Lisdexamfetamine: Difference between revisions
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In rodents and primates, sufficiently high doses of amphetamine cause dopaminergic neurotoxicity, or damage to dopamine neurons, which is characterized by reduced transporter and receptor function. | In rodents and primates, sufficiently high doses of amphetamine cause dopaminergic neurotoxicity, or damage to dopamine neurons, which is characterized by reduced transporter and receptor function. There is no evidence that amphetamine is directly neurotoxic in humans. However, large doses of amphetamine may cause indirect neurotoxicity as a result of increased oxidative stress from reactive oxygen species and autoxidation of dopamine. | ||
A severe amphetamine overdose can result in a stimulant psychosis that may involve a variety of symptoms, such as paranoia and delusions.[64] A Cochrane Collaboration review on treatment for amphetamine, dextroamphetamine, and methamphetamine psychosis states that about 5–15% of users fail to recover completely. | A severe amphetamine overdose can result in a stimulant psychosis that may involve a variety of symptoms, such as paranoia and delusions.[64] A Cochrane Collaboration review on treatment for amphetamine, dextroamphetamine, and methamphetamine psychosis states that about 5–15% of users fail to recover completely. According to the same review, there is at least one trial that shows antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis. Psychosis very rarely arises from therapeutic use. | ||
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug. | It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug. | ||
===Tolerance and addiction potential=== | ===Tolerance and addiction potential=== | ||
Addiction is a serious risk with heavy recreational amphetamine use but is unlikely to arise from typical long-term medical use at therapeutic doses. | Addiction is a serious risk with heavy recreational amphetamine use but is unlikely to arise from typical long-term medical use at therapeutic doses. Compared to other amphetamine pharmaceuticals, lisdexamfetamine may have a lower liability for abuse as a recreational drug. Drug tolerance develops rapidly in amphetamine abuse (i.e., a recreational amphetamine overdose), so periods of extended use require increasingly larger doses of the drug in order to achieve the same effect. | ||
Repeated use of lisdexamfetmine will result in a gradual tolerance proportional to the dosage taken. Patients prescribed this drug often must increase their dosage after a time to maintain its efficacy. | Repeated use of lisdexamfetmine will result in a gradual tolerance proportional to the dosage taken. Patients prescribed this drug often must increase their dosage after a time to maintain its efficacy. | ||
==Legal issues== | ==Legal issues== | ||
Lisdexamfetamine is a Class B/Schedule II substance in the United Kingdom and a Schedule II controlled substance in the United States | Lisdexamfetamine is a Class B/Schedule II substance in the United Kingdom and a Schedule II controlled substance in the United States | ||
Revision as of 05:16, 11 October 2016
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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 | ||||||||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||||||||
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| Summary sheet: Lisdexamfetamine |
Lisdexamfetamine (contracted from L-lysine-dextroamphetamine), also known as Vyvanse, is a central nervous system (CNS) stimulant and dextroamphetamine prodrug of the phenethylamine class and amphetamine class that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and binge eating disorder. Lisdexamfetamine was designed to act as a chemical slow release dextroamphetamine analogue.
Lisdexamfetamine is a Class B/Schedule II substance in the United Kingdom and a Schedule II controlled substance in the United States.
Chemistry
Lisdexamfetamine is an inactive prodrug that is converted in the body to dextroamphetamine, a pharmacologically active compound which is responsible for the drug’s activity.[117] After oral ingestion, lisdexamfetamine is broken down by enzymes in red blood cells to form L-lysine, a naturally occurring essential amino acid, and dextroamphetamine.
Pharmacology
Lisdexamfetamine was developed with the goal of providing a long duration of effect that is consistent throughout the day, with reduced potential for abuse. The attachment of the amino acid lysine slows down the relative amount of dextroamphetamine available to the blood stream. Because no free dextroamphetamine is present in lisdexamfetamine capsules, dextroamphetamine does not become available through mechanical manipulation, such as crushing or simple extraction. A relatively sophisticated biochemical process is needed to produce dextroamphetamine from lisdexamfetamine.[118] As opposed to Adderall, which contains roughly equal parts of racemic amphetamine and dextroamphetamine salts, lisdexamfetamine is a single-enantiomer dextroamphetamine formula.
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.
While the subjective effects are almost identical to that of amphetamine, lisdexamfetamine is significantly longer in its duration and more consistent in its intensity due to the slow release metabolism. Although this drug is rate-limited in its metabolism, sufficiently high doses are comparable to its instant release counterparts.
Physical effects
- Spontaneous tactile sensations - TThe "body high" of lisdexamphetamine can be described as a moderate euphoric tingling sensation that encompasses the entire body, radiating from the core. This sensation maintains a consistent presence that steadily rises with the onset and hits its limit once the peak has been reached.
- Bodily control enhancement
- Increased heart rate
- Pupil dilation
- Tactile enhancement - Feelings of enhanced tactile sensation are consistently present at mild to moderate levels proportional to dosage.
- Stimulation
- Teeth grinding
- Appetite Suppression
- Bronchodilation
- Physical Euphoria
Cognitive effects
Lisdexamfetamine shares most of its cognitive effects with other amphetamines, although it is less forceful in its come-up due to the slow release mechanism. It produces a variety of cognitive enhancements associated with stimulants. However, during latter third of the duration, these cognitive enhancements may compete with or be nullified by the accumulated dopamine depletion and its effects.
The most prominent of these cognitive effects generally include:
- Analysis enhancement
- Conceptual thinking
- Creativity Enhancement
- Ego inflation
- Emotion enhancement
- Focus enhancement
- Irritability
- Immersion enhancement
- Increased music appreciation
- Memory enhancement
- Motivation enhancement
- Novelty enhancement
- Increased libido
- Novelty enhancement
- Personal bias suppression
- Thought acceleration
- Thought organization
- Thought connectivity
- Wakefulness
- Time distortion
- Wakefulness
- Cognitive Euphoria
- Depersonalization - This drug is commonly reported to induce depersonalization on the second half of the duration due to an accumulation of dopamine depletion mixed with the residual stimulation of the substance.
Visual effects
Enhancements
Toxicity and harm potential
 Main articles: Research chemicals § Toxicity and harm potential & Responsible use § Hallucinogens
|
In rodents and primates, sufficiently high doses of amphetamine cause dopaminergic neurotoxicity, or damage to dopamine neurons, which is characterized by reduced transporter and receptor function. There is no evidence that amphetamine is directly neurotoxic in humans. However, large doses of amphetamine may cause indirect neurotoxicity as a result of increased oxidative stress from reactive oxygen species and autoxidation of dopamine.
A severe amphetamine overdose can result in a stimulant psychosis that may involve a variety of symptoms, such as paranoia and delusions.[64] A Cochrane Collaboration review on treatment for amphetamine, dextroamphetamine, and methamphetamine psychosis states that about 5–15% of users fail to recover completely. According to the same review, there is at least one trial that shows antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis. Psychosis very rarely arises from therapeutic use. It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
Addiction is a serious risk with heavy recreational amphetamine use but is unlikely to arise from typical long-term medical use at therapeutic doses. Compared to other amphetamine pharmaceuticals, lisdexamfetamine may have a lower liability for abuse as a recreational drug. Drug tolerance develops rapidly in amphetamine abuse (i.e., a recreational amphetamine overdose), so periods of extended use require increasingly larger doses of the drug in order to achieve the same effect.
Repeated use of lisdexamfetmine will result in a gradual tolerance proportional to the dosage taken. Patients prescribed this drug often must increase their dosage after a time to maintain its efficacy.
Legal issues
Lisdexamfetamine is a Class B/Schedule II substance in the United Kingdom and a Schedule II controlled substance in the United States
Experience reports
Anecdotal reports which describe this compound within our experience index include:
- Experience: 70 mg Lisdexamfetamine (Oral/Insufflated) - Intense Study Session
- Experience:Lisdexamfetamine (70 mg, Orally) - Daily use for someone with ADHD
Additional experience reports can be found here:
See also
External links
References