4-FA

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4-FA
The skeletal formula of 4-FA
4fa.png
Chemical Nomenclature
Common names 4-FA
Substitutive name 4-Fluoroamphetamine
Systematic name (RS)-1-(4-fluorophenyl)-N-propan-2-amine <-- Class Membership -->
Class Membership
Psychoactive class Stimulant
Chemical class Amphetamine
Routes of Administration



Oral
Dosage
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
DISCLAIMER: PW's dosage information is a summary of data gathered from users and resources. It is not a recommendation and should be verified with other sources for accuracy.
Threshold 10 - 25 mg
Light 25 - 50 mg
Common 50 - 100 mg
Strong 100 - 150 mg
Heavy 150 mg +
Duration
Total 6 - 12 hours
Onset 20 - 40 minutes
Peak 3 - 6 hours
Offset 1 - 2 hours
Afterglow 3 - 5 hours









Summary sheet: 4-FA

4-Fluoroamphetamine (4-FA) is a substituted amphetamine with stimulant, entactogenic and nootropic effects. It is described subjectively as being between amphetamine and MDMA. It is rarely found on the streets but commonly sold as a grey area research chemical through online vendors along with related compounds such as 2-fluoroamphetamine and 4-fluoromethamphetamine.[1][2]

Chemistry

4-Fluoroamphetamine (4-FA) is a synthetic molecule of the amphetamine family. Molecules of the amphetamine class contain a phenethylamine core featuring a phenyl ring bound to an amino (NH2) group through an ethyl chain with an additional methyl substitution at Rα. Amphetamines are alpha-methylated phenethylamines. 4-fluoroamphetamine contains a flourine group at R4 of its phenyl ring and is a fluorinated analogue of amphetamine.

Pharmacology

4-Fluoroamphetamines pharmacology differs based on the amount of substance consumed.

When 100mg or more is introduced, 4-FA acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine, producing euphoric, enactogenic effects similar to MDMA. When lower doses of ~75mg are ingested, it only acts on dopamine and norephinephrine, producing effects more similar to a functional stimulant. The mechanism of action of 4-FA effectively boosts the levels of the norepinephrine, dopamine, and serotonin neurotransmitters in higher doses in the brain by binding to and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. This allows dopamine, norepinephrine and serotonin to accumulate within the brain, resulting in stimulating, euphoric and entactogenic effects.[3] [4] [5]

Studies demonstrate that 4-flourine amphetamine substitutions limit activity of the compound at the alpha-1 adrenergic receptor with an over 200-fold increased selectivity for A2 receptors over A1 receptors.[6] It has also been demonstrated that 4-substitution of a hydrogen with fluorine on the aromatic ring of norepinephrine produces a beta-adrenergic agonist with little alpha activity.[7] This has led the online community to speculate that the milder uncomfortable cognitive and/or physical side effects and greater efficacy as a nootropic associated with this substance are at least partially due to decreased activity at the alpha-1 adrenergic receptors resulting in significantly less norepinephrine reuptake inhibition.

Subjective effects

In comparison to other substituted amphetamines, 4-FA is particularly free of side effects such as nausea, high blood pressure, anxiety and an uncomfortable offset. In low doses, it is considered to be an extremely functional and effective nootropic for performing tasks or general productivity of any sort. At higher dosages, however, it becomes dysfunctional and recreational due to the intensity of its euphoria and stimulation.

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

Cognitive effects

After effects

The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. Its effects commonly include:

Toxicity and harm potential

The toxicity and long-term health effects of recreational 4-FA use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because 4-FA has very little history of human usage. Anecdotal evidence from people who have tried 4-FA within the community suggest that there do not seem to be any negative health effects attributed to simply trying this drug at low to moderate doses by itself and using it sparingly (but nothing can be completely guaranteed).

The LD50 (mouse; i.p.) of 4-FA is 46 mg/kg.[8] 4-FA does not cause long-lasting depletion of brain serotonin unlike MDMA or 4-FA's analogues 4-CA and 4-BA.

It is also worth noting that 4-FA is particularly caustic in comparison to other compounds and can therefore cause chemical burns within the nasal passage and throat if it is insufflated.

It is strongly recommended that one use harm reduction practices when using this drug.

Tolerance and addiction potential

As with other stimulants, the chronic use of 4-FA can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage.

Tolerance to many of the effects of 4-FA develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). 4-FA presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of 4-FA all stimulants will have a reduced effect.

Psychosis

Main article: Stimulant psychosis

Abuse of compounds within the amphetamine chemical class at high dosages for prolonged periods of time can result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[9] A review on treatment for amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[10][11] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[12] Psychosis very rarely arises from therapeutic use.[13][14]

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

Serotonin syndrome risk

Combinations in the list below may increase the amount of neurotransmitters such as serotonin and dopamine to dangerous or even fatal levels.

Legal issues

  • Arizona: The drug was added to the "Dangerous Drug" list in April 2014.
  • Louisiana: 4-FA is currently listed as a Schedule I drug as of June 2013.
  • Virginia: The drug is classified as a Schedule I drug.
  • Germany: 4-fluoroamphetamine was added to "Anlage I" in January 2012.
  • Hungary: In January 2012, 4-flouroamphetamine became controlled in Hungary.
  • France: 4-fluoroamphetamine was added to the list of illicit substances in March 2011.
  • Israel: In December 2007, 4-flouroamphetamine was added to Israel's list of controlled substances, making it illegal to buy, sell, or possess.
  • Poland: 4-Fluoroamphetamine is controlled in Poland.
  • Slovak Republic: Beginning March 1, 2011, 4-Fluoroamphetamine is controlled in the Slovak Republic.
  • United Kingdom: 4-fluoroamphetamine is a Class A drug under the Misuse of Drugs Act. 4-FA is covered by the 1977 addition to the Misuse of Drugs Act of 1971.

Experience reports

Anecdotal reports which describe this compound within our experience index include:

See also

External links

References

  1. The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain | https://www.ncbi.nlm.nih.gov/pubmed/17223101
  2. Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues (designer drugs). | http://www.ncbi.nlm.nih.gov/pubmed/15639609
  3. http://www.sciencedirect.com/science/article/pii/0028390875900994 | Comparison of 4-chloro-, 4-bromo-and 4-fluoroamphetamine in rats: drug levels in brain and effects on brain serotonin metabolism
  4. http://www.sciencedirect.com/science/article/pii/S0014299906013811
  5. http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain
  6. 2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands | http://pubs.acs.org/doi/abs/10.1021/jm00169a015
  7. Effect of fluorine substitution on the agonist specificity of norepinephrine | http://www.sciencemag.org/content/204/4398/1217.short
  8. E. Costa and S. Garattini (1970). Amphetamines and Related Compounds. New York: Raven Press. p. 28.
  9. Treatment for amphetamine psychosis | [1]
  10. Treatment for amphetamine psychosis | [2]
  11. Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
  12. Treatment for amphetamine psychosis | [3]
  13. Stimulant Misuse: Strategies to Manage a Growing Problem | http://www.acha.org/prof_dev/ADHD_docs/ADHD_PDprogram_Article2.pdf
  14. http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
  15. Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity | http://bja.oxfordjournals.org/content/95/4/434