Description
Actovegin 200 mg (40mg/ml), 5 ml. – 5 ampoules
Description of Actovegin:
Each milliliter (ml) of Actovegin contains 40.0 mg of deproteinized hemoderivate of calf blood (in terms of dry matter). The excipient used is water for injection. It should be noted that approximately 26.8 mg of sodium chloride is present in each dosage.
Pharmacokinetics:
Actovegin exhibits an antihypoxic effect, which becomes evident within 30 minutes of parenteral administration. The maximum effect is observed 3 hours after parenteral administration and 2-6 hours after oral administration.
Pharmacodynamics:
Actovegin is a gemoderivate obtained through dialysis and ultrafiltration, allowing compounds with a molecular weight of less than 5000 daltons to pass through. It acts as an antihypoxant and exhibits three types of effects: metabolic, neuroprotective, and microcirculatory.
Actovegin enhances the uptake and utilization of oxygen. The phospho-oligosaccharides found in the preparation, particularly inositol, positively affect the transport and utilization of glucose. This leads to an improvement in cellular energy metabolism and a reduction in lactate formation under ischemic conditions. The activity of Actovegin has been confirmed through increased absorption and utilization of glucose and oxygen.
The neuroprotective mechanism of Actovegin involves multiple pathways. It prevents the development of apoptosis induced by the beta-amyloid peptide (Aβ25-35). It also modulates the activity of nuclear factor kappa B (NF-kB), which regulates apoptosis and inflammation in the central and peripheral nervous systems.
Another mechanism of action involves the nuclear enzyme poly (ADP-ribose) polymerase (PARP). While PARP is crucial for detecting and repairing single-stranded DNA damage, excessive activation of the enzyme can lead to cell death in conditions such as cerebrovascular disease and diabetic polyneuropathy. Actovegin inhibits the activity of PARP, resulting in functional and morphological improvement in the central and peripheral nervous systems.
Actovegin’s positive effects on microcirculation and the endothelium include increased capillary blood flow rate, reduced pericapillary zone, and decreased myogenic tone of precapillary arterioles and capillary sphincters.
In various studies, Actovegin has shown its effects within 30 minutes of administration. The maximum effect is observed 3 hours after parenteral administration and 2-6 hours after oral administration.
The effects of Actovegin on oxygen uptake, utilization, and its insulin-like activity with stimulation of glucose transport and oxidation are significant in the treatment of diabetic polyneuropathy (DPN).
In patients with diabetes mellitus and diabetic polyneuropathy, Actovegin significantly reduces symptoms such as stabbing pain, burning sensation, paresthesia, and numbness in the lower extremities. Sensory disorders are objectively reduced, leading to improved mental well-being in patients.
Special Instructions:
It is important to administer the drug through parenteral (injection) route under sterile conditions.
To minimize the risk of an anaphylactic reaction, it is recommended to perform a test injection (hypersensitivity test) beforehand.
If there are electrolyte disorders like hyperchloremia and hypernatremia, appropriate adjustments should be made.
The injection solution may have a slightly yellowish color, which can vary between batches due to the characteristics of the starting materials. However, this color variation does not affect the effectiveness or tolerability of the drug.
Do not use the solution if it is opaque or contains particles.
Once the ampoule is opened, the solution should not be stored.
Clinical Data:
In a multicenter, randomized, double-blind, placebo-controlled study called ARTEMIDA (NCT01582854), which involved 503 patients with ischemic stroke, Actovegin’s therapeutic effect on cognitive impairment was investigated. The incidence of serious adverse events and mortality was similar in both treatment groups. While the frequency of recurrent ischemic strokes was expected in this patient population, there were slightly more cases in the Actovegin group compared to the placebo group, but this difference was not statistically significant. No conclusive evidence was found to establish a direct link between recurrent stroke events and the study drug.
Use in Pediatric Patients:
Currently, there is a lack of data on the use of Actovegin in children, so its administration is not recommended for this age group.
Influence on Driving and Operating Machinery
No specific effects on driving or operating machinery have been established.
Use during Pregnancy and Lactation:
Actovegin should only be used during pregnancy and lactation if the potential therapeutic benefits outweigh the potential risks to the fetus or child.
