Vinpocetine is a substance synthesized from vincamine, a natural constituent found in the leaves of Vinca minor (lesser periwinkle). Vinpocetine appears to have neuro-protective, antioxidant, circulatory stimulant and other effects that may be beneficial to brain function. Studies point at possible benefits in people with tinnitus, visual impairment, Meniere's disease, memory disorders (dementias) and people who have suffered strokes. It may be helpful in age-related cognitive decline, after stroke, in vertigo, Alzheimer's disease, memory enhancement, retinopathy and urinary incontinence.
Published Clinical Studiescl top
"Brain-specific" nutrients: a memory cure?1
McDaniel MA, Maier SF, Einstein GO.
Department of Psychology, University of New Mexico, Albuquerque, New Mexico 87131, USA. mcdaniel@umn.edu
OBJECTIVE: We review the experimental evaluations of several widely marketed nonprescription compounds claimed to be memory enhancers and treatments for age-related memory decline. We generally limit our review to double-blind placebo-controlled studies. The compounds examined are phosphatidylserine (PS), phosphatidylcholine (PC), citicoline, piracetam, vinpocetine, acetyl-L-carnitine (ALC), and antioxidants (particularly vitamin E). RESULTS: In animals, PS has been shown to attenuate many neuronal effects of aging, and to restore normal memory on a variety of tasks. Preliminary findings with humans, though, are limited. For older adults with probable Alzheimer's disease, a single study failed to demonstrate positive effects of PS on memory performance. For older adults with moderate cognitive impairment, PS has produced consistently modest increases in recall of word lists. Positive effects have not been as consistently reported for other memory tests. There is one report of consistent benefits across a number of memory tests for a subset of normal adults who performed more poorly than their peers at baseline. The choline compounds PC and citicoline are thought to promote synthesis and transmission of neurotransmitters important to memory. PC has not proven effective for improving memory in patients with probable Alzheimer's disease. The issue remains open for older adults without serious degenerative neural disease. Research on citicoline is practically nonexistent, but one study reported a robust improvement in story recall for a small sample of normally aging older adults who scored lower than their peers in baseline testing. Animal studies suggest that piracetam may improve neuronal efficiency, facilitate activity in neurotransmitter systems, and combat the age-related decrease in receptors on the neuronal membrane. However, for patients with probable Alzheimer's disease, as well as for adults with age-associated memory impairment, there is no clear-cut support for a mnemonic benefit of piracetam. Vinpocetine increases blood circulation and metabolism in the brain. Animal studies have shown that vinpocetine can reduce the loss of neurons due to decreased blood flow. In three studies of older adults with memory problems associated with poor brain circulation or dementia-related disease, vinpocetine produced significantly more improvement than a placebo in performance on global cognitive tests reflecting attention, concentration, and memory. Effects on episodic memory per se have been tested minimally, if at all. ALC participates in cellular energy production, a process especially important in neurons, and in removal of toxic accumulation of fatty acids. Animal studies show that ALC reverses the age-related decline in the number of neuron membrane receptors. Studies of patients with probable Alzheimer's disease have reported nominal advantages over a range of memory tests for ALC-treated patients relative to placebo groups. Significant differences have been reported rarely, however. Whether ALC would have mnemonic benefits for aging adults without brain disease is untested as far as we know. Antioxidants help neutralize tissue-damaging free radicals, which become more prevalent as organisms age. It is hypothesized that increasing antioxidant levels in the organism might retard or reverse the damaging effects of free radicals on neurons. Thus far, however, studies have found that vitamin E does not significantly slow down memory decline for Alzheimer's patients and does not produce significant memory benefits among early Parkinson's patients. Neither did a combination of vitamins E and C significantly improve college students' performance on several cognitive tasks. CONCLUSIONS: In sum, for most of the "brain-specific" nutrients we review, some mildly suggestive effects have been found in preliminary controlled studies using standard psychometric memory assessments or more general tests designed to reveal cognitive impairment. We suggest that future evaluations of the possible memory benefits of these supplements might fruitfully focus on memory processes rather than on memory tests per se.
PMID: 14624946 [PubMed - in process]
Asymptomatic ischemic cerebrovascular disorders and neuroprotection with vinpocetine.2
Hadjiev D.
University Hospital of Neurology and Psychiatry, St. Naum Compl. Javorov, B-1504 Bulgaria, Sofia, bl. 21. A. dimiter_hadjiev@hotmail.com
The asymptomatic ischemic cerebrovascular disorders (AICVD) is an early manifestation of cerebrovascular disease. It is also known as latent insufficiency of the cerebrovascular circulation or as asymptomatic cerebrovascular disorders. Recently, the term subclinical disease, detected noninvasively, has been introduced by American Heart Association. The diagnosis is based on the following criteria: evidence of vascular risk factors; episodic nonspecific complaints without any focal cerebral symptoms; mild cognitive deficit, detected by neuropsychological tests; carotid ultrasonography often shows intimal-medial thickening, atherosclerotic plaques and carotid stenosis; CT and MRI occasionally reveal silent cerebral infarctions, white matter hyperintensities or cerebral atrophy; regional hypoperfusion above the ischemic threshold is also seen by rCBF measurements. Treatment of the AICVD, modifying the vascular risk factors and using neuroprotective agents, should be the cornerstone of primary prevention of ischemic stroke and cognitive decline, caused by cerebrovascular disorders. Vinpocetine has been found to interfere with various stages of the ischemic cascade: ATP depletion, activation of voltage-sensitive Na(+)- and Ca(++)-channels, glutamate and free radicals release. The inhibition of the voltage-sensitive Na(+)-channels appears to be especially relevant to the neuroprotective effect of vinpocetine. Pronounced antioxidant activity of the drug could also contribute to the neuroprotection. PET studies in primates and man showed that 11C labelled vinpocetine passes the blood-brain barrier rapidly. Heterogeneous brain distribution of the compound was observed mainly in the thalamus, basal ganglia, occipital, parietal and temporal cortex, regions which are closely related to the cognitive functions. PET studies in chronic ischemic stroke patients revealed favourable effects of vinpocetine on rCBF and glucose metabolism in the thalamus, basal ganglia and primary visual cortex. It seems, vinpocetine, affecting the multiple mechanisms of the AICVD, could be of benefit for the treatment in this early stage of cerebrovascular disease. Vinpocetine may also become a new therapeutic approach to prophylactic neuroprotection in patients at high risk of ischemic stroke.
Publication Types:
PMID: 12861957 [PubMed - indexed for MEDLINE]
3
[Effect of vinpocetin on the hemorheologic parameters in patients with chronic cerebrovascular disease]
Szapary L, Horvath B, Alexy T, Marton Z, Kesmarky G, Szots M, Nagy F, Czopf J, Toth K.
Pecsi Tudomanyegyetem, Altalanos Orvostudomanyi Kar, Neurologiai Klinika. szapary@neuro.pote.hu
INTRODUCTION: Data collected from large number of multicenter, randomized trials in acute and chronic stroke patients provide evidence, that incidence and high mortality of cerebrovascular disorders can be decreased mainly by prevention and that the effectiveness of acute stroke treatment is limited. The terminology of "chronic cerebrovascular diseases" involves many pathologic entities and often atypical clinical symptoms refer to the focal or global hypoperfusion of the brain. However, hemorheological disturbances seem to be important factors of the complex pathomechanism. Vinpocetine has successfully been used in the treatment of cerebrovascular diseases, the part of the mechanism of action are the favourable rheological effects demonstrated after oral administration in more previous studies. AIMS AND METHODS: In this study the hemorheological changes after administration of small (30 mg/day) and high dose (increased to 70 mg/day) intravenous vinpocetine for 7 days in 30 patients in chronic phase of ischemic cerebrovascular disease were investigated. RESULTS: High dose parenteral vinpocetine treatment significantly (p < 0.05-0.005) decreased the hematocrit, the whole blood and plasma viscosity and red blood cell aggregation compared to the values before the treatment. Only red blood cell aggregation was improved significantly (p < 0.05) by small dose treatment. CONCLUSION: This study and other hemorheological studies in cerebrovascular patients demonstrated persistent rheological abnormalities despite the preventive therapy. The beneficial rheological effect of high dose parenteral vinpocetine indicates the use of this drug in the treatment of chronic cerebrovascular diseases.
Publication Types:
PMID: 12830727 [PubMed - indexed for MEDLINE]
4
[Neuroprotective effects of vinpocetine in vivo and in vitro. Apovincaminic acid derivatives as potential therapeutic tools in ischemic stroke]
Dezsi L, Kis-Varga I, Nagy J, Komlodi Z, Karpati E.
Richter Gedeon Vegyeszeti Gyar Rt., Budapest, Gyomroi ut 19-21.-1103.
The aim of the present study was to review neuroprotective therapy from the preclinical point of view as a potential tool for the treatment of stroke, as well as to discuss neuroprotective effects of the apovincaminic acid derivative vinpocetine (Cavinton). Our own in vivo and in vitro experiments were aimed at further characterizing pharmacological effects involved in the vinpocetine-induced neuroprotection. The effect of vinpocetine on infarct volume (obtained by 2,3,5-triphenyltetrazolium-chloride staining) was studied in permanent middle cerebral artery occlusion (MCAO) in rats (3 mg/kg i.p., 30 min postischemia). Vinpocetine treatment significantly decreased infarct volume (by 42%, p < 0.05) compared to control, which was better than the effect of nimodipine (17%) or MK-801 (18%). Neurotoxicity measurements were made in primary cortical cell culture using LDH release as an indicator. Vinpocetine dose-dependently inhibited prolonged (24 h) or transient (15 min) glutamate, and transient N-metil-D-aspartate (NMDA) or veratridine (0.1-1 mM) induced excitotoxicity (IC50 = 2-7 x 10(-6) M). In these tests the neuroprotective potency of vinpocetine was lower than that of MK-801, but it was similar to those of flunarizine or nimodipine. These results together with former literature data indicate that apovincaminic acid derivatives possessing strong neuroprotective potential may play an important role in the therapy of ischemic stroke.
PMID: 12498034 [PubMed - indexed for MEDLINE]
5
A vinca alkaloid enhances morphological dynamics of dendritic spines of neocortical layer 2/3 pyramidal cells.
Lendvai B, Zelles T, Rozsa B, Vizi ES.
Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary.
We imaged neocortical layer 2/3 pyramidal cells in rat brain slices with two-photon laser scanning microscopy to investigate that spine motility can be influenced by the voltage-dependent Na(+) and Ca(2+) channel inhibitor, vinpocetine, which exhibited positive cognitive effects in human studies. Veratridine, which enhances sodium influx, was also tested on dendritic spine motility. Perfusion with vinpocetine, a derivative of vinca alkaloids, caused a substantial increase in the structural dynamics of dendritic spines measured by the changes in length or the number of new/retracted spines. In contrast, enhancement of sodium influx with veratridine failed to change spine motility. Our results indicate that the rapid changes in spine shape and size could occur, when calcium and sodium influx has been decreased by this vinca alkaloid. Spine motility induced by vinpocetine may be associated to microtubule alterations, an effect that was described for other vinca alkaloids. On the other hand, the potential of vinpocetine to enhance cognition in clinical studies suggests that the increased spine motility may be related to cognitive functions.
PMID: 12464397 [PubMed - indexed for MEDLINE]
[Complex effects of cavinton on climacteric symptoms]6
Kolarov G, Orbetsova M, Nalbanski B, Kamenov Z, Georgiev S, Filipov E, Petrova Iu, Marinov B, Georgiev G.
The use of nonhormonal drugs in order to ameliorate climacteric symptoms makes it possible to treat also those women in whom there are some contraindications or lack of compliance for taking hormonal replacement therapy. The drugs with complex effects on the whole body functions are more widely used recently. The aim of the present study is to assess the therapeutic effect of Cavinton (vinpocetin) on the degree of climacteric symptoms and to verify its complex beneficial influence. The study comprises of three groups of women in early menopause--control group (n = 30), treatment groups with normolipidaemia (n = 32) and with hyperlipidaemia (n = 29). All women presented with moderately expressed climacteric symptoms as assessed by Kupperman menopausal index and Hamilton-Anxiety-Skala (HAMA). The women in the 2nd and 3rd groups have been taking Cavinton in an oral dose of 5 mg three times daily for 3 months. The following parameters of lipid metabolism were determined in the beginning and at the end of the study: total, HDL- and LDL-cholesterol, triglycerides, and two indexes of lipid atherogenic risk--total/HDL-cholesterol ratio and atherogenic index (AI) = total--HDL/LDL-cholesterol. The menopausal complaints were assessed by Kupperman index and HAMA. Blood vessels reactivity was determined by pulsation index (PI). Statistically significant decrease in total cholesterol and LDL-cholesterol levels as well as amelioration of atherogenic indexes was observed in the 3rd group. Kupperman index and HAMA decreased significantly on the 45th day and the 3rd month in the women under treatment. No significant changes in PI were observed but a tendency towards a decrease was seen in the 3rd group. Our data suggest that Cavinton possesses complex beneficial effects in climacteric women significantly ameliorating climacteric symptoms as well as some parameters of lipid metabolism in women with hyperlipidaemia.
Publication Types:
PMID: 11799757 [PubMed - indexed for MEDLINE]