ES2198196A1 - Composiciones topicas que comprenden un analgesico opioide y un antagonista de nmda. - Google Patents

Composiciones topicas que comprenden un analgesico opioide y un antagonista de nmda.

Info

Publication number
ES2198196A1
ES2198196A1 ES200150003A ES200150003A ES2198196A1 ES 2198196 A1 ES2198196 A1 ES 2198196A1 ES 200150003 A ES200150003 A ES 200150003A ES 200150003 A ES200150003 A ES 200150003A ES 2198196 A1 ES2198196 A1 ES 2198196A1
Authority
ES
Spain
Prior art keywords
morphine
topical
tolerance
nmda
peripheral
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.)
Granted
Application number
ES200150003A
Other languages
English (en)
Other versions
ES2198196B2 (es
Inventor
Yuri Kolesnikov
Gavril W Pasternak
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Memorial Sloan Kettering Cancer Center
Original Assignee
Sloan Kettering Institute for Cancer Research
Memorial Sloan Kettering Cancer Center
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sloan Kettering Institute for Cancer Research, Memorial Sloan Kettering Cancer Center filed Critical Sloan Kettering Institute for Cancer Research
Publication of ES2198196A1 publication Critical patent/ES2198196A1/es
Application granted granted Critical
Publication of ES2198196B2 publication Critical patent/ES2198196B2/es
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/33—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Anesthesiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

En un modelo de opioide tópico, la morfina tópica así como péptidos tales como [D-Ala2,MePhe4,Gly(ol)5] encefalina (DAMGO) produjeron una potente analgesia dependiente de la dosis. Los fármacos tópicos potenciaron agentes sistémicos, de forma similar a la sinergia previamente establecida entre los sitios de acción periféricos y centrales. Se produjo rápidamente una tolorancia local por una exposición tópica diaria repetida a la morfina. La tolerancia a la morfina tópica se bloqueó de forma eficaz por el antagonista MK801 de los receptores N-metil-D- aspartato (NMDA) y Ketamina administrados bien por vía sistématica o tópica. Los antagonistas del receptor NMDA inviertieron la tolerancia a la morfina ya existente. La actividad de los antagonistas NMDA tópicos para bloquear la tolerancia a la morfina tópica sugiere que los receptores NMDA periféricos median la tolerancia a la morfina tópica. Se describen composiciones farmacéuticas tópicas que comprenden un analgésico que funciona a tráves deun receptor opioide y un antagonista del receptor NMDA para producir analgesia sin inducir tolerancia.
ES200150003A 1998-07-16 1999-07-15 Composiciones topicas que comprenden un analgesico opioide y un antagonista de nmda. Expired - Fee Related ES2198196B2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9298298P 1998-07-16 1998-07-16
US60/092982 1998-07-16

Publications (2)

Publication Number Publication Date
ES2198196A1 true ES2198196A1 (es) 2004-01-16
ES2198196B2 ES2198196B2 (es) 2006-04-01

Family

ID=22236108

Family Applications (1)

Application Number Title Priority Date Filing Date
ES200150003A Expired - Fee Related ES2198196B2 (es) 1998-07-16 1999-07-15 Composiciones topicas que comprenden un analgesico opioide y un antagonista de nmda.

Country Status (15)

Country Link
US (1) US7700122B1 (es)
EP (1) EP1102589B1 (es)
JP (2) JP2002520363A (es)
KR (1) KR100762018B1 (es)
CN (1) CN1309562A (es)
AT (1) ATE344035T1 (es)
AU (1) AU758448B2 (es)
BR (1) BR9912827A (es)
CA (1) CA2336902C (es)
DE (1) DE69933874T2 (es)
DK (1) DK1102589T3 (es)
ES (1) ES2198196B2 (es)
IL (2) IL140834A0 (es)
PT (1) PT1102589E (es)
WO (1) WO2000003716A1 (es)

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PT1102589E (pt) 1998-07-16 2006-12-29 Memorial Sloan Kettering Inst Composições tópicas compreendendo um analgésico opióide e um antagonista do nmda
KR20020001797A (ko) 1999-03-23 2002-01-09 제임스 쿡 유니버시티 신체 기관의 정지, 보호 및 보존
US6455066B1 (en) * 2000-03-10 2002-09-24 Epicept Corporation Intradermal-penetration agents for topical local anesthetic administration
KR20030060771A (ko) 2000-04-28 2003-07-16 메모리얼 슬로안-케터링 캔서 센터 국소용 마취제/아편양약물 제제 및 이들의 용도
DE10025946A1 (de) * 2000-05-26 2001-11-29 Gruenenthal Gmbh Wirkstoffkombination
US20020013331A1 (en) 2000-06-26 2002-01-31 Williams Robert O. Methods and compositions for treating pain of the mucous membrane
US7820688B2 (en) 2001-04-27 2010-10-26 Memorial Sloan-Kettering Cancer Center Topical anesthetic/opioid formulations and uses thereof
ATE491474T1 (de) 2001-06-07 2011-01-15 Sang Christine Dr Behandlung von neuropathischen schmerzen mittels eines n-methyl-d-aspartate (nmda)-rezeptor- antagonists
DE10141650C1 (de) 2001-08-24 2002-11-28 Lohmann Therapie Syst Lts Transdermales Therapeutisches System mit Fentanyl bzw. verwandten Substanzen
JP2006500395A (ja) * 2002-09-09 2006-01-05 エンド ファーマシューティカルズ インコーポレーテッド 組み合わされた即時放出及び徐放の鎮痛組成物
CA2551169A1 (en) * 2002-12-23 2004-07-08 Global Cardiac Solutions Pty Ltd Organ preconditioning, arrest, protection, preservation and recovery
DE10340428B4 (de) * 2003-09-02 2015-02-12 Acino Ag Opioides Analgetikum enthaltende transdermale Formulierung
US20060052370A1 (en) * 2004-08-24 2006-03-09 Meyerson Laurence R Methods and compositions for treating nociceptive pain
EP2659773A1 (en) 2006-05-29 2013-11-06 Hibernation Therapeutics Limited Improved tissue maintenance
CA2692256C (en) 2006-07-25 2017-01-10 Hibernation Therapeutics Limited Trauma therapy
WO2008106724A1 (en) 2007-03-02 2008-09-12 Hibernation Therapeutics Limited Transplants
CN101317844B (zh) * 2007-06-08 2010-11-17 章劲夫 化合物(+)-5-甲基-10，11-二氢-5H-二苯并〔a，d〕环庚烯-5，10-亚胺在制备避孕药物中的应用
TWI380992B (zh) 2010-03-11 2013-01-01 Univ Ishou 一種抑制ｎｍｄａ受體ｎｒ１之小段干擾ｒｎａ、該小段干擾ｒｎａ用以抑制皮下組織ｎｍｄａ受體ｎｒ１之方法、該小段干擾ｒｎａ之用途以及一種減緩皮膚炎症性疼痛之藥物化合物
RU2589692C2 (ru) * 2010-06-15 2016-07-10 Грюненталь Гмбх Фармацевтическая комбинация для лечения от боли
DE102010024105A1 (de) 2010-06-17 2011-12-22 Grünenthal GmbH Transdermale Verabreichung von Memantin
TWI417109B (zh) 2010-12-30 2013-12-01 Univ Ishou 一種用以抑制ｎｍｄａ受體ｎｒ１之短夾ｒｎａ、一種以短夾rna製備用以抑制ｎｍｄａ受體ｎｒ１之試劑之用途以及一種減緩皮膚炎症性疼痛之藥物
FR2998892B1 (fr) 2012-12-04 2015-01-02 Pf Medicament Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments
CN105705151A (zh) 2013-07-17 2016-06-22 低温药理Kf有限公司 一种用于治疗出血、休克和脑损伤的方法
CN107028968B (zh) * 2016-02-03 2020-12-04 江苏恒瑞医药股份有限公司 一种含有葡萄糖醛酸吗啡或其可药用盐的药物组合物
CN114642744B (zh) * 2022-02-09 2023-05-23 南京医科大学 一种筛选缓解吗啡耐受药物的方法

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WO1997010815A1 (en) * 1995-09-22 1997-03-27 Frome Bruce M The preparation of topical regional compositions for the relief of pain
US5635204A (en) * 1994-03-04 1997-06-03 Montefiore Medical Center Method for transdermal induction of anesthesia, analgesia or sedation
WO1998031358A1 (en) * 1997-01-22 1998-07-23 Cornell Research Foundation, Inc. d-METHADONE, A NONOPIOID ANALGESIC

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WO1997010815A1 (en) * 1995-09-22 1997-03-27 Frome Bruce M The preparation of topical regional compositions for the relief of pain
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Also Published As

Publication number Publication date
IL140834A (en) 2009-02-11
CA2336902C (en) 2009-04-21
KR100762018B1 (ko) 2007-10-04
ES2198196B2 (es) 2006-04-01
ATE344035T1 (de) 2006-11-15
WO2000003716A1 (en) 2000-01-27
CA2336902A1 (en) 2000-01-27
PT1102589E (pt) 2006-12-29
CN1309562A (zh) 2001-08-22
AU4998799A (en) 2000-02-07
US7700122B1 (en) 2010-04-20
DE69933874D1 (de) 2006-12-14
EP1102589A1 (en) 2001-05-30
BR9912827A (pt) 2001-05-02
AU758448B2 (en) 2003-03-20
JP2002520363A (ja) 2002-07-09
JP2007246546A (ja) 2007-09-27
EP1102589B1 (en) 2006-11-02
IL140834A0 (en) 2002-02-10
DK1102589T3 (da) 2006-12-04
KR20010070969A (ko) 2001-07-28
DE69933874T2 (de) 2007-10-04

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