Flephedrone belongs to the cathinone family of drugs. It belongs to the same chemical family as meth and ecstasy but is much less chemically active than them. It can be found in a great variety of different powders, sprays, and capsules. It is also known as 4-fluoromethcathinone and 4-FMC (1).
What are flephedrone effects?
Flephedrone is an encephalopathic (drug that is not in the body) cathinone (a precursor of several other chemicals including dopamine, epinephrine, norepinephrine, and serotonin) stimulant (2). When taken by an individual, it will convert into a highly concentrated androgens which are also called tropane hormones. This will result in extremely elevated blood pressure and increased heart rate. It is believed that this spike in blood pressure and heart rate creates the peak or “peak” of the euphoric effect which results from the highly intense euphoria experienced. The main question is, how does it work? How do cathinones, in this very concentrated form, cause such a “rush” of serotonin? (3)
It is believed that a combination of these two chemicals, namely 4-fluorophenol and ephedrine (also commonly referred to as speed), work together to produce a highly potent and highly addictive substance. In animal studies, it was shown that the excitation of neurons that contained GABA (Gamma Amino Butyric Acid), the blocker of neurotransmitters, was significantly increased when combined with flephedrone. The level of excitotoxicity reached a level that could only be handled by causing long-term damage to the neurons. It was further suggested that the increased levels of dopamine released from the nucleus accumbens, the seat of emotion in the brain, may play a major role in this process.
Research and Animal Studies.
Animal research has provided further evidence to confirm that the effects of the cathinone that formed this unique spike in euphoria were produced by combining the amino acids L-Methyphenamine and Phenyl tertiary butylamine. Other possible causes of this unusually powerful excitatory neurotransmitter are the interaction of some other drugs such as cocaine, alcohol, or other stimulants with the brain’s neurotransmitters or the body’s natural production of the neurotransmitter dopamine. Another likely scenario is the direct action of L-Methyphenamine on the limbic system of the brain through a pathway controlling emotions, moods, and motivations. Whatever the cause of flephedrone serum levels being elevated, it seems clear that there is a strong correlation between the two substances (4).
Questions for More Investigation
The question now lies whether the high levels of dopamine and L-Methyphenamine in the bloodstream are adequate to trigger a full-blown serotonin syndrome, which is often associated with Flephedrone use. There is no consensus on this question among medical professionals and addiction specialists, although some have pointed out that medical studies that have used pure Flephedrone in isolation do not produce a peak of serotonin levels in the bloodstream. In fact, a number of medical researchers have reported that heavy users can produce levels of serotonin in the blood that are similar to those attained by chronic heavy smokers without causing any harmful health effects. Still, there are those who believe that heavy use of cathinones can produce more serious consequences than mild stimulation of neurotransmitters in the brain.
Groups With Effects on the cardiovascular and cognitive systems
The second major category of substances believed to exert opposite effects on the cardiovascular and cognitive systems is ephedrine and cathinones, derived from the plant ‘meow’. Except for the relatively tame “bath salts“, ephedrine has largely been regarded as more harmful than its cathinone counterpart (5). However, in the recent past, some investigators have claimed that ephedrine has similar cardiovascular effects to that of flephedrone, even when dosages are taken in very low doses. Because of this research, the Forensic Science Service of England has taken samples of three deceased users and tested them for ephedrine concentration using sophisticated mass spectrophotometry (6).
Effects on the Cardiovascular System
While all three substances are believed to have at least marginal effects on the cardiovascular system, the main question is as to what effects they might have on the central nervous system and cognitive function?
The results of a study conducted by the Royal Society for the Prevention of Accidents (RSPCA) focused exclusively on the effects of ephedrine on memory loss. Despite consistent evidence that ephedrine has a pronounced impact on short-term memory retention in users, the researchers noted that the effect is significantly reduced when the drug is taken in greater dosages. This observation may be explained by the difficulty of assessing the oral consumption of larger doses of ephedrine. For anecdotal reports to be useful as indicators of dosage levels, it is necessary to investigate the oral absorption and retention of the drug over long periods of time.
Because of the prevalence of seemingly severe side effects, including liver failure, in recent years many people have been seeking alternatives to cocaine and other controlled substances. While there is no shortage of such products, including a variety of supplements including powders and capsules, it can be difficult to find one that actually contains pure forms of cathinones. Flephedrone and ephedrine are substances that are not easily absorbed into the system. While some research has been done concerning the absorption and elimination of these two drugs, much more research is needed to determine their safety in long-term use. Until this research is complete, it will be difficult to regulate the sale of these two drugs since there is no standard definition for a controlled substance.
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