DE4130918A1 - Alpha-sympatholytic and beta-sympathomimetic contg. solns. - for injection after dental anaesthesia to relieve vasoconstriction and reduce anaesthetic effect - Google Patents

Alpha-sympatholytic and beta-sympathomimetic contg. solns. - for injection after dental anaesthesia to relieve vasoconstriction and reduce anaesthetic effect

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Publication number
DE4130918A1
DE4130918A1 DE19914130918 DE4130918A DE4130918A1 DE 4130918 A1 DE4130918 A1 DE 4130918A1 DE 19914130918 DE19914130918 DE 19914130918 DE 4130918 A DE4130918 A DE 4130918A DE 4130918 A1 DE4130918 A1 DE 4130918A1
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Germany
Prior art keywords
beta
alpha
sympatholytic
sympathomimetic
solution according
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Withdrawn
Application number
DE19914130918
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German (de)
Inventor
Juergen Dr Huhnt
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Individual
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Individual
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Priority to DE19914130918 priority Critical patent/DE4130918A1/en
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim

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  • Health & Medical Sciences (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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A novel injection soln. (I) contains at least one alpha-sympatholytic and a beta-sympathomimetic. Pref. the alpha-sympatholytic is a n alpha1-sympatholytic, esp. Terazosin or Urapidil or their pharmaceutically acceptable salts and the beta-sympathomimetic is a beta1-sympathominetic esp. Salbutanol, Terbutalin, Fenoterol, Clenbuterol, Bamethan, Buphenia, Isoxsuprin or their pharmaceutically acceptable salts. Esp. (I) contains Isoxsuprin hydrochloride and Urapidil hydrochloride. The wt. ratio of alpha-sympatholytic to beta-sympathomimetic is 0.5-1.5:2. USE/ADVANTAGE - (I) can be used to interrupt local anaesthesia, esp. after dental treatment. (I) counteracts the vasoconstricting effect of the local anaesthetics used in dentistry as soon as possible after treatment. The increased blood flow in the area of the operation after admin. of (I) reduces the duration of action of the local anaesthetic

Description

Die Erfindung betrifft Arzneimittel zur Unterbrechung der lokalen Anästhesie, insbesondere nach zahnärzt­ licher Behandlung sowie deren Verwendung.The invention relates to pharmaceuticals for interruption of local anesthesia, especially after dentist Licher treatment and their use.

Bei zahnärztlichen Eingriffen wie dem Zementieren einer Krone oder eines Inlays, dem Legen einer Füllung oder ähnlichen Behandlungsmaßnahmen ist eine Lokal­ anästhesie im Kieferbereich von Vorteil, da sie dem Patienten während der Behandlung Schmerzen nimmt und dem behandelnden Arzt eine störungsfreie Behandlung ermöglicht.For dental procedures such as cementing a crown or an inlay, laying a filling or similar treatments is a local Anesthesia in the jaw area of advantage, since they are the Patients taking pain during treatment and the treating doctor a trouble-free treatment allows.

So vorteilhaft eine Lokalanästhesie während der Behand­ lung auch ist, so ist sie für den Patienten nach der Behandlung häufig mit einer langandauernden mimischen und sprachlichen Beeinträchtigung verbunden.So beneficial a local anesthetic during the treatment mentation, it is after the patient Treatment often with a long-lasting mimic and linguistic impairment.

Bei den meisten in der Zahnheilkunde gebräuchlichen Lokalanästhetika sorgen Adrenalin oder verwandte Sub­ stanzen für eine mehr oder weniger starke vasokonstrik­ torische Wirkung im Bereich der Einstichstelle, wodurch eine relative Anämie im Operationsgebiet erzeugt wird, so daß das eigentliche Anästhetikum in diesem Bereich eine lange Verweildauer hat.Used by most in dentistry Local anesthetics provide adrenaline or related sub punching for a more or less strong vasoconstrict toric effect in the area of the puncture site, causing a relative anemia in the operating area is generated so that the actual anesthetic in this area has a long residence time.

Der Erfindung liegt die Aufgabe zugrunde, die vasokon­ striktorische Wirkung im Operationsgebiet nach Ab­ schluß der Behandlung so schnell wie möglich aufzu­ heben. The invention is based on the object vasokon striktorische effect in the operation area after Ab conclusion of the treatment as soon as possible to lift.  

Diese Aufgabe wird durch die Injektionslösung nach Anspruch 1 gelöst.This task is followed by the injection solution Claim 1 solved.

Die Wirkung basiert auf der gesteigerten Durchblutung des Behandlungsgebietes, so daß die Verweildauer des Lokalanästhetikums verringert und die Anästhesie aufgehoben wird.The effect is based on the increased blood flow of the treatment area, so that the residence time of Local anesthetic decreases and anesthesia will be annulled.

Besonders geeignete alpha-Sympatholytika sind sogenan­ nte alpha1-Sympatholytika wie Urapidil, die auch als pharmazeutisch verträgliche Säureadditionssalze ein­ gesetzt werden können.Particularly suitable alpha-sympatholytic agents are so-called alpha 1 -sympatholytics, such as urapidil, which can also be used as pharmaceutically acceptable acid addition salts.

Besonders geeignete beta-Sympathomimetika sind soge­ nannte beta2-Sympathomimetika wie Salbutamol, Terbu­ talin, Fenoterol, Clenbuterol, Bamethan, Buphenin und Isoxsuprin.Particularly suitable beta-sympathomimetics are so-called beta 2 -sympathomimetics such as salbutamol, terbu talin, fenoterol, clenbuterol, bamethane, buphenin and isoxsuprin.

Die Herstellung der erfindungsgemäßen Injektions­ mittel erfolgt nach den in den Arzneibüchern festge­ legten Regeln. Ein geeignetes Lösungsmittel ist beispielsweise physiologische Kochsalzlösung. Zur Verbesserung der Löslichkeit kommen Zusätze von Ethanol, Glycerol, 1,2-Propylenglykol oder Poly­ ethylenglykolen in Betracht.The preparation of the injection according to the invention The medium is determined by the pharmacopoeias set rules. A suitable solvent is for example, physiological saline. to Solubility enhancements come from additives Ethanol, glycerol, 1,2-propylene glycol or poly ethylene glycols into consideration.

Als besonders geeignet zur Beendigung der Anästhesie erwies sich eine Injektionslösung aus Isoxsuprinhydro­ chlorid und Urapidil. Dabei sind etwa 10 mg Isoxsuprin­ hydrochlorid und 21,8 mg Urapidilhydrochlorid in 6 ml eines Gemisch aus physiologischer Kochsalzlösung und Propylenglykol gelöst.Especially suitable for stopping anesthesia proved an injection solution of Isoxsuprinhydro chloride and urapidil. This is about 10 mg isoxsuprin hydrochloride and 21.8 mg urapidil hydrochloride in 6 ml a mixture of physiological saline and Dissolved in propylene glycol.

Geeignete Zubereitungen sind:Suitable preparations are:

Urapidilhydrochlorid|21,8 mgUrapidil hydrochloride | 21.8 mg Isoxsuprinisoxsuprine 10,0 mg10.0 mg Propylenglykolpropylene glycol 400,0 mg400.0 mg NaCl 0,9%NaCl 0.9% ad 5,0 mlad 5.0 ml

Urapidilhydrochlorid|21,8 mgUrapidil hydrochloride | 21.8 mg BupheninhydrochloridBupheninhydrochlorid 10,0 mg10.0 mg Propylenglykolpropylene glycol q. s.q. s. NaCl 0,9%NaCl 0.9% ad 5,0 mlad 5.0 ml

Urapidilhydrochlorid|21,8 mgUrapidil hydrochloride | 21.8 mg BamethanhydrochloridBamethanhydrochlorid 10,0 mg10.0 mg Propylenglykolpropylene glycol q. s.q. s. NaCl 0,9%NaCl 0.9% ad 5,0 mlad 5.0 ml

In den erfindungsgemäßen Injektionslösungen beträgt das Gewichtsverhältnis alpha-Sympatholytikum zu beta- Sympathomimetikum ungefähr 0,5 bis 1,5 zu 2. Bei etwa 90% der Patienten zeigt sich nach Injektion von 1 bis 2 ml der erfindungsgemäßen Lösungen pro Zahn eine Aufhebung der Lokalanästhesie innerhalb weniger Minuten.In the injection solutions according to the invention the weight ratio alpha sympatholytic to beta Sympathomimetic about 0.5 to 1.5 to 2. At about 90% of patients appear after injection of 1 to 2 ml of the solutions according to the invention per tooth Cancellation of local anesthesia within less Minutes.

Claims (8)

1. Injektionslösung, enthaltend wenigstens ein alpha- Sympatholytikum und ein beta-Sympathomimetikum.1. Injection solution containing at least one alpha Sympatholytic and a beta-sympathomimetic. 2. Injektionslösung nach Anspruch 1, dadurch gekenn­ zeichnet, daß das alpha-Sympatholytikum ein alpha1-Sympatholytikum ist.2. Injection solution according to claim 1, characterized in that the alpha sympatholytic is an alpha 1 -Sympatholytikum. 3. Injektionslösung nach einem der Ansprüche 1 oder 2, dadurch gekennzeichnet, daß das beta-Sympatho­ mimetikum ein beta2-Sympathomimetikum ist.3. Injection solution according to one of claims 1 or 2, characterized in that the beta-Sympatho mimetic is a beta 2 -Sympathomimetikum. 4. Injektionslösung nach Anspruch 2 oder 3, dadurch gekennzeichnet, daß das alpha1-Sympatholytikum aus der Terazosin, Urapidil sowie deren pharmazeu­ tisch einsetzbarer Salze enthaltenden Gruppe ausgewählt ist.4. Injection solution according to claim 2 or 3, characterized in that the alpha 1 -Sympatholytikum from the terazosin, Urapidil and their pharmazeu table-usable salts containing group is selected. 5. Injektionslösung nach einem der Ansprüche 3 oder 4, dadurch gekennzeichnet, daß das beta2-Sympatho­ mimetikum aus der Salbutamol, Terbutalin, Fenote­ rol, Clenbuterol, Bamethan, Buphenin, Isoxsuprin sowie deren pharmazeutisch einsetzbarer Salze enthaltenden Gruppe ausgewählt ist.5. Injection solution according to one of claims 3 or 4, characterized in that the beta 2 -Sympatho mimetic from salbutamol, terbutaline, fenote rol, clenbuterol, bamethane, buphenin, Isoxsuprin and their pharmaceutically acceptable salts containing group is selected. 6. Injektionslösung nach einem der Ansprüche 1 bis 5, enthaltend Isoxsuprinhydrochlorid und Ura­ pidilhydrochlorid.6. Injection solution according to one of claims 1 to 5, containing isoxsuprine hydrochloride and urea pidilhydrochlorid. 7. Injektionslösung nach einem der Ansprüche 1 bis 6, dadurch gekennzeichnet, daß das Gewichtsver­ hältnis alpha-Sympatholytikum zu beta-Sympatho­ mimetikum 0,5 bis 1,5 zu 2 beträgt. 7. Injection solution according to one of claims 1 to 6, characterized in that the Gewichtsver alpha-sympatholytic ratio to beta-sympatho Mimetic 0.5 to 1.5 to 2.   8. Verwendung der Lösung nach einem der Ansprüche 1 bis 7 zur Aufhebung der vasokonstriktorischen Wirkung nach Gabe von Lokalanästhetika.8. Use of the solution according to one of claims 1 to 7 to lift the vasoconstrictor Effect after administration of local anesthetics.
DE19914130918 1991-09-17 1991-09-17 Alpha-sympatholytic and beta-sympathomimetic contg. solns. - for injection after dental anaesthesia to relieve vasoconstriction and reduce anaesthetic effect Withdrawn DE4130918A1 (en)

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Application Number Priority Date Filing Date Title
DE19914130918 DE4130918A1 (en) 1991-09-17 1991-09-17 Alpha-sympatholytic and beta-sympathomimetic contg. solns. - for injection after dental anaesthesia to relieve vasoconstriction and reduce anaesthetic effect

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DE19914130918 DE4130918A1 (en) 1991-09-17 1991-09-17 Alpha-sympatholytic and beta-sympathomimetic contg. solns. - for injection after dental anaesthesia to relieve vasoconstriction and reduce anaesthetic effect

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072016A1 (en) * 2003-02-14 2004-08-26 Kissei Pharmaceutical Co., Ltd. Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof
CN101200451B (en) * 2006-12-15 2010-12-15 重庆药友制药有限责任公司 Method for preparing hydrochloride urapidil
CN104173281A (en) * 2014-09-05 2014-12-03 河北一品制药有限公司 Urapidil hydrochloride injection and preparation method thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
1979,Vol.90, Ref.16458c *
Chem.Abstr.: 1992,Vol.116,Ref.143858k *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072016A1 (en) * 2003-02-14 2004-08-26 Kissei Pharmaceutical Co., Ltd. Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof
JPWO2004072016A1 (en) * 2003-02-14 2006-06-01 キッセイ薬品工業株式会社 Aminoalcohol derivatives, pharmaceutical compositions containing them, and uses thereof
US7423185B2 (en) 2003-02-14 2008-09-09 Kissei Pharmaceutical Co., Ltd. Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof
US7674938B2 (en) 2003-02-14 2010-03-09 Kissei Pharmaceutical Co., Ltd. Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof
JP4567596B2 (en) * 2003-02-14 2010-10-20 キッセイ薬品工業株式会社 Aminoalcohol derivatives, pharmaceutical compositions containing them, and uses thereof
CN101200451B (en) * 2006-12-15 2010-12-15 重庆药友制药有限责任公司 Method for preparing hydrochloride urapidil
CN104173281A (en) * 2014-09-05 2014-12-03 河北一品制药有限公司 Urapidil hydrochloride injection and preparation method thereof
CN104173281B (en) * 2014-09-05 2017-01-11 河北一品制药有限公司 Urapidil hydrochloride injection and preparation method thereof

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