What is Vinpocetine?
Vinpocetine is a semisynthetic derivative alkaloid of vincamine that was first developed in the 1960s. Whereas vincamine is directly extracted from the periwinkle plant (Vinca minor), vinpocetine is a man-made compound that is designed to resemble it. The chemical name of vinpocetine is ethyl apovincaminate, but it is sold under several brand names, including Cavinton, Cogvin, and Intelectol. It has been used in Europe for many years to treat cerebrovascular diseases (including stroke) and is available by prescription in Germany. In recent years, it has been marketed as a memory booster with minimal side effects.
How does it work?
The primary mechanism of vinpocetine is its inhibition of phosphodiesterase (PDE) type-1. Inhibiting activity of this enzyme leads to blood vessel dilation, which occurs when the smooth muscle cells that line arteries ‘relax’, opening the vessel lumen and increasing blood flow and circulation. This has several downstream effects, including enhanced oxygen and glucose delivery to the brain. It is also believe to increase production of adenosine triphosphate (ATP), which is the primary cellular energy molecule.
It has also been demonstrated to modulate the activity of neuronal ion channels, specifically those that allow sodium (Na+) and calcium (Ca2+) into cells.
Vinpocetine also seems to have anti-inflammatory effects. It prevents increased expression of inflammatory cytokines and NF-κB in cell culture models.
This compound has been demonstrated to increase neuronal plasticity; it improves spatial memory in animal models and enhances cognitive test performance in humans. Anecdotal reports from users suggest that it improves concentration, focus, and possibly vision (due to increased blood flow). Others feel that is normalizes cognition in people with low-thyroid function. Clinical evidence supports the concept that vinpocetine improves attention, concentration, and memory, however, many of the studies that have been published do not have appropriate control groups taking placebo.
In pathological conditions, vinpocetine seems to protect neurons from glutamate toxicity, likely through its effect on neuronal ion channels. This property has made it an attractive candidate to treat epilepsy. It also appears to attenuate damaging neuroinflammation that occurs after transient ischemia or stroke. While some studies suggest that may be useful for people in the early stages of Alzheimer’s disease, others found that it was not effective in preventing cognitive decline. Vinpocetine has also been used to treat symptoms of menopause and chronic fatigue syndrome, but evidence for its efficacy in these conditions is lacking.
More recently, scientists have begin to study the utility of this compound on other neurological conditions. Vinpocetine decreases hyperactivity in a rodent model of fetal alcohol syndrome.
Vinpocetine Side Effects
Reported side effects include lightheadedness, dizziness, sleep disturbances, headache, and upset stomach. Some people have noted weaker immune systems, after using vinpocetine for a long period of time. Others have reported these symptoms when they stopped using the compound.
Vinpocetine is usually sold in 5-10 mg capsules, and the usual dosage is 5-60 mg per day. Many studies employ doses of 10-30 mg. People just beginning a vinpocetine regimen should consider starting with a lower dose in order to avoid some of the side effects associated with higher doses (see above).
Approximately 0.7% of the total dose actually reaches the brain. Maximal effects are seen approximately 60-90 minutes after ingestion. However, vinpocetine has a relatively short half-life. Levels of its main metabolite decreased by 50% only 3.6 hours after intravenous administration in healthy volunteers. For this reason, divided dosing is recommended (2-3 doses per day, not to be taken before bed time).
Because of its effect on blood flow, individuals taking blood thinners or anti-platelet drugs or who have a clotting disorder should check with their doctor or pharmacist before taking vinpocetine.
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