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BR9912827A - Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda - Google Patents

Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda

Info

Publication number
BR9912827A
BR9912827A BR9912827-6A BR9912827A BR9912827A BR 9912827 A BR9912827 A BR 9912827A BR 9912827 A BR9912827 A BR 9912827A BR 9912827 A BR9912827 A BR 9912827A
Authority
BR
Brazil
Prior art keywords
morphine
topical
tolerance
nmda
peripheral
Prior art date
Application number
BR9912827-6A
Other languages
English (en)
Inventor
Yuri Kolesnikov
Gavril W Pasternak
Original Assignee
Sloan Kettering Inst Cancer
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 Inst Cancer filed Critical Sloan Kettering Inst Cancer
Publication of BR9912827A publication Critical patent/BR9912827A/pt

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/33Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • A61P23/02Local anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-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)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Anesthesiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Patente de Invenção: <B>"COMPOSIçõES TóPICAS COMPREENDENDO UM ANALGéSICO OPIóIDE E UM ANTAGONISTA DE NMDA"<D>. Um paradigma de opióide tópico foi desenvolvido para determinar os efeitos periféricos analgésicos da morfina. A morfina tópica, assim como os peptídeos, tais como [D-Ala2, MePhe4, Gly(ol)5]encefalina (DAMGO) produziu uma potente analgesia dependente de dose, usando o ensaio de calor radiante de agitação da cauda. As drogas tópicas potenciaram os agentes sistêmicos, de modo similar à sinergia previamente estabelecida entre os locais de ação periférico e central. A tolerância local foi rapidamente produzida mediante exposição diária tópica repetida à morfina. A tolerância à morfina tópica foi efetivamente bloqueada pelo antagonista do receptor de N-metil-D-aspartato (NMDA), MK801, e foi dado cetamina de forma sistêmica ou de forma tópica. Os antagonistas do receptor de NMDA reverteram a tolerância à morfina já existente. A atividade tópica dos antagonistas de NMDA para bloquear a tolerância local à morfina, sugere que os receptores periféricos de NMDA promovem a mediação da tolerância tópica à morfina. A morfina foi cruzada com a tolerância do [D-Ala², MePhe^ 4^, Gly(ol)^ 5^]encefalina (DAMGO), mas não foi cruzada com a morfina-6ß-glucuronida, vinculando diferentes mecanismos de ação. Essas observações são de grande importância no modelo e uso dos opióides clinicamente. São descritas composições farmacêuticas tópicas que compreendem um analgésico que atua através de um receptor de opiato e um antagonista de receptor de NMDA, para produção de analgesia sem induzir tolerância.
BR9912827-6A 1998-07-16 1999-07-15 Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda BR9912827A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9298298P 1998-07-16 1998-07-16
PCT/US1999/016049 WO2000003716A1 (en) 1998-07-16 1999-07-15 Topical compositions comprising an opioid analgesic and an nmda antagonist

Publications (1)

Publication Number Publication Date
BR9912827A true BR9912827A (pt) 2001-05-02

Family

ID=22236108

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9912827-6A BR9912827A (pt) 1998-07-16 1999-07-15 Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda

Country Status (15)

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

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BR9912827A (pt) 1998-07-16 2001-05-02 Sloan Kettering Inst Cancer Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda
BR0010653A (pt) 1999-03-23 2002-02-05 Univ James Cook Parada, proteção e preservação de orgãos
US6455066B1 (en) * 2000-03-10 2002-09-24 Epicept Corporation Intradermal-penetration agents for topical local anesthetic administration
CA2407683C (en) * 2000-04-28 2010-04-13 Memorial Sloan-Kettering Cancer Center Topical anesthetic/opioid formulations and uses thereof
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
DK2266558T3 (en) 2001-06-07 2017-07-31 Analgesic Neuropharmaceuticals Llc TREATMENT OF NEUROPATHIC PAIN WITH RECEPTOR ANTAGONIST: N-METHYL-D-ASPARTATE (NMDA)
DE10141650C1 (de) 2001-08-24 2002-11-28 Lohmann Therapie Syst Lts Transdermales Therapeutisches System mit Fentanyl bzw. verwandten Substanzen
EP1545461A4 (en) * 2002-09-09 2011-06-22 Endo Pharmaceuticals Inc COMBINED ANALGESIC COMPOSITION WITH IMMEDIATE AND PROLONGED RELEASE
US20060034941A1 (en) * 2002-12-23 2006-02-16 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
US20090258092A1 (en) 2006-05-29 2009-10-15 Hibernation Threapeutics Limited Improved Tissue Maintenance
KR101490836B1 (ko) 2006-07-25 2015-02-09 하이버네이션 테라퓨틱스, 어 케이에프 엘엘씨 외상 치료법
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
ES2560676T3 (es) * 2010-06-15 2016-02-22 Grünenthal GmbH Combinación farmacéutica para el tratamiento del dolor
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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Also Published As

Publication number Publication date
US7700122B1 (en) 2010-04-20
IL140834A (en) 2009-02-11
ATE344035T1 (de) 2006-11-15
AU758448B2 (en) 2003-03-20
PT1102589E (pt) 2006-12-29
IL140834A0 (en) 2002-02-10
DE69933874T2 (de) 2007-10-04
CA2336902A1 (en) 2000-01-27
JP2007246546A (ja) 2007-09-27
EP1102589B1 (en) 2006-11-02
CA2336902C (en) 2009-04-21
KR100762018B1 (ko) 2007-10-04
ES2198196A1 (es) 2004-01-16
DE69933874D1 (de) 2006-12-14
DK1102589T3 (da) 2006-12-04
KR20010070969A (ko) 2001-07-28
WO2000003716A1 (en) 2000-01-27
EP1102589A1 (en) 2001-05-30
ES2198196B2 (es) 2006-04-01
JP2002520363A (ja) 2002-07-09
AU4998799A (en) 2000-02-07
CN1309562A (zh) 2001-08-22

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A,6A,7A, E 8A ANUIDADES

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1911 DE 21/08/2007.