Pyritinol

Pyritinol (pyridoxine disulphide) is a semi-synthetic derivative of vitamin B6 (pyridoxine), obtained by merging two molecules of pyridoxine with disulfide “bridge”, developed as an attempt to create a form of the aforementioned vitamin with enhanced bioavailability to the central nervous system and thus maximized nootropic properties. It was first synthesized in 1961 at the labs of pharmacological company Merck KGaA.

Since the ’70s, it has been a prescription and OTC drug in several countries (trade names include, inter alia,  Encephabol, Encefabol, Cerbon 6), approved for cognitive impairment in dementia syndromes, supportive treatment of after-effects of cerebral trauma, and learning disorders. Additionally, in France, it is indicated for rheumatoid arthritis as a disease modifying drug, based on the results of clinical trials.

Pyritinol promotes the metabolism of neurons, i.e., by increasing the uptake and utilization of glucose in the brain, thereby potentially improving the availability of energy and overall cognitive performance. It also facilitates signal transduction within the nerve cells. Vitamin B6 is a critical factor in the dopamine synthesis pathway, helping convert ingested amino acids into this neurotransmitters, and pyritinol fulfills the same function, being particularly efficient in that respect. By boosting dopamine levels amount to optimal level of mental and physical energy, motivation, ability to focus as well as adequate working memory, and abstract reasoning. In addition to that, pyritinol modulates dopamine release, potentially improving motor coordination, cognitive flexibility and capacity to multitask.

It has also been proven to facilitate the regeneration of neurons that produce acetylcholine. In animal studies, it has been found to induce choline acetyltransferase activity, leading to acetylcholine accumulation in cholinergic neurons. Furthermore, it increases the blood-brain barrier permeability to glucose, inhibits excessive production of lactic acid, thereby raising the resistance of brain tissue to hypoxia. In addition to that, pyritinol restored normal concentrations of the excitatory neurotransmitter NMDA in elderly mice, reversing its age-related decline.

Just like its parent compound, pyritinol might have a prominent impact on mood, since it stimulates the production of serotonin and GABA, and therefore contributes to positive emotional baseline and low anxiety, maintaining balance between stimulation and inhibition, crucial for equlibrium, equanimity, and stress resistance, which in turn ensure the stability of concentration.

Pyritnol has also been found to exert anti-oxidant action and provide substantial anti-inflammatory effects.  It is believed to regulate the immune response, and anti-inflammatory response in particular. Thus, it might prevent the development of chronic inflammation, implicated in neurodegenerative disorder and cancer. It could potentially play a protective role against auto-immune disorders.

Studies in patients with traumatic brain injury have shown that pyritinol “is a drug of therapeutic benefit in the treatment of the sequelae of cerebral trauma“. In a recent study, it has been demonstrated that joint effects of vinpocetine and pyritinol improve blood and plasma viscosity in patients with cerebrovascular disorders.

Certain pro-cognitive effects of pyritinol have also been studied in healthy volunteers, and its supplementation turned out to improve the scores of psychometric tests whose results may be interpreted as a measure of vigilance, perception resolution, and response time. These findings are consistent with the general improvement of psychomotor performance found in both healthy subjects and clinical populations.

Given that subclinical vitamin B6 deficiency has been linked to depression, ADHD, and ASD, individuals with these conditions might benefit from using pyritinol as an adjunct to their treatment regimen.

Some research suggests that vitamin B6 helps reduce histamine levels, so pyritinol might alleviate the symptoms of histamine intolerance.

As an aside, according to anecdotal reports, pyritinol seems to reduce the severity of alcohol-induced hangover. Currently, there is only one experimental study in humans that supports these claims. It is theorized that this could be due to prostaglandin inhibition, however, more studies on the subject are needed in order to explain the underlying mechanism.

 

Benefits of taking pyritinol

• boost in motivation;
• improved concentration and focus;
• higher energy levels;
• enhanced mood;
• increased vigilance;
• lower anxiety;
• enhanced memory;
• improved reflexes and motor coordination;
• enhanced sensory acuity;
• neuroprotection;
• improved neuroregeneration;
• might ameliorate the symptoms of alcohol-induced hangover;
• potential aid in body detox;
• healthy metabolism;
• anti-inflammatory and anti-oxidant action;
• might help with neuropathic pain;
• possible aid in histamine intolerance.

Side effects

Note: unlike its parent compound, no accumulation of pyritinol was observed, toxic concentrations were not reached even in patients with renal impairment.

The vast majority of below adverse effects tend to resolve within the initial few weeks of supplementation.

• nausea;
• heartburn;
• vomiting;
• diarrhea;
• irritability;
• restlessness;
• insomnia;
• allergic reactions (rare): skin rash.

Interactions and contraindications

• penicillamine;
• levamizole;
• Aurum salts;
• might potentiate the action of CNS stimulants (caution is advised);
• in case of kidney or renal function impairment it is advised to consult a healthcare professional.

Dosage

While the minimum daily dose of pyritinol is 300 mg, well-documented nootropic effects were observed at 600 – 1200 mg.

It is typically taken twice or thrice a day, and while it is water soluble and best absorbed when taken without food, it is not uncommon to take it with meals in order to reduce gastrointestinal discomfort.