Life Extension Magazine®

Issue: Jun 1998

Life Extension Foundation

The Life Extension Foundation searches the world for therapies that may slow human aging. Here is an update on two intriguing brain-enhancing compounds, pyritinol and Picamilon.

Scientifically reviewed by: Dr. Gary Gonzalez, MD, on January 2021.

The Life Extension Foundation searches the world for
therapies that may slow human aging. Here's an
update on two intriguing brain-enhancing compounds.

In last month's Life Extension magazine, we presented an extensive review of cognitive-enhancing nutrients that are freely available in the United States. We pointed out that many of the brain-boosting supplements Americans buy over the counter are sold as prescription drugs in Europe.

Many readers and Life Extension Foundation members called, asking our opinion about European drugs that are not sold in the United States. In reviewing the published scientific literature, we continue to be impressed with two relatively new drugs that improve cerebral blood flow and boost brain cell energy metabolism.

Life Extension has reported on both pyritinol and Picamilon in the past, and present here additional rationales for using one or both of these promising therapies.

What's interesting about these European "drugs" is that they are analogues of popular vitamin supplements. If you're seeking to prevent or treat neurological impairment, you may wish to consider these exceedingly safe medications. (In addition, a company that offers European therapies to American citizens for personal use has significantly reduced its prices, thus making advanced medications more affordable.)

The drug pyritinol is used in Europe for the treatment of several forms of neurologic impairment. Based upon published research, this therapy shows benefits in the treatment of early stage Alzheimer's disease, stroke, vertigo, head trauma and age-associated mental impairment.

The evidence shows that pyritinol enhances neuronal metabolic function. It works by increasing brain-cell energy levels so that youthful, cognitive function can be at least partially restored. There is a large volume of human clinical data supporting the safety and efficacy of this European therapy.

The pyritinol molecule is structurally similar to vitamin B6, but functions in the brain in a different way. The dose of pyritinol used in most of the human clinical studies is one 200-mg capsule taken three times a day.

(In referring to the studies described below, a "double-blind" trial is one in which neither the subjects nor the persons administering the treatment know which treatment a subject is receiving. When a trial is "randomized," it means that subjects are assigned to treatment groups in a known probability distribution, to help produce more accurate results.)

The journal Alzheimer's Research (2/3 1996) reported on a double-blind study conducted in the United States in which pyritinol was compared to Hydergine and placebo (a dummy treatment) in treating 100 patients with Alzheimer's disease. Two measures of cognitive function were used to assess treatment effects.

After 12 weeks of treatment, "the results indicated that treatment with pyritinol was associated with a significant and continuous improvement in cognitive functioning over the course of the study, while treatment with Hydergine was associated with a more modest improvement that tended to plateau early in the treatment phase."

In the journal Neuropsychobiology (26(1-2) 1992), a 12-week, double-blind clinical trial was performed to investigate the benefit of pyritinol in the treatment of several forms of senile dementia. A total of 156 patients were allocated to either of two groups: the "senile dementia of the Alzheimer's type" group, or the "multi- infarct dementia (stroke)" group.

In a 12-week, double-blind treatment, the researchers used three well-established tests to evaluate cognitive function. In addition, EEG brain mapping was employed to measure brain-cell function.

The doctors stated, "The therapeutic efficacy of pyritinol was clearly demonstrated by confirmatory analysis as the drug was statistically significantly superior to placebo in all three target variables. The EEG mapping demonstrated significant differences between placebo and pyritinol.

Based on the results of this trial, it can be accepted that the therapeutic effect of pyritinol is superior to placebo in patients with mild to moderate dementia of both degenerative (Alzheimer's) and vascular (stroke) etiology."

As reported in a study in the British journal International Clinical Psychopharmacology (January, 1989), 26 patients with Alzheimer's disease were randomly assigned in a double- blind trial of pyritinol versus placebo. The patients had a mild to moderate degree of dementia.

The results of the study showed that "pyritinol was associated with a significant improvement in cognitive performance. Regional cerebral blood-flow data showed that treatment with pyritinol normalized the pattern of blood flow increase during activation and improved the score on the test used for activation."

In the German journal Pharmacopsychiatry (September 1986), the effects of pyritinol were investigated in a placebo-controlled, randomized, double-blind study in geriatric patients suffering from cerebral functional disorders, with a moderate to severe degree of chronic brain syndrome. In a previous study, a rise in the vigilance (wakefulness, alertness) level was demonstrated in patients undergoing pyritinol treatment. Data from 107 patients were included in the statistical analysis, 54 on pyritinol and 53 on placebo. No notable adverse drug reactions were observed.

The doctors reported, "Statistically significant results were found in favor of pyritinol, compared with placebo, in both the level of clinical symptomatology and the performance level. Particularly impressive was the superiority of pyritinol in the factor 'social behavior.'"

In the journal Neuropsychobiology (24(3) 1990), 12 healthy male volunteers received pyritinol in doses of 600 or 1,200 mg per day, or placebo for three days according to a randomized, double-blind design. On the first and third days of each of the three treatment periods, subjects completed a battery of psychological tests. The doctors reported, "Significant improvements in the Critical Flicker Fusion test and the Choice Reaction Time test were found after pyritinol."

In a study conducted at the Max-Planck-Institute of Neurology and published in Annals of the New York Academy of Sciences (640, 1991), pyritinol was tested along with piracetam and phosphatidylserine in Alzheimer's patients. Positron emission tomography (PET) was used to measure the brain's energy metabolism, which is closely coupled to brain function.

The doctors noted that glucose metabolism decreases slightly with age, but Alzheimer's disease shows severe deficits in glucose metabolism. In the assessment of the effects of pyritinol on disturbed glucose metabolism, the doctors stated, "PET studies showed general increases in glucose utilization with piracetam, pyritinol and phosphatidylserine. The therapeutic relevance of such metabolic effects, however, must be proved in controlled clinical trials."

In the Journal of International Medical Research (9/3, 1981) 270 patients suffering from different forms of brain injury were treated with pyritinol for six weeks. It was shown that, "compared with placebo therapy, pyritinol produces statistically significant improvement in clinical and psycho neurological manifestations. It is concluded that pyritinol is a drug of therapeutic benefit in the treatment of the [results] of cerebral trauma."

In Pharmatherapeutica (England, 2/5, 1980) a double-blind, placebo- controlled trial was carried out on 40 patients suffering from moderately advanced dementia. The patients were allocated randomly either to pyritinol or placebo for three months. Assessments of cognitive function were made pre-treatment and monthly up to three months, and then at follow-up at six months. The doctors concluded, "Patients on pyritinol showed significantly higher levels of improvement than did those on placebo. Laboratory tests conducted throughout remained within normal limits for both groups."

In the German journal Med. Klin. (73/31 1978), 161 patients with chronic organic brain syndrome (average age 64 years) were treated with various oral doses of pyritinol for different periods of time. The doctors stated, "Statistical analysis of the data showed that the success rate of treatment increases significantly with increasing dose and duration of the treatment."

In the French journal Ouest Medicine (29/1 1976), pyritinol was tested on people who suffered from vertigo. The doctors described a complicated mechanism by which pyritinol was effective against vertigo, and reported the following:

"In a clinical experience with 60 cases of vertigo, the author obtained a cure rate of 83.33 percent, accompanied by an improvement in the patients' mental and social state. The drug was tolerated well by patients of all ages."

The Czech journal Cs. Pediat. (29/10 1974) reported that pyritinol was tested on 41 children (28 boys and 13 girls) with various diseases of the central nervous system. The doctors reported, "In severe contusions of the skull with apallic syndrome (a total of nine children), improvement was recorded in the majority, and marked improvement in one-third.

In meningo-encephalitis (eight children), treatment was successful in half the patients; in infantile cerebral palsy and malformations on the brain (19 children), treatment was successful in about one-third of cases. In minor disorders of the brain (five children), the effect was smallest. According to these results, pyritinol treatment offers a certain contribution to treatment used in pediatric neurological practice."

Those with any of the neurological impairments that pyritinol has been documented to alleviate should consider taking 200 mg three times a day of this European medication under the care of a physician, preferably a neurologist. It appears that pyritinol can produce both an immediate and a cumulative beneficial effect on neurologic function.

Those seeking to preserve and enhance cognitive function may consider trying two 200-mg capsules of pyritinol early in the day in place of drugs such as Hydergine. It is suggested that pyritinol be taken early in the day because its cerebral-energizing benefits can interfere with sleep if taken too close to bedtime.

A number of offshore suppliers ship medications to American citizens under the Food and Drug Administration's personal use guidelines. The Life Extension Foundation recommends only companies whose products meet pharmaceutical standards, and who guarantee delivery of products. Many companies in Europe ship at the customers' risk.

Nootropic Vitamin-like Drug

image Picamilon, introduced in Russia in 1989, appears to be more effective than Hydergine or vinpocetine in improving blood flow to the cerebral vessels in the brain. Picamilon readily crosses the blood-brain barrier to protect neurons against the effects of diminished oxygen flow. It also enhances cognitive function. For these reasons, Picamilon is called a "nootropic" treatment, meaning it has a positive impact on the brain and cognition.

Aging causes a reduction in cerebral vascular circulation that precipitates the degeneration of brain cell structure and function. Cognitive decline, depression and various neuropsychic diseases result from the progressive effects of diminished cerebral circulation. Picamilon enhances cerebral vascular perfusion-that is, the ability of blood to flow through vessels-and alleviates neurologic impairment caused by trauma, alcoholism, stroke and aging.

While Picamilon is approved as a pharmaceutical in Russia, it's really a vitamin-like compound consisting of a niacin analogue (n-nicotinoyl) uniquely bonded to GABA (gamma aminobutyric acid). When niacin is bound to GABA, it readily penetrates the blood-brain barrier and enhances cerebral and peripheral circulation. What enables Picamilon to work so well is the synergism between the niacin and GABA.

Refer to the Abstracts section of this issue for additional information about the published scientific research on Picamilon.