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Actovegin 5×5 ml ampoules for IV/IM use by Nycomed
200 mg/ 5ml active substance
Product description: Actovegin® is a protein-free prescription product obtained from calf blood. Actovegin® has been in clinical use for over 40 years. Actovegin® is prescribed by hospital specialists and general practitioners in selected European markets, Russia and the CIS, China and South Korea. Actovegin® is available as tablets, injections and infusions. Over-the-counter (OTC) formulations (cream, gel, ointment) are also available.
Sports Performance: Suspected to be used by athletes for injury repair, recovery and increased oxygen transport and delivery. Used as I.M. injections at site of injury similar to Prolotherapy techniques and for general recovery. Used as I.V. injection several hours pre-event for increased oxygen delivery/ uptake. Side effects include lowered blood sugar levels and possible allergic reaction.
Medical need: Actovegin® is used in indications that include disturbances in cerebral circulation (e.g. cranio-cerebral traumas), peripheral blood flow (e.g. arterial angiopathy), skin graftings, burns, scalds, abrasions, wound-healing impairment, and radiation-induced skin and mucous membrane lesions (prophylaxis and therapy).
The drug Actovegin was initially licensed for intravenous use to improve cellular oxygen transport to tissues in patients with arterial disease. As a gel or cream it is also used to treat slow-healing skin lesions such as burns or skin-grafted wounds. In recent years it has gained notoriety for its use by elite cyclists as a performance-enhancing drug, with the consequence that the World Anti-Doping Agency (WADA) has banned its use in competition.
Actovegin is a protein-free derivative of calf’s blood, rich in electrolytes, trace elements and various organic components. It improves tissue uptake and use of glucose and oxygen; hence it can be used to improve the oxygenation and energy supply to muscles after injury. Patients receiving Actovegin injections for muscle injury resumed full sporting activity in a clinically significant reduced timescale when compared with placebo(5). Actovegin may thus be used to accelerate the healing of muscle injuries acquired through trauma or overuse.
Actovegin® produces an organ-unrelated increase of the cellular energy metabolism. The activity is confirmed by measurement of the increased uptake and of the elevated utilization of glucose and oxygen. These two effects are coupled and they result in a rise of the ATP-turnover and thus in a greater provision of energy in the cell. In deficiency states with impairment of the normal functions of the energy metabolism (hypoxia, substrate deficiency) and in states of increased energy requirement (reparation, regeneration) Actovegin® promotes the energy-dependent processes of the functional metabolism and of the conservation metabolism. An increase of the blood supply is seen as a secondary effect
Actovegin activates metabolism in tissues. It also decreases tissue’s hypoxia , improves trophicity and stimulates the process of regeneration. Actovegin increases not only the intracellular content of glucose, but also improves oxidizing metabolism, therefore the energy of the cell is improved, the blood circulation in brain is also improved.
The drug is believed to have major endurance boosting benefits as well as being an aid to decrease recovery time from injuries and fatigued muscles. The drug has been used by cycling teams and other sports teams which compete in international competitions such as the Olympics. Nicknamed the “gas bus” by cyclist and other athletes who commonly use it, the drug is often mixed with lactic acid and caffeine and injected the morning of competition. This combination provides short, yet strong increase in endurance and power output ability.
Actovegin contains only natural physiological components such as amino acids, electrolytes (Mg, Na, Ca, P, K ),oligopeptides, nucleosides, intermediary products from fat and carbohydrare metabolism. One of the main physiologically active component in Actovegin is inositol phospho-oligosaccharides.
Actovegin contains only low molecular weight organic compounds which are below 5000 daltons.
According to its pharmacological effects, Actovegin can be attributed to the group antihypoxants and antioxidants. Anti-hypoxic action is associated with increasing the consumption of oxygen by the tissues and decreasing the demand in oxygen by the cellular structure. Actovegin also helps increase the resistance of cellular structures to hypoxia. This it its turn increases the formation of high-energy phosphates in cellular structural and leads to activation of oxidative phosphorylation enzymes. Actovegin stimulates carbohydrate and proteins synthesis and disintegration of anaerobic glycolysis. The improvement of blood flow in the microcirculatory system under the action of Actovegin is associated with normalization of endothelium-dependent reactions (vasodilatation) and decreasing peripheral vascular resistance.
Moreover, free-protein extract of calf bloods stimulates endothelial production of natural anticoagulants and antiplatelet agents that significantly helps reduce the risk of wall thrombosis.
Antioxidant effect of Actovegin is associated with the substances called superoxide dismutase as well as magnesium ions which increase the activity of glutathione synthetase. Another pharmacological effect of Actovegin consists in improving the transport of glucose in the cells due to activation of its transporters (GluT) (via increasing of oligosacharides). The action of Actovegin is insulin-independent which is clinically significant for patients with insulin-resistance.
The results of numerous studies show that Actovegin modulates the activity of intracellular glucose transport leading to intensification of lypolysis. It intensifies the speed of oxidative-restorative processes in hepatocytes, decreases ultra-structural and functional damages of mitochondria in cardiomyocytes, increases the decreased level of glucose metabolism in patients with chronic alcoholism.
Actovegin is recommended for widespread use in different branches of medicine. It is actively indicated for the prophylaxis of reperfusion in patients with heart attacks, in the treatment of different shocks, after circulatory arrest and asphyxia, in severe heart failure.
Currently, Actovegin is actively used for the treatment of cerebrovascular diseases and cognitive disorders of different severity. The preparation significantly improves mnestic functions, attention and brain work.