A method of treatment of conditions involving giperagregatsiyu platelets
(57) Abstract:The invention relates to medicine, and is intended for the treatment of conditions involving giperagregatsiyu platelets. To autoplaza add adenosine triphosphate (ATP), determine the amount sufficient for maximal platelet aggregation, and put it in the same amount of intact autoplasma. Then its center and the resulting nadosadocnuu liquid (autokeratometry preparation) is injected 5,0 -10,0 ml Method can effectively treat conditions associated with giperagregatsiyu platelets. table 2. The present invention relates to the treatment and is intended for treatment of conditions and diseases involving giperagregatsiyu platelets. Currently, as a result of numerous experimental and clinical studies have established that increased platelet aggregation accompanies the course of a number of severe human diseases: myocardial infarction, cardiac and cerebral ischemia, atherosclerosis, diabetes, hypertension and other diabetes, in particular, hypercoagulation is one of the etiological factors Dacia leads to the accumulation of circulating blood platelet aggregates and ultimately to the occlusion of blood vessels. It is known that the progression of the above diseases increases the blood hypercoagulation and depression of fibrinolysis.In the treatment and prevention of diseases and conditions involving giperagregatsiyu platelets, currently widely used antiplatelet agents: pentoxifylline (trental); ticlopidine (ticlid).The disadvantage of the above drugs as in intravenous and oral application are hemorrhagic complications, trombopenia, leukopenia, agranulocytosis, severe allergies, as well as the inability to use these drugs because of their contraindications in patients with severe coronary atherosclerosis and vascular brain with acute gastric ulcer and duodenal ulcer, liver disease, pregnancy and breastfeeding.The objective of the proposed method is to obtain the drug, which extends the range of use and allows you to get the desired disaggregated effect in the absence of side hemorrhagic complications and etc. due to the use of the drug, possessing both disaggregated and fibrinolytic effect.It is well known that platelets play an important of NCCI contain more than fifty of biologically active substances. All these substances are found in platelets separately in the dense granules - granules and lysosomes. Interestingly, platelets carry biologically active substances diametrically opposite actions, for example, activators and inhibitors of fibrinolytic system, agregaty and disaggregants. Therefore, it is difficult to imagine that the process is irreversible platelet aggregation when there is a simultaneous selection of biologically active substances, and the formation of platelet plugs to keep yourself in the equilibrium content of activators and inhibitors of fibrinolytic system, and Agrigento and antiplatelet. In this case, the platelets are unlikely to have been able to implement its main physiological function in the closure of the defect in a blood vessel.This was the task, obtaining the drug from autoplasma with disaggregated and fibrinolytic action. As in platelet plug is dominated by substances that inhibit fibrinolysis and agregaty, substances of the opposite action as the formation of platelet clot (thrombus) are platelets in the plasma and are carried away by the blood stream, therefore, the running mechanism of the drug, having disaggregated and fibrinolytic action. The formation of platelet plugs, i.e., the launching mechanism of irreversible aggregation occurs when exposed to platelets, thrombin, collagen and ADP (adenosine diphosphorous acid). The above agregaty widely used in clinical and laboratory practice. It is known that adenosine trifosfornaya acid (ATP) does not belong to agrigentum and therefore never used in clinical and laboratory practice. However, in 1965, G. Marr showed that in plasma after a few seconds, 50% of ATP turns into ADP (Barkagan 3.S., "Hemorrhagic diseases and syndromes". M., 1980, S. 12-13).Studies have shown that with the proposed method of treatment of conditions involving giperagregatsiyu platelets by intravenous autohematopoietic the drug significantly reduced platelet aggregation (P 0,01) (see tab. 1). In addition, autoprepare compared with intact plasma occur following qualitative and quantitative changes: increased concentration of plasminogen (P 0.01), and reduced (P 0,01) concentration of inhibitors of proteolytic enzymes (1- protease inhibitor;2- macroglobulin), snige the(P 0,01) (see table. 2). Determination methods specified in the table of indicators of well-known (Kalashnikov B. B., Markov 0.A., Platonov because, Svishchev A. B. // Abstracts of the international Symposium "problems of development of laboratory diagnostic techniques". VNMO the USSR Ministry of health, Smolensk, 1988, S. 41-44 and S. 47-50; Andreenko, Century, Karabasov M. A., Lutuli L. Century. and other research Methods fibrinolytic system of blood. - M, Moscow University Publishing house, 1981, 43 - 46; Manchini G., I. P. Vaerman, Carbonava A. 0. Heremans kept carrying out renovation I. E. A single-radial-diffusion method for the immunological quantitation of proteins, in Peeters H (Ed.). Protides of thebiological Fluids, Elsevier Publisching Comp. Amsterdam, London, New-York, 1964; 11th colloguirn, Brudes, 1963, p. 370-373). Disaggregated property and increase fibrinolytic activity autohematopoietic of the drug was achieved only when a single cell in the ATP required for maximum aggregation autochromatic. The results of these studies was the prerequisite for the proposed method of treatment.The method was as follows: blood is taken from the cubital vein in an amount of, usually, 10.0 ml, a syringe with a capacity of 10.0 ml, in which the anticoagulant is heparin 34 ED. Next, determine platelet aggregation by a known method Born O'brien (Born V. R. Aggregation of blood platelete is islote ATP used in an amount of 0.1-0.5 mg/ml depending on the individual response of platelets to the effects of ATP for maximal platelet aggregation (average 50% decrease of optical density of the platelet). Then, the resulting suspension was centrifuged at a speed of 3000 rpm for 2-3 min and the thus obtained supernatant (autokeratometry drug) was administered intravenously in the amount of 5.0-10.0 ml.Example 1. Patient N. And.D., 37 years. Diagnosis. Diabetes mellitus. Preproliferative diabetic retinopathy in both eyes. Suffering from diabetes for 20 years. The reduced visual acuity in both eyes marks the last 2 years. The ratio of platelet aggregation increased 165,0 mm for 4 years takes trental and tickled, but the rate of platelet aggregation remains sharply increased.Before treatment. The ratio of platelet aggregation 170,0 mm fluorescent angiogram of the fundus of both eyes revealed ischemia of the retina. Visual acuity: right eye -0,3 with correction = 0,4, left eye - 0,3 correction = 0,5.Treatment. Blood was taken from the cubital vein of 20.0 ml sterile syringe with a capacity of 10.0 ml, which before the blood sampling was heparin 34,0 ED. The conventional method of separating red blood cells from blood plasma. The resulting plasma was divided for convenience, portions of 2.0 ml was first identified platelet aggregation (by the above methods), gradually adding ATP is nactoy plasma simultaneously injected the same amount of ATP and-0.4 mg/ml and the maximum platelet aggregation produced centrifugation at a speed of 3000 rpm for 2-3 min and the thus obtained supernatant (autokeratometry drug) was administered intravenously in the amount of 5.0-10.0 ml, after 14 days, all 5 injections.The results of the treatment. The ratio of platelet aggregation decreased to the upper limit of normal - 41,0 mm visual Acuity of 0.1 on each eye; decreased number of areas of ischemia of the retina.Example 2. Patient W. C. A., 58 years old, suffers from ischemic heart disease (angina) for about 9 years. Over the past year the pain in the heart area increased to 4-5 times a day, despite the maximum receive mode sushka, nitronga and Panangin, pain was not relieved until 2 h, the pain was accompanied by the feeling of shortness of breath (dyspnoea) and palpitations. In addition to the changes on the electrocardiogram characteristic of ischemic heart disease was increased almost 5 times (180,0 mm) coefficient of platelet aggregation.The treatment was carried out autokeratometry drug (compared with the usual treatment - nitrong, sustak), which was injected intravenously in the amount of 5.0-10.0 ml, for the treatment took 4 injections. On the second day after the treatment the patient's condition has improved markedly - disappeared dyspnea, frequency, and intensity of pain in the heart area decreased in the study of platelet aggregation is revealed pronounced disaggregating effect. Coefficient which was stvovala about the effectiveness of the used drug. A method of treatment of conditions involving hypergravity platelets by intravenous drug desegregate, characterized in that as desegregate use autokeratometry the drug, which is a supernatant autologous blood of the patient, the resulting platelet aggregation under simultaneous exposure to 0.1 - 0.5 mg ATP per 1 ml of plasma and subsequent centrifugation, and the drug is administered in the amount of 5.0 - 10.0 ml.
FIELD: organic chemistry, medicine, oncology.
SUBSTANCE: invention relates to new glycosides of indolo[2,3-a]-pyrrolo[3,4-c]carbazol-5,7-diones of the general formula (1)
wherein: -R1 means residue of mono- or disaccharide in pyranose form taken among the group: D-Rib, L-Ara, D-Xyl, D-Gal, D-Glc, D-Lac; -R2 means hydrogen atom, methyl group or residue of mono- or disaccharide; -R3 means hydrogen atom, hydroxyl group, amino-group or formamido-group; each -X1 and -X2 means independently of one another hydrogen atom or bromine atom under condition that they can't mean hydrogen atom simultaneously and under condition also that if R1 means disaccharide residue then R2 differs from hydrogen atom. Prepared derivatives show, in particular, cytotoxic and antitumor activity against melanoma B16 and Ehrlich tumor.
EFFECT: valuable medicinal properties of derivatives.
3 cl, 3 tbl, 2 dwg, 8 ex
SUBSTANCE: method involves treating hepatitis C virus infection or hepatitis B virus infection by introducing carboxamidine of formula 1 or its pharmaceutically permissible salt at a dose of 0.1-40.0 mg/kg of body mass. Α-interferon is also introduced. Compound of formula 1 is in D-configuration.
EFFECT: enhanced effectiveness of treatment.
7 cl, 5 dwg
SUBSTANCE: composition comprises Clindamycin phosphate and water-soluble zinc salt taken in molar proportion of 1.2:1 to 1:2. Arising polymer gel is applicable in local treatment of acne vulgaris and acne rosacea under very low systemic Clindamycin level being retained. Aqueous nature of the drug prevents skin from drying. The drug exerts both immediate and prolonged action allowing its application once a day.
EFFECT: enhanced effectiveness of treatment.
39 cl, 5 dwg, 6 tbl
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel derivatives of glucopyranosyloxypyrazole of the general formula: wherein R means hydrogen atom, lower alkyl, acyl, alkoxycarbonyl, acyloxymethyl or alkoxycarbonyloxymethyl; one of Q and T represents a group of the general formula: wherein P means hydrogen atom, lower acyl or alkoxycarbonyl but other radical means lower alkyl or halogen(lower alkyl); R2 means hydrogen atom, lower alkyl, alkoxy-, alkylthio-group, halogen(lower)alkyl) or halogen atom under condition that P doesn't represent hydrogen atom when R means hydrogen atom or lower alkyl. Also, invention relates to pharmaceutically acceptable salts of these compounds, pharmaceutical compositions used for prophylaxis of renal glucose re-absorption and eliciting the inhibitory activity with respect to human SGLT2, pharmaceutical combinations that are used for prophylaxis or treatment of diseases associated with hyperglycemia.
EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.
36 cl, 1 dwg, 6 tbl, 48 ex
SUBSTANCE: method involves treating gingival pocket, separating circular ligament from cervix and gingiva, cleaning alveoli from granulation tissue, tamponing alveoli, treating replant, introducing it into cell and fixing with splint. Treating gingival pocket, separating circular ligament from cervix and gingival is carried out with ultrasound of 26.5 kHz frequency and instrument oscillation amplitude of 30-35 mcm through continuously supplied 1% Chlorhexin solution layer with 1 min long exposure time. Alveoli are cleaned from granulation tissue with ultrasound of 26.5 kHz frequency and instrument oscillation amplitude of 30-35 mcm through 1-2 mm thick 30% Lincomycin solution layer with 2 min long exposure time.
EFFECT: enhanced effectiveness of treatment; reduced risk of complications.
FIELD: medicine; pharmacology.
SUBSTANCE: invention relates to the benzo-iso-selenium zolonyl derivatives with the general formula (I) or (II) , where R - C1-C6-alkylen, phenyliden, biphenyliden, R' - polysaccharide residue or residue , where M - Pt or Pd.
EFFECT: compounds possess anti-inflammatory, antiviral and antithrombotic activities.
12 cl, 7 ex, 8 tbl
FIELD: medicine; dental surgery.
SUBSTANCE: for this purpose first of all root canals are filled with paste based on eugenol, zinc oxide, dry iodoform and lincomycin hydrochloride taken in ratio 3:3:1:1. Then cortical plate trepanation and cyst membrane extraction are followed with ultrasonic treatment of bone cavity through 0.05% miramistine within 5 minutes using ultrasonic device US-102 at exposure intensity 0.05-0.4 Wt/cm in pulse mode. Treated bone cavity is introduced with filling-bandage "Collost" and with mixed osteoplastic gel "Collost" and lincomycin hydrochloride taken in ratio 2:1, and is covered with membrane "Collost". Wound is isolated from mouth cavity with film "Dyplene-denta" with lincomycin.
EFFECT: enables to accelerated wound healing process due to complete osteointegration and angioosteogenesis of implanted material.
SUBSTANCE: invention concerns substituted heterocyclic fluorglucoside derivatives of the formula (I) , where R1 and R2 are independently F, H, or one of R1 or R2 residues is OH; R3 is OH or F, so that at least one of R1, R2, R3 residues is F; R4 is OH; A is O; X is C or N, so that if Y = S, X should be C; Y is N or S; m = 1; R5 is hydrogen, OH or (C1-C6)-alkyl optionally mono- or polysubstituted by fluorine; R6 is H or (C1-C6)-alkyl, if required; or, if Y = S, R5 and R6 form phenyl together with carbon atoms to which they are linked; B is (C1-C6)-alcandiyl or -CO-NH-CH2-; n = 2 or 3; Cyc1 is phenyl or thiophenyl; R7 is hydrogen, F, CI, Br, J, (C1-C6)-alkyl or (C1-C6)-alkoxy optionally mono- or polysubstituted by fluorine; R8 is hydrogen or halogen; R9 is hydrogen; or R8 and R9 together mean -CH=CH-CH=CH-, -CH=CH-C((C1-C6)-alkoxy)=CH- or -OH=CH-O- and together with carbon atoms to which they are linked form Cyc2, which is phenyl, optionally substituted (C1-C6)-alkoxy or furanyl respectively; and their pharmaceutically acceptable salts.
EFFECT: obtaining efficient medicine for sugar level decrease in blood.
7 cl, 1 tbl, 31 ex