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Sulbutiamine
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| Systematic (IUPAC) name | |
| [4-[(4-amino-2-methyl-pyrimidin-5-yl)methyl-formyl- amino]-3-[2-[(4-amino-2-methyl-pyrimidin-5-yl)methyl- formyl-amino]-5-(2-methylpropanoyloxy)pent-2-en-3- yl]disulfanyl-pent-3-enyl] 2-methylpropanoate |
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| Identifiers | |
| CAS number | |
| ATC code | A11 |
| PubChem | |
| Chemical data | |
| Formula | C32H46N8O6S2 |
| Mol. mass | 702.89 g/mol |
| SMILES | & |
| Synonyms | Arcalion, bisibuthiamine, youvitan |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 5 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | Oral |
Sulbutiamine (brand name: Arcalion) is a precursor to thiamine (i.e., vitamin B1).
Contents |
Uses
It is indicated for the treatment of asthenia.[1] Furthermore, the ability of sulbutiamine to reduce fatigue is considered desirable by athletes, and it is available for over-the-counter sale as a nutritional supplement. Additionally, the demonstrated ability of sulbutiamine to improve memory in rats[2] and patients of schizophrenia[2] suggests that it is a nootropic. New research show support for use in erectile dysfunction [3]
Effects
Sulbutiamine reduces fatigue, memory difficulties, intellectual tiredness and may speed convalescence.[4]
Dosage
Sulbutiamine is sometimes supplied in 200 mg tablets. The proper therapeutic dosage has been reported to be 12.5 mg/kg,[2] which corresponds to 850 mg for a 68 kg (150 lb) person. However, it should be noted that dosage recommendations vary; the manufacturer of Arcalion, for example, recommends no more than 600 mg per day.
Mechanisms of action
Sulbutiamine crosses the blood brain barrier more easily than vitamin B1 because of its lipophilic properties. It leads to an increased formation of thiamine triphosphate (TTP) that acts as a regulator of the synaptic transmission of many neurotransmission systems.
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.
References
- ^ Shah SN; Sulbutiamine Study Group (2003). "Adjuvant role of vitamin B analogue (sulbutiamine) with anti-infective treatment in infection associated asthenia.". J Assoc Physicians India 51: 891–5. PMID 14710977.
- ^ a b c Bizot JC, Herpin A, Pothion S, Pirot S, Trovero F, Ollat H (2005). "Chronic treatment with sulbutiamine improves memory in an object recognition task and reduces some amnesic effects of dizocilpine in a spatial delayed-non-match-to-sample task.". Prog Neuropsychopharmacol Biol Psychiatry 29 (6): 928–35. doi:. PMID 15951087.
- ^ Urologiia. 2005 Jan-Feb;(1):32-5. [Clinical efficacy of the drug enerion (sulbutiamine) in the treatment of patients with psychogenic (functional) erectile dysfunction] Dmitriev DG, Gamidov SI, Permiakova OV.
- ^ Serdia Pharmaceuticals | About Serdia | Product Portfolio | Arcalion
External links
- "New Drugs that Make you Smart" by John Morgenthaler at hoboes.com
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