Knowde Enhanced TDS
Identification & Functionality
- Active Component
- Chemical Name
- Pharma & Nutraceuticals Functions
- Molecular Formula
- C21H26N2O3
- Laboratory code
- DMF-400
- CAS No.
- 42971-09-5
- EC No.
- 256-028-0
Features & Benefits
- Benefits
In the United States, it is commonly sold as a dietary supplement for the general population either alone or with other ingredients. Its numerous proposed uses include for improvement of brain function, rapid weight/fat loss, increases in energy, enhancement in focus and visual acuity, prevention of motion sickness, hearing and eye disorders, chronic fatigue syndrome and treatment of menopausal symptoms. Some of these purposes make it a product for athletes too. (Chemical Information Review Document for Vinpocetine, National Toxicology Program, U.S. Department of Health and Human Services, Research Triangle Park, NC, 2013) According to the Physicians' Desk Reference for Nutritional Supplements, doses may range from 5-20 mg/day.
Applications & Uses
Properties
- Appearance
- White or slightly yellow, crystalline powder.
- Soluble in
- methylene chloride, slightly soluble in anhydrous ethanol.
- Insoluble in
- Practically in water
- Typical Properties
- Microbiological Values
| Value | Units | Test Method / Conditions | |
| Molecular Weight | 350.45 | — | — |
| Specific optical rotation (dried substance) | 127.0° to +134.0° | — | — |
| Infrared absorption spectrophotometry | According to Vinpocetine CRS. | — | — |
| HPLC | The retention time of the main peak of the Sample solution corresponds to that of the principal peak for the Stock standard solution, as obtained in the test for Organic Impurities. | — | — |
| Loss On Drying of its weight | max. 0.5 | % | — |
| Sulphated Ash (Residue On Ignition) | max. 0.1 | % | — |
| Heavy Metals | max. 10 | ppm | — |
| Acidimetric Assay (Titrimetry, of C22H26N2O2, calculated on the dried basis) | 98.5 - 101.5 | % | — |
| Residual Solvents (Ethanol, 0.20%) | max. 2000 | ppm | — |
| Residual Solvents (Methylene chloride, 0.01%) | max. 100 | ppm | — |
| Value | Units | Test Method / Conditions | |
| Tamc | max. 103 | cfu/1 g | — |
| Tymc | max. 102 | cfu/1 g | — |
| Gram-Bile Tol. | max. 10 | cfu/1 g | — |
| Pyrogens | Apyrogens | — | — |
Technical Details & Test Data
- Efficacy
- As compared with placebo, Vinpocetine was found to be capable of reducing hypoxia through oxygenation in healthy men that were submitted to induced hypoxia with a lower than normal concentration of oxygen (10.5 %). The volunteers reported better subjective well-being in the treated vs. Placebo group. Vinpocetine was also capable of improving memory retention time processes in middle-aged (25-40) healthy women. This result was confirmed by another study on a different group of women of similar age. In patients with a low level of vestibular stability, vinpocetine was shown to be able to prevent antimotion. In Italian patients with CNS degenerative disorders or chronic cerebral dysfunctions of vascular origin, the authors observed an improvement in all the parameters used to measure the efficacy of the treatment. In the first study, 73-77 % of patients showed an improvement in terms of the severity of illness, and in the second, approximately 56 % reflected a similar improvement. In both cases, this is significantly better than with placebo. Hindmarch et al. in England and Blaha et al. in Germany have both studied the effect of vinpocetine on organic psychosyndrome with doses of up to 60 mg/day or placebo. A dose related effect was seen between doses of 15 mg/day or 60 mg/day. A significant improvement was seen in both trials, with up to 80 % of patients showing improvements. This was significantly better than with placebo. The last of this group of trials was on patients with chronic degenerative cerebrovascular function and they also showed marked improvement beyond the placebo effect.
- Some of the trials studying the effects of vinpocetine as compared with reference therapies have yielded the following results. Vinpocetine is markedly better than Ifenprodil tartrate or DHEM for the treatment of sequels of cerebral infarction, cerebral arteriosclerosis and transient ischemia attacks. The parameter used is a subjective index of the physician´s impression. However, there seems to be little evidence of bias and at the very least, the efficacy of vinpocetine in these diseases is clearly established. Vinpocetine also proved more efficacious than Xantinol nicotinate in cerebrovascular patients. An improvement of the condition was observed in 60.6 % of cases, significantly better than the 47.1 % attained by Xantinol nicotinate alone. However, the patients were at a near-terminal stage and in fact a large proportion of patients died during the treatment, which makes assessment difficult. In the last trial, vinpocetine proved as useful as Lucidril in the treatment of auditive disorders of vascular origin, but did not improve on it.
- The last set of clinical trials is the set of non-controlled, open studies. As stated before, the most impressive is the Portuguese study with more than 8.000 patients included. This study concludes that an improvement in the condition was observed in approximately 76 % of assessable cases in patients with a wide variety of vascular disorders. Inconclusive cases were low, at less than 25 %, considering the size and scope of the study.
- The other open study showed that vinpocetine can significantly improve the condition of patients with cerebrovascular disorders, such as cerebral apoplectic sequela or transient ischaemic attack in up to 77 % of cases.
- In the case of cerebral arteriosclerosis, and chronic cerebral insufficiency, the therapy was also effective as judged by psychological tests and circulatory parameters.
The conclusion regarding the efficacy of VINPOCETINE is that it can be useful in the treatment of the following diseases:
- Symptoms of cerebrovascular disorders such as memory loss, aphasia, apraxia, motion sickness, vertigo, headache, and vasovegetative symptoms associated with menopause; other cerebral affectations such as cerebrovascular insufficiency, or ischaemic lesions;
- Certain eye diseases;
- Hearing impairment due to circulatory disorders.
Safety & Health
- Clinical trial safety and efficacy information
- This information has been divided into three groups: the standard controlled studies with placebo, the controlled studies with a reference therapy, and non-controlled studies.
- Several placebo controlled studies are presented. They were performed in Germany, England, Italy, Hungary and Russia and have resulted in publications in peer-reviewed literature. Subjects could be healthy volunteers (without treatment or subjected to hypoxia) or patients with cerebral vascular disorders, low level of vestibular stability, central nervous system (CNS) degenerative disorders, mild to moderate OPS (Organic Psycho-syndrome), ischemia or senile dementia of vascular origin. Treatment doses, schedules and routes were varied and could be from 10 mg/day to as high as 120 mg/day administered p.o. in most cases during up to two years of treatment. Age groups were also very varied, with some studies concentrating on younger patients, patients of no specific age group, and most on older subjects. As was the case for pharmacokinetics, children are absent from the trials since the drug is not intended for them. Sex ratios were adequate. Each of the clinical trials was correctly conducted as can be seen from the publications, with scientifically valid preparation and monitoring. Placebo was always given with the same regimen as the drug, and in a way as to make it indistinct. A very wide range of parameters were studied: from the least scientific subjective evaluation to more sophisticated neurological and psychological evaluation tools such as the Clinical Global Impressions (CGI), “Sandoz clinical assessment geriatric” (SCAG) scale and Line Analog Rating scales (LARS), as well as side and other effects.
- The authors have also presented also data from several controlled trials with reference therapies to better establish the usefulness of their pharmaceutical products. The trials were conducted in Japan and Hungary, and meet international standards for such trials. Vinpocetine was compared with Ifenprodil tartrate (known for its cerebral vasodilator effect), DHEM (Dihydroergotoxine mesylate), Xantinol nicotinate (known for its vasodilatory effect in the ear), and Lucidril (also a vasodilator). A study attempting to identify the best dose for vinpocetine is also presented in this section. As in the previous section, groups were of adequate size, sex ratio and age distribution. The patients suffered from a variety of disorders: cerebral infarction, cerebral arteriosclerosis, ischemia, and different types of deafness. The authors examine the effect of vinpocetine in terms of neurological parameters, metabolic and circulatory indicators, and patients’ hearing impairment symptoms.
- The last part of the studies, the non-controlled studies, contains some different clinical trials (in Russia, Japan, Portugal, etc.). The most impressive of these trials is the Portuguese trial which examined 8.940 patients suffering from a wide range of cerebrovascular disorders. The other trials were carried out on groups of 30-288 patients, male or female, of different ages. Posology was p.o. one or three times daily (except for two of the Russian studies, which used the i.v. route) with doses of 10-30 mg/day. Patients suffered from various cerebrovascular diseases, chronic ischemia and epilepsy. Clinical symptoms were examined, with SCAG scale, cerebral blood flow, neurological and symptomatological indicators.
- On the whole, all these studies can be considered as valid clinical trials, as demonstrated by their publication in peer-reviewed international scientific journals. Observations and conclusions can now be drawn in the following sections.
- Safety
- An exhaustive list of all the different side-effects observed in all these trials would be redundant. In most of the trials, no side-effects were observed. However, in some trials, especially in those with older patients, some small disturbances were reported.
- In the studies with placebo, the following side effects were reported in five cases: face-flushing, dyspepsia, dry mouth, palpitations, vertigo, and more minor disturbances. In all cases, these side effects were not distinguishable from those caused by the placebo studies. All of the authors conclude that vinpocetine has no clinically relevant side-effect.
- In trials dealing with patients treated with Vinpocetine or a reference substance, no more side-effects have surfaced. Adverse reactions were at a very low frequency (always less than 5 % of total) and the symptoms were trivial (epigastric pain, hot flashes). In the trial involving Xantinol nicotinate, 15.1 % of the vinpocetine patients died during treatment. This was not due to a toxic effect of the drug and in fact, some 30.6 % of the reference therapy group also died during the study. This drug is known not to be toxic and the deaths were due to the near-terminal stage of the patients at the start of the trials.
- In the open non-controlled studies no side effects were reported in the smaller trials except for the one by Ebi where slightly more than 2 % of patients exhibited adverse reactions. One discontinued treatment due to a mild allergic reaction. An in-depth study of side effects was carried out by Diogo on the 500 cases of reported adverse reaction (5.59 % of total). The most important reactions reported are hypotension and tachycardia. The frequencies of these affectations are not distinguishable from those obtained in the previous placebo studies.
- From these very thorough studies of side effects in several thousand patients, it can be safely concluded that vinpocetine has virtually no side effect. In the technical file and the leaflet the different observed side-effects are included. None were left out and it can even be said that those included are superfluous, as data shows that this is no more than placebo effect.
- An interaction with hypotensive drugs is not discarded. Furthermore, no evidence of interactions has surfaced in more than 10 years of marketing in other countries so it can safely be said that Vinpocetine has no interactions. Contraindications for pregnancy arise from animal studies and have been discussed in the relevant section.
- From the series of clinical trials, it can be concluded that it is satisfyingly demonstrated that the indications for Vinpocetine are accurate and based on solid medical evidence. In the same way, it can be said that the proposed contraindications and warning of possible side-effects cover all the known aspects of Vinpocetine.