Method of reducing spontaneous erythrocyte aggregation in case of dyslipidemia
SUBSTANCE: invention relates to medicine, namely to hematology and cardiology, and can be sued for reduction of spontaneous erythrocyte aggregation in case of dyslipidemia. For this purpose, at the background of hypolipidemic diet, dosed static and dynamic physical exercise and daily swimming for not less than 30 minutes per day, in the middle of the day simvastatin is introduced. Physical exercise includes morning hygienic gymnastics, therapeutic and preventive gymnastics, dosed physical exercise throughout the day. Simvastatin is introduced in dose 10 mg 1 time per day in the evening after meal. Treatment is carried out for 1.5 months.
EFFECT: method makes it possible to normalise spontaneous erythrocyte aggregation during 1,5 months, bringing its level close to that of healthy people, thus favouring prevention of vascular complications in patients with dyslipidemia.
1 tbl, 2 ex
The invention relates to medicine, namely to Hematology and cardiology.
Analogues of the proposed method of reducing the spontaneous aggregation of erythrocytes (SAE) in patients with dyslipidemia (D) does not exist.
For the correction D often be prescribed statins, including simvastatin, in the correction pattern of patients with Dr are often included lipid-lowering diet, physical exercise and swimming.
In preparing this proposal was tasked to develop an effective and affordable way to reduce aggregation of erythrocytes in patients with D, which would solve the problem of correction of D with simultaneous normalization of SAE and thereby prevention in a wide range of patients with D development of myocardial infarction, cerebral stroke and thrombosis of different localization.
When ever medical complex consisting of lipid-lowering diet, individually tailored physical training, swimming in the pool and drug simvastatin, were not used in patients with D to normalize SAE.
The aim of the invention is to increase the efficiency of correction of violations SAE in patients with D.
The essence of the proposed method lies in the fact that for the correction SAE patients On long-term is assigned a complex of lipid-lowering diet, exercise workouts, daily swimming for at least 30 minu day in the middle of the day and of the drug simvastatin 10 mg 1 time in the evening after a meal.
The method allows to correct SAE in patients with D for 1.5 months, translating it to a level close to that of healthy people. Subject to the subsequent recommendations of the proposed method can be maintained SAE, and therefore, the rheology of blood in an optimal state, which will significantly reduce the risk of thrombotic complications, reduce the number of cases of temporary disability, to accelerate and improve the quality of patient treatment, reduce disability, and also to prolong the life and reduce mortality of patients with D from a heart attack, stroke and thrombosis of different localization.
The inventive method is carried out as follows. Taking 9 ml of blood is produced in the morning after a 14-hour fast from Vienna through the thick needle by gravity into a test tube with sodium citrate in the ratio of 9:1 to assess the aggregation of erythrocytes.
Erythrocyte aggregation is assessed by the degree of ability of erythrocytes to spontaneously aggregate (Pokrova O.A., Grineva MR, Ivanov K.S. Methodology and clinical significance, the study of rheological properties of blood // Bulletin of the Ivanovo medical Academy. - 2008. - T13, No. 1-2. - s.89-98).
To assess the aggregation of erythrocytes blood from a vein taken in sodium citrate in the ratio of 9:1 and centrifuged 10 min at 3000 rpm/min In 96-well pad fill 2 holes 0.2 ml plasma survey, which has been created. From the tube removed all the plasma and the layer of leukocytes. Erythrocytes resuspended standard phosphate buffer in the ratio 1:4, followed by centrifugation for 10 min at 3000 rpm, allowing you to wash them from the remnants of the plasma when removing the supernatant. After this is taken as 0.02 ml of erythrocytes and resuspended first filled with autologous plasma-well 96-well Ouija boards, allowing you to get 10% hematocrit. Then from this hole, take a clean, dry pipette 0,02 ml content and placed in the second filled the hole that allows you to get 1% hematocrit. After that 1 grid in the camera Goryaeva fill obtained a suspension of red blood cells, incubated 3 min for the occurrence of spontaneous aggregation and shall count free erythrocytes (including 2 of the erythrocyte together) and units, starting with 3 cells, connected in the form of "monetary columns") in 2 large squares of the camera (lens×40, eyepiece×10). Considered the number of "coin of columns and the number of red blood cells, involved in them.
Based on these results, calculate the following indicators that assess SAE:
1) Average unit size (CPA):
Sea - the sum of all cells in the units;
KA - the number of units
2) the Index of aggregation (PA):
CTU - free number is red blood cells
3) the Percentage of non-aggregated RBCs (PNA):
Normative values for CPA are 4-5, PA 1,05-1,30, for the PNA 80,0-92,0%. The increase in CPA above 5, and PA above 1.30 and lowering the PNA below 80,0% talks about increasing the SAE. In case of violation of at least one of these three indicators in patients with D must be treated according to the inventive method.
The inventive method is carried out as follows.
To reduce the level of lipids in blood of patients assigned patients lipid-lowering diet, the basic principles of which are set out in the table below.
|Featured products (1)||Products, whose consumption should be limited to (2)||The food products that are not recommended (3)|
|Bread||Wholemeal bread, cereals cereals, porridge, pasta, crisp bread, matzo, rice||Crosby, brioches|
|Products every day||Skim milk, cheese with all the ü low fat, for example: peasant cheese or quark, yoghurt with very low fat content, the white of an egg substitutes eggs||Semi-skimmed milk, cheeses with reduced fat content, for example: Brough, Camembert, Eden, Year, feta, yogurt with ricote, low fat, two whole eggs per week||Whole milk, evaporated milk, cream, milk substitutes, fatty cheeses and yogurt|
|Soups||Soups consommé, vegetable soups||Thick soups, meat soups|
|Fish||White fish, oily fish (cooked in the grill, boiled, smoked). Not to eat the skin of the fish (skin sardines, Snetkov)||Fish fried on a suitable oil||Eggs, fish, fried on the unknown or unsuitable oil or fat|
|Seafood||Oysters, scallops||Clams, lobster, shrimp||Shrimp, including serrate, squid|
|Meat||Turkey, chicken, veal, venison, rabbit, lamb||Of all the ü lean veal, ham, bacon, lamb, (one or 2 times a week). Veal, sausages, chicken, liver 2 times per month||Ducks, geese, all kinds of fatty meat, the usual sausages, salami, meat pies, bacon, leather birds|
|Fats||Polyunsaturated oils, such as: sunflower, corn, peanut, soybean; monounsaturated oils (olive, canola). Soft margarine, low fat, made on the basis of these oils||Butter, suet, lard, fat, palm oil, hard Margarines|
|Fruits and vegetables||All fresh and frozen vegetables, especially legumes: beans, dried beans, lentils, peas, corn, boiled potatoes or jacket potatoes; all fresh or dried fruit, canned unsweetened fruit||Fried potatoes, potato flakes, cooked in sunflower oil||Fried potatoes or potato flakes, vegetables or rice, fried on the unknown or unsuitable oil or fat fries, baked chips, pickles (canned vegetables)|
|Dessert||Sorbitol, jellies, puddings n is the basis of skim milk fruit salad, meringue||Ice cream, puddings, dumplings, sauces, prepared on the basis of cream or butter|
|Grocery||Cake, biscuits, cooked in margarine or oil containing unsaturated fats||Factory cake, biscuits, cakes, snacks and puddings|
|Pastry||Oriental sweets, nougat, candy||Marzipan, halva||Chocolate, candy sugar and butter, sweet coconut, candy of burnt sugar and butter|
|Nuts||Walnuts, almonds, chestnuts||Brazil nuts, peanuts, pistachios||Cashew, coconut, salted nuts|
|Drinks||Tea, ground and instant coffee, light diet drinks||Alcohol, liquid chocolate with low fat||Liquid chocolate, Irish coffee, malt beverages with a high content of fat, brewed coffee|
|Seasoning||Pepper, mustard, spices||Salad sauces with low fat||Douliana food, sauces for salads, mayonnaise for salads|
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 waking up to 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 amplit the water movements 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 On recommended treatment and preventive exercises. Depending on the initial fitness may apply at the beginning of the lightweight option, physical activity, and subsequently enhanced option.
2. Complexes of preventive and curative gymnastics for persons suffering from D.
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 gadgets is a great 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 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 the emphasis of 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 down. 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 - ver the return to the starting position and the breath. 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 breathing; C) exercise 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. The enhanced treatment and prevention is gimnastiki.
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 down. 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. On the Lona body forward, touch right brush left toe of the feet, another 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) proprietary 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 straight, keep ravenous the E.
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 to 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 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 Russ is alleny 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 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.
Depending on the conditions of real life patients On to recommend various exemplary embodiments of the fractional loads to increase physical (motor) activity during the day.
Exercise 1. Sitting - dilute the elbows to the sides, inhale, extend hands forward in the ed with 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.
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.
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
Walk the pedestrian varying length.
Physical work in different ways and with different duration depending on the conditions (cleaning, home services, cleaning, gardening work, and others).
The third component of the claimed method is a daily swim in the sea, the river or the pool for at least 30 minutes a day in the middle of the day.
The fourth component of the way of leveling advanced SAE patients D is the purpose simvas the Atina 10 mg 1 time in the evening after a meal.
Example 1. Patient C., 44 years old, suffers D. for 7 years, screened during the follow up inspection regarding the Doctor, The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,5, PA=1,67, PNA=73,0%), indicating that the increase of the AOC.
The patient was recommended lipid-lowering diet, dosed physical load, swimming in the pool at least 30 minutes a day in the middle of the day and simvastatin 10 mg 1 time in the evening after a meal.
After 1 month. it is established that the patient SAE (CPA=4,2, PA=1.07, and the PNA=85,7%) is normalized.
Example 2. Patient K., 58 years old, suffering from D. for 11 years, were examined during the follow up inspection regarding the Doctor, The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,9, PA=1,62, PNA=49,8%), indicating that the increase of the AOC and the risk of thrombosis.
The patient was recommended lipid-lowering diet, measured static and dynamic exercise, daily swimming for at least 30 min a day in the middle of the day, simvastatin 10 mg 1 time in the evening after a meal.
After 1.5 months. treatment indicators aggregation of erythrocytes (CPA=4,4, PA=1,15, PNA=84,0%) normalized, indicating a normalization of the AOC of the patient.
The use of the proposed method of correction is SAE in Hematology and cardiology will help to avoid many of vascular complications in patients with D, to reduce their number of cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality.
The way to reduce the spontaneous aggregation of erythrocytes with dyslipidemia, including the use of lipid-lowering diet, measured static and dynamic physical loads, which includes morning hygienic gymnastics, therapeutic gymnastics, fractional exercise throughout the day, daily swimming for at least 30 min a day in the middle of the day and the introduction of simvastatin 10 mg 1 time in the evening after eating for 1.5 months.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to an ester presented by formula  where R1' represents 1) C1-C6 alkyl which is optionally substituted by one or more identical or different halogens, or 2) -CO-C1-C6 alkoxy; R2' represents 1) hydrogen or 2) C1-C6 alkyl, R3', R4' and R5' are identical or different, and each represents 1) hydrogen, 2) halogen, 3) C1-C6 alkyl which is optionally substituted by one or more identical or different halogens, 4) C1-C6 alkoxy, 5) -COR13' where R13' represents (a) hydroxy, (b) C1-C6 alkyl, (c) C1-C6 alkoxy which is optionally substituted by one or more identical or different substitutes selected from (1) hydroxy, (2) C1-C6 alkoxy which is optionally substituted by phenyl, (3) -NR11'CO-C1-C6 alkyl where R11' represents hydrogen, (4) -CONR8'R9' where R8' and R9' are identical or different, and each represents C1-C6 alkyl, (5) -CO- C1-C6 alkoxy optionally substituted by phenyl, (6) phenyl optionally substituted by one or more identical or different substitutes selected from halogen, C1-C6 alkoxy and -CO-C1-C6 alkoxy, and (7) a heterocycle selected from pyridyl, thienyl and which all can be substituted by one or more identical or different C1-C6 alkyl groups, or (d) -OR19' where R19' represents a group or a group or piperidyl which is optionally substituted by -CO-C1-C6alkyl, 6) a heterocycle selected from oxadiazolyl and tetrazolyl, and said heterocycle is optionally substituted by C1-C6 alkyl optionally substituted by one or more identical or different substitutes selected from -CONR8'R9' (R8' and R9' have the same values as defined above) and -CO-aralkyloxy, or 7) nitrile; R6' and R7' are identical or different, and each represents 1) C1-C6 alkyl or 2) a nitrogen-containing 5 or 6-members saturated heterocycle containing a monocycle formed when R6', R7' and a neighbouring nitrogen atom are taken together, and optionally including oxygen as a heteroatom; Y1, Y2, Y3 are identical or different, and represent, 1) all carbon atoms, or 2) one of Y1, Y2, Y3 represent a nitrogen atom, and the others are carbon atoms; Y4 represent a carbon or nitrogen atom ;-X- represents 1) -(CH2)1 where 1 represents an integer 1 to 3, 2) -CH2-NR18'-CH2- where R18' represents C1-C6 alkyl, or 3) or to its pharmaceutically acceptable salt.
EFFECT: compounds presented by formula are effective as agents for treatment or prevention hyperlipidemia, arteriosclerosis, coronary artery disease, obesity, diabetes and hypertension or similar diseases since they are withdrawn very quickly and exhibit excellent MTP inhibitory activity.
23 cl, 32 tbl, 137 ex
SUBSTANCE: what is offered is a liquid drug characterised by the fact that it contains mixed pumpkin seed oil and water-melon seed oil in the following proportions: pumpkin seed oil 40-70%, water-melon seed oil 60-30%.
EFFECT: invention enables effective and safe normalisation of lipid metabolism in an individual.
5 ex, 1 tbl
SUBSTANCE: invention refers to Trecresan applications as an acid lipase activator.
EFFECT: invention enables extending the range of cholesterol-lowering drugs.
2 tbl, 1 ex
SUBSTANCE: claimed are method of reducing in circulating blood of LDL-cholesterol, triglycerides, total cholesterol and their mixtures, including introduction of efficient amount of one or more phosphate derivatives of one or more electron-transfer agents, which represent monotocopheryl phosphate, dotocopheryl phosphate, monotocotrienyl phosphate, ditocotrienyl phosphate and their mixtures, their application for relief of symptoms, treatment and/or prevention of disease, selected from group which consists of chronic renal failure, primary and secondary hyperemias and dislipemia, retinopathy, enlargement of liver and spleen, xanthomas and their combinations by reduction of lipid content in circulating blood.
EFFECT: reduction under action of claimed tocopherylphosphates of levels of total cholesterol, LDL in mice and reduction in them of atherosclerotic lesions, in people - improvement of dislipidemia state and increase of HDL cholesterol in comparison with tocopherol acetate.
5 cl, 3 dwg, 5 tbl, 2 ex
SUBSTANCE: invention relates to compounds of formula (I) given below or pharmaceutically acceptable salts thereof:
[where: each of X, Y, Z and W independently denotes a methane group which optionally contains substitutes selected from a group of substitutes α, or a nitrogen atom (except when all elements X, Y, Z and W denote a methane group which optionally contain substitutes selected from the group of substitutes α); A denotes -(C(R3)(R4))m1-; B denotes -O-; D denotes -C(O)-; m1 equals 0; Q denotes a methane group or a nitrogen atom; R denotes a group of formula (II)
, where R6 denotes a lower alkyl group; R7 and R8, together with the nitrogen atom with which they are bonded, form a 5-6-member nitrogen-containing aliphatic heterocyclic group; and where the group of substitutes α includes the following substitutes. Group of substitutes α: halogen atom, hydroxyl group, lower alkyl group, alkoxyl group (said group can be substituted with a cycloalkyl group), amino group, mono- or disubstituted lower alkylamino group, aryl group (said group can be substituted with a halogen atom, a -SO2CH3 group), aryloxy group (said group can be substituted with a halogen atom), heteroaryl group, where 'heteroaryl group' denotes a 5- or 6-member monocyclic saturated or unsaturated group containing 1-2 heteroatoms selected from an oxygen atom or a nitrogen atom (said group can be substituted with an alkoxyl group, alkyl group). The invention also relates to a histamine 3 receptor antagonist, histamine 3 receptor inverse agonist, a prophylactic or medicinal agent, as well as a pharmaceutical composition.
EFFECT: obtaining novel biologically active compounds having histamine H3 receptor antagonist or inverse agonist action.
15 cl, 57 ex, 1 tbl
SUBSTANCE: invention refers to new polypeptides of pancreatic polypeptide family ("PPF") and to methods of their application for body weight reduction, triglyceride level decrease and fatty acid β-oxidation intensification with preserving body muscle bulk.
EFFECT: higher efficacy.
38 cl, 4 tbl, 54 dwg (at 57 seets), 10 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present group of inventions refers to medicine, namely to therapy and endocrinology, and concerns blood pressure reduction in metabolic syndrome and pre-hypertension. That is ensured by introduction of a composition containing an effective amount of a polyphenolic grape extract, containing 2 wt % and more of polyphenols having end links of epicatechin-gallate.
EFFECT: grape extract composition containing low concentrations of polyphenol having end links of epicatechin-gallate, and high concentration of mono- and oligomeric compounds, provides effective treatment of said pathology ensured by blood pressure reduction and lipid exchange normalisation.
38 cl, 7 ex, 4 dwg, 8 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new compounds of formula (I): or to their pharmaceutically acceptable derivatives selected from a group consisting of pharmaceutically acceptable salts and esters; in which: R1, R2, R3, R4, R5, R6, R7, R8a, R8b, R8c and R8d are such as presented in the patent claim 1. The invention also refers to compounds of formula (I), to a compounds selected from a group, to a pharmaceutical composition, to methods of treating, to a method of decreasing the plasma cholesterol level in a patient, to a method of modulating cholesterol metabolism, catabolism, synthesis, absorption, re-absorption, secretion or excretion in a mammal, to a method of modulating farnesoid X receptor activity, to a compound representing 3-(3,4-difluorobenzoyl)-1,1-dimethyl-1,2,3,6-tetrahydroazepino [4,5-b]indole-5-isopropylcarboxamide, to a composition, to a method of reducing the risk of an onset or a recurrence, to a method of modulating triglyceride metabolism, catabolism, synthesis, absorption, re-absorption, secretions or excretion in a mammal, and also to a method of modulating bile acid metabolism, catabolism, synthesis, absorption, re-absorption, secretions or excretion in a mammal.
EFFECT: preparation of the new biologically active compounds showing possessing nuclear receptor activity.
73 cl, 76 ex, 3 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to medicine, namely to pharmacology and cardiology, and deals with prevention of lipid exchange disorders. For this purpose, at the background of introduction of lovastatin in average therapeutic dose, additionally, intramuscularly introduced is 3-oxy-6-methyl-2-ethyl-pyridine succinate, also in dose 0.7 mg/kg daily 1 time per day during 10 days.
EFFECT: method ensures prolongation of hypolipidemic effect of lovastatin after its cancelling.
2 tbl, 4 dwg, 2 ex
SUBSTANCE: invention relates to novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidine-2,6-diamines of general formula 1, their pharmaceutically acceptable salts and/or hydrates which have serotonin 5-HT6 receptor antagonist properties and can be used in treating or preventing development of various central nervous system diseases, whose pathogenesis is associated with 5-HT6 receptors, particularly Alzheimer's disease, Parkinson's disease, Huntington disease, schizophrenia, other neurodegenerative diseases, cognitive and anxiety disorders and obesity. In general formula (I): R1, R2 and R4, which are optionally identical, independently denote C1-C3 alkyl; R3 and R4, which are optionally identical, denote: a hydrogen atom, optionally substituted C1-C3 alkyl or acetyl; R5 denotes a hydrogen atom or halogen atom.
EFFECT: high treatment efficiency.
13 cl, 12 dwg, 4 tbl, 12 ex
SUBSTANCE: invention refers to application of nitrogen oxide extracting compounds of formula (1) for treating muscular dystrophies.
EFFECT: higher clinical effectiveness.
4 cl, 2 tbl, 1 ex
SUBSTANCE: for treatment of patients with ischemic heart disease in addition to basic therapy introduced is cudesan in dose 25 drops simultaneously with preductal MB 35 mg 2 times per day during meal for 3 months, with further parenteral introduction of essentiale H in dose 0.5-1 g for 10 days, after that, enterally in dose 1 capsule 3 times per day for 20 days. Course of treatment is repeated 3 times per year.
EFFECT: expressed anti-ischemic effect and normalisation of processes of lipid peroxidation, including in patients with severe affection of coronary channel and expressed diastolic dysfunction of left ventricle.
2 ex, 3 tbl
SUBSTANCE: invention relates to medicine, namely to traumatology and orthopedics and can be used for prevention of commissure formation in case of injury of tendons. For this purpose after finishing tendon plasty sutured tendon and internal surface of paratenon are processed with adhesive "Sulfacrylate".
EFFECT: method makes it possible to prevent formation of commissures between tendon and paratenon in post-operation period without additional introduction of other medications due to formation of biodegradable barrier with prolonged effect.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to field of medicine, namely to cardiology, and can be used for correction of kidney dysfunction in patients with stable stenocardia in combination with hypertension. For this purpose at the background of standard therapy, which includes inhibitor of angiotensin-converting enzyme, beta-adrenoblocker, aspirin and statin, Medicaqtion ivabradin is administered in day dose 5-15 mg in 2 intakes, daily, during 6 months.
EFFECT: method makes it possible to increase efficiency of kidney malfunction correction due to positive dynamics of GFR, level of C-terminal telopeptide type I collagen and TIMP-1.
1 tbl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to certain N-alkylcarbonylaminoacid esters of formula where R1 independently represents hydrogen or methyl; R2 independently represents alkyl C1-C2 and R3 independently represents alkyl C1-C4, offered in the present invention, as well as to compositions and therapies with using the declared compounds.
EFFECT: preparing new compounds which effect on sensory processes.
27 cl, 7 tbl, 2 dwg
SUBSTANCE: invention relates to novel compounds of formula (I), optical isomers or pharmaceutically acceptable salts thereof which can be used to inhibit or block reuptake of 5-hydroxytryptamine (5HT) and/or norepinephrine (NA), as well as for treating diseases associated with the central nervous system, a pharmaceutical composition based on said compounds and use thereof in preparing a medicinal agent. (I), where the chiral centre (*) can be R or S or RS (racemic mixture), R3 and R4 are independently selected from saturated alkyl, having 1-6 carbon atoms, and R1 and R2 are as described in the formula of invention.
EFFECT: high effectiveness of the compounds.
12 cl, 10 tbl, 3 dwg, 15 ex
SUBSTANCE: invention relates to medicine, namely to hematology and cardiology. Method includes administration to patients of complex from hypocaloric diet, dosed static and dynamic physical activity, including morning hygienic gymnastics, preventive medical gymnastics, divided physical exercise throughout the day, daily swimming for not less than 30 min per day in the middle of the day, intake of lisinopril in dose 10 mg 1 time per day in the morning and simvastatin 20 mg 1 time per day in the morning during 2 months. Combined application of all components makes it possible to reduce SEA in patients with AH with AO and D, reducing it to the level close to such for healthy people, during 2 months of treatment.
EFFECT: reduction of spontaneous erythrocyte aggregation (SEA) in case of arterial hypertension (AH) with abdominal obesity (AO) and dyslipidemia (D).
SUBSTANCE: for treating Hashimoto disease, simvastatin Vazilip 20 mg once a day in the evening and cytoprotector Mexicor 0.1 1 capsule 3 times a day on an empty stomach for 3 months are introduced.
EFFECT: method provides effective treatment ensured by immune corrective action indicated by anti-thyroid peroxidase autoantibodies level decrease that maintains a functional potential of a thyroid gland.
SUBSTANCE: ophthalmic composition contains a water carrier ingredient and an effective amount of at least one compatible soluble substance for eye surface protection against hyperosmotic stress where the compatible soluble substance is chosen from a group consisting of carnitine and erythrite. The ophthalmic composition has osmolarity in the range 200 to 1000 mOsmol/kg. Also, the ophthalmic composition can contains glycerine and carboxymethyl cellulose, a preserving agent. The ophthalmic composition delivers compatible soluble substances to eye surface cells to counterbalance an osmotic stress thereon. The composition is applied for manufacturing a drug for eye surface protection against hyperosmotic stress. A method of treating human dry eye keratitis involves administration of said composition.
EFFECT: eye protection in adverse effect of cationic compounds on the eye surface and simplified process of eye restoration following a surgical intervention.
13 cl, 7 tbl, 8 dwg, 20 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to new compounds - ester of retinyl, selected from the group, which consists of ester of 9-cis-retinyl of formula I and ester of 11-cis-retinyl of formula II, where A stands for CH2OR and R is a residue of ester-forming polycarboxilic acid, which is selected from succinic acid, citric acid, keto-glutaric acid, fumarci acid, malonic acid and oxalacetic acid; and also to pharmaceutical compositions and to method to recover photoreceptor function in case of deficit of endogenic 11-cis-retinal, which provides for introduction of efficient amount of derivative of retinal as an active ingredient, where retinal derivative is converted into retinal, capable of forming a functional complex opsin/retinal, where derivative of retinal represents an ester of 9-cis-retinyl of formula I, ester of 11-cis-retinyl of formula II or their combination, where A stands for CH2OR and R represents ester-forming residue of monocarboxilic acid C1-C10 or polycarboxilic acid, which is selected from succinic acid, citric acid, keto-glutaric acid, fumaric acid, malonic acid and oxalacetic acid.
EFFECT: production of new compounds, which may find application in treatment of visual impairment.
54 cl, 5 ex, 7 dwg
SUBSTANCE: invention relates to medicine, namely to hematology and cardiology, and can be used for reduction of spontaneous erythrocyte aggregation in case of arterial hypertension with abdominal obesity. For this purpose at the background of hypocaloric diet, dosed static and dynamic physical exercise and daily swimming for not less than 30 minutes per day in the middle of the day lisinopril and metformin are introduced. Physical exercise includes morning hygienic gymnastics, therapeutic and preventive gymnastics, dosed physical exercised throughout the day. Lisinopril is introduced in dose 10 mg 1 time per day in the morning. Metformin is introduced in dose 500 mg 2 times per day. Treatment is carried out for 2 months.
EFFECT: method makes it possible to normalise spontaneous erythrocyte aggregation during 2 months, bringing it to the level close to that of healthy people, thus favouring prevention of vascular complications in patients with arterial hypertension with abdominal obesity.