The way to prevent recurrent myocardial infarction |
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IPC classes for russian patent The way to prevent recurrent myocardial infarction (RU 2180843):
 4-(allumination)-2,4-dihydropyrazol-3-ones, the method of production thereof and pharmaceutical composition / 2180659
The invention relates to 4-(allumination)-2,4-dihydropyrazol-3-Onam General formula I, where R1denotes benzyl, alkoxybenzyl with 1-3 C-atoms in the alkyl part, unsubstituted or substituted once to three - fold amino, acyl, halogen, nitro, CN, AO, carboxyla, carbamoyl, N-allylcarbamate, N, N-dialkylammonium (with 1-6 C-atoms in the alkyl part), A-CO-NH-, AND-O-CO-NH-, AND-O-CO -, NA-, SO2NR4R5(R4and R5can denote H or alkyl with 1-6 C-atoms or NR4R5represents 5 - or 6-membered ring, optionally with other heteroatoms, like N, or O, which may be substituted),-CO-NH-SO2-, A-CO-NA-SO2- (AND-SO2-)2N-, tetrazolium phenyl; or pyridyl; R2denotes alkyl with 1-5 C-atoms, ethoxycarbonylmethyl, hydroxycarbonylmethyl; R3denotes unbranched or branched alkyl with 1-5 C-atoms, unbranched or branched alkoxy with 1-5 C-atoms or CF3And denotes unbranched or branched alkyl with 1-6 C-atoms or CF3and their salts
 Derived 4-oxo-1,4-dihydropyrimidin having antihypoxic, cerebroprotective and immunotropic activity / 2179974
The invention relates to a new compound - derived 4-oxo-1,4-dihydropyrimidin formula I, having antihypoxic, cerebroprotective and immunotropic activity, and may find application in medicine
 Method of correction of lipid peroxidation in patients with ischemic heart disease / 2178704
The invention relates to medicine, namely cardiology, and can be used for the correction of lipid peroxidation in patients with ischemic heart disease
 The combination of inhibitors of no-synthetase and catchers reactive forms of oxygen / 2174844
The invention relates to pharmaceutical compositions containing as active ingredient at least one substance inhibiting NO-synthetase, and at least one substance that traps the reactive forms of oxygen, and, optionally, a pharmaceutically acceptable carrier
 Chetyrehskatnye imidazole derivatives, processes for their preparation, intermediate compounds and pharmaceutical composition / 2174513
The invention relates to a method for producing compounds of formula (I) consists in the fact that the compound of formula (IX):
 < / BR>in which R1' has the abovementioned meaning and M represents a hydrogen atom or the radical R2' which has the values specified above for R2in which the possible reactive functions can be protected by a protective group, is subjected to reaction with the compound of the formula (VIII) defined above, to obtain a product of formula (X):  < / BR>in which R1' M and R4' have the above values, the obtained compound of formula (X), if M implies R2' defined above, is subjected to a halogenation reaction, to obtain the product of formula (XI):  < / BR>in which R1', R2', R4' and Hal have the above values, which is subjected to the reaction of the exchange of the halogen-metal, then the reaction with the compound of the formula (XII):  < / BR>in which R9' matter referred to in paragraph 1 for R9where possible reaction ф�g/rupat4/200110/01/2174513-36t.gif" ALIGN="ABSMIDDLE">< / BR> in which R1', R2', R4' and R9' have the above meanings and, if necessary, or interact product of formula (I2) with the compound of the formula (XV): O=C=N-R6' (XV) in which R6' matter referred to in paragraph 1 for R6in which the possible reactive functions can be protected by a protective group, to obtain a product of formula (I3):  < / BR>in which R1', R2', R4', R6' and R9' have the above meanings, or the product of formula (I2) is subjected to a saponification reaction with the product of formula (I4):  < / BR>in which R1', R2', R4' and R9' have the above meanings, is subjected to reaction with COCl2to obtain a product of formula (I5):  < / BR>in which R1', R2', R4' and R9' have the above meanings, or the product of formula (X), provided that M denotes a hydrogen atom, is subjected to a halogenation reaction to obtain a product of formula (XIV): in which R1', R4'Hal and R3" have the above values, the compound obtained is subjected to the reaction of the exchange of the halogen-metal, then the processing of the compound of formula (IVa') (IVb'), (IVc'), (IVd') or (IVe') defined above, to obtain a product of formula (I7):  < / BR>in which R1', R4', R2and R3" have the above meanings; then the above products of formula I2, I3, I4, I5, I6, I7that are a product of the formula I, allocate or subjected, if necessary, one or more reactions of transformation to other products of the formula I, in any order: a) esterification of the acid function, (b) saponification functions of ester to acid functions, C) transforming functions of ester function acyl, d) transforming Sinopoli in an acid function, e) conversion of the acid function to an alcohol function, g) transforming functions alkoxy function hydroxyl or hydroxyl function in the function alkoxy, h) oxidation of the alcohol function to the aldehyde, acid or keto-function i) the conversion of the formyl radical in the radical carbarnoyl, j) turning radical carbarnoyl in the nitrile radical, k) converting the nitrile radical in tetrazolyl, l) oxidation of ancilliary or aristocraty to the corresponding sulfoxide or sulfone, m) the transformation function sulfide, sulfoxide or sulfone function corresponding sulfoximine, n) the transformation function oxo function of thioxo, a) transforming radical  < / BR>in radical  < / BR>p) conversion of the acid function in function  < / BR>q) is the transformation function of beta-keto-sulfoxide in the function of alpha-ketotioefir, r) the conversion of carbamate into urea and, in particular, sulfonylamino in the sulfonylurea, s) removal of protective groups, which can protect the reaction functions, t) salt formation using mineral or organic cisisomer, enantiomers and diastereoisomers  Salt ethyl ester 3-(2-(4-(4-(aminoiminomethyl)phenyl)-4 - methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3 - phenylpropionic acid, method for their production and pharmaceutical composition based on them / 2174119
The invention relates to compounds of the formula I, in all stereoisomeric forms and mixtures in any ratio, where NV denotes maleic acid, to a method for producing compounds of formula I, which lies in the fact that compounds of the formula II exercise anionic exchange with maleic acid and/or maleate
 Substituted 1,2,3,4-tetrahydro-2-naphthalenamine, the method of production thereof and pharmaceutical composition based on them / 2169727
The invention relates to new substituted 1,2,3,4-tetrahydro-2-naphthalenamine formula I, where R1and R2independently represent hydrogen, C1-4alkyl, C1-4alkoxy, halogen, trifluoromethyl; R3represents hydrogen, hydroxyl, C1-4alkoxyl, cyano, carbarnoyl; R4and R5independently represent hydrogen, C1-4alkyl, hydroxy2-4alkyl, or form together with the nitrogen atom to which they are attached, piperidine; in the form of free bases or salts obtained by attaching acid
 Drug for the treatment of mastitis in animals / 2180839
The invention relates to agriculture, in particular animal, and can be used for treatment of mastitis in animals
Drug for the treatment of mastitis in animals / 2180839
The invention relates to agriculture, in particular animal, and can be used for treatment of mastitis in animals
 Drug for the treatment of mastitis in animals / 2180559
The invention relates to the field of veterinary medicine
 The method of treatment of subclinical mastitis in cows / 2180221
The invention relates to the field of veterinary medicine, in particular to methods of treatment of subclinical mastitis in animals
 The remedy for the prevention and treatment of gastrointestinal and respiratory diseases in calves / 2179846
The invention relates to medicines veterinary medicine
 Tool for the prevention of technological stress in cattle / 2179803
The invention relates to agriculture and can be used in animal husbandry
The way to prevent complications of extracorporeal shock wave lithotripsy / 2179438
The invention relates to medicine, in particular to urology
 Substituted imidazolidin-2,4-dinavia compounds as pharmaceutical active ingredients / 2163603
The invention relates to substituted imidazolidin-2,4-donovin compounds, method of their production and to the use of these compounds in medicine
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(57) Abstract: The invention relates to medicine, particularly cardiology, and for the prevention of a second heart attack in people without hypertension. The essence of the method lies in the fact that at 16-18 days from the onset of myocardial infarction enter atenolol 12.5 mg in the morning and Enap 2.5 mg in the evening. In the second week, increase the dose of atenolol to 12.5 mg in the morning and in the evening, leaving the dose of Enap 2.5 mg in the evening. On the third week of atenolol continue to impose 12.5 mg in the morning and evening and Enap 2.5 mg in the morning and evening. In the absence of hypotension on a 4-5 week, increase the dose of atenolol to 25 mg in the morning and evening. therapy continued for two years with the regular a single dose of 125 mg of aspirin and extended-release nitrates in conventional dosages. The method improves the efficiency of prevention of recurrence of myocardial infarction. 4 C.p. f-crystals, 2 tab. The invention relates to the field of medicine, particularly cardiology. Coronary heart disease (CHD) is one of the most important medical and social problems of our time. In most economically developed countries, up to 40% of deaths are from coronary heart disease (Oganov, R., Maslennikova, I., 2000). The heart of michaelene. A particularly high risk of mortality and development of heart failure with repeated myocardial infarction. Therefore, prevention of recurrent myocardial infarction is the most important task of the medicine. It is now established that the most effective drugs for the secondary prevention of CHD are beta-blockers (BAB) and disaggregants, in particular acetylsalicylic acid (aspirin) or ticlopidine (ticlid). Antiischemic and antiarrhythmic properties BAB serve as the basis for their long-term assignment with the preventive purpose in patients after myocardial infarction. There is a method of secondary prevention of coronary heart disease using beta-blockers. Aggregate data analysis of 17 controlled studies were conducted by S. Yusuf et al., 1985 (Yusuf, S., Peto R, Lewis j, Collins R, Sleight P. Beta blockade during and after myocardial infarction: an overwew of the randomised. //Prog. Cardiovasc. Dis. 1985, v. 27, p. 335-371) and Gottlieb S. S. et al., 1998 (S. S. Gottlieb, G., McCarter, R. J., Vogel R. A. Effect of beta-blockade on mortality among high-risk and low-risk patients after myocardial infarction. //New England Journal of Medicine, 1998, v. 339, 8, p. 489-496), where they showed that long-term therapy BAB patients after myocardial infarction, reduce the overall mortality of 22% of sudden deaths by 32% and the frequency of non-fatal re is RDA (Q-Abrazame heart attack). In all these studies used high doses of beta-blockers: propranolol daily dose of 180-240 mg, atenolol 100-200 mg etc. The disadvantage of this method is that such high doses give a rather high percentage of complications (from 16% to 42%), which limits the widespread use of beta-blockers in clinical practice. In addition, their effectiveness is still not more than 27%. There is ongoing research aimed at improving the efficiency of the BAB. In the last 10 years there has been active research on the efficiency of the inhibitors angiotenzinovymi enzyme (ACE) inhibitors at various cardiovascular diseases. However, most research focusing on the effectiveness of ACE inhibitors in hypertension and heart failure. There are few works that assess the effectiveness of ACE inhibitors in acute myocardial infarction (SAVE, 1992, AJRE, 1994) and single-evaluating their effectiveness in secondary prevention of coronary heart disease (CONSENSUS II, SOLVD, 1992). In all the above studies assessed mainly the effect of ACE inhibitors on mortality and prevention of heart failure. The world is April. In the research CONSENSUS II, 1992 (Swedberg K., Held p, Kjekshus J et al. Effects of the early administration of enalapril on mortality in patients with acute myocardial infarction. Result of the Cooperative New Scandinavian Enalapril Survival Study II. //New Engl. J. Med, 1992, v. 327, p. 678-684) and SOLVD, 1992 (Yusuf, S., Pepine C., C. Garces et al. Effect of enalapril on myocardial infarction and unstable angina in patients with low ejection fraction. //Lancet, 1992, v. 340, p. 1173-1178) enalapril was used in increasing the dosage from 2.5 to 20 mg 2 times a day. It was found that enalapril decreases the incidence of repeated heart attacks, episodes of unstable angina and reduces the need for carrying out operations of myocardial revascularization. It was proved that ACE inhibitors are particularly effective in patients with systolic dysfunction of the left ventricle is paced after myocardial infarction, ejection fraction 40% or less, and in patients with arterial hypertension. The disadvantages of this method is that in patients with preserved ejection fraction monotherapy with enalapril were ineffective. In patients without hypertension, the use of enalapril was limited by the frequency of complications and, in particular, arterial hypotension and tachycardia. This is due to the fact that this study used high doses of enalapril 10 to 20 mg 2 times in subfora ACE and beta-blocker is relatively rare and mainly in the treatment of hypertension. However, as stated at the meeting of the Moscow scientific society of General practitioners (November 1999), it can be a very useful combination (Cardiology, 2000, 6, S. 91-104). We have not found studies where would this combination was used for secondary prevention of CHD, especially without concomitant hypertension. The objective of the invention is to increase the effectiveness of secondary prevention of coronary heart disease and reduce complications after undergoing a primary krupnovesovogo myocardial infarction without concomitant arterial hypertension using joint application cardioselektivee beta-blocker atenolol and the ACE inhibitor of Enap in small doses. This object is achieved in that at 16-18 days from the onset of myocardial infarction patients without concomitant arterial hypertension was prescribed atenolol 12.5 mg in the morning and Enap 2.5 mg in the evening. On the 2nd week increased the dose of atenolol to 12.5 mg in the morning and in the evening, leaving the dose of Enap 2.5 mg in the evening. On the 3rd week atenolol continued to take 12.5 mg in the morning and evening and Enap 2.5 mg in the morning and evening. In the absence of hypotension on a 4-5 week increased the dose of atenolol to 25 mg in the morning and evening and EN is but momentary and long-acting nitrates in conventional dosages. The novelty of the method:1. The proposed method is based on the combined use of atenolol and Enap in patients undergoing primary krupnooptovyj (Q-wave) myocardial infarction with preserved ejection fraction (>45%). 2. This allows the use of both drugs in small doses, increasing the effectiveness of secondary prevention and reducing the number of side effects. 3. The simultaneous use of two drugs at low doses can reduce the number of side effects and, in particular, hypotonia and allows the use of this method of treatment in patients without concomitant arterial hypertension. The method consists in the following. Patients undergoing primary krupnooptovyj myocardial infarction, and in the absence of hypertension at 16-18 days of a heart attack is assigned to combination therapy cardioselektivee beta-blocker-atenolol and ACE inhibitor with enalapril (for example, Enap company KRKA, Slovenia). Treatment start with the minimum dose. Atenolol is administered in a dose of 12.5 mg in the morning, enalapril (Enap) 2.5 mg in the evening. If tolerated treatment and no side effects as hypotension next week dose atenolol prolonged considering the dose of enalapril 2.5 mg 2 times a day (morning and evening), dose atenolol remains 12.5 mg 2 times a day. In the absence of hypotension on a 4-5 week, increase the dose of atenolol to 25 mg 2 times a day - morning and evening dose of enalapril (2.5 mg 2 times a day). This therapy patients receive within 2 years, continuing to take from the first day of disease of heart attack the aspirin 125 mg once daily and, if necessary, prolonged nitrates in accepted dosages, such as kardiket 40 mg 2 times a day. Gradually increasing doses of the drugs helped to avoid the complications of therapy in the form of hypotension, which was observed only in 2,08% of patients. We conducted a study which assessed the efficacy of combination therapy with atenolol and amlodipine with monotherapy one atenolol. Materials and methods. The study included 66 men aged 42-60 years), who underwent primary krupnooptovyj myocardial infarction (myocardial infarction Q-wave). None of them had concomitant hypertension. Randomly patients were divided into 2 identical groups. Cm. table. 1. In the 1st group of 36 patients within 2 years were treated by the proposed method. At 16-18 days of myocardial infarction cured to the Slovenia) 2.5 mg once in the evening. With good endurance next week dose of atenolol was increased to 12.5 mg 2 times a day, the dose of Enap remained 2.5 mg once in the evening. After another week had increased the dose of Enap to 2.5 mg 2 times a day (morning and evening) dose atenolol remained 12.5 mg 2 times a day. In the 2nd control group of 30 patients within 2 years received cardioselektivee beta-blocker atenolol. 12-16 days of myocardial infarction to treatment with nitrates and acetylsalicylic acid were added to atenolol. Treatment was started with a dose of 12.5 mg once daily, with a gradual increase in the dose of 12.5 mg every 3 days, if tolerated. The average daily dose of atenolol in the group amounted to 66,93,4 mg, which was significantly more than in the 1st group, p<0,001. Results. Within 1 year in each group died, one patient that was 2,82,0% in the 1st and 3,32,2% in the 2nd, the difference unreliable. Re nonfatal myocardial infarction occurred in 1-St group 1 (2,8+2,0%) patient in the 2 nd - 3 (10,0+3.7 percent). the th nonfatal myocardial infarction occurred in 1-St group 1 (2,82,0%) patients, which is somewhat lower than in the 2 nd - 2 (6,6+3,1%), the difference unreliable. Thus, within 2 years of deaths observed in the 1-St group 2 (5,62,8%) patients in the 2-nd also 2 (6,73,1%). Re myocardial infarction within 2 years evolved into the 1st group 2 (5,62,8%) patients, which was significantly lower than in the 2 nd - 5 (16,74,5%), p<0,05. In the 2nd group for 2 years in one patient developed tromboliticaskie stroke, if there are none in the first. Summarizes adverse outcomes (death+re myocardial infarction+strokes) installed in the 1st group 4 (11,1+3,9%) patients, which was significantly lower than in the 2nd - 8 (26,7+5,4%), p<0,01 (t=2,4). Improvement in clinical status in the 1st group was noted in 30 (83,36,2%) patients, which was significantly higher than in the 2nd - 16 (53,06,1%), p<0,001 (t=3,5). Cm. table. 2. Complications of therapy reliably rarely observed in the group receiving combination therapy with atenolol and Enap than in the group receiving monotherapy with atenolol: the 1st group - 2 (5,62,8%), in the 2nd - 6 (20,0+8,1%) patients, respectively, p<0,01 (t=2,6). In the 1st group the main complication was hypotension, which disappeared after dose reduction of Enap. In the 2nd group, complications were the following: hypotension 2, marked sinus has reditribute cancel atenolol. The conclusions. Combination therapy with atenolol and enalapril patients undergoing krupnooptovyj myocardial infarction, without concomitant arterial hypertension can significantly reduce the number of adverse outcomes, especially repeated heart attacks and complications versus monotherapy atenololum in large doses. Example. Patient S. 54 years 26.10.97 underwent primary krupnooptovyj myocardial infarction in the Antero-septal region, the apex of the left ventricle. With 26.10 on 14.11.97 inpatient treatment in the cardiology Department of hospital 29. Before discharge from hospital the patient had a rare strokes with physical loads up to 2 times a week, stopping by the nitrosorbid. Physical activity 1.0 km/day. Tolerance to physical loads according to the VEM from 13.11.97 - 450 KGM. Termination criteria of ischemic samples. On ECHOCARDIOGRAPHY: CSR - 78,0 ml, CDALE - 146 ml, PE - 47%. The patient received treatment cardice-40 1 tab. 2 times a day and aspirin 250 mg once. The patient was discharged 14.11.97 to outpatient treatment in the cardiology clinic. In the cardiology clinic with 15.11.97 in treatment were added atenolol 12.5 mg in the morning and Enap 2.5 mg at night. Tolerability was good. Next week is 5 mg 2 times a day. 4 week outpatient treatment dose atenolol increased to 25 mg 2 times a day, Enap left in the dose of 2.5 mg 2 times a day. Tolerability of treatment remained good. HELL was within 110/80 to 120/80 mm RT. Art. The patient indicated the disappearance of angina, increased tolerance to physical loads up to 750 KGM, increasing physical activity (walks up to 4.5 km/day). On day 113 drawn to work in their profession mechanic. Within 2 years continued to take atenolol 25 mg 2 times a day, Enap 2.5 mg in the morning and in the evening, at night, aspirin 125 mg once. Angina and shortness of breath no. He walks without restrictions. The exercise tolerance after 1 year 900 KGM 2 years 750 KGM. Termination criteria sample neishemicescoy, in both cases, the fatigue. On ECHOCARDIOGRAPHY in 2 years CSR to 61.2 ml, CDALE - 189 ml, ejection fraction increased to 67.6%. Within 2 years tolerability remained good. 1. The way to prevent recurrent myocardial infarction in patients without hypertension, including therapy cardioselektivee beta-blocker, characterized in that it further prescribed ACE inhibitor, with treatment beginning at 16-18 days of myocardial infarction and spend 3 this is the ATA in the conventional dosage. 2. The method according to p. 1, characterized in that as cardioselektivee beta-blocker use atenolol. 3. The method according to p. 1, characterized in that as the ACE inhibitor use enalapril. 4. The method according to p. 1, characterized in that, in the absence of hypotension during the first week prescribed 12.5 mg atenolol in the morning and 2.5 mg of amlodipine in the evening, during the second week appoint 12.5 mg atenolol in the morning and evening and 2.5 mg of amlodipine in the evening during the third week atenolol 12.5 mg and amlodipine 2.5 mg in the morning and evening and continue treatment for two years atenolol 25 mg morning and evening, enalapril 2.5 mg in the morning and also evening. 5. The method according to p. 1, characterized in that, with the development of hypotension at any stage of treatment prescribed atenolol 12.5 and enalapril 2.5 mg for the duration of treatment.
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