Method of treating "dry" form of age-related macular degeneration

FIELD: medicine.

SUBSTANCE: invention relates to medicine, in particular opthalmology, and may be used for treating the patients with a "dry" form of age-related macular degeneration. That is combined with using lutein-containing antioxidants and carotenoids for one year every 2-3 months. Fenofibrate (Tricor 145) is additionally used for a period of time long enough to normalise a lipid profile and to maintain the above values at the attained level. Vitrum vision forte and nutrof total are used as the above lutein-containing antioxidants and carotenoids.

EFFECT: invention provides arresting the progression of the "dry" form of age-related macular degeneration.

2 cl, 1 ex

 

The present invention relates to ophthalmology and is intended for the treatment of patients with "dry" form of age-related macular degeneration (AMD). According to statistics, the "dry" form of AMD occurs in 90% of cases, the "wet" form - 10%. For the "dry" form of AMD is characterized by: dvuhstoronnej process and chronic slow the progression from minor in the early stages to low vision and blindness in the later stages of the disease, for this reason, the disease ranks third among causes of blindness in the second half of life after glaucoma and diabetic retinopathy.

Research in this area are highly relevant with regard to the loss of total disability due to AMD persons of working age. This categories of patients with disorders of lipid metabolism leading to a drastic imbalance of oxidative processes in the cardiovascular system (oxidative stress)causing damage to large vessels, as well as the smallest. This category includes microvessels supplying the photoreceptors in the macular area. Numerous studies confirm that the primary influence on the development of AMD are atherosclerotic changes in vessels choriocapillaris layer of the eyeball. Ophthalmoscope changes when "dry" AMD is manifested in the form of druses and different is offered by the degree of destruction of the retinal pigment epithelium in the macula.

Considering that the AMD atherosclerotic changes occur at the level of small and smallest vessels of the body, the drugs used in the treatment of this disease should also be consistent with the purpose and impact on the improvement of microvascular system of the eye. Therefore, this category of patients is mandatory simultaneously with treatment by an ophthalmologist to be under the supervision of a physician or cardiologist for simple compensation of blood pressure and control and normalization of the lipid profile.

The level of technology

In the treatment of "dry" form of AMD effectiveness of medicines to date has not been confirmed by multicenter randomized placebo-controlled studies. Therefore, the vast majority of domestic hospitals for patients with "dry" form of AMD effectiveness of parenteral use of drugs to date have not been confirmed. It is mandatory assignment vasoprotection, nootropics, vitamins, coenzymes and renoprotection (pharmacological, fosfaden, cytoflavin, cytochrome C, Cavinton). These drugs are almost no influence on the process in the fundus, causing only a slight positive temporary influence on the General condition of patients. In poslednego in the treatment of patients with "dry" form of AMD used peptide bioregulators (Retinalamin for local use and Cortexin - for intramuscular). Retinalamin is a complex of low molecular weight polypeptides with a molecular mass of from 1000 to 10,000 daltons, sufficient to pass through gematologicheskii barrier. One of the drawbacks of the drug is a sharp pain when subconjunctival and parabulbarnom. The drug is used in numerous eye diseases of the retina and optic nerve, but the expectations of obtaining a stable therapeutic effect, in any disease is not obtained. Cortexin in patients with "dry" form of AMD is used as a means of correcting the functional state of the Central nervous system, improves intellectual function and psycho-emotional state, as well as having antioxidant activity (Boyko EV, Zhuravleva L.V., Sosnovsky C.B. Methodical recommendations "Age-related macular degeneration (risk factors, classification, diagnosis, prevention, treatment). 2010). Thus, the effect of this drug carries several indirect function without impacting directly on the disease process.

More focused on the pathological processes occurring in the macular area in the "dry" form of AMD is the use of drugs, engaged in antioxidant protection. The main recognized the governmental antioxidants are: vitamin C (ascorbic acid), vitamin E (dl-alpha tocopherol acetate), vitamin zinc (zinc oxide), vitamin b2(Riboflavin), selenium (as selenium amino acid chelate complex), rutin, bilberry extract. However, these drugs are essentially a favorable condition, is a member of the greater or lesser dose of this vitamin complexes. The main components of these drugs are the carotenoids (lutein and zeaxanthin)that have a positive impact on the state of the macular pigments. The mechanism of the protective action of carotenoids is based on their ability to absorb light (especially short-wave spectrum) and their high antioxidant activity, due to which slow down the damaging photo-oxidative processes directly in the Central area of the retina. Clinical studies have confirmed that long-term use systems, including carotenoids, delivers lutein and zeaxanthin directly in the macular region, therefore, at present the quality of the drugs is estimated depending on the quantitative content of zeaxanthin, and, in particular, lutein.

In recent years there have been many lateinamerika agents of domestic and foreign production.

The closest analogue of the present invention is a method of the same purpose, providing Perera is inoe drug use Nutri total (Bausch & Lomb), which, along with antioxidants and carotenoids (lutein 10 mg zeaxanthin 2 mg), is anticholesterol drug - OMEGA-3 covering when the recommended dose is 1 tablet per day 50% of the daily requirements for an adult (P.A. Bezdetko // optimizing prevention and treatment of age-related macular degeneration. // Health of Ukraine, No. 23-24, December 2008, P.74-75.)

Recently much attention is paid to positive pharmacological action of OMEGA-3 PUFA (polyunsaturated fatty acid) in the pigment epithelium and the vascular endothelium. Reliable clinical study AREDS 2 (Age-Related Eye Disease Study Group) (2007-2009) was to use a combination of lutein 10 mg zeaxanthin 2 mg with including OMEGA-3 (polyunsaturated fatty acids 1 g - docosahexaenoic and eicosapentaenoic acids) in patients with "dry" form of AMD. The results of this study allowed us to conclude that the risk of an early form of AMD is lower in people with higher levels of consumption of OMEGA-3 (DHA), compared with those who did not use them or have used in smaller quantities. When the recommended dose of the drug from 1 to 3 months of documented cases of stabilization and suspension of progression "dry" form of AMD. Numerous clinical studies have shown, copolymerisate fatty acids OMEGA-3 are the basis of healthy nutrition to sustain the heart and a positive effect on reducing low-density lipoprotein, normalize the ratio of cholesterol and triglycerides in the blood. Polyunsaturated fatty acids OMEGA-3 inhibit thrombus formation processes, maintain the immune status of the organism, normalizes blood circulation in the brain, increasing the resistance of cerebral vessels during hypoxia and low blood pressure. Important representatives of a number of polyunsaturated fatty acids OMEGA-3 are eicosapentaenoic acid and docosahexaenoic acid. The drug prevents the deposition of cholesterol in the walls of blood vessels, protects cells, protects the heart from damage caused by a magnesium deficiency or lack of oxygen. However, to date there is no evidence concerning the specific effects of OMEGA-3 microvessels and their blood flow. OMEGA-3 also does not have the property "capacity" of high-density lipoproteins, which is very important not only in terms of atherogenic protection of the vascular system, but in relation to microvascular protection.

The majority of patients with "dry" form of AMD suffers from vascular diseases (hypertension, ischemic heart disease), and some patients with AMD develops on the background of diabetes of the 2nd type. In the study of lipid profile in these patients almost always new what are violations of this kind of exchange with a high rate of haemoglobin, because of the threat of serious vascular accidents (heart attacks, strokes, thrombosis). On the other hand, the drug Nutri Total, which includes OMEGA-3, is used in a limited time (1-3 months), followed by the replacement lateinamerika drugs or pause in the appointment of preparations of this type. However, this category of patients need constant microvascular antilipidny protect against the background of periodic intake of antioxidants and carotenoids.

The technical result of the invention is to provide suspension to the progression of the "dry" form of AMD.

The technical result is ensured by full microvascular antilipidny protection against admission lateinamerika antioxidants and carotenoids oral use fenofibrate (Fenofibrate 145) for a time sufficient to normalize the lipid and maintain these indicators at that level. Lateinamerika medication repeat courses for 2-3 months with breaks for 1-2 months.

The lipid profile, as is known, reflects the values of cholesterol profile: total cholesterol, triglyceride, low density lipoprotein (LDL), high density lipoprotein (HDL), very low density lipoprotein (VLDL). The relationship of these indicators is very important for the s, as they reflect the haemoglobin rate - the risk of developing vascular accidents in the body.

Pathogenetically directed treatment anticholesterol exercising will microcosmical protection and antioxidant, positively affecting the damaging photo-oxidative processes directly in the Central area of the retina.

The proposed method for the treatment of "dry" form of AMD is significantly different from similar that ensures the full long-term microvascular protection of the patient due to a significant decrease in lipid profile and alignment of their relationship. So Fenofibrate 145, unlike OMEGA-3, is able to "grow" HDL, which plays an important role for achieving safe for the patient in the atherogenicity. This is achieved the effect of long-term purpose of the drug Fenofibrate 145 monthly monitoring of lipid profile of the patient's blood. Unlike OMEGA-3 positive effect of Fenofibrate cholesterol profile of patients is already apparent after 3-4 weeks and usually improves the performance of several factions at the same time.

The fenofibrate 145 belongs to the class of fibrates-derivatives fibroeva acid used since the late 50-tenths of years in the treatment of vascular diseases accompanied by increased levels of cholesterol and its fractions (ischemic Bo is esgn heart). However, it was later revealed that these drugs are thoroughly carried out microvascular protection and only partially affect atherosclerotic changes of large vessels in the heart. Currently used fenofibrate (Fenofibrate 145) is the drug already in the 3rd generation and at the moment he is the most well-studied, safe and proven use in domestic and foreign clinical practice. In Russia, the drug appeared in September 2008, currently supplied by the company "Abbott products" in the form of a special form nanoparticles obtained by the method technologies Nano Cristall in the Irish city of cork. Currently it is the only drug that is obtained in such a way that provides: moneyline dose at admission; 2. maximum bioavailability; mochimaru security; 4. full absorption from the digestive tract; 5. the independence of the meal; 6. intake of 1 tablet per day at any time of the day; 7. no need appropriate doses of the drug. The fenofibrate is administered in a single dosage 145 mg once a day for all patients regardless of age, duration of disease and severity of complications. Studied that the Fenofibrate is well tolerated by patients, as confirmed by large clinical experience of its use abroad, where it is taken more than 36 million diabetic patients retinopathy is she.

The mechanism of action of fenofibrate - Fenofibrate 145 due to its ability to stimulate a certain fraction of the alpha receptors, which are cells in the liver are responsible for metabolism of lipids. These receptors play a dominant role in the intracellular regulation of migration and rewriting of the genomes of DNA responsible for the levels of lipid metabolism and inflammatory cytokines. Activation of the receptors occurs as a result of linking them with Fenofibrate 145 by complex biochemical processes leading to the excitation of lipase enzyme system. This process is accompanied by a decrease in the concentration of triglycerides, the normalization of the size of the particles of low-density lipoprotein (LDL) - from small, dense atherogenic to larger, more buoyant and less atherogenic particles, increasing levels of high density lipoprotein (HDL), total manifestoes reduction of the atherogenic lipid profile.

In addition, Fenofibrate 145 has a non-lipid pleiotropic effects, which explains the positive effect of Fenofibrate 145 on the retina of the patient's "dry" form of macular degeneration in normal lipid profile. This effect contributes not only to slow the progression of microvascular retinal changes its positive influence also extends to the progression at which rosclerosis and cardiovascular events in these patients.

Us clinical trials were selected modes of applications of the drug Fenofibrate 145 on the background of periodic receptions lateinamerika antioxidants in patients with "dry" form of macular degeneration. He was selected the most optimal mode, the purpose of which was to: 1. The results of studies of lipid metabolism of the patient to normal or close to normal physiological and maintain at this level to address the underlying pathogenetic causes of the disease. 2. Improve metabolic functions in the body as a whole against the background of reception of broad-spectrum antioxidants included in lateinamerika drugs to prevent oxidant stress in the vasculature and in the retina. 3. To slow down or completely halt the progression of the dry form of AMD with the help of the above drugs.

The method is as follows.

Therapy with Fenofibrate 145 appointed after examination of the ocular fundus of the patient, receiving the results of the lipid profile, as well as data of computer tomography. The drug is prescribed 1 tab. 1 once a day for continuous reception. At the same time with Fenofibrate 145 is assigned to any lateinamerikas antioxidant drug (mainly with the highest amount of lutein in its composition). Currently, these drugs are wits the m vision Forte and nutri total. These drugs are prescribed with an interval of 2-3 months during the year. Vitrum vision Forte and nutri totals differ slightly in composition, so their perception of the patients also varies. Depending on the individual preferences of patients report that some of the drugs seems more effective. This drug them and recommended. Every 3 months is the study of lipid profile of the patient, and explores visual function.

Example: a Patient, 62 years of age. Age-related macular degeneration (AMD) "dry" form of both eyes. Related: Coronary heart disease. Hypertensive heart disease. Complaints gradual (within 2 years) reduced vision in both eyes, "blurring" of the image in the center that can interfere with the reading. Appealed to the Institute in 09.02.2011 B.C. this was observed in the clinic by place of residence, where he was treated mainly vasodilator and nootropic drugs (Cavinton, afobazole, the pharmacological) locally, with the combination of hard and soft drusens installation emoxipin.

Visual acuity of the right eye = 0.3 s +2,0D=0.3 to 0.4; the visual Acuity of the left eye = 0,4+2,5D or=0.6. The test Amsler negative distortion-free. In the study perimetric studies pathology it is not revealed. According to the OCT (optical coherence perimetric studies) in the presence of friends indicates undulating contour with the HHS pigment epithelium. This epithelium retains its thickness changes of the photoreceptors was not detected.

The thinned retina, the optical density of underlying tissues increased. In connection with ischemic heart disease study PHAGE was carried out. The fundus of both eyes practically identical with ophthalmologically: optic nerve pink, boundaries clear, veins slightly extended, long, tortuous artery, their walls are sealed, sclerotic (fibrous). Observed symptom Salus 1-11, which indicates the hypertonic nature of the lesion of blood vessels. In the macular and paramacular areas of both eyes many friends hard and soft, partially drain.

The patient was recommended: 1. Control and compensation of arterial pressure. Ansedonia of lipid, which revealed a significant significant increase of total cholesterol (up to 6.9 when remennik values of 3.1 and 5.2) and low density lipoprotein (4,56 to when remennik values of 1.5-3,50), other lipid parameters were at the upper limit of normal. The patient was prescribed: 1. The fenofibrate 145 1 tablet 1 time per day. The duration of reception no less than 8 months. 2. Vitrum vision Forte 1 tab. 2 times a day orally during the year, with an interval of 2-3 months.

After 3 months: visual acuity and the condition of the fundus without negative dynamics, however, the patient noted improvement comfortably the t of view, the feeling of "blur" the image in the center when reading appears much less frequently. These CLOUDS without negative dynamics. Blood pressure normalized with regular intake of antihypertensive drugs. In the study of lipid - lowering levels of total cholesterol to 4.8 and low-density lipoprotein to 3.2. Continued use of Fenofibrate 145 1 table 1 time a day. Welcome Vitrum vision Forte resumed after 2 months.

After 3 months at follow-up visual acuity: right eye = 0.3 s +2,0D=0,4. Visual acuity of the left eye = 0,4 +2,5D=0.5 to 0.6. The feeling of "blur" the image in the center disappeared completely.

Retinoscopy showed some recovery caliber and decrease tension veins, the condition of the arteries at the same level. The number of friends is not added, there is no calcification, no increase in the number of drain druses, which indicates the absence of negative dynamics. OCT without deterioration. In the study of lipid indicators total cholesterol = 4.2, and the low-density lipoprotein level of 2.4. Recommended to continue taking Fenofibrate 145 in the previous regime. It is recommended to repeat the course of treatment of Vitrum vision Forte 3 months.

Over the next 3 months (total observation period = 12 months). Visual acuity of the right eye = 0,3-0,4 +2,0D=0,40,5. Visual acuity of the left eye = 0,4 +2,5D=0.5 to 0.6. Comfort when reading has increased, "blur" is not resumed. Blood pressure remains offset by receiving antihypertensive drugs. In the fundus, compared with the previous survey, no negative dynamic. The lipid parameters: total cholesterol = 4,0; low-density lipoprotein level of 2.2. The remaining lipid profile levels remennik values. Because the patient noted that while taking Fenofibrate she has greatly improved the General condition with some improvement in visual function, it is proposed to continue taking Fenofibrate 145 on the background of periodic courses receive Vitrum vision Forte.

The proposed method of treatment, including the prescription of Fenofibrate 145 and lateinamerika antioxidants to date was used in 26 patients with "dry" form of AMD, in all cases, a positive result, in any case, there was no progression of the disease with significant follow-up period, none of the patient revealed no side effects or complications.

Thus, the proposed method for the treatment of "dry" form of AMD can improve the quality of life of patients on the background of stabilization or slight improvement in not only the visual features, but also the General condition, to avoid behold lesnych vascular accidents, reflected in the lipid profile of blood.

1. A method of treating patients with "dry" form of age-related macular degeneration, including oral use lateinamerika antioxidants and carotenoids, characterized in that they are used during the year with an interval of 2-3 months and additionally use fenofibrate in a period of time sufficient to normalize the lipid and maintain these indicators at that level.

2. The method according to claim 1, characterized in that as lateinamerika antioxidants and carotenoids use Vitrum vision Forte or nutri total.



 

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FIELD: medicine.

SUBSTANCE: invention relates to medicine, in particular to ophthalmology, and can be applied for treatment of "dry" form of age-related macular degeneration. Three-component complex, which contains mesenchymal stem cells, labelled with magnetic micro particles, is introduced to patient extrasclerally in macular zone projection. Cells in this complex are transposed into biological or synthetic fine-pore material. This material is fast connected with polymeric magnetic material with induction of permanent magnetic field 1.5 mT, with multipolar reversible magnetisation.

EFFECT: invention ensures improvement or stabilisation of visual functions due to directed delivery of cells to pathologic focus and holding cells in focus for the time, necessary for obtaining therapeutic effect.

FIELD: medicine, pharmaceutics.

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 pyrrol derivatives of formula (1): or a pharmaceutically acceptable salt thereof wherein the values A, R1-R3, n are specified in clause 1 of the patent claim.

EFFECT: compounds (1) inhibit activity against the interleukin IL-6 production that allows using them both in pharmaceutical compositions, and in a prophylactic drug for ocular inflammatory disease.

23 cl, 2 tbl, 22 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to granulated from liquid pharmaceutical compositions, which contain rhein or diacerein, or their salts, and pharmaceutically acceptable carrier. Compositions contain from 20 to 45 mg of rhein or diacerein. Invention also relates to methods of producing claimed compositions. Compositions by invention are bioequivalent to preparative form of diacerein in dosage 50 mg, sold under the trade name Art 50®. Compositions do not demonstrate variability in after meal condition and on an empty stomach.

EFFECT: considerable reduction of side effects, such as pulpy stool, in comparison with Art 50®.

13 cl, 37 tbl, 17 ex

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