Immunomodulator Trekrezan: profile of general and immunotropic activity


The drug trekrezan, the price of which is affordable, is an immunomodulatory agent. It has pronounced adaptogenic properties and allows you to resist various external negative factors that provoke stress for the body. Due to the similarity of the names, trekrezan and triclosan should not be confused. These are different medications.

Content

  • 1 Trecrezan 1.1 Mechanism of action
  • 1.2 Indications for use
  • 1.3 Side effects
  • 2 Research
      2.1 Immunopoiesis and erythropoiesis
  • 2.2 Immunoactive properties of trekrezan
  • 2.3 Pharmacological activity and clinical effects
  • 2.4 Trecresan: Inhibitor of acid cholesterol esterase synthesis in platelets and monocytes
  • 2.5 Effect of trekrezan on immunogenesis under experimental conditions
  • 2.6 Comparative study of the properties of trekrezan and polyoxidone regarding energy stabilization and immunotropism in a bronchopulmonary model of inflammation in rats
  • 2.7 Efficacy of trekrezan in experimental bronchopneumonia in rats
  • 2.8 Functional and metabolic changes in healthy volunteers after cold exposure and administration of the meteoadaptogen trekrezan
  • 2.9 Metabolic effects of Trecresan during rat adaptation to intermittent hypoxic hypoxia
  • 2.10 Cresatin – stimulator of liver cell regeneration activity
  • 2.11 Effect of trekrezan on lipid peroxidation in patients with chronic heart failure
  • 3
  • Trekrezan[edit | edit code]

    Trekrezan (0.2 g tablets)
    Trekrezan

    (Krezacin, Irkutin) is a synthetic adaptogen and immunostimulant, the active ingredient is
    hydroxyethylammonium methylphenoxyacetate
    . The drug is a continuation of the domestic pharmacological school, associated with the creation of numerous adaptogenic drugs (for example, dibazol), which have never received international recognition. Most of the studies on trekrezan have a weak design and were carried out only in Russia by interested people. The effectiveness of the drug is extremely doubtful, as is the case with other domestic interferon inducers such as Anaferon, Arbidol, Kagocel, Amiksin. The use of trekrezan in sports is also unfounded.

    The oxyethylammonium methylphenoxyacetate molecule is structurally similar to some biological molecules of the human body and plants: choline, lecithin, heteroauxin and has hydrophilic and lipophilic properties.

    Mechanism of action[edit | edit code]

    Trecrezan stimulates the production of α- and γ-interferons, helps to increase and correct the body’s immune status by activating cellular and humoral immunity, and stimulates the phagocytic activity of macrophages.

    Hydroxyethylammonium methylphenoxyacetate was synthesized in 1972 by Professor M.G. Voronkov and his group of scientists at the Irkutsk Institute of Organic Chemistry. Experiments have shown that the new substance is similar in action to herbal and natural adaptogenic agents.

    Indications for use[edit | edit code]

    A remedy for almost all diseases:

    • Immunodeficiency
    • To improve performance
    • Infections
    • Stress Prevention
    • Radiation sickness
    • Cardiopsychoneurosis
    • Multiple sclerosis
    • Cardiac pathology
    • Infertility
    • Oncological diseases

    Side effects[edit | edit code]

    With the exception of rare cases of intolerance, there are no side effects.

    Peculiarities

    Trekrezan is produced in the form of white flat-cylindrical tablets in contour packages. Sometimes they can be yellowish-brown.

    The active ingredient of the same name in the drug, which also has another name - oxyethylammonium methylphenoxyacetate, increases the production of alpha and gamma interfenrons. This increases endurance under conditions of great physical or mental stress. The active substance reduces the effects of toxins on the body. It stabilizes the condition during oxygen starvation, when exposed to low and high temperatures, etc.

    Research[edit | edit code]

    Immunopoiesis and erythropoiesis[edit | edit code]

    The effect of the drug trecrezan was studied in (C57BL/6 x DBA/2) F1 mice with immunodeficiency and anemia syndrome caused by chronic guest-versus-host reaction. The drug combines immuno- and erythromodulatory properties, is able to eliminate anemia, reduce the number of erythrokaryocytes and BFUs in the bone marrow of sick mice, and normalize the primary humoral immune response [1].

    Immunoactive properties of trekrezan[edit | edit code]

    It has been shown [2] that under natural conditions, trekrezan exhibits powerful immunoactive properties: it reduces the formation of spots by pluripotent blood stem cells, stimulates lympho- and hematopoiesis, the formation of antibodies, and exhibits sustained anti-inflammatory activity. The drug stimulated in vitro mononuclear cell proliferation in humans due to its direct effect on B lymphocytes and increased production of lymphokines and monokines.

    Pharmacological activity and clinical effects[edit | edit code]

    Experimental and clinical research[3] has been carried out on the pharmacological properties of new compounds representing tris-(2-hydroxyethyl) ammonium salts (TES) of arylheteroacetic acids, in particular, tris(2-hydroxyethyl) ammonium-2-methylphenoxyacetate (trecresan). Trecrezan exhibits modulating effects on immunity and hematopoiesis and offers a promising approach to immune correction for the treatment of immune deficiency and autoimmune disorders. Restoring the proliferative activity of early erythropoiesis precursors using trekrezan (experimental model) leads to normalization of immunity and hematopoiesis. Trecrezan was developed for the complex treatment of acute viral hepatitis B, as well as hepatitis A and B, complicated by a work history. Trecrezan has also been successfully used for the complex treatment of coronary heart disease and multiple sclerosis. Trecrezan stimulates the regeneration of hepatocytes during partial hepatectomy and acts as an effective adjuvant in the complex therapy of tuberculosis. Analogs of Trecresan (TES) demonstrate antitumor, hepatoprotective and adaptive effects, increase the resistance of animals to oxygen deficiency and poisoning with salts of heavy metals and organophosphorus compounds, and also improve the endurance of animals during physical activity and emotional stressful situations.

    Trecrezan: Inhibitor of acid cholesterol esterase synthesis in platelets and monocytes[edit | edit code]

    It was found [4] that the use of the domestic drug trekresan for the treatment of atherosclerosis in experimental rabbits led to a decrease in the level of cholesterol and total lipids in platelets (Tc) and monocytes (Mc) in the blood. The results of enzymatic analysis showed that the development of atherosclerosis was accompanied by an increase in the activity of acid cholesterol esterase by 64% in Mc and by 22.7% in Tc compared to the standard. Intramuscular administration of trekrezan (25 mg/kg) significantly reduced acid cholesterol esterase activity by 35% in MS and 26% in Tc compared to control.

    The influence of trekrezan on immunogenesis under experimental conditions[edit | edit code]

    The dynamics of immune reactions to trecrezan in mice were studied [5] after vaccination of adult mice during pregnancy and mice at different times after birth with Salmonella Typhimurium 34-96. The drug modulated the activity of the immune system and stimulated the production of antibodies in the pre- and postpartum period.

    Comparative study of the properties of trekrezan and polyoxidone regarding energy stabilization and immunotropism in a bronchopulmonary model of inflammation in rats[edit | edit code]

    The energy stabilizing effects and immunotropic properties of the immunomodulators trekrezan (25 mg/kg) and polyoxidone (0.75 mg/kg) were compared[6] in rats with a model of bronchopulmonary inflammation caused by the introduction of turpentine into the trachea. Both drugs exhibited an energy stabilizing effect, which was manifested in a decrease in the level of lactate and hydrolysis products ATP-ADP and AMP and an increase in the level of pyruvate and ATP in blood lymphocytes and lung tissue. The energy-stabilizing effect of polyoxidone was more pronounced in lung tissue. The effect of this drug was generally the same, but less pronounced, than that of Trecrezan. Parallel experiments showed that trekrezan and polyoxidone normalized the immune status of lymphocytes in rats with a model of acute bronchopulmonary inflammation.

    The effectiveness of trekrezan in experimental bronchopneumonia in rats[edit | edit code]

    Trekrezan at a dose of 25 mg/kg normalizes the immune status of lymphocytes and produces an energy-stabilizing effect, which is manifested in a decrease in the levels of lactate, ADP and AMP and an increase in the content of pyruvate and ATP in the lymphocytes of the blood and lung tissue of rats with experimental acute bronchopneumonia [7].

    Functional and metabolic changes in healthy volunteers after cold exposure and administration of the meteoadaptogen trekresan[edit | edit code]

    The effect of exposure to cold (-10 degrees C, air speed -2.5 m/sec, 40 minutes) on physical activity, cognitive processes and metabolic status of 75 volunteers, healthy men 20-24 years old, was studied in the Tabaj thermobarocomplex (Japan) [8]. Cold exposure decreased physical and cognitive performance, creatine phosphokinase activity, superoxide dismutase activity, and redox glutathione and pyruvate levels. Preliminary administration of the adaptogenic drug trecrezan at a dose of 0.2 g before cold exposure normalized the indicators of the studied physical activity and metabolic status. It is assumed that trekrezan can be used as a meteoadaptogenic drug for rapid and effective adaptation to cold.

    Metabolic effects of Trecrezan during rat adaptation to intermittent hypoxic hypoxia[edit | edit code]

    The animals were adapted to intermittent hypoxic hypoxia in a pressure flow chamber for 3 days[9]. Each one-day training session consisted of 4 ascents to an altitude of 6000 m for 20 minutes (15 m/sec, at 20-minute intervals). Trecresan (25 mg/kg i.p.) was administered immediately after completion of daily exercise for 3 days. The drug has been shown to increase the degree of adaptive metabolic changes in the brain, heart and liver of rats during adaptation to hypoxic hypoxia.

    Cresatin is a stimulator of liver cell regeneration activity[edit | edit code]

    In experiments with partial hepatectomy in rats[10], it was shown that the use of krezacin potentiates the processes of regeneration of hepatocytes, increasing high-energy compounds in them, and also accelerates some stages of the mitotic cycle. These processes occur along with inhibition of lipid peroxidation in hepatocytes, a decrease in the rate of transmembrane oxygen transport in mitochondria, and a decrease in the amount of cytochrome oxidase. It was concluded that kresacin directly stimulates various parts of the metabolic pathway.

    The effect of trekrezan on lipid peroxidation in patients with chronic heart failure[edit | edit code]

    The antioxidant properties of krezacin were studied[11] in a model of galactosamine hepatitis and in isolated liver cells of white male rats. Kresacin at a dose of 20 mg/kg has been shown to effectively inhibit hepatotoxin-induced lipid peroxidation. Krezacin also normalized some components of the enzymatic and non-enzymatic antioxidant system. In particular, the activity indices of superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, and the level of reduced glutathione, total phospholipids and ascorbic acid increased. In vitro, on isolated hepatocytes, krezacin showed a dose-dependent antioxidant effect. This fact confirms its ability to inhibit the rate of formation of malondialdehyde in the incubation medium.

    Recommendations for use

    The dosage of trekrezan for the treatment of various pathologies may be different. When a medicine is prescribed during the season of infection for preventive purposes to minimize the risks of acute respiratory viral infections, the recommended dose is 1 tablet per day after meals. Duration of treatment is two weeks.

    When using trecrezan, it is possible to increase the effectiveness of complex treatment of ARVI. In this case, the product should be taken for 8 days in accordance with the regimen specified in the instructions for use. Namely:

    • On the first day, take 1 tablet in the morning, lunch and evening.
    • In the next week - 1 tablet per day.

    A similar dosage is also recommended to support the body in other cases:

    • During periods of increased intellectual or physical stress.
    • Under stressful external influences.

    You should also pay attention to other recommendations for using the product specified in the instructions. It is important to understand that the medication has a complex effect on the patient’s body. Therefore, the doctor can select the most appropriate dosage and duration of treatment based on the patient’s condition. Improper use of Trekrezan can lead to unpleasant consequences.

    If the condition does not improve within three days while taking the drug, and the symptoms become more pronounced, then you should inform your doctor. It should also be understood that after the course of treatment, the break before re-using the drug should be at least a month.

    Sources[edit | edit code]

    1. Sukhenko TG1, Kolesnikova OP, Kozlov VA.Immunopoiesis- and erythropoiesis-modulating properties of trecresan in experimental immune deficiency. PMID: 11589109
    2. Shirinskiĭ VS, Kolesnikova OP, Kudaeva OT, Semenova NV, Zhuk EA, Mirskova AN, Tuzova MN, Sukhenko TG, Voronkov MG, Kozlov VA. The immunoactive properties of trekrezan. PMID: 8219991
    3. MG Voronkov, OP Kolesnikova, MM Rasulov, AN Mirskova. Pharmacological activity and clinical effects of trecrezan and other tris-(2-hydroxyethyl)ammonium salts of arylheteroacetic acids (A review). Pharmaceutical Chemistry Journal. May 2007, Volume 41, Issue 5, pp. 244-248. Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 41, No. 5, pp. 13–17, May, 2007.
    4. Rasulov, MM, Bobkova, SN, Belikova, OA et al. Pharm Chem J (2012) 46: 523. doi:10.1007/s11094-012-0838-5
    5. Voronkov MG1, Pavel YG, Karus AL, Kumar YA, Shattshneider TK, Myuirsepp EY, Pavel KhY, Poverina E, Rasulov MM. Effect of trekrezan on immunogenesis under experimental conditions. PMID: 15662463
    6. Zarubina IV, Bolekhan AV, Shabanov PD. Comparative study of the energy-stabilizing and immunotropic properties of trekrezan and polyoxidon on a bronchopulmonary inflammation model in rats. PMID: 17153967
    7. Zarubina IV, Bolekhan AV, Shabanov PD. Efficiency of trekrezan in experimental bronchopneumonia in rats. Bull Exp Biol Med. 2006 Aug;142(2):205-8. PMID: 17369940
    8. Zarubina IV, Ganapol'skiĭ VP, Shabanov PD. Functional and metabolic changes of healthy volunteers after cold exposure and administration of meteoadaptogen trekrezan. Ross Fiziol Zh Im IM Sechenova. 2008 Jan;94(1):62-7. PMID: 18383733
    9. Zarubina. Metabolic effects of Trekrezan during adaptation of rats to intermittent hypoxic hypoxia. Bull Exp Biol Med. 2008 Jan;145(1):47-50. PMID: 19024000
    10. Rasulov MM, Kuznetsov IG, Belousov AA, Zabozlaev AG, Khvylia SI, Voronkov MG. Krezatsin – a stimulant of the activity of regenerating liver cells. PMID: 8471975
    11. Sabadyshin RO, Slipak OIa, Koval'chuk SF, D'iakov VM, Kazimirovskaia VB. Effect of trekrezan on the lipid peroxidation in patients with chronic cardiac insufficiency. Ukr Biokhim Zh (1978). 1998 Jan-Feb;70(1):63-8. PMID: 9777233
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