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Cardiology

Everything about Actovegin: what it is prescribed for and how to use it

Instructions for use of the drug

Indications: what is the medicine prescribed for?

Indications for the use of Actovegin:

  1. Metabolic and circulatory dysfunctions of the central nervous system:
    1. Acute ischemic stroke;
    2. Residual effects of hemorrhagic stroke;
    3. Consequences of craniocerebral trauma;
    4. Encephalopathy of various origins (discirculatory, hypertensive);
    5. Peripheral polyneuropathy (alcoholic, diabetic)
  2. Thermal, solar, chemical burns of I-III degree.
  3. Occlusive peripheral arterial disease in patients with contraindications to other vasoactive drugs or obvious intolerance.
  4. Chronic venous insufficiency with trophic changes in the skin.
  5. Wound healing and scarring prevention:
    1. Various etiology of ulcerative skin defects;
    2. Trophic disorders;
    3. Pressure sores;
    4. Radiation damage to the skin and mucous membranes.
  6. Dystonia of the cerebral vessels with osteochondrosis;
  7. Treatment of muscle sprains in athletes.

Composition and release forms

The composition of the drug Actovegin includes a deproteinized hemoderivat from the blood of dairy calves and excipients (sodium chloride, dextrose and water).

Forms of release of Actovegin:

  • Ready solution for intravenous or intra-arterial infusion 10%, 20%;
  • Ampoules 40 mg / ml, 2 or 5 ml for intravenous or intramuscular administration;
  • 200 mg tablets;
  • Ointment 5%;
  • Gel 20%;
  • Cream 5%.

Active ingredient: what is the mechanism of action?

The active ingredient of Actovegin is deproteinized (protein-free) hemoderivat (a substance obtained from blood) with a high degree of purification, which is obtained from dairy calves by dialysis and ultrafiltration.

Blood goes through 2 stages of purification: filtration of large molecules and titration to pH 6.4, then sterilization and complete elimination of all proteins. At the end, the agent is checked by electrophoresis for the presence of proteins and heavy molecules. Going through all the stages, the drug is deprived of large-molecular compounds, and the mass of organic substances in it does not exceed 5000 daltons.

The pharmacological properties of the obtained ultrafiltrate have only been partially studied by chemical and biological methods.

According to the results of gas and liquid chromatography and mass spectrometry, the final substance contains more than 200 biologically active molecules:

  • Amino acids;
  • Biogenic amines;
  • Sphingolipids;
  • Hexoses;
  • Eicosanoids;
  • Lactate;
  • Succinate;
  • Choline;
  • Vitamins;
  • Microelements (Magnesium, Sodium, Calcium, Phosphorus, Copper);
  • Adenosine Monophosphate (AMP);
  • Isothiolphosphooligosaccharides;
  • Acylcarnitines;
  • Phsfolipids;
  • Free fatty acids;
  • Prostaglandins;
  • Oxidized polyunsaturated fatty acids.

It is not possible to study the pharmacokinetics and pharmacodynamics of Actovegin, since the components of the drug are usually already in the human body.

But according to the manufacturer, Actovegin has a wide range of positive effects on the course of many different diseases and the body as a whole. Some of them:

  • Antihypoxic;
  • Stimulation of enzymes of oxidative phosphorylation;
  • Increasing the metabolism of phosphates (energy source);
  • Acceleration of the breakdown of lactate and β-hydroxybutyrate;
  • Normalizes pH balance;
  • Promotes the optimization of blood circulation;
  • Increases the intensity of energy-consuming processes (regeneration and repair);
  • In general, it improves tissue trophism.

But in reality, most of the above effects have not been confirmed in accordance with the parameters of evidence-based medicine, since the drug has not passed large-scale clinical trials.

Preclinical studies show the presence of substances in Actovegin that are involved in many intracellular processes and change specific metabolic pathways.

Specifications:

  1. Stimulates wound healing by activating cell growth, collagen synthesis and suppressing the processes of disintegration in the matrix.
  2. Neuroprotective effect (increasing the viability of nervous tissue in vitro).
  3. Slowing down the progress of peripheral polyneuropathy in diabetes (when removing the pancreas in rats);
  4. Optimization of glucose metabolism at the molecular level. According to research, this effect enhances energy metabolism in the brain. Also, an increase in oxygen consumption causes stabilization of cells of the central nervous system in conditions of ischemia and a decrease in the formation of lactate.

The components of Actovegin enhance the expression of GLUT1 and GLUT4 (transport proteins), which increases the permeability of the blood-brain barrier for glucose in cerebrovascular diseases.

  1. Protection of brain cells from hypoxia, improvement of cognitive processes in the cortex during age-related changes, Alzheimer's disease, vascular dementia
  2. Reduced oxidative stress. The trace elements that make up the drug activate the enzyme superoxide dismutase (converts free oxygen radicals into a neutral form).
  3. Insulin-like effect. Due to inositol phosphate oligosaccharides, intracellular glucose transport is enhanced bypassing the receptors located on the membrane. That is, the transfer of sugar into the cell occurs even under conditions of resistance, without changing the level of glycemia.
  4. Optimization of neurotransmitter metabolism in the brain due to choline and glutamate included in this medication.
  5. Improvement of enzymatic processes in the body by enhancing the formation of ATP (cellular "fuel", which is necessary for all types of life).

Also, manufacturers indicate that Actovegin helps to improve microcirculation (capillary blood flow) and metabolic activity of the endothelium of small vessels.

Thus, the action of the drug is aimed at protecting body tissues that are in a state of hypoxia or nutritional deficiency, regenerating damaged areas, and accelerating wound healing.

Multiple recommendations for the use of Actovegin in neurological practice (intensive therapy of ischemic stroke) are based on preventing oxidative damage to brain cells. With an acute lack of oxygen, the antioxidant systems malfunction and a large number of active radicals accumulate, which damage the tissues of the nervous system. The so-called oxidative stress provokes intracellular accumulation of Ca ions2+ followed by necrosis and apoptosis of nerve cells. According to the results of a study of the effectiveness of Actovegin in the acute period of stroke, it can be seen that the use of the drug in the first 6 hours can halve mortality compared to its appointment after the first day. But this study was not double-blind, placebo-controlled, which negates its results in terms of evidence-based medicine.

The promotion of Actovegin insulin-independent glucose utilization indicated its use in patients with type 2 diabetes mellitus complicated by encephalopathy and cognitive impairment. In a small group of patients, intravenous administration of large doses of the drug improved the indices of memory, vision and orientation in space and coordination. There was also a decrease in pain syndrome and a positive dynamics of sensitivity restoration in diabetic polyneuropathy.

Actovegin has practically no effect on blood pressure.The drug has a weak and unstable vasodilator effect aimed at the microvasculature. It slightly reduces the total peripheral vascular resistance and myocardial afterload. In general, its use as a basic drug for hypertensive patients is impractical.

Method of administration and dosage

Injection.

Actovegin in ampoules is used intravenously (including drip) or intra-aortic.

The dose of the drug is calculated depending on the severity of the clinical condition.

The ready-made solution for intravenous administration is used at a dose of 250 ml per day (if necessary, the initial dose is increased to 500 ml). The injection rate is 2-3 ml / minute. Mixing several drugs in one bottle is prohibited.

It is recommended to dilute the contents of ampoules for intravenous injection with saline or 5% glucose.

Schemes of drug therapy for various diseases:

  1. Circulatory disorders in the brain:
    1. Intravenous administration of 250-500 ml for 14 days, then 250 ml several times a week - 1-2 months.
  2. Ischemic stroke.
    1. Injection administration of 250-500 ml of solution daily, in a course of 2-3 weeks.
    2. Then 2-3 tablets 3 times a day for 4-6 weeks.
  3. Arterial angiopathy.
    1. 250 ml of Actovegin intravenously every day or 3-4 times a week for a month.
  4. Trophic and other ulcers, bedsores.
    1. 250 ml of solution daily.
    2. Additionally, 20% gel on the affected area 3-4 times a day.
    3. As the healing progresses, it is recommended to switch to a 5% cream or ointment, apply 2-3 times a day until complete remission.
  5. Diabetic polyneuropathy.
    1. Intravenous administration of Actovegin 2000 mg per day for 3 weeks.
    2. Further, the transition to a tablet form - 2-3 tons. 3 times a day with a course of 4-5 months.
  6. Diseases of the gastrointestinal tract (chronic gastritis, gastric ulcer and duodenal ulcer):
    1. Intramuscular or intravenous administration of 2 grams of the drug per day for 14 days.
    2. Then 1-2 tablets 3 times a day for a course of 4-6 weeks.
  7. Radiation skin lesions (in oncology):
    1. Applications and dressings with 20% gel to the affected areas 3-4 times a day for 2-3 weeks.

Instructions for the use of Actovegin tablets recommend dosing the drug 1-2 times a day for 1 month.

The composition contains substances of animal origin, which can cause allergic reactions in patients prone to atopy. It is recommended to conduct an intradermal sensitivity test before using the drug.

Side effects

Due to the lack of large-scale clinical trials, there is no comprehensive data on all possible reactions to the use of Actovegin.

Side effects described in the annotation:

  • Allergic reactions (urticaria, anaphylaxis, pruritus, polymorphic erythema, angioedema);
  • Increased body temperature, skin hyperemia;
  • Fluctuations in blood pressure, palpitations, dizziness;
  • Headaches, general weakness.

If the above reactions occur, the administration of Actovegin is discontinued. Side effect therapy is symptomatic.

Contraindications

Actovegin is contraindicated for:

  • Hypersensitivity to the components of the drug;
  • Decompensation of heart failure;
  • Cardiogenic pulmonary edema;
  • Terminal renal failure (oliguric and anuric stages);
  • Overhydration;
  • Atopic reactions and allergy to cow's milk protein;

There is also no reliable data on the safety of using Actovegin during pregnancy and lactation. It is worth carefully weighing the benefits of the drug against the possible risk to the fetus.

The use of Actovegin in children is not recommended due to the lack of an evidence base.

The drug is not compatible with alcohol, according to some reports, their simultaneous use leads to the accumulation of Actovegin in the body, potentiation of the anticoagulant effect and an increase in the risk of side effects.

Storage conditions

The components of Actovegin are capable of being destroyed by sunlight. Therefore, the drug should be stored in a cool, dark place, protected from children (in the refrigerator).

Excretion from the body

It is impossible to study the pharmacokinetic parameters of Actovegin:

  • Absorption from the intestine and the effect of food on the absorption of the drug;
  • Bioavailability;
  • Distribution in the body;
  • Half-life;
  • The possibility of accumulation in tissues and organs;
  • Elimination pathways;
  • Compatibility and interaction with other medications.

The manufacturer explains this nuance by the fact that the drug consists exclusively of physiological components that are already present in the human body.

When studied on animals, it was found that Actovegin begins to act in 10-30 minutes from administration and retains the effect for 3 hours.

Analogues and cheap substitutes

The only generic (non-proprietary analogue) of Actovegin is Solcoseryl (the same active ingredient and indications for use and almost the same cost of 600-1700 rubles, depending on the form of drug release).

Actovegin is produced in Austria at the branch of the Swiss pharmaceutical company Nykomed, and Solcoseryl in Germany. The drugs are made from the blood of Austrian and German calves, but in no Western European country is this medicine allowed not only for use, but also for sale.

It is also worth remembering that cattle are susceptible to the incidence of so-called slow prion infections (including mad cow disease, to which a person is susceptible). The pathogen can enter the body with parenteral administration of the drug; it is stable to high temperatures and antiseptics. Prion infection is slow (the incubation period can be up to 8 years), and clinical manifestations are masked by other diseases. A case of release of a batch of Actovegin from raw materials that did not undergo appropriate control was registered.

Conditional analogues of Actovegin on the Russian market:

  • Cerebrolysin;
  • Cortexin;
  • Mildronate;
  • Mexidol.

Conclusions

At the moment, Actovegin has not passed a single study according to the rules of the GHP (international code of good medical practice, which guides scientists in conducting clinical trials). But at the same time, the company, the manufacturer of the medication, does not set such a goal, since a solid evidence base is not required for the main fish to be sold on the shelves (CIS countries).

According to the study of case histories of patients with hypertension, who stayed in a hospital, it was revealed that the percentage of money spent on Actovegin treatment averaged 17% of the total amount. This is an irrational spending on a drug without an evidence base for hypertension, concomitant conditions, and its inclusion in the prescription lists is inappropriate.

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