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Scientific Research

Table of Contents: Sources and Composition Structure Neurology and the Brain Kinetics and Distribution Neuroprotection Neuropathy Glutaminergic Signalling Cholinergic Signalling Memory Fatigue Addiction and Withdrawal nteractions with Glucose Metabolism nteractions with !rgan Systems "yes nteractions with Se#uality

Edit1. Sources and Composition


Sulbutiamine is a molecule which is two $hiamin %B&' molecules bound together( similar to how )yritinol is two )yrido#ine %B*' molecules bound together+ Sulbutiamine is ,nown as isobutyryl thiamine disulfide and sometimes re-erred to by its Brand Names o"reon or Arcalion. it is most commonly used -or Asthenia( or wea,ness %part neurological and part myopathic' as well as treatment o- somatic and psychic inhibition+/&0 t is said to not possess psychostimulant properties( although it is designed to act centrally %in the brain'+/&0 1.1. Structure Sulbutiamine is synthesi1ed -rom $hiamine( where a-ter opening o- the thia1ole ring o$hiamin and dimerisation to a disul-ide compound it is then esteri-ied+/20

Edit2. Neurology and the Brain


2.1. inetics and !istribution Due to the lipophilicity %-at3solubility' o- Sulbutiamine( transport into the brain -rom systemic circulation is greater relati4e to $hiamin+ A-ter an in5ection o- Sulbutiamine %&*mg6,g' and $hiamine %&7+8mg6,g' were both able to acutely increase plasma thiamine le4els without in-luencing serum $hiamin Diphosphate %demonstrating the e--icacy oSulbutiamine as a 4itamin deli4ery -orm( able to biotrans-orm into $hiamin in vivo'+/90 A chronic study o- in5ecting sulbutiamine %72mg6,g' and thiamine %7:mg6,g' daily -or 2

wee,s in rats noted that despite these similar doses that sulbutiamine was able to increase total circulating thiamin( $hiamine diphosphate( and $hiamine Monophosphate le4els 2+8& times higher than that o- $hiamin itsel-+/90 n other measured organs %hippocampus( medulla( cerebellum( corte#( and ,idney' le4els o- $hiamin $riphophate were only increased with sulbutiamine( and sulbutiamine increased total thiamine compounds higher than $hiamine in all organs e#cept the hippocampus+/90 2.2. Neuroprotection Sulbutiamine may protect neuronal cells %in the hippocampus' -rom o#ygen6glucose depri4ation according to one study+/80 $his study used a staining protocol to identi-y dead cells -rom glucose6o#ygen depri4ation( and the *+&3-old increase seen in control was attenuated to a 8+&3-old increase when Sulbutiamine was incubated at 7:uM+ $he disruption o- synaptic transmission that occurs under these conditions o- nutrient depri4ation/70 was preser4ed with sulbutiamine to a degree( measuring preser4ation at 27+&;632+2&<( 8=+9;639+&&< and **+9;63&&+:< -or the concentrations o- &( &:( and 7:uM when control was standardi1ed to &::< and the group without Sulbutiamine recorded &2+>;63?+><+/80 2.". Neuropathy A * wee, trial in humans with type diabetes and diabetic neuropathy using Sulbutiamine at 8::mg daily noted that on the signs and symptoms scores %constricting sensation( paraesthesia( pain and wea,ness -or symptoms. etc+' there was an impro4ement when compared against baseline but no impro4ement against placebo %and thus it was deemed no o4erall impro4ement'+/*0 mpro4ement was noted in electrophysical measures( including ner4e conduction 4elocity and compound motor action potential+/*0 2.#. $lutaminergic Signalling )ositi4e glutaminergic and dopaminergic transmission has been noted in anterior corticol regions( speci-ically the pre-rontal and cingular cortices which organi1e decisions and strategies+/&0 Daily in5ections o- &2+7mg6,g sulbutiamine -or 2 wee,s prior to sacri-ice noted decreases in ,ainate receptors in tested areas as well as decreased dopamine le4els( despite no changes in dopamine receptor content+/&0 No 4ariations in dopaminergic or glutaminergic receptors were noted in the nuclear accumbens(/&0 and in a model o- glucose6o#ygen depri4ation( Sulbutiamine at &( 7( and 7:uM -ailed to modi-y e#citability o- neurons in the hippocampus+/80 2.%. Cholinergic Signalling n an animal model where Sulbutiamine was -ed at 9::mg6,g -or &: days( the rate osodium3dependent choline upta,e into the hippocampus appeared to be increased appro#imately &:+&< when compared to gum acacia control+/=0 2.&. 'emory n a model o- BA@B6c mice &83&* wee,s o- age( &: days o- 9::mg6,g sulbutiamine by oral ga4age with 7< gum acacia appeared to impro4e memory %assessed by operant tas,'. this study noted that there were no di--erences between groups in acAuisition but there were signi-icant di--erences in retention which resulted in increased per-ormance+/=0 n5ections o- &2+7 and 27mg6,g Sulbutiamine daily -or ? wee,s -ailed to modi-y

per-ormance in a DNM$S tas, %operant conditioning ma1e' and at times &2+7mg sulbutiamine was associated with a greater amount o- encoding errors+/>0 When di1ocilpine %NMDA antagonist that induces amnesia' was administered during the DNM$S tas,( sulbutiamine was able to negate the amnesiac e--ects o- it on the mice and preser4e per-ormance+/>0 Sulbutiamine has been implicated in increasing ob5ect3recognition memory in mice at both &2+7 and 27mg6,g in5ections o4er ? wee,s+/>0 2.(. )atigue !ne study has been conducted on chronic postin-ectious -atigue %C) F' with sulbutiamine at either 8:: or *::mg daily -or 2> days noted that both groups had signi-icantly less -atigue than placebo( but that -or the most part there was no signi-icant di--erence between groups with the *::mg group inconsistently per-orming better at times+/?0 A similar study using a large %uncontrolled( unblinded' sample o- persons seeing their doctors about in-ection who reported at least one symptom o- -atigue gi4en 8::mg Sulbutiamine at brea,-ast daily -or &7 days alongside their anti3in-ecti4e treatment noted complete resolution o- sel-3reported asthenic symptoms in 7&+=< o- the study population+
/&:0

mpro4ement has also been noted regarding -atigue in ?&+9=< o- persons tested %nB*:' with Multiple Sclerosis( with =8+&9< o- the sample reporting the impro4ement as CsubstantialC %analysis was done 4ia sub5ecti4e impro4ement' with no reported e#acerbation in -atigue state+/&&0 2.*. +ddiction and ,ithdra-al A case study currently e#ists where a patient with bipolar disorder became addicted to sulbutiamine+/&20 $he sub5ect was using high dose antipsychotics %olan1apine and haloperidol at 2:mg( the ben1odia1epines dia1epam and tema1epam at 8:mg and &:mg( &:mg biperiden( unspeci-ied doses o- lithium and carbama1epine' and reported that his large doses %abo4e *::mg but otherwise unspeci-ied' made him -eel stronger and warmer+
/&20

!ne study in primeapes using a large dose o- sulbutiamine %9::mg6,g daily -or &: days' noted that while Sulbutiamine was able to in-luence the circadian rhythm %increasing wa,e-ulness and reducing phase 2 sleep while increasing phase & and not a--ecting D"M' that &: days o- usage was associated with 237 days o- withdrawal+/&90

Edit". .nteractions -ith $lucose 'etabolism


An inter4ention o4er * wee,s in type diabetics using 8::mg sulbutiamine -ailed to -ind a decrease in blood glucose or EbA&c associated with treatment+/*0

Edit#. .nteractions -ith /rgan Systems


#.1. Eyes Due to the interactions o- proo#idation and e#citoto#icity in glaucoma as well as $haimine being lower in glaucoma patients/&80 with a case study showing $hiamin in5ections increase 4isual acuity(/&70 Sulbutiamine has been in4estigated -or its interactions with retinal cells+/&*0 An in vitro study using DGC37 %Ganglion3li,e' cells noted that Sulbutiamine was able to attenuate cell death when cells were depri4ed o- serum( and

&:uM Sulbutiamine was as e--ecti4e as &:uM $rolo# %anti3o#idant standard' while attenuation was seen signi-icantly at &uM. these protecti4e e--ects were associated with a seAuestering the increase in supero#ide and pero#ide radicals( with no in-luence on hydro#yl radicals( and a relati4e increase in glutathione+/&*0

Edit%. .nteractions -ith Se0uality


At least one study has noted bene-its to psychogenic erectile dys-unction that can be treated with Sulbutiamine( increasing per-ormance as assessed by the nternational nde# o- "rectile Function % "F' -rom &=+7 to 28+> on a4erage+/&=0

Scientific Support 1 Reference Citations


References
&3$ro4ero F( et al+ "4idence -or a modulatory e--ect o- sulbutiamine on glutamatergic and dopaminergic cortical transmissions in the rat brain+ Neurosci Lett+ %2:::' 23Determination o- sulbutiamine and its disul-ide deri4ati4es in human plasma by E)@C using on3line post3column reactors and -luorimetric detection 93Bettendor-- @( et al+ n5ection o- sulbutiamine induces an increase in thiamine triphosphate in rat tissues+ Biochem Pharmacol+ %&??:' 83Kwag F( Ma5id AS( Kang KD+ "4idence -or neuroprotecti4e e--ect o- sulbutiamine against o#ygen3glucose depri4ation in rat hippocampal CA& pyramidal neurons+ Biol Pharm Bull+ %2:&&' 73$anabe M( Nitta A( !no E+ Neuroprotection 4ia strychnine3sensiti4e glycine receptors during post3ischemic reco4ery o- e#citatory synaptic transmission in the hippocampus+ J Pharmacol Sci+ %2:&:' *3Kiew KK( et al+ "--ects o- sulbutiamine on diabetic polyneuropathyG an open randomised controlled study in type 2 diabetics+ Malays J Med Sci+ %2::2' =3Micheau F( et al+ Chronic administration o- sulbutiamine impro4es long term memory -ormation in miceG possible cholinergic mediation+ Pharmacol Biochem Behav+ %&?>7' >3Bi1ot FC( et al+ Chronic treatment with sulbutiamine impro4es memory in an ob5ect recognition tas, and reduces some amnesic e--ects o- di1ocilpine in a spatial delayed3non3match3to3sample tas,+ Prog Neuropsychopharmacol Biol Psychiatry+ %2::7' ?3$ie4 K)( Cabane F( mbert FC+ $reatment o- chronic postin-ectious -atigueG randomi1ed double3blind study o- two doses o- sulbutiamine %8::3*:: mg6day' 4ersus placebo+ Rev Med Interne+ %&???' &:3Shah SN. Sulbutiamine Study Group+ Ad5u4ant role o- 4itamin B analogue %sulbutiamine' with anti3in-ecti4e treatment in in-ection associated asthenia+ J Assoc Physicians India+ %2::9' &&3Sulbutiamine( an CinnocentC o4er the counter drug( inter-eres with therapeutic outcome o- bipolar disorder+ orld J Biol Psychiatry+ %2::*' &93Bal1amo "( Huillon3Cacciuttolo G+ Facilitation o- a state o- wa,e-ulness by semi3

chronic treatment with sulbutiamin %Arcalion' in Macaca mulatta+ Rev !lectroencephalogr Neurophysiol "lin+ %&?>2' &83Asregadoo "D+ Blood le4els o- thiamine and ascorbic acid in chronic open3angle glaucoma+ Ann #phthalmol+ %&?=?' &73Sedel F( et al+ $hiamine responsi4e pyru4ate dehydrogenase de-iciency in an adult with peripheral neuropathy and optic neuropathy+ J Neurol Neurosurg Psychiatry+ %2::>' &*3Kang KD( et al+ Sulbutiamine counteracts trophic -actor depri4ation induced apoptotic cell death in trans-ormed retinal ganglion cells+ Neurochem Res+ %2:&:' &=3Dmitrie4 DG( Gamido4 S ( )ermia,o4a !H+ Clinical e--icacy o- the drug enerion in the treatment o- patients with psychogenic %-unctional' erectile dys-unction+ $rologiia+ %2::7' %Common phrases used by users -or this page include sulbutiamine ta,e it daily( sulbutaiamine dosage( salbutamine( composition o- sulbutiamin( arcalion bodybuilding( Sulbutamine beni-its' %Isers who contributed to this page include KurtisFran,'

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