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WO2004006903A1 - Traitement des vomissements - Google Patents

Traitement des vomissements Download PDF

Info

Publication number
WO2004006903A1
WO2004006903A1 PCT/GB2003/003002 GB0303002W WO2004006903A1 WO 2004006903 A1 WO2004006903 A1 WO 2004006903A1 GB 0303002 W GB0303002 W GB 0303002W WO 2004006903 A1 WO2004006903 A1 WO 2004006903A1
Authority
WO
WIPO (PCT)
Prior art keywords
use according
condition
induced
emesis
receptor antagonists
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.)
Ceased
Application number
PCT/GB2003/003002
Other languages
English (en)
Inventor
Michael Harvey Lyne
John Brew
Robin Mark Bannister
Andrew Douglas Baxter
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.)
Sosei R&D Ltd
Original Assignee
Arakis Ltd
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
Priority claimed from GB0216223A external-priority patent/GB0216223D0/en
Priority claimed from GB0216220A external-priority patent/GB0216220D0/en
Priority claimed from GB0222947A external-priority patent/GB0222947D0/en
Priority claimed from GB0222948A external-priority patent/GB0222948D0/en
Application filed by Arakis Ltd filed Critical Arakis Ltd
Priority to AU2003281158A priority Critical patent/AU2003281158A1/en
Publication of WO2004006903A1 publication Critical patent/WO2004006903A1/fr
Anticipated expiration legal-status Critical
Ceased 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone

Definitions

  • This invention relates to the use of a known compound in the treatment of emesis and related conditions.
  • Venlafaxine ( ⁇ )-1 -[2-(dimethylarnino)-1 -(4-methoxyphenyl)ethyl]- cyclohexanol, is an important drug used for the treatment of depression and pain.
  • the most common side-effects are nausea (experienced by about 45% of patients under treatment with racemic venlafaxine hydrochloride) and vomiting (occurs in about 17% of the patients).
  • emesis or a related condition is treated by the use of (+)- or (-)-venlafaxine.
  • (+)- or (-)-venlafaxine Given venlafaxine's side-effect profile, it was surprising to find that either stereoisomer of venlafaxine can prevent or diminish these side-effects and similar side-effects caused by other means.
  • the stereoisomer of venlafaxine is used in substantially enantiopure form.
  • the enantiomeric excess (with respect to the opposite enantiomer) may be at least 90% and is preferably at least 95%.
  • the enantiomer may be in the free form or as a salt, e.g. the hydrochloride, or metabolite or prodrug, or a desmethyl analogue.
  • Such analogues include (+)-O- desmethylvenl afaxi ne, ( + )-N -desmethylven lafaxine, (+)-N, N- didesmethylvenlafaxine, (+)-N,O-didesmethylvenlafaxine, (+)-O-desmethyl-N,N- didesmethylvenlafaxine and the corresponding (-)-enantiomers.
  • a single enantiomer of venlafaxine is used to treat nausea, dizziness, blurred vision or emesis, including, but not limited to, acute, delayed, post-operative, last-phase and anticipatory emesis.
  • This condition may be induced by, for example, chemotherapy, radiation, toxins, pregnancy, alcohol withdrawal, nicotine withdrawal, drug withdrawal, vestibular disorder, motion, post-operative sickness, surgery, gastrointestinal obstruction, reduced gastrointestinal motility, dysmenorrhoea, visceral pain, migraine, increased intracranial pressure, decreased intracranial pressure, depression or opioid analgesics.
  • the enantiomer of venlafaxine may be used to treat emesis caused by certain drugs such as antidepressants (examples including amitriptyline, imipramine, desipramine, venlafaxine, citalopram, trazadone, paroxetine, nefazodone, fluoxetine and (S)-citalopram), anticonvulsants (examples including lamotrigine, gabapentin and carbamezepine), antipsychotics (examples including clozapine, chlorpromazine, fluphenazine, haloperidol and loxapine), anxiolytics (examples including buspirone and lorazepam), anti-Parkinson's agents (examples including apomorphine, pergolide, levodopa, dopamine, naxagolide, bromocriptine and amantadine), CNS stimulants (examples including dexamp, cor
  • a single enantiomer of venlafaxine may be used according to the invention when the patient is also being given another anti-emetic agent.
  • agents include phenothiazines, 5HT3 receptor antagonists, dopamine antagonists, anticholinergic agents, anti-histamines, histamine analogues, cannabinoids, corticosteroids, GABA receptor antagonists, NK1 receptor antagonists, and ⁇ 2 and ⁇ 3 adrenoceptor antagonists.
  • these types of compounds are cyclizine, dolasetron, granisetron, ondansetron, tropisetron, nabilone, scopolenine, cinnerizine, promethazine, betahistine, dexamethasome, methylprednisolone, metoclopramide, chlorpromazine, perphenazine, prochlorperazine, thiethylperazine, droperidol, domperidoneand haloperidol.
  • any suitable route of administration can be used.
  • any of oral, topical, ocular, rectal, vaginal, inhalation and intranasal delivery routes may be suitable.
  • the dose of the active agent will depend on the nature and degree of the condition, the age and condition of the patient, and other factors known to those skilled in the art.
  • a typical dosage is 10-100 mg given one to three times per day. The evidence upon which this invention is based follows.
  • Male ferrets ( 0.9- 1.7 kg) were housed in pairs at 22 ⁇ 1°C and had free access to food (SDS Diet 'C (E), Special Diet Services, UK) and water. They were housed under artificial lighting with lights on between 07:00 and 21:00 hours. For experimental use, animals were removed from their holding cages and placed individually into observation cages. The animals were allowed free access to water and food.
  • Emesis was characterized by rhythmic abdominal contractions which were either associated with the oral expulsion of solid or liquid material from the gastrointestinal tract (i.e. vomiting) or not associated with the passage of material (i.e. retching movements). The number of highly distinctive abdominal contractions was counted.

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un procédé consistant à utiliser un seul énantiomère de venlafaxine pour traiter la nausée, l'étourdissement, la vision trouble ou le vomissement.
PCT/GB2003/003002 2002-07-12 2003-07-11 Traitement des vomissements Ceased WO2004006903A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003281158A AU2003281158A1 (en) 2002-07-12 2003-07-11 The treatment of emesis

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
GB0216223A GB0216223D0 (en) 2002-07-12 2002-07-12 The treatment of emesis, nausea and other disorders
GB0216220A GB0216220D0 (en) 2002-07-12 2002-07-12 The treatment of emesis nausea and other disorders
GB0216223.8 2002-07-12
GB0216220.4 2002-07-12
GB0222947A GB0222947D0 (en) 2002-10-03 2002-10-03 The treatment of emesis,nausea and other disorders
GB0222948.2 2002-10-03
GB0222948A GB0222948D0 (en) 2002-10-03 2002-10-03 The treatment of emesis,nausea and other disorders
GB0222947.4 2002-10-03

Publications (1)

Publication Number Publication Date
WO2004006903A1 true WO2004006903A1 (fr) 2004-01-22

Family

ID=30119203

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2003/003002 Ceased WO2004006903A1 (fr) 2002-07-12 2003-07-11 Traitement des vomissements

Country Status (2)

Country Link
AU (1) AU2003281158A1 (fr)
WO (1) WO2004006903A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009143572A1 (fr) * 2008-05-27 2009-12-03 The University Of Melbourne Procédés de traitement de mammifères souffrant de dysfonctionnements de la trompe d’eustache
US8556939B2 (en) 2008-01-08 2013-10-15 Fraser Cummins Henderson Mathematical relationship of strain, neurological dysfunction and abnormal behavior resulting from neurological dysfunction of the brainstem

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000032556A1 (fr) * 1998-12-01 2000-06-08 Sepracor Inc. Derives de (-)-venlafaxine et leurs procedes de preparation et d'utilisation
WO2000076956A2 (fr) * 1999-06-15 2000-12-21 American Home Products Corporation Enantiomeres de n-desmethyl venlafaxine
US20010055612A1 (en) * 1996-03-25 2001-12-27 American Home Products Corporation Five Giralda Farms Extended release formulation

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20010055612A1 (en) * 1996-03-25 2001-12-27 American Home Products Corporation Five Giralda Farms Extended release formulation
WO2000032556A1 (fr) * 1998-12-01 2000-06-08 Sepracor Inc. Derives de (-)-venlafaxine et leurs procedes de preparation et d'utilisation
WO2000076956A2 (fr) * 1999-06-15 2000-12-21 American Home Products Corporation Enantiomeres de n-desmethyl venlafaxine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GRUBB B P ET AL: "Preliminary observations on the effects of venlafaxine hydrochloride in the treatment of severe refractory orthostatic hypotension", JOURNAL OF SEROTONIN RESEARCH 1996 UNITED KINGDOM, vol. 3, no. 2, 1996, pages 85 - 89, XP009019140, ISSN: 1350-7702 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8556939B2 (en) 2008-01-08 2013-10-15 Fraser Cummins Henderson Mathematical relationship of strain, neurological dysfunction and abnormal behavior resulting from neurological dysfunction of the brainstem
WO2009143572A1 (fr) * 2008-05-27 2009-12-03 The University Of Melbourne Procédés de traitement de mammifères souffrant de dysfonctionnements de la trompe d’eustache
US8642631B2 (en) 2008-05-27 2014-02-04 University Of Melbourne Methods of treating mammals with eustachian tube dysfunctions
AU2009253739B2 (en) * 2008-05-27 2014-02-06 Otolanum Ag Methods of treating mammals with eustachian tube dysfunctions
EA022565B1 (ru) * 2008-05-27 2016-01-29 Дзе Юниверсити Оф Мельбурн Способы лечения млекопитающих с дисфункциями евстахиевой трубы

Also Published As

Publication number Publication date
AU2003281158A1 (en) 2004-02-02

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