(57) Abstract:The invention relates to medicine, in particular to pulmonology and pharmacology. Goal - increase the effectiveness of treatment of chronic obstructive bronchitis by increasing bronchodilatory effect. To do this, as a bronchodilator encouraged to use levodopa. The invention relates to medicine, in particular to pulmonology, and for the treatment of chronic obstructive bronchitis.The purpose of the invention is the expansion of the range of funds and effectiveness of the treatment of chronic obstructive bronchitis by applying a known drug "Levodopa" new appointment as bronholiticheskih tools.The drug levodopa (L-DOPA) is widely used in medical practice as ANTIPARKINSONISM funds. Meanwhile, the amino acid dioxyphenilalanin (DOPA) can not only be considered as an antiparkinsonian drug. The range of its therapeutic effect is much broader, as it is the precursor of all catecholamines. As you know, the catecholamines noradrenaline and adrenaline play an extremely important role in the regulation of bronchial tone muskulatur bronchitis, especially with clinical symptoms of bronchospasm, it is customary to include agonists, aimed at restoration of bronchial obstruction (adrenaline, izadrin, alupent, Berotec and others). However, the use of these drugs causes only short-term effect (usually no more than 3-4 h), and therefore must enter (by inhalation, injection, and other ways) many times, which is associated with a reduction in the duration of effect and adverse effect on the cardiovascular system. Additionally, repeated use may even intensify bronchial spasm.The above stimulated the search means, the current softer, longer and more physiological. These requirements are met by the drug levodopa, which increases the activity of the sympathetic-adrenal system, by strengthening the own products of catecholamines - epinephrine and norepinephrine. This examined through the regulatory systems of the organism, the mechanism of action of levodopa provides a softer, more gradual and prolonged therapeutic effect compared with direct agonists (epinephrine), including selective effect on2the adrenergic receptors (berotek, salbutamol and others).In about the high doses of the drug. In this case, as a rule, it is possible to avoid unwanted side effects.Thus, it is proposed the application of a known drug, "Levodopa" new appointment as bronchospasmolytic tools in chronic obstructive bronchitis is as follows: 0.25 g 2 times a day for the first 3 days, 0.25 g 3 times a day over the next 2 days and 0.5 g 2 times a day for the remaining 9 days; the duration of treatment 14 days, the dose rate of 12.0 gThe use of the drug for this scheme allows you to obtain a softer, more gradual and prolonged effect than the SS known agonists (including selective) and to avoid unwanted side effects on the cardiovascular system.P R I m e R 1. Patient M to N. M., 53 years old (case history N 1136 1983). Complaints of cough with phlegm, shortness of breath on mild exertion, recurrent attacks of difficult breathing. Sick himself for many years, when gradually appeared cough with little sputum. In the future, cough increased, periodically acquired paroxysmal character, increased shortness of breath. Exacerbation of the disease celebrates the th acrocyanosis. The nail plate type "hour glass". Chest expanded slightly in the anteroposterior dimension and the lower lateral parts. Lung sound with boxed shade. The excursion of the diaphragm 4 see Breathing hard. Dry, mostly treble rales on both sides in moderation. In the lower sections of the resonant subcapitata. Borders of the heart is within normal limits. Muffled heart sounds, clean, rhythmic. Pulse 76 beats per 1 minute, Blood pressure 120/70 mm RT.article The liver is not enlarged. Peripheral edema no.Fluoroscopy and radiography of the lungs: lung fields several high transparency. Figure lungs strengthened. Vessels strain, fuzzy. The roots extended, sealed. Excursions of the diaphragm is reduced. On 3-phase x-ray light, the difference in transparency Unsharp reduced. On roentgenogram breath teeth apertures have an elongated knee exhalation, there is a flattening of the tops of the teeth.Functional tests: VC/ANNUALLY - to 54.4%.Pneumotonometry: inspiratory flow 3.2 l/C, expiratory flow - 0.7 l/sSputum analysis: a slimy character, there is a spiral of Churchman, eosinophils places, occasionally the bronchial epithelium; tubercle bacilli not detecting the,4109/l WBC: eosinophils 3%, stab neutrophils 3%, segmented neutrophils 44%, lymphocytes 43% , monocytes 7%, ESR - 2 mm/hUrine analysis: without deviation from the norm.Clinical diagnosis: chronic obstructive bronchitis. Emphysema of the I century Pulmonary insufficiency II Art.On the background of General medical complex (alkaline inhalations, expectorant medicine, oxygen therapy) patients received a course of treatment with levodopa: 3 days 0.25 g 2 times, then 2 days 0.25 g 3 times and the next 9 days 0.5 g 2 times (dose rate of 12.0 g). The drug the patient did not cause discomfort and side effects. By the end of treatment the patient's health has improved significantly. Significantly decreased cough, stopped the attacks of difficult breathing, decreased the number of sputum (5-10 ml). When the inspection has decreased acrocyanosis, less hard was the breath has disappeared treble wheezing, preserved subtropical. Improved the speed parameters of external respiration function: VC/ANNUALLY - 59,3%; inspiratory flow - 5.4 l/C, expiratory flow rate of 3.8 l/s Favorable therapeutic effect was noted on the back of a marked activation of the sympathetic-adrenal system, as evidenced Dialin 12.1 n/mol and 25.3 n/mol, norepinephrine and 31.7 n/mol and of 62.4 n/mol).Thus, in a patient with chronic obstructive bronchitis with moderately severe asthmatic syndrome under the influence of a course of treatment with levodopa showed a significant improvement of clinical symptoms, speed parameters of external respiration function and activation of the functional state of the sympathetic-adrenal system.P R I m m e R 2. Patient K. O. I., 55 years old (case history N 1256 1983). Complaints about constant cough, shortness of breath with little exertion, frequent bouts of shortness of breath, General weakness.Ill for 10-12 years, when he began to notice the cough with scanty sputum, small shortness of breath. In subsequent health deteriorated, cough increased, the volume of sputum increased, appeared the attacks of difficult breathing. Annual exacerbation of the disease up to 3-4 times. Periodically, the treatment in the hospital.When viewed astenikov, low power. Moderate acrocyanosis. Expanded anterior-posterior dimension of the chest. In the act of breathing participate intercostal muscles. Nail phalanxes remind drum sticks, nail plate type "hour glass". Boxed what about the treble. Borders of the heart is within normal limits. The colours are muted, clean, rhythmic. Pulse 62 strike in 1 min. Blood pressure is 130/70 mm RT.article The abdomen is soft. The liver is not enlarged. Stool and urine output was normal.Fluoroscopy and radiography of the lungs: lung fields increased transparency. The roots extended sealed. Figure lungs moderately enhanced. The excursion of the diaphragm of small amplitude. Lesions not identified. When 3-phase x-ray the difference in transparency is reduced. If roentgenokymography breathing lengthened the expiratory phase.Functional tests: VC/ANNUALLY 59,3%, FEV124.9% of the sample tiffe to 31.2%.Sputum analysis: character - Muco-purulent, eosinophils - occasionally, leucocytes - a moderate amount, partially in decay. The epithelium of the bronchi - occasionally. Tubercle bacilli not found.The analysis of a blood: erythrocytes 4,61012/l, hemoglobin 154 g/l, color index of 1.0. Leukocytes 5,1109/l WBC: eosinophils 2%, stab neutrophils 62%, monocytes 2%, lymphocytes 32, ESR 15 mm/hUrine analysis without deviation from the norm.Clinical diagnosis: chronic obstructive bronchitis (pedasthma). Emphysema of the I century Pulmonary insufficiency II-III degree.
the I) was not effective enough. After the appointment of a course of treatment with levodopa in increasing dosage (first 3 days 0.25 g 2 times, then 2 days 0.25 g 3 times and the next 9 days 0.5 g 2 times) was observed satisfactory therapeutic effect. Much less coughing. A twofold decrease in the volume of sputum, much less had any attacks of difficult breathing, stopped accepting astropart. Slightly improved the speed parameters of external respiration function (sample tiffe 39% ). Parallel to the clinical improvement was observed stimulatory effect of levodopa on the state of the sympathetic-adrenal system (respectively the daily urinary excretion of adrenaline 6,0 n/mol and 39.6 n/mol, norepinephrine 24,0 n/mol and 79.2 n/mol).Thus, the use of a course of treatment with levodopa in gradually increasing the dosage has had a positive impact on the disease in a patient with chronic obstructive bronchitis with severe asthmatic syndrome (pedasthma). Drug use has significantly increased the efficiency of complex treatment has eliminated the need for frequent use of short-term sympathomimetic actions.Thus, on the basis of the above mentioned materials of the proposed extension of the ve drug providing a relatively low dose (daily dose of 0.5-1.0 g course treatment - 12.0 g) beneficial effect on the clinical manifestations of the disease, improve the function of external respiration, primarily bronchial patency, which allows in many cases to stop or significantly reduce the use of short-acting sympathomimetic agents (epinephrine, izadrina, alupent, Berotec and others), which have a number of negative side effects with frequent use. Application levodopa as a bronchodilator.
FIELD: medicine, anesthesiology, resuscitation.
SUBSTANCE: one should perform puncturing of epidural space at Th12-L1 level. Through the lumen of puncture needle one should introduce catheter to move it cranially at the depth of 3 cm. After that one should inject 10 ml 05%-marcaine solution to perform repeated injections per 5.0 ml every 4 h during 1-8 d. The effect is achieved due to unloading minor cycle of circulation.
EFFECT: higher efficiency of therapy.
FIELD: medicine, oncology.
SUBSTANCE: the present innovation deals with treating patients with uterine cervix cancer with relapses in parametral fiber and in case of no possibility for radical operative interference and effect of previous radiation therapy. During the 1st d of therapy one should intravenously inject 30 mg platidiam incubated for 1 h at 37 C with 150 ml autoblood, during the next 3 d comes external irradiation per 2.6 G-r. During the 5th d of therapy one should introduce the following composition into presacral space: 60 ml 0.5%-novocaine solution, 1 ml hydrocortisone suspension, 2 ml 50%-analgin solution, 1 ml 0.01%-vitamin B12 solution, 1.6 g gentamycine, 800 mg cyclophosphan, 10 mg metothrexate. These curative impacts should be repeated at mentioned sequence four times. The method enables to decrease radiation loading and toxic manifestations of anti-tumor therapy at achieving increased percent of tumor regression.
EFFECT: higher efficiency of therapy.
FIELD: organic chemistry, medicine.
SUBSTANCE: invention proposes new compounds of the general formula (I):
wherein R1 means one or more similar or different substitutes taken among the group consisting of hydroxy-group, halogen atom including F, Cl, Br and J, (C1-C5)-alkyl, (C1-C5)-alkoxy-group under condition that when R1 means one substitute then it is in ortho-position and when R1 means above one substitute then at least one substitute at R1 is in ortho-position; R2 means halogen atom including F, Cl, Br and J, (C1-C5)-alkyl, (C1-C5)-alkoxy-group; R3 means halogen atom including F, Cl, Br and J; R6 means hydrogen atom or methyl; and its salts with pharmaceutically acceptable acids, hydrates or solvates. Compounds elicit activity against acne and acne-related diseases.
EFFECT: valuable medicinal properties of compounds.
7 cl, 4 tbl, 43 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention proposes new tablets with size less 3 mm with sustained-releasing the opioid analgesic drug for 30 min in the amount above 75%. Invention provides opioid for oral intake with taking into account individual necessity of patient due to selection of required amount of mictotablets by dispenser.
EFFECT: valuable properties of tablet, expanded assortment of medicinal formulations of opioid analgesics.
19 cl, 4 tbl, 4 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention describes compound of the formula (I):
as a free form or salt wherein Ar means group of the formula (II):
wherein R1 means hydrogen atom or hydroxy-group; R2 and R3 each means independently of one another hydrogen atom or (C1-C4)-alkyl; R4, R5, R6 and R7 each means independently of one another hydrogen atom, (C1-C4)-alkoxy-group, (C1-C4)-alkyl or (C1-C4)-alkyl substituted with (C1-C4)-alkoxy-group; or R5 and R6 in common with carbon atoms to which they are joined mean 6-membered cycloaliphatic ring or 6-membered heterocyclic ring comprising two oxygen atoms; R8 means -NHR13 wherein R13 means hydrogen atom, (C1-C4)-alkyl or -COR14 wherein R14 means hydrogen atom; or R13 means -SO2R17 wherein R17 means (C1-C4)-alkyl; R9 means hydrogen atom; or R8 means -NHR18 wherein -NHR18 and R9 in common with carbon atoms to which they are joined mean 6-membered heterocycle; R10 means -OH; X means (C1-C4)-alkyl; Y means carbon atom; n = 1 or 2; p = 1; q = 1; r = 0 or 1. Also, invention describes pharmaceutical composition based on compound of the formula (I), a method for preparing compound of the formula (I) and intermediate compound that is used in the method for preparing. Compounds elicit the positive stimulating effect of β2-adrenoceptor.
EFFECT: improved preparing method, valuable medicinal properties of compounds.
13 cl, 3 tbl, 35 ex
FIELD: medicine, intensive therapy, resuscitation.
SUBSTANCE: along with conventional therapy one should apply serotonin adipinate, 10-500 mg of its solution should be intravenously injected at the rate of 10-30 mg/h. Injection should be repeated during 10-14 d. The method provides improved function of smooth muscle cells of pulmonary vessels by increasing efficiency of oxygenation in this category of patients.
EFFECT: higher efficiency.
1 cl, 2 ex, 1 tbl
FIELD: medicine, ophthalmology.
SUBSTANCE: one should introduce 1.0% serotonin adipinate solution intravenously due to infusion once daily for 10-12 d. The method enables to increase visual functions due to decreased tissue hypoxia and normalization of retinal microcirculation, resorption of hemorrhages, reverse development of retinal edema, normalization of functional thrombocytic activity and hemostatic values.
EFFECT: higher efficiency for therapy.