Method of treating obesity
SUBSTANCE: method involves a combination of peloid applications and ultrasonic exposure. Peloid is applied on anterolateral thighs and an anterior abdominal wall. The applications are alternated every second day. Peloid is silt sulphide mud of Melkovodnenskiy deposit. The mud is applied in layer 10 mm thick at temperature 34-36°C. The applications are exposed to ultrasound at frequency 880 kHz in a continuous mode. The applications of the anterior abdominal wall are exposed to ultrasound at intensity 0.2-0.4 Wt/cm2 for 5 - 10 minutes. The anterolateral thighs are exposed to ultrasound at intensity 0.4-0.6 Wt/cm2, for 6-8 minutes for each thigh. Upon the completion of the procedure, the patient is covered with a hydrophobic tissue and left for 10 minutes. The therapeutic course is 10 procedures.
EFFECT: reducing obesity effectively by exposing on the hormonal activity of fat tissue, maintains the results obtained within three months.
The invention relates to medicine, namely to physiotherapy, and can be used in Spa, outpatient practice for restorative treatment of obesity with metabolic disorders.
The obesity epidemic is an unprecedented public health challenge, which is also underestimated, poorly understood and not fully recognized as a national problem, with significant economic consequences. Obesity has a significant impact on morbidity and mortality in the population. This is evidenced by large-scale epidemiological study that has proven that obesity is one of the major risk factors of diabetes type II, cardiovascular disease (myocardial infarction, ischemic stroke). In this regard, the prevention of obesity - relevant medical and social problem that can be solved through the implementation of innovative approaches [1, 2].
Main recommendations for treatment are based on non-pharmacological approaches and primarily correction lifestyle (good nutrition, Smoking cessation, dosed physical load and so on). Current pharmacological therapy and surgical treatment methods are "despair", have many contraindications, complications, appointed in exceptional cases.
Among non-pharmacological treatments for obesity are important natural and preformed physical factors. Important benefits of physiotherapy treatment are accessibility, physiology action on the whole body [3, 4].
Properties such as the ability to form of compensatory-adaptive reactions, lack of toxicity and allergization of an organism, the absence of adverse reactions and long-lasting aftereffect together with good compatibility with other methods of treatment have caused physical therapy techniques in the treatment of patients with obesity.
Traditionally from hardware physiotherapy treatment of patients with obesity, it is recommended to use methods that act on the Central mechanisms of regulation of fat metabolism (transcranial electrostimulation, bitemporally inductothermy, carbon dioxide, radon baths)enhancing thermogenesis (electrical myostimulation, contrast baths) and motor function of the intestine .
However, the above methods do not have a marked influence on metabolic disorders in the adipose tissue. Modern studies have demonstrated that the adipose tissue is an endocrine organ and secretes hormones and cytokines involved in regulationregulation, lipid, carbohydrate metabolism [6, 7].
The immediate impact of ultrasound on adipose tissue exerts a biological effect - increases blood flow, causes muscle relaxation. In addition, ultrasonic vibrations change the structure of cell membranes, increasing their permeability, increase the permeability of the skin.
The known method for the complex weight correction, the essence of which consists in the combined therapeutic effect directly on adipose tissue, and the area responsible for the metabolism of fat in the body. For the direct impact of the proposed use separately or in various combinations svetoindutsirovannoi fototale, photoacoustic and photodynamic effects, inducing ultrasonic vibrations. Fat removal is achieved by converting it into other compounds or destruction of heat, oxidation, acoustic or ultrasonic vibrations. Control of selective exposure is carried out using ultrasound and magnetic resonance imaging. The method allows to provide effective regulation of the weight of the person .
However, the method involves the use of complex and expensive equipment, the destruction of adipose tissue is achieved by exposure to heat, and does not change its hormonal activity.
Shiro is the first application in the complex treatment of different forms of obesity have been mud. This is due to the fact that, being a natural formation, mud has a complex physiological and therapeutic effects of all the complex components of its chemical, mechanical and thermal components. therapeutic effect of mud through neuro-endocrine-humoral mechanisms of regulation. This enables adaptation mechanisms, restores the impaired functions. Under the influence of mud restored blood and lymph circulation, normalize the metabolism, redox processes, improves tissue respiration, stimulates regeneration processes, nonspecific immunological resistance of the organism. The effect of mud largely due chemically and biologically active substances contained in the mud: macro - and microelements, vitamins, hormones, humic grounds, biogenic stimulators. Increased metabolism of collagen fibers and the main substance of the connective tissue normalizes muscle tone and improves trophism of the skin .
The use of mud in patients with different forms of obesity, as a rule, limited to the following options pelotherapy :
the first option is the application of the mud applications on a collar zone in patients with symptoms of hypercortisolism is, rare forms of obesity, severe secondary obesity, with mixed forms of obesity;
the second option - holding mud applications on the collar area and projections of the adrenal gland. Appointed in all forms of obesity without the effects of hypercortisolism and at any degree of obesity.
These techniques should be administered with caution, because in addition to the imperfect mechanisms of thermoregulation in patients with obesity often have concomitant diseases of the cardiovascular system (hypertension, ischemic heart disease, heart rhythm disorder), in which the purpose of pelotherapy is limited.
The known method of applying pelotherapy, help to reduce the glycemic profile, reduce lipid metabolism, improve regional blood flow . However, it is limited to use only for the treatment of diabetes mellitus with angiopathies, pelotherapy is carried out on the area of the lower limbs to improve regionalnej hemodynamics, and this method comprises a treatment regimen alternating pelotherapy and carbon dioxide baths, which have a pronounced metabolic effect (reduces the level of glucose, total cholesterol and triglycerides in the blood), and nick by the way there is no impact on the endocrine function of adipose tissue.
Strengthen or about timeserving action mud by combining it with the influence of ultrasound (peodophiles). Thus, there is a synergistic effect of various physical factors that act simultaneously on different stages of the disease.
In some cases, the combined effect of dirt and other physical factors (phonophoresis) have a more gentle effect on the body. Combined treatments are more economical, as they significantly reduce the flow of mud.
The closest technical solution adopted for the prototype, is a method of treating obesity appliques Tambukan silt mud. The mud is heated on a water bath to 45°C, is applied to the region of the hips, upper and lower limbs, cover compress paper or cellophane and wrap the blanket. The length appliques 60 minutes .
In the result, the amount of body fat is reduced, however, the parameters of physical therapy effects cannot be considered adequate for the treatment of obese patients with concomitant diseases of internal organs.
Without limiting the foregoing effects from the use of mud therapy, ultrasound therapy, was of interest to develop a method for the treatment of obesity, aimed at correcting the hormonal activity of adipose tissue, carbohydrate and lipid metabolism.
The objective of the invention is improving the efficiency of treatment by simultaneous effect of peloid and ultras ukowym factor on the areas of greatest deposits of fat for correcting hormonal activity of adipose tissue, carbohydrate and lipid metabolism in patients with concomitant diseases of internal organs.
To solve the problem in the treatment of obesity, including peloidoterapiya on the thighs of the patient, according to the invention, the procedures prescribed in the field of anterolateral surface of the thigh and the anterior wall of the abdomen, alternating field applications through the day, and combining peloidoterapiya with ultrasound exposure, the peloid for applications using sulphide silt mud Melkovodninskii field, which is applied with a layer thickness up to 10 mm at a temperature of 34-36°C, then using mud application as a contact environment affect the ultrasound frequency of 880 kHz in continuous mode on the field of application of the anterior abdominal wall at the intensity of 0.2-0.4 W/cm2in 5-10 minutes, and on the anterolateral surface of the thigh at the intensity of 0.4-0.6 W/cm26-8 minutes on each hip, after ultrasonic treatment of the patient served hydrophobic cloth, blanket and leave for 10 minutes, the course of treatment 10 treatments.
The technical result consists in the effectiveness of treatment of obesity due to applications sulphide silt mud Melkovodninskii field as a contact medium by ultrasound exposure on the areas of greatest is the accumulation of fat in adequately selected exposure parameters, reflected in the claims; there has been decline in glycemic profile, improved indicators of lipid metabolism, improved regional blood flow, and as a consequence reducing obesity; the result achieved from the treatment, persists after three months.
Serves as an adequate method, potentiating therapeutic effect, use in patients with obesity thin-layer applications from the muds, which on the one hand act as a medium of contact for ultrasonic therapy, with biologically active substances mud can directly penetrate into the tissue through the intact epithelium, providing a therapeutic effect, on the other hand, quantitative consumption, minimal dirt. In addition, it is recommended elaborada applique, i.e. the temperature applied to the surface of the human body mud corresponds to 34-36°C. This is due to the fact that minimizes thermal effects of the mud, because obesity is combined with disorders of the cardiovascular and autonomic systems, and therapeutic effect is achieved due to the rich mineral and biological composition of the mud. Increase the penetrating ability of the mud and improve the effectiveness of the developed method for ultrasound therapy the right near St is only on the area of the mud applications. The choice of parameters in the intensity of the impact (on the field of application of the anterior abdominal wall at the intensity of 0.2-0.4 W/cm2on the anterolateral surface of the thigh at the intensity of 0.4-0.6 W/cm2) due to the fact that small doses of ultrasound therapy (0.1 to 0.4 W/cm2) stimulates the capillary circulation, improves trophism, stimulate metabolic processes, and medium (0.5 to 0.7 W/cm2) anti-inflammatory action, as well as the fact that the boundary of thermal action of ultrasound is 0.4-0.5 W/cm2for continuous ultrasonic vibrations (thermal effect occurs as a result of transformation of mechanical energy into thermal energy and the temperature of the tissue increases).
Common features with the prototype are:
- the use of pelotherapy on the thighs of the patient
Distinctive features are
procedures prescribed in the field of anterolateral surface of the thigh and the anterior wall of the stomach,
the alternation of areas of applications through the day,
the combination of mud therapy with ultrasonic treatment (phonophoresis),
as peloid for applications using sulphide silt mud Melkovodninskii field, which is applied with a layer thickness up to 10 mm at a temperature of 34-36°C,
- mud application is used as a medium of contact with who is actvie ultrasound frequency of 880 kHz in continuous mode
- on the field of application of the anterior abdominal wall is affected by ultrasound with intensities of 0.2-0.4 W/cm25-10 minutes
on the anterolateral surface of the thigh is affected by ultrasound at the intensity of 0.4-0.6 W/cm26-8 minutes on each hip,
after ultrasonic treatment of the patient served hydrophobic cloth, blanket and leave for 10 minutes, the course of treatment 10 treatments.
To substantiate the claimed invention in the clinic of the research Institute of Medical climatology and rehabilitation (, Vladivostok) clinical studies were conducted.
In the study on voluntary informed consent included 65 patients with obesity I degree: 30 men and 35 women 24-73 years (mean age of 55.7±2,1). The diagnosis of obesity was guided by the practical recommendations of the who (1998).
The patients were divided into 2 comparable clinical and functional characteristics of the group. All patients complied with the recommendations on diet and dosed physical load.
In the 1st group (n=30) treatment included thin-layer applications sulphide silt mud on the abdomen and anterolateral surface of the thigh (the prototype).
In the 2nd group (n=35) was used phonophoresis sulphide silt mud by the present method.
The method is as follows.
Self is dnow silt mud Melkovodninskii field (TU 9318-001-10239943-2008) when the brush is applied to the area of the anterior abdominal wall and on the anterolateral surface of the thigh in the thickness of the mud layer to 10 mm, temperature +34+36°C. To prevent drying mud, the field of application wrap hydrophobic cloth (or cover), you can use the film or sheet.
The area of mud application (abdomen and anterolateral thighs alternate every other day) install ultrasonic emitter, including apparatus (UST-f, UST-105 and other). Slowly move the emitter surface area applications, maintaining good contact of the emitter with dirt, affect the ultrasound frequency of 880 kHz: at the region of the anterior abdominal wall at the intensity of 0.2-0.4 W/cm2and on the anterolateral surface of the thigh (the area of one field - 250 cm2) when the intensity of 0.4-0.6 W/cm2.
The continuous mode, the method labile, method of contact. Duration of exposure on the abdomen for 5-10 min on the thighs for 6-8 minutes on each hip. Then the patient wrap plastic film, sheets and cover woolen blanket for 10 minutes. After the procedure, dirt, rinse with warm water, wipe the body, dress and entertain 30-40 minutes.
Procedures perform daily, 5 times a week, in the first half of the day, in the course of 10 treatments.
To control the dynamics in the patient selected the following indicators:
- height-weight: Quetelet index (IR), waist circumference, hip circumference (ABOUT), is the rate of FROM ABOUT; carbohydrate metabolism: glucose, insulin, index NOMA; lipid profile: triglycerides (TG), total cholesterol (TC), LDL cholesterol, high-density (HDL cholesterol), LDL cholesterol low-density (LDL), atherogenic index (IA), characterizing the ratio of atherogenic and anti-atherogenic lipid fractions, as well as hormones: adiponectin, as the most highly expressed transcript in adipose tissue, and leptin, as regulating the processes of fat deposition in adipose tissue, and anti-inflammatory cytokine is TNF-α.
The results of the comparative analysis of the treatment of patients presented in the table. The analysis of the results indicates the effectiveness of treatment in patients. Proven positive dynamics of objective data, with changes in patients treated with phonophoresis dirt, were more pronounced due to the action of ultrasound and action of the mud. So, changing the ratio of waist circumference to hip circumference in the 2nd group decreased an average of 6.45%and in the 1st only 3.3%. Besides the reduction of the volumes in the 2nd group significantly decreased the body-mass index IR (table).
The changes were made and carbohydrate metabolism. Holding phonophoresis dirt by the method of the invention resulted in significant reduction of insulin levels with 14,21±0,69 µIU/ml to 11,09±156 µIU/ml (p< 0.05) and a significant factor in the progression of obesity (insulin resistance) index NOMA decreased 1.5 times. While in the 1st group rate IR (insulin resistance) remained unchanged.
Analysis of laboratory parameters showed that after a course of treatment in the 2-nd group significantly decreased the content of total cholesterol in serum by 19% (p<0.001), LDL by 42% (p<0,001) (table). The atherogenic index in these patients after treatment significantly decreased by 43.5%. Significantly increased HDL-C by 18% and reached the target values (p<0,001). In the 1st group changes in lipid metabolism are less pronounced.
As you know, a significant role in the progression of obesity belongs to cytokines that are synthesized in the adipose tissue. Obesity (in both groups), a decrease of the synthesis by adipocytes adiponectin. Holding phonophoresis sulphide silt mud on the area of the highest deposits of adipose tissue contributed to the change of its content. The initial low concentration of adipokine in the 2nd group on the background of treatment increased (table). Increased levels of adiponectin may explain the decrease of the concentration in the blood plasma level of LDL cholesterol (table), and also the decrease in the waist and hips, because, adiponectin reduces hypertrophy of adipocytes.
Change konolige level of leptin. Its original high level in both groups is associated with an increase in the mass of adipose tissue in the body and with the increased size of adipocytes. The combined effect of two factors (ultrasound and sulphide silt mud) contributed to the significant reduction of leptin levels by 41%. In both groups there is a decrease in the level of proinflammatory cytokine TNF-α, and in the 2nd group more pronounced.
|The dynamics of clinical and laboratory parameters in patients with obesity therapy|
|Index||1st group treated mud (n=35)||2nd group treated with phonophoresis mud (n=30)|
|The Quetelet index, kg/m2|
|Waist circumference, cm|
|Hip circumference, cm|
|The ratio of/ABOUT|
|The HOMA index|
|Total cholesterol, mmol/l|
|HDL cholesterol, mmol/l|
|LDL cholesterol, mmol/l|
|Note: significance of difference between mean values of the indicators compared with the data before treatment: * p<0,05; ** - p<0,01; *** p<0,001|
The results of the study indicate that the use of the method of treatment of patients with obesity I degree allows not only to normalize the clinical manifestations of obesity, lipid and carbohydrate metabolism, but may also have a significant effect on the secreted peptide factors of adipose tissue, which plays a key role in the progression of obesity and insulin resistance.
The essence of the claimed invention is illustrated by clinical examples.
Example 1. Patient K., 51, lives in Vladivostok. Were treated at the Clinic of the research Institute MCVL with 16.06.2010, 08.07.2010, with a diagnosis of Abdominal obesity. Hypertension Art. I, arterial hypertension 2 tbsp., risk 2 tbsp. (obesity, dyslipidemia). CHF 0.
Upon receipt complained of excessive body weight, recurrent severe headaches in the occipital region, dizziness.
The objective of the study on the PTO is t revenues: right physique, high power (weight 79 kg with height of 160 cm, the Quetelet index 30,86, FROM 104 cm-110 cm, FROM/ABOUT-0,95). HELL 140/80 mm Hg no Edema.
These additional studies:
Biochemical blood test:
Glucose 6.4 mmol/l, Insulin 15 µIU/ml) HOMA Index 4,27, Total cholesterol 6.1 mmol/l, triglycerides of 0.68 mmol/l, cholesterol high-density lipoprotein 1.1 mmol/l, the index of atherogenic 4,55, cholesterol low-density lipoprotein 4,69 mmol/l adiponectin 9,02 µg/ml, leptin of 38.7 µg/ml, TNF-α) and 26.1 mg/ml
From the second day of stay in Hospital the patient received peloidoterapiya in combination with ultrasonic influence on the developed method.
As a result of the treatment to 21 days, the patient's condition has significantly improved: decreased weight (IR 29,8 kg/m)decreased the ratio of FROM ABOUT 0.88 to have disappeared headaches, dizziness, blood pressure has stabilized at the level of 125/75 mm RT. Art.
When you study the following data:
Biochemical blood test:
Glucose 5.2 mmol/l, Insulin 7,9 µIU /ml, Index NOMA 1,83, Total cholesterol 5.33 mmol/l, triglycerides of 1.36 mmol/ l, cholesterol high-density lipoprotein 1.5 mmol/l, the atherogenic index of 2.55, cholesterol low-density lipoprotein is 3.21 mmol/l adiponectin to 11.52 mg/ml, leptin 28,1 µg/ml, TNF-α and 17.2 μg/ml.
Thus, the use of recommended methods showed the considerable improvement as anthropometric, and biochemical parameters.
After three months of treatment carried out an additional examination of the patient. It was found that targets corresponded to those that were obtained by repeating the study, the relapse of obesity is missing.
Example 2. Patient K., 32, lives in Chernigovka Primorsky Krai. Were treated at the Clinic of the research Institute MCVL with 08.08.2010, 08.09.2010, with a diagnosis of Abdominal obesity. Hypertension Art. I, arterial hypertension 2 tbsp., risk 1 tbsp. (dyslipidemia). CHF 0.
Upon receipt complained of excessive weight, noise in the head.
The objective of the study at the time of admission: weight 115 kg with height 190 cm, Quetelet index 32,05,-110,-108, FROM ABOUT -1,01). HELL 140/90 mm Hg no Edema.
These additional studies:
Glucose 7.4 mmol/l, Insulin 17,9 µIU/ml, Index NOMA of 5.89 Total cholesterol to 6.9 mmol/l, triglycerides 1.01 mmol/l, cholesterol high-density lipoprotein 1,45 mmol/l, the index of atherogenic 4,99, cholesterol low-density lipoprotein 3,76 mmol/l adiponectin to 9.45 mg/ml, leptin 38,8 µg/ml of TNF-α to 25.3 mg/ml
From the second day of stay in hospital for correction of metabolic abnormalities, the patient received treatment according to the developed method.
As a result of the treatment to 21 days, the patient considerable is improved: weight decreased to 109 kg, IR 30,45 kg/m2FROM-106 cm-108 cm, FROM/ABOUT-0,96.
When you study the following data: Glucose 6.2 mmol/l, Insulin 11 µIU/ml, Index NOMA 3,03, Total cholesterol 5.9 mmol/l, triglycerides 0,99 mmol/ l, cholesterol high-density lipoprotein and 1.63 mmol/l, the index of atherogenic 2,62, cholesterol low-density lipoprotein is 3.82 mmol/l, adiponectin and 11.8 ág/ml, leptin 24,9 µg/ml, TNF-α and 13.4 ág/ml
After three months of treatment carried out an additional examination of the patient. It was found that targets corresponded to those that were obtained by repeating the study.
The second example also confirms the high efficiency of proposed according to the invention method.
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A method of treating obesity, comprising peloidoterapiya on the thighs of the patient, characterized in that the procedures prescribed in the field of anterolateral surface of the thigh and the anterior wall of the abdomen, alternating field applications through the day, and combining peloidoterapiya with ultrasound exposure, the peloid for applications using sulphide silt mud Melkovodninskii mestorozhdenii what I which is applied with a layer thickness up to 10 mm at a temperature of 34-36°C, then using mud application as a contact medium, effect of ultrasound frequency of 880 kHz in continuous mode on the field of application of the anterior abdominal wall at the intensity of 0.2-0.4 W/cm2in 5-10 minutes, and on the anterolateral surface of the thigh at the intensity of 0.4-0.6 W/cm26-8 minutes on each hip, after ultrasonic treatment of the patient served hydrophobic cloth, blanket and leave for 10 minutes, the treatment course of 10 treatments.
SUBSTANCE: invention relates to versions of a compound of formula where R1 is a hydrogen atom; R2 is a lower alkyl group; P is H; , where P1, P2 and P3 are identical or different and are selected from a hydrogen atom, a lower alkyl group and a C14-C22 alkenyl group substituted with a lower alkyl group; or where P1 is an alkenyl group, and each of P2 and P3 is a hydrogen atom; and Y is a C14-C22 alkenyl group with at least one double bond having a Z-configuration, and having a first double bond at the third carbon-carbon bond from the omega (ω)-end of the carbon chain, capable of lowering the level of triglycerides and cholesterol, a pharmaceutical or lipid composition based on the disclosed compounds, as well as use (versions) of the disclosed compounds.
EFFECT: high efficiency of using compounds.
32 cl, 6 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutics, and aims at the prevention and treatment of hypovitaminosis and the normalisation of metabolism. The drug preparation contains vitamin A, vitamin D3, vitamin E, vitamin C; a selenium compound is presented by DAFS-25 in the following ratio of the ingredients in 1 l of the solution: vitamin A - 25.0-35.0 ml, vitamin D3 - 0.03-0.05 ml, vitamin E - 55.0-65.0 g, vitamin C - 90.0-110.0 g, DAFS-25 - 0.2-0.4 g, polysorbate-80 - 190.0-210.0 ml, 2-pyrrolidone 39.0-41.0 ml, distilled water - up to one litre.
EFFECT: using the declared invention enables increasing the immune status in poultry, normalising the antioxidant and detoxifying systems, improving the livability, egg production and meat production along with reducing the feed consumption per a unit of product.
3 tbl, 3 ex
SUBSTANCE: invention refers to medicine, namely to cardiology, and may be used for treating and preventing arterial hypertension with metabolic syndrome. That is ensured by adding the food ration with the functional foodstuff 'Samarskiy Zdorovyak' No 61 in a min daily dose of 33.3 g per one intake - with breakfast or lunch or dinner with underlying drug-induced therapy.
EFFECT: enabled treatment and prevention of arterial hypertension with metabolic syndrome
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to medicine. A pharmaceutical formulation for the treating diseases associated with endothelial dysfunction contains an active ingredient presented by a methyl pyridine derivative - 1.0-6.0 wt %; purine - 10.0-80.0 wt % and additive agents - the rest. The active substance is presented by compounds of a group: 3 -(N,N-dimethyl carbamoyloxy)-2-ethyl-6-methylpyridinium succinate, 3-methylpyridinium succinate, 2-ethyl-6-methyl-3-hydroxypyridinium hydrochloride, 6-trichloromethyl-2-chloropyridine (nitrapyrin), 2-ethyl-6-methyl-3-hydroxypyridine succinate. Purine is presented by inosine, adenosine, hypoxanthine. The pharmaceutical formulation may be presented in the form of injections, lyophilisate, solid capsules, tablets and suppositories.
EFFECT: formulation according to the invention provides creating the stable drug dosage form which considerably exceeds the existing analogues in pharmacodynamics activity on the endothelial dysfunction and toxicological properties.
4 cl, 4 tbl, 9 ex
SUBSTANCE: present compounds can be used, for example, in treating diseases of the central nervous system, peripheral nervous system, cardiovascular system, pulmonary system, gastrointestinal system and the endocrine system.
EFFECT: described compounds are useful in treating a range of diseases or conditions in which interaction with the histamine H3 receptor is beneficial.
9 cl, 216 ex
SUBSTANCE: invention relates to novel phenylaminopyrimidine compounds of formula I, which are JAK kinase inhibitors. In particular, these compounds selectively act on JAK2 kinase. The compounds can be used to treat diseases such as immunological and inflammatory diseases; hyperproliferative diseases, myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. In the compound of formula I , Q and Z are independently selected from N and CR1; R1 is independently selected from hydrogen, halogen, R2, OR2, OH, R4, OR4, CN, CF3, (CH2)nN(R2)2, where n equals 1,2 or 3, NO2, R2R4, NR2SO2R3, COR4, NR2COR3, CO2H, CO2R2, NR2COR4, R2CN, R2OH, R2OR3 and OR5R4; or two substitutes R1 together with carbon atoms with which they are bonded form an unsaturated 5- or 6-member heterocyclic ring containing 1-4 N atoms; R2 is C1-4alkyl; R4 is R2, C2-4alkenyl or phenyl; R4 is NH2, NHR2, N(R1)2, substituted or unsubstituted morpholine, CH2morpholine, substituted or unsubstituted thiomorpholine, substituted or unsubstituted thiomorpholino-1-oxide, substituted or unsubstituted thiomorpholino-1,1-dioxide, substituted or unsubstituted piperazinyl, substituted or unsubstituted piperidinyl, substituted or unsubstituted pyridinyl, substituted or unsubstituted pyrrolidinyl, substituted or unsubstituted pyrrolyl, substituted or unsubstituted oxazolyl, substituted or unsubstituted imidazolyl, substituted or tetrahydrofuranyl unsubstituted and substituted or unsubstituted tetrahydropyranyl; R5 is C2-4alkylene; R6-R9 are independently selected from H, RXCN, halogen, substituted or unsubstituted C1-4alkyl, OR1, CO2R1, N(R1)2, NO2 and CON(R1)2, wherein at least one of R6-R9 is RXCN; the rest of the values of the radicals are given in the claim.
EFFECT: high efficiency of treatment.
29 cl, 7 dwg, 2 tbl, 93 ex
SUBSTANCE: invention relates to compounds of general formula (1) or salts thereof, where in formula (1) R1 is a lower C1-C6alkyl group, a lower C3-C6cycloalkyl group, a phenyl group, a heterocyclic group, which relates to a residue formed by removing a hydrogen atom from a saturated or unsaturated monocyclic heterocyclic ring containing one, two or three heteroatoms in the ring, selected from a nitrogen atom, an oxygen atom and a sulphur atom, or a phenyl(C1-C6alkyl) group; in cases when R1 is a lower C1-C6alkyl group, that lower C1-C6alkyl group can have, as substitute(s), one, two or three groups selected from a halogen atom, a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one or two heteroatoms in the ring, selected from a nitrogen atom and an oxygen atom, a carboxyl group, a lower C1-C6alkoxycarbonyl group, a lower C1-C6alkylamino group, a lower C1-C6alkylamino group, substituted with a lower C1-C6alkylamino group, a lower C1-C6alkylamino group, substituted with a phenyl group; in cases when R1 is a phenyl group, a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated or unsaturated monocyclic heterocyclic ring containing one, two or three heteroatoms in the ring, selected from a nitrogen atom, an oxygen atom or a sulphur atom, or a phenyl(C1-C6alkyl) group, that phenyl, heterocyclic or phenyl(C1-C6alkyl) group can contain, as substitute(s), one, two or three groups selected from a halogen atom, a lower C1-C6alkyl group, a hydroxyl group or a lower C1-C6alkoxy group; R2 is a hydrogen atom or a lower C1-C6alkyl group; R3 is a hydrogen atom or a lower C1-C6alkyl group; R4 and R5 can be identical or different and are a hydrogen atom or a lower C1-C6alkyl group; R6 is a hydrogen atom or a lower C1-C6alkyl group; R7 is a phenyl group or a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one heteroatom in the ring, selected from an oxygen atom and a sulphur atom; in cases where R7 is a phenyl group or a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one heteroatom in the ring, selected from an oxygen atom and a sulphur atom, that phenyl or heterocyclic group can contain, as substitute(s), one or two groups selected from a halogen atom, a lower C1-C6alkyl group, a hydroxyl group, a lower C1-C6alkoxy group and a nitro group; W is an oxygen atom or NR8; R8 is a hydrogen atom or a lower C1-C6alkyl group; X is an oxygen atom or a sulphur atom; Y is a lower C1-C6alkylene group; Z is an oxygen atom, a sulphur atom, NR9 or OCO; R9 is a hydrogen atom or a lower C1-C6alkyl group. The invention also relates to a pharmaceutical composition based on said compounds, having GR binding activity.
EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine as glucocorticoid receptor modulators.
10 cl, 1 tbl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to naphthalene carboxamide derivatives of general formula I which possess the properties of protein kinase or histone deacetylase inhibitors. The compounds can find application for preparing a drug for treating inflammatory diseases, autoimmune diseases, oncological disease, diseases of the nervous system and neurodegenerative diseases, allergies, asthma, cardiovascular diseases and metabolic diseases or disease related to hormonal diseases. In general formula I: , Z represents CH or N; each of the groups R1, R2 and R3 represents hydrogen, halogen, alkyl, alkoxy or trifluoromethyl; R4 represents or X represents a benzene ring or a pyridine ring; R5 represents one or more substitutes specified in a group consisting of hydrogen, halogen, alkyl, alkoxy or trifluoromethyl. The invention also refers to a method for preparing the above compounds, a pharmaceutical preparation and using them.
EFFECT: preparing the compounds which possess the properties of protein kinase or histone deacetylase inhibitors.
13 cl, 10 tbl, 6 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention also relates to pharmaceutical compositions. Compounds of the formula given below are used for treatment of diabetes mellitus of type 1 or type 2, hyperglycemia, diabetic complications, insulin-resistance, metabolic syndrome, hyperinsulinemia, hypertension, obesity, edema, dislipidemia, chronic heart failure, atherosclerosis or related diseases, and can be introduced simultaneously or successively with at least one additional therapeutic agent, selected from group consisting of anti-diabetes agent, agent, which reduces content of lipids/modulates lipids, agent for treatment of diabetic complications, anti-obesity agent, hypotensive agent, anti-hyperuricemia agent and agent for treatment of chronic heart failure, atherosclerosis or related diseases.
EFFECT: claimed are compounds which possess inhibiting action on sodium-dependent co-carrier of glucose SGLT.
8 cl, 50 ex, 1 tbl, 15 dwg
SUBSTANCE: invention refers to medicine, namely paediatric resuscitation, and may be used for treating depressed cases in newborns with a surgical pathology. That is ensured by intravenous administration of 20% neat human serum albumin 3-5 ml/kg (no more than 1 g/kg) a day for 10 minutes. Observing persistent arterial hypertension requires an additional intravenous infusion of normal saline 3 ml/kg for 15 minutes, while in the presence of recurrent persistent arterial hypertension, 6% hydroxyethyl starch 3 ml/kg for 30 minutes is administered intravenously.
EFFECT: method enables a higher effect of the performed anti-shock therapy combined with reduced postoperative complications ensured by the prevented liquid outflow from the blood flow that might happen due to high oncotic and osmotic pressure of the concentrated solution of human albumin with contracting the infusion therapy extent.
SUBSTANCE: invention refers to medicine, namely - to physiotherapy, urology. A method involves the integrated physiotherapeutic effect of three physical factors. The ultrasonic exposure is characterised by frequency 2.7 kHz + 0.2 kHz, length 9 ms, pulse period 200 ms. The exposure to magnetic field is characterised by magnetic induction amplitude 1300 mT, pulse period 80 ms. The laser exposure is characterised by power 5.0 Wt, frequency 80 Hz. Total duration of a procedure is 30 minutes.
EFFECT: due to using the sequential effect of three physical factors, the method reduces the period of small urolith evacuation, the intensity of pain syndrome, requirement in analgesic and anti-spasmodic drugs, minimises the development of sclerotic changes in the ureter wall that improves urinary outflow and reduces a risk of recurrent urolith formation.
SUBSTANCE: invention refers to medicine, namely - to dermatology. A method involves the ointment application and the ultrasound exposure. The ointment is methylprednisolone aceponate. The ultrasound exposure has an intensity of 0.7-1.0 Wt/cm2. The exposure length is 2-5 minutes per one field. The duration of a procedure is 12 minutes. The therapeutic course is 7 procedures.
EFFECT: method reduces the side effects and complications provides achieving the immediate clinical effect and prolongs the remission length.
1 tbl, 2 ex
SUBSTANCE: invention relates to field of medicine, namely to dentistry, physiotherapy. Method includes influence by defocused shock wave through applications of enterosorbent "BS-P", applied on upper and lower jaw. Influence by shock wave is realised through soft tissues of maxillofacial area. Influence is performed with pulse duration 0.4-0.7 mcs, pulse frequency 90 Hz, pressure amplitude from 6 to 9 MPa, total number of pulses 1000. Procedures are carried out every second day. Course includes 7-10 sessions.
EFFECT: method enhances reparative processes due to correction of disorders of microcirculation and metabolism stimulation.
SUBSTANCE: invention relates to surgery and can be applied for prevention of recurrence in low anterosuperior apparatus resection. After formation of low stump of rectum by suturing apparatus before formation of apparatus anastomosis with preventive ileostomy, physiological saline is introduced into stump through anus and extracted with measurement of its volume. Chemical preparation is diluted, with application of solvent volume, equal to volume of rectum stump lumen minus volume of introduced ultrasonic instrument. Solution of chemical preparation is introduced into rectum stump. Ultrasonic instrument is placed into rectum stump through anus. Ultrasonic vibrations with mode 880 Hz, 0.2 W/m2 are excited in solution for 7 minutes. After that, low apparatus anastomosis is formed.
EFFECT: method makes it possible to reduce risk of recurrence.
SUBSTANCE: relates to medicine and can be applied for prevention of metastatic disease in case of right-side hemicolectomy. After laparotomy, 30 ml of solution,which contains chemical preparation, are introduced into mesentery with formation of infiltrate along mesostenium vessels in direction of orifice of upper mesenteric artery. Infiltrate is exposed to ultrasonic instrument with mode 880 Hz, 0.7 W/m2 for 15 minutes, with obtaining maximal concentration of preparation in walls of vessels, lymph nodes and tissues of mesentery.
EFFECT: method makes it possible to reduce risk of metastatic disease.
SUBSTANCE: invention relates to medical equipment. An ultrasonic probe comprises a body with a connector, and a syringe. The spring comprises a working portion of the probe coupled with the connector. The connector is provided with a cap. An internal diameter of the cap matches with an external diameter of the connector. A cap point is conical. The cap is plastic; it has long slots and a lock ring. The spring is coupled with the cap point. The working portion of the probe is bend and coupled with the connected. The cap slot length makes 0.4-0.45 of its length, while the spring length makes 0.55-0.60 of the cap length.
EFFECT: using the invention enables improving the clinical effectiveness with the improved use reliability of the probe ensured by providing greater flexibility of the working part and connector coupling.
SUBSTANCE: invention refers to medical equipment, namely to apparatuses for thermal and photochrome ultrasound treatment of osteoarthrosis of various nosologies. The apparatus comprises a control unit, a low-frequency ultrasonic vibration source in the form of an acoustic system accommodating a disc emitter connected to a piezoelectric transducer; there are also provided a knee pad impregnated with an ozone/NO-containing agent, a light-emitting array with distributed red, green and blue solid-state light-emitting diodes. The solid-state light-emitting diodes are seated into the spring light-emitting array coupled with an insulating guard spring plate secured on a carrying pad coupled form the inside with a damping element contacting with the knee pad. The solid-state light-emitting diodes are yellow, infer-red and ultraviolet and seated in the holes formed in the carrying pad and damping element. Each acoustic system is fixed on the carrying pad and configured so that it operates at a resonance frequency within the range of frequencies of 22 kHz to 100 kHz. The piezoelectric transducer contacts with a disc spring hollow guide filled with an immersion medium contacting with the knee pad. The carrying pad is connected from the outside with a carrying holder coupled with a control unit body comprising a display; further, it is provided with two elastic fastening belts on each side.
EFFECT: using the invention enables the higher clinical effectiveness in osteoarthrosis ensured by providing the effect of the complex of physical and physical-chemical factors on the joint.
1 cl, 10 dwg
SUBSTANCE: invention relates to medicine, namely to rheumatology and physiotherapy, and can be used for treatment of osteoarthrosis. For this purpose general iodine-bromine baths are carried out. Additionally from the second day of treatment on days, free of general iodine-bromine baths, ultraphonophoresis of gel "Bishofit" is performed. For this purpose area of flexion surface of knee, elbow, radiocarpal, field of anterior surface with transition on the rear of foot of ankle joint, field of external surface with transition on anterior and posterior surface of shoulder joint are preliminarily processed with 30% dimexide solution and after 15 minutes with thin, 1-2 mm thick, layer of gel "Bishofit". After that, zones of affected joints are influenced by irradiating head of apparatus "UZT-1.01 F", with area 4 cm2 in contact, labial manner, in continuous mode, with irradiation intensity from 0.4-0.6 to 1.0 W/cm2, time of exposure constitutes 10 minutes. Course of treatment includes 8 physio- and 8 balneo- procedures.
EFFECT: method ensures increase of efficiency and reduction of terms of treatment due to expressed anti-inflammatory, pain-killing effect, positive general and local trophic influence, improvement of state of vegetative nervous system, as well as elimination of balneopathological reaction.
6 tbl, 1 ex
SUBSTANCE: invention relates to medicine, namely to maxillofacial surgery, plastic, reconstructive surgery, otolaryngology. Selective destruction of water-saturated components of tumour tissue of rhinophyma is carried out by waveguide with fluctuation frequency 25 kHz and fluctuation amplitude from 100 to 120 mcm. Fibrous adhesions of rhinophyma are excised at frequency of fluctuations 35-55 kHz and amplitude of fluctuations from 100 to 120 mcm to healthy tissues layer-by-layer. Coagulation of superficial components of rhinophyma is performed by argon plasma coagulator with flow rate 1-3 l/min to the moment of scab formation.
EFFECT: method makes it possible to increase treatment efficiency due to minimal thermal injury to tissues and reduction of blood loss, which makes it possible to avoid coarse scab deformations of soft tissues and internal structures of nose.
SUBSTANCE: invention refers to medicine, specifically to surgery. The heart ultrasound is involved. A set of heart compression attributes is scored. If observing a pyriform change of the right ventricle geometry, 2 points is scored; and a dumbbell change of the right ventricle geometry stands for 2 points. That is followed by describing an M-mode systolic excursion of an interventricular septum being 3 mm - 1 point is scored, 2 mm - 2 point, and 1 mm - 3 points. Asynchronous contractions of the interventricular septum shows 3 points. Then, 1 point is scored if observing a speed increase of the transtricuspid flow. A decrease of the M-mode end diastolic size of the right ventricle makes scoring 1 point. Further, 1 point is added if observing the changes of the right atrium changes. Total score is calculated: the value of 10 points and more is an invariable indication for a surgical intervention; the total score of 4-5 requires the Nuss surgical intervention; 2-3 points mean a relative indication for the surgical intervention; and 1 point means no indications for the surgical intervention.
EFFECT: method enables the objective assessment of the heart compression to ensure the adequate planning of the surgical intervention.
1 tbl, 5 dwg
SUBSTANCE: invention refers to medicine, namely rheumatology, balneotherapy and physiotherapy. The method involves the integrated treatment. There are prescribed sulphide bath with the total hydrogen sulphide concentration of 158 mg/l, the free hydrogen sulphide concentration of 108 mg/l at temperature 36-37°C. The length of the first 2-3 baths is 6-8 minutes. The length is to be increased to 8-12 minutes. The baths are taken within the period of 10.00 to 12.00 every second day. The therapeutic course is 10-12 procedures. On the same days, within the period of 14.00 to 16.00, therapeutic exercises are done, and the climatic and landscape therapy is prescribed. On the days free from taking baths, within the period of 10.00 to 12.00, the EHF therapy is prescribed to cover biologically active points (BAP) at frequency 40-43 GHz. The points G-41, 3E-5 are exposed. The hip osteoarthrosis requires the exposure on the points G-29, G-30. If observing the upper extremity osteoarthrosis, the points 3E-4, Du-4, Du-5, Di-5 are covered. In case of the knee osteoarthrosis, the points M-34, M-35, Le-7, Le-8 are exposed. The length of the exposure covering one BAP makes 5-6 minutes. The total length of the procedure is 20-30 minutes. On the same days within the period of 14.00 to 16.00, high-mineralised average sulphide mud is applied at temperature 38-40°C on the involved joints and respective spinal reflexogenic zones. A single procedure covers not more than 2-3 greater joints. The length of one procedure is 20-25 minutes. The therapeutic course is 8-10 procedures. The total length of the rehabilitation makes 20-24 days.
EFFECT: method prolongs the remission.
2 tbl, 1 dwg, 1 ex