Vinpocetine is a well-known nootropic in the health-hacking community that has a variety of health benefits. For example, vinpocetine is used to increase brain circulation, alertness, cognitive function, concentration, memory and mood, and lower inflammation and oxidative stress.

This article will explore vinpocetine’s history, how it works, it’s possible health benefits, and any possible safety issues you should consider before taking it.

Introduction

Source and Use

Vinpocetine is as synthetic alkaloid derived from the compound Vincamine. Vincamine is the main ingredient of the lesser periwinkle plant, Vinca minor – a common garden plant (R).

Many countries, including Japan, Mexico, Russia, and many in Europe, prescribe Vinpocetine for the treatment of cognitive and circulatory brain disorders. However, in the United States and Canada, Vinpocetine is an over-the-counter supplement.

The main use of Vinpocetine is to increase blood flow to the brain.

History of Vinpocetine

Vinpocetine was first isolated from the lesser periwinkle plant in 1975 by chemist Csaba Szántay.

Gedeon Richter, a Hungarian drug company, began manufacturing Vinpocetine in 1978 under the brand name, Cavinton (R).

Vinpocetine has historically been used in European countries as a way to enhance blood flow to the brain in the treatment of cognitive decline, stroke recovery, and epilepsy.

More recently, vinpocetine has been picked up by the nootropic community for its potential to enhance memory and cognition.

Mechanisms of Action

Vinpocetine influences the flow of certain ions by:

  • Inhibiting sodium channels (R).
  • Inhibiting certain types (L-type) of calcium channels (R, R2).
  • Slowing down net potassium channel flow (R).

These ion channel interactions result in lowered neurotransmitter release. Neuroprotection occurs as dopamine or glutamate (both neurotransmitters), which can increase oxidative damage when stimulated by toxins, are suppressed (R)

Vinpocetine inhibits PDE1. PDE1 inhibitors have inherent cardioprotective and cognitive-boosting properties (R, R2).

By inhibiting PDE1, Vinpocetine increases cGMP concentrations, which is assumed to explain the vasodilation seen after Vinpocetine ingestion (R).

Vinpocetine may lower inflammatory processes by inhibiting IKKβ activation as well as the transportation of NF-kB across cell membranes (R).

Vinpocetine has also been shown to interact with the alpha adrenergic receptors and the TPSO receptor, although it is still unclear how these interactions affect the brain.

Pharmacology of Vinpocetine

Bioavailability

Studies demonstrate that, in humans, Vinpocetine has a bioavailability of 6.2-6.7% when consumed in water-based solution (R).

Interestingly, Vinpocetine has a much higher bioavailability in rodents – close to 52%. It might be the case that a similar bioavailability can be achieved in humans under certain circumstances (R, R2).

For example, ingesting Vinpocetine with a meal, rather than in a fasted state, can increase its bioavailability by 60-100% (R).

Certain delivery systems, such as liposomal delivery, can also increase vinpocetine’s absorption (R, R2).

One study found that a topical Vinpocetine patch was twice as bioavailable as oral ingestion (R).

Metabolism

Upon consumption, Vinpocetine is quickly metabolized into its active metabolite, cis-apovincaminic acid (R, R2).

Vinpocetine is excreted after being metabolized. This is why no Vinpocetine residue can be found in urine – only its metabolites (R).

Blood Levels

Vinpocetine is detectable in the blood within 20 minutes of consumption (R).

Oral administration with 5mg of vinpocetine resulted in peak blood levels of approximately 64ng/mL (R).

The half-life of Vinpocetine is around 1.46 hours (R).

Vinpocetine is undetectable in the blood 2-3 hours after ingestion (R).

Vinpocetine binds to proteins in the blood at rates from 86.6% to complete binding (R).

Blood levels of apovincamic acid, vinpocetine’s main metabolite, peak within one hour after consumption and return to normal within 3-4 hours (R).

Vinpocetine does not accumulate in the body when sensible oral doses (5-30mg daily) are used (R).

Brain Pharmacology

Studies in primates and humans have shown that Vinpocetine can pass through the blood-brain barrier (R, R2)

Indeed, Vinpocetine is rapidly absorbed into the human brain, with 3.18–4.27% entering the brain within 2 minutes of an IV dose (R)

After consumption, Vinpocetine appears to increase in the brains of humans more than the rest of the body (R).

Vinpocetine has an affinity to specific areas of the brain e.g. thalamus (24% higher than average), basal ganglia, putamen, and visual cortex (R, R2). These parts of the brain then receive the most additional blood flow (R).

My Favorite Vinpocetine Product

       Vinpocetine Snapshot

  • Longevity8.0/10
  • Inflammation8.5/10
  • Mood9.0/10
  • Cognition9.5/10
  • Energy8.0/10

  Pros

  • Boosts Brain Function
  • Slows Cognitive Decline
  • Potent Anti-inflammatory
  • Enhances Memory
  • Boosts Circulation

  Cons

  • Minimal Downsides

 

Health Benefits of Vinpocetine

1) Vinpocetine Enhances Memory

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In a mice study, researchers deliberately damaged neurons in the brain in order to inhibit hippocampus function and long-term memory potentiation. However, administration of Vinpocetine after the operation caused a complete restoration of long-term potentiation and memory formation (R).

40mg of Vinpocetine, taken 3 times per day, improved memory in 12 female subjects (measured by Steinberg technique) (R).

At 40mg per day, Vinpocetine increases memory scanning speed (R).

Vinpocetine increases memory by long-term potentiation – the strengthening of synapses based on recent patterns of activity (R).

Inhibition of sodium and calcium channels leads to memory improvement. Vinpocetine’s inhibition of these ion channels may explain it’s memory-enhancing properties (R, R2).

Another way Vinpocetine enhances memory is by affecting alpha-adrenergic receptors in the brain (R).

2) Vinpocetine Increases Brain Blood Flow & Oxygenation

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In six healthy men, an infusion of 20mg vinpocetine resulted in a 7% increase in blood flow to the brain (R).

Another 20mg infusion of Vinpocetine improved blood flow in stroke victims without altering average blood pressure (R).

This enhanced blood flow is linked with cognitive protection (R).

Vinpocetine also increases microcirculation in the brain, probably by enhancing red blood cell flexibility and, therefore, reducing blood viscosity (R, R2).

30-45mg of oral Vinpocetine improves brain oxygenation in individuals with circulation issues (R, R2).

3) Vinpocetine Increases Cognitive Power

In one study, patients received either 30 mg of Vinpocetine per day, 60 mg of Vinpocetine per day or a placebo. After 16 weeks, both Vinpocetine groups had notable improvements in cognitive performance.

Thus, Vinpocetine is a candidate for the management of symptoms of dementia.

There was no significant difference in cognitive benefits between taking 30mg and 60mg per day (R).

4) Vinpocetine Slows Cognitive Decline

One week of intravenous infusions of vinpocetine, followed by 90 days of 30mg oral dosage, significantly improved the symptoms of cognitive decline in individuals with poor blood circulation in the brain. For example, physical balance was markedly improved (R).

Another study gave Vinpotropile (Vinpocetine & Piracetam) to patients aged 50-78 with low blood flow to the brain. The rate of cognitive decline slowed significantly (e.g. speech performance tests), and subjective measures of well-being improved (R).

The TPSO system (a sensor of brain injury and microglia activation) is upregulated in people with cognitive impairment or brain trauma (R, R2). By attaching to receptors in the TSPO system, Vinpocetine might be able to reduce the activity of this system and, thus, reduce cognitive decline & aging (R, R2).

5) Vinpocetine Improves Mitochondrial Function

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Vinpocetine reduces the loss in mitochondrial membrane potential (needed to create ATP) caused by excitotoxicity (when neurons are damaged and killed by the overactivations of receptors for the excitatory neurotransmitters) (R).

Similarly, at high blood levels, Vinpocetine is able to reverse the decrease in mitochondrial function seen with beta-amyloid pigmentation (R).

6) Vinpocetine Might be a Useful Pain Killer

Vinpocetine blocks certain sodium channels associated with pain (e.g. NaV1.8)  (R, R2).

7) Vinpocetine Improves Reaction Times

In healthy female volunteers between the ages of 25-40, 80mg of Vinpocetine a day significantly reduced reaction times, from approximately 610ms to 430ms (R).

8) Vinpocetine is Anti-Inflammatory

Vinpocetine confers anti-inflammatory properties by inhibiting IKKβ and reducing the transportation of NF-kB across cell membranes (R, R2).

Potent anti-inflammatory effects occurred in mice given Vinpocetine at 5mg/kg per day (R).

9) Vinpocetine May Inhibit Cancer Growth

Vinpocetine slows the growth of breast cancer cells by interfering with the cell cycle and inhibiting the activation of certain signaling pathways (PI3K) and proteins (STAT3) (R).

In mice, 10-20mg/kg of injected Vinpocetine reduced tumor growth and caused no adverse effects (R).

10) Vinpocetine is Heart Healthy

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In mice with a deficiency in ApoE (Apolipoprotein E), 5mg/kg Vinpocetine given every other day almost halved the amount of plaque in the arteries (R).

This improvement was likely due to a reduction in the receptor for oxidized LDL (LOX-1) and, thus, less LDL oxidation (R).

The process of atherosclerosis is associated with vascular smooth muscle cell (VSMC) proliferation, which worsens atherosclerosis (R). At 5mg/kg, Vinpocetine reduces VSMC proliferation by 50% (R).

11) Vinpocetine Improves Liver Function

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Vinpocetine, given orally at 2.1-8.4mg/kg, reduces elevations of liver enzymes (ALT, AST, ALP) in rats given the liver toxin, CCL(R).

At the highest dose (8.4mg/kg) there was an 82.6% reduction in liver cell death (R).

12) Vinpocetine Prevents Hearing Loss

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In Guinea pigs, Vinpocetine, given at 2mg/kg injections, offers protection against hearing loss caused by taking antibiotics (R).

13) Vinpocetine May Treat Headaches

Vinpocetine enhances blood flow to the brain without changing blood pressure throughout the body (R).

Thus, Vinpocetine might be able to reduce headaches caused by excessive pressure. This makes sense given that the traditional usage of the periwinkle plant (source of Vinpocetine) is to reduce headaches.

Safety

Dosage

Take Vinpocetine with meals to enhance absorption.

The standard low dose is 5mg of Vinpocetine at each of these three meals, with 20mg per meal seen as a high dose. This dose range is suitable for the purposes of neuroprotection, enhancing cerebral blood flow, and reducing the rate of cognitive decline.

Side Effects

IV administration of Vinpocetine can cause serious adverse effects, such as death from sudden falls in blood pressure and heart rate (R, R2). However, this is not an issue with oral Vinpocetine at the standard dosages.

There have been reports of skin allergy to vincamine (R).

There was also one report of a sudden drop in white blood cell count at 15mg per day (R).

Technical

PDE1 – a phosphodiesterase enzyme 

cGMP – a cyclic nucleotide derived from guanosine triphosphate

TPSO system – a sensor of brain injury and microglia activation

Liposome – a spherical vesicle with at least one lipid bilayer, used to efficiently administer nutrients and drugs.

ApoE – a class of apolipoprotein found in the that is important for the normal breakdown of triglyceride-rich lipoprotein constituents

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2 COMMENTS

  • Ben

    That has hypothyroid written all over it. Although I didn’t have the fungus issue, I had the other symptoms you mentioned. Get his thyroid checked and find a doc who will opt for Nature Throid, not Synthroid.

  • Pat Coburn

    If someone has a tendency towards low BP, is this product safe. My husband really needs this for cognitive issues. He has poor circulation — cold hands, lots of fungus on toes, hands always cold, low endurance for focus and concentration. How much would you suggest?

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