DE2821778A1 - Prophylactic antidotes to organo-phosphorus poisoning - contain hyoscine butyl bromate, a propanol chlor:hydrate, di:methyl-carbamoxy-phenyl-tri:methyl ammonium bromate and ephedrine - Google Patents
Prophylactic antidotes to organo-phosphorus poisoning - contain hyoscine butyl bromate, a propanol chlor:hydrate, di:methyl-carbamoxy-phenyl-tri:methyl ammonium bromate and ephedrineInfo
- Publication number
- DE2821778A1 DE2821778A1 DE19782821778 DE2821778A DE2821778A1 DE 2821778 A1 DE2821778 A1 DE 2821778A1 DE 19782821778 DE19782821778 DE 19782821778 DE 2821778 A DE2821778 A DE 2821778A DE 2821778 A1 DE2821778 A1 DE 2821778A1
- Authority
- DE
- Germany
- Prior art keywords
- bromate
- methyl
- ephedrine
- phenyl
- prophylactic
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000000729 antidote Substances 0.000 title claims description 7
- SXDBWCPKPHAZSM-UHFFFAOYSA-M bromate Inorganic materials [O-]Br(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-M 0.000 title claims description 3
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 title abstract description 6
- 230000000069 prophylactic effect Effects 0.000 title abstract description 6
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 title abstract description 3
- 229960002179 ephedrine Drugs 0.000 title abstract description 3
- RHSFBTRXGVQTDB-UHFFFAOYSA-N C(CC)O.[Cl] Chemical compound C(CC)O.[Cl] RHSFBTRXGVQTDB-UHFFFAOYSA-N 0.000 title 1
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 title 1
- BAVYZALUXZFZLV-UHFFFAOYSA-O Methylammonium ion Chemical compound [NH3+]C BAVYZALUXZFZLV-UHFFFAOYSA-O 0.000 title 1
- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 title 1
- 208000007964 Organophosphate Poisoning Diseases 0.000 title 1
- 229940075522 antidotes Drugs 0.000 title 1
- JSIHECHJIZCUQI-UHFFFAOYSA-N butyl bromate Chemical compound CCCCOBr(=O)=O JSIHECHJIZCUQI-UHFFFAOYSA-N 0.000 title 1
- STECJAGHUSJQJN-FWXGHANASA-N scopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-FWXGHANASA-N 0.000 title 1
- 229960002646 scopolamine Drugs 0.000 title 1
- 239000000575 pesticide Substances 0.000 claims description 8
- BDERNNFJNOPAEC-UHFFFAOYSA-N 1-propanol Substances CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 2
- SXDBWCPKPHAZSM-UHFFFAOYSA-N bromic acid Chemical compound OBr(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-N 0.000 claims description 2
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 8
- 102000003914 Cholinesterases Human genes 0.000 abstract description 3
- 108090000322 Cholinesterases Proteins 0.000 abstract description 3
- 229940048961 cholinesterase Drugs 0.000 abstract description 3
- 239000003795 chemical substances by application Substances 0.000 abstract description 2
- BALXUFOVQVENIU-GNAZCLTHSA-N Ephedrine hydrochloride Chemical compound Cl.CN[C@@H](C)[C@H](O)C1=CC=CC=C1 BALXUFOVQVENIU-GNAZCLTHSA-N 0.000 abstract 2
- HWHLPVGTWGOCJO-UHFFFAOYSA-N Trihexyphenidyl Chemical compound C1CCCCC1C(C=1C=CC=CC=1)(O)CCN1CCCCC1 HWHLPVGTWGOCJO-UHFFFAOYSA-N 0.000 abstract 2
- HOZOZZFCZRXYEK-GSWUYBTGSA-M butylscopolamine bromide Chemical compound [Br-].C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)CCCC)=CC=CC=C1 HOZOZZFCZRXYEK-GSWUYBTGSA-M 0.000 abstract 2
- 229960002534 ephedrine hydrochloride Drugs 0.000 abstract 2
- 229960001499 neostigmine bromide Drugs 0.000 abstract 2
- LULNWZDBKTWDGK-UHFFFAOYSA-M neostigmine bromide Chemical compound [Br-].CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 LULNWZDBKTWDGK-UHFFFAOYSA-M 0.000 abstract 2
- 229960001032 trihexyphenidyl Drugs 0.000 abstract 2
- 206010008428 Chemical poisoning Diseases 0.000 abstract 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 abstract 1
- 229960004373 acetylcholine Drugs 0.000 abstract 1
- 239000000812 cholinergic antagonist Substances 0.000 abstract 1
- 230000007062 hydrolysis Effects 0.000 abstract 1
- 238000006460 hydrolysis reaction Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000003987 organophosphate pesticide Substances 0.000 abstract 1
- 229940127230 sympathomimetic drug Drugs 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 description 7
- 241001465754 Metazoa Species 0.000 description 3
- 231100000331 toxic Toxicity 0.000 description 3
- 230000002588 toxic effect Effects 0.000 description 3
- 231100000614 poison Toxicity 0.000 description 2
- 231100000572 poisoning Toxicity 0.000 description 2
- 230000000607 poisoning effect Effects 0.000 description 2
- 230000001681 protective effect Effects 0.000 description 2
- LBKUQHSINDZGJA-UHFFFAOYSA-N 1-phenylpropan-1-ol;hydrochloride Chemical compound Cl.CCC(O)C1=CC=CC=C1 LBKUQHSINDZGJA-UHFFFAOYSA-N 0.000 description 1
- 208000028048 Accommodation disease Diseases 0.000 description 1
- 208000006550 Mydriasis Diseases 0.000 description 1
- 239000000150 Sympathomimetic Substances 0.000 description 1
- 230000003153 cholinolytic effect Effects 0.000 description 1
- 230000010339 dilation Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000004438 eyesight Effects 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 230000009931 harmful effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 231100000566 intoxication Toxicity 0.000 description 1
- 230000035987 intoxication Effects 0.000 description 1
- 230000002427 irreversible effect Effects 0.000 description 1
- 231100000636 lethal dose Toxicity 0.000 description 1
- GEPDYQSQVLXLEU-AATRIKPKSA-N methyl (e)-3-dimethoxyphosphoryloxybut-2-enoate Chemical compound COC(=O)\C=C(/C)OP(=O)(OC)OC GEPDYQSQVLXLEU-AATRIKPKSA-N 0.000 description 1
- ALWKGYPQUAPLQC-UHFFFAOYSA-N neostigmine Chemical compound CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 ALWKGYPQUAPLQC-UHFFFAOYSA-N 0.000 description 1
- 229960002362 neostigmine Drugs 0.000 description 1
- 150000002903 organophosphorus compounds Chemical class 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 239000002574 poison Substances 0.000 description 1
- 229940043274 prophylactic drug Drugs 0.000 description 1
- 210000001747 pupil Anatomy 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 239000013037 reversible inhibitor Substances 0.000 description 1
- 230000001975 sympathomimetic effect Effects 0.000 description 1
- 231100000816 toxic dose Toxicity 0.000 description 1
- 239000003440 toxic substance Substances 0.000 description 1
- NFACJZMKEDPNKN-UHFFFAOYSA-N trichlorfon Chemical compound COP(=O)(OC)C(O)C(Cl)(Cl)Cl NFACJZMKEDPNKN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
Landscapes
- Health & Medical Sciences (AREA)
- Emergency Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Beschreibung description
Die Erfindung betrifft ein prophylaktisches Antidot für phosphororganische Pestizide.The invention relates to a prophylactic antidote for organophosphorus Pesticides.
Es sind bis heute keine wirksamen und sicheren medikamentösen prophylaktischen Mittal bekannt, welche von landwirtschaf-tlichen Arbeitern, die in einem ständigen Kontakt mit phosphororganischen Pestiziden stehen, benutzt werden können. Es werden in der Praxis die üblichen Schutzmasken und Schutzanzüge der Gesundheitspflege und des Arbeitsschutzes bei der Arbeit mit äußerst giftigen Stoffen benutzt, die sich in vielen Fällen als nicht wirksam erwiesen hoben. Das führt dadurch zu schwächeren oder stärkeren Intoxikationen.To date, there are no effective and safe prophylactic drugs Mittal known which of agricultural workers who work in a permanent Contact with organophosphorus pesticides can be used. It will in practice the usual protective masks and protective suits for health care and of occupational safety when working with extremely toxic substances that are used in many cases not proven effective. This leads to weaker ones or more severe intoxication.
Bei der Arbeit mit Pestiziden werden Überhaupt keine Regeln über die Benutzung prophylaktischer Mittel erwähnt, da bai uns (in Bulgarien) solche Präparate z.Zt. noch nich-t hergestellt worden, und in der Weltpraxis solche fast vollstärdig fehlen.When working with pesticides there are no rules at all about that Use of prophylactic means mentioned because we (in Bulgaria) have such preparations currently has not yet been produced, and in world practice such almost full strength miss.
Ziel der Erfindung ist ein prophylaktisches Antidot zu schaffen, welches von den Landwirtschaftlichen Arbeitern vor Arbeitsbeginn mit phosphororganischen Pestiziden, die eine hohe Toxizität aufwaisen, oral eingenommen wird, um dieselben vor Vergiftung zu schützen.The aim of the invention is to provide a prophylactic antidote which by the agricultural workers before starting work with organophosphorus Pesticides that are highly toxic, taken orally, are the same protect from poisoning.
Die erfindungsgemäße Aufgabe wird durch ein Mittel gelöst, welches Hydrozin-H-butilum-bromat 10 bis 15 mg Buskolisine o 5 peridyl) 1 -phenyl-1 -propanol-hydrochlorid 6 bis 12 mg Parkisan 3-Dimethyl-carbamoxy-phenyl-trimethyl-ammonium-bromat 5 bis 6 mg Neostigmine 1-1-Phenyl-2-methyl-aminopropanolhydrochlorid 5 bis 6 mg Ephedrin enthält.The object of the invention is achieved by a means which Hydrozine H-butilum bromate 10 to 15 mg buscolisine o 5 peridyl) 1 -phenyl-1-propanol hydrochloride 6 to 12 mg Parkisan 3-dimethyl-carbamoxy-phenyl-trimethyl-ammonium-bromate 5 bis 6 mg neostigmine 1-1-phenyl-2-methyl-aminopropanol hydrochloride 5 contains up to 6 mg ephedrine.
Die ersten zwei Komponenten weisen gemeinsam zentrale und periphere M- und H»cholinolytische Eigenschaften auf und antagonisieren die toxische Wirkung der phosphororganischen Pestizide. Die dritte Komponente ist ein umkehrbarer Inhibitor der Cholinesterase und verstärkt die Antidoteffekte der ersten zwei Komponenten, indem sie die Cholinesterase vor einer nichtumkehrbaren Inhibierung schützen. Die vierte Komponente ist sympathikomimetisch und spielt eine korrigierende Rolle auf die atropinähnlichen Effekte der ersten zwei Koinponenten, ohna deren Effektivität zu vermindern. Das Präparat besitzt eine große Schutzfähigkeit bei einem Kontakt mit toxischen Dosen der phosphororganischen Pestizide, während einer Zeitspanne von 6 bis 8 Stunden von dem oralen Einnehmen des Pr;:-jparates und dem Inkontakttreten mit dern Gift.The first two components have in common central and peripheral M and H »cholinolytic properties and antagonize the toxic effect organophosphorus pesticides. The third component is a reversible inhibitor of cholinesterase and strengthens the antidote effects of the first two components, by protecting cholinesterase from irreversible inhibition. the fourth component is sympathomimetic and plays a corrective role the atropine-like effects of the first two components, without their effectiveness to diminish. The preparation has a great ability to protect against contact with toxic doses of the organophosphorus pesticides, for a period of time from 6 to 8 hours from oral ingestion of the product and contact with the poison.
I)ie Erfindung hat folgende Vorteile: Bei der Einnahme seitens des Menschen von jeweils einer Dosis pro Tag werden keine Nebenerscheinungen festgestellt, außer einer leichten Trockenheit im Munde in einzelnen Fällen. Bei der Einnahme von zwei bis drei Dosen des Präparates pro Tag werden einige Nebenerscheinungen festgestellt, wie Trockenheit im Munde, eine mäßige Mydriasis (Pupillenerweiterung), Akkomodationsstörungen der Sehkraft und andere, die nach Einstellung der Einnahme des Präparats schnell vorübergehen. Dieselben Erscheinungen sind Folge der atropinähnlichen Wirkungen der Komponente des Präparates.I) he invention has the following advantages: When taken by the People taking one dose per day will not experience any side effects, apart from a slight dryness in the mouth in isolated cases. When ingested Two to three doses of the preparation a day will cause some side effects noted, such as dryness in the mouth, moderate mydriasis (dilation of the pupil), Disorders of accommodation of eyesight and others after cessation of use of the preparation pass quickly. The same phenomena are the result of the atropine-like ones Effects of the component of the preparation.
Eine oral eingenommene Tablette genügt, um den Menschen vor der toxischen Wirkung der phosphororganischen Pestizide für einen ganzen Arbeitstag zu schützen.One tablet taken orally is enough to protect humans from the toxic To protect the effect of the organophosphorus pesticides for a whole working day.
Das erfindungsgemäße Antidotmittel enthält in seinem prophylaktischen Bereich folgende Komponente: Beispiel Hyoszin-H-butilum-bromat 10 mg 3-(II-Piperidyl) -1 -phenyl-l -cyclohexyl-1 -propanol-hydrochlorid 6 mg 4-Dimethyl-carbamoxy-phenyl-trimethyl-ammonium-bromat 5 mg 1-1-Phenyl-2-methyl-aminopropanolhydrochlorid 6 mg Bei Versuchstieren oral eingenommen sichert es einen sicheren medikamentösen Schutz gegen die schädliche Wirkung einer absoluten letalen Dosis (1 LD100) von Phosdrin, Neguvon und anderen phosphororganischen Verbindungen, wobei alle Versuchstiere eine volle Genesung erreichen, wenn die Vergiftung bis zur sechsten Stunde nach Einnahme des Präparates stattgefunden hat, gegenüber einer 1000,4-igen Mortalität der Kontrolltiere. Beim Ilenschen oral eingenommen, verursacht das Präparat keine besonderen Nebenerscheinungen, außer einer leichten Trockenheit im Munde in einzelnen Fällen.The antidote agent according to the invention contains in its prophylactic Area of the following components: Example Hyoszin-H-butilum-bromat 10 mg 3- (II-Piperidyl) -1-phenyl-1 -cyclohexyl-1-propanol hydrochloride 6 mg 4-dimethyl-carbamoxy-phenyl-trimethyl-ammonium-bromate 5 mg 1-1-phenyl-2-methyl-aminopropanol hydrochloride 6 mg orally in test animals taken it ensures a safe drug protection against the harmful Effect of an absolute lethal dose (1 LD100) of Phosdrin, Neguvon and others organophosphorus compounds, whereby all test animals achieve a full recovery, if the poisoning occurred up to the sixth hour after taking the preparation compared to a mortality of 1000.4 in the control animals. Oral in Ilenschen taken, the preparation does not cause any particular side effects, except a slight dryness in the mouth in isolated cases.
Claims (1)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19782821778 DE2821778A1 (en) | 1978-05-18 | 1978-05-18 | Prophylactic antidotes to organo-phosphorus poisoning - contain hyoscine butyl bromate, a propanol chlor:hydrate, di:methyl-carbamoxy-phenyl-tri:methyl ammonium bromate and ephedrine |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19782821778 DE2821778A1 (en) | 1978-05-18 | 1978-05-18 | Prophylactic antidotes to organo-phosphorus poisoning - contain hyoscine butyl bromate, a propanol chlor:hydrate, di:methyl-carbamoxy-phenyl-tri:methyl ammonium bromate and ephedrine |
Publications (1)
Publication Number | Publication Date |
---|---|
DE2821778A1 true DE2821778A1 (en) | 1979-12-20 |
Family
ID=6039661
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE19782821778 Withdrawn DE2821778A1 (en) | 1978-05-18 | 1978-05-18 | Prophylactic antidotes to organo-phosphorus poisoning - contain hyoscine butyl bromate, a propanol chlor:hydrate, di:methyl-carbamoxy-phenyl-tri:methyl ammonium bromate and ephedrine |
Country Status (1)
Country | Link |
---|---|
DE (1) | DE2821778A1 (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5430030A (en) * | 1991-05-13 | 1995-07-04 | Arzneimittelwerk Dresden Gmbh | Nerve gas antidote |
WO2001068137A2 (en) * | 2000-03-14 | 2001-09-20 | Brown University Research Foundation | Compositions for regulating memory consolidation |
-
1978
- 1978-05-18 DE DE19782821778 patent/DE2821778A1/en not_active Withdrawn
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5430030A (en) * | 1991-05-13 | 1995-07-04 | Arzneimittelwerk Dresden Gmbh | Nerve gas antidote |
WO2001068137A2 (en) * | 2000-03-14 | 2001-09-20 | Brown University Research Foundation | Compositions for regulating memory consolidation |
WO2001068137A3 (en) * | 2000-03-14 | 2002-04-11 | Univ Brown Res Found | Compositions for regulating memory consolidation |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
OAR | Request for search filed | ||
OB | Request for examination as to novelty | ||
OC | Search report available | ||
8139 | Disposal/non-payment of the annual fee |