Vinpocetine is derived from the periwinkle plant and is a substance that has been shown to boost brain blood circulation, improve memory and increase brain metabolism. It was first made widely available in 1978 and since then has been consistently used in Japan, Europe and Russia for the prevention and treatment of cerebrovascular diseases (including stroke). There it has also been used to treat depression, memory loss and headaches. For these reasons Vinpocetine has been used in a number of study pills. A number of clinical studies have confirmed that Vinpocetine has neuroprotective effects, antioxidant and vasodilating effects ( [Dezsi et al., 2002], [Pereira et al., 2003]and [Santos et al., 2000]).

 

How Vinpocetine is Absorbed in The Body

One of the primary questions researchers tried to answer about Vinpocetine is how it is absorbed in the body. They learned that Vinpocetine typically reaches the bloodstream about an hour after ingestion. The majority of Vinpocetine leaves the body within eight hours. Recent clinical research has demonstrated that Vinpocetine crosses the blood-brain barrier and is absorbed by cerebral tissue. A number of PET studies (Positron emission tomography – A technique that produces 3D images of the body) have shown that a considerable amount is absorbed by the brain compared to the brains overall weight distribution in the body. Vinpocetine was especially absorbed in the thalamus, putamen, and neocortical areas of the brain.

How Vinpocetine Works

Vinpocetine works by inhibiting the enzyme phosphodiesterase (PDE) type1. PDE1 typically causes contraction and narrowing of blood vessels in the brain. By inhibiting PDE vinpocetine dilates brain blood vessels and increases blood flow. The act of inhibiting PDE1 also allows vinpocetine to reduce the stickiness of red blood cells allowing blood to flow easier.

In addition to increasing brain blood flow, Vinpocetine also has been shown to increase brain energy metabolism by increasing the rate of ATP production, speeding up glucose use in the brain, speeding up the use of oxygen in the brain and increasing levels of critical neurotransmitters. Specifically, Vinpocetine increases levels of these key neurotransmitters involved in memory function:

Norepinephrine – A hormone and neurotransmitter involved in alertness and focus.
Acetylcholine – Plays an important role in memory.
Serotonine – Low levels can cause depression and sleep disorders.

Vinpocetine and Memory

In a randomized, double-blind study 12 healthy females were given either vinpocetine or a placebo for 2 days and tested on their memory(Subhan). They showed significant improvements in short term memory. There have also been a number of studies that showed memory improvement in the elderly.

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Selected Clinical Studies

Possible Memory-Enhancing Properties of Vinpocetine
Donna M. Coleston and Ian Hindrnarch

Human Psychopharmacology Research Unit, Department of Psychology, University of Leeds, Leeds, England. Critical flicker fusion threshold, choice reaction time, total reaction time, and Sternbergtype memory tasks of digits/words were measured in twelve volunteers after having received vinpocetine or placebo for two days. A significant improvement was recorded in the short-term memory test following 40 mg of the drug when compared to placebo.

A double-blind placebo controlled evaluation of the safety and efficacy of vinpocetine in the treatment of patients with chronic vascular senile cerebral dysfunction.

Balestreri R, Fontana L, Astengo F.
J Am Geriatr Soc. 1987

In a double-blind clinical trial, vinpocetine, a synthetic ethyl ester of apovincamine, was shown to effect significant improvement in elderly patients with chronic cerebral dysfunction. Forty-two patients received 10 mg vinpocetine three times a day (tid) for 30 days, then 5 mg tid for 60 days. Matching placebo tablets were given to another 42 patients for the 90 day trial period. Patients on vinpocetine scored consistently better in all evaluations of the effectiveness of treatment including measurements on the Clinical Global Impression (CGI) scale, the Sandoz Clinical Assessment-Geriatric (SCAG) scale, and the Mini-Mental Status Questionnaire (MMSQ). There were no serious side effects related to the treatment drug.

Vinpocetine effects on cognitive impairments produced by flunitrazepam.

Bhatti JZ, Hindmarch I
Human Psychopharmacology Research Unit, University of Leeds, U.K.

The effects of pre-treatment with vinpocetine 40 mg, on flunitrazepam-induced impairment of memory, were studied in 8 normal volunteers. Tests of Critical Flicker Fusion Threshold, a Sternberg Memory Scanning Task, along with subjective ratings of drug action were used. Drug effects were found to be modest. Treatment with vinpocetine was associated with improvements in short-term memory processes.

Role of vinpocetine in cerebrovascular diseases.
Patyar S, Prakash A, Modi M, Medhi B.

Department of Pharmacology & Neurology, Postgraduate Institute of Medical Education and Research, Chandigarh 160012, Chandigarh, India.

Vinpocetine, chemically known as ethyl apovincaminate, is a vinca alkaloid that exhibits cerebral blood-flow enhancing and neuroprotective effects. Non-clinical and clinical studies have suggested multiple mechanisms responsible for the beneficial neuroprotective effects of vinpocetine. As no significant side effects related to vinpocetine treatment have been reported, it is considered to be safe for long-term use. The present review focuses on studies investigating the role of vinpocetine in cerebrovascular diseases.

Correlation Between Cerebral Circulation and Intelectual lmpairment in Patients With “Aging Brain” and the Effect of Vinpocetine on Cerebral Circulation

Manabu Miyazaki
Department of Internal Medicine, Bell-land Hospital, Sakai City, Osaka, Japan

The Doppler ultrasonic technique is useful for the examination of cerebral circulation as well as for the evaluation of cerebral circulation-improving drugs. This study deals with a correlation of cerebral circulation with intellectual impairment in subjects with aging brain syndrome and with measuring the effect of vinpocetine on cerebral circulation, using the Doppler technique.

The correlation between cerebral circulation and intellectual impairment was first studied in 48 patients with aging brain and intellectual impairment. As a parameter for cerebral circulation, the Continuous lndex (CI), as calculated from the blood flow pattern recorded at the internal carotid artery, was used together with Hasegawa’s Dementia Scale (HDS) for intellectual impairment.

The results suggest some correlation between cerebral circulation and intellectual impairment in the aging brain, especially in patients with the vascular type.An increase of blood flow was recognizable after a single oral dose of 5 mg vinpocetine

References

Dezsi et al., 2002 L. Dezsi, I. Kis-Varga, J. Nagy, Z. Komlodi, E. Karpati
Neuroprotective effects of vinpocetine in vivo and in vitro. Apovincaminic acid derivatives as potential therapeutic tools in ischemic stroke
Acta Pharmaceutica Hungarica, 72 (2) (2002), pp. 84–91

Pereira et al., 2003 C. Pereira, P. Agostinho, P.I. Moreira, A.I. Duarte, M.S. Santos, C.R. Oliveira
Neuroprotection strategies: Effect of vinpocetinein in vitro oxidative stress models Estratégias de neuroprotecção: Efeito da vimpocetina em modelos in vitro de stresse oxidativo, 16 (6) (2003), pp. 401–406
Santos et al., 2000 M.S. Santos, A.I. Duarte, P.I. Moreira, C.R. Oliveira
Synaptosomal response to oxidative stress: Effect of vinpocetine
Free Radical Research, 32 (1) (2000), pp. 57–66

Nunes et al., 2011 Fernanda Nunes, Kélvia Ferreira-Rosa, Maurício dos S. Pereira, Regina C. Kubrusly, Alex C. Manhães, Yael Abreu-Villaça, Cláudio C. Filgueiras

Acute administration of vinpocetine, a phosphodiesterase type 1 inhibitor, ameliorates hyperactivity in a mice model of fetal alcohol spectrum disorder
Drug and Alcohol Dependence, Volume 119, Issues 1–2, 1 December 2011, Pages 81-87