Vinpocetine

Definition:
Vinpocetine (pronounced vin-poe-ce-teen) is a synthetic compound derived from vincamine, a substance found naturally in the leaves of the lesser periwinkle plant (Vinca minor). Vinpocetine was developed in the late 1960s.

Vinpocetine (brand names: Cavinton, Intelectol; chemical name: ethyl apovincaminate) is a semisynthetic derivative alkaloid of vincamine (sometimes described as “a synthetic ethyl ester of apovincamine”), 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.

Vinpocetine is widely marketed as a supplement for vasodilation and as a nootropic for the improvement of memory. There exists anecdotal report of uncomfortable adverse reactions to vinpocetine in a small subset of users. A low initial dosage is often recommended.

Vinpocetine is available as a prescription drug in Europe and Japan. In the the United States and Canada. It is sold in health food stores and online as a dietary supplement.

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Possible Nootropic Properties
A number of studies on healthy volunteers have demonstrated vinpocetine may elicit improvement on some aspects of memory. The degree which the nootropic effects of vinpocetine are mediated by mechanisms beyond vasodilation is currently unknown.

 

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.

Use Of Vinpocetine:
Vinpocetine widely used in the body building community as an antivasoconstrictor. However, no studies have been conducted on the effectiveness of vinpocetine on performance enhancement during exercise

Vinpocetine is naturally occurring from the plant Crioceras Longiflorus and also can be obtained from Vincamine.

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Vinpocetine derived from Tabersonine, an alkaloid extracted from seeds of the Voacana tree that is native to West Africa.

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Vinpocetine is a cerebral metabolic activator and a neuronal protector. Clinical studies indicate that vinpocetine helps increase blood flow; cerebral vasodilation produces an immediate increase in the cerebral oxygenation and this results finally in the activation of the cerebral metabolism, the increase of glucose and the improvement of certain neurotransmitters´utilization . Another benefit that has been observed by using vinpocetine is its neuronal protection effects which increase resistance of the brain to hypoxia and ischemia , reduce platelet aggregation, and improve red blood cells deformability allowing oxygen to feed neurons through microcapillaries . Evidence also shows that Vinpocetine has antioxidant properties.
The are more than 100 clinical studies on Vinpocetine performed on over 30,000 patients proving its safety and effectiveness. Vinpocetine has many different effects of varying importance on cognitive functions such as increase of attention, concentration, and memory .

Almost anyone can benefit from taking vinpocetine. From people who have already cognitive deterioration, through baby boomers who are starting to suffer the symptoms of memory loss to young people and students who want to enhance their memory to increase their intellectual intelligence as well as to get good results at exams.
Stroke and vascular dementia
Vinpocetine is thought to increase blood circulation in the brain, which may explain why some preliminary studies suggest that it may reduce brain impairment and dementia after an ischemic stroke. Although promising, well-designed human studies are needed.

Alzheimer’s disease
Vinpocetine is also being explored as a complementary treatment for people with Alzheimer’s disease. It’s thought to enhance the brain’s use of oxygen, protect brain cells against damage, and increase blood flow to the brain by inhibiting an enzyme called phosphodiesterase.

Although preliminary studies on the use of vinpocetine for Alzheimer’s disease showed promise, a critical review of previously published studies found that the evidence as a whole was too weak to rely on, due to limitations in the design of the studies. More research is needed.

Tinnitus
Studies suggest that vinpocetine may help with tinnitus after trauma to the ear.

To boost brain function
Vinpocetine is marketed in North America as a supplement that can boost memory and brain function in healthy people, but there is no real evidence yet that it can help.

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).


Side Effects and Safety Concerns

No adverse reactions to vinpocetine have been reported in human trials. Due to the small sample size of existing trials the prevalence of adverse reactions is still unknown although thought to be rare. Anecdotal evidence has suggested that a small subset of users may experience adverse reactions. Due to the possibility of adverse reactions, a low initial dose is typically recommended. The small size of existing studies precludes conclusion on the prevalence or severity of possible adverse reactions in vinopocetine usage.

The safety of vinpocetine in pregnant women has not been evaluated.

Vinpocetine has been implicated in one case to induce agranulocytosis, a condition in which granulocytyes – an important type of white blood cell, are markedly decreased. Some people have anecdotally noted that their continued use of vinpocetine reduces immune function. Commission E warned that vinpocetine reduced immune function and could cause apoptosis in the long term.

Side effects of vinpocetine may include indigestion, nausea, dizziness, anxiety, facial flushing, insomnia, headache, drowsiness and dry mouth. Vinpocetine may also cause a temporary drop in blood pressure.

Vinpocetine shouldn’t be taken by pregnant or nursing women. The safety of vinpocetine in people with liver or kidney damage isn’t known. People with bleeding disorders, low blood pressure or seizure disorders shouldn’t use vinpocetine. It also shouldn’t be used two weeks before or after a surgical or dental procedure.

There is one case report of agranulocytosis associated with the use of vinpocetine.

Possible Drug Interactions
Vinpocetine shouldn’t be taken by people who are taking drugs or herbs that “thin” the blood (anticlotting or antiplatelet medications), such as aspirin, Plavix (clopidogrel), Ticlid (ticlopidine), (Trental) pentoxifylline, vitamin E, garlic or ginkgo. It should not be used with Coumadin (warfarin).

Disclaimer:The information presented herein is intended for educational purposes only. Individual results may vary, and before using any supplements, it is always advisable to consult with your own health care provider.

Resources:
http://en.wikipedia.org/wiki/Vinpocetine
http://altmedicine.about.com/od/herbsupplementguide/a/vinpocetine.htm
http://www.vinpocetine.com/