Amphetamine

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Amphetamine
The skeletal formula of Amphetamine.
Amphetamine.png
3damphetamine.png
Chemical Nomenclature
Common names Amphetamine, speed
Substitutive name Benzedrine, Adderall, dextroamphetamine
Systematic name (RS)-1-phenylpropan-2-amine

(RS)-1-phenyl-2-aminopropane

<-- 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 5 mg
Light 10 - 30 mg
Common 30 - 60 mg
Strong 60 - 100 mg
Heavy 100+ mg
Duration
Total 6 - 8 hours
Onset 20 - 60 minutes
Peak 3 - 6 hours
Offset 3 - 5 hours
Afterglow 5 - 10 hours









Summary sheet: Amphetamine

Amphetamine (contracted from α-Methylphenethylamine) is a strong central nervous system stimulant that increases activity in the brain and induces temporary improvements such as enhanced alertness, wakefulness, and locomotion. It is the parent compound of the substituted amphetamines class which also includes MDMA, methamphetamine, DOM, and DOC.

Amphetamine is widely used throughout the world as a prescription medicine for the treatment of attention deficit hyperactivity disorder (ADHD) and the sleeping disorder narcolepsy.[1][2] It is also used without prescription as an illicit substance of recreational use or abuse.

Although the term amphetamine traditionally refers to an equal combination of the two enantiomers levoamphetamine (l-amphetamine) and dextroamphetamine (d-amphetamine), it is frequently used for any mixture of the two or only one of them. The popular prescription drug Adderall contains both enantiomers. The drug is usually taken orally, but can also be insufflated, injected, or administered rectally.

Chemistry

Amphetamine is comprised of a phenethylamine core featuring a phenyl ring bound to an amino (NH2) group through an ethyl chain with an additional methyl substitution at Rα. It can be referred to as a methyl homologue of phenethylamine as it has the same general formula, differing only in the addition of one methyl group.

Pharmacology

Amphetamine is a full agonist of the trace amine-associated receptor 1 (TAAR1), which is a key regulator of common and trace brain monoamines such as dopamine, serotonin and noradrenaline.[3][4][5] The agonism of this set of receptors results in the release of increased concentrations of dopamine, serotonin and noradrenaline in the synaptic cleft. This leads to an increased rate firing of the post-synaptic neuron, triggering both cognitive and physical stimulation within the user.

Subjective effects

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

The physical effects of amphetamine can be broken down into several components which progressively intensify proportional to dosage. These are described below and generally include:

Cognitive effects

The cognitive effects of amphetamine can be broken down into several components which progressively intensify proportional to dosage. The general head space of amphetamine is described by many as one of extreme mental stimulation, increased focus, and powerful euphoria. It contains a large number of typical stimulant cognitive effects. Although negative side effects are usually mild at low to moderate dosages, they become increasingly likely to manifest themselves with higher amounts or extended usage. This particularly holds true during the offset of the experience.

The most prominent of these cognitive effects generally include:

Toxicity and harm potential

This radar plot shows therelative physical harm, social harm, and dependence of amphetamine.[6]

In rodents and primates, sufficiently high doses of amphetamine cause dopaminergic neurotoxicity (or damage to dopamine neurons) which is characterized as reduced transporter and receptor function.[7] As of March 2014, there is no evidence that amphetamine is directly neurotoxic in humans.[8] High-dose amphetamine can cause indirect neurotoxicity as a result of increased oxidative stress from reactive oxygen species and autoxidation of dopamine.[9][10][11]

Lethal dosage

The LD50 (the dosage required to kill 50% of the test subjects) of amphetamine in rats has been found to be between roughly 15mg and 180mg per kilogram depending on the study.[12] No formal studies in humans have been carried out.

Tolerance and addiction potential

Tolerance develops rapidly in amphetamine abuse, so periods of extended use require increasing doses of the drug in order to achieve the same effect.[13][14] Addiction is a serious risk with heavy recreational amphetamine use, but is unlikely to arise from typical medical use.[15][16][17]

Psychosis

Main article: Stimulant psychosis

Abuse of amphetamine can result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, delusions).[18] A Cochrane Collaboration review on treatment for amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[19][20] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[21] Psychosis very rarely arises from therapeutic use.[22][23]

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.

Legal issues

Amphetamine is legally approved for medical purposes worldwide. However, it is a controlled substance and is illegal to sell and possess in most countries without a prescription.

  • United States: Amphetamine is a Schedule II controlled substance.[26]
  • Canada: It is a Schedule I drug.[27]
  • United Kingdom: Amphetamine is considered a Class B drug.[28]
  • Thailand: The drug is classified as a category 1 narcotic in the Thai Narcotic Act of 2012. [29]
  • South Korea: Amphetamine is banned even for medical purposes.[30]
  • Japan: Amphatamine is prohibited. [31]

See also

External links

References

  1. The pharmacology and clinical outcomes of amphetamines to treat ADHD: does composition matter? | http://www.ncbi.nlm.nih.gov/pubmed/22329564
  2. Narcolepsy: current treatment options and future approaches |http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2526380/
  3. The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/
  4. Drug banks amphetamine targets | http://www.drugbank.ca/drugs/DB00182#targets
  5. TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364
  6. Development of a rational scale to assess the harm of d rugs of potential misuse | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  7. Update on Amphetamine Neurotoxicity and Its Relevance to the Treatment of ADHD | http://jad.sagepub.com/content/11/1/8
  8. Human health effects - Amphetamine | http://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+300-62-9
  9. Malenka RC, Nestler EJ, Hyman SE (2009). "15". In Sydor A, Brown RY. Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (2nd ed.). New York: McGraw-Hill Medical. p. 370. ISBN 9780071481274. "Unlike cocaine and amphetamine, methamphetamine is directly toxic to midbrain dopamine neurons."
  10. Toxicity of amphetamines: an update | http://link.springer.com/article/10.1007%2Fs00204-012-0815-5
  11. Dopaminergic neuron-specific oxidative stress caused by dopamine itself. | http://www.ncbi.nlm.nih.gov/pubmed/18596830
  12. Amphetamine - human health effects | http://toxnet.nlm.nih.gov/cgi-bin/sis/search/a?dbs+hsdb:@term+@DOCNO+3287
  13. "Amphetamines: Drug Use and Abuse" | http://web.archive.org/web/20070217053619/http://www.merck.com/mmhe/sec07/ch108/ch108g.html
  14. Efficacy of psychostimulant drugs for amphetamine abuse or dependence | [1]
  15. "Adderall XR Prescribing Information" | http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
  16. Stolerman IP (2010). Stolerman IP, ed. Encyclopedia of Psychopharmacology. Berlin; London: Springer. p. 78. ISBN 9783540686989.
  17. "Miscellaneous Sympathomimetic Agonists" | http://accessmedicine.mhmedical.com/content.aspx?bookid=374&sectionid=41266218&jumpsectionID=41268855
  18. Treatment for amphetamine psychosis | [2]
  19. Treatment for amphetamine psychosis | [3]
  20. Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
  21. Treatment for amphetamine psychosis | [4]
  22. Stimulant Misuse: Strategies to Manage a Growing Problem | http://www.acha.org/prof_dev/ADHD_docs/ADHD_PDprogram_Article2.pdf
  23. http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
  24. Adderall Prescription info | http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
  25. Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity | http://bja.oxfordjournals.org/content/95/4/434
  26. Controlled Drugs and Substances Act | http://www.fda.gov/regulatoryinformation/legislation/ucm148726.htm
  27. Controlled Drugs and Substances Act | http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-24.html#h-28
  28. Misuse of Drugs Act of 1971 | http://www.legislation.gov.uk/ukpga/1971/38/schedule/2
  29. Thai Narcotic Act of 2012 | http://narcotic.fda.moph.go.th/faq/upload/Thai%20Narcotic%20Act%202012.doc._37ef.pdf
  30. What Can't Be Brought Into Seoul, Korea? | http://traveltips.usatoday.com/cant-brought-seoul-korea-63319.html
  31. The problem of the abuse of amphetamines in Japan | https://www.unodc.org/unodc/en/data-and-analysis/bulletin/bulletin_1957-01-01_3_page003.html