Vinpocetine is a well-known substance in the health-hacking community that has a variety of health benefits. Vinpocetine is used to increase brain circulation, alertness, cognitive function, concentration, memory, lower inflammation and decrease oxidative stress. This article will explore vinpocetine’s history, how it works, it’s benefits, and any possible safety issues you should consider before taking it.

What is Vinpocetine?

Vinpocetine is an alkaloid derived from the compound Vincamine. Vincamine is the main ingredient of the lesser periwinkle plant, Vinca minor – a common garden plant.

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.

A Brief 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 it in 1978 under the brand name, Cavinton [1].

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

Vinpocetine Snapshot

PROs

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

CONs

  • Minimal Downsides

How Vinpocetine Works

Vinpocetine influences the flow of important electrolytes by:

  • Inhibiting sodium channels [2].
  • Inhibiting certain types (L-type) of calcium channels [3, 4].
  • Slowing down net potassium channel flow [5].

These ion channel interactions can result in decreased neurotransmitter release (dopamine and/or glutamate). Excess dopamine and glutamate in the brain can cause excitotoxicity (cell death caused by the overactivation of neurons) and increased oxidative damage. Therefore, vinpocetine is thought to have neuroprotective properties by decreasing the amount of dopamine and/or glutamate released in the brain [6].

Vinpocetine also inhibits PDE1. PDE1 inhibitors have inherent cardioprotective and cognitive-boosting properties (increase blood flow) [7, 8].

By inhibiting PDE1, vinpocetine increases cGMP concentrations, which is assumed to explain the vasodilation seen after vinpocetine ingestion [2].

Vinpocetine may lower inflammation by inhibiting IKKβ activation as well as the transportation of NF-kB across cell membranes [9].

Vinpocetine has also been shown to interact with alpha-adrenergic and TPSO (translocator protein) receptors. The impact of vinpocetine actions on these receptors is not fully understood.

How Vinpocetine is Processed by the Body

Bioavailability

Studies demonstrate that, in humans, vinpocetine has a bioavailability of 6.2 6.7% when consumed in a waterbased solution [10].

Interestingly, it 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 [10, 11].

For example, ingesting vinpocetine with a meal (independent of composition), rather than in a fasted state, can increase its bioavailability by 60 100% [12].

Certain delivery systems, such as liposomal delivery, can also increase its absorption [13, 14].

One study found that a topical vinpocetine patch was twice as bioavailable as oral ingestion [15].

Metabolism

Upon consumption, vinpocetine is quickly metabolized into its active metabolite, cis-apovincaminic acid [16, 17].

Vinpocetine is excreted after being metabolized. This is why no residue can be found in urine – only its metabolites [18].

Blood Levels

Vinpocetine is detectable in the blood within 20 minutes of consumption [19].

Oral administration with 5 mg of vinpocetine resulted in peak blood levels of approximately 64 ng/mL and the half-life of vinpocetine is around 1.46 hours [15, 15].

Vinpocetine is undetectable in the blood 2 – 3 hours after ingestion and it binds to proteins in the blood at rates from 86.6% to complete binding [20, 2].

Blood levels of apovincamic acid, vinpocetine’s main metabolite, peak within one hour after consumption and return to normal within 3 – 4 hours [20].

Vinpocetine does not accumulate in the body when sensible oral doses (5 – 30 mg daily) are used [20].

Does Vinpocetine Reach the Brain?

Yes. Studies in primates and humans have shown that vinpocetine can pass through the blood-brain barrier [21, 22].

Indeed, vinpocetine is rapidly absorbed into the human brain, with 3.18 – 4.27% entering the brain within 2 minutes of an IV dose [21].

After consumption, Vinpocetine appears to increase in the brains of humans more than the rest of the body [2].

Vinpocetine has an affinity to specific areas of the brain e.g. thalamus (24% higher than average), basal ganglia, putamen, and visual cortex. These parts of the brain then receive the most additional blood flow [23, 24, 23].

Benefits of Vinpocetine

1) Increases Brain Blood Flow & Oxygenation

In six healthy men, an infusion of 20 mg vinpocetine resulted in a 7% increase in blood flow to the brain [25].

Vinpocetine also improves brain oxygenation in individuals with circulation issues [26, 27].

Another 20 mg infusion improved blood flow in stroke victims without altering average blood pressure [26].

This enhanced blood flow is linked with cognitive protection [28].

Vinpocetine also increases microcirculation in the brain, probably by enhancing red blood cell flexibility and, therefore, reducing blood viscosity [29, 30].

2) May Enhance Memory

In a small pilot study involving 12 females, 40 mg of vinpocetine, taken 3 times per day, improved memory and memory scanning speed [31].

Vinpocetine also increases memory by long-term potentiation – the strengthening of synapses based on recent patterns of activity [32].

Inhibition of sodium and calcium channels leads to memory improvement. Vinpocetine’s inhibition of these ion channels may explain it’s memory-enhancing properties [33, 34].

Another way vinpocetine enhances memory is by affecting alpha-adrenergic receptors in the brain [35].

3) May Increase Cognitive Performance

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 [36].

4) May Improve Reaction Times

In healthy female volunteers between the ages of 25 – 40, 40 mg of vinpocetine a day significantly reduced reaction times, from approximately 610 ms to 430 ms [31].

5) Slows Cognitive Decline

One week of intravenous infusions of vinpocetine, followed by 90 days of 30 mg 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 [37].

Another study gave vinpocetine (vinpotropile) 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 [38].

The TPSO system (a sensor of brain injury and microglia activation) is upregulated in people with cognitive impairment or brain trauma [39, 40]. 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 [21, 23].

6) Improves Mitochondrial Function

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) [41].

Similarly, at high blood levels, it is able to reverse the decrease in mitochondrial function seen with beta-amyloid pigmentation [42].

7) Might be a Useful Pain Killer

Vinpocetine blocks certain sodium channels associated with pain (e.g. NaV1.8) [43, 44].

8) Anti-Inflammatory

Vinpocetine confers anti-inflammatory properties by inhibiting IKKβ and reducing the transportation of NF-kB across cell membranes [45, 46].

Potent anti-inflammatory effects occurred in mice given vinpocetine at 5 mg/kg per day [46].

9) 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) [47].

In mice, 10 – 20 mg/kg of injected vinpocetine reduced tumor growth and caused no adverse effects [47].

10) Heart Healthy

In mice with a deficiency in ApoE (Apolipoprotein E), 5 mg/kg vinpocetine given every other day almost halved the amount of plaque in the arteries [48].

This improvement was likely due to a reduction in the receptor for oxidized LDL (LOX-1) and, thus, less LDL oxidation [49].

The process of atherosclerosis is associated with vascular smooth muscle cell (VSMC) proliferation, which worsens atherosclerosis [50]. At 5 mg/kg, vinpocetine reduces VSMC proliferation by 50% [51].

11) Improves Liver Function

Vinpocetine, given orally at 2.1 – 8.4 mg/kg, reduces elevations of liver enzymes (ALT, AST, ALP) in rats given the liver toxin, CCL[52].

At the highest dose (8.4 mg/kg) there was an 82.6% reduction in liver cell death [52].

12) May Prevents Hearing Loss

In Guinea pigs, vinpocetine, given at 2 mg/kg injections, offers protection against hearing loss caused by taking antibiotics [53].

13) May Treat Headaches

Vinpocetine enhances blood flow to the brain without changing blood pressure throughout the body [54].

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

Side Effects

IV administration can cause serious adverse effects, such as death from sudden falls in blood pressure and heart rate [55, 56]. However, this is not an issue with the oral form at the standard dosages.

There have been reports of skin allergy to vincamine [57].

There was also one report of a sudden drop in white blood cell count at 15 mg per day [58].

Dosage

Take vinpocetine with meals to enhance absorption.

The standard low dose is 5 mg at each of these three meals, with 20 mg 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.

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