Amphetamine |
| Amphetamine | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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| The skeletal formula of Amphetamine. | |||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||
| Psychoactive class | Stimulant | ||||||||||||||||||||||||||||||||||||||||||||||||||||
| Chemical class | Amphetamine | ||||||||||||||||||||||||||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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 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
- Stimulation - In terms of its effects on the physical energy levels of the user, amphetamine is usually considered to be extremely energetic and stimulating in a fashion that is identical to that of methamphetamine, but stronger than that of modafinil, caffeine, and MDMA. It is similar, yet distinct, from the stimulation experienced on MDMA, encouraging physical activities such as dancing, socializing, running, or cleaning. The particular style of stimulation which amphetamine presents can be described as forced. This means that, at higher dosages, it becomes difficult or impossible to keep still as jaw clenching, involuntarily bodily shakes and vibrations become present, resulting in extreme shaking of the entire body, unsteadiness of the hands, and a general lack of motor control.
- Increased heart rate
- Dehydration
- Appetite suppression
- Nausea
- Frequent urination
- Abnormal heartbeat
- Vasoconstriction
- Temporary erectile dysfunction
- Bronchodilation
- Increased perspiration
- Increased blood pressure
- Teeth grinding
Cognitive effects
- Focus enhancement - This component is most effective at low to moderate doses as anything higher will usually impair concentration.
- Thought acceleration
- Thought organization
- Analysis enhancement
- Wakefulness
- Memory enhancement
- Motivation enhancement
- Cognitive euphoria
- Compulsive redosing
- Increased libido
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
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] However, 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 and the exact toxic dosage is unknown.
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 amphetamine 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.[13][14] Addiction is a serious risk with heavy recreational amphetamine use, but is unlikely to arise from typical medical use.[15][16][17]
Tolerance to many of the effects of amphetamine 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). amphetamine presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of amphetamine all stimulants will have a reduced effect.
Withdrawal symptoms
After taking amphetmine on a regular basis, some users will become addicted. When the drug is discontinued immediately, the user will experience what has come to be known as a "crash" along with a number of other amphetamine withdrawal symptoms including paranoia, depression, anxiety, itching, mood swings, irritability, fatigue, insomnia, an intense craving for more amphetamine or other stimulants, and, in some cases, nausea and vomiting.
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 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.
- Stimulants - Amphetamine can be potentially dangerous in combination with other stimulants as it can increase one's heart rate and blood pressure to dangerous levels.
- Tricyclic antidepressants - Amphetamine may increase the effects of tricyclic antidepressants to dangerous levels.[24]
- 25x-NBOMe - Both the NBOMe series and this compound induce powerful stimulation and their interaction may cause severe side effects. These can include thought loops, seizures, increased blood pressure, vasoconstriction, increased heart rate, and heart failure (in extreme cases).
- Alcohol - It is dangerous to combine alcohol, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of alcohol which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of alcohol will be significantly increased, leading to intensified disinhibition as well as respiratory depression. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - This combination may cause increased heart rate and panic attacks.
- MXE - Increased heart rate and blood pressure may occur.
- Tramadol - This combination can increase the risk of seizures.
- MDMA - The neurotoxic effects of MDMA may be increased when combined with amphetamines.
- MAOIs - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, 2C-T-2, 2C-T-7, αMT, and some antidepressants.[25]
- Cocaine - This combination may increase strain on the heart.
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
- ↑ The pharmacology and clinical outcomes of amphetamines to treat ADHD: does composition matter? (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/22329564
- ↑ Narcolepsy: current treatment options and future approaches |http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2526380/
- ↑ The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/
- ↑ Drug banks amphetamine targets | http://www.drugbank.ca/drugs/DB00182#targets
- ↑ TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364
- ↑ Development of a rational scale to assess the harm of d rugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
- ↑ Update on Amphetamine Neurotoxicity and Its Relevance to the Treatment of ADHD | http://jad.sagepub.com/content/11/1/8
- ↑ Human health effects - Amphetamine | http://toxnet.nlm.nih.gov/cgi-bin/sis/search/r?dbs+hsdb:@term+@rn+@rel+300-62-9
- ↑ 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."
- ↑ Toxicity of amphetamines: an update | http://link.springer.com/article/10.1007%2Fs00204-012-0815-5
- ↑ Dopaminergic neuron-specific oxidative stress caused by dopamine itself. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/18596830
- ↑ Amphetamine - human health effects | http://toxnet.nlm.nih.gov/cgi-bin/sis/search/a?dbs+hsdb:@term+@DOCNO+3287
- ↑ "Amphetamines: Drug Use and Abuse" | http://web.archive.org/web/20070217053619/http://www.merck.com/mmhe/sec07/ch108/ch108g.html
- ↑ Efficacy of psychostimulant drugs for amphetamine abuse or dependence | [1]
- ↑ "Adderall XR Prescribing Information" | http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
- ↑ Stolerman IP (2010). Stolerman IP, ed. Encyclopedia of Psychopharmacology. Berlin; London: Springer. p. 78. ISBN 9783540686989.
- ↑ "Miscellaneous Sympathomimetic Agonists" | http://accessmedicine.mhmedical.com/content.aspx?bookid=374§ionid=41266218&jumpsectionID=41268855
- ↑ Treatment for amphetamine psychosis | [2]
- ↑ Treatment for amphetamine psychosis | [3]
- ↑ Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
- ↑ Treatment for amphetamine psychosis | [4]
- ↑ Stimulant Misuse: Strategies to Manage a Growing Problem | http://www.acha.org/prof_dev/ADHD_docs/ADHD_PDprogram_Article2.pdf
- ↑ http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
- ↑ Adderall Prescription info | http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
- ↑ Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity | http://bja.oxfordjournals.org/content/95/4/434
- ↑ Controlled Drugs and Substances Act | http://www.fda.gov/regulatoryinformation/legislation/ucm148726.htm
- ↑ Controlled Drugs and Substances Act | http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-24.html#h-28
- ↑ Misuse of Drugs Act of 1971 | http://www.legislation.gov.uk/ukpga/1971/38/schedule/2
- ↑ Thai Narcotic Act of 2012 | http://narcotic.fda.moph.go.th/faq/upload/Thai%20Narcotic%20Act%202012.doc._37ef.pdf
- ↑ What Can't Be Brought Into Seoul, Korea? | http://traveltips.usatoday.com/cant-brought-seoul-korea-63319.html
- ↑ 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