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Sulbutiamine article. This is not a forum for general discussion of the article's subject. |
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Can someone that understands this better look at the 'mechanisms of action' section and fix the wording of this sentence?:
"Sulbutiamine is a thiamine derivative which has two different properties in comparison with vitamin B1 as a result of structural modification of free thiamine, namely opening of the thiazole ring, esterification of the alcohol groups and dimerization, with formation of a disulfide bridge." 209.63.116.205 ( talk) 16:51, 2 October 2008 (UTC)
Excuse me if this is a dumb question, but I notice that the systematic name doesn't seem to take account of the fact that sulbutiamine is a dimer: the two aromatic groups are listed as "[4-[(4-amino-2-methyl-pyrimidin-5-yl]" and "3-[2-[(etc." despite being identically placed. I don't do this at all often, but I would render sulbutiamine as S-S'-5-aza-N-formyl-6-(4-amino-2-methyl-pyrimidin-5-yl)-3-thio-3-hexenyl 2-methylpropionate, or even S-bis- etc. If the suffix conflicts with the dimerization, then a 2-methylpropoxycarbonyl could be stuck in before the pyrimidinyl, or could it? Scutigera ( talk) 18:10, 4 July 2012 (UTC)
Over the past week, I have made numerous content additions and improvements to the article. At this point, practically every published source on sulbutiamine has been incorporated into the article and cited. Compared to other drugs, there is not a lot of information on sulbutiamine, and the length of the article will invariably be limited by the number of reliable sources. However, I believe that the article is currently B quality on the assessment scale, and I would like to see it reach GA quality in the future. Firewall62 ( talk) 19:39, 6 April 2009 (UTC)
The abstract used for source 5 doesn't seem to really support the wording used in the adverse events portion about the bipolar person. It doesn't seem to mention anything about a prescription being written, and, in fact, speaks of the dangers of over the counter medications. This section of the article seems to imply more of a medical distinction on sulbatiamine than is warranted by the source cited. Maybe this is in the full-text, but I doubt it based upon how the abstract is worded (i.e. "his psychiatric care was severely compromised through him defaulting appointments and frequent changes of psychiatrists")
71.2.123.68 ( talk) 19:22, 25 August 2009 (UTC)
We need more adverse effects mentioned. So far, I'm just finding anecdotes and conjecture, but what I find are many reports of addiction or discontinuation side-effects. The rationale seems to be that it makes dopamine receptors more sensitive but causes there to be less of them. There are articles in journals that make you wonder this, but they are too technical for me to understand. There are even people using sulbutiamine recreationally. They claim they quit taking it after 4 days and feel lethargy and headache. There has to be some real information on this out there.
72.11.53.145 (
talk)
05:13, 26 May 2014 (UTC)
Is a reference available for the erectile dysfunction and memory claim? Or is it included in the bi-polar article of reference 5? Access to the full article requires a paid subscription. From the abstract it doesn't sound like it would cover erectile dysfunction or memory aspects of Sulbutiamine. —Preceding unsigned comment added by 184.77.198.218 ( talk) 18:17, 15 June 2010 (UTC)
I have removed fairly extensive claims of therapeutic benefit that were based on sources failing our sourcing requirements for such claims. Please don't restore that content without high-quality, recent secondary sources. -- Scray ( talk) 09:04, 15 March 2013 (UTC)
This will require some heavy citation but I feel the mechanism section does not address the fundamental issue of how sulbutiamine is transformed into thiamine. It should be added that the disulfide bond is cleaved in vitro, likely after entering the CNS where the thiol monomers are deprotonated to the thiolate anions leading to an intramolecular attack on the amide carbonyl, which is followed by ring closure and dehydration to the thiazolium cation. Or something like that. Glucuronide ( talk) 05:59, 20 March 2015 (UTC)
DE1620538 is a valid granted patent with a priority date of 1965-03-18 and a granted date of 1977-12-31 that contains a composition of matter claim for the chemical structure that corresponds to sulbutiamine and process claims for synthesizing it. If the structure of sulbutiamine had previously been reported in the patent or scientific literature, this would have been regarded as prior art and a patent would never have been granted. Furthermore it is obvious that if the structure had never been reported before, then a synthesis for could not have been previously described either. Hence to say this is the first reported synthesis of sulbutiamine is not original research. This is implicit in the patent. What we are relying on is the patent examiners doing their job to identify relevant prior art and not on any original research on our part. Boghog ( talk) 12:48, 15 March 2015 (UTC)
DE1620538 patent family bibliographic information
|
---|
For reference, GB1089475 is in the same patent family (essentially the same patent filed in a different country):
Both claim a priority date of 1965-03-18 from Japanese patent application JP19650015344. Also for reference, the Chemical Abstract Service reports that the following citations are the first publications of sulbutiamine by the same group. These were published shortly after the Japanese patent application filed:
|
OK so change it to "A synthesis of sulbtiamine was reported..." although I find it very unlikely there is a synthesis that predates the one I posted, it is the earliest synthesis indexed by scifinder and reaxys. It's amazing how outright errors can persist on wikipedia for so long (like the version the preceded my edit) but the moment well cited information is introduced everyone is up in arms. Glucuronide ( talk) 05:58, 20 March 2015 (UTC)
The following makes definitive statements in the content about how this drug that people take, works in people. It is invalid to make blanket statements like this for CNS drugs (cancer is one thing, where we can pull a tumor out of somebody and get a decent idea of what it is doing to human tissue. can't do that with a human brain). This needs to be way, way toned down and it made clear this is rodent work.
![]() | The following mainly relies on primary sources. |
![]() | Animal studies referred to are not clearly stated as such. |
Sulbutiamine is a lipophilic molecule that crosses the blood–brain barrier more easily than thiamine. Its metabolism in the brain leads to an increase in the levels of thiamine and thiamine phosphate esters. [1] [2] While the exact mechanism of action of sulbutiamine is unknown, it is thought to occur through the upregulation of the reticular activating system, which is the center of arousal and motivation in the brain. [3] The administration of sulbutiamine potentiates glutamatergic activity in the prefrontal cortex through a reduction in the density of kainate glutamate receptors, which may occur in response to a modulation of intrasynaptic glutamate. [4] The facilitation of central glutamatergic transmission is a likely explanation for the ability of sulbutiamine to improve memory. [5] [6] [7] [8] In addition to its action on cholinergic and glutamatergic transmission, the administration of sulbutiamine reduces the release of dopamine in the prefrontal cortex, which increases the density of D1 dopamine receptors through a compensatory mechanism. [4] The modulation of dopaminergic transmission may also contribute to the ability of sulbutiamine to improve memory. [9] [10] [11] A possible explanation for the pharmacodynamics of sulbutiamine is the increased availability of thiamine triphosphate (ThTP). Although the full physiological role of ThTP is unknown, it is an integral component of synaptosomal membranes, [12] participates in the phosphorylation of proteins, [13] and activates chloride channels that have a large unit conductance. [14] The activation of chloride channels by ThTP may be involved in the modulation of receptor binding.
References
Bettendorff_2
was invoked but never defined (see the
help page).Van Reeth
was invoked but never defined (see the
help page).{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
- Jytdog ( talk) 10:30, 24 April 2016 (UTC)
This whole page is a commercial for sulbutiamine. Having taken sulbutiamine a while, and gotten really sick from it, as did other people on amazon reviews I can say it does not have thiamine activity. It is chemically similar to thiamine disulfide which is a known thiamine transporter inhibitor in several studies. So it induces thiamine deficiency in the user. How about a section about this. Canyouguessmyname ( talk) 23:23, 23 January 2018 (UTC)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1192637/pdf/jphysiol00562-0096.pdf https://www.ncbi.nlm.nih.gov/pmc/articles/PMC235561/pdf/jbacter00304-0307.pdf
I will change the page accordingly to something like "Sulbutiamine is a thiamine transporter inhibitor that is marketed as a nootropic" Canyouguessmyname ( talk) 01:08, 27 January 2018 (UTC)
So
Going to need to dig for books and other stuff it seems
starting to dig through various books... will post things as I find them... Jytdog ( talk) 03:46, 27 January 2018 (UTC)
Arcalion is a brand of sulbutiamine 200 mg per tablet. Sulbutiamine was first marketed by Servier in France in 1973, with the name Arcalion. The tablet doses at 100 mg were discontinued in January 1989, leaving only 200 mg tablets in the market. The product has since undergone a 'validation procedure', as required by European directive 75/319/EEC, in the 1983 to 1994 editions of the French data slheet compendium (Vidal), the licenced indication was 'proposed for symptomatic treatmnent of functional fatigue'. According to a statement by the French medicine agency the expression 'proposed for' means that, despite pharmacological properties. the clinical indications for a given drug have not been validated in comparative clinical trials. In the conclusion it says "The wording of the indications for sulbutiamine is unacceptable. The term 'certain inhibitory states' is meaningless" (Prescrire International, August 1996, vol 5, no 24). Mental and physical inhibition can correspond to a variety of conditions, ranging from exhaustion due to overwork to depression or psychosis. When a patient complains of fatigue, every attempt must be made to identify the precise cause: it is not enough simply to rule out depression. There are no clinical trial data on which health professionals can base their judgment on sulbutiamine. The only published clinical trial is totally worthless. Neither Servier group nor the French medicines agency should be proud of this affair.
This is the
talk page for discussing improvements to the
Sulbutiamine article. This is not a forum for general discussion of the article's subject. |
Article policies
|
Find sources: Google ( books · news · scholar · free images · WP refs) · FENS · JSTOR · TWL |
![]() | This article is rated B-class on Wikipedia's
content assessment scale. It is of interest to the following WikiProjects: | ||||||||||
|
![]() | Ideal sources for Wikipedia's health content are defined in the guideline
Wikipedia:Identifying reliable sources (medicine) and are typically
review articles. Here are links to possibly useful sources of information about Sulbutiamine.
|
![]() | Sulbutiamine received a peer review by Wikipedia editors, which is now archived. It may contain ideas you can use to improve this article. |
Can someone that understands this better look at the 'mechanisms of action' section and fix the wording of this sentence?:
"Sulbutiamine is a thiamine derivative which has two different properties in comparison with vitamin B1 as a result of structural modification of free thiamine, namely opening of the thiazole ring, esterification of the alcohol groups and dimerization, with formation of a disulfide bridge." 209.63.116.205 ( talk) 16:51, 2 October 2008 (UTC)
Excuse me if this is a dumb question, but I notice that the systematic name doesn't seem to take account of the fact that sulbutiamine is a dimer: the two aromatic groups are listed as "[4-[(4-amino-2-methyl-pyrimidin-5-yl]" and "3-[2-[(etc." despite being identically placed. I don't do this at all often, but I would render sulbutiamine as S-S'-5-aza-N-formyl-6-(4-amino-2-methyl-pyrimidin-5-yl)-3-thio-3-hexenyl 2-methylpropionate, or even S-bis- etc. If the suffix conflicts with the dimerization, then a 2-methylpropoxycarbonyl could be stuck in before the pyrimidinyl, or could it? Scutigera ( talk) 18:10, 4 July 2012 (UTC)
Over the past week, I have made numerous content additions and improvements to the article. At this point, practically every published source on sulbutiamine has been incorporated into the article and cited. Compared to other drugs, there is not a lot of information on sulbutiamine, and the length of the article will invariably be limited by the number of reliable sources. However, I believe that the article is currently B quality on the assessment scale, and I would like to see it reach GA quality in the future. Firewall62 ( talk) 19:39, 6 April 2009 (UTC)
The abstract used for source 5 doesn't seem to really support the wording used in the adverse events portion about the bipolar person. It doesn't seem to mention anything about a prescription being written, and, in fact, speaks of the dangers of over the counter medications. This section of the article seems to imply more of a medical distinction on sulbatiamine than is warranted by the source cited. Maybe this is in the full-text, but I doubt it based upon how the abstract is worded (i.e. "his psychiatric care was severely compromised through him defaulting appointments and frequent changes of psychiatrists")
71.2.123.68 ( talk) 19:22, 25 August 2009 (UTC)
We need more adverse effects mentioned. So far, I'm just finding anecdotes and conjecture, but what I find are many reports of addiction or discontinuation side-effects. The rationale seems to be that it makes dopamine receptors more sensitive but causes there to be less of them. There are articles in journals that make you wonder this, but they are too technical for me to understand. There are even people using sulbutiamine recreationally. They claim they quit taking it after 4 days and feel lethargy and headache. There has to be some real information on this out there.
72.11.53.145 (
talk)
05:13, 26 May 2014 (UTC)
Is a reference available for the erectile dysfunction and memory claim? Or is it included in the bi-polar article of reference 5? Access to the full article requires a paid subscription. From the abstract it doesn't sound like it would cover erectile dysfunction or memory aspects of Sulbutiamine. —Preceding unsigned comment added by 184.77.198.218 ( talk) 18:17, 15 June 2010 (UTC)
I have removed fairly extensive claims of therapeutic benefit that were based on sources failing our sourcing requirements for such claims. Please don't restore that content without high-quality, recent secondary sources. -- Scray ( talk) 09:04, 15 March 2013 (UTC)
This will require some heavy citation but I feel the mechanism section does not address the fundamental issue of how sulbutiamine is transformed into thiamine. It should be added that the disulfide bond is cleaved in vitro, likely after entering the CNS where the thiol monomers are deprotonated to the thiolate anions leading to an intramolecular attack on the amide carbonyl, which is followed by ring closure and dehydration to the thiazolium cation. Or something like that. Glucuronide ( talk) 05:59, 20 March 2015 (UTC)
DE1620538 is a valid granted patent with a priority date of 1965-03-18 and a granted date of 1977-12-31 that contains a composition of matter claim for the chemical structure that corresponds to sulbutiamine and process claims for synthesizing it. If the structure of sulbutiamine had previously been reported in the patent or scientific literature, this would have been regarded as prior art and a patent would never have been granted. Furthermore it is obvious that if the structure had never been reported before, then a synthesis for could not have been previously described either. Hence to say this is the first reported synthesis of sulbutiamine is not original research. This is implicit in the patent. What we are relying on is the patent examiners doing their job to identify relevant prior art and not on any original research on our part. Boghog ( talk) 12:48, 15 March 2015 (UTC)
DE1620538 patent family bibliographic information
|
---|
For reference, GB1089475 is in the same patent family (essentially the same patent filed in a different country):
Both claim a priority date of 1965-03-18 from Japanese patent application JP19650015344. Also for reference, the Chemical Abstract Service reports that the following citations are the first publications of sulbutiamine by the same group. These were published shortly after the Japanese patent application filed:
|
OK so change it to "A synthesis of sulbtiamine was reported..." although I find it very unlikely there is a synthesis that predates the one I posted, it is the earliest synthesis indexed by scifinder and reaxys. It's amazing how outright errors can persist on wikipedia for so long (like the version the preceded my edit) but the moment well cited information is introduced everyone is up in arms. Glucuronide ( talk) 05:58, 20 March 2015 (UTC)
The following makes definitive statements in the content about how this drug that people take, works in people. It is invalid to make blanket statements like this for CNS drugs (cancer is one thing, where we can pull a tumor out of somebody and get a decent idea of what it is doing to human tissue. can't do that with a human brain). This needs to be way, way toned down and it made clear this is rodent work.
![]() | The following mainly relies on primary sources. |
![]() | Animal studies referred to are not clearly stated as such. |
Sulbutiamine is a lipophilic molecule that crosses the blood–brain barrier more easily than thiamine. Its metabolism in the brain leads to an increase in the levels of thiamine and thiamine phosphate esters. [1] [2] While the exact mechanism of action of sulbutiamine is unknown, it is thought to occur through the upregulation of the reticular activating system, which is the center of arousal and motivation in the brain. [3] The administration of sulbutiamine potentiates glutamatergic activity in the prefrontal cortex through a reduction in the density of kainate glutamate receptors, which may occur in response to a modulation of intrasynaptic glutamate. [4] The facilitation of central glutamatergic transmission is a likely explanation for the ability of sulbutiamine to improve memory. [5] [6] [7] [8] In addition to its action on cholinergic and glutamatergic transmission, the administration of sulbutiamine reduces the release of dopamine in the prefrontal cortex, which increases the density of D1 dopamine receptors through a compensatory mechanism. [4] The modulation of dopaminergic transmission may also contribute to the ability of sulbutiamine to improve memory. [9] [10] [11] A possible explanation for the pharmacodynamics of sulbutiamine is the increased availability of thiamine triphosphate (ThTP). Although the full physiological role of ThTP is unknown, it is an integral component of synaptosomal membranes, [12] participates in the phosphorylation of proteins, [13] and activates chloride channels that have a large unit conductance. [14] The activation of chloride channels by ThTP may be involved in the modulation of receptor binding.
References
Bettendorff_2
was invoked but never defined (see the
help page).Van Reeth
was invoked but never defined (see the
help page).{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
{{
cite journal}}
: CS1 maint: multiple names: authors list (
link)
- Jytdog ( talk) 10:30, 24 April 2016 (UTC)
This whole page is a commercial for sulbutiamine. Having taken sulbutiamine a while, and gotten really sick from it, as did other people on amazon reviews I can say it does not have thiamine activity. It is chemically similar to thiamine disulfide which is a known thiamine transporter inhibitor in several studies. So it induces thiamine deficiency in the user. How about a section about this. Canyouguessmyname ( talk) 23:23, 23 January 2018 (UTC)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1192637/pdf/jphysiol00562-0096.pdf https://www.ncbi.nlm.nih.gov/pmc/articles/PMC235561/pdf/jbacter00304-0307.pdf
I will change the page accordingly to something like "Sulbutiamine is a thiamine transporter inhibitor that is marketed as a nootropic" Canyouguessmyname ( talk) 01:08, 27 January 2018 (UTC)
So
Going to need to dig for books and other stuff it seems
starting to dig through various books... will post things as I find them... Jytdog ( talk) 03:46, 27 January 2018 (UTC)
Arcalion is a brand of sulbutiamine 200 mg per tablet. Sulbutiamine was first marketed by Servier in France in 1973, with the name Arcalion. The tablet doses at 100 mg were discontinued in January 1989, leaving only 200 mg tablets in the market. The product has since undergone a 'validation procedure', as required by European directive 75/319/EEC, in the 1983 to 1994 editions of the French data slheet compendium (Vidal), the licenced indication was 'proposed for symptomatic treatmnent of functional fatigue'. According to a statement by the French medicine agency the expression 'proposed for' means that, despite pharmacological properties. the clinical indications for a given drug have not been validated in comparative clinical trials. In the conclusion it says "The wording of the indications for sulbutiamine is unacceptable. The term 'certain inhibitory states' is meaningless" (Prescrire International, August 1996, vol 5, no 24). Mental and physical inhibition can correspond to a variety of conditions, ranging from exhaustion due to overwork to depression or psychosis. When a patient complains of fatigue, every attempt must be made to identify the precise cause: it is not enough simply to rule out depression. There are no clinical trial data on which health professionals can base their judgment on sulbutiamine. The only published clinical trial is totally worthless. Neither Servier group nor the French medicines agency should be proud of this affair.