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

    • 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
    • A61K31/44—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
    • 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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Rheumatology (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

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)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69933874T2 (de) 1998-07-16 2007-10-04 Memorial Sloan-Kettering Institute For Cancer Research Topische zusammensetzung enthaltend ein opioid-analgetika und einen nmda-antagonist
IL145552A0 (en) 1999-03-23 2002-06-30 Univ James Cook Organ arrest, protection and preservation
US6455066B1 (en) * 2000-03-10 2002-09-24 Epicept Corporation Intradermal-penetration agents for topical local anesthetic administration
IL152473A0 (en) * 2000-04-28 2003-05-29 Sloan Kettering Inst Cancer 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
DE60143671D1 (de) 2001-06-07 2011-01-27 Sang Christine 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
EP1545461A4 (en) * 2002-09-09 2011-06-22 Endo Pharmaceuticals Inc COMBINED ANALGESIC COMPOSITION WITH IMMEDIATE AND PROLONGED RELEASE
WO2004056180A1 (en) * 2002-12-23 2004-07-08 Global Cardiac Solutions Pty Ltd Organ preconditioning, arrest, protection, preservation and recovery (1)
DE10340428B4 (de) * 2003-09-02 2015-02-12 Acino Ag Opioides Analgetikum enthaltende transdermale Formulierung
WO2006024018A2 (en) * 2004-08-24 2006-03-02 Neuromolecular Pharmaceuticals, Inc. Compositions for treating nociceptive pain
AU2006345361B2 (en) 2006-05-29 2014-04-10 Hibernation Therapeutics, A Kf Llc Improved tissue maintenance
CN101516185A (zh) 2006-07-25 2009-08-26 低温药理有限公司 创伤治疗
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
US8846765B2 (en) 2010-06-15 2014-09-30 Gruenenthal Gmbh Pharmaceutical combination
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
WO2015006827A1 (en) 2013-07-17 2015-01-22 Hts Therapeutics Pty Ltd A method for inducing whole body arrest
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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5322683A (en) * 1989-05-01 1994-06-21 Leonard Mackles Anhydrous aerosol foam
JP2669951B2 (ja) * 1991-03-28 1997-10-29 雍憲 森本 麻薬性鎮痛剤を含有する経皮吸収組成物
JPH0733681A (ja) * 1993-05-18 1995-02-03 Sekisui Chem Co Ltd 経皮吸収貼付剤
US5635204A (en) * 1994-03-04 1997-06-03 Montefiore Medical Center Method for transdermal induction of anesthesia, analgesia or sedation
US5589480A (en) * 1994-08-17 1996-12-31 Elkhoury; George F. Topical application of opioid analgesic drugs such as morphine
JPH10513471A (ja) * 1995-02-10 1998-12-22 メドトロニック、インコーポレイテッド 鎮痛薬投与のための方法と装置
US5840731A (en) * 1995-08-02 1998-11-24 Virginia Commonwealth University Pain-alleviating drug composition and method for alleviating pain
US5849761A (en) * 1995-09-12 1998-12-15 Regents Of The University Of California Peripherally active anti-hyperalgesic opiates
US6197830B1 (en) * 1995-09-22 2001-03-06 Bruce M. Frome Method for achieving relief from sympathetically mediated pain
AUPN605795A0 (en) * 1995-10-19 1995-11-09 F.H. Faulding & Co. Limited Analgesic pharmaceutical composition
JPH09143061A (ja) * 1995-11-20 1997-06-03 Showa Denko Kk 鎮痛剤用経皮吸収製剤
US5891885A (en) * 1996-10-09 1999-04-06 Algos Pharmaceutical Corporation Method for treating migraine
WO1998016197A1 (en) * 1996-10-15 1998-04-23 Needham Charles W Surgical method and composition therefor
EP0946157B1 (en) 1996-12-16 2002-03-13 Alcon Laboratories, Inc. The topical use of kappa opioid agonists to treat ocular pain
US6008258A (en) 1997-01-22 1999-12-28 Cornell Research Foundation, Inc. d-methadone, a nonopioid analegesic
DE69933874T2 (de) 1998-07-16 2007-10-04 Memorial Sloan-Kettering Institute For Cancer Research Topische zusammensetzung enthaltend ein opioid-analgetika und einen nmda-antagonist
JP2000169378A (ja) 1998-12-10 2000-06-20 Taisho Pharmaceut Co Ltd 咽頭疾患用組成物
IL152473A0 (en) * 2000-04-28 2003-05-29 Sloan Kettering Inst Cancer Topical anesthetic/opioid formulations and uses thereof

Also Published As

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

Similar Documents

Publication Publication Date Title
BR9912827A (pt) Composições tópicas compreendendo um analgésico opióide e um antagonista de nmda
Sacerdote et al. Antinociceptive and immunosuppressive effects of opiate drugs: a structure‐related activity study
Miranda et al. Antinociception, tolerance, and physical dependence comparison between morphine and tramadol
PT845989E (pt) Composicao de farmacos para aliviar a dor
CR6767A (es) Una composicion farmaceutica para el tratamiento del dolor agudo, cronico y/o el dolor neuropatico y las migranas
HK1031692A1 (en) Pharmaceutical oral dosage form comprising a combination of an opioid agonist and naltrexone
AU2003275357A1 (en) Analgesic compositions comprising nmda receptor antagonists and benzalkonium chloride
WO2003090697A3 (en) Chimeric hybrid analgesics
RU2000119778A (ru) Комбинации агонист/антагонист опиоида
AU3080499A (en) Analgesic combination comprising nmda receptor antagonists and narcotic analgesics
CO5011096A1 (es) Medicamentos que contienen antagonistas del receptor 5-ht3 para el tratamiento de la ibs
ATE296629T1 (de) Pharmazeutische zusammensetzungen mit nmda- rezeptor-agonist
EP1762236A3 (en) Formulations of alpha adrenergic receptor antagonists and their uses
AP2002002617A0 (en) Tamper-resistant oral opioid agonist formulation
CA2325739A1 (en) Combination for the treatment of alcohol and drug dependence containing an opioid antagonist and a nmda receptor complex modulator
AU2161599A (en) Pharmaceutical combination with analgesic activity, containing an adenosinergic agonist and a compound selected from opiates, benzodiazepines and nmda antagonists
NO983945L (no) Isokinoliner som er nyttige som analgetika
BR0008468A (pt) Método para fertilização humana in vitro, uso de um hormÈnio hipotalânico e/ou hormÈnio pituitário ou de um agonista ou antagonista do mesmo ou de um derivado ativo do mesmo, kit farmacêutico em forma de dosagem única, e, qualquer novo aspecto ou combinação de aspectos
ATE252377T1 (de) Kontrolliert freisetzende pharmazeutische zusammensetzung mit tilidinmesylat als wirkstoff
ES2189252T3 (es) Composiciones analgesicas que comprenden un antagonista de la colecistoquinina y un opioide.
Benthuysen et al. Synthetic opioids compared with morphine and ketamine: catalepsy, cross-tolerance and interactions in the rat
AU3393000A (en) Opioid agonist in a fast dispersing dosage form
WO2001085153A3 (en) Potentiation of antineoplastic agents using sigma-2 ligands
Kwon et al. A Study of Epidural Droperidol Dosage for Reducing Nausea, Vomiting and Pruritus Due to Epidural Morphine and Fentanyl in Epidural Pain Management of Patients Undergoing Vaginal Total Hysterectomy.
Mattox et al. Pharmacological Analysis of the Rate-Decreasing Effects of Mu and Kappa Opioids in Pigeons

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.