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Lisdexamfetamine: Difference between revisions
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===Pharmacodymanics=== | ===Pharmacodymanics=== | ||
Amphetamine is a [[Agonist|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]].<ref>The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | Amphetamine is a [[Agonist|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]].<ref>{{cite journal | vauthors=((Miller, G. M.)) | journal=Journal of neurochemistry | title=The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity | volume=116 | issue=2 | pages=164–176 | date= January 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005101/ | issn=0022-3042 | doi=10.1111/j.1471-4159.2010.07109.x}}</ref><ref>{{Citation |title=Drug banks amphetamine targets |url=http://www.drugbank.ca/drugs/DB00182#targets}}</ref><ref>TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364</ref> 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 [[Thought acceleration|cognitive]] and [[Stimulation|physical stimulation]] within the user. | ||
<small>d</small>-amphetamine's affinity for the TAAR1 receptor is twice that of <small>l</small>-amphetamine.<ref>https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3236098/</ref> As a result, <small>d</small>-amphetamine produces three to four times as much central nervous system (CNS) stimulation as <small>l</small>-amphetamine. <small>l</small>-amphetamine, on the other hand, has stronger cardiovascular and peripheral effects. | <small>d</small>-amphetamine's affinity for the TAAR1 receptor is twice that of <small>l</small>-amphetamine.<ref>{{cite journal | vauthors=((Lewin, A. H.)), ((Miller, G. M.)), ((Gilmour, B.)) | journal=Bioorganic & medicinal chemistry | title=Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class | volume=19 | issue=23 | pages=7044–7048 | date=1 December 2011 | url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3236098/ | issn=0968-0896 | doi=10.1016/j.bmc.2011.10.007}}</ref> As a result, <small>d</small>-amphetamine produces three to four times as much central nervous system (CNS) stimulation as <small>l</small>-amphetamine. <small>l</small>-amphetamine, on the other hand, has stronger cardiovascular and peripheral effects. | ||
===Conversion rate=== | ===Conversion rate=== | ||
29.7% of the weight of lisdexamfetamine dimesylate (the usual prescribed form) is dexamphetamine: 30 mg lisdexamfetamine dimesylate is equivalent to 8.9 mg of dexamfetamine.<ref>https://www.medicines.org.uk/emc/medicine/27442/SPC/</ref><ref>[https://39f93cda-b262-4d28-a694-bf36a6802943.filesusr.com/ugd/1da6d0_55267f5b04204cb58bcc848398c0286f.pdf Stimulant Equivalency Table]</ref> | 29.7% of the weight of lisdexamfetamine dimesylate (the usual prescribed form) is dexamphetamine: 30 mg lisdexamfetamine dimesylate is equivalent to 8.9 mg of dexamfetamine.<ref>{{Citation | title=Elvanse 20mg, 30mg, 40mg, 50mg, 60mg & 70mg Capsules, hard - Summary of Product Characteristics (SmPC) - (emc) | url=https://www.medicines.org.uk/emc/medicine/27442/SPC/}}</ref><ref>[https://39f93cda-b262-4d28-a694-bf36a6802943.filesusr.com/ugd/1da6d0_55267f5b04204cb58bcc848398c0286f.pdf Stimulant Equivalency Table]</ref> | ||
The subjective experience will differ due to the slower, more steady release of active substance in the [[prodrug]]. An equivalent dose of dexamphetamine will have a higher peak plasma concentration and shorter duration. | The subjective experience will differ due to the slower, more steady release of active substance in the [[prodrug]]. An equivalent dose of dexamphetamine will have a higher peak plasma concentration and shorter duration. | ||
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*'''[[Effect::Spontaneous bodily sensations]]''' - The "body high" of lisdexamphetamine 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. | *'''[[Effect::Spontaneous bodily sensations]]''' - The "body high" of lisdexamphetamine 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. | ||
*'''[[Effect::Abnormal heartbeat]]'''{{citation needed}} | *'''[[Effect::Abnormal heartbeat]]'''{{citation needed}} | ||
*'''[[Effect::Increased heart rate]]'''<ref>Huang | *'''[[Effect::Increased heart rate]]'''<ref>{{cite journal | vauthors=((Huang, Y.-S.)), ((Tsai, M.-H.)) | journal=CNS Drugs | title=Long-Term Outcomes with Medications for Attention-Deficit Hyperactivity Disorder: Current Status of Knowledge | volume=25 | issue=7 | pages=539–554 | date= July 2011 | url=http://link.springer.com/10.2165/11589380-000000000-00000 | issn=1172-7047 | doi=10.2165/11589380-000000000-00000}}</ref> | ||
*'''[[Effect::Increased blood pressure]]'''{{citation needed}} | *'''[[Effect::Increased blood pressure]]'''{{citation needed}} | ||
*'''[[Effect::Appetite suppression]]''' - This effect is more pronounced compared to [[amphetamine]], sometimes causing people to not eat for the entire duration of action. Lisdexamfetamine is sometimes prescribed to treat binge eating disorder due to its strong appetite suppressing effect. | *'''[[Effect::Appetite suppression]]''' - This effect is more pronounced compared to [[amphetamine]], sometimes causing people to not eat for the entire duration of action. Lisdexamfetamine is sometimes prescribed to treat binge eating disorder due to its strong appetite suppressing effect. | ||
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*'''Australia''': It is a Schedule 8 drug.{{citation needed}} | *'''Australia''': It is a Schedule 8 drug.{{citation needed}} | ||
*'''Canada''': Lisdexamfetamine, as well as other amphetamines, is a Schedule I drug.<ref> | *'''Canada''': Lisdexamfetamine, as well as other amphetamines, is a Schedule I drug.<ref>{{Citation | year=2022 | title=Consolidated federal laws of Canada, Controlled Drugs and Substances Act | url=https://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-15.html}}</ref> | ||
*'''Germany''': Lisdexamfetamine is controlled under Anlage III BtMG (''Narcotics Act, Schedule III'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html|title=Anlage III BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref> as of July 17, 2013.<ref>{{cite web|url=https://www.bgbl.de/xaver/bgbl/start.xav#__bgbl__//*%5B@attr_id=%27bgbl113s2274.pdf%27%5D|title=Siebenundzwanzigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften|publisher=Bundesanzeiger Verlag|access-date=December 19, 2019|language=de}}</ref> It can only be prescribed on a narcotic prescription form.<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmvv_1998/__8.html|title=§ 8 BtMVV|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref> | *'''Germany''': Lisdexamfetamine is controlled under Anlage III BtMG (''Narcotics Act, Schedule III'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html|title=Anlage III BtMG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref> as of July 17, 2013.<ref>{{cite web|url=https://www.bgbl.de/xaver/bgbl/start.xav#__bgbl__//*%5B@attr_id=%27bgbl113s2274.pdf%27%5D|title=Siebenundzwanzigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften|publisher=Bundesanzeiger Verlag|access-date=December 19, 2019|language=de}}</ref> It can only be prescribed on a narcotic prescription form.<ref>{{cite web|url=https://www.gesetze-im-internet.de/btmvv_1998/__8.html|title=§ 8 BtMVV|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 19, 2019|language=de}}</ref> | ||
*'''Norway''': Lisdexamfetamine is a Class A drug under particularly strict control. | *'''Norway''': Lisdexamfetamine is a Class A drug under particularly strict control. | ||
*'''Sweden''': Lisdexamfetamine is a Class II narcotic, with strict requirements for prescription. It has been placed under "utökad övervakning" (extended surveillance).<ref name="swe"> | *'''Sweden''': Lisdexamfetamine is a Class II narcotic, with strict requirements for prescription. It has been placed under "utökad övervakning" (extended surveillance).<ref name="swe">{{Citation | title=Elvanse - FASS Allmänhet | url=https://www.fass.se/LIF/product?userType=2&nplId=20140730000117}}</ref> | ||
*'''Switzerland''': Lisdexamphetamine is a controlled substance as of October 1, 2014 specifically named under Verzeichnis A. Medicinal use is permitted.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref> | *'''Switzerland''': Lisdexamphetamine is a controlled substance as of October 1, 2014 specifically named under Verzeichnis A. Medicinal use is permitted.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref> | ||
*'''United Kingdom''': Lisdexamfetamine is a Class B scheduled drug.{{citation needed}} | *'''United Kingdom''': Lisdexamfetamine is a Class B scheduled drug.{{citation needed}} | ||
*'''United States''': Lisdexamfetamine is a Schedule II controlled drug.<ref>https://www.law.cornell.edu/uscode/text/21/812#b_4</ref> | *'''United States''': Lisdexamfetamine is a Schedule II controlled drug.<ref>{{Citation | title=21 U.S. Code § 812 - Schedules of controlled substances | url=https://www.law.cornell.edu/uscode/text/21/812#b_4}}</ref> | ||
==See also== | ==See also== | ||