Method for treating atrial fibrillations
FIELD: medicine, cardiology.
SUBSTANCE: along with injecting antiarrhythmic remedy one should introduce varfarin at the dosage of 1-5 mg for 6-8 d followed by a maintenance course in 1-1.5 mo at the dosage of 2-3 mg for 6-7 d and in 2-3 mo at the dosage of 1-2 mg for 5-7 d.
EFFECT: higher efficiency of therapy.
The invention relates to medicine and can be used in the treatment of atrial fibrillation.
There is a method of treatment of atrial fibrillation by application of cyclic urethanes, taken as the analog of (1).
There is a method of treatment of atrial fibrillation, which has been in use for treatment of drugs: dofetilide, flecainide, amiodarone and other drugs - prototype (2).
However, the use of these drugs, including amiodarone, leads to fibrosis of the lung, paroxysmal ventricular tachycardia, thyroid gland, increasing the level of liver enzymes.
The aim of the invention is to increase efficiency of treatment by reducing side effects of drug therapy.
The technical result is achieved by the fact that in addition to drugs antiarrhythmic actions impose drug warfarin at a dose of 1.0-5.0 mg for 6-8 days followed through 1-1,5 months. supporting course of warfarin at a dose of 2-3 mg for 6-7 days, with subsequent 2-3 month course of warfarin at a dose of 1-2 mg for 5-7 days.
The introduction of the drug warfarin is carried out in doses below therapeutic that reduces symptoms side effects of the drug. On the other hand, the combination of drugs antiarrhythmic actions and warfarin can reduce the RAM drugs antiarrhythmic actions for example quinidine (amiodarone), 1.2 times, and consequently, reduce the appearance pomocnych actions used antiarrhythmic therapy.
The method is as follows.
At admission the patient find out the presence of organic heart disease, particularly involving high electrical activity in the left atrium (stenosis and insufficiency of the mitral valve rheumatic syndrome sick sinus, thyrotoxicosis. Possible idiopathic variants of atrial fibrillation with no evidence of organic heart failure.
Auscultation of suspected atrial fibrillation can be irregular and of different intensity heart rate (delirium cordis). A characteristic symptom is the “pulse deficit” compared with the heart rate.
Electrocardiographically symptoms of atrial fibrillation are:
wave atrial (f) of varying amplitude, morphology and duration without atrial wave P;
irregular ventricular rhythm;
the QRS complexes of normal or aberrant.
The number of contractions of the Atria ranges from 400-700 per min and submitted, f-waves, which are most salient in the right precardiac leads (V 1-V 2), and II, III, aVF-leads. The amplitude of the f-waves can be relatively large (largest is the wave flicker, f-wave greater than 3 mm) and small (melbournejoe flicker). And krupnovesovoe flicker correlates with increased atrium (for example, in congenital heart defects), melbournejoe, prognostically less favorable associated with cardio. Patients perceive frequent abnormal rhythm in atrial fibrillation as painful palpitations or a feeling of discomfort in the chest. Hemodynamic consequences of atrial fibrillation can manifest as weakness, dizziness and shortness of breath.
In atrial fibrillation with a high frequency of contractions observed deeper parabolicheskoi braking (blockage) in the AV connection, in accordance with this, the rhythm of the ventricles will be more rare (less than 60 min) - a bradycardia form flicker. On the contrary, when the low-frequency form of atrial fibrillation atrioventricular connection skips a large number of pulses, resulting develops theoreticheskaya form (more than 100 ventricular contractions per minute), which is often accompanied by signs of refractory heart failure. An intermediate position is epistolica form. In addition, isolated paroxysmal (rare) and permanent (lasting longer than 2 weeks) forms of atrial fibrillation.
For relief of atrial fibrillation in enaut drugs components cardioversion, class 1A, 1C, class II and class III and warfarin at a dose of 1.0-5.0 mg for 6-8 days followed through 1-1,5 months supporting a course of warfarin at a dose of 2-3 mg for 6-7 days, with subsequent 2-3 month course of warfarin at a dose of 1-2 mg for 5-7 days.
Way of the following examples.
Patient K., 43 years old, when receiving complains of palpitations, discomfort in the chest, weakness, dizziness. History of the patient revealed the presence of rheumatic stenosis and insufficiency of the mitral valve.
Auscultation marked irregular and different intensity of heart contractions. A characteristic symptom is the “pulse deficit” compared with the heart rate.
Electrocardiographically there are waves of atrial different amplitude and duration without atrial wave R. the Frequency of contractions of the Atria is 560-700 min and presents f-waves, which are more pronounced in leads V 1-V 2. The amplitude of the f-waves are relatively large, f-wave greater than 3 mm
The patient is prescribed antiarrhythmic drugs of class 1A (procainamide), 1C and class II (β-blockers), and optionally the drug warfarin. With warfarin, used according to the following scheme:
5.0 mg for 8 days, followed by 1 month support ku is com warfarin at a dose of 3 mg for 7 days followed by a 2 month course of warfarin at a dose of 2 mg for 7 days.
As a result of the treatment of atrial fibrillation cropped, which is confirmed by electrocardiographically. Complaints of palpitations, discomfort in the chest does not show. The applied dose of warfarin is 75% of therapeutic, which allowed the number of complications during warfarin treatment. On the other hand, the applied dose arrhythmic funds were also lower than usually prescribed (by 30-40%)that Pospolita to reduce the number of complications arising from the treatment antiaritmikami. Discharged in a state of clinical remission.
Patient S., 37 years old, was admitted with complaints of discomfort in the chest, weakness and shortness of breath. From the anamnesis it is known that the patient is suffering from myocarditis. During the examination the patient looks pale; heart size increased; blood pressure is reduced, and the pulse Ochsen.
Auscultation also noted the presence of irregular intensity heart rate, characteristic of atrial fibrillation. Marked “pulse deficit” compared with the heart rate.
Electrocardiographically identified: the absence of atrial, and P wave and wave-atrial (f) of varying amplitude, morphology and duration, most pronounced in II, III and aVF-leads. The number is krasheny fibrillation varies between 400-550 in minutes
Patient prescribed drugs class 1A (quinidine), as well as voltaren and warfarin. And warfarin take on the following diagram:
at a dose of 1.0 mg for 6 days, followed in 1.5 months. supporting course of warfarin at a dose of 2 mg for 6 days, followed after 3 month course of warfarin at a dose of 1 mg for 5 days.
As a result of the treatment of atrial fibrillation cropped, which is confirmed by electrocardiographically. Complaints of discomfort in the chest, weakness does not show. The use of complex therapy with antiarrhythmic drugs number and warfarin reduced dose as antiaritmikov, and warfarin, which allowed to reduce the dose and the number of oslojenni medicamentous therapy. Discharged in a state of clinical remission.
Patient 3., 56 years old, when he complained about painful palpitations, dizziness and shortness of breath. History of the signs of organic disease of the heart is not marked.
Auscultation is an irregular and different intensity of heart contractions delirium cordis).
Electrocardiographically there are waves of atrial varying amplitude, irregular ventricular rhythm. The number of contractions of the Atria ranges 560-640 min and presents f-waves, which are more pronounced in the right precardiac otede is s (V 1-V 2), and the amplitude of f-waves is relatively small (melbournejoe flicker).
The patient is prescribed the drug amiodarone and warfarin. And warfarin take the following scheme: at a dose of 3.0 mg for 7 days, followed after 5 weeks of maintenance rate of warfarin at a dose of 2.5 mg for 6 days, followed after 2.5 month course of warfarin at a dose of 1.5 mg for 6 days.
The result of the treatment is reduction of atrial fibrillation. Complaints of palpitations, dizziness and shortness of breath does not show. Discharged in a state of clinical remission.
The treatment according to the claimed method 31 of the patient. The mentioned combination of warfarin and antiarrhythmic drugs with the stated combination of low doses ensures the achievement of the technical result in the exclusion of the manifestations of the side effects of the applied drug therapy. Follow-up monitoring within 6-12 months. found no recurrence of atrial fibrillation in all the examined patients.
Sources of information
1. RF patent №2125568.
2. J. Am. Coll. Cardiol. 2001; 38:1266.
A method of treating atrial fibrillation by introducing antiarrhythmic drugs, characterized in that it further impose warfarin at a dose of 1.0-5.0 mg for 6-8 days followed through 1-1,5 months. supporting course of warfarin at a dose of 2-3 mg in those who tell 6-7 days with the next 2-3 months. the rate of warfarin at a dose of 1-2 mg for 5-7 days.
FIELD: pharmaceutical chemistry, medicine.
SUBSTANCE: invention relates to new compounds of formula I ,
solvates or pharmaceutically acceptable salts having antiarrhythmic activity, including ventrical fibrillation, as well as pharmaceutical compositions containing the same. Compounds of present invention are useful in treatment or prevention of arrhythmia, modulation of ion channel activity, for topic or local anesthesia, etc. In formula I X is direct bond, -C(R6,R14)-Y- and C(R13)=CH-; Y is direct bond, O, S, and C1-C4-alkylene; R13 is hydrogen, C1-C6-alkyl, C3-C8-cycloalkyl, unsubstituted aryl or benzyl; R1 and R2 are independently C3-C8-alkoxyalkyl, C1-C8-hydroxyalkyl and C7-C12-aralkyl; or R1 and R2 together with nitrogen atom directly attached thereto form ring of formula II ,
wherein said ring is formed by nitrogen and 3-9 ring atoms selected independently from carbon, sulfur, nitrogen and oxygen, etc; R3 and R4 are independently attached to cyclohexane ring in 3-, 4-, 5-, or 6-position and represent independently hydrogen, hydroxyl, C1-C6-alkyl and C1-C6-alkoxy; and when R3 and R4 are bound with the same atom of cyclohexane ring they may form together 5- or 6-membered spiroheterocycle ring containing one or two heteroatoms selected from oxygen and sulfur; A is C5-C12-alkyl, C3-C13-carbocyclic ring, or ring structure as defined herein.
EFFECT: new antiarrhythmic drugs.
30 cl, 12 dwg, 34 ex
FIELD: organic chemistry, pharmacology.
SUBSTANCE: invention relates to compounds of formula I ,
where R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30), and R(31) are disclosed in claims. Compound of present invention are particularly useful as new antiarrythmia bioactive substances, in particular for treatment and prophylaxis of atrial arrhythmia (e.g., atrial fibrillation or auricular flutter).
EFFECT: higher efficiency.
13 cl, 18 ex, 1 tbl
FIELD: organic chemistry, heterocyclic compounds, purines, medicine.
SUBSTANCE: invention relates to a method for treatment of arrhythmia in mammal. Method involves administration of agonist of adenosine A1-receptors in the therapeutically effective minimal dose of the formula:
wherein R1 represents optionally substituted heterocyclic group. The indicated dose of agonist is in the range from 0.0003 to 0.009 mg/kg. Method shows the enhanced effectiveness and doesn't result to undesirable adverse effects.
EFFECT: improved treatment method, valuable medicinal properties of substances.
11 cl, 1 dwg, 2 ex
FIELD: organic chemistry, chemical technology, medicine.
SUBSTANCE: invention relates to synthesis of new biologically active substance, namely, to γ-hydroxypropylammonium-5-hydroxynicotinate of the formula (I): , eliciting an anti-ischemic, anti-arrhythmic and hypolipidemic activity. This compound shows low toxicity and absence of cardiodepressive effect. Compound of the formula (I) is prepared by interaction of 5-hydroxynicotinic acid with 3-amino-1-propanol in the presence of a solvent at heating.
EFFECT: valuable medicinal properties of compound.
1 cl, 7 tbl, 3 ex
where R and R1have the meanings indicated in the claims
FIELD: pharmaceutical industry and technology, pharmacy.
SUBSTANCE: invention relates to the improved method for preparing dihydroquercitin. Invention involves preliminary separation of volatile nonpolar compounds with steam at rapid change of pressure from 0.1 to 0.3 MPa in reactor carried out before extraction stage and with reduced time of raw extraction being without milling wood under conditions of mild mechanical-chemical effect and without destruction of wood occurring in rapid change of pressure from 0.1 to 0.5 MPa using mixture of polar solvent with water or their mixtures as an extractant. Invention reduces extraction time in intensifying and optimization of the process of dihydroquercitin that provides reducing total time of process from 60-75 min to 7-9 min and to simplify technology in carrying out the process without milling wood.
EFFECT: improved method for preparing.
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to an antiviral medicinal preparation. The preparation comprises ribavirin, phosphatidylcholine, cholesterol, α-tocopherol, sucrose, sodium chloride and represents lyophylizate in isotonic solution. Invention provides preparing the liposomal ribavirin eliciting high biological and therapeutic effectiveness with low toxicity.
EFFECT: improved, enhanced and valuable medicinal properties of preparation.
3 cl, 2 tbl
FIELD: medicine, radiation therapy.
SUBSTANCE: it is suggested to apply mixture prepared ex tempore out of: 5 mg hyoxison ointment, 1 ml 10% alpha-tocopherol acetate and 100 mcg superlymph-1 dissolved in 1 ml sterile distilled water. The suggested mixture should be applied twice daily onto affected part with thin layer to accelerate regeneration of affected tissue.
EFFECT: higher efficiency of therapy.
FIELD: pharmaceutical industry, in particular new bioactive chalcones.
SUBSTANCE: invention relates to new chalcones of formula I
, pharmaceutically acceptable salts or solvates thereof, wherein Ar is optionally substituted C5-C10-carbocycle group or 5- or 6-membered heterocycle group having sulfur atom in cycle, and Ar substituents are selected independently from Cl, Br, F, CN, SCH3 and OR10, wherein R10 is linear or branched C1-C6-hydrocarbon; R is OH or R10; R2 and R3 are independently phenyl, saturated linear or branched C1-C6-hydrocarbon, or R2 and R3 together with carbon atom attached thereto form 5- or 6-membered carbocycle group with the proviso, that in compounds where R is OH and both R2 and R3 are methyl, Ar is not phenyl, 4-chlorophenyl, 4-chlorophenyl, 4-methylphenyl, 2-chlorophenyl, 3,4-dimethoxyphenyl, or 4-methoxyphenyl. Also disclosed are drug component for treatment or prophylaxis of neoplasm and pharmaceutical compositions with antiproliferation effect based on compounds of formula I.
EFFECT: new chalcone derivatives with value bioactive action.
26 cl, 2 tbl, 22 ex
FIELD: veterinary science.
SUBSTANCE: about 20-25 d before calving one should introduce intramuscularly 0.5%-sodium selenite solution for cows at the dosage of 10 ml. Twice before and twice after calving at 10-d-long interval - tetravit at the dosage of 10 ml at the content of 50000 IU vitamin A, 25000 IU vitamin D, 20 mg vitamin E and 5 mg vitamin F per 1 ml. Succinic acid should be introduced 20-25 d both before and after calving at the dosage of 1.0 g. The method provides efficient correction of the main values of homeostasis in cows after calving.
EFFECT: higher efficiency of normalization.
2 ex, 4 tbl
FIELD: organic chemistry, pharmacology.
SUBSTANCE: invention relates to new flavone, xanthone and coumarone derivatives of formula I
[R and R1 each are independently lower C1-C6-alkyl or together with nitrogen atom attached thereto form 4-8-membered heterocycle, optionally containing one or more heteroatoms, selected from group comprising N or O, wherein said heterocycle is optionally substituted with benzyl; Z has formula (A) , wherein R3 and R4 each are independently hydrogen, optionally substituted aromatic group containing in cyclic structure from 5 to 10 carbon atoms, wherein substituents are the same or different and represent lower C1-C4-alkyl, OR10 (OR10 is hydrogen, saturated or unsaturated lower C1-C6-alkyl or formula ) or linear or branched C1-C6-hydrocarbon; or R2 and R3 together with carbon atom attached thereto form 5-6-membered carbocycle; and R4 represents hydrogen or attaching site of group –OCH2-C≡CCH2NRR1; or formula (B) , wherein R5 is hydrogen, linear or branched lower C1-C6-hydrocarbon, with the proviso, that when Z represents R and R1 both are not methyl or R and R1 together with nitrogen atom attached thereto cannot form groups , or ]. Also disclosed are drug component with proliferative activity for prophylaxis or treatment of neoplasm and pharmaceutical composition with proliferative activity based on the same. Derivatives of present invention have antyproliferative properties and are useful as modulators of drug resistance in cancer chemotherapy; as well as in pharmaceuticals for prophylaxis or treatment of neoplasm, climacteric disorders or osteoporosis.
EFFECT: new compounds with value bioactive effect.
31 cl, 2 tbl, 32 ex
FIELD: pharmaceutical chemistry.
SUBSTANCE: invention relates to treatment of patients suffering from diseases associated with pathologic activity of matrix proteases. Treatment involves administration of compounds depicted by general formula (I).
EFFECT: increased treatment efficiency.
136 cl, 448 ex
SUBSTANCE: the present innovation deals with phospholipid complexes of proanthocyanidine A2 and pharmaceutical compositions upon their basis as antiatherosclerotic agents, those for preventing and treating myocardial and cerebral infarction. Phospholipids of the above-mentioned complex should be preferably chosen out of lecithins, phosphatidyl choline, phosphatidyl ethanolamine, phosphatidyl serine. The innovation provides the preparation to treat the above-mentioned diseases due to decreasing the quantity and burden of atheromatous plaque, decreased obstruction of carotid arteries and decreased thickness of vascular walls.
EFFECT: higher efficiency of prophylaxis and therapy.
9 cl, 11 dwg, 6 ex, 2 tbl
FIELD: organic chemistry, medicine, pharmacology.
SUBSTANCE: invention relates to new derivatives of carbamic acid esters of the general formula (I):
and their pharmaceutically acceptable salts eliciting activity with respect to metabotropic glutamate receptors mGlu of group I that can be used for treatment of acute and/or chronic neurological disorders. In the general formula (I) R1 means hydrogen atom or (C1-C7)-alkyl; R2 and R2' mean independently of one another hydrogen atom, (C1-C7)-alkyl, (C1-C7)-alkoxy-group, halogen atom or trifluoromethyl; X means oxygen (O), sulfur (S) atom or two hydrogen atoms not forming a bridge; A1/A2 mean independently of one another phenyl or 6-membered heterocycle comprising 1 or 2 nitrogen atom; B represents group of the formula:
wherein R3 means (C1-C7)-alkyl and others; Y means -O-, -S- or a bond; Z means -O- or -S-; or B means 5-membered heterocyclic group of formulae: (a) , (b) , (c) or (d) . Also, invention relates to methods for preparing compounds and to a medicinal agent based on thereof.
EFFECT: improved preparing methods, valuable medicinal properties of compounds.
22 cl, 1 tbl, 2 sch, 78 ex
FIELD: organic chemistry, medicine.
SUBSTANCE: invention relates to new compounds of coumarone class, namely, to 6-nitro-2-iminocoumarin 3-carboxylic acid 4-toluidide silver salt of the formula (1): that elicits an antibacterial effect and can be used in medicine. Invention provides preparing a new compound eliciting an antibacterial effect with respect to S. aureus, E. coli, and C. albicans with mononuclear cells values 0.25; 0.5 and 7.8 mcg/ml, respectively, and with acute toxicity value LD50 for these compounds 2 460 ± 230 mg/kg.
EFFECT: valuable properties of compound.
1 cl, 1 tbl, 2 ex
FIELD: organic synthesis.
SUBSTANCE: invention provides compounds of general formula I:
, where R1 represents -CO-Ra, -SO2-Rb, or aryl optionally substituted by lower alkoxy, wherein Ra represents cycloalkyl, cycloalkyl(lower)alkyl, cycloalkyloxy, aryl, aryloxy, aryl(lower)alkyl, aryl(lower)alkoxy, aryloxy(lower)alkyl, aryl-S-(lower)alkyl, aryl(lower)alkenyl, provided that aryl group can be optionally substituted by halogen, lower alkyl, hydroxy, nitro, cyano, lower alkoxy, phenyl, CF3, cyano(lower)alkyl, lower alkyl-C(O)NH, lower alkyl-CO, and lower alkyl-S; heteroaryl, heteroaryl(lower)alkyl, or heteroaryl(lower)alkoxy, provided that heteroaryl group is 5- or 6-membered ring or bicyclic aromatic group constituted by two 5- or 6-membered rings including 1-3 heteroatoms selected from oxygen, nitrogen, and sulfur and that heteroaryl group can be optionally substituted by lower alkoxy; Rb represents aryl, aryl(lower)alkyl, or heteroaryl, aryl group optionally substituted by halogen, cyano, or lower alkyl-C(O)NH; R2 and R3 represent hydrogen atoms; R4 representshydrogen or lower alkyl; R5 represents hydrogen, lower alkyl, cycloalkyl, benzodioxyl, or aryl optionally substituted by lower alkyl, halogen, lower alkoxy, hydroxy, or (lower)alkyl-C(O)O; n is 1 or 2; and pharmaceutically acceptable salts thereof and/or pharmaceutically acceptable esters thereof. Invention also provides a pharmaceutical composition exhibiting inhibitory activity with regard to cysteine proteases of the cathepsin family, which composition comprises compound of formula I, pharmaceutically acceptable recipient, and/or adjuvant.
EFFECT: increased choice of cysteine protease inhibitors.
34 cl, 1 tbl, 13 ex