Method of normalising functional reactivity of cardiovascular system in arterial hypertension, impaired glucose tolerance and abdominal obesity

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) in arterial hypertension, impaired glucose tolerance and abdominal obesity. That is ensured by estimating the condition of functional reactivity of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after load by formula: FRI=(BPav.dyn. × HR)×100(standard units). The post-load FRI increment more than by 20 standard units requires the integrated treatment including individually prescribed hypocaloric diet calculated by considering sex, age and body weight, rationally graduated static and dynamic physical activity, administration of irbesartan 150 mg once a day in the morning and pioglitazone 30 mg once a day in the morning at least within 4 months.

EFFECT: complex drug-induced and drug-free therapy combined with empirically prescribed treatment length provides normalisation of functional reactance of the CVS in the given group of patients due to potentiation of therapeutic effect of separate components of an individual care.

1 ex

 

The invention relates to medicine, cardiology, and can be used in therapeutic departments of clinics and hospitals. Analogues of the method of normalization of the functional reactivity of the cardiovascular system with arterial hypertension (AH) with impaired glucose tolerance (IGT) and abdominal obesity (AO) does not exist.

The aim of the invention is to increase the efficiency of correction of the functional reactivity of the cardiovascular system in AG with IGT and AO.

The essence of the proposed method of correction of the functional activity of the cardiovascular system is to increase the tolerance of patients with arterial hypertension with IGT and AO to emotional stress and increase functional reactivity of cardiac-vascular system in the execution of their metered emotional load and reducing the risk of cardiovascular complications during emotional stress, measured after holding dosed emotional load with the ever increasing speed for 18-20 minutes with every minute registration parameters of Central hemodynamics: arterial systolic pressure (SBP), diastolic blood pressure (Add), arterial pressure medium dynamic Map. Dean) and heart rate (HR), determine the value of showing the El functional reactivity (FIU), which is the work of the AD medium dynamic on heart rate, calculate the relative increment values FIU when performing load compared with the value at rest and largest values FIU assess the type of functional reactivity of the cardiovascular system: when the FIU is more than 20 usled reactivity assessed as hyperfunctional (with AG in combination with IGT and AO), the FIU is less than 10 usled response to the load estimate as Hypo-functional and, when values of the FIU from 10 to 20 usled type functional reactivity assessed as normal.

Time psychoemotional load no more than 20 minutes. To normalize the indicator functional reactivity in patients with IGT and JSC uses a combination of individualized low-calorie diet, rationally dosed static and dynamic physical loads, irbesartan and pioglitazone for at least 4 months.

The inventive method is carried out as follows. The value of the FIU is determined by Lebedeva OD, Radziejewski S.A., Bugaeva S.A. Method of assessment of the functional reactivity of the cardiovascular system EN 2207044. The patient is seated in front of the screen. The patient on the left shoulder impose cuff for measuring blood pressure catolicismo is, arterial pressure diastolic arterial pressure medium dynamic and heart rate prior to loading and during loading. The patient offer two sets of 4 letters: 'ÀNEU and BLOG, of which he must choose to remember one. After registration of the hemodynamic parameters within 3 minutes and the memory (30) of the selected set of letters begin conducting psycho-emotional loads, namely, that the subject pressing notes scattered letters from the selected set of progress on the monitor screen square frames situated in a random sequence the letters of the alphabet. The speed of advancement of the frames in the series of letters in the process of conducting samples increases with 3 letters 1 at the beginning of the load up to 6 letters 1, starting from 6 min load, and this provides a gradual vrabatavaemomu patient. Errors in elevation of letters from a selected set of auditory signals, for which the subject may be oriented in the proper execution of the load and try to adjust its execution. After the load calculates the average value of the BPA, Add, Map. Dean and heart rate in the periods: prior to loading and during loading. HELL the average dynamic calculated by the formula: Adsin=Add+[0,42(SBP-Add)].

HELL the average dynamic is a complex result of yuusha all variables HELL. The test with emotional stress in healthy individuals the HELL the average dynamic changes slightly, and the heart rate usually increases. According to the study, increased heart rate and HELL leads to increased demand of oxygen and increase its energy costs. In pathology, for example, when AG with IGT and Autonomous vessels in a state of spasm, unable to provide the required increased amount of oxygen, which may result nanostate hypoxia, be coming the cerebral circulation, etc.

On the basis of the data used to calculate the functional reactivity, which allows an integrative measure of the increase in hemodynamic load on the heart and, consequently, the risk of developing cardiovascular complications, defined as follows:

FIU=(Adsens)*/100(used)

The increment values FIU during the transition from rest to execution of the load determines the index:

FIU=PFR-PFR,

where the FIU is the dierence between the values of the FIU before and during loading

PFR - averaged value of the index before load

PFR - averaged value of the index under load.

The relative increment values FIU assess the type of functional reactivity of the cardiovascular system: if the value is *, then divide 100 to obtain conventional units (used - the double digits).

When you study in the dynamics of treatment the patient was given to remember a different set of letters in order to prevent addiction.

When the increment values after conducting dosed emotional load FIU from 10 to 20 usled functional type of reactivity is assessed as normal. When the FIU to load more than 20 usled type functional reactivity assessed as hyperfunctional. In this case the patient AG with IGT and AO must be assigned at least 4 months a combination of individualized low-calorie diet, measured static and dynamic physical loads, irbesartan 150 mg in the morning of 1 times and pioglitazone 30 mg in the morning 1 times.

To create a negative energy balance in the body of patients they can as an option be recommended following an individually customized low-calorie diet.

Calorie daily diet individually for each patient is calculated in kcal by 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 60 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 coefficient remains is izmenenii with minimal physical activity is multiplied by 1.3 in moderate and 1.5 - high physical activity (usually in patients with hypertension, IGT and JSC physical activity level low).

It is recommended that 3 main meals and 2 intermediate. With regular skipping one meal significantly increases the incidence of obesity, also revealed a positive correlation between obesity and skipping Breakfast. 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, the use of which can be as one of the options in the form below.

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 waking up to Breakfast in a ventilated premises of the Institute. 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, patients are recommended treatment and preventive exercises. Depending on the initial fitness may n the applicatio at the beginning of lightweight option exercise, then the enhanced version.

2. Complexes of preventive and curative gymnastics for persons suffering from hypertension with IGT and JSC

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.

Exercise 6. Standing, feet apart, hands in front of chest with palms down. With a turn of the body weight and hand in hand with turning the palms up - the 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 the leg at the knee and pressed his hands to his stomach exhale. 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. The walk is quiet with a steady breath average depth of 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 son-in-law in the supine position; (e) self-massage of the abdomen small polukrugom movements clockwise - 1-2 minutes Rest 2 min; W) quiet breathing; C) exercise the protrusion (calm) and retraction (active) abdominal wall. Retraction alive is and 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 apart, 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 to 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 quiet breathing average depth of 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) proprietary with subsequent lifting in socks and tension legs. The exercise is performed 4-6 times with possibly large trowel napryazheniem, and 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 the average depth of 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 stretch the legs. To repeat such a circular motion feet 3-6 times in each direction of paperman is. 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 direction.

Exercise 26. Standing, feet apart at shoulder width, hands on the 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

Sick AG with IGT and AO is the patient 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 with IGT and AO should be implemented by the distribution of physical activity in small doses throughout the day. This method of increasing the physical activity of patients should be considered as a method of fractional loads.

Depending on the real conditions of life of patients 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

Panel shall Znanie 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 services, cleaning, gardening work, and others).

Timely and effective correction of the FIU in patients with IGT and JSC will allow in the short term to normalize the functional reactivity of the cardiovascular system is s, that will reduce these patients the period of temporary disability, renders prophylactic action against strokes and heart attacks, reduce the number of outputs on disability and reduce mortality among patients with hypertension with IGT and AO.

Example. Examined the patient With. 48 years old, suffering from hypertension of II degree, stage II with IGT, JSC for 8 years. In the study of hemodynamics in the initial state before conducting psycho-emotional loads the BPA was equal to 144 mm Hg, Add - 92 mm Hg, Adsin - 113,8 mm Hg, heart rate of 78 beats per 1 minute FIU before psychoemotional load was equal 88,7 used When conducting psycho-emotional loads BPA increased to 168 mm Hg, Add - 105 mm Hg, Adsin to 131, 5mm mm Hg, heart rate is up to 92 beats per 1 minute, the FIU is increased to 120,9 used, i.e. the increment of the FIU on the load or what is the same - FIU, was 32.2 used (from 88.7 to 120,9 used), which can be considered as a manifestation of hyperthyroidism cardiovascular system. The patient is assigned to a combination of individualized low-calorie diet, rationally dosed static and dynamic physical loads, irbesartan 150 mg in the morning and pioglitazone 30 mg in the morning. After 4 months of treatment, the magnitude of the FIU fell before the load compared to the same before the treatment: the BPA - up to 130 mm Hg, Add - up to 82 mm Hg, Adsin up to 102.2 mm Hg, heart rate of 70 beats per 1 minute, FIU - to 71.5 used When performing load-mark the expected decrease compared with the condition before treatment the increase in value of the BPA - to 142 mm Hg, Add - up to 88 mm Hg, Adsin to 110,6 mm Hg, heart rate of 80 beats per 1 minute, FIU - to 88.5 used, that is marked increment values FIU, or FIU, 17 used (before treatment - 32.2 used), which may be indicative of increased tolerance of the cardiovascular system to psycho-emotional stress, about the reduction of hyperthyroidism cardiovascular system and, consequently, about the economization of cardiac activity.

As a result of application of the proposed method of correction of functional reactivity of the cardiovascular system in patients with IGT and AO is achieved normalization of the functional reactivity of the cardiovascular system for dosed psycho-emotional stress, which allows the use of the method for normalization of tolerance AH patients with IGT and AO to psycho-emotional stress, which can reduce the degree of hemodynamic load when exposed to stress, reducing the risk of development of psycho-emotional loads adverse cardiovascular reactions (angina, myocardial infarction, ischemic, and others).

The method of normalization of the functional reactivity of the cardiovascular system (CVS) in hypertensive patients with impaired glucose tolerance and abdominal obesity, including assessment of functional p is the activity of SSS during emotional stress, why register systolic, diastolic, srednetehnicheskoe pressure (Adsin.), heart rate (HR), on the basis of these indicators define the indicator functional reactivity (FIU), and with increasing values FIU after load of more than 20 usled implement a comprehensive treatment, including a personalised low-calorie diet, calculated in kcal by the formula:
for women 18-30 years (0,621 ∙ body weight, kg + 2,0357)∙ 240,
31-60 years (0,0342 ∙ body weight, kg + 3,5377)∙ 240,
over 60 years of age (0,0377 ∙ body weight, kg + 2,7545)∙ 240,
for men 18-30 years (0,630 ∙ 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,
rationally dosed static and dynamic physical loads, the introduction of irbesartan 150 mg 1 every morning and pioglitazone 30 mg 1 every morning, for at least 4 months.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) in arterial hypertension and impaired glucose tolerance. That is ensured by estimating the condition of functional reactivity of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure (BPav.dyn.) and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after stress by formula: FRI=(BPav.dyn. x HR)/100(standard units). The post-load value PFR increased more than by 20 standard units requires the complex therapy including graduated static and dynamic physical activity, and introduction of irbesartan in a dose 150 mg in the morning once a day and pioglitazone in a dose 30 mg in the morning once a day at least within 4 months.

EFFECT: complex of drug-induced therapy combined with physical activity and empirically prescribed treatment length provides normalisation of functional reactivityof the CVS in the given group of the patients due to potentiation of therapeutic effect of the used drugs.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, particularly to cardiology, and concerns normalising the functional responsiveness of cardiovascular system in arterial hypertension and dyslipidemia. That is ensured by estimation of the functional responsiveness of CVS while psychoemotional stress to record systolic, diastolic, average dynamic blood pressure (BPav.dyn.) and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after stress by formula: FRI=(BPav.dyn. × HR)/100 (standard units). The after-stress FRI increment by more than 20 standard units require the integrated therapy involving swimming in a swimming pool for at least 20 minutes a day, morning hygienic and therapeutic gymnastics within a day, graduated physical exercises within a day and administration of losartan in a dose 50 mg once a day in the morning. The therapeutic course is at least 4 months.

EFFECT: integrated pharmacotherapy and drug-free modalities combined with empirically prescribed treatment length provides normalised functional responsiveness of CVS in the given group of patients due to potentiation of therapeutic effect of separate components of the integrated treatment.

1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new crystalline modifications of N-α-(2,4,6-triisopropylphenylsulphonyl)-3-hydroxyamidino-(L)-phenylalanine-4-ethoxycarbonyl piperazide and/or its salts. Such crystalline modifications have high stability particularly at low hygroscopicity compared to known amorphous forms of the compound.

EFFECT: invention relates to a method of obtaining such new crystalline modifications, to pharmaceutical compositions containing these new crystalline modifications and their use as an anti-tumour agent.

26 cl, 7 tbl, 13 ex, 20 dwg

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) at arterial hypertension and abdominal obesity. To that end, the state of CVS functional reactivity at psychoemotional stress is assessed by recording systolic, diastolic and average dynamic blood pressure (BP av.dyn) and heart rate (HR). These data serve as the basis for determining functional reactivity index (FRI) prior to and after the stress, according to the following formula: FRI = (BP av.dyn. × heat rate)/100 (conv. un.). If FRI value after stress rises by more than 20 conventional units, complex therapy is implemented including individual hypocaloric diet calculated by a formula considering sex and age, sensibly graded static and dynamic physical exercise as well as administration of irbesartan in a dose of 50 mg once a day, in the morning, over at least 4 months.

EFFECT: complex of drug and non-drug treatment combined with empirically chosen course duration ensures normalisation of CVS functional reactivity among the specified group of patients due to potentiation of certain components of the therapeutic complex.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) at arterial hypertension and abdominal obesity. To that end, the state of CVS functional reactivity at psychoemotional stress is assessed by recording systolic, diastolic and average dynamic blood pressure (BP av.dyn) and heart rate (HR). These data serve as the basis for determining functional reactivity index (FRI) prior to and after the stress, according to the following formula: FRI = (BP av.dyn. × heat rate)/100 (conv. un.). If FRI value after stress rises by more than 20 conventional units, complex therapy is implemented including individual hypocaloric diet calculated by a formula considering sex and age, sensibly graded static and dynamic physical exercise as well as administration of losartane in a dose of 50 mg once a day, in the morning, over at least 4 months.

EFFECT: complex of drug and non-drug treatment combined with empirically chosen course duration ensures normalisation of CVS functional reactivity among the specified group of patients due to potentiation of certain components of the therapeutic complex.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology, and concerns normalisation of cardiovascular system (CVS) functional reactivity among patients suffering from arterial hypertension at the stage of recovery form cerebral circulation disorder without pareses or paralyses. To that end, the state of CVS functional reactivity at psychoemotional stress is assessed by recording systolic, diastolic and average dynamic blood pressure. These data serve as the basis for determining functional reactivity index (FRI) prior to and after the stress, according to the following formula: FRI = (BP av.dyn. × heat rate)100 (conv. un.). If FRI value after stress rises by more than 20 conventional units, telmisartan and labetalole are administered in doses of 40 mg per day and 200 mg twice a day respectively.

EFFECT: method normalises functional reactivity of cardiovascular system and increases tolerance to psychoemotional stresses at the specified group of patients during a 2 month course of therapy.

2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of perindopril of formula I: . Also proposed are methods for synthesis of amorphous and crystalline perindopril using starting substance in form of stereospecific amino acid, N-[(S)-carbethoxy-1-butyl]-(S)-alanine, which is protected by a trimethylsilyl group and converted to reactive acid chloride using thionyl chloride or its complex with 1-H-benzotriazole (1:1), which reacts with (2S, 3aS, 7aS)-octahydroindole-2-carboxylic acid, having a protected carboxy group. The invention also relates to a pharmaceutical composition based on the said crystalline form of perindopril.

EFFECT: novel form of perindopril is obtained, which can be used in medicine for treating cardiovascular diseases.

8 cl, 4 dwg, 7 ex

FIELD: medicine.

SUBSTANCE: therapeutic course involves examination that implies photography of eye-ground vessels and measurement of diametre of retinal vessels on an empty stomach of the patient prior to and after administration of a medicine. Observed increase in diametre of supero-temporal branch of central retinal artery at a distance of one vertical diametre of disk of optic nerve from an edge of disk of optic nerve by 10% and more from the initial one ensures to diagnose efficiency of the administered medicine. The absence of increase in diametre of supero-temporal branch of central retinal artery by 10% and more in administration of the same dosage of the medicine enables to diagnose development of tolerance.

EFFECT: method extends range of means to determine antihypertensive drug tolerance.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

or

or to their pharmaceutically acceptable salts, where ring A, R2, R3, R4 and X are as defined in the description. The disclosed compounds are useful as 11βHSD1 inhibitor. The invention also relates to a pharmaceutical composition, an agent for treating or preventing pathology related to glucocorticoids, a 11βHSD1 inhibitor containing the disclosed compound or its pharmaceutically acceptable salt, and use of the disclosed compounds.

EFFECT: compounds are highly effective.

40 cl, 48 tbl, 191 ex

FIELD: chemistry.

SUBSTANCE: invention relates to an improved method of producing 2H-1-benzopyran-2-methanol-α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-[2R*[R*[R*(S*)]]]], i.e. a nebivolol base of formula (IX), or its hydrochloride salt

as well as to a method of producing an intermediate compound - benzylated nebivolol of formula (VIII),

EFFECT: invention also relates to a pharmaceutical composition with antihypertensive action without using a wetting agent, and to a tablet containing this pharmaceutical composition.

21 cl, 20 tbl, 21 ex

FIELD: medicine.

SUBSTANCE: invention concerns normalising functional reactivity of cardiovascular system (CVS) in arterial hypertension, dyslipidemia, impaired glucose tolerance and abdominal obesity. That is ensured by estimating the condition of functional reactivity of the CVS in psychoemotional load, with recording systolic, diastolic, average dynamic pressure (PBav.dyn.) and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after stress by formula: FRI=(BPav.dyn. x HR)/100 (standard units). The post-load value PFR increased more than by 20 standard units requires the complex therapy including individually prescribed hypocaloric diet calculated by formula considering sex and age, rationally graduated static and dynamic physical activity, and introduction of losartan in a dose of 50 mg once in the morning, and pioglitazone in a dose of 30 mg once in the morning at least within 4 months.

EFFECT: such complex drug-induced and drug-free therapy combined with empirically prescribed treatment length provides normalisation of functional reactance of the CVS in the given group of the patients due to potentiation of therapeutic effect of separate components of an individual care.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) in arterial hypertension and impaired glucose tolerance. That is ensured by estimating the condition of functional reactivity of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure (BPav.dyn.) and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after stress by formula: FRI=(BPav.dyn. x HR)/100(standard units). The post-load value PFR increased more than by 20 standard units requires the complex therapy including graduated static and dynamic physical activity, and introduction of irbesartan in a dose 150 mg in the morning once a day and pioglitazone in a dose 30 mg in the morning once a day at least within 4 months.

EFFECT: complex of drug-induced therapy combined with physical activity and empirically prescribed treatment length provides normalisation of functional reactivityof the CVS in the given group of the patients due to potentiation of therapeutic effect of the used drugs.

1 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts and esters. The disclosed compounds have LXR-alpha and/or LXR-beta agonist properties. In formula (I) R1 is hydrogen, halogen; R2 is lower alkyl, flouro-lower alkyl; R3 is hydrogen, phenyl; R4 is hydrogen, hydroxy; R5 is hydrogen; phenyl; R6 is phenyl, a 5-6-member heteroaryl with one or two heteroatoms selected from nitrogen and sulphur, a 9-member bicyclic heteroaryl with a sulphur atom as a heteroatom, which can be optionally substituted with a halogen, or R6 is , R7 is a lower alkyl; R8 is phenyl which is optionally substituted with one substitute selected from a group consisting of halogen, fluoro-lower alkyl, R9-O-C(O)-, R10R11NC(O)-, phenyl-lower alkoxy; R9, R10, R11 independently represent hydrogen or lower alkyl; L is a single bond, lower alkylene or lower alkenylene; m assumes values from 0 to 3; n is equal to 0 or 1.

EFFECT: obtaining a new compound and a pharmaceutical composition which contains the disclosed compound as an active ingredient for therapeutic and/or preventive treatment of diseases.

23 cl, 47 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel hexafluoroisopropanol substituted derivatives of cyclohexane of formula (I) with LXRα- and/or LXRβ agonist modulation properties, as well as to their pharmaceutically acceptable salts. In formula (I) R1 denotes hydrogen, lower alkyl, fluoro-lower alkyl, lower alkyl-carbonyl, fluoro-lower alkyl-carbonyl, phenyl-lower alkyl, C3-C6-cycloalkyl-lower alkyl, C3-C6-cycloalkylcarbonyl or C3-C6-cycloalkyl-lower alkyl-carbonyl; R2 denotes hydrogen or lower alkyl; R3 denotes lower alkyl, phenyl-lower alkyl, where phenyl is possibly substituted with lower alkoxycarbonyl, lower alkoxycarbonyl, or if X represents a single bond and m is not equal to 0, R3 can also denote a hydroxy group; R4 denotes phenyl or heterocyclyl, where heterocyclyl is a five-member aromatic heterocyclic ring containing two heteroatoms selected from nitrogen and sulphur, optionally substituted with 1-3 substitutes independently selected from a group which includes lower alkyl and halogen; X denotes a single bond, SO2, CO or C(O)O; m equals 0, 1, 2 or 3; n equals 0 or 1. The invention also relates to a pharmaceutical composition containing formula (I) compounds.

EFFECT: novel compounds have useful biological properties.

20 cl, 35 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula , where Qa is phenyl or heteroaryl, and Qa can possibly carry 1 or 2 substitutes selected from hydroxy, halogen, amino, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkylamino and di-[(1-6C)alkyl]amino; R1 and R2 are each independently selected from hydrogen and (1-6C)alkyl; Qb is phenyl or heteroaryl, and Qb can possibly carry 1 or 2 substitutes selected from hydroxy, halogen, (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)alkoxy, (1-6C)alkoxycarbonyl, amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, amino-(1-6C)alkyl, (1-6C)alkylamino-(1-6C)alkyl, (1-6C)alkylthio, (1-6C)alkylsulfinyl and (1-6C)alkylsulfonyl; where any of the substitutes Qa and Qb defined above, containing a CH2 group which is bonded to 2 carbon atoms, or a CH3 group bonded to a carbon atom, can possibly carry on each of the said CH2 or CH3 group one or more substitutes selected from hydroxy, amino, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkylamino and di-[(1-6C)alkyl]amino; where heteroaryl is an aromatic 5- or 6-member monocyclic ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulphur, and can be condensed with a benzene ring or a five-member nitrogen-containing ring containing 2 nitrogen atoms; as well as pharmaceutically acceptable salts thereof. The invention also relates to a method of producing formula I compounds, a pharmaceutical composition and use of these compounds for treating conditions mediated by effect of TNF cytokines.

EFFECT: more effective treatment.

13 cl, 3 tbl, 46 ex

FIELD: medicine.

SUBSTANCE: invention concerns derivatives of thiazolidine-4-one of general formula (I) and general formula (II), to their isomers and pharmaceutically acceptable salts which can be used as a medical product with immunosuppressive activity. In formulae (I) and (II), R1 and R14 independently represent lower alkyl, lower alkenyl; cycloalkyl; 5,6,7,8-tetrahydronaphth-1-yl; phenyl group or phenyl group independently mono- or disubstituted with lower alkyl, halogen, lower alkoxy or group -CF3; R2 and R15 independently represent lower alkyl; allyl; cyclopropyl; or di- lower alkylamino; R3 represents -NR5R6 or -O-CR7R8-CR9R10-(CR11R12)n-O-R13; R23 represents hydrogen; hydroxycarbonyl-lower alkyl or 1-glyceryl. Values of the other radicals are specified in the patent claim. The invention also concerns application of one or more compounds of general formula (I) or (II) for preparation of a medical product with immunosuppressive activity.

EFFECT: agent exhibits improved efficiency.

24 cl, 1 tbl, 157 ex

FIELD: medicine.

SUBSTANCE: in formula (1), R1 is di-C1-6alkoxyphenyl group; A is one of the following groups (i)-(vi); (i) -CO-B-, where B is C1-6alkylene group; (ii) -CO-Ba-, where Ba is C2-6alkenylene group; (iii) -CH(OH)-B-; (iv) -COCH((C)OOR3)-Bb-, where R3 is C1-6alkyl group and Bb is C1-6alkylene group. Values of the other radicals are specified in the patent claim. Invention also concerns the pharmaceutical composition exhibiting properties of a phosphodiesterase PDE4 inhibitor containing the compound under the invention; the phosphodiesterase 4 inhibitor containing as an active component the compound of the invention; preventive or therapeutic preparation for atopic dermatitis containing as an active component the compound of the invention.

EFFECT: higher effectiveness of application of the compound.

8 cl, 24 tbl, 262 ex

FIELD: medicine.

SUBSTANCE: invention includes description of novel pharmaceutical combination, pharmaceutical composition, which includes said combination, application of said combination for obtaining medication and commercial packing. Combination includes (a) at least one anti-inflammatory agent, selected from group, which includes inhibitors of topoisomerase I and inhibitors of topoisomerase II, and (b) epothilone B derivative of formula (I), and optionally at least one pharmaceutically acceptable carrier, for simultaneous, separate or successive application.

EFFECT: obtaining of effective combination for treatment of proliferative disease, namely disease connected with considerable tumor and resistant to other medications.

12 cl

FIELD: pharmacology.

SUBSTANCE: invention deals with formula I compounds and their sals pharmaceutically relevant in the capacity of phosphatidylinositol 3-kinase inhibitors, their preparation method as well as their application for production of a pharmaceutical preparation, a pharmaceutical compounds based thereon and a therapy method envisaging their application. In a formula compound R1 is represented by aminocarbonyl, non-obligatorily displaced with nitrile, or R1 is represented by C1-C8-alkylcarbonyl that is non-obligatorily displaced with hydroxi, carboxi, C1-C8-alcoxicarbonyl, nitrile, phenyl, C1-C8-halogenalkyl or C1-C8-alkyl, non-obligatorily displaced with hydroxi or R1 is represented by C1-C8-alkyl aminocarbonyl alkylcarbonyl that is non-obligatorily displaced with halogen, hydroxi, C1-C8-alkylanimo, di(C1-C8-alkyl)amino, carboxi, C1-C8-alcoxicarbonyl, nitrile, C1-C8-halogenalkyl or C1-C8-alkyl, non-obligatorily displaced with hydroxi or R1 is represented by C1-C8-alkylaminocarbonyl, non-obligatorily displaced with C1-C8-cycloalkyl or R1 is represented by C1-C8-alkylcarbonyl or C1-C8-alkylaminocarbonyl, each of them non-obligatorily displaced with C1-C8-alcoxi, non-obligatorily displaced with hydroxi or R1 is represented by C1-C8-alkylaminocarbonyl, displaced with phenyl, additionally displaced with hydroxi or R1 is represented by C1-C8-alkylcarbonyl that is non-obligatorily displaced with a 5- or 6-membered heterocyclic ring that has 1-4 cyclic nitrogen heteroatom(s) where the ring is non-obligatorily displaced with C1-C8-alkyl on condition that the 6-membered heterocyclic ring is no 1-piperidyl or R1 is represented by C1-C8-alkylaminocarbonyl that is non-obligatorily displaced with a 5- or 6-membered heterocyclic ring that has 1-2 cyclic nitrogen heteroatom(s) selected from among the group consisting of oxygen and nitrogen where the ring is non-obligatorily displaced with C1-C8-alkyl or R1 is represented by -(C=O)-(NH)a-Het, where a stands to denote 0 or 1 and Het stands to denote a 4-, 5- or 6-membered heterocyclic ring that has 1-2 cyclic nitrogen heteroatom(s) where the ring is non-obligatorily displaced with hydroxi, C1-C8-alkyl, C1-C8-alcoxi or a 6-membered heterocyclic ring that has 1-2 cyclic nitrogen heteroatom(s) selected from among the group consisting of oxygen and nitrogen or R1 is represented by -(C=O)-(NH)b-T, where b stands to denote 0 or 1 and T stands to denote C3-C8-cycloalkyl that is non-obligatorily displaced with hydroxi or C1-C8-alkyl displaced with hydroxi or R1 is represented by -(C=O)-(NH)b-T, where b stands to denote 1 and T stands to denote phenyl that is non-obligatorily displaced with C1-C8-alkyl or C1-C8-alkyl displaced with hydroxi, R2 is represented by C1-C3-alkyl; one of R3 and R4 is represented by R6 while the other is represented by R7; R5 is represented by hydrogen or a halogen; R6 is represented by hydrogen, hydroxi, amino, -SOR8, -SO2R8, -SO2NH2, -SO2NR9R10, -COR8, -CONHR8, -NHSO2R8, nitrile, carboxi, -OR8 or C1-C8-halogenalkyl; R7 is represented by hydrogen, R11, -OR11, halogen, -SO2R8, ciano or C1-C8-halogenalkyl or, when R4 is represented by R7, R7 may equally be represented by -NR12R13; R8 and R11 are independently represented by C1-C8-alkyl or C3-C8-cycloalkyl, non-obligatorily displaced with hydroxi, nitrile, amino, C1-C8-alkylamino or di(C1-C8-alkyl)amino; any R9 is represented by C1-C8-alkyl or C3-C8-cycloalkyl, non-obligatorily displaced with hydroxi, C1-C8-alcoxi, nitrile, amino, C1-C8-akrylamino, di(C1-C8-alkyl)amino or 5- or 6-membered heterocyclic ring that has 1-2 cyclic nitrogen heteroatom(s) selected from among the group consisting of oxygen and nitrogen where the ring where the ring is non-obligatorily displaced with C1-C8-alkyl, and R10 is represented by hydrogen or C1-C8-alkyl or R9 and R10 together with the nitrogen atom they are connected to form a 5- or 6-membered heterocyclic ring that has 1-2 cyclic nitrogen heteroatoms where the ring is non-obligatorily displaced with C1-C8-alkyl; any R12 is represented by C1-C8-alkyl or C3-C8-cycloalkyl, non-obligatorily displaced with amino, C1-C8-alkylamino or di(C1-C8-alkyl)amino and R13 is represented by halogen or C1-C8-alkyl or R12 and R13 together with the nitrogen atom they are connected to form a 5- or 6-membered heterocyclic ring that has 1-2 cyclic nitrogen heteroatoms where the ring is non-obligatorily displaced with C1-C8-alkyl.

EFFECT: proposed compounds are to be utilised for treatment of diseases mediated by phosphatidilinozitol 3-kinase such as allergy, psoriasis, diabetes, atherosclerosis, diabetes, cancer.

19 cl, 3 tbl, 181 ex

FIELD: medicine.

SUBSTANCE: there are described 2-(R)-phenylpropionic acid derivatives of formula (1) and their pharmaceutically acceptable salts where R' is chosen from H, OH and provided R' represents H, R is chosen from H, C1-C5-alkyl, C3-C6-cycloalkyl, C1-C3-alkoxy, thiazolyl, substituted CF3, the remained formula -CH2-CH2-Z-(CH2- CH2O)nR', where n is equal to 2, and Z represents oxygen, the remained formula - (CH2)n-NRaRb, the remained formula SO2Rd, provided R' represents OH, R is chosen from C1-C5alkyl. The compounds are applied to inhibit chemotactic activation of neutrophils (PMN leukocytes) induced by interaction of interleukine-8 (IL-8) and membrane receptors CXCR1 and CXCR2. The compounds are applied to prevent and treat the pathologies generated by specified activation. There are also described application of the compounds for manufacturing of medicinal agents for treating psoriasis, nonspecific ulcerative colitis, melanoma, angiogenesis, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and to prevent and treat the damages caused by ischemia and reperfusion, the pharmaceutical composition and method for making the compounds of formula (1) where R' represents H and R - group SO2Rd.

EFFECT: higher clinical effectiveness.

8 cl, 3 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, particularly to cardiology, and concerns normalising the functional responsiveness of cardiovascular system in arterial hypertension and dyslipidemia. That is ensured by estimation of the functional responsiveness of CVS while psychoemotional stress to record systolic, diastolic, average dynamic blood pressure (BPav.dyn.) and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after stress by formula: FRI=(BPav.dyn. × HR)/100 (standard units). The after-stress FRI increment by more than 20 standard units require the integrated therapy involving swimming in a swimming pool for at least 20 minutes a day, morning hygienic and therapeutic gymnastics within a day, graduated physical exercises within a day and administration of losartan in a dose 50 mg once a day in the morning. The therapeutic course is at least 4 months.

EFFECT: integrated pharmacotherapy and drug-free modalities combined with empirically prescribed treatment length provides normalised functional responsiveness of CVS in the given group of patients due to potentiation of therapeutic effect of separate components of the integrated treatment.

1 ex

Up!