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Sulbutiamine was initially synthesized in Japan as an adjunct treatment for B vitamin deficiencies (e.g. beri-beri) and asthenia. Exact date of its development is unknown; however, early studies involving sulbutiamine use were documented on the early 1970s. It was primarily created to enhance thiamine lipophilicity which helps to increase levels of thiamine phosphate esters and thiamine in the brain.
Sulbutiamine, also known by its brand name, Arcalion, is a synthetic analog of vitamin B1 (thiamine). It is a fat soluble lipophilic drug compound which readily passes the blood brain barrier resulting to enhanced pharmacokinetic properties. Since sulbutiamine is a derivative of thiamine, both compound share similar structure. Sulbutiamine however has been modified as it contains disulfide dimer, ester and thiazole ring.
[msgbox]Chemical/IUPAC name: [4-[(4-Amino-2-methylpyrimidin-5-yl) methylformylamino]-3-[2-[(4-amino-2-methylpyrimidin-5-yl) methylformylamino]-5-(2-methylpropanoyloxy) pent-2-en-3-yl] disulfanylpent-3-enyl] 2-methylpropanoate
Chemical formula: C32H46N8O6S2
Chemical properties: White/off-white powder
Uses: Beri-beri treatment, asthenia treatment[/msgbox]
Mechanism of action
The specific modes of action of sulbutiamine are known to be related on choline, dopamine and glutamate receptor activities. Studies claim that sulbutiamine exhibits its functions through increasing cholinergic activities on the hippocampal area. Thus, short term and long term memory consolidation, memory and spatial awareness is improved.
It also demonstrates a dopaminergic activity through decreasing and suppressing prefrontal cortex dopamine release. Decreased dopamine levels are indicative of enhanced memory and overall cognition. Lastly, sulbutiamine is believed to potentiate prefrontal cortex glutamatergic activity, which leads to enhanced memory functions. These mechanisms are generally observed on nootropic supplements; hence, sulbutiamine is recognized by many individuals under this label.
Several clinical studies showed that sulbutiamine has numerous potential therapeutic effects. These include neuronal communication, mental alertness, increased attention span and concentration, asthenia treatment, erectile dysfunction treatment, fat burner and appetite suppressant.
Diabetic polyneuropathy treatment
In a randomized control study, the efficacy of sulbutiamine as a treatment of diabetic polyneuropathy was carried out. Hypothesis of sulbutiamine as a potential diabetic neuropathy treatment arose from its purported ability to influence synaptic transmission. A total of 30 diabetic patients were enrolled in the study. The participants were divided into two – the study and the control group. The study group received sulbutiamine while the control group was not given any treatment for 6 weeks.
After the study period, results showed that patients who consumed sulbutiamine demonstrated electrophysiological parameter improvement. Although there were no improvements on symptoms scores, this study indicated that sulbutiamine can potentially help in improving nerve functions on diabetic patients manifesting polyneuropathy .
Major depressive disorder is often characterized by psycho-behavioral inhibition which may lead to significant psychosocial impairment. Although there are supplemental drugs to treat depression, a French double blind, multicentric, randomized controlled trial was undertaken to assess the safety and efficiency of sulbutiamine in treating psycho-behavioral symptoms amongst patients diagnosed with Major Depressive Episode (MDE). Participants were randomly treated with sulbutiamine and clomipramine (control) for a period of 8 weeks.
The efficacy of sulbutiamine and placebo as a psycho-behavioral inhibitor was assessed using different scales (Norris Visual Analog Scale, Sheehan Disability Scales, and Depressive Psychomotor Retardation Scale). Results showed that sulbutiamine does not exert any anti-depressant activity. Nevertheless, it was revealed that it can accelerate psycho-behavioral inhibition assimilation whilst facilitate MDE patient rehabilitation which improves family, social and professional life functioning .
Adjuvant treatment for Alzheimer’s disease
Acetylcholinesterase inhibitors are one of the mainstay pharmacological therapeutic agents for Alzheimer’s disease (AD). However, some AD patients do not react to these treatments. As such, a double-blind randomized, multicentric research was carried out to evaluate if sulbutiamine, (a lipophilic drug which stimulates glutamatergic and cholinergic effects) in combination with an anticholinesterasic medication can help treat symptoms of cognitive decline on AD patients (attention, episodic memory, executive functions and working memory).
Participants was divided into two groups in which, one group was treated with donepezil and the other group with sulbutiamine for the first three months. The ones who previously took donezepil were given placebo while the group who were treated with sulbutiamine was given donepezil on the subsequent months (3). Results showed that the group who were treated with donepezil and placebo manifested decreased episodic memory and attention improvement. On the other hand, the participants who were given sulbutimaine and donepezil presented improved episodic memory, attention and activities of daily living. This study shows that sulbutiamine can be an effective adjunct treatment with acetylcholinesterase inhibitors on mild to moderate AD .
Illnesses and infectious diseases are often accompanied by asthenic manifestations (e.g. weakness, appetite loss, inability to concentrate). Previous studies showed B vitamin analogs particularly sulbutiamine can reduce asthenia. Researchers of this prospective, observational trial decided to measure the efficacy of sulbutiamine in treating asthenia when combined with explicit anti-infective therapy. A total of 1772 patients diagnosed with infectious illnesses and asthenic symptoms were enrolled in the study. Subjects were treated with ant-infective drugs and sulbutiamine for 15 days. Results showed that sulbutimine may be used as an adjuvant therapy on individuals diagnosed with infectious diseases and asthenic symtoms .
A randomized, double-blind study was undertaken to assess chronic fatigue after an infectious illness. Chronic post infectious fatigue (CPIF) is considered to be a therapeutic failure and a mystery. Hence, use of sulbutiamine in treating CPIF was measured. 326 individuals who manifest CPIF symptoms were randomly treated with different doses of sulbutiamine for 28 days. Unfortunately, there were no persistent effects amongst the data gathered. However, women taking 600 mg/day of sulbutiamine had less fatigue on the 7th day. Since the results of this study is lacking, further researchers is warranted .
Sulbutiamine is particularly effective in treatment of asthenia. Use of this particular drug however, should be done after a consultation or advice. Further human trials should be done to substantiate its other purported benefits.