Sulbutiamine: What is Sulbutiamine?
Sulbutiamine: What is Sulbutiamine?
Sulbutiamine is also known as Bisbuthiamine, Arcalion, Youvitan, and Enerion (Examine, 2015). It is known as isobutyryl thiamine disulfide. A sulfur group creates an ester of two vitamin B1 (Thiamine) together to create the synthetic molecule. The drug is a lipophilic compound with the ability to dissolve in cross cell membranes or fatty tissue (Trialx, 2015). It is designed to act in the brain, but is not thought to have psychostimulant properties (Trovero, 2000). Essentially a nootropic vitamin, Thiamine is mimicked by sulbutiamine to a certain extent. Sulbutiamine is stronger and can either be used with other nootropics or alone.
Sulbutiamine is the drug recommended for asthenia, and psychic and somatic inhibition (Examine.com, 2015). Asthenia is defined by mental fatigue and there are several types: postpartum asthenia with symptomatic polymorphisms, viral and bacterial postinfection, emotional lability, intellectual asthenia, and psychological stress (Trialx.com, 2015). Sulbutiamine is obtained over the counter so exercise enthusiasts, and athletes use it to combat fatigue without a prescription (Medicalook.com, 2015). Some people experience a mild stimulatory effect without the common side effects of amphetamine. This is probably because sulbutiamine only affects dopamine and not other catecholamines. In addition, it has been reported to improve problems with memory. This is probably due to glutamate and acetylcholine activity. Some patients with Parkinson’s disease and schizophrenia that experience intellectual asthenia finds relief through use of Sulbutiamine. Cognitive effects have been demonstrated in several research projects, and some patients experience mood elevation for a short period of time.
Method of Action
Sulbutiamine acts faster than Thiamin moving from blood circulation to the brain; the lipophilicity is the responsible factor. An essential vitamin within the body, Thiamine is used for GABA and acetylcholine biosynthesis. Its absorption in the intestines is poor secondary to folic deficiency. Higher concentrations inhibit absorption further. Sulbutiamine administration results in nootropic benefits due to its effectiveness on the dopamine, glutamatergic, and cholinergic systems. In addition to higher absorption rates than Thiamine, it acts to increase the efficiency of the blood-brain barrier.
Sulbutiamine Dosage and Suggested Usage
Dosages for Sulbutiamine is suggested at 400-1000 mg. Some brands suggest 12.5 mg per kilogram of body weight. The overall recommended Sulbutiamine dosage is usually 600 mg per day, taken in three 200 mg doses, one in the morning and one in the afternoon and another in the evening. As a non-prescription drug, individuals have the option of reading the label on the bottle or consulting a physician. Dosages for elderly patients should be approximately half the normal dose for an active adult. It is sold in tablet capsule and powder form, generally in doses 200 mg each.
Sulbutiamine Side Effects
People using sulbutiamine may experience side effects such as mild agitation or an allergic skin rash (Trialx, 2015). This is generally a result of taking an abnormally high dose. There have been some reports of depression, nausea, and headaches. It is recommended to discontinue use if experiencing side effects.
Sulbutiamine has demonstrated the ability to build tolerance quickly. Nootropic benefits decrease to a certain extent, but the effects of energizing and mood elevation are more quickly affected. Therefore, sulbutiamine should be taken as needed rather than as a continuous supplement. As a non-psychoactive compound, there is small risk of addiction to the drug.
Additional Information on Sulbutiamine
Sulbutiamine is a synthetic derivative of thiamine, or Vitamin B1, first synthesized in Japan to aid in treating Beriberi and Asthenia. Although the exact date of initial synthesization is unknown, the first reports containing Sulbutiamine were recorded in 1973. Sulbutiamine was created to help increase the lipophilicity of Thiamine allowing an increase in Thiamine and Thiamine Esters in the brain causing a more effective treatment versus other analogues of Vitamin B1.
Sulbutiamine is a fat-soluble nootropic, that passes the Blood-Brain Barrier more readily than Thiamine. Sulbutiamine is known to be cholinergic, glutamatergic and dopaminergic. The potentiation of glutamatergic activity in the Prefrontal Cortex is believed to be one of the Mechanisms of Action that grants Sulbutiamine the ability to increase memory functionality. Sulbutiamine is shown to cause an increase in cholinergic activities in the Hippocampus, this area of the brain plays a pivotal role in the consolidation of both short and long-term memory as well as spatial navigation and memory. Another plausible cause of Sulbutiamine improving cognition and memory is through the suppression and reduction of dopamine released in the Prefrontal Cortex. These various Mechanisms of Action make Sulbutiamine an understandable choice in improving cognitive and memory abilities.
Sulbutiamine has various benefits beyond cognition and memory improvement. In one study, Sulbutiamine was shown to help treat erectile dysfunction in 16 participants out of 20 over a 30-day period, including those with arterial disorders. At the conclusion of the study, Sulbutiamine was found to be an effective treatment for erectile dysfunction. Clinical efficacy of the drug Enerion in the treatment of patients with psychogenic (functional) erectile dysfunction (Urologiia. 2005 Jan-Feb).
It has also been shown to aid in treating various psycho-behavioral inhibitions such as shyness and depression, which when coupled with other Nootropics (such as Aniracetam) could prove beneficial in aiding those suffering from social anxiety and depression. Although Sulbutiamine is not an antidepressant, it was concluded to be useful in the rehabilitation for those suffering with depression in their Social, Family and professional lives. Effects of sulbutiamine (Arcalion 200) on psycho-behavioral inhibition in major depressive episodes (Encephale. 2000 Mar-Apr).
In one double-blind trial, Sulbutiamine was found to be a plausible treatment in early Alzheimer’s Disease through potentiation of both the glutamatergic and cholinergic transmissions of the Prefrontal Cortex and Hippocampus versus donepezil, and a placebo over a 3 month study period. Effects of the association of sulbutiamine with an acetylcholinesterase inhibitor in early stage and moderate Alzheimer disease (Encephale. 2007 Mar-Apr).
The overall suggested Sulbutiamine dosage is usually 600 mg per day, taken in three 200 mg doses, one in the morning and one in the afternoon and another in the evening. It is sold in tablet capsule and powder form, generally in doses 200 mg each.
Does Sulbutiamine Work?
Sulbutiamine is an analogue of Vitamin B1 (Thiamine), that passes the blood-brain barrier more readily as well as improves the functionality of several transmissions within the brain. Sulbutiamine is recognized widely as one of the only plausible treatments for Asthenia, a simple over the counter treatment for erectile dysfunction, a treatment for psycho-behavioral inhibitions, and as a cognitive and memory enhancing Nootropic by increasing the availability of Thiamine Triphosphate.
There are still many variables though that have to be looked at with improving cognitive abilities. As a result, it is very hard to determine just how effective Sulbutiamine would be for a specific person. It all comes down to their own needs and current cognitive ability as well as lifestyle choices.