Method of normalisation of functional activity of vessel wall in patients with arterial hypertension of i-ii degree with metabolic syndrome, after thrombosis of eye vessels

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology and angiology, and deals with normalisation of functional activity of vessel wall in patients with arterial hypertension of I-II degree with metabolic syndrome, after thrombosis of eye vessels. For this purpose, indices of anti-aggregation, anti-coagulation and fibrinolytic activity of vascular wall are determined. On the basis of said indices general anti-thrombotic potential of vessels is calculated and if its value is 0.069 and lower, administered is complex treatment, including application of individually selected hupocaloric diet, dosed physical load, introduction of pioglitazone in dose 30 mg 1 time per day and lisinopril in dose 20 mg 1 time per day for 4 months.

EFFECT: complex of drug and non-drug therapy in combination with empirically selected treatment duration ensures complete normalisation of functional activity of vascular wall and, thus, reduction of risk of thrombotic complications in said group of patients due to potentiation of therapeutic effect of separate components of medicinal complex.

2 ex, 1 dwg

 

The invention relates to medicine, namely to cardiology and angiology.

Analogues of the proposed method of normalization of functional activity of blood vessels in patients with arterial hypertension (AH) I-II degree in the metabolic syndrome (MS)who have had blood clots in the eye, does not exist.

There is information on the use of a low-calorie diet (Savelyeva L. Modern approaches to treatment of obesity. // The doctor, 2000, No. 12 - p.12-14; Kadyrov, BC, Salhanov B.A. Nutrition in obesity. Alma-ATA, Kazakhstan, 1990) or physical training (V. Moshkov. Exercise in obesity. M, "Medicine", 1976. - 56 S.) in patients with various components of MILLISECONDS.

In patients with MS to reduce blood pressure often is prescribed lisinopril. For the correction of insulin resistance in patients hypertension I-II degree when the MS is assigned to pioglitazone. However, never before medical complex, consisting of a low-calorie diet, exercise stress, drugs pioglitazone and lisinopril, was not used in patients with arterial hypertension I-II degree with MS who have had blood clots in the eye to correct them vasaputi.

The aim of the invention is the correction of the attenuation functions of blood vessels in patients with arterial hypertension I-II degree with MS who have had blood clots in the eye.

The essence of the proposed method is that the correction of the attenuation function of the Nations blood vessels sick AG I-II degree at MS after thrombosis eyes, 4 months is assigned to a low-calorie diet, measured static and dynamic exercise, the drug pioglitazone at a dose of 30 mg 1 time per day, and lisinopril 20 mg 1 time per day.

The method allows to adjust the weakening of the functions of blood vessels in patients with arterial hypertension I-II degree with MS who have had blood clots in the eye for 4 months. Even when not in strict compliance with follow-up recommendations the proposed method can be maintained at a normal level functions of the vascular wall, which will significantly improve the quality of life of patients with arterial hypertension I-II degree with MS who have had blood clots in the eye, to reduce their pathological burden, reduce the number of cases of temporary disability, to accelerate and improve the quality of patient treatment, to exclude disability, as well as extend the life and reduce mortality of patients with arterial hypertension I-II degree with MS who have had blood clots in the eyes, heart attack and stroke, excluding re-thrombosis of vessels of the eye.

The inventive method is carried out as follows.

To diagnose weakening of the functions of blood vessels sick AG I-II degree with MS who have had blood clots in the eye, is the next examination.

Antiaggregatory activity of the vascular wall is determined according to the method (baluda VP, Luciano is and TI, Baluda M.V. Method of determining the antiaggregatory activity of the blood vessels of man. // The laboratory. Case, 1983. No. 6. - p.17-20). The basis of this method is the calculation of the degree of inhibition of platelet aggregation in plasma obtained from the blood after a temporary venous occlusion.

On the shoulder of vessels which have not been manufactured blood sampling is applied to the cuff of the sphygmomanometer and creating pressure by 10 mm Hg above systolic. After 3 minutes was made taking 9 ml of blood in 1 ml of 3.8% solution of sodium citrate. It was immediately centrifuged for 5 minutes at 1000 rpm to obtain platelet-rich plasma. The plasma was aspirated with a pipette and immediately placed in melting ice, where they were kept until the beginning of the research. Again the sample was centrifuged for 20 minutes at 3000 rpm to obtain estramboticos plasma. After counting the number of platelets in platelet-rich plasma obtained prior to venous congestion (described in detail below), it was diluted with platelet-poor plasma (Betp)taken before (1 sample) and after (2 samples) venous stagnation to a concentration of 200,000 platelets/µl. The mixture was shaken and incubated for 10 minutes at 20-22°C. Then held platelet aggregation (AT) with collagen (dilution 1:2 primary suspension) on the glass.

Assessment AT for this research is performed in the following way (sitic the VA A.S. In the book: Hemostasis. Physiological mechanisms, principles of diagnostics of the main forms of hemorrhagic diseases. Edited Yea, Lpparam. SPb.: 1999. 49-52).

The blood is taken with sodium citrate 3.8% in the ratio of 9:1, centrifuged 5 min at 1000 rpm to obtain platelet-rich plasma (BTP). Part of the plasma is taken, and the remainder centrifuged at 3000 rpm for 20 min, receiving platelet-poor plasma (Betp). BTP standardise the number of platelets by dilution of the original BTP autologous sample Betp (obtained prior to venous stagnation - 1-I sample-or post - 2nd test) up to 200·109/L. the Concentration of blood platelets in the original BTP is calculated in the camera Goriaev (50 large squares). The volume mix BTP and Betp determined by the formula

VBetp=VBTP·[(N/200000)-1],

VBetp- the volume of platelet-poor plasma,

VBTP- the volume of platelet rich plasma,

N is the number concentration of platelets in the original BTP (cells/µl).

Selected standardized volume of plasma on a glass slide cause of 0.02 ml of plasma and other pipette 0,02 ml R-RA inducer of collagen in the standard concentration (dilution 1:2 primary suspension). Glass wand mix plasma with inductors and include a stopwatch. The mixture is stirred so that the fluid occupied environment is of a diameter of about 2 cm

Shaking the glass in a circular motion in transmitted light illuminator on a black background is watched through a magnifying glass for the occurrence of aggregates. With the appearance of distinct units, the enlightenment of the solution and the adhesion of some units to the glass stopwatch off, fixing the time of platelet aggregation.

The reaction is repeated 2-3 times in the 1st and 2nd sample, finding for each of the arithmetic mean value.

The degree of inhibition of platelet aggregation after venous congestion is judged antiaggregatory activity of blood plasma, due to the arrival of a blood of prostacyclin from vascular wall. Index antiaggregatory activity of the vascular wall (IAAS) in the study AT the glass was calculated by the formula

Normal values for collagen can be considered IAAS 1,50-1,60.

The definition of anti-platelet properties of the vascular wall that are dependent on the production of substances that activates antithrombin III, assessing its basal level before and after the temporary metered ischemia wall of the vein below (Barkagan SS, Momot A.P. bases of diagnostics of disorders of hemostasis. M., 1999 - 214 C.).

The principle of the method is based on detecting the reduction of the activity (in the absence of heparin) plasma anti-thrombin III (AT III), which is determined by the ability of the investigated plasma to inactivate tro the bin, for what it is pretreated sorbent heparin, then subjected to heat defibrinate and mixed with a standard amount of thrombin. After incubation of the mixture in it determine the residual coagulation activity of thrombin. The level of reduction of the activity of thrombin in percent from the norm estimate the activity of AT III in the plasma.

Use the following reagents. 1. Tris-HCl buffer 0.05 M, pH 7.4. 2. A solution of thrombin in buffer: 0.2 ml of a solution should minimize 0.3 ml of 0.4% solution of fibrinogen for 15-16 seconds. The working solution of thrombin is prepared in a plastic or silikonizirovannoj tube, stored at room temperature and used in the test on the day of the study. 3. Sorbent heparin Jasonb-1 (firm "Technology Standard"). 4. A freshly prepared solution of fibrinogen at a concentration of 3.5-4.0 g/l, which is used for testing residual activity of thrombin. May be replaced with a solution of fibrinogen normal platelet-poor citrate plasma, diluted with buffer 2 times; 5. Fresh citrate platelet-poor plasma obtained from 6-8 healthy people, or freeze brand, with the known activity of AT III, which is used to construct a calibration graph.

The research material is citrate platelet-poor plasma.

For the preparation of sorbed and defibs nizovannoj plasma in a test tube and mixed with 10 mg of sorbent heparin with 1.0 ml of the investigated plasma. Constantly shaking the test tube, mix the contents at room temperature for 8 min, excluding foam and sediment at its bottom. After that, the mixture was centrifuged for 2 min at 1000-1500 rpm Plasma in nadeshiko transferred into a clean tube and defibrinated in a water bath at +56°C for 6 min, then centrifuged at 3000 rpm for 10 min, remove the supernatant portion and explore within the first 2 hours

The course definition. In test tube add 0.4 ml of the working solution of thrombin and heat it in a water bath at +37°C for 2 minutes Then add 0.1 ml of the investigated adsorbed and defibrinating plasma include stopwatch. After 2 minutes (exactly!) 0.2 ml of the mixture is transferred into a test tube with 0.3 ml of a solution of fibrinogen (or diluted normal plasma), pre-warmed to +37°C. Immediately include stopwatch and record the clotting time.

On the calibration curve to find the activity of AT III in percent.

The calibration curve carried out as follows. The plasma of healthy people are defibrinating, as described above. Then from preparing cultivation to prepare the calibration curve in accordance with the table.

The scheme of preparation of dilutions of plasma for p the structure of the calibration curve for the determination of the activity of at III
The number of breedingPlasma + bufferThe activity of at III, %
1Plasma without buffer100
20.2 ml + 0.2 ml50
30.1 ml + 0.3 ml25

With each of the dilutions to determine the clotting time according to the above method. All the measurements were carried out three times, calculate the average result. When constructing a calibration curve on a logarithmic ordinate axis delay the clotting time in seconds on the x-axis is the activity of AT III in % in accordance with the above dilutions. A sample calibration curve is shown in the drawing.

A calibration curve for one type and one series of thrombin and buffer build once. Periodically inspects only the activity of the working solution of thrombin.

In a normal venous occlusion activity of AT III is 85-115%. When blood samples are taken after the temporary venous occlusion, as described in the method evaluation antiaggregatory activity of the vessels, and defining AT III it is possible to indirectly evaluate the level of synthesis in the vessel wall tissue activators AT III. the and the background of temporary venous occlusion activity of AT III rises and falls within the boundaries of 120-143%. Calculates the index of synthesis activators AT III vessels (ISAAC) by dividing the value of the activity of AT III on the background of venous occlusion on the value of AT III without it. In norm it is 1,20-1,45.

The activity of the synthesis of tissue plasminogen activators time of lysis euglobulin clot before and after the temporary venous occlusion was evaluated as follows.

The principle of the method consists in depositing euglobulin fraction of the plasma, the main inhibitor of fibrinolysis, refers α2-antiplasmin remain in the supernatant portion and removed. So euglobulin lysis reflects the activity of fibrinolysis in conditions of exclusion inhibitory effect of antiplasmin. Its rate reflects mainly the amount of plasminogen in the plasma and the degree of its activation. Determine the time of spontaneous lysis of the clot derived from euglobulin fraction of the plasma by adding to it a solution of calcium chloride.

Use the following reagents 1. 1% solution of acetic acid. 2. 0,277% solution of calcium chloride. 3. The Michaelis buffer or Tris-NA buffer, 0.05 M, pH 7.3 to 7.4.

The research material is citrate platelet-poor plasma before and after the temporary venous occlusion.

The course definition. To obtain euglobulin faction to 8.0 ml of distilled water is added 0.15 ml of 1% acetic acid and 0.5 ml of investigated is lazmi. After a 30-minute cooling the mixture in the refrigerator at +2-8°C euglobulin precipitated by centrifugation at 1500 rpm for 7 minutes the Supernatant is drained, the drain tube rollover on filter paper. Sediment euglobulin diluted in 0.5 ml of buffer and placed in a water bath (37°C). Then, without removing the tube from the bath, add 0.5 ml of a solution of calcium chloride, gently mixed by shaking the tube (not shaking!), include stopwatch and incubated in a water bath at +37°C. Record the time from the moment of addition of calcium chloride to dissolve the clot.

The results are expressed in minutes. Normal spontaneous lysis euglobulin clot is 180-240 minutes After the temporary venous occlusion time of lysis is reduced, while in the borders 126-170 min. by dividing the value of the duration of spontaneous lysis euglobulin clot to occlusion by the value after the calculated index fibrinolytic activity of the vascular wall (IFAS), the norm is equal 1,40-1,50.

Each laboratory needs to be examined group of healthy people in order to find the average normative values with the calculation of S2in all three methods for subsequent calculations.

By each method in each patient for greater accuracy diagnostic test is done 3-4 times with calculation sredneperiodicheskii the values which are used in subsequent calculations and the calculation of S2.

To determine the individual weight of the investigated parameters in vascular patients and calculation of common antithrombotic potential of the vessels was applied multivariate analysis system that allows you to translate the multidimensional quantitative characteristics of the process under investigation is not comparable absolute values in comparable relative values (methods of morphometric and statistical analysis in morphological studies. Comp. Mwhoa, Baglow, Rio and other Kuibyshev, 1982. - 47 S.). The calculation was carried out according to the formula

Xj- analyzed parameter,- regulatory option- the relative difference.

Pi- the weight coefficient (influence), and is a constant factor (in our research and=0,1), σj- srednekvadraticheskogo deviation values of Xjin relative units.

Si2the variance of the investigated parameter Xini- the number of observations in the definition of Xi, S02- regulatory dispersion parameter X0n0- the number of observations in the definition of X0.

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XBi oops- amount integrally characterize the process within the specified time (in relative units)is the total antithrombotic potential of vessels (oaps).

The combined application of the described methods with subsequent processing of the obtained values IAAS, ISAAC and IFAS system multifactor analysis to determining the General antithrombotic potential vessels (XBi oops), the value of which is considered normal when 0,201 and above. When the value of antithrombotic activity of vessels (XBi oopsfrom 0.200 to 0,070 patients noted the risk of weakening activity in the walls of blood vessels, which requires normalization lifestyle, stable normalization of blood pressure and monthly status control of vascular functions. When the value of XBi oopsfrom 0,069 and below, you should immediately treat patients according to the claimed method.

To create a negative energy balance in the body, patients are advised individually selected low-calorie diet.

Calorie intake is calculated in kcal individually for each patient hypertension I-II degree with MS who have had blood clots in the eye, according to the formula

for women 18-30 years (0,0621 × body weight (kg) + 2,0357) × 240,

31 - 60 years (0,0342 × body weight (kg) + 3,5377) × 240,

over 6 years of age (0,0377 × body weight, kg + 2,7545) × 240,

for men 18-30 years (0,0630 × body weight (kg) + 2,8957) × 240,

31 - 60 years (0,0484 × body weight (kg) + 3,6534) × 240,

over 60 years of age (0,0491 × body weight (kg) + 2,4587) × 240.

The resulting value remains unchanged with minimal physical activity, multiplied by a factor of 1.3 at a moderate and 1.5 - high physical activity (usually in patients with hypertension I-II degree with MS who have had blood clots in the eye, physical activity level low).

It is recommended that 3 main meals and 2 intermediate. It is recommended that the following distribution of daily calories: Breakfast - 25%, 2nd Breakfast - 10%, lunch - 35%, tea - 10%, dinner - 20%.

To compile menu the patient uses a special table with the instructions of the chemical composition and caloric content of products, given that the main sources of energy: protein (1 g contains 4 kcal), fat (9 kcal), carbohydrates (4 kcal) and alcohol (7 kcal).

The second component of the proposed method is feasible regular physical exercise,

In real life you can implement the three forms of physical activity: 1) morning hygienic gymnastics (charging); 2) health care gymnastics; 3) fractional exercise during the day.

1. Morning hygienic gymnastics (charging).

Morning gymnastics should do after SN is before Breakfast in a ventilated room. Under the influence of training the body is released from the state of inhibition of the physiological processes taking place during sleep.

The sequence of the exercises involves the alternation of load on different muscle groups (arms, legs, body). Exercises are performed with gradually increasing excursion breathing, stretching, limited use of power conditions. Breathing exercise should be free, rhythmic, without delay, mainly through the nose; the exhalation should be longer than the inhale (breath in 2-3 sec, exhale 3-5).

In good health the load, you can increase the number of repetitions faster, increase range of motion and shorter pauses between exercises.

When fatigue should reduce the load, increase the duration of pauses between exercises, to fill their quiet breathing.

After gymnastics, you must go to the rubbing or take a shower.

Morning exercises should evoke a sense of vitality, increase activity, improve well-being and health.

If you feel unwell, develop shortness of breath or pain in the heart and behind the sternum should be temporarily suspend classes and consult a doctor.

During the day, sick AG I-II degree with MS who have had blood clots in the eyes, recommended treatment and preventive exercises is. Depending on the initial fitness may use first lightweight option, physical activity, and subsequently enhanced option.

2. Complexes of preventive and curative gymnastics

2.1. The lightweight version of preventive and curative gymnastics.

Exercise 1. Standing. A quiet walk with a gradual acceleration and deceleration 1-2 minutes on the exercise of the gradual deepening of the breath.

Exercise 2. Circular motion in the shoulder joints. When breeding - breath, when the note - exhale with a slight tilt of the torso and retraction of the abdominal wall 6-8 times. The fingers touch the shoulders, elbows close to the torso.

Exercise 3. Standing, hands on his belt. Alternately shifting the weight of the body from one foot to the other with a small bending the legs at the knee joint without lifting the feet from the floor. Exercise done 10-16 times with the muscles of the legs.

Exercise 4. Standing, feet apart at shoulder width, hands on his belt. Bending the trunk forward, touch right hand to left toe. 4-6 times alternately. When straightened position - breath, when the tilt - exhale. To look ahead.

Exercise 5. Standing with arms along the body. At the same time to take straight arm and one leg to the side with alternating lead leg. 4-6 times in each direction in turn. A wave of the hands and feet, breathe freely, do not delay.

Uprajnenie is 6. Standing, feet apart, hands in front of chest with palms down. With a turn of the body to dissolve hand in hand with turning the palms up - breath. To return to the original position with a small tilting forward, exhale. 3-5 times in each direction in turn. Breathing to harmonize with the movement of hands and body. By the end of exhalation to engage the wall of the abdomen.

Exercise 7. Standing, hands free. The walk free - 1 min, then with high flexion of the hips - 10-20 movements with subsequent transition to a peaceful walk 1-2 minutes Breathing rhythmic, medium depth.

Exercise 8. Sitting on the edge of the chair, hands on the waist. The bowing of the back and bending forward of the body. Repeat 6-10 times. Breathing is not to delay.

Exercise 9. Sitting on the edge of the chair, the emphasis tassels on the edge of a chair, and your feet slightly in front of the chair. Squats with a focus hands on the edge of a chair - 4-6 times. When you squat exhale.

Exercise 10. Standing sideways to the back of the chair to hold it with one hand. Swing free straight arm with leg pulling back. To return to the original position. Repeat 4-6 times for each leg and arm. Breathing is not to delay.

Exercise 11. Standing, legs apart widely, hands on waist. Turns the body right and left - 6-10 times alternately. The head does not turn, to look forward.

Exercise 12. Standing, feet together, hands down. Move the hands to the sides, inhale, bend your knee is pressed a hand to his stomach - exhalation. 3-5 times each leg alternately. Strive to maintain balance; on the exhale, draw your abdomen.

Exercise 13. Standing, feet together, hands pubescent. The side slopes of the case with flexion of the opposite hand ("pump"). Breathing is not to delay, to strive for greater excursion of movement.

Exercise 14. Standing. A quiet walk with a uniform average depth of breathing. 1-2 minutes

Exercise 15. Lying on the Mat to put under your head with a pillow. Go to a half-sitting position and bent to hug the hips, exhale, return to the starting position and inhale. Breath hold. Strive in a semi-sitting position to maintain balance. Run 4-6 times.

Exercise 16. Lying down, arms at sides, legs apart. A semi-circular motion right straight leg to the left with the rotation of the pelvis - exhale - return to the starting position and inhale. 3-5 times in each direction. Alternately left and right, with the greatest possible excursion movement of the leg, keeping the emphasis brushes the floor.

Exercise 17. Sitting on the floor; a) to stand on all fours; b) to move into position on his knees; hands up - breath, torso, and hands to take back - exhale. When the tilt pull the stomach. Repeat 4-6 times; d) to go into a standing position, and then in the supine position; (e) self-massage of the abdomen small polukrugom movements clockwise-1-2 minutes Rest 2 min; W) quiet on the Chania; C) exercise in the protrusion (calm) and retraction (active) abdominal wall. The retraction of the abdomen combined with exhale through the mouth. Repeat 4-6 times.

Exercise 18. Standing with arms bent. Energetic walking on the spot or area of high flexion of the hips and waving of hands - 20-30 steps. Breathing is not to delay.

Exercise 19. Sitting on a chair, legs apart, hands on the waist or rest against the edge of a chair. The circular motion of the pelvis with the retraction of the abdomen when moving the pelvis back. 4-6 times in each direction.

Exercise 20. Standing. A peaceful walk with the breath of the average depth of 2-3 minutes

When the source sufficient trained or arising in the course of the practice of tolerance to physical loads you can use the following set of exercises.

2.2. Enhanced preventive and curative gymnastics.

Exercise 1. Standing. The quiet walk with rubbing the palms of the thorax, abdomen, lower back. Runs 1-2 minutes

Exercise 2. Standing, hands down. Simultaneous bending with tension and free "throwing" hand forward, sideways and upwards of 12-16 times. When you bend exhale, when the alignment of breath.

Exercise 3. Standing, hands on waist, legs shoulder-width apart. Lateral motion of the pelvis to the right and left, back and forth. Is 6-10 times alternately. Breathe freely.

Exercise 4. Standing, feet shoulder width p is once they have reached, hands pubescent. Circular motion direct hand in the shoulder joints, 6-10 times with a maximum excursion, breathing, do not delay.

Exercise 5. Standing, hands in front of chest, bent at the elbows. Walking with high flexion of the hips, with a touch of the hand. 6 -10 times for each leg alternately. Motion of energetic, hip flexion - exhale through the mouth.

Exercise 6. The quiet walk 1-2 minutes

Exercise 7. Sitting on the edge of the chair, hands on the waist. Bending and bowing of the body. The exercise is performed 8-10 times. The energetic movement. When straightening - breath, bending exhale.

Exercise 8. Standing sideways to the chair, to hold back, the other hand on the waist. Alternate sweeps straight leg forward, with the greatest possible tour. Swing legs to be combined with the exhalation. Runs 4-6 times.

Exercise 9. Standing, feet apart, hands at sides. Bending the body forward, touch right brush left toe of the feet, the other hand is allotted up. To return to the original position. Tilt combined with exhalation, by straightening the breath by 4-6 times.

Exercise 10. Walking the quiet breathing of medium depth. 1-2 minutes

Exercise 11. Standing, hands in a fist and lowered: (a) bending of the arms at the elbows with the power and extension of their diverting ago, with possibly large rectification and voltage and delay in the stress state within 2-3 C. Standing, hands on waist; b) palupi is edenia with subsequent lifting in socks and tension legs. The exercise is performed 4-6 times with possibly large rectification and voltage, and the delay in the stress state within 2-3 C.

Exercise 12. Sitting on the edge of the chair. In the raised position and bent knee leg to make alternate shaking the hands of the calf muscles and thighs. To reduce muscle tension. 1-2 minutes

Exercise 13. Sitting on the edge of the chair, straight leg divorced. Pinch open and direct the hands and feet. When breeding breath, when the note - exhale. Is 4-8 times.

Exercise 14. Standing. The quiet walk with the transition to the rhythmic quiet running (Jogging) on the spot or moving. For fatigue to go on a peaceful walk with the breath of medium depth. 2-5 minutes

Exercise 15. Lying on the Mat. Simultaneous lifting of the body and legs on the exhale. 4-6 times. Arms and legs should be straight, to keep the balance.

Exercise 16. Lying on the Mat, the emphasis brushes the floor. Cross movement straight leg - scissors. 4-8 times. Breathing is not to delay.

Exercise 17. With a quick straightening of the legs to move into a sitting position, then to lie down. You can help stroke 4-6 times.

Exercise 18. Lying on your back, legs bent. Calm breathing 4-6 times.

Exercise 19. Lying on his back, hands diluted with emphasis brushes the floor. With the rotation of the pelvis to the left, bend the legs, rotate the pelvis with legs crossed to the right and pull the legs is. To repeat such a circular motion feet 3-6 times in each direction alternately. Hands not off the floor. Breathing is not to delay.

Exercise 20. Lying on your back, arms and legs separated. Alternate turns the body right and left laying one hand to the other. Feet are not slipping. When divorced hands - breath, turning exhale. Performed 3-6 times.

Exercise 21. Lying on your back, arms along the body: a) turn on your left side; b) to turn on the right side; C) switch to lying on his stomach; to kneel; d) to move in a standing position; (e) walking on the spot with high flexion of the hips and the movement of the hand - 20-30 steps; g) to sit on the Mat; C) lie on your back, relaxing breath. The whole complex repeat 3-4 times.

Exercise 22. Standing. Walking the quiet breathing of the average depth of 1-2 minutes

Exercise 23. Standing, feet apart on the width of the foot, hands on waist. Circular motion of the pelvis, right and left 6-8 times. Breathing is not to delay.

Exercise 24. Standing with legs wide apart, hands in front of chest. Alternately bending the legs with the transfer to it of gravity of the body with stretching hand to toe of the bent leg. 4-6 times in each direction. The other leg is straight. When straightening - breath, when the tilt - exhale.

Exercise 25. Standing, feet apart at shoulder width, hands on waist. Circular head movements by 4-10 times in each is the thoron.

Exercise 26. Standing, feet apart at shoulder width, hands on waist. Bend trunk to the right, pulling the left arm up - breath. Return to starting position - exhale. 4-6 times alternately.

Exercise 27. The same hands to the shoulders. Circular motion of the brushes with the maximum excursion in the shoulder joints, when breeding - breath during the mixing and retraction of the abdominal wall exhale. Breathing deep.

Exercise 28. Standing. A peaceful walk and breath the average depth. The reduction of the total load. 1-2 minutes

3. Fractional exercise during the day.

Patient A.G. I-II degree with MS who have had blood clots in the eye, is sick with a number of related disorders, primarily the cardiovascular system. This circumstance limits the simultaneous application of a high physical load during morning exercises, as well as in the main lesson, curative gymnastics. This is why increasing the physical activity of persons suffering from hypertension I-II degree when MS after thrombosis of vessels of the eye, it must be done by the distribution of physical activity in small doses throughout the day. This method of increasing physical activity in these patients should be considered as a method of fractional loads.

Depending on the conditions of real life in patients with arterial hypertension I-II degree with MS undergoing tro the Bose blood vessels of the eye, suffering from varying degrees of abdominal obesity, you can recommend various exemplary embodiments of the fractional loads to increase physical (motor) activity during the day.

Option 1.

Exercise 1. Sitting - dilute the elbows to the sides, inhale, extend hands forward voltage exhale, 4-6 times.

Exercise 2. Sit - to stand with the deflection of the housing and land - 8-10 times.

Exercise 3. Sitting mimicking the movements of a boxer with possibly a large turn of the body is 10-12 times.

Option 2.

Exercise 1. Standing - walking with high flexion in the hip - 16-30 times.

Exercise 2. Standing - circular head movements to the right and left - 3-8 times in each direction.

Exercise 3. Standing legs apart widely imitated the movements of Costa - 10-12 times.

Exercise 4. Sitting - transition into the standing - 10-12 times.

Option 3.

Exercise 1. The quiet walk - 1 min

Exercise 2. Walking fast - 1 minute

Exercise 3. Walking with high flexion of the hips and alternate wave of the hands 20-30 times.

Exercise 4. Walking the quiet breathing of 1-2 min; quiet running on the spot or move around the room - 2-5 minutes

Option 4.

Walk the pedestrian varying length.

Option 5.

Physical work in different ways and with different duration depending on the conditions (cleaning, home maintenance, RA the PTA cleaning, garden work and other).

The third component of the proposed method - the purpose of pioglitazone 30 mg 1 time per day, fourth of lisinopril 20 mg 1 time per day at the same time.

The introduction of this method of correction functions of blood vessels in patients with arterial hypertension I-II degree with MS who have had blood clots in the eyes, into practice will allow you to solve a number of pressing socio-economic problems. Effective correction of these patients will reduce these patients the period of temporary disability, prevent strokes, heart attacks and re-thrombosis of vessels of the eyes, to reduce the number of outputs on disability and reduce mortality among this group of patients.

Example 1. Patient J. 51, 76 kg, body mass index and 32.3 kg/m2suffering from arterial hypertension of I degree with metabolic syndrome for 11 years, is not systematically treated, examined while in ophthalmic hospital about thrombosis eyes. The patient was taken blood and investigated for the above scheme assessment IAAS, ISAAC and IFASS and calculating the total antithrombotic potential of the vessels.

The patients were identified expressed signs of oppression antithrombotic function of the vascular wall. IAASS was 1.17, ISAAC 1.16 and IPASS 1,22. Overall the antithrombotic potential of vessels amounted X Bi oops=0,057. The patient was assigned to the medical complex of low-calorie diet (1914,7 kcal), dosed physical activity, pioglitazone 30 mg 1 time per day and lisinopril 20 mg 1 time per day. The study of the functions of the vascular wall were performed monthly. After 4 months the body weight was 64 kg, BMI of 27.2 kg/m2, IAASS was 1,55, ISAAC 1,41 and IPASS 1,46, normalization of total antithrombotic potential vessels (XBi oops=0,205). Further sometimes acute patient compliance recommendations in terms of diet and exercise helped to support in next investigated parameters antithrombotic activity of vessels in normal limits.

Example 2. Patient A. age 46, 72 kg, body mass index 29,8 kg/m2suffering from arterial hypertension of II degree with metabolic syndrome for 5 years, not systematically treated, examined while in ophthalmic hospital about thrombosis eyes. The patient was taken blood and investigated for the above scheme assessment IAAS, ISAAC and IFASS and calculating the total antithrombotic potential of the vessels.

The patients were identified expressed signs of oppression antithrombotic function of the vascular wall. IAASS was 1,09, ISAAC 1.11 and IPASS 1,14. Overall antithrombotic the ski potential vessels amounted X Bi oops=0,051. The patient was assigned to the medical complex of low-calorie diet (1872,0 kcal), dosed physical activity, pioglitazone 30 mg 1 time per day and lisinopril 20 mg 1 time per day. The study of the functions of the vascular wall were performed monthly. After 4 months the body weight was 65 kg, body mass index 26.8 kg/m2, IAASS was 1,56, ISAAC of 1.42 and IPASS 1,48, normalization of total antithrombotic potential vessels (XBi oops=0,210). Further sometimes not strict adherence to patient data recommendations in terms of diet and exercise helped to support in next investigated parameters antithrombotic activity of vessels in normal limits.

The use of the proposed correction method attenuation functions of blood vessels in Hematology, cardiology and endocrinology will help to avoid many of vascular complications in patients with arterial hypertension I-II degree in the metabolic syndrome who have had blood clots in the eye, they reduce the number of cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality, excluding re-thrombosis of vessels of the eye.

The method of normalization of functional activity of blood vessels in patients with arterial hypertension I-II degree in the metabolic syndrome, lane is carrying blood clots in the eye, involving the use of individualized low-calorie diet, exercise loads, pioglitazone 30 mg 1 time per day and lisinopril 20 mg 1 time per day at the same time of day for 4 months, appointed after treatment in patients index antiaggregatory activity of the vascular wall, the index of the anticoagulant activity of the vessel wall and the index of the fibrinolytic activity of the vessel wall using a system of multivariate analysis, translating each of the identified parameters in comparable relative values, on the basis of which taking into account the weighting factor determined for each indicator on the basis of the standard deviation for this measure and a constant factor, equal to 0.1 calculation of total antithrombotic potential of vessels XBi oops=0,069 and lower diagnosticums the development of impaired functional activity of blood vessels.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to cardiology and endocrinology, and concerns treating the patients with chronic cardiac failure compromised by type 2 diabetes. That is ensured by the additional introduction of the selective β1 adrenoceptor antagonist nebivolol in a single dose 5-7.5 mg/day within 12 months with underlying ACE inhibitor and diuretic therapy in the patients with a higher level of basal glycemia by more than 4.5 mmol/l and preserved LVEF by more than 52 %.

EFFECT: method provides effective treatment in the given group of patients due to ability of nebivolol to improve nitrogen oxide synthesis by a vascular endothelium and to provide normalising haemodynamic, metabolic, anti-ischemic and immune-correcting action.

1 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to novel 3,4-substituted pyrrolidine derivatives of general formula or pharmaceutically acceptable salts thereof, where R1 is an acyl selected from values given paragraph 1 of the formula of invention; R2 is unsubstituted C1-C4-alkyl or C3-C7-cycloalkyl; R3 is a fragment selected from a group of fragments of formulae: (a), (b),

(c) and (f), where any of the fragments of formulae given above (a), (b) and (f), the star (*) indicates a bond of the corresponding fragment R3 with the molecule residue in formula I; Ra denotes N-C1-C4-alkylaminocarbonyl, N-phenylaminocarbonyl, N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl- C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(C3-C7-cycloalkyl-C1-C4-alkyl)aminocarbonyl, N,N-di-(C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl)aminocarbonyl or hydrogen; Rb and Rc are independently selected from a group comprising unsubstituted C1-C4-alkyl, unsubstituted monocyclic aryl, unsubstituted monocyclic heterocyclyl, unsubstituted or substituted monocyclic C3-C7-cycloalkyl, unsubstituted aryl- C1-C4-alkyl, usubstituted monocyclic C3-C7-cycloalkyl- C1-C4-alkyl, hydrogen or acyl, where the acyl is selected from values given in paragraph 1 of the formula of invention; or Rb and Rc together may form a 6-member nitrogen-containing ring which may be unsubstituted or disubstituted with =O; Rd in the fragment of formula (c) denotes a phenyl or phenyl-C1-C4-alkyl; Re denotes hydrogen or C1-C4-alkyl; and m equals 2; each of R4 and R5 denotes hydrogen; and T denotes methylene. The invention also relates to the pharmaceutical composition based on the compound of formula I and a method of treating hypertension using the compound of formula I.

EFFECT: novel pyrrolidine derivatives having renin inhibiting activity are obtained.

7 cl, 19 tbl, 37 ex

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, namely, to therapy and cardiology, and deals with treatment of arterial hypertension. For this purpose into complex of conventional therapy additionally introduced is prostaglandin E2 in form of 0.0008% solution. Prostaglandin is introduced intravenously, starting with rate 50-100 ng/kg/min, increasing rate of introduction each 10 minutes on 20-40 ng/kg/min, bringing rate to 150-300 ng/kg/min during 40-60, minutes. Altogether there are three introductions per a course with 1-2 day intervals between them.

EFFECT: additional introduction of prostaglandin E2 in elaborated doses and regimen ensures efficient normalisation of arterial pressure during long term due to enhance of excretion of prostaglandins by kidneys, expressed vasodilation of vessels of kidneys, heart and brain, as well as normalisation of functional activity of platelets.

6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I): where: A is a monocyclic or polycyclic aryl or heteroaryl group, where the heteroaryl radical denotes a 5-10-member cyclic system containing at least one heteroaromatic ring and containing at least one heteroatom selected from O, S and N; optionally substituted with one or more substitutes independently selected from a group comprising halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, C1-4alkoxy and a hydroxyl group; B is a monocyclic nitrogen-containing heteroaryl group, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from S and N; optionally substituted with one or more substitutes selected from a group consisting of halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, aryl and C1-8alkylthio; either a) R1 is a group of formula: -L-(CR'R")n-G, where L is a binding group selected from a group consisting of a direct bond, -(CO)-, -(CO)NR'- and -SO2-; R' and R" is independently selected from hydrogen atoms; n assumes values from 0 to 1; and G is selected from a group consisting of a hydrogen atom and C1-4alkyl, aryl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O, S and N; C3-8cycloalkyl and saturated heterocyclic groups, where heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one or two carbon atoms are substituted with a N heteroatom; where alkyl, C3-8cycloalkyl, aryl or heteroaryl groups are unsubstituted or substituted with one or more substitutes selected from halogen atoms; and R2 is a group selected from hydrogen atoms, halogen atoms and C1-4alkyl, C2-5alkynyl, C1-4alkoxy, -NH2 and cyano groups, where alkyl and alkynyl groups may be unsubstituted or substituted with one aryl group; or b) R2, R1 and -NH- group to which R1 is bonded form a group selected from groups of formulae and , where: Ra is selected from a hydrogen atom or groups selected from C1-4alkyl, C3-8cycloalkyl, aryl, aryl-C1-4alkyl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O and N; saturated heterocyclic rings, where the heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one carbon atom is substituted with a heteroatom selected from O and N; and C1-4alkylthio; where the aryl or heteroaryl groups are unsubstituted or substituted with one or more groups selected from halogen atoms, cyano group, trifluoromethoxy and carbamoyl; Rb denotes hydrogen; and pharmaceutically acceptable salts thereof and N-oxides; provided that the compound is not selected from N-[6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, and N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]formamide. The invention also relates to a pharmaceutical composition, use of compounds in any of claims 1-20, a method of treating a subject, as well as a composite product.

EFFECT: obtaining novel biologically active compounds having adenosine A2B receptor antagonist activity.

27 cl, 160 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof where R1 and R2 together denote a group selected form groups of formula (III-1): , where R9 denotes 1) a lower alkyl group, optionally substituted with a halogen atom or lower alkoxy group, 2) an aryl group, 3) an aralkyl group, 4) a heteroarylalkyl group, 5) a heteroaryl group, where the aryl, aralkyl, heteroarylalkyl and heteroaryl groups can be substituted with a halogen atom, lower alkyl group, optionally substituted with a lower alkoxy group or 1-3 halogen atoms, lower alkoxy group, optionally substituted with 1-3 halogen atoms, cyano group, hydroxy group, alkylsulphonyl group, cycloalkylsulphonyl group, aryl group, heteroaryl group, alkylaminocarbonyl group, alkanoyl amino group, alkyl amino group or dialkylamino group; R10 denotes a lower alkyl group, optionally substituted with 1-3 halogen atoms, or a lower alkylsulphonyl group; X9-X12 denotes a carbon atom or a nitrogen atom, where the carbon atom can be independently substituted with a lower alkyl group, optionally substituted with a halogen atom or a lower alkoxy group, lower alkoxy group, optionally substituted with a halogen atom, or a cyano group or a halogen atom; R3 denotes a) a group of formula (II-1): (ii-U where R4 and R5, taken together with a nitrogen atom, form a 5- or 6-member monocyclic ring, where the monocyclic ring may contain a substitute in form of a lower alkyl group, m1 equals 3; or b) a group of formula (II-2): , where R6 denotes a lower alkyl group or cycloalkyl group; m2 equals 1 or 2; X1-X4 all denote carbon atoms, or one of X1-X4 denotes a nitrogen atom and the rest denote carbon atoms; and where "heteroaryl" in each case relates to a 5- or 6-member aromatic ring containing 1-3 heteroatoms selected from a nitrogen atom, oxygen atom and a sulphur atom. The invention also relates to a histamine H3 receptor antagonist or inverse agonist, as well as a preventive or medicinal agent.

EFFECT: obtaining novel biologically active compounds, having histamine H3 receptor antagonist or inverse agonist activity.

11 cl, 8 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: compounds are suitable for use as kinase 1β-adrenergic receptor (βARK-1) inhibitors. The invention also relates to compositions containing such compounds and to use of compounds of formula to treat and prevent chronic heart failure, hypertension myocardial ischemia and hepatitis C viral infections (HCV) and for preventing opiate addiction. The invention also pertains to methods of producing formula (I) compounds.

EFFECT: more effective use of the compounds.

11 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described 3,4-substituted piperidines applicable in diagnostics and drug therapy of a warm-blooded animal, preferentially for therapy of a disease which depends on renin activity; application of a compound of such kind for preparing a pharmaceutical composition for therapy of the disease which depends on renin activity; application of the compound of such kind for therapy of the disease which depends on renin activity; the pharmaceutical compositions containing 3,4-substituted piperidine, and/or a therapeutic mode involving administration of 3,4-substituted piperidine, a method for producing 3,4-substituted piperidine. The preferential compound (which also can be presented in the form of salts) are described by formula I' wherein R1, R2, T, R3 and R4 are such as described by the patent claim.

EFFECT: production of the compounds for therapy of the disease which depends on renin activity.

28 cl, 1 tbl, 375 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: agent for treating systemic hypertension contains as an active ingredient a compound presented by formula (1): or its pharmaceutically acceptable salt.

EFFECT: preparation of the new agent for treating systemic hypertension.

12 cl, 7 ex, 7 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula (I) , where the dotted line is either absent or denotes a double bond; R1 denotes H or C1-6-alkyl, possibly substituted with a CN group, or denotes a phenyl or sulphonyl phenyl, substituted with one or more B groups, or denotes -(CH2)m-Ra, where Ra denotes: NRiRii, C3-6-cycloalkyl, 6-member heterocycloalkyl, which denotes a univalent saturated group which contains one nitrogen heteroatom, the rest are carbon atoms, aryl, which can be substituted with one or more B groups, or denotes -(CH2)n-(CO)-Rb or -(CH2)n-(SO2)-Rb, where Rb denotes: NRiRii, 5-6-member heterocycloalkyl, which denotes a univalent saturated group containing one or more heteroatoms selected from nitrogen, oxygen, the rest are carbon atoms, aryl or 5- or 6-member heteroaryl, which denotes an aromatic ring containing two heteroatoms as ring members, the said heteroatoms selected from N or O, the rest are carbon atoms; which can possibly be substituted with one or more B groups, R2 denotes one or more H, halo, C1-6-alkyl, C1-6-alkoxy, R3 denotes H or-(CO)-Rc, where Rc denotes: C1-6-alkyl, 5-member heterocycloalkyl, which denotes a univalent saturated group containing one nitrogen heteroatom, the rest are carbon atoms possibly substituted with C1-6-alkyl, or denotes C1-6-alkyl; R4 denotes H; R5 denotes H, C1-6-alkyl, -(CH2)m-NRiRii, -(CH2)n-(CO)-Rb, where Rb denotes NRiRii or a 6-member heterocycloalkyl which denotes a univalent saturated group which contains one nitrogen heteroatom, the rest are carbon atoms, when the dotted line is absent or is absent when the dotted line denotes a double bond; R6 is absent, when the dotted line denotes a double bond; R7 denotes Cl or NReRf, where Re and Rf denotes H or C1-6-alkyl, or Re and Rf together with the nitrogen atom to which they are bonded form a 6-member heterocycloalkyl which denotes a univalent saturated group containing one or two heteroatoms selected from nitrogen, oxygen, the rest are carbon atoms; which can be substituted with C1-6-alkyl, or R6 and R7 together form a C=O group, when the dotted line is absent; B denotes halogen, C1-6-alkoxy, (CRiiiRiv)n-phenyl; Ri and Rii denote H, C1-6-alkyl -C(O)-C1-6-alkyl; Riii and Riv denote C1-6-alkyl; m equals to 1 or 2, n equals 0 or 1; as well as to pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition, as well as to use of compounds of formula (I), (I-a) or (1-b).

EFFECT: obtaining novel biologically active compounds having activity on V1a receptor.

12 cl, 48 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine and concerns methods of treating diseases with using VEGF antagonists. Substance of the invention involves application of a VEGF antagonist containing VEGFR1R2-FcΔ C1 (a) SEQ ID NO:4 in preparing a drug for hypertension reduction, in treating the diseases associated with administering the VEGF antagonist where the treatment is conducted by subcutaneous introduction.

EFFECT: advantage of the invention consists in reducing side effects associated with treating the diseases by administering the VEGF antagonist.

8 cl, 3 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmacology and deals with method of obtaining microspheres from biodegradable polymer, including: addition of organic solvent to polymer, obtaining polymer solution (stage 1); dispersion of glucose level-regulating peptide in stage 1 polymer solution, obtaining medication dispersion and mixing alcohol or mixture of alcohol and organic acid with medication dispersion, obtaining solution with dispersed in it medication (stage 2); and obtaining microsphere from solution with dispersed in it stage 2 medication (stage 3), where glucose level-regulating peptide represents exedin-4 and where biodegradable polymer is selected from group, consisting of poly-L-lactic acid, D-lactic acid and glycolic acid copolymer, L-lactic acid and glycolic acid copolymer and D,L-lactic acid and glycolic acid copolymer.

EFFECT: invention ensures obtaining microsheres which demonstrate neither initial burst effect nor incomplete release, ensure release of medications of zero order and high efficiency of incapsulation and high stability.

13 cl, 15 ex, 7 tbl, 5 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel oxadiazole compounds of formula (1) and pharmaceutically acceptable salts thereof, where R1 and R2 assume values given in the description, Y is a single bond. The invention also relates to use of said compounds as DGAT1 inhibitors, for example for treating obesity and diabetes, and a method of inhibiting.

EFFECT: high treatment efficiency.

13 cl, 65 tbl, 712 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I, which are HSP90 (heat-shock proteins) inhibitors and can be used to prepare a medicinal agent for treating tumorous diseases affected by HSP90 inhibition. In formula I R1 denotes Hal, H, OA or A, R2, R3 each independently denotes -O-(X)s-Q, -NHCO-(X)s-Q, -CONH-(X)s-Q, -NH(CO)NH-(X)s-Q, -NH(CO)O-(X)s-Q, -NHSOr(X)s-Q, NHCOA, Hal, Het or H, where, if R2=H, then R3≠H, or if R3=H, then R2≠H, R4 denotes H, R5 denotes H, Hal, A, OA, (CH2)nCOOH, (CH2)nCOOA, O(CH2)oCONH2, NHCOOA, NHCO(CH2)nNH2, NHCONHA or O(CH2)oHet1, A denotes a straight or branched alkyl containing 1-10 carbon atoms, in which 1-5 hydrogen atoms may be substituted with F, Cl and/or Br, X denotes a straight or branched C1-C10 alkylene which is unsubstituted or substituted once, twice or thrice by A, O A, OH, Hal, CN, COOH, COOA, CONH2, NH2, NHCOA, NHCOOA, Q denotes H, Ar or Het, Ar denotes phenyl which is unsubstituted or substituted once, twice or thrice with A, OA, OH, NO2, Hal, CN, (CH2)nCOOH, (CH2)nCOOA and/or tetrazole, Het denotes a cyclic saturated or aromatic 5-6-member heterocycle containing 1-2 N and/or O atoms, optionally condensed with a benzene ring which may be substituted once, twice or thrice with A, OA, OH and/or =O (carbonyl oxygen), Het1 denotes a monocyclic saturated, unsaturated or aromatic heterocycle containing 1-2 N and/or O atoms, which may be mono- or disubstituted with A, OA, OH, Hal and/or =O (carbonyl oxygen), Hal denotes F, Cl, Br or I, n equals , 1, 2, 3 or 4, o equals 1, 2 or 3, s equals 0, 1 or 2.

EFFECT: high efficiency of using said derivatives.

4 cl, 4 dwg, 1 tbl, 29 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to pharmaceutical compositions containing a peptide and propylene glycol, to methods of preparing such compositions, and also concerns methods of reducing contamination of injection devices by a peptide composition and reducing sediment formation in the production equipment during manufacturing of the peptide composition. The agonist GLP-1 is used as said peptide in the composition.

EFFECT: reduced contamination of the injection devices during injection.

23 cl, 6 ex, 7 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, and concerns a method of body weight reduction, diabetes treatment, HbAlC level decrease or plasma glucose level decrease on an empty stomach by the use of exendin or an exendin agonist analogue.

EFFECT: invention provides a specific plasma level (170 pg/ml to 290 pg/ml) of exendin or its agonist analogue for at least 1 month.

19 cl, 1 ex, 3 dwg, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to cardiology and endocrinology, and concerns treating the patients with chronic cardiac failure compromised by type 2 diabetes. That is ensured by the additional introduction of the selective β1 adrenoceptor antagonist nebivolol in a single dose 5-7.5 mg/day within 12 months with underlying ACE inhibitor and diuretic therapy in the patients with a higher level of basal glycemia by more than 4.5 mmol/l and preserved LVEF by more than 52 %.

EFFECT: method provides effective treatment in the given group of patients due to ability of nebivolol to improve nitrogen oxide synthesis by a vascular endothelium and to provide normalising haemodynamic, metabolic, anti-ischemic and immune-correcting action.

1 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention is related to alimentation, in particular - to a method and composition for improvement of glucose and insulin balance. Proposed is a compound that includes: a protein source, a fat source and a carbohydrate source, the protein source to the fat source ratio being approximately 1:1:1, each source accounting for 15% - 45% of the total calorie content of the compound. The fat source accounts for approximately over 2% of the total calorie content of the composition in the form of linoleic acid (18:2). According to an alternative version, the food compound for normalisation of insulin and glucose in the organism contains a protein source, a fat source and a carbohydrate source at a ratio of 1:1:1, each of these components accounting for approximately a third of the total calorie content of the compound. Additionally proposed are a diet for enhancement of sensitivity to insulin, a method to reduce resistivity to insulin, a method to reduce insulin levels in the plasma during after dinner time, a method to delay occurrence of insulin in one's blood and a method to increase fat clearance during after dinner time envisaging usage of the above food compound.

EFFECT: invention allows to improve glucose regulation and insulin effect.

68 cl, 34 dwg, 38 tbl

FIELD: medicine.

SUBSTANCE: in formula (I) , the ring A represents 6-members aryl or 5-6-members heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulphur; Q means C3-8 cycloalkyl, 5-6-members heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulphur, C1-6 alkyl or C2-6 alkenyl; the ring T represents 5, 6, 9 or 10-members heteroaryl or 9-members heterocycle optionally additionally substituted by 1-3 heteroatoms independently selected from nitrogen or sulphur. The values of other substitutes are specified in the patent claim. Also, the invention refers to methods for preparing oxime derivatives of general formula (I), to pharmaceutical compositions containing the compound of the invention as an active ingredient and to applications of the compounds of the invention in preparing a drug.

EFFECT: compounds of the invention exhibit properties of a glucokinase activator.

33 cl, 1499 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds - benzoquinone derivatives of formula (I): , where each of R1 and R2 is O-C(O)phenyl; where the phenyl is substituted with 1 substitute selected from halide, nitro, C1-C6 alkyl or C1-C6 alkoxy, and pharmaceutically acceptable salts thereof.

EFFECT: low activity of pancreatic lipase based on compounds of the said formula.

6 cl, 3 tbl, 23 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed is application of biologically active substance for production of medication for treatment of syndrome of resistance to insulin, diabetes, including type I diabetes and type II diabetes, syndrome of ovary polycystosis, treatment or reduction of probability of atheroslerosis development, arterioslerosis, obesity, hypertension, hyperlipidemia, fatty infiltration of liver, nephropathy, neuropathy or retinopathy, feet ulceration or cataracts associated with diabetes, where medication represents compound of formula , as well as corresponding treatment method, pharmaceutical composition and biologically active substance of the same purpose.

EFFECT: increase of compound activity: 75% reduction of glucose level with loading in contrast to 10% reduction for analogues known before, as well as reduction of level of triglycerides in blood serum.

17 cl, 1 dwg, 2 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, and concerns a EP2 agonist which exhibits the EP3 agonist action, and induce a neurotising and/or protective effect and thereby is effective as a therapeutic agent for a peripheral nerve disease, such as lower and upper motor neuron disorder, nerve root disease, plexopathy, brachial plexus compression syndrome, peripheral neuropathy, neurofibromatosis and nervomuscular conduction disease.

EFFECT: EP2 agonist which exhibits the EP3 agonist action; it is a safe and effective neurotisation and/or protection agent which has an insignificant impact on the cardiovascular system.

13 cl, 36 ex, 1 tbl

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