Actovegin^® (Tablets, Solution) Instructions for Use

ATC Code

B06AB (Other blood preparations)

Active Substance

Deproteinized calf blood haemoderivate

Clinical-Pharmacological Group

Drug that activates tissue metabolism, improves trophism and stimulates the regeneration process

Pharmacotherapeutic Group

Tissue regeneration stimulant

Pharmacological Action

Antihypoxant with three types of effects: metabolic, neuroprotective and microcirculatory.

It increases the uptake and utilization of oxygen; the inositol phospho-oligosaccharides contained in the preparation have a positive effect on the transport and utilization of glucose, which leads to an improvement in the energy metabolism of cells and a reduction in lactate formation under ischemic conditions.

Several pathways for the realization of the neuroprotective mechanism of action of the drug are considered.

It prevents the development of apoptosis induced by beta-amyloid (Aβ25-35).

It modulates the activity of nuclear factor kappa B (NF-kB), which plays an important role in the regulation of apoptosis and inflammation processes in the central and peripheral nervous system.

Another mechanism of action is associated with the nuclear enzyme poly(ADP-ribose) polymerase (PARP).

PARP plays an important role in the detection and repair of single-stranded DNA damage, but excessive activation of the enzyme can trigger cell death processes in conditions such as cerebrovascular diseases and diabetic polyneuropathy.

It inhibits PARP activity, leading to functional and morphological improvement of the central and peripheral nervous system.

The positive effects of this agent on microcirculation and endothelium include an increase in the capillary blood flow rate, a reduction in the pericapillary zone, a decrease in the myogenic tone of precapillary arterioles and capillary sphincters, a reduction in the degree of arteriolo-venular shunting with predominant blood circulation in the capillary bed, and stimulation of the function of endothelial nitric oxide synthase, which affects the microcirculatory bed.

Various studies have established that the effect of this agent occurs no later than 30 minutes after its administration.

The maximum effect is noted 3 hours after parenteral and 2-6 hours after oral administration.

Pharmacokinetics

It is impossible to study the pharmacokinetic parameters of the active substance using pharmacokinetic methods because it consists only of physiological components that are normally present in the body.

Indications

As part of complex therapy

• Cognitive impairments, including post-stroke cognitive impairments and dementia;
• Peripheral circulation disorders and their consequences;
• Diabetic polyneuropathy.

ICD codes

Dosage Regimen

Tablets

The drug is taken orally before meals.

The tablet should not be chewed and should be swallowed with a small amount of liquid.

In the acute period of ischemic stroke (starting from day 5-7) – 2000 mg/day IV drip up to 20 infusions with a switch to the tablet form of 2 tablets 3 times/day (1200 mg/day). The total duration of treatment is 6 months.

For dementia – 2 tablets 3 times/day (1200 mg/day). The total duration of treatment is 20 weeks.

For peripheral circulation disorders and their consequences – 1-2 tablets 3 times/day (600-1200 mg/day). The duration of treatment is from 4 to 6 weeks.

For diabetic polyneuropathy – 2000 mg/day IV drip 20 infusions with a switch to the tablet form of 3 tablets 3 times/day (1800 mg/day). The duration of treatment is from 4 to 5 months.

Solution

Intra-arterial, intravenous (including as infusion) and intramuscular.

Depending on the severity of the clinical picture, initially 10-20 ml should be administered IV or IA daily; then – 5 ml IV or IM slowly, daily or several times a week.

For infusion administration, from 10 to 50 ml of the solution containing this active substance should be added to 200-300 ml of the base solution (isotonic sodium chloride solution or 5% glucose solution). The infusion rate is about 2 ml/min.

For IM injections, use no more than 5 ml of the solution, which should be administered slowly because the solution is hypertonic.

In the acute period of ischemic stroke (starting from day 5-7) – 2000 mg/day IV drip up to 20 infusions with a switch to oral administration in the appropriate dosage form at a dose of 1200 mg/day in 3 divided doses. The total duration of treatment is 6 months.

For dementia – 2000 mg/day IV drip. The duration of treatment is up to 4 weeks.

For peripheral circulation disorders and their consequences – 800-2000 mg/day IA or IV drip. The duration of treatment is up to 4 weeks.

For diabetic polyneuropathy – 2000 mg/day IV drip 20 infusions with a switch to oral administration in the appropriate dosage form at a dose of 1800 mg/day in 3 divided doses. The duration of treatment is from 4 to 5 months.

Instructions for using ampoules with a break point

Position the ampoule tip pointing upwards.

Gently tap and shake the ampoule to allow the solution from the tip to flow down.

Holding the ampoule in one hand with the tip pointing upwards, use the other hand to break off the ampoule tip at the break point.

Adverse Reactions

The frequency of side effects was determined in accordance with the classification of the Council for International Organizations of Medical Sciences (CIOMS): very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10000 to <1/1000); very rare (<1/10000); frequency not known (cannot be estimated from the available data).

Immune system disorders rare – allergic reactions (drug fever, shock symptoms).

Skin and subcutaneous tissue disorders rare – urticaria, sudden redness.

Musculoskeletal and connective tissue disorders frequency not known – myalgia.

Contraindications

• Hypersensitivity to this agent, similar drugs, excipients that may be part of the used dosage form;
• Decompensated heart failure;
• Pulmonary edema;
• Oliguria, anuria;
• Fluid retention in the body;
• Children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

Use during pregnancy and lactation only in cases where the therapeutic benefit outweighs the potential risk to the fetus or child.

Use in Renal Impairment

Contraindicated in oliguria, anuria.

Pediatric Use

Use in children and adolescents under 18 years of age is contraindicated.

Special Precautions

Parenteral administration should be carried out under sterile conditions.

Due to the possibility of an anaphylactic reaction, a test injection (hypersensitivity test) is recommended.

In case of electrolyte disorders (such as hyperchloremia and hypernatremia), these conditions must be appropriately corrected.

Use in pediatrics

Currently, use in children and adolescents has not been studied, therefore use in this category of patients is not recommended.

Effect on ability to drive vehicles and operate machinery

Not established.

Drug Interactions

Drug interactions of this agent are currently unknown.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.