Method of decreasing blood microvesicles in crisis course of arterial hypertension

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to haematology and cardiology, and concerns decreasing microvesicles in blood in crisis course of arterial hypertension. That is ensured by administration of Irbesartan in dosage 150 mg once in the morning and Nebivolol in dosage 2.5 mg once in the morning for at least 7 weeks.

EFFECT: method ensures normalised blood concentration of microvesicles that in turn allows reducing risk of thrombotic complications in said group of patients.

1 ex

 

The invention relates to medicine, namely to Hematology and cardiology.

Analogues of the proposed method of correction of the level of microvesicles in the blood with arterial hypertension (AH) with crisovan course does not exist.

It is known that an important feature of the cytoplasmic membrane is asymmetric phospholipid and protein composition of the two leaflets of the bilayer, which occurs under the action of intracellular enzymes, differences in the ionic composition of the cytoplasm and the extracellular fluid. The asymmetry of the bilayer determines thrombogenicity and hemocoagulation properties of blood cells and endothelium of blood vessels and, in addition, participates in the creation of the gradient of curvature of the folds, morsiani, outsoruce areas of the membrane in the form of microvesicles.

Formed by exocytosis, necrosis and apoptosis fragments of cell membranes are able to withdraw and form bubbles with a diameter of from 0.05 to 3.0 μm. The size of the microvesicles depends on the nature of the agent acting on the target cell. Microvesicles are platelet and nitrobacteria origin. They are formed on the cell surface, lusiwasi with the cytoplasmic membrane. Therefore, they contain various membrane glycoproteins, proteins of the cytoskeleton, fibers, chains of myosin, etc.

Microvesicles are not only of the catalytic surface is for internal tenaz" (supramolecular complex, consisting of factor IXa, factor VIIIa, and phospholipids) and prothrombinase complex, but also able to influence the proteolytic inactivation of factors Va and VIIIa by activated protein C in combination with protein S. Therefore reducing the level of microvesicles in the blood leads to reduction of hemocoagulation potential estramboticos blood plasma.

Angiography with crisovan over the rise in blood levels of microvesicles, causing the increase of coagulation opportunities plasma. However, the approaches to reduce the level of microvesicles in the blood remain very poorly developed. Angiography with crisovan over such approaches has not previously been used. In patients with hypertension with crisovan over to reduce blood pressure are applied blockers angiotensin receptor and β-blockers (Vstudio.net and other Arterial hypertension in the metabolic syndrome: pathogenesis, therapy basics". Consilium medicum 2004, Vol.6, No. 9, http://www.voed.ru/art.gip.metab.sindr.htm).

However, never before medical complex, consisting of irbesartan and nebivolol, was not used in patients with AH crisovan over to reduce the level of microvesicles.

The aim of the invention is the lowering of the level of microvesicles in the blood in patients with AH crisovan over.

The essence of the proposed method lies in the fact that for the correction of the level of microvesicles blood Bolnisi with crisovan over at least 7 weeks assigned irbesartan 150 mg 1 every morning and nebivolol 2.5 mg 1 every morning.

The method allows to adjust the level of microvesicles in the blood of patients with hypertension with crisovan over for at least 7 weeks, putting it on a level close to that of healthy people. Subject to the subsequent recommendations of the proposed method it is possible to maintain the level of microvesicles at the optimal level, which will significantly reduce the risk of thrombotic complications, reduce the number of cases of temporary disability, to expedite patient treatment and improve the quality, reduce disability, and also to prolong the life and reduce mortality of patients with arterial hypertension with crisovan over from a heart attack and stroke.

The inventive method is carried out as follows.

The setting microphysical blood carry out activity 5-nucleotidase in serum (Ldzierba, Dimswart, Ihantola and other Cellular microvesicles in the dynamics of experimental endotoxinemia // Bulletin of experimental biology and medicine: monthly international scientific-theoretical journal / RAMS. - 2006. volume 142, No. 11. - S-520). OK its level representing 63.8±2,5 ncat. When the level of microvesicles in the blood of patients with AH with crisovan over to the appointment of treatment with irbesartan 150 mg 1 every morning and nebivolol 2.5 mg 1 every morning.

Example. Examined the patient L., 46 years old, with hypertension grade 2, stage 2 with crises is m over H0. At the time of examination, blood pressure was 165/100 mm Hg, when examined, was found increased levels of microvesicles in blood plasma 189,7 ncat. The patient had been assigned irbesartan 150 mg 1 every morning and nebivolol 2.5 mg 1 every morning. The patient was regularly looked after the start of treatment. Simultaneously with the inspection was carried out to determine the level of blood microvesicles.

After 7 weeks of treatment, the patient's blood pressure stabilized at 125/85 mm Hg at normal levels, blood microvesicles comprising 60,9 ncat.

The patient is asked to comply with these recommendations in future.

The use of the proposed method of correction of the level of microvesicles blood Hematology and cardiology will help to avoid many of vascular complications in patients with AH crisovan over, they reduce the number of cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality.

The method of reducing the content of microvesicles in the blood in arterial hypertension crisovan over by applying irbesartan 150 mg 1 every morning and nebivolol 2.5 mg 1 every morning for at least 7 weeks.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention refers to medicine, particularly to cardiology, and concerns normalising the functional responsiveness of cardiovascular system in elderly and senile patients suffering arterial hypertension and metabolic syndrom. That is ensured by estimating the condition of functional reactivity of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure (BPav.dyn.) and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after load by formula: FRI=(BPav.dyn. x HR)100 (standard units). The value PFR increased more than by 20 standard units requires the complex therapy including individually prescribed hypocaloric diet calculated by formula considering sex and age and body weight, graduated static and dynamic physical activity, and introduction of irbesartan in dosage 150 mg once in the morning, and pioglitazone in dosage 30 mg once in the morning at least for 3 months.

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

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FIELD: medicine.

SUBSTANCE: invention refers to medicine, particularly to cardiology, and concerns normalising the functional responsiveness of cardiovascular system in arterial hypertension. That is ensured by estimating the condition of functional responsiveness of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure and heart rate (HR). These data are used to evaluate a functional responsiveness index (FRI) before and after load by formula: FRI=(BPav.dyn. x HR)100 (standard units). When observing the FRI gain by 20 standard units and more, losartan is prescribed in dosage 50 mg in the morning once a day and lacidipine in dosage 2 mg in the morning once a day for at least 2 months.

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2 ex

FIELD: chemistry.

SUBSTANCE: invention refers to compounds of the formula (I) and pharmaceutically acceptable salts, where R1-R7 mean the same as provided in the invention description and claim. Compounds of the formula (I) are specific inhibitors of 11b-HSD1. They can be applied in treatment and/or prevention of diseases caused by dysfunctions related to 11b-HSD1 enzyme, particularly in treatment and/or prevention of metabolic diseases, obesity, dyslipidemia, hypertension and/or diabetes, especially diabetes type "П". Additionally subject matter includes pharmaceutical composition for treatment and/or prevention of the said diseases.

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21 cl, 1 tbl, 146 ex

FIELD: medicine.

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2 ex

FIELD: medicine.

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1 ex

FIELD: medicine.

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

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1 ex

FIELD: medicine.

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1 ex

FIELD: chemistry.

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

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26 cl, 7 tbl, 13 ex, 20 dwg

FIELD: medicine.

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1 ex

FIELD: medicine.

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

1 ex

FIELD: medicine.

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2 ex

FIELD: medicine.

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

1 ex

FIELD: medicine.

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

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

1 ex

FIELD: medicine.

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

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

1 ex

FIELD: medicine.

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

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1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a free base (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)- ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine in crystalline form, having a powder X-ray diffraction pattern with peaks at diffraction angles (2θ) 15.7±0.1, 17.3±0.1 and 19.7±0.1. The invention also relates to a pharmaceutical composition, to methods of treating cancer in mammals, as well as to a method of treating abnormal cell growth in mammals in need of such treatment.

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12 cl, 1 ex, 3 tbl, 2 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound or its salt of formula 1: , where A, E, D, R0, R1-R4 and a assume values given in the formula of invention. The invention also relates to an antioxidant medicinal agent.

EFFECT: effectiveness during treatment of ischemic diseases of organs, during treatment of diseases caused by oxidation cell disorders and when inhibiting disorders of the retina.

4 cl, 1 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

or

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

EFFECT: compounds are highly effective.

40 cl, 48 tbl, 191 ex

FIELD: chemistry.

SUBSTANCE: invention proposes 5-member heterocyclic inhibitors of kinase p38, including kinase p38α and kinase p38β, based on pyrazoles and imidazoles, with the general formula given below , in which ring B is phenyl, and C is a pyrazole or imidazole ring, and the rest of the symbols assume values given in paragraph 1 of the formula of invention.

EFFECT: there are described pharmaceutical compositions containing said compounds, as well as methods of using the compounds and compositions, including a method of treating, preventing or suppressing one or more symptoms of diseases and conditions mediated by kinase p38 which include, but not limited to, inflammatory diseases and conditions.

31 cl, 6 tbl, 175 ex

Pyrazoles // 2381217

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I), where one of R1 and R2 is hydrogen or alkyl, and the other is (CH2)PY, where p=0 or 1, Y is a saturated mono-, bi- or tricyclic 5-10-member cycloalkyl ring optionally substituted with alkyl, or R1 and R2 together with N form a 7-10-member saturated bicyclic ring Z, optionally substituted with halogen, or a 5-7-member monocyclic ring Z, optionally substituted with alkyl, phenyl, phenylalkyl or pyridinyl; R3 is [2,2']bithiophenyl, 1-methylindole, 2,3-dihydrobenzo[1,4]dioxin, benzo[1,3]dioxole, benzothiophene, dibenzofuran, furan, naphthalene, quinoline, thianthrene, thiophene or pyrrole, or biphenyl substituted with halogen, or phenyl optionally substituted with one or more amino, cyano, formyls, halogens, hydroxyl, hydroxymethyls, acyls, acylamino, alkoxy, nitro, trifluoromethoxy, trifluoromethyls, phenoxy or benzyloxy, or R3 is a group, where Ar is phenyl substituted with halogen; and R4 is alkyl; and pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition with inhibitory activity towards the 11β-hydroxysteroid dehydrogenase1 (11(β-HSD1) enzyme.

EFFECT: pyrazole composition is disclosed.

22 cl, 1 tbl, 116 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to cardiology and concerns normalising functional reactivity of cardiovascular system (CVS) in stenocardia function classes I-II. That is ensured by estimating the condition of functional reactivity of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure. These data are used to evaluate a functional responsiveness index (FRI) before and after stress by formula: FRI=(BPav.dyn. x HR)/100 (standard units). The PFR gain by more than 20 standard units requires administration of lisinopril in a dose 5 mg a day in the morning and metoprolol in a dose 50 mg a day in the morning.

EFFECT: method provides normalising functional reactance of cardiovascular system and higher psychoemotional load tolerance in the given group of patients within two-month therapeutic course.

3 ex

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