One of the most commonly used nootropic drugs is Actovegin, which has a wide spectrum of pharmacological effects and has an extensive evidence base that confirms its effectiveness in the treatment of various diseases of the nervous system. The drug Actovegin made by Nycomed (Austria) contains highly purified hemodialysate, obtained by ultrafiltration from calves’ blood.
Actovegin is a mixture of natural substances of inorganic (sodium, potassium, calcium, magnesium, chlorides, nitrogen compounds) and organic (acetate, lactate, amino acids, nucleosides, glycosphingolipids, antioxidant enzymes) genesis.
The composition of the drug includes low-molecular compounds, which excludes the presence of prion diseases, such as Creutzfeldt-Jakob disease. The technology of obtaining Actovegin excludes the presence of protein components that possess antigenic and pyrogenic properties.
Precise data on the pharmacokinetics of Actovegin is not available since it is a multi-component drug and consists of substances naturally occurring in the human body. The method of production of Actovegin and the results of studies on the mechanisms of its action are discussed in detail in a review devoted to almost a half-century history of the use of this drug.
It is known from experimental studies that Actovegin activates glucose uptake by cells within 5 minutes after intravenous administration, with its peak after 120 minutes. At present, it is believed that the insulin-like effect of Actovegin and the stimulation of glucose metabolism are associated with inositolphospho-oligosaccharides contained in the preparation. Due to the fact that Actovegin modulates the activity of intracellular glucose transport, activation of lipolysis takes place.
The antihypoxic effect of Actovegin is related to its ability to increase oxygen uptake by tissues, which increases the resistance of cells to hypoxia. As the result of increased oxygen uptake by the tissues, the formation of macroergic phosphates (adenosine triphosphate, adenosine diphosphate) increases, enzymes of oxidative phosphorylation are activated, the synthesis of carbohydrates and proteins is accelerated and the products of anaerobic glycolysis (lactate) decay, energy cellular imbalance is reduced.
The increase in oxygen absorption by the vascular wall after administration of Actovegin leads to normalization of endothelium-dependent reactions and a decrease in peripheral vascular resistance. As a result, the formation of high-energy phosphates in the cellular structures increases. Improvement of blood flow in the system of microcirculation mediated by Actovegin associated with the normalization of endothelium-dependent reactions (vasodilation) and the reduction of peripheral vascular resistance provides an increase in the oxygen metabolism of the vascular wall.
The antioxidant effect of Actovegin is mediated by the presence of superoxide dismutase in the formulation (as confirmed by atomic emission spectrometry), as well as magnesium ions that increase the activity of glutathione synthetase, which translates glutathione into glutamine. In a recent study, it was found that Actovegin reduces apoptosis (by the activity of caspase-3), increases the number of synaptic connections, and dose-dependently reduces oxidative stress in neurons.
In a study by A. Diekmann et al. (2011) it was found that Actovegin improves the excitation of sensory fibers and reduces apoptosis in the sciatic nerve fibers by decreasing the activity of PARP, which emphasizes the effect of Actovegin on the pathogenetic mechanisms of the formation of cellular damage in diabetes.
Treatment with Actovegin in patients with various neurological diseases is reviewed in a number of reviews. At present, Actovegin is widely used for the treatment of vascular diseases of the brain and cognitive disorders of varying severity. In a study on the efficacy of Actovegin on the effect on cognitive function in elderly and elderly patients, a statistically significant improvement in memory, attention, and thinking was observed within 2 weeks of the treatment course.
Clinical improvement of the state of cognitive functions from the data of neuropsychological testing was accompanied by normalization of the electroencephalogram and an increase in the amplitude of the evoked cognitive potentials P300, and even a single Actovegin injection led to an improvement in the electrophysiological parameters of the function of the brain.
There are data on the treatment of Actovegin with diseases of the peripheral nervous system. The vascular component is present in various mononeuropathies, including radiculopathy, multiple mononeuropathies, and polyneuropathies. An attempt was made to treat Actovegin in combination with Lornoxicam and Indometacin in elderly patients with discogenic radiculopathies who have an intense pain syndrome. With the application of Actovegin, patients experienced a faster regression of the pain syndrome than patients who received only Lornoxicam or Indometacin.