Epub 2011 Jun 23.PubMed: 21723935
  8. 8 . Tognoni G, Morselli PL, Garattini S: Amphetamine concentrations in rat brain and human urine after fenproporex administration. Eur J Pharmacol. 1972 Oct;20(1):125-6.PubMed: 4637940
  9. 9 . Mancini MC, Halpern A: Pharmacological treatment of obesity. Arq Bras Endocrinol Metabol. 2006 Apr;50(2):377-89. Epub 2006 May 23.PubMed: 16767304