Sulbutiamine (Arcalion, Enerion)

What Is Sulbutiamine?

Sulbutiamine is a synthetically produced derivative of thiamine (vitamin B1). Since it is a dimer of two modified molecules of thiamine, it has lipophilic properties, which allows more easily penetrate into the brain through the blood-brain barrier and increase the levels of thiamine phosphate esters and thiamine in the brain. Sulbutiamine was discovered in Japan during attempts to develop a more potent formula of vitamin B1 on account of increased lipophilicity.

Although clinical effectiveness of Sulbutiamine remains uncertain, it is the only compound used for the treatment of asthenia known to target certain areas of the brain responsible for this health condition. Not only can it treat chronic fatigue, but it can also be used or improving memory and managing erectile dysfunction (ED). When used in therapeutic doses, the drug rarely causes severe side effects, although it may affect the course of bipolar affective disorder. It is available for sale over-the-counter because it is classified as a nutritional supplement.

Sulbutiamine is sometimes added to sports nutrition in order to increase athletic performance. The drug has a real sports potential, and its use is reasonable.

History

The history of the creation of Sulbutiamine is closely related to the study of thiamine conducted in Japan. A deficit of thiamine in a nervous system causes beriberi. Until the twentieth century, this disorder was widespread in Japan and a range of other Asian countries due to the use of white rice as a staple food. The relationship between diet and beriberi was first noted by Takaki Kanehiro, a military surgeon. Additional studies led to the discovery of thiamine. In 1926 it was isolated, and in 1936 it was synthesized for the first time. The foundation of the Vitamin B Research Committee in Japan led to other studies of the properties of thiamine and its derivatives.

Allithiamine was the first derivative of lipophilic isolated from garlic in 1951. After allithiamine had been discovered, several additional derivatives were synthesized with the hope that they would have better pharmacological properties than thiamine. Due to a positively charged thiazole moiety, thiamine cannot diffuse across plasma membranes. That is why it has to be transported by high-affinity carriers, which results in the low rate of transport. Sulbutiamine comes with high oral bioavailability thanks to its ability to easily dissolve in fats. It is unknown when exactly Sulbutiamine was synthesized, but the earliest references date back to 1973.

Mechanism of Action

The molecules of Sulbutiamine are dissolvable in fat, so the drug penetrates into the brain much more easily than thiamine. During its metabolism in the brain, the levels of thiamine and thiamine phosphate ester increase. Sulbutiamine inhibits cholinesterase and influences certain parts of the brain, in particular, the reticular formation, increasing its activity, which leads to increased mental activity, increased motivation, and elimination of a feeling of fatigue. Scientists also found potential cholinergic activity in the hippocampus. Glutamatergic activity of Sulbutiamine allows accelerating the process of transmission of nervous impulse in the prefrontal area of ​​the brain, which leads to improvement of mental activity and memory. Moreover, there was found an additional mechanism improving memory and brain activity — activation of dopamine receptors.

Effects of Sulbutiamine (Arkalion, Enerion)

The complex mechanism of action of Sulbutiamine causes multiple effects of the drug:

  • Improving memory;

  • Stimulation;

  • Reducing fatigue;

  • Stimulating the processes of thinking;

  • Improvement of potency.

Therapeutic Uses

For Asthenia

Sulbutiamine is used for the treatment of asthenia. Asthenia is a condition of chronic fatigue or weakness, which has cerebral origin rather than neuromuscular.

Several studies have shown that Sulbutiamine effectively relieves the symptoms of asthenia. In a study of 1,772 patients with infectious diseases and asthenic symptoms, Sulbutiamine was used along with the anti-infective drugs for 15 days. 916 patients were diagnosed to fully red rid of all asthenic symptoms. Another study showed that Sulbutiamine was effective in relieving symptoms in patients with mild to moderate craniocerebral trauma. Nevertheless, the clinical effectiveness of Sulbutiamine has not yet been fully proven. In a study of patients with chronic fatigue after infectious diseases, Sulbutiamine showed no convincing effects compared with placebo, which caused doubts about the clinical effectiveness of Sulbutiamine. However, the authors of this study suggest that more research is needed to evaluate the potential effectiveness of Sulbutiamine in the treatment of chronic weakness.

For Memory

Several studies have shown that Sulbutiamine improves memory by enhancing dopaminergic, cholinergic, and glutamatergic transmissions. Mice with the injected Sulbutiamine show better results in tests using operant conditioning and pattern recognition.

Sulbutiamine is also effective in reducing the amnesic effects of dizocilpine and improving memory in people with schizophrenia. Recently, Sulbutiamine has shown effectiveness in improving daily activity in patients suffering from early and middle stages of Alzheimer's disease if Sulbutiamine is combined with an acetylcholinesterase inhibitor. In a randomized, double-blind study of patients with Alzheimer's disease, the combination of Sulbutiamine and donepezil improved performance of daily activities and episodic memory better than the combination of placebo and donepezil.

For Erectile Dysfunction

According to a recent study, Sulbutiamine is effective in treating ED. Twenty patients suffering from psychogenic ED used it within thirty days. After the treatment had finished, erectile function was improved in 16 men.

Availability

Sulbutiamine is available in several forms. Enerion is supplied in the form of tablets with 200 mg of Sulbutiamine. Generic Sulbutiamine is available in powder, tablets, and capsules.

Doses and Administration

A noticeable effect of Sulbutiamine occurs with a dose of 800-1,000 mg per day. There are cases of taking the drug in dosages of 2,000 mg per day without any side effects.

A reasonable therapeutic dose is 12.5 mg of Sulbutiamine per 1 kg of patient weight, which corresponds to 850 mg for a patient weighing 68 kg. However, you should note that the recommended doses vary depending on a manufacturer. For instance, the manufacturer of Arcalion recommends taking Sulbutiamine in a daily dosage of no more than 600 mg.

Side Effects

Sulbutiamine rarely causes undesirable side effects if used in therapeutic doses. According to the statement of the drug’s manufacturer, a slight skin allergy may occur. A small behavioral arousal was also noted in elderly patients.

There is only one report showing complications occurred due to a chronic overdose of Sulbutiamine. A patient suffering from bipolar disorder took Sulbutiamine, as he complained about weakness. He decided that the medicine was helpful and increased the daily dose up to 2 g, which was much higher than the prescribed dosage. Later, he stopped using other medications prescribed to him, since he insisted that the Sulbutiamine was the only substance that helped him.

The authors of the report concluded that Sulbutiamine might influence the course of bipolar disorder. The effects of a chronic overdose of Sulbutiamine are similar to those occurred due to an overdose of Vitamins B. For example, there is only one published report on a patient experiencing undesirable side effects from a chronic overdose of pyridoxine (vitamin B6). This patient suffered from developed acute sensory and average motor neuropathy due to prolonged, excessive abuse of the medication.