
Lisdexamphetamine
Lisdexamphetamine | |||||||||||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||||||||||
Common names | Lisdexamfetamine, Vyvanse, Elvanse | ||||||||||||||||||||||||||||||||||
Substitutive name | L-lysine-dextroamphetamine | ||||||||||||||||||||||||||||||||||
Systematic name | (2S)-2,6-Diamino-N-[(2S)-1-phenylpropan-2-yl]hexanamide | ||||||||||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||||||||||
Psychoactive class | Stimulant | ||||||||||||||||||||||||||||||||||
Chemical class | Amphetamine | ||||||||||||||||||||||||||||||||||
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Lisdexamphetamine (full name L-lysine-dextroamphetamine, brand names Vyvanse, Elvanse) is a prodrug for dextro-amphetamine, a strong central nervous system stimulant. It is indicated for the medical treatment of ADHD and moderate to severe binge-eating disorder.[2]
Like other amphetamines, it is also used illicitly as a study drug and for recreational purposes.
While amphetamine sulfate contains 50% L-amphetamine, and the ADHD medication Adderall contains a mix of four amphetamine salts totaling 75% D-amphetamine and 25% L-amphetamine, lisdexamfetamine, once converted into an active form, is pure dextroamphetamine. This leads to stronger central and weaker peripheral nervous system effects. Lisdexamphetamine effects are independent of the route of administration, and oral is, therefore, the preferred method of ingestion, unlike other amphetamines, which are insufflated, smoked or injected by some recreational users.
Chemistry
Lisdexamphetamine consists of the dextro-rotary stereoisomer of amphetamine bonded to the essential amino acid lysine. See the entry on amphetamine.
Pharmacokinetics
As a prodrug, lisdexamfetamine is inactive in the form administered. Once ingested, it is enzymatically cleaved into L-lysine, a naturally occurring essential amino acid, and D-amphetamine, a central nervous system stimulant. Thus lisdexamfetamine functions as an extended release version of dexamphetamine. Because D-amphetamine needs to be liberated from lysine via contact with red blood cells, effects are independent of the route of administration. Conversion of lisdexamfetamine into active D-amphetamine is enzymatically rate-limited, slowing down the time to achieve and decreasing the magnitude of peak concentration of active substance and subsequent striatal dopamine release.[3]
Pharmacodymanics
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.[4][5][6] 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.
D-amphetamine's affinity for the TAAR1 receptor is twice that of L-amphetamine.[7] As a result, D-amphetamine produces three to four times as much Central Nervous System stimulation as L-amphetamine. L-amphetamine, on the other hand, has stronger cardiovascular and peripheral effects.
Subjective effects
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
- Spontaneous tactile sensations - The "body high" of amphetamine can be described as a moderate euphoric tingling sensation that encompasses the entire body. This sensation maintains a consistent presence that steadily rises with the onset and hits its limit once the peak has been reached.
- Stimulation - In terms of its effects on the physical energy levels of the user, amphetamine is usually considered to be moderately energetic and stimulating in a fashion that is slightly weaker to that of methamphetamine, but stronger than that of modafinil, caffeine, and methylphenidate. 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.
- Abnormal heartbeat
- Appetite suppression
- Bronchodilation
- Dehydration
- Frequent urination
- Increased bodily temperature [citation needed]
- Increased blood pressure [citation needed]
- Increased heart rate [citation needed]
- Increased perspiration
- Nausea
- Perception of decreased weight
- Pupil dilation
- Stamina enhancement
- Teeth grinding
- Temporary erectile dysfunction
- Vasoconstriction [citation needed]
Cognitive effects
- Analysis enhancement
- Cognitive euphoria
- Compulsive redosing
- Dream suppression
- Ego inflation
- Focus enhancement - This component is most effective at low to moderate doses as anything higher will usually impair concentration.
- Increased libido
- Increased music appreciation
- Memory enhancement
- Motivation enhancement
- Thought acceleration
- Thought organization
- Wakefulness
Visual effects
The visual effects of amphetamine are usually less consistent and are only mildly noticeable at higher dosages. They are somewhat comparable to deliriants and are more frequent in darker areas. Effects intensify with sleep deprivation, and long binges without sleep can escalate into full-blown stimulant psychosis.
Suppressions
Distortions
- Drifting (breathing and morphing) - This effect is usually subtle and barely noticeable and only occurs at higher dosages or when combined with cannabis. Commonly this consists of level 1-2 drifting.
- Brightness alteration
Hallucinatory states
- Transformations - These are usually very mild.
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:
- Anxiety
- Appetite suppression
- Cognitive fatigue
- Depression
- Irritability
- Motivation suppression
- Sleep paralysis - Some users note sleep paralysis after consuming amphetamine.
- Thought deceleration
- Wakefulness
Experience reports
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and Harm Potential
Like other amphetamines, lisdexamfetamine is addictive and sufficiently high doses can cause neurotoxicity. Other dangers include stimulant psychosis.
The addiction and harm potential of lisdexamfetamine is theoretically lower than that of straight amphetamine due to the rate-limiting step of hydrolysis necessary to convert LDX into active D-amphetamine. Caution is nonetheless warranted.
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 - 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.[8]
- "[[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 Lisdexamphetamine 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.]] - Lisdexamphetamine 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[9] and combinations with stimulants may further increase this risk.
- MDMA - The neurotoxic effects of MDMA may be increased when combined with amphetamines.
- "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, and some antidepressants.[10]
- Cocaine - This combination may increase strain on the heart.
Please refer to the article on amphetamine for a more thorough discussion of tolerance, toxicity and harm potential.
Legal issues
Lisdexamphetamine is approved for medical use with a doctor's prescription, but in most countries, it is illegal to sell or possess without a prescription.
- UK: Lisdexamfetamine is a Class B scheduled drug.
- US: It is a Schedule II controlled drug.
- Germany: Lisdexamphetamine is scheduled in Anlage III.[11]
- Australia: It is a Schedule 8 drug.
- Canada: Lisdexamfetamine is a Schedule I drug.
- Norway: Elvanse is a Class A drug under particularly strict control.[12]
- Sweden: Elvanse is a Class II narcotic, with strict requirements for prescription. It has been placed under "utökad övervåkande" (extended surveillance).[13]
- Schengen Area: Lisdexamphetamine requires a special certificate while traveling within the Schengen Area, which covers most of Europe, but not the United Kingdom.[13]
See also
External links
- Amphetamine (Wikipedia)
- Lisdexamphetamine (Wikipedia)
- Amphetamine (Erowid)
- Amphetamine experiences (Erowid)
- Lisdexamphetamine experiences (Erowid)
- Amphetamine (TripSit)
- Vyvanse (TripSit)
- Potential Adverse Effects of Amphetamine Treatment on Brain and Behavior: A Review
- Dextroamphetamine and Amphetamine (Medicine Plus)
References
- ↑ https://web.archive.org/web/20140826115717/http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con261790.pdf
- ↑ https://www.drugs.com/pro/vyvanse.html
- ↑ http://www.sciencedirect.com/science/article/pii/S0028390814000781
- ↑ 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
- ↑ https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3236098/
- ↑ Adderall Prescription info | http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021303s026lbl.pdf
- ↑ 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.
- ↑ 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.
- ↑ https://en.wikipedia.org/wiki/Drugs_controlled_by_the_German_Bet%C3%A4ubungsmittelgesetz#Anlage_III
- ↑ http://www.felleskatalogen.no/medisin/elvanse-shire-pharmaceutical-contracts-ltd-588199
- ↑ 13.0 13.1 http://www.fass.se/LIF/product?userType=2&nplId=20140730000117