Method of treating patients suffering primary open-angle glaucoma

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely ophthalmology, physiotherapy. The method involves endonasal cortexin electrophoresis with underlying glaucoma therapy. Cortexin is administered from an anode. For this purpose, a bifurcated positive electrode is applied on cotton swabs wetted in a drug solution. The electrodes are introduced into the middle nasal passages. An indifferent electrode is fixed with elastic bandages on the skin of the posterior surface of the neck. The first two procedures require galvanisation at current intensity 0.5 mA for 7 minutes. That is followed by medical cortexin electrophoresis from 3rd to 12th sessions. The current intensity from the 3rd to 5th sessions is 1 mA for 10 minutes. The current intensity from the 6th to 12th sessions is 1 mA for 15 minutes. The procedures are performed every second day.

EFFECT: method improves the clinical functional, perimetric and electrophysiological characteristics of the visual analyser, slows down the disease development and improves the patient's quality of life.

2 ex

 

The present invention relates to medicine, in particular to ophthalmology and rehabilitation of patients with primary open-angle glaucoma, and can be used in practical health care, clinics, health centers.

Currently, glaucoma is one of the most common eye diseases; the number of patients suffering from this disease in the world is more than 60 million people.

Affecting persons as the working-age and elderly, glaucoma is the leading cause of irreversible blindness, occupying first place in the structure of primary disability that defines the social importance of effective medical rehabilitation of these patients (Libman E.S. State and dynamics of blindness and disability due to pathology in Russia / Eshleman, Eveva // proc. Dokl. VII Congress of ophthalmologists of Russia. - M., 2000. - Part 1. - S-214).

Views on the etiology and pathogenesis of glaucoma has changed over time, depending on the accumulated knowledge and introduction of new methods of research. For many decades leading ophthalmologists adhered to the views of primary open-angle glaucoma as ophthalmoparesis arising from the obstruction of the outflow of intraocular fluid, and pathological changes vdisk optic nerve was seen solely as the result of increased intraocular pressure (Nesterov A.P. Glaucoma. M - 1995. - 256).

Currently, the views on the pathogenesis of glaucoma has expanded considerably since the pathophysiology of glaucomatous process includes not only changes in the drainage system of the eye, and hemodynamic disorders. Including violation of intracranial pressure, mechanical and metabolic factors in the development of glaucoma, genetic component, some endocrine diseases and a number of other factors that can lead to the development of glaucomatous process (Kiseleva T.N., Grigorieva T.N., Tarasova LN. Glaucomatous neuropathy, combined with carotid disease: specificity of pathogenesis and diagnostics, " Vestn. ophthalm. - 2003. -T. - N-6. - P.5-7; EVGENIY Grigoriev Modern aspects in the study of the pathogenesis of glaucoma, normal pressure // West. ophthalm. - 2004. - So 120. No. 6. - ñ.38-40; Bezrukov BT Genetic hypotheses and assessment of penetratesthe gene primary glaucoma /Glaucoma. -2006. No. 3. - p.3-6).

In this regard, currently glaucoma is considered as optic neuropathy, with specific changes of the optic disc and visual field, with increased intraocular pressure is measured as a risk factor in the development of glaucoma, and glaucoma - as a multifactorial disease, which is based on profound vascular changes.

The practical importance sampling the volumes of treatment and rehabilitation of patients with glaucoma due to the fact, currently, modern medicine has not sufficiently effective for the treatment of primary open-angle glaucoma. If this conservative treatment of glaucoma varied, but in some cases ineffective, and the effect is unstable, which explains the etiology of this disease. It is proved that the loss of vision in glaucoma is caused by the death of the ganglion cells of the retina and the cells of the optic nerve, which explains the use of neuroprotective therapy in the treatment of glaucoma.

This trend in conservative therapy, is neuroprotective, is one of the most promising and new in the treatment of glaucoma. Neuroprotective therapy involves the use of drugs, possessing properties to protect the retina and optic nerve fibers from the damaging effects of various factors. Neuroprotection is primarily aimed at the correction of metabolic disorders caused by glaucoma the optic nerve head. In addition, the goal of treatment is improvement of local microcirculation and tissue trophism, normalization of blood rheological properties, increasing the volume of the main and collateral circulation.

At the same time up to the present time the search is conducted and the development of optimal physical therapy uses drugs drugs the the ATA, allowing in the framework of secondary prevention to reduce the number and frequency of complications, as well as to stabilize the progression of the process in order to preserve the existing visual functions and the existing quality of life in patients with chronic eye diseases, which is an important task for both ophthalmology and regenerative medicine (Arutyunova O.V. development Concept ophthalmic directions in the framework of rehabilitation medicine // journal of rehabilitation medicine - 2006. No. 2. - P.7-10. Regenerative ophthalmology. Edited Antisoma and Iguain.- M., 2006. - 96 S.).

This position is due to the fact that the traditional methods of introducing the patient neuroprotective drugs in the form of tabloids, parabulbar and intramuscular injections are not always able to provide a high level of concentration of therapeutic agent in the pathological focus.

There is a method of treatment of patients with primary open-angle glaucoma with the use of hardware therapy (Dolich P.P. patent Application 2004133945/14, 23.11.2004). For this exercise electromagnetic effect successively on the area of the orbits, temporal, occipital region of the brain, the carotid sinuses cervical sympathetic plexus, and also intravenous gliatilin of 1.0 (for 10 days) in the conjunction with installations of 0.5% solution of betaxolol 2 drops 2 times a day in the conjunctival cavity of the eye. The disadvantage of this method is the need for invasive method of drug administration (by intravenous injection) and the need for continuous instillation of drops into the conjunctival cavity (glaucomatous patients often fail to comply with treatment and the required frequency of instillation). In addition, the disadvantage is the presence of extended contraindications to the use of magnetic therapy in patients with cardiovascular disease, which typically suffer from glaucoma patients. These are: pathology of the blood coagulation system, the presence of a pacemaker, systemic blood diseases, thrombosis and recurrent thromboembolic complications, aneurysm of heart, aorta and large vessels, cardiovascular collapse above stage II and severe heart rhythm disturbances and conditions after acute myocardial infarction.

Known methods of treatment of glaucomatous optic neuropathy using neuroprotective therapy (patent Application 2006128668/14, 07.08.2006, Dolgic GI, Bazilevich O.V., Rebenko NA). In the specified method of treatment Cortexin is applied intramuscularly in combination with the introduction of intramuscular medication and Nik inside. The disadvantage of this method is the high cost of treatment (including the cost of additional drugs), as well as remote Loka is isace the introduction of medicines, that significantly reduces the access of the drug to the target organ (the eye), and hence the efficiency of the method.

The known method involving the simultaneous use of complexes of peptide drugs: ritilin - parabulbarno and Cortexin and epithalamin intramuscularly (RF Patent "Method of treatment of diabetic retinopathy" No. 2157154, 2000, bull. Fig. 31). The disadvantage of this method is the use of the preparation epithalamin, which (according to the Patent of the Russian Federation 944191, 1980. Bull. Fig. No. 19, "Method of obtaining compounds having antitumor action) increases the sensitivity of the hypothalamus to endogenous influences that may contribute to increased intraocular pressure and reduction of visual functions in patients with glaucoma. As well as the need for multiple invasive route of administration (by parabulbar injection), which entails the potential for development of subsequent vascular, inflammatory and infectious complications in orbit.

The closest in technical essence to the proposed method is a method of treating glaucoma, which consists in the use of the drug of Cortexin in the treatment of glaucomatous optic neuropathy (experience in the use of Cortexin in the treatment of glaucomatous optic neuropathy. Volik H. // TERRA MEDICA nova. - 2006. No. 2. - P.1-3). With 10 mg of the cortex is to enter into the tenon's space in a volume of 1 ml during surgical hypotensive antiglaucomatous operations (non-penetrating deep sclerectomy). The disadvantages of this method are the invasiveness, the possibility of developing infectious and exudative inflammatory reactions in orbit, carrying out the procedure in the operating conditions, difficulty re-introduction of the drug, as well as the lack of data on long-term results. Moreover, the drug is not approved for introduction into the tenon's space.

The technical result of the proposed method of treatment of patients with primary open-angle glaucoma is pronounced vasodilator, reparative, desensibilizing, trophic, cerebroprotective, neuroprotective and antioxidant effect, which contributes to the improvement of clinical, functional, parametric and electrophysiological indices of visual analyzer, slows disease progression, and increases the quality of life of patients.

This technical result is achieved by conducting sessions endonasal electrophoresis of Cortexin; the course consists of 10 treatments in a day; when the first two procedures are performed galvanization with the force of a current of 0.5 mA for 7 minutes, then, from the 3rd to 12th sessions endonasal electrophoresis of Cortexin; 3 through 5 sessions current is 1 mA for 10 minutes, and from 6th to 12th - current of 1 mA for 15 minutes; a treatment on the background of the individual who happens antiglaucoma therapy - standard drugs ocular hypotensive drops - medication β-blocker or its combination with drug inhibitor of carbonic anhydrase.

A distinctive feature of this method of treatment is a complex exposed to a constant electric current having a pronounced analgesic, vasodilatory, anti-inflammatory, trophic, reparative and desensitizing effect, and neuropeptide drug Cortexin, which has tissue-specific effects on the cerebral cortex, providing cerebroprotective, neuroprotective and antioxidant effects. These impacts have a positive effect on the function of the optic nerve, as in glaucoma the fibers undergo atrophic changes. The drug also enhances the efficiency of the energy metabolism of brain cells, improves metabolic protein synthesis, regulates the processes of lipid peroxidation in brain cells, reduces the formation of free radicals and blocks the processes of free radical oxidation. Effect of Cortexin is aimed at the stimulation of reparative processes in the brain and the acceleration of recovery of brain function after stress effects.

The endonasal electrophoresis due to the anatomical and topographical proximity of the place of application preformed physical factors and visual analyzer (since the electrodes are placed in the nasal cavity, and the cavity of the orbit and nasal cavity anatomically adjacent to each other). Thus, the endonasal medicinal electrophoresis allows to achieve the maximum concentration of drug substance in the posterior pole of the eye and optic nerve head. Neuropeptide drug Cortexin is a complex of polypeptide fractions isolated from the cortex of cattle and pigs, and contains low-molecular biologically active neuropeptides. In the preparation includes 20 amino acids, with a molecular weight not higher than 10,000 daltons and sufficient for penetration through the blood-brain barrier. The drug has a tissue-specific effect on the cerebral cortex, has cerebroprotective, neuroprotective and antioxidant effects, increase the efficiency of energy metabolism of brain cells, improves metabolic protein synthesis, regulates the processes of lipid peroxidation in brain cells. The positive effect of Cortexin in nerve cells allows directed pathogenetic treatment of patients with primary open-angle glaucoma, the main negative manifestations of which is the death of the ganglion cells of the retina (which are the neurons of the first order in the way the visual Ana is Isadora) and the development of glaucomatous optic neuropathy optic nerve.

In the application of the proposed method of treatment of the first two sessions of procedures disposed galvanization is due prior "training" structures of the visual analyzer to conduct medicinal electrophoresis. During this "training" improves hemodynamic microcirculation in the area of impact, which subsequently allows us to achieve a greater concentration of the drug in the structures of the posterior pole of the eye, starting from the third session. Gradual increase of time (exposure) exposure to electric current allows to achieve a more pronounced therapeutic effect, including in the long term.

Description of the method

The method is performed in the following way: a glaucoma patient, the treatment of which is on the background of basic individual hypotensive antiglaucoma therapy, lying spend endonasal electrophoresis drug Cortexin by the following procedure: at the ends of the forked electrode cotton pads moistened with a solution of Cortexin, enter in the middle of the nasal passages - after pre-rinsing the nose with water; the indifferent electrode placed on the skin of the back of the neck and fixed with an elastic bandage, the drug is injected from the anode. During the first two procedures are performed galvanization with the force of a current of 0.5 mA flows is their 7 minutes then, from the 3rd to 12th sessions - medicinal electrophoresis of Cortexin (3 through 5 sessions current is 1 mA for 10 minutes, and from 6th to 12th sessions current -1 mA for 15 minutes); thus, the course endonasal medicinal electrophoresis with Cortexin is ten treatments every other day. The method has a beneficial effect on visual function.

Examples of the method.

Example 1. Patient P., born in 1955 Diagnosis: OI - primary open-angle glaucoma 1A. Antiglaucoma therapy - OI - Betoptic 0.5% of 2 p/day. Vis OD with Corr. to 1.0, OS Corr. to 1.0; P0(according to pneumotonometry) OD - 18,1, OS - 17.1 mm Hg OI - pigmented rim of the iris is saved, the optic nerve disc JOI pale pink, clear boundaries. Excavation of the optic nerve disc OD of 0.2, the OS is 0.3. Computerized static perimetry: OD-single relative scotomas, the boundaries of the blind spot in the norm, OS-single relative scotomas, the boundaries of the blind spot in the norm. The narrowing of the total boundaries of the field of view ML - 30°, OS - 35°. The indicator light sensitivity of the retina in the Central zone on ONE of 25.2 dB, OS is 24.5 dB. Electrophysiological data indicators: ccsm ML - 40 Hz, OS - 39 Hz, PAC OD - 65 mA, the OS is 64 mA, West Nile virus ML - 38 Hz, OS - 39 Hz.

The patient underwent a course of medicinal electrophoresis of Cortexin: cotton pads moistened with a solution of Cortexin entered in environments which their nasal passages (after pre-rinsing the nose with water); the indifferent electrode is placed on the skin of the back of the neck, fixed elastic bandage, the drug was injected from the anode. The first two procedures were galvanized with the force of a current of 0.5 mA for 7 minutes, then, from the 3rd to 12th sessions - medicinal electrophoresis of Cortexin (3 through 5 sessions current of 1 mA for 10 minutes, and from 6th to 12th - current of 1 mA for 15 minutes); course endonasal medicinal electrophoresis with Cortexin was ten treatments every other day.

After treatment: Vis OD with Corr. to 1.0, OS Corr. to 1.0; P0(according to pneumotonometry) OD - 18,1, OS - 17.1 mm Hg OI - pigmented rim of the iris is saved, the optic nerve disc JOI pale pink, clear boundaries. Excavation of the optic nerve disc OD of 0.2, the OS is 0.3. Computerized static perimetry: OD - no relative cattle, the boundaries of the blind spot in the norm, OS - the relative absence cattle, the boundaries of the blind spot in the norm. Expanded total field of vision: OD - 25°, OS - 30°. Indicators of the sensitivity of the retina in the Central zone on ONE of 28.4 dB, OS) to 27.6 dB. Electrophysiological data indicators: ccsm ML - 43 Hz, OS - 42 Hz; PAC OD - 61 mA, OS - 62 mA; West Nile virus ML - 43 Hz, OS - 42 Hz.

Example 2. Patient G., born in 1950 Diagnosis: OI - primary open-angle glaucoma. Antiglaucoma therapy - OI - timolol 0.5% 2P/day azopt 2P/day. Vis OD with Corr. 1,0, OS Corr. to 1.0; P0(according to pneumotonometry) OD - 14,3, OS - 13,5 mm Hg OI - pigmented rim of the iris partially leached, the optic nerve disc JOI pale pink, clear boundaries. Excavation of the optic nerve disc OD of 0.3, the OS is 0.4. Computerized static perimetry: OD - single relative scotomas 4° field of view, absolute and relative scotoma nasal half of the visual field, a slight expansion of the boundaries of the blind spot, OS - deep relative scotoma 4° field of view, expressed "nasal step", a slight expansion of the boundaries of the blind spot. The narrowing of the total boundaries of the field of view on OD - 60°, OS - 55°. The indicator light sensitivity of the retina in the Central zone on ONE of 21.3 dB, OS - 22,1 dB. Electrophysiological data indicators: ccsm ML - 37 Hz, OS - 37 Hz; PAC OD - 75 mA, OS - 74 mA; West Nile virus OD - 31 Hz, OS - 32 Hz.

The patient underwent a course of medicinal electrophoresis of Cortexin: cotton pads moistened with a solution of Cortexin, introduced in the middle of the nasal passages (after pre-rinsing the nose with water); the indifferent electrode placed on the skin of the back of the neck, fixed elastic bandage, the drug was injected from the anode. The first two procedures were galvanized with the force of a current of 0.5 mA for 7 minutes, then, from the 3rd to 12th sessions - medicinal electrophoresis of Cortexin (3 through 5 sessions currents from 1 mA to use the e 10 minutes and from 6th to 12th - current of 1 mA for 15 minutes); course endonasal medicinal electrophoresis with Cortexin was ten treatments every other day.

After treatment: Vis OD with Corr. to 1.0, OS Corr. to 1.0; P0(according to pneumotonometry) OD - 13,7, OS - 13.2 mm Hg OI - pigmented rim of the iris partially leached, the optic nerve disc JOI pale pink, clear boundaries. Excavation of the optic nerve disc OD of 0.3, the OS is 0.4. Computerized static perimetry: OD - single relative scotomas field of view, the boundaries of the blind spot in the norm, OS-1 relative order scotoma 4° field of view, increased peripheral borders of the nasal half of the field of view of 10°, is a minor expansion of the boundaries of the blind spot. The total extension of the boundaries of the field of view on OD - 50°, OS - 45°. The indicator light sensitivity of the retina in the Central zone on ONE 26,2 dB, OS, while 26.1 dB. Electrophysiological data indicators: ccsm ML - 42 Hz, OS - 41 Hz; PAC AR - 67 mA, OS - 63 mA; West Nile virus ML - 35 Hz, OS - 36 Hz.

The proposed method of treatment was performed in 93 patients. All patients diagnosed with primary open-angle glaucoma I-III stage with normalized intraocular pressure despite medical or surgical treatment (P0>20 mm Hg), including 51 women and 42 men aged 50 to 65 years. Limitation established the diagnosis of the open-angle glaucoma ranged from 3 to 17 years.

Ophthalmologic examination of patients was performed according to the General scheme: examination of visual acuity, biomicroscopy, pneumatonometry, tonometry on Maklakova, ophthalmoscopy, the study of the field of view on the projection perimeter Octopus 101 at a white object on a specialized computer program. The function of the inner layers of the retina and axial beam optic nerve was evaluated by the method of determining thresholds electrical sensitivity and lability of the optic nerve. Researched than the critical frequency of flicker fusion. The survey was conducted before, after treatment and after 6 months. The treatment was carried out on the background of the individual baseline antihypertensive antiglaucoma therapy. Statistical processing of the research results was carried out using the methods of variation statistics, which confirmed their authenticity.

As a result of this treatment approach in patients with primary open-angle glaucoma was a significant improvement of visual acuity on average by 13.1% (p<0.05)and the positive dynamics of this indicator was observed in 72,6% of cases. In the long term (6 months) after end of treatment, patients showed a slight decrease in visual acuity compared with the results obtained directly the donkey treatment, this indicator remained significantly above initial results on average by 9.8% (p<0,05).

The computer static perimetric studies after treatment increased the total boundaries of the field of view in 92.7% of cases at 60-120°. Significantly increased the average sensitivity of the retina in the average rate of 6.1±1,2 dB (p<0.05) and indicator foveolar speed 5.6±0,2 dB (20,0%) (p<0,05). This decreased size, depth and number of relative and absolute cattle, some of which were transformed into relative. Perimetric examination in the remote period showed a slight tendency to decline foveolar and the average sensitivity of the retina obtained after treatment, which, however, remained significantly elevated relative to benchmarks, on average, higher than initial values of 5.3±0,1 dB (p<0,05).

Analyzing electrophysiological indices obtained after treatment, the observed increase in performance critical frequency of flicker fusion on average 28.4% from baseline values (p<0,05). Indicator threshold electrical sensitivity has improved on average by 28% from baseline values (p<0,05). Figure lability of the optic nerve was significantly increased in average of 24.4% (p<0,05). 6 months after treatment of the mentioned slight decline investigated the electrophysiological parameters who remained significantly higher than baseline values.

Thus, in the treatment of glaucomatous optic neuropathy method proposed in patients with primary open-angle glaucoma improved clinical and functional characteristics of the visual analyzer: decreased number and depth relative and absolute cattle, expanded the total field of vision, increased rates foveolar and the average sensitivity of the retina and improved electrophysiological indicators (critical frequency of flicker fusion threshold electrical sensitivity and lability of the optic nerve). The method is effective, which is confirmed by the statistically significant difference between the original and "posttherapeutic" indicators of total and foveolar light sensitivity of the retina, the values of electrophysiological parameters, as well as stabilization and conservation received positive treatment results in long-term period up to 6 months. Adverse reactions or worsening of visual function of patients not reported. Thus, the study showed that the timely inclusion of medicinal electrophoresis of Cortexin in the complex treatment of glaucomatous optic neuropathy with open-angle glaucoma in the early stages of its development on the it shows a beneficial effect on the severity and pace of the recovery processes, contributing to the improvement of visual functions.

Application of the proposed method of treatment helps effectively protect neural tissue of the retina and optic nerve from the effects of hypoxic damage. Well documented positive clinical dynamics, assessed on the increase in the foveolar the light sensitivity of the retina, positive change field of view and increase the electrical sensitivity and conductivity of the optic nerve.

All this allows us to recommend the above method as neuroprotective, antioxidant, anti-ischemic and neuroprotective treatment in complex restorative therapy in patients with primary open-angle glaucoma.

A method of treating primary open-angle glaucoma by introducing medicinal substances physical factor, characterized in that on the background of basic individual hypotensive antiglaucoma therapy to the patient in the supine position hold endonasal electrophoresis drug Cortexin: at the ends of the forked electrode cotton pads moistened with a solution of Cortexin, enter in the middle of the nasal passages - after pre-rinsing the nose with water; the indifferent electrode placed on the skin of the back of the neck and fixed with an elastic bandage, the drug is injected from the anode when the first choice of the two procedures is galvanized with the force of a current of 0.5 mA for 7 minutes, then, from the 3rd to 12th sessions - medicinal electrophoresis of Cortexin; 3 through 5 sessions current is 1 mA for 10 minutes; and from 6th to 12th sessions current - 1 mA for 15 minutes; thus, the course endonasal electrophoresis with Cortexin is ten treatments every other day.



 

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SUBSTANCE: present invention refers to organic chemistry, namely to new 1,2-dihydroquinoline derivatives of general formula , or to a pharmaceutically acceptable salt thereof, wherein R1 represents a lower alkyl group; R2 represents a hydrogen atom; each of R3 and R4 represents a lower alkyl group; R5 represents a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group; X represents -CO-, -C(O)NR8 - or -S(O)2-; each of R7 and/or R8 may be identical or different, and represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower cycloalkyl group, a phenyl or naphthyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a lower alkoxy group, a phenoxy group; provided R7 and/or R8 represent a lower alkyl group, a lower alkoxy group, the mentioned lower alkyl group and lower alkoxy group may contain one or three groups specified in a halogen atom, a phenyl group, an unsubstituted monocyclic 6-member heterocyclyl with one heteroatom specified in a nitrogen atom, and 5 carbon atoms in a cycle, a lower alkoxy group, and -NRaRb as a substitute (substitutes); provided R7 and/or R8 represent a phenyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a phenoxy group, the mentioned phenyl group, saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, phenoxy group may contain one or two groups specified in a halogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a phenyl group, a hydroxyl group, a lower alkoxy group, a halogen-substituted lower alkoxy group, a lower alkylthio group, a lower alkylcarbonyl group, a lower alkoxycarbonyl group, a lower alkylcarbonyloxy group, -NRaRb, a nitro group and a cyano group as a substitute (substitutes); Ra and Rb may be identical or different, and each of them represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group; Y represents a lower alkylene group; Z represents an oxygen atom; p is equal to 2, provided p is equal to 2, R6 may be identical or different. The invention also relates to a pharmaceutical composition and a glucocorticoid receptor modulator of the compound of formula (1).

EFFECT: there are produced new 1,2-dihydroquinoline derivatives possessing glucocorticoid receptor binding activity.

7 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula: , wherein Y represents -CO2H; A represents -(CH2)n-Ar-(CH2)o-, wherein Ar represents thiophenyl; total m and o is equal to 3, and wherein 1 group -CH2- may be substituted by O; G and G' represents -H; and B represents phenyl containing 1 to 2 substitutes independently specified in -F, -Cl and -Br. The invention also refers to a composition on the basis of the mentioned compounds.

EFFECT: there are produced new compounds and pharmaceutical composition on their basis which can find application in medicine for treating glaucoma or ocular hypertension.

10 cl, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compounds of formula: , wherein R represents H, or R consists of: 1) C1-6 alkyl and 2) 0 to 1 -OH groups; Y represents -Cl or -F; and X consists of: 1) a linear alkyl or alkynyl having 4 to 10 carbon atoms, and 2) 0 to 1 -OH groups. The invention also refers to an ophthalmologically acceptable fluid based on these compounds.

EFFECT: there are prepared new compounds that may be used in medicine for treating glaucoma.

9 cl, 2 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely traumatology and neurosurgery. Transient electrodes are implanted under neurophysiological control and by means of an image converter: the first electrode is epidural and implanted in a projection of the segment L3-4 or L4-5 or L5-S1. Soft tissue hydropreparation in a projection of a sciatic nerve is followed by implanting the second epineural electrode under a gluteal fold. If observing the voluntary activity in an innervation zone of a peroneal nerve, a third electrode is placed and fixed in an upper one-third of the shin in a projection of the peroneal nerve. The postoperative electric stimulation is performed 2 times a day for 14 days.

EFFECT: method extends the range of products for treating sciatic neuropathy.

2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely physiotherapy. A method involves the administration of chophytol, diet therapy, magnetic therapy and exposure to electric current. The magnetic therapy is performed by a low-frequency sinusoidal alternating magnetic field. The exposure covers a collar zone and liver for 10-15 minutes. A continuous mode, frequency 50 Hz, grade I-II magentic induction are specified. The magnetic therapy is immediately followed by the exposure to complex-modulated pulse electric current with a neural-like pulse shape. The exposure is generated at the level ThVII - ThXI, paravertebrally to the right, and cover skin projections within the liver and gallbladder transversally. For this purpose, the electrodes are placed in 6 procedure fields: 1 - paravertebrally to the right at the level of the ThVII spine, 2 - paravertebrally to the right at the level of the ThXI spine, 3 - in a projection of the liver on a front surface of the body, 4 - in a projection of the liver on a back surface of the body, 5 - in a projection of the gallbladder on the front surface of the body, 6 - in a projection of the gallbladder on the back surface of the body. The 1st and 2nd electrodes are connected to the channel IV, while the 3rd and 4th electrodes - to the channel I, and the 5th and 6th electrodes are connected to the channel II. The channels I, II work in a frequency-drift group mode. The channel IV work in a continuous mode at fixed frequency 20 Hz. The current intensity is adjusted to apparent vibration sensation. Duration of a session is 10-15 minutes. The therapeutic course is 10-12 daily procedures.

EFFECT: method improves the motor function of the gall bladder ensured by the improved cholekinesis, hepatic circulation and cholestasis elimination.

2 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to - arthrology, physiotherapy, balneology. The method involves physical methods of therapy, therapeutic exercises, massage, acupuncture and phytotherapy. The patients are trained to give a self-massage of the knee joints additionally during the resort therapy and after the termination of the rehabilitation. From the 1st to 10th day of the therapeutic course patient's knee joint is exposed to polychromatic polarised light at 20 cm for 6 minutes. The patients take 10 iodine-bromine baths at temperature 37°C for 10 minutes. From the 1st to 5th therapeutic days, the patients do combined therapeutic exercises; their lower extremities are massaged manually for 10 minutes. From the 6th to 15th days, the knee joints are exposed to sinusoid modulated currents (SMC) at modulation frequency 100 Hz, at a depth of 50 - 70%, current intensity to moderate vibration for 7 minutes. From the 6th to 10th days, the braking acupuncture follows by giving a 1-2-minute massage of the points 10RP, 9RP, 36E, 34E by introducing a needle for 30 seconds and by giving a point massage of cheng-fu, cuan, yang-lin-cuan, zu-sang-li, wei-yang, cheng-shan, chung-feng, hun-lun, nei-ting. The patients take a herbal infusion. From the 11th to 15th days, the knee joints are exposed to decimetric waves (DMW). That is followed by a hydro-massage of the lower extremities and lumbar region for 15 minutes up to 3 atm. Thereafter, the 10-minute post-isometric relaxation of the quadriceps muscle of thigh is applied. The patients do the complex of weight reduction exercises and take the herbal infusion. From the 16th to 20th day, the mud applications on the knee joints are prescribed at temperature 42°C for 30 minutes. If suffering gonarthrosis, the patients do the complex of therapeutic exercises. That is followed by the paravertebral vacuum therapy of the vertebral column. The 10-minute knee joint traction is applied. The patients take 20 g of the herbal infusion.

EFFECT: method recovers the joint mobility, improves the exercise tolerance of the lower extremities.

1 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely neurology, physiotherapy. The solution of proserine is introduced 30 minutes before conducting low intensity electrical stimulation. Amplitude of the electrical stimulation is 10-20 mA, frequency is 40-40 Hz, and length is 900 seconds.

EFFECT: method reduces the length of treatment, raises muscle tone, desensitizes the peripheral innervation region.

3 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to neurosurgery and rehabilitation medicine. A principal stage of the surgical intervention is followed by placing at least one electrode for neuromodulation in an abnormal focus. In the postoperative period, the Kronlein - Brusova scheme is used to localise a projection of anterior central gyri on the head skin, and the transcranial Doppler sonography follows. The presence and location of the temporal and suboccipical window are stated. It is the temporal window the closest to a projection of the anterior central gyri that is selected. Local magnetic emitters are placed in projections of the selected temporal and suboccipital windows. That is combined with the local exposure to the magnetic field by means of the placed emitters and electric current through the electrodes for neurostimulation. The 10-15-minute stimulation is performed three times a day for 15-20 days.

EFFECT: method provides higher clinical effectiveness and reduced risk of complications ensured by the combined electromagnetic stimulation of the adequately selected exposed areas.

2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically urology. A method involves the complex postoperative rehabilitation. From the 10th postoperative day, the patient is exposed to electric myostimulation at current intensity to pelvic floor muscle contraction, frequency 30-50 Hz, modulation depth 100% for 10-15 minutes. The therapeutic course is 12-20 daily procedures. In one month from the operation, the ischiocavernous and bulbospongiosus muscles are trained. That involves doing three exercises thinking of 'penis contraction'. The first exercise represents 5 tensions with maximum intensity (100%), length 5 seconds and tension pauses 90 seconds. The second exercise represents 5 tensions with intensity 50% of maximum intensity, length 15 seconds and tension pauses 20 seconds. The second exercise represents 5 tensions with intensity 30% of maximum intensity, length 30 seconds and tension pauses 20 seconds. The exercises are done min. 3 times, once a week in the morning and evening. They are added with doing the interval exercises for lower extremity muscles. The exercises include 15-minute warm-up activities and doing the exercises of intensity 70-80% of maximum intensity, 50-60% of maximum heart rate, repeated for 5 times with 3-minute pauses. The exercises are done not less than 3 times. From the second postoperative month, a phosphodiesterase-5 inhibitor is administered.

EFFECT: method provides improving the quality of erection ensured by erection compression of the superficial veins of penis and blood outflow blocking from the cavernous body and prolonged therapeutic effect.

4 cl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely - to traumatology, physiotherapy. The method involves electric stimulation of superficial muscles involved in forearm rotative motions. The electric stimulation is started from the third day of immobilisation. The exposure is conducted in the subthreshold mode, at current frequency 2 Hz, length 500 msec, pulse current 10 to 60 mA. The procedures are performed twice a day for 10-15 days. From the 10th day of immobilisation, the muscles are electrically stimulated in the subthreshold mode. The exposure is conducted at current frequency 50-100 Hz, half-cycle length 2-3 s, twice a day for 10-15 minutes.

EFFECT: method provides the early recovery of rotative motions ensured by early normalisation of the fracture microcirculation, preserves the muscle tonus for the period of immobilisation.

2 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to gynecology, physiotherapy. Transcreanial electrostimulation is carried out, performing impact in accordance with fronto-occipital method with pulse monopolar current to 2 mA. First electrostimulation procedure is performed with current intensity until sensation of vibration in the range 0.5-1.0 mA, in each following procedure current intensity is increased from 0.2 to 0.4 mA, but not more than 2.0 mA. Duration of first and second procedures constitutes 15-20 minutes, duration of the following procedures being 30 minutes. Transcranial electrostimulation is performed every second day, alternating it with iodine-bromine balneotherapy. Balneotherapy is performed in form of vaginal irrigations and general baths with application of iodine-bromine water with temperature 36-37 degrees, with 10-15 minute duration. Course consists of 8 balneo- and physio-procedures.

EFFECT: method increases treatment efficiency due to enhancement of pain-killing effect, normalisation of menstrual function, improvement of function of ovaries, increases non-specific resistance of organism, normalises psychoemotional status, cellular and humoral immunity, activity of vegetative nervous system and system of lipid peroxidation.

1 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely rehabilitation medicine, physiotherapy and urology and may be used for the purpose of rehabilitation of the patients suffering urolithiasis following lithitripsy. That is ensured by the intake of the herbal tea "Veres" containing wild camomile blossom, knotgrass herb, nosebleed herb and horsetail herb, juniper fruits, sage leaves, birch leaves, red bilberry leaves, linseeds taken in equal proportions. The infusion is taken in a dose of 100 ml 3 times a day 30 minutes before meals for 5-7 preoperative days. The common background therapy follows the lithotripsy procedure. That is combined with the additional intake of the herbal tea "Veres" for 10 days following the above procedure and hydrocarbonate sulphate calcium-magnesium mineral water "Kazachinskaya" of mineralisation 1.44g/l for 24 days following lithotripsy. The mineral water "Kazachinskaya" is taken in a dose of 200-250 ml 3 times a day before meals. Further, after the lithotripsy procedure, a projection of the involved kidneys and renal duct is exposed to the apparatus Bemer-3000 at AC field frequency 30-1000 Hz and magnetic field intensity 8.5-100 mcT. The exposure is generated by an intensive contact applicator from 2 fields in the mode-1 (2-4 stages) of 8 minutes. The therapeutic course makes 10 daily procedures. The background therapy is followed by another one-month intake of the herbal tea "Veres", as well as by another exposure to the apparatus "Bemer-3000" at the same parameters of the electromagnetic field. The contact exposure also covers the kidneys and the lower one-third of the renal duct by means of the intensive application from 2-4 fields in the mode-2 (2-4 stages) of 12 minutes. The exposure is daily, two times a day.

EFFECT: method provides reducing the length of calculus fragments discharge following the lithotripsy procedure, improving the clinical and biochemical blood and urine statuses, renal blood flow, treating and preventing the postoperative complications, recovering the immunological responsiveness and antioxidant protection.

4 dwg, 3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, education science. The method involves the brain exposure to electric current following frontal-mastoid technique. The exposure is generated by pulse current of frequency 800 Hz - 1200 Hz. A pulse length is 0.25 ms + 20%. The procedures are performed for 5 days before noon. A duration of the exposure is 25 minutes. It is followed by 10-minute self-massage of the head and neck regions.

EFFECT: method provides the higher effectiveness of mental activity ensured by the successive exposure to electric current of the above parameters, and self-massage.

1 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely rheumatology, physiotherapy. The method involves drug-induced and drug-free methods of treating. In addition, the area of two affected symmetrical joints is applied with the preparation Biol in a combination with the exposure to high-tone therapy. The length of procedures is 1 to 4-5 to 30 minutes per each joint. Starting from the 4-5th to 8-10th procedure, the length of procedures is 20 minutes per each joint. The procedures are daily. The therapeutic course is 8-10 procedures.

EFFECT: method provides higher therapeutic effectiveness ensured by improved microcirculation, ensured anaesthetic effect, reduced drug-induced load.

1 ex

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