4-FA

Revision as of 06:55, 13 February 2018 by >Maethor1337 (Grammatics)
Summary sheet: 4-FA


4-Fluoroamphetamine (also known as 4-FA, 4-FMP, para-Fluoroamphetamine, PAL-303 and colloquially as Flux) is a novel synthetic substituted amphetamine compound that produces a unique progressive mixture of entactogenic and stimulant effects when administered. It is part of a series of fluorinated amphetamine analog that initially included such compounds as 2-FA, 2-FMA, and 3-FA.[1]

4-FA
Chemical Nomenclature
Common names 4-FA, 4-FMP, PAL-303, Flux
Substitutive name 4-Fluoroamphetamine, para-Fluoroamphetamine
Systematic name (RS)-1-(4-Fluorophenyl)-N-propan-2-amine
Class Membership
Psychoactive class Stimulant / Entactogen
Chemical class Amphetamine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 40 mg
Light 40 - 100 mg
Common 100 - 130 mg
Strong 130 - 150 mg
Heavy 150 mg +
Duration
Total 5 - 8 hours
Onset 45 - 75 minutes
Come up 30 - 75 minutes
Peak 2.5 - 3.5 hours
Offset 2 - 3 hours
After effects 6 - 12 hours









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Interactions
Alcohol
GHB
GBL
Benzodiazepines
Opioids
Cannabis
Caffeine
Ketamine
Methoxetamine
Gabapentinoids
Psychedelics
Acetazolamide
Ascorbic acid
Guanethidine
Haloperidol
Lithium carbonate
Norepinephrine
Phenothiazines
Sodium bicarbonate
TCAs
DXM
PCP
25x-NBOMe
2C-T-x
5-MeO-xxT
DOx
Furazolidone
Cocaine
Tramadol
aMT
MAOIs

Anecdotal reports have described the subjective effects of 4-FA as having a moderate MDMA-like entactogenic onset for the initial few hours of the experience that then gradually transitions into traditional amphetamine-type stimulation (for a total duration of around 6 to 8 hours) with residual effects that can last a few hours afterward.[citation needed]

4-FA is rarely found on the streets but commonly sold as a grey area research chemical by online vendors along with related compounds such as 2-FMA and 3-FA.[2][3] Very little data exists about the pharmacological properties, metabolism, and toxicity of 4-FA, and it has only a brief history of human usage. Due to its strong psychostimulant effects, likely habit-forming properties as well as poorly understood toxicity profile, it is strongly recommended that one use proper harm reduction practices if choosing to use this substance.

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 fluorine atom at R4 of its phenyl ring and is a fluorinated analogue of amphetamine.

 
Substitutive structure of an amphetamine molecule

Pharmacology

4-Fluoroamphetamine acts as a releasing agent and reuptake inhibitor of dopamine, serotonin, and norepinephrine producing stimulating amphetamine-like effects at lower doses and euphoric, entactogenic effects similar to MDMA at dosages above 100mg. 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.[4][5][6]

Subjective effects

It is commonly reported that the first three to four hours of 4-FA present distinct entactogenic effects that have been reported as feeling somewhat similar to MDMA although not quite as powerful. This is thought to correlate with the duration in which it is promoting the release of serotonin (in addition to dopamine and norepinephrine). After this first phase of the experience, the effect then shifts towards something which feels like classic amphetamine stimulation which can persist for an extended period.[citation needed]

Do not use 4-FA if you have a history of heart-related issues or experience a severe headache after its use. We have been made aware of a report released by Trimbos-instituut[7] and Nationaal Vergiftigingen Informatie Centrum[8] (NVIC), describing incidents of strokes after an increased use of 4-FA. In addition to the common amphetamine-like effects (agitation, anxiety, tachycardia, hypertension, chest pain et al.), serious cardio- and cerebrovascular complications have been reported, including rhythm (sinus arrhythmia, ventricular extrasystoles (bigeminy), conduction disturbances) and acute cardiac failure. Although a causal relationship has not been confirmed, when presented with a severe headache and lateralization after 4-FA usage, a medical evaluation at an emergency department should be conducted immediately. [9]

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects
 

Visual effects
 

Cognitive effects
 

Transpersonal effects
 

After effects
 

Experience reports

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

Additional experience reports can be found here:

Toxicity and harm potential

The toxicity and long-term effects of recreational 4-FA use have only scarcely been studied because 4-FA has very little history of human usage. Anecdotal evidence, as well as several case reports, suggest there is a small to moderate individual health risk associated with the use of 4-FA. Among these, it appears there is an especially a high risk for acute cardiovascular toxicity. Some people in the Netherlands, only using a moderate dose, have died due to cardiac arrest or suffered severe brain damage due to a stroke. The mechanism of this acute toxicity is not yet known, but it seems as though the stroke starts off as an intense headache or even a migraine attack, that slowly worsens.[10]

The LD50 (mouse; i.p.) of 4-FA is 46 mg/kg.[11] 4-FA does not cause long-lasting depletion of brain serotonin unlike MDMA or 4-FA's analogs 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. This method of administration is discouraged.

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

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). This is how long it takes to reduce the tolerance for the stimulating effects. Tolerance for the entactogenic effects may take a longer period to reduce. 4-FA presents cross-tolerance with [[Cross-tolerance::all dopaminergic stimulants]], meaning that after the consumption of 4-FA all stimulants will have a reduced effect.

Psychosis

Main article: Stimulant psychosis

4-FA, like other stimulants, can result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[12][13] A review on treatment for amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[13][14] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[13]

Dangerous interactions

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

  • Stimulants - 4-FA can be potentially dangerous in combination with other stimulants as it can increase one's heart rate and blood pressure to dangerous levels.
  • "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] & "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 25x compounds are highly stimulating and physically straining. Combinations with 4-FA should be strictly avoided due to the risk of excessive stimulation and heart strain. This can result in increased blood pressure, vasoconstriction, panic attacks, thought loops, seizures, and heart failure in extreme cases.
  • "[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Combining alcohol with stimulants can be dangerous due to the risk of accidental over-intoxication. Stimulants mask alcohol's depressant effects, which is what most people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects will be left unopposed, which can result in blackouts and severe respiratory depression. If mixing, the user should strictly limit themselves to only drinking a certain amount of alcohol per hour.
  • "[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Combinations with DXM should be avoided due to its inhibiting effects on serotonin and norepinephrine reuptake. There is an increased risk of panic attacks and hypertensive crisis, or serotonin syndrome with serotonin releasers (MDMA, methylone, mephedrone, etc.). Monitor blood pressure carefully and avoid strenuous physical activity.
  • "[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Any neurotoxic effects of MDMA are likely to be increased when other stimulants are present. There is also a risk of excessive blood pressure and heart strain (cardiotoxicity).
  • "[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Some reports suggest combinations with MXE may dangerously increase blood pressure and increase the risk of mania and psychosis.
  • "[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Both classes carry a risk of delusions, mania and psychosis, and these risk may be multiplied when combined.
  • "[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 4-FA may be dangerous to combine with other stimulants like cocaine as they can increase one's heart rate and blood pressure to dangerous levels.
  • "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Tramadol is known to lower the seizure threshold[15] and combinations with stimulants may further increase this risk.
  • MDMA - The neurotoxic effects of MDMA may be increased when combined with other stimulants.
  • Cocaine - This combination may increase strain on the heart to dangerous levels.

Combinations with the following substances can cause dangerously high serotonin levels. Serotonin syndrome requires immediate medical attention and can be fatal if left untreated.

Legality

 

This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

  • 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.
  • Brazil - Possession, production and sale is illegal as it is listed on Portaria SVS/MS nº 344.[17]
  • 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-FA is considered a Class A drug as a result of the amphetamine analogue clause of the Misuse of Drugs Act 1971.[18]
  • New Zealand: 4-FA is an amphetamine analogue, so is a Schedule 3 controlled substance in New Zealand.[19]
  • The Netherlands: 4-FA is, as of May 25th 2017, a Schedule 1 drug in the Netherlands. [20]
  • Canada: 4-FA would fall under Schedule I as it is considered an analog of amphetamine.[21]

See also

Forums

References

  1. Quednow, B., Girreser, U., Junge, T., & Ro, P. (2005). Isomeric Fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues (designer drugs), 148, 143–156. https://doi.org/10.1016/j.forsciint.2004.05.003
  2. The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/17223101
  3. Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled substance analogues (designer drugs). (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/15639609
  4. 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
  5. http://www.sciencedirect.com/science/article/pii/S0014299906013811
  6. http://www.sciencedirect.com/science/article/pii/S0014299906013811 | The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain
  7. https://www.trimbos.nl/
  8. https://www.vergiftigingen.info/
  9. https://psychonautwiki.org/wiki/File:Behandeling-4-fa-intoxicatie.pdf
  10. https://psychonautwiki.org/wiki/File:4-FA%20risicobeoordeling%20(2016).pdf
  11. E. Costa and S. Garattini (1970). Amphetamines and Related Compounds. New York: Raven Press. p. 28.
  12. http://www.drugabuse.gov/drugs-abuse/emerging-trends
  13. 13.0 13.1 13.2 Shoptaw, S. J., Kao, U., & Ling, W. (2009). Treatment for amphetamine psychosis. The Cochrane Library.
  14. Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
  15. Talaie, H.; Panahandeh, R.; Fayaznouri, M. R.; Asadi, Z.; Abdollahi, M. (2009). "Dose-independent occurrence of seizure with tramadol". Journal of Medical Toxicology. 5 (2): 63–67. doi:10.1007/BF03161089. eISSN 1937-6995. ISSN 1556-9039. OCLC 163567183. 
  16. Gillman, P. K. (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of Anaesthesia. 95 (4): 434–441. doi:10.1093/bja/aei210 . eISSN 1471-6771. ISSN 0007-0912. OCLC 01537271. PMID 16051647. 
  17. http://portal.anvisa.gov.br/documents/10181/3115436/%281%29RDC_130_2016_.pdf/fc7ea407-3ff5-4fc1-bcfe-2f37504d28b7
  18. Misuse of Drugs Act 1971 (Legislation.gov.uk) |http://www.legislation.gov.uk/ukpga/1971/38/schedule/2/part/I
  19. http://www.legislation.govt.nz/act/public/1975/0116/latest/whole.html#DLM436576
  20. https://www.rijksoverheid.nl/actueel/nieuws/2017/05/24/verbod-op-drug-4-fluoramfetamine-gaat-vrijdag-25-mei-in
  21. Controlled Drugs and Substances Act (S.C. 1996, c. 19) | http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-12.html#h-28