Method of treating experimental myocardial infarction in rats

FIELD: medicine.

SUBSTANCE: for treating experimental myocardial infarction in rats, after modeling myocardial infarction, L-17 compound of 1,3,4-thiadiazine class is injected intravenously.

EFFECT: effective treatment ensured by ability of said compound to reduce an inflammation, to intensify a fibroplastic reaction and vascularisation.

2 cl

 

The invention relates to experimental medicine, namely to the experimental form of myocardial infarction, and can be used for modeling myocardial infarction with subsequent drug exposure for monitoring its effectiveness.

Myocardial infarction is one of the most frequent forms of diseases and is 3.9% among males and 2.2% among women, which puts it on one of the first places in the world. In Russia from myocardial infarction die 330 men and 154 women per 100 thousand population, which is 3.2 times more than in the US. These circumstances indicate a high relevance of the problem to THEM, in particular his treatment.

The Recommendations of the working group of the European society of Cardiology (2000) and based on them the Russian Recommendations (2001) the treatment of the developed myocardial infarction is based on the use of beta-blockers, nitrates, calcium antagonists and antiplatelet agents (aspirin, thienopyridine, antagonists of glycoprotein IIb/IIIA receptor of platelets). Despite the large number of different surgical and conservative methods of treatment, mortality in acute myocardial infarction continues to be high: early complications lead to 10-15% of hospital mortality.

The main causes of fatal outcome is the development of heart not is dostatochnosti and disorders of rhythm and conduction, due primarily to the value of developing myocardial infarction and progressive involvement in the process of intact cells of the myocardium. High mortality dictates the need to develop new treatments for this debilitating disease that would prevent the development or reduced the severity of these complications of myocardial infarction.

Modeling of acute myocardial infarction in rats, in our opinion, is the most reasonable, because these laboratory animals are similar to humans during physiological and pathological processes, which allows to use the results of animal studies to develop new methods of treatment of this disease in humans.

Known for the treatment of myocardial infarction drug atenolol, which has a complex mechanism of action: blocks beta-1-adrenergic receptors, which decreases the stimulating effect on the heart sympathetic innervation and circulating in the blood catecholamines, has antianginal, hypotensive and antiarrhythmic effect.

Introduction: a basic introduction is given intravenously in a dose of 5 mg over 5 min 5 mg, then after 1 h begins taking the drug inside of 50-100 mg per day.

Disadvantage: the drug is contraindicated in bronchial obstructive syndrome, syndrome, sick sinus, AV-block is hell and congestive heart failure; reliable performance in ischemia of repeated heart attacks and reducing mortality appears only in long-term care (about 2 years).

Source:

1. Selected topics in internal medicine. Ekaterinburg, 2007, volume 4, p.101-172.

2. Drugs in Russia: a Handbook. M: Attraversare, 2003, p.3-1104.

Known PCT patent RF №2259371 (27.08.2005). The invention relates to the field of biologically active compounds, in particular substituted 5R1, 6R2-thiadiazin-2-amines containing pharmaceutical compositions, which can be used in medicine as a potential pharmacologically active substances. The action of these substances differs from that currently used in medical practice drugs. Disadvantage: not studied the effect in the acute phase of myocardial infarction.

Known drug acetylsalicylic acid, which is included in international and national recommendations for the treatment of myocardial infarction PROTOTYPE.

Acetylsalicylic acid inhibits the activity of COX - the main enzyme of arachidonic acid metabolism, which is a precursor of prostaglandins, which provides anti-inflammatory, analgesic and antipyretic effects, and inhibits formation of THE, thereby inhibiting platelet aggregation.

Its positive side: the ri long-term use (at least 2 years) reduces the frequency of repeated heart attacks.

Negative sides: the drug is contraindicated in peptic ulcers, local bleeding, hemorrhagic diathesis; 40% of patients do not manifest antiaggregatory effect, considered to be the basic element protivoinfektsionnogo of action of the drug.

Source:

3. Selected topics in internal medicine. Ekaterinburg, 2007, volume 4, p.101-172.

4. Drugs in Russia: a Handbook. M: Attraversare, 2003, p.3-1104.

An object of the invention is to increase the effectiveness of treatment of myocardial infarction is more likely to cure.

To solve this problem is proposed correction method of the acute phase of the syndrome of systemic inflammatory response in experimental myocardial infarction, based on modeling of myocardial infarction with subsequent medical intervention, characterized in that the running intravenous connection L-17 from the class 1,3,4-thiadiazines at a dose of 40 mg/kg after creating a model of myocardial infarction with subsequent study of indicators of cytolytic syndrome - transaminase and histological studies of myocardial tissue. Connection L-17, influencing the nature of the acute inflammatory reaction (reducing intake of neutrophilic leukocytes that produce factors that stimulate inflammation), corrects for acute f the threat of myocardial infarction, which leads to a decrease in the intensity of leukocyte reactions, stimulates migration immunocompetent cells - lymphocytes, plasma cells, mast cells, macrophages in the necrotic foci, accelerates the formation of granulation tissue with proliferation of fibroblastic cells number and calls the substitution necrosis scar tissue, represented by the active fibroblasts and fibrous structures.

The treatment is as follows.

Is intravenous connection L-17 from the class 1,3,4-thiadiazines at a dose of 40 mg/kg after creating a model of myocardial infarction with subsequent study of indicators of cytolytic syndrome - transaminase and histological examination of tissue infarction within 7 days.

Influencing the nature of the acute inflammatory response, reducing the flow of neutrophilic leukocytes that produce factors that stimulate inflammation, the compound L-17 from the class 1,3,4-thiadiazines at a dose of 40 mg/kg corrects for the acute phase of the syndrome of systemic inflammatory response, which leads to a decrease in the expression of leukocyte reactions, stimulates migration immunocompetent cells-lymphocytes, plasma cells, mast cells, macrophages in the necrotic foci, accelerates the formation of granulation tissue with proliferation of cells fibroblastic the ski range and causes the substitution zone of necrosis, scar tissue, presents active fibroblasts and fibrous structures, without the effects of purulent inflammation of scar tissue.

Tracked action connection L-17 during acute phase of experimental myocardial infarction in 50 cases. The experimental results.

On the first day of myocardial infarction without the introduction of the drug was observed pronounced dystrophic reaction with stromal edema, loss of transverse and longitudinal iscertainly myofibrils, and in the future - grained and glycated decay.

Areas adjacent to the area of infarction, were subject to significant changes and expressed partial atrophy of myocardiocytes and structural changes similar to those in the zone of necrosis, until dystrophic and necrobiotic changes in individual muscle fibers and their groups, kalinovaya in the wall of the left ventricle (in most cases transmural) was represented by cardiomyocytes events karyolysis, plasmolysis and plasmolysis. Showed moderate diffuse infiltration segmented by leukocytes without forming the demarcation zone. In adjacent structures was observed phenomenon of swelling, the plethora of vessels Indonesia with the formation of the sludge systems.

On the first day of myocardial infarction with drug area of necrosis, also lokalizovalsya in the wall of levov the ventricle (mainly subepicardial), was represented by cardiomyocytes events karyolysis, plasmolysis and plasmolysis. Demarcation another area is not formed. In the infiltrate appear in a small number of lymphocytes (immunocompetent cells). Infiltration necrosis minimum

On the fifth day of myocardial infarction without injection area of infarction was defined as mainly transmural. The necrotic cardiomyocytes were surrounded demarcation shaft, showed signs of formation of granulation tissue, fibroblasts appear, emocapella. In adjacent structures were detected distribution of infiltration on Indonesia

On the fifth day of myocardial infarction with drug area damage replaced by granulation tissue, represented by fibroblasts, thin collagen fibers and numerous sinusoidal capillaries. Granulation tissue was infiltrated by lymphocytes, macrophages. Polymorphonuclear leukocytes were isolated.

On the seventh day of myocardial infarction without injection area of necrosis in the wall of the left ventricle in 100% of cases were characterized as transmural. Histological signs of stage (formation of granulation tissue at the edges of the zone of necrosis with a large number of fibroblasts and macrophages, sinusoidal gemok jetty is illaroo, substitute the affected area) when the continuing disintegration of muscle cells and the continuing infiltration of the myocardium by lymphocyte and segmented by leukocytes. In some cases the vessels was determined by the boundary distance of cells with signs of leukodepleted.

On the seventh day of myocardial infarction with drug area of necrosis was completely replaced by granulation tissue, which is determined by numerous emocapella sinusoidal type, forming a thin collagen fibers, intercellular substance, a significant number of functionally active fibroblasts and macrophages. Cellular composition of the infiltrate lymphocytic with a small number of polymorphonuclear leukocytes. In adjacent areas of the myocardium preserved signs of interstitial edema, vascular Indonesia were extended and fulfilling

From the material presented shows that the introduction of compounds L-17 indicates a more favorable functional picture in the myocardium of animals with experimental myocardial infarction after 1-5 days by increasing the number of hypertrophied muscle, located at the periphery of necrotic areas: this area was somewhat more limited than in control animals, and transverse and longitudinal striated myofibrils more or less saved. Noted condition is by fibroblastic reaction and the formation of new blood vessels.

1. Treatment of experimental myocardial infarction, based on modeling of myocardial infarction with subsequent medical intervention, characterized in that the running intravenous connection L-17 from the class 1,3,4-thiadiazines at a dose of 40 mg/kg after creating a model of myocardial infarction with subsequent histological examination of tissue of the myocardium.

2. The method according to claim 1, characterized in that the compound L-17, influencing the nature of the acute inflammatory response, reduces the intake of neutrophilic leukocytes that produce factors that stimulate inflammation, correcting for the acute phase of the syndrome of systemic inflammatory response, which leads to a decrease in the expression of leukocyte reactions, stimulates migration of immune cells-lymphocytes, plasma cells, mast cells, macrophages in the necrotic foci, accelerates the formation of granulation tissue with proliferation of fibroblastic cells number and calls the substitution necrosis scar tissue, represented by the active fibroblasts and fibrous structures.



 

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