Vinpocetine
Encyclopedia
Vinpocetine is a semisynthetic derivative alkaloid of vincamine
(sometimes described as "a synthetic
ethyl ester of apovincamine"), an extract from the periwinkle
plant.
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. In other words, Vinpocetine may help support brain functions such as concentration and memory by activating cerebral metabolism. A small subset of users report uncomfortable, adverse reactions to vinpocetine. A low initial dosage is ordinarily recommended.
Vinpocetine has been identified as a potent anti-inflammatory agent that might have a potential role in the treatment of Parkinson's disease
and Alzheimer’s disease.
s had tested "older adults with memory problems," and these studies had promising results, in which a 2003 Cochrane review decided that the results were inconclusive.
Prior to 2003, a different study from 1985 had tested young, healthy adults, but this study had 12 subjects and used a short treatment period.
agent. Vinpocetine inhibits the up-regulation of NF-κB by TNFα in various cell tests. Reverse transcription polymerase chain reaction
also shows that it reduced the TNFα-induced expression of the mRNA of proinflammatory molecules such as interleukin-1 beta
, monocyte chemoattractant protein-1 (MCP-1), and vascular cell adhesion molecule-1 (VCAM-1). In mice, vinpocetine reduced lipopolysaccharide
inoculation induced polymorphonuclear neutrophil infiltration into the lung. Neuroinflammatory processes can result in neuronal death in Parkinson's disease
(PD) and Alzheimer’s disease (AD). It has been suggested that "it would be interesting to test whether vinpocetine’s antiinflammatory properties would have a protective effect in models of neurodegenerative conditions such as AD and PD."
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 causes the vasorelaxant effects of vinpocetine on cerebral smooth muscle tissue.
Independent of vinpocetine's action on PDE, vinpocetine inhibits IKK
preventing IκB degradation and the following translocation of NF-κB to the cell nucleus.
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 causes depression
as a side effect of the cardiovascular and anti-psychotic effects. However, this effect tends to be reversible upon cessation of Vinpocetine administration, with full remission typically occurring within 3–4 weeks.
."
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 granulocytes 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.
Other alkaloids extracted from the periwinkle family, including Vincristine
and Vinblastine
are powerful chemotherapeutic agents which impair formation of microtubules and thus growth of related cancers, intestinal epithelium and bone marrow.
Vincamine
Vincamine is a peripheral vasodilator that increases blood flow to the brain . Generic drugs containing vincamine exist in specific regions. Most common drug preparations are in the sustained release forms...
(sometimes described as "a synthetic
Chemical synthesis
In chemistry, chemical synthesis is purposeful execution of chemical reactions to get a product, or several products. This happens by physical and chemical manipulations usually involving one or more reactions...
ethyl ester of apovincamine"), an extract from the periwinkle
Vinca minor
Vinca minor, Lesser periwinkle and Dwarf periwinkle, is a plant native to central and southern Europe, from Portugal and France north to the Netherlands and the Baltic States, and east to the Caucasus, and also in southwestern Asia in Turkey...
plant.
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
Vasodilation
Vasodilation refers to the widening of blood vessels resulting from relaxation of smooth muscle cells within the vessel walls, particularly in the large arteries, smaller arterioles and large veins. The process is essentially the opposite of vasoconstriction, or the narrowing of blood vessels. When...
and as a nootropic
Nootropic
Nootropics , also referred to as smart drugs, brain steroids, memory enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration...
for the improvement of memory. In other words, Vinpocetine may help support brain functions such as concentration and memory by activating cerebral metabolism. A small subset of users report uncomfortable, adverse reactions to vinpocetine. A low initial dosage is ordinarily recommended.
Vinpocetine has been identified as a potent anti-inflammatory agent that might have a potential role in the treatment of Parkinson's disease
Parkinson's disease
Parkinson's disease is a degenerative disorder of the central nervous system...
and Alzheimer’s disease.
Controlled clinical trials
As of 2003 only three controlled clinical trialClinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
s had tested "older adults with memory problems," and these studies had promising results, in which a 2003 Cochrane review decided that the results were inconclusive.
Prior to 2003, a different study from 1985 had tested young, healthy adults, but this study had 12 subjects and used a short treatment period.
Use as a vasodilator
Vinpocetine is widely used in the body building community as a vasodilator. Although no studies have been conducted on the effectiveness of vinpocetine on performance enhancement during exercise, in trial both beneficial and adverse effects have been reported on body building forums.Anti-inflammatory action
Vinpocetine has been identified as a novel anti-inflammatoryAnti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....
agent. Vinpocetine inhibits the up-regulation of NF-κB by TNFα in various cell tests. Reverse transcription polymerase chain reaction
Reverse transcription polymerase chain reaction
Reverse transcription polymerase chain reaction is a variant of polymerase chain reaction , a laboratory technique commonly used in molecular biology to generate many copies of a DNA sequence, a process termed "amplification"...
also shows that it reduced the TNFα-induced expression of the mRNA of proinflammatory molecules such as interleukin-1 beta
IL1B
Interleukin-1 beta also known as catabolin, is a cytokine protein that in humans is encoded by the IL1B gene. IL-1β precursor is cleaved by caspase 1 . Cytosolic thiol protease cleaves the product to form mature IL-1β.- Function :Interleukin 1 was discovered by Gery in 1972...
, monocyte chemoattractant protein-1 (MCP-1), and vascular cell adhesion molecule-1 (VCAM-1). In mice, vinpocetine reduced lipopolysaccharide
Lipopolysaccharide
Lipopolysaccharides , also known as lipoglycans, are large molecules consisting of a lipid and a polysaccharide joined by a covalent bond; they are found in the outer membrane of Gram-negative bacteria, act as endotoxins and elicit strong immune responses in animals.-Functions:LPS is the major...
inoculation induced polymorphonuclear neutrophil infiltration into the lung. Neuroinflammatory processes can result in neuronal death in Parkinson's disease
Parkinson's disease
Parkinson's disease is a degenerative disorder of the central nervous system...
(PD) and Alzheimer’s disease (AD). It has been suggested that "it would be interesting to test whether vinpocetine’s antiinflammatory properties would have a protective effect in models of neurodegenerative conditions such as AD and PD."
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
Phosphodiesterase
A phosphodiesterase is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below...
(PDE) type-1 inhibitor, (with an IC50
IC50
The half maximal inhibitory concentration is a measure of the effectiveness of a compound in inhibiting biological or biochemical function. This quantitative measure indicates how much of a particular drug or other substance is needed to inhibit a given biological process by half...
of approximately 10−5 M.) leading to increases in intracellular levels of cyclic guanosine 3'5'-monophosphate (cGMP), an action that causes the vasorelaxant effects of vinpocetine on cerebral smooth muscle tissue.
Independent of vinpocetine's action on PDE, vinpocetine inhibits IKK
IκB kinase
The IκB kinase is an enzyme complex that is involved in propagating the cellular response to inflammation.The IκB kinase enzyme complex is part of the upstream NF-κB signal transduction cascade...
preventing IκB degradation and the following translocation of NF-κB to the cell nucleus.
Increases in neuronal levels of DOPAC, a metabolic breakdown product of dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
, 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
Reserpine
Reserpine is an indole alkaloid antipsychotic and antihypertensive drug that has been used for the control of high blood pressure and for the relief of psychotic symptoms, although because of the development of better drugs for these purposes and because of its numerous side-effects, it is rarely...
, a structural relative of vinpocetine, which depletes catecholamine levels and causes depression
Depression (mood)
Depression is a state of low mood and aversion to activity that can affect a person's thoughts, behaviour, feelings and physical well-being. Depressed people may feel sad, anxious, empty, hopeless, helpless, worthless, guilty, irritable, or restless...
as a side effect of the cardiovascular and anti-psychotic effects. However, this effect tends to be reversible upon cessation of Vinpocetine administration, with full remission typically occurring within 3–4 weeks.
Side effects
Vinpocetine is generally tolerated well and without many cases of adverse reaction reported. No serious side effects have been reported in any clinical trials, although none of these trials have been long-term. According to a Dr. Wollschlaeger, "a critical review of the literature has reported no adverse effects. Vinpocetine appears to be safe, without any adverse affects. The only reported side effect, in a very small number of cases, was a slightly upset stomach, which is almost always a side effect for some people taking herbs. We have not seen any adverse effects or drug-herb interactions, and it seems safe to take with other drugs, including diabetes drugs, and blood thinners like CoumadinCoumadin
*For the rodenticide class of anticoagulant poisons sometimes loosely referred to as coumadins or coumarins, see 4-hydroxycoumarins.*For the pharmaceutical with the trade name Coumadin, see warfarin....
."
The safety of vinpocetine in pregnant women has not been evaluated.
Vinpocetine has been implicated in one case to induce agranulocytosis
Agranulocytosis
Granulopenia, also known as Agranulosis or Agranulocytosis, is an acute condition involving a severe and dangerous leukopenia , most commonly of neutrophils causing a neutropenia in the circulating blood. It represents a severe lack of one major class of infection-fighting white blood cells...
, a condition in which granulocytes are markedly decreased. Some people have anecdotally noted that their continued use of vinpocetine reduces immune function. Commission E
Commission E
The German Commission E Monographs are a therapeutic guide to herbal medicine with 380 monographs evaluating the safety and efficacy of herbs for licensed medical prescribing in Germany. The commission itself was formed in 1978, and no longer exists....
warned that vinpocetine reduced immune function and could cause apoptosis
Apoptosis
Apoptosis is the process of programmed cell death that may occur in multicellular organisms. Biochemical events lead to characteristic cell changes and death. These changes include blebbing, cell shrinkage, nuclear fragmentation, chromatin condensation, and chromosomal DNA fragmentation...
in the long term.
Other alkaloids extracted from the periwinkle family, including Vincristine
Vincristine
Vincristine , formally known as leurocristine, sometimes abbreviated "VCR", is a vinca alkaloid from the Catharanthus roseus , formerly Vinca rosea and hence its name. It is a mitotic inhibitor, and is used in cancer chemotherapy.-Mechanism:Tubulin is a structural protein that polymerizes to...
and Vinblastine
Vinblastine
Vinblastine is an antimicrotubule drug used to treat certain kinds of cancer, including Hodgkin's lymphoma, non-small cell lung cancer, breast cancer, head and neck cancer, and testicular cancer. It is also used to treat Langerhan cell histiocytosis....
are powerful chemotherapeutic agents which impair formation of microtubules and thus growth of related cancers, intestinal epithelium and bone marrow.
Dosage
It is recommended that first-time users ingest only 2–5 mg of vinpocetine with meals to make sure they are not hypersensitive to it. Users may then increase the dosage to 10–40 mg a day (which may, although very rarely, cause some light side effects).External links
- ErowidErowidErowid, also called The Vaults of Erowid, is an online library of information about psychoactive plants and chemicals and other topics on altered states of consciousness such as meditation and lucid dreaming. It provides information about legal and illegal substances, including their desired and...
Vinpocetine Vault - Vinpocetine article from PDRhealth
- Vinpocetine for cognitive impairment and dementia - CochraneCochrane CollaborationThe Cochrane Collaboration is a group of over 28,000 volunteers in more than 100 countries who review the effects of health care interventions tested in biomedical randomized controlled trials. A few more recent reviews have also studied the results of non-randomized, observational studies...
review - Information about Vinpocetine