Vinpocetine (brand names: Cavinton, Intelectol; chemical name: ethyl apovincaminate) is a semisynthetic derivative alkaloid of vincamine, an extract from the periwinkle (plant) Vinca minor.

Vinpocetine is reported to have cerebral blood-flow enhancing and neuroprotective effects, and is used as a drug in Eastern Europe for the treatment of cerebrovascular disorders and age-related memory impairment.

The substance is widely sold as a supplement and marketed as a "memory enhancer" for otherwise normal individuals. However, the evidence for such an effect is very small. There appears to be some controversy over the possibility of adverse reactions, and low initial dose is therefore recommended by some retailers.

Health and physiological applications of Vinpocetine

Possible Nootropic Properties

It has been claimed by some that Vinpocetine has applications in improving memory and possibly, other forms of cognitive function. Whether this has been confirmed scientifically and objectively is yet to be established.

Vinpocetine is included in many performance-enhancing supplements to enhance mental clarity and focus in periods of intense physical activity.

Applications to muscle performance

Vinpocetine is regarded by some as having some applications in improving muscle performance/efficiency, though no studies have been conducted to confirm such an effect.

Mechanism of Action

Vinpocetine has been shown to selectively inhibit voltage-sensitive Na+ channels, resulting in a dose-dependent decrease in evoked extracellular Ca+ ions in striatal nerve endings. The Na+ channel inhibiting properties of Vinpocetine are thought to contribute to a general neuroprotective effect through blockade of excitotoxicity and attenuation of neuronal damage induced by cerebral ischemia/reperfusion.

Vinpocetine is also a phosphodiesterase (PDE) type-1 inhibitor, (with an IC50 of approximately 10^-5 M.) leading to increases in intracellular levels of cyclic guanosine 3'5'-monophosphate (cGMP), an action that has been attributed to the vasorelaxant effects of Vinpocetine on cerebral smooth muscle tissue.

Increases in neuronal levels of DOPAC, a metabolic breakdown product of dopamine, have been shown to occur in striatal isolated nerve endings as a result of exposure to Vinpocetine. Such an effect is consistent with the biogenic pharmacology of reserpine, a structural relative of Vinpocetine, which depletes catecholamine levels and may cause depression as a side-effect of the cardiovascular and anti-psychotic effects.

Side-effects

Overall, Vinpocetine side-effects reported in the literature are rare, usually minor, frequently disappear with prolonged use, and rarely require discontinuance of the drug.

Stomach/ GI upset; dry mouth, rapid heart beat, low blood pressure, and rash/ hives are the main (rarely-occurring) reported side-effects. There have been no real adverse effects to this drug during human trials.

Vinpocetine is not recommended for pregnant women (at doses higher than 2-5 mg).

Care should be taken when it is taken with other nootropics. It is always recommended that a physician be consulted before use.

Vinpocetine has been reported in one case to induce agranulocytosis, a condition in which granulocytyes - an important type of white blood cell, are markedly decreased.

Many supplement store preparations are definitely not pharmaceutical level of quality control, particularly relative to amount in the preparation. Where possible, pay more for the pharmaceutical preparations.

Dosage

It is recommended that first-time users ingest only 2-5 mg of Vinpocetine to make sure they are not hypersensitive to it. Users may then increase the dosage to 10-30 mg a day (which may, although very rarely, cause some side-effects).

[ Source: Wikipedia; This portion licensed under the GNU Free Documentation License ]