RU2051671C1 - Substance showing antiarrhythmic action - Google Patents
Substance showing antiarrhythmic action Download PDFInfo
- Publication number
- RU2051671C1 RU2051671C1 SU3384340A RU2051671C1 RU 2051671 C1 RU2051671 C1 RU 2051671C1 SU 3384340 A SU3384340 A SU 3384340A RU 2051671 C1 RU2051671 C1 RU 2051671C1
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- RU
- Russia
- Prior art keywords
- antiarrhythmic action
- substance showing
- antiarrhythmic
- substance
- treatment
- Prior art date
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- 230000003288 anthiarrhythmic effect Effects 0.000 title claims abstract description 6
- 239000000126 substance Substances 0.000 title claims abstract 3
- 230000000694 effects Effects 0.000 abstract description 2
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000001228 spectrum Methods 0.000 abstract 1
- 206010003119 arrhythmia Diseases 0.000 description 6
- 239000003814 drug Substances 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 239000001961 anticonvulsive agent Substances 0.000 description 4
- CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 description 3
- 230000001773 anti-convulsant effect Effects 0.000 description 3
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 description 3
- CTNPHHZPAJYPFO-PDXBGNJTSA-N (3s,5s,8r,9s,10s,13r,14s,17r)-3-[(2r,4s,5r,6r)-5-[(2r,3s,4s,5r,6s)-3,4-dihydroxy-6-(hydroxymethyl)-5-[(2s,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5,14-dihydroxy-13-methyl-17-(5-oxo-2h-furan Chemical compound C1([C@@H]2[C@@]3(C)CC[C@@H]4[C@@]5(C=O)CC[C@@H](C[C@@]5(O)CC[C@H]4[C@@]3(O)CC2)O[C@H]2C[C@@H]([C@@H]([C@@H](C)O2)O[C@@H]2[C@H]([C@H](O)[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O3)O)[C@H](CO)O2)O)OC)=CC(=O)OC1 CTNPHHZPAJYPFO-PDXBGNJTSA-N 0.000 description 2
- XFSBVAOIAHNAPC-XTHSEXKGSA-N 16-Ethyl-1alpha,6alpha,19beta-trimethoxy-4-(methoxymethyl)-aconitane-3alpha,8,10alpha,11,18alpha-pentol, 8-acetate 10-benzoate Chemical compound O([C@H]1[C@]2(O)C[C@H]3[C@@]45C6[C@@H]([C@@]([C@H]31)(OC(C)=O)[C@@H](O)[C@@H]2OC)[C@H](OC)[C@@H]4[C@]([C@@H](C[C@@H]5OC)O)(COC)CN6CC)C(=O)C1=CC=CC=C1 XFSBVAOIAHNAPC-XTHSEXKGSA-N 0.000 description 2
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 2
- XFSBVAOIAHNAPC-UHFFFAOYSA-N Aconitin Natural products CCN1CC(C(CC2OC)O)(COC)C3C(OC)C(C(C45)(OC(C)=O)C(O)C6OC)C1C32C4CC6(O)C5OC(=O)C1=CC=CC=C1 XFSBVAOIAHNAPC-UHFFFAOYSA-N 0.000 description 2
- FHIREUBIEIPPMC-UHFFFAOYSA-N K-Strophanthin-beta Natural products O1C(C)C(OC2C(C(O)C(O)C(CO)O2)O)C(OC)CC1OC(CC1(O)CCC2C3(O)CC4)CCC1(C=O)C2CCC3(C)C4C1=CC(=O)OC1 FHIREUBIEIPPMC-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 229940039750 aconitine Drugs 0.000 description 2
- STDXGNLCJACLFY-UHFFFAOYSA-N aconitine Natural products CCN1CC2(COC)C(O)CC(O)C34C5CC6(O)C(OC)C(O)C(OC(=O)C)(C5C6OC(=O)c7ccccc7)C(C(OC)C23)C14 STDXGNLCJACLFY-UHFFFAOYSA-N 0.000 description 2
- 239000003416 antiarrhythmic agent Substances 0.000 description 2
- 229960003965 antiepileptics Drugs 0.000 description 2
- 230000006793 arrhythmia Effects 0.000 description 2
- JBSMSVZHETUQQA-UHFFFAOYSA-N 5,5-diphenylimidazolidine-2,4-dione;sodium Chemical compound [Na].N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 JBSMSVZHETUQQA-UHFFFAOYSA-N 0.000 description 1
- 206010003591 Ataxia Diseases 0.000 description 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 1
- XPFRXWCVYUEORT-UHFFFAOYSA-N Phenacemide Chemical compound NC(=O)NC(=O)CC1=CC=CC=C1 XPFRXWCVYUEORT-UHFFFAOYSA-N 0.000 description 1
- 229940125681 anticonvulsant agent Drugs 0.000 description 1
- 229910001628 calcium chloride Inorganic materials 0.000 description 1
- 239000001110 calcium chloride Substances 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- 208000007565 gingivitis Diseases 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229960003396 phenacemide Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Изобретение относится к клинической фармакологии и касается средств лечения аритмий сердца различного генеза. The invention relates to clinical pharmacology and relates to the treatment of cardiac arrhythmias of various origins.
Известны лекарственные средства для лечения аритмий сердца, например, хинидин-(6-метоксихинолил-3-(4)(-)(5-винилхину- клидил-(2)(-карбинол; новокаинамид-β-диэтил-аминоэтиламида парааминобензойной кислоты гидрохлорид; этмозин-2-карбэтокси-амино-10-(3-морфолил-пропионил)-фе- нотиазина гидрохлорид. Known drugs for the treatment of cardiac arrhythmias, for example, quinidine- (6-methoxyquinolyl-3- (4) (-) (5-vinylquin-clidyl- (2) (-carbinol; novocainamide-β-diethylaminoethylamide para-aminobenzoic acid hydrochloride; ethmosin-2-carbethoxy-amino-10- (3-morpholyl-propionyl) phenothiazine hydrochloride.
Из противосудорожных средств антиаритмическими свойствами обладает дифенин (5,5-дифенил-гидантоин-натрий) и финлепсин (5-карбамоил-5Н-дибензо(b, f)-азепин) (Биггер, Бассет, Гоффман, 1967; Liberson et al. 1967; Kaufman, Hauser, 1968; Козлова Н.П. 1970; Мотовилов П.Е. 1972; Pinto et al. 1976; Singh, Hauswirth, 1979). Однако вследствие побочных эффектов (головокружение, атаксия, гингивит и пр.) длительное применение дифенина и финлепсина для лечения больных с нарушениями сердечного ритма нежелательно. У линейных производных мочевины (фенурон, крампол, детурид), обладающих противосудорожным действием, антиаритмические свойства не описаны. Of anticonvulsants, diphenin (5,5-diphenylhydantoin sodium) and finlepsin (5-carbamoyl-5H-dibenzo (b, f) -azepine) have antiarrhythmic properties (Bigger, Bassett, Goffman, 1967; Liberson et al. 1967 ; Kaufman, Hauser, 1968; Kozlova, N.P. 1970; Motovilov, P.E. 1972; Pinto et al. 1976; Singh, Hauswirth, 1979). However, due to side effects (dizziness, ataxia, gingivitis, etc.), prolonged use of diphenin and finlepsin for the treatment of patients with cardiac arrhythmias is undesirable. In linear derivatives of urea (phenuron, krampol, deturid), which have an anticonvulsant effect, antiarrhythmic properties are not described.
Целью настоящего изобретения является расширение арсенала лекарственных средств для лечения аритмий сердца различного генеза. The aim of the present invention is to expand the arsenal of drugs for the treatment of cardiac arrhythmias of various origins.
Поставленная цель достигается применением оригинального противосудорожного средства галодифа по новому назначению в качестве антиаритмического средства. The goal is achieved by the use of the original anticonvulsant halodif for a new purpose as an antiarrhythmic agent.
Предложение использовать новый противосудорожный препарат галодиф в качестве антиаритмического средства стало возможным благодаря обнаруженным авторами новым свойствам этого препарата. The proposal to use the new anticonvulsant drug galodif as an antiarrhythmic agent was made possible thanks to the new properties of this drug discovered by the authors.
Галодиф-мета-хлор-бензгидрилмочеви- на, в эксперименте на животных показал выраженную антиаритмическую активность при нарушениях деятельности сердца, вызванных хлоридом кальция, аконитином и строфантином. Препарат значительно повышает выживаемость животных, укорачивает и облегчает характер течения аритмий (см. таблицу). Наиболее активен галодиф при строфантиновой и аконитиновой аритмиях, при которых он по величине ЭД50 и широте терапевтического действия, значительно превосходит эталонный препарат дифенин.Halodif-meta-chloro-benzhydrylurea, in an animal experiment showed pronounced antiarrhythmic activity in cases of cardiac impairment caused by calcium chloride, aconitine, and strophanthin. The drug significantly increases the survival of animals, shortens and facilitates the nature of the course of arrhythmias (see table). The most active halodif with strophanthin and aconitine arrhythmias, in which it is in magnitude of ED 50 and the breadth of the therapeutic effect, significantly exceeds the reference drug diphenin.
Предлагаемое по новому назначению соединение галодиф, по решению фармакологического комитета МЗ СССР проходит клиническое испытание в качестве противосудорожного средства для лечения эпилепсии (протокол 2 от 13 января 1978 года). The galodif compound proposed for a new purpose, by decision of the pharmacological committee of the Ministry of Health of the USSR, is undergoing a clinical trial as an anticonvulsant for the treatment of epilepsy (
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SU3384340 RU2051671C1 (en) | 1981-12-16 | 1981-12-16 | Substance showing antiarrhythmic action |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SU3384340 RU2051671C1 (en) | 1981-12-16 | 1981-12-16 | Substance showing antiarrhythmic action |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2051671C1 true RU2051671C1 (en) | 1996-01-10 |
Family
ID=20993216
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SU3384340 RU2051671C1 (en) | 1981-12-16 | 1981-12-16 | Substance showing antiarrhythmic action |
Country Status (1)
| Country | Link |
|---|---|
| RU (1) | RU2051671C1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2155034C1 (en) * | 1999-11-29 | 2000-08-27 | Научно-исследовательский институт психического здоровья Томского научного центра СО РАМН | Agent decreasing alcoholic motivation |
| RU2283099C1 (en) * | 2005-04-14 | 2006-09-10 | Владимир Никитович Ярыгин | Method for prophylaxis of cardiac activity rhythm disorder |
| US20160244404A1 (en) * | 2013-07-18 | 2016-08-25 | Obschestvo S Ogranichennoy Otvetstvennostiyu "Sintegal" | Optical isomers of (+) and (-)-benzhydryl ureas and (+) and (-)-1-[(3-chlorophenyl)-phenyl-methyl] urea, a pharmaceutical composition based thereon and a method for producing said optical isomers |
-
1981
- 1981-12-16 RU SU3384340 patent/RU2051671C1/en active
Non-Patent Citations (1)
| Title |
|---|
| 1. Тареев Е.М. Коллагеновые болезни и ревматизм, 1962, с.19. 2. Авторское свидетельство СССР N 510890, кл. C 07C127/00, 1974. * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2155034C1 (en) * | 1999-11-29 | 2000-08-27 | Научно-исследовательский институт психического здоровья Томского научного центра СО РАМН | Agent decreasing alcoholic motivation |
| RU2283099C1 (en) * | 2005-04-14 | 2006-09-10 | Владимир Никитович Ярыгин | Method for prophylaxis of cardiac activity rhythm disorder |
| US20160244404A1 (en) * | 2013-07-18 | 2016-08-25 | Obschestvo S Ogranichennoy Otvetstvennostiyu "Sintegal" | Optical isomers of (+) and (-)-benzhydryl ureas and (+) and (-)-1-[(3-chlorophenyl)-phenyl-methyl] urea, a pharmaceutical composition based thereon and a method for producing said optical isomers |
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