Lisdexamfetamine: Difference between revisions

>David Hedlund
lisdexamfetamine dimesylate (the usual prescribed form)
>David Hedlund
lisdexamfetamine _dimesylate_ converts into a total 29.7% (not 29.5: 8,9÷30 = 0,296666667 ~= 29.7%) its weight in dextroamphetamine
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{{SubstanceBox/Lisdexamfetamine}}
{{SubstanceBox/Lisdexamfetamine}}


'''Lisdexamfetamine''' (also known as '''Lisdextroamphetamine''', '''L-lysine-dextroamphetamine''', or '''lisdexamfetamine dimesylate''' when under the brand names '''Vyvanse''' and '''Elvanse''') is a [[psychoactive class::stimulant]] substance of the [[chemical class::amphetamine]] class. Lisdextroamphetamine a [[prodrug]] for [[Amphetamine#Enantiomers|<small>d</small>-amphetamine]] (dexamphetamine, or dextroamphetamine) which is known to be a strong central nervous system (CNS) stimulant.  
'''Lisdexamfetamine''' (also known as '''Lisdextroamphetamine''', '''L-lysine-dextroamphetamine''', or '''lisdexamfetamine dimesylate''' ('''LDX''')<ref>http://www.sciencedirect.com/science/article/pii/S0028390814000781</ref> when under the brand names '''Vyvanse''' and '''Elvanse''') is a [[psychoactive class::stimulant]] substance of the [[chemical class::amphetamine]] class. Lisdextroamphetamine a [[prodrug]] for [[Amphetamine#Enantiomers|<small>d</small>-amphetamine]] (dexamphetamine, or dextroamphetamine) which is known to be a strong central nervous system (CNS) stimulant.  


Lisdexamfetamine is indicated and widely prescribed for the medical treatment of ADHD and moderate to severe binge-eating disorder.<ref>https://www.drugs.com/pro/vyvanse.html</ref> This means that outside of the oral route, its effects are independent of [[route of administration]]. Other routes of administration like [[insufflation]], [[Route of administration#Smoked|smoking]] or [[Route of administration#Injection|injection]] do not provide faster absorption or onset.
Lisdexamfetamine is indicated and widely prescribed for the medical treatment of ADHD and moderate to severe binge-eating disorder.<ref>https://www.drugs.com/pro/vyvanse.html</ref> This means that outside of the oral route, its effects are independent of [[route of administration]]. Other routes of administration like [[insufflation]], [[Route of administration#Smoked|smoking]] or [[Route of administration#Injection|injection]] do not provide faster absorption or onset.
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==Pharmacology==
==Pharmacology==
Lisdexamfetamine was developed with the goal of providing a long duration of effect that remains consistent throughout the day as well as reduced potential for abuse. The attachment of the amino acid lysine slows down the relative amount of dextroamphetamine that is released into the bloodstream (Lisdexamfetamine converts into a total 29.5% its weight in Dextroamphetamine). Because no free dextroamphetamine is present in lisdexamfetamine capsules, dextroamphetamine does not become available through mechanical manipulation, such as crushing or simple extraction. There is, therefore, no way to speed up absorption via alternate [[routes of administration]], such as via [[insufflation]], [[vaporization]], or [[injection]], making the drug theoretically less abusable.
Lisdexamfetamine was developed with the goal of providing a long duration of effect that remains consistent throughout the day as well as reduced potential for abuse. The attachment of the amino acid lysine slows down the relative amount of dextroamphetamine that is released into the bloodstream (lisdexamfetamine dimesylate converts into a total 29.7% its weight in dextroamphetamine). Because no free dextroamphetamine is present in lisdexamfetamine capsules, dextroamphetamine does not become available through mechanical manipulation, such as crushing or simple extraction. There is, therefore, no way to speed up absorption via alternate [[routes of administration]], such as via [[insufflation]], [[vaporization]], or [[injection]], making the drug theoretically less abusable.


===Pharmacokinetics===
===Pharmacokinetics===
As a [[prodrug]], lisdexamfetamine is inactive in the form administered. Once ingested, it is enzymatically cleaved into two parts: L-lysine, a naturally occurring essential amino acid, and <small>d</small>-amphetamine, a central nervous system stimulant. Thus lisdexamfetamine functions as an extended release version of dexamphetamine. Because <small>d</small>-amphetamine needs to be liberated from lysine via contact with red blood cells, effects are independent of route of administration. Conversion of lisdexamfetamine into active <small>d</small>-amphetamine is enzymatically [[Rate-Limiting Step|rate-limited]], slowing down the time to achieve peak concentrations and decreasing its magnitude and dampening consequent striatal dopamine release, which is thought to be responsible for its euphoric and [[compulsive redosing]] effects. The rate of conversion is a total 29.5% of its weight in Dextroamphetamine. <ref>http://www.sciencedirect.com/science/article/pii/S0028390814000781</ref>
As a [[prodrug]], lisdexamfetamine is inactive in the form administered. Once ingested, it is enzymatically cleaved into two parts: L-lysine, a naturally occurring essential amino acid, and <small>d</small>-amphetamine, a central nervous system stimulant. Thus lisdexamfetamine functions as an extended release version of dexamphetamine. Because <small>d</small>-amphetamine needs to be liberated from lysine via contact with red blood cells, effects are independent of route of administration. Conversion of lisdexamfetamine into active <small>d</small>-amphetamine is enzymatically [[Rate-Limiting Step|rate-limited]], slowing down the time to achieve peak concentrations and decreasing its magnitude and dampening consequent striatal dopamine release, which is thought to be responsible for its euphoric and [[compulsive redosing]] effects.


===Pharmacodymanics===
===Pharmacodymanics===