EP1207883A1 - Utilisation d'au moins une substance a base de nicotine et/ou d'une substance produite a partir de la substance precitee et destinee a la preparation d'un medicament et methode de traitement de maladies pulmonaires obstructives - Google Patents

Utilisation d'au moins une substance a base de nicotine et/ou d'une substance produite a partir de la substance precitee et destinee a la preparation d'un medicament et methode de traitement de maladies pulmonaires obstructives

Info

Publication number
EP1207883A1
EP1207883A1 EP00959096A EP00959096A EP1207883A1 EP 1207883 A1 EP1207883 A1 EP 1207883A1 EP 00959096 A EP00959096 A EP 00959096A EP 00959096 A EP00959096 A EP 00959096A EP 1207883 A1 EP1207883 A1 EP 1207883A1
Authority
EP
European Patent Office
Prior art keywords
nicotine
medicament
substance
intended
use 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Withdrawn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
EP00959096A
Other languages
German (de)
English (en)
Inventor
Laszlo Bense
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.)
Individual
Original Assignee
Individual
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 SE9903085A external-priority patent/SE516807C2/sv
Application filed by Individual filed Critical Individual
Publication of EP1207883A1 publication Critical patent/EP1207883A1/fr
Withdrawn legal-status Critical Current

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
    • A61K31/465Nicotine; Derivatives thereof

Definitions

  • the present invention refers to a use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament to be supplied to an individual of a human being or an animal.
  • the invention also refers to a method for prophylactic or therapeutic treatment of obstructive lung diseases of in individual of a human being or an animal.
  • Pulmonary emphysema is a common disease, which in particular affects smokers. The disease is characterised by a permanent expansion and destruction of the finest bronchi and the walls of the alveoli. Pulmonary emphysema is a very serious disease and the destruction process is irreversible so that the disease leads to increasing respiratory difficulties.
  • Pulmonary emphysema belongs to a group of diseases usually called obstructive lung diseases due to the fact that the disease obstructs the flow in the respiratory tracts.
  • the obstruction is the underlying cause also to pulmonary barotrauma, including spontaneous pneumothorax.
  • These diseases have symptoms and localised effects to the lung tissue similar to pulmonary emphysema.
  • the bronchi are expanded, which counteracts the obstruction to a certain extent.
  • the lung tissue is compressed, including the bronchi, and a somewhat smaller gas volume may therefore flow through the respiratory tract. This leads to a valve effect when a certain balance arises.
  • the obstruction By a certain overpressure in the respiratory tracts and the lung, the obstruction may be overcome and the inhaled gas volume be emptied.
  • the pressure in the lung is however not sufficient for completely emptying the lung.
  • Pulmonary barotrauma appears due to such a tissue destruction by the inner pressure. Pulmonary barotrauma may principally refer to one single alveolus or a smallest respiratory tract, or several small alveoli within the lung. If this tissue destruction process is expanded to the whole lung it is called pulmonary emphysema. In the cases when air is collected diffusely in the lung tissue proper, we have an interstitial emphysema or in a delimited way, a bulla (blister). If the air is collected adjacent to the pleura in a delimited manner we have a subpleural bleb.
  • the air may also come to the intrapulmonary space and we have a so-called pneumomediastinum or into the heart sack; pneumopericardium. If the tissue destruction is expanded so that the pleura is destroyed, we have a spontaneous pneumothorax (SP). With regard to the fact that pathophysiological changes in the lung are documented in case of SP, it is not any longer relevant to call SP a disease of the pleura.
  • SP spontaneous pneumothorax
  • the obstruction leads to an expansion in a lung part and thus to a compression of the surrounding lung part.
  • Such an expansion and compression is irreversible for a smoker even if he would stop smoking.
  • If the surrounding compressed lung part is very large, surgery could be considered for removing a large significant blister and thus create space for the respiratory work.
  • it is very rare that a patient is suitable for such an operation, whereby an expected effect is far from being optimal.
  • AAT is an enzyme protecting the elastic fibres of the lung. The fibres are subjected to the largest load in the lower part, where the largest expansion of the lung takes place when we breathe. If the protecting effect ceases, the elasticity is lost and this can be easily seen on the most stressed tissue part.
  • the destruction may also be general without anomaly or AAT- deficiency due to smoking.
  • Bilateral bronchial anomaly is an anatomical congenital obstruction with a characteristically changed branching structure of the respiratory tracts and this obstruction may be increased by smoking. Bilateral bronchial anomaly may today be shown by diagnostic methods known per se, for instance by means of X-ray pictures disclosing the bronchial structure of a patient.
  • the respiratory tracts consist of bronchi, which from the main bronchus are divided to smaller and smaller bronchi.
  • the first bronchus forms the bronchus of the first generation, the bronchi after the first division are called the bronchi of the second generation, after the second division the bronchi of the third generation, etc.
  • Bilateral bronchial anomaly means that the bronchi of the third generation are missing in an individual and are replaced by very characteristic, irregular narrowing connections. The air exchange to and especially from the alveoli will thus be hampered by this defect bronchial structure, which is identifiable.
  • the object of the present invention is to provide a means, which counteracts such obstructive lung diseases in a prophylactic or therapeutic manner.
  • This object is obtained by the use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament to be supplied to an individual of a human being or an animal for the purpose of counteracting obstructive lung diseases in a prophylactic or therapeutic manner.
  • nicotine if it is not supplied via the respiration, has an inhibitory effect on the development of respiratory tract obstruction followed by the irreversible substance loss, elasticity loss and expansion of the lung tissue, i.e. the negative effects arising from pulmonary emphysema, pulmonary barotrauma and spontaneous pneumothorax.
  • Nicotine also ought to have a prophylactic effect, i.e. the origin of pulmonary emphysema of persons having a risk to be effected by this disease, for instance smokers, which have stopped smoking, may be prevented by the supply of nicotine, however not via the bronchi, respiratory organs.
  • At least one substance based on nicotine and/or a substance produced from said one substance is to be given a broad interpretation and in this definition are included substantially pure nicotine, nicotine compounds, nicotine related compounds, nicotine derivatives, intermediate metabolites of nicotine and/or nicotine compounds, degradation products from nicotine or nicotine compounds with completely or partly identical, similar effects.
  • Nicotine acts via nicotine receptors partly in the vegetative system and partly in the muscles. The nicotine has firstly an irritating (vasoconstrictive) effect on the blood vessels. The vasoconstriction leads to a decongestion of the mucous membrane in the respiratory tracts, which counteracts the obstruction. If nicotine is supplied in significantly higher doses than intended by the present invention, a paralysis (vessel relaxion) arises via the vegetative ganglions and the central nervous system.
  • the nicotine is to be supplied via the blood. It is essential that the nicotine reaches the lungs via the blood and not via the respiration.
  • the positive effect of nicotine to the disease pulmonary emphysema can thus not be obtained if nicotine is supplied via tobacco smoke.
  • nicotine has a positive effect if it is supplied to the blood immediately at the same time as the patient is smoking even if the positive effect in this case will be reduced.
  • the nicotine may be administered via the gastrointestinal tract, transdermally, intravascularly, intranasally or intravaginally.
  • the nicotine may thus be supplied in various manners except via the respiratory tracts and the lungs.
  • the nicotine may be supplied by means of plasters, spray, suppository, pills to be swallowed or in the form of chewable tablets or oral tablets, which are known in connection with smoking cessation.
  • the nicotine may be administered by means of inhalation in such a way that most of the nicotine is taken up by the mucous membranes in the mouth (gastrointestinal tract).
  • said substance based on nicotine and/or substances produced by said one substance are absorbed in a binding agent.
  • a binding agent may permit a slow administration of the active nicotine substance, so-called “slow release”.
  • the use is intended for said individual, which has a congenital bilateral bronchial anomaly. As mentioned initially, the destruction of the lung tissue, due to smoking, may be general without anomaly or due to AAT-deficiency.
  • the risk of serious obstructions in the lungs which leads to pulmonary barotrauma, such as spontaneous pneumothorax and pulmonary emphysema, is substantially higher for smokers having a congenital bilateral bronchial anomaly than for smokers not having such an anomaly.
  • This risk ought to be in the order of 2000-3000 % higher for smokers with, than smokers without bilateral bronchial anomaly.
  • the formed structure of a bilateral bronchial anomaly is associated with a different function, such as ventilation, perfusion, and a high sensibility for external factors, such as smoking.
  • the object is also obtained by a method for prophylactic or therapeutic treatment of obstructive lung diseases of an individual of a human being or an animal, wherein said individual is supplied with a nicotine-based substance.
  • a suitable dosing for obtaining the desired effect may be 1 -100 mg/24h, preferably 5-50 mg/24h, for instance 7mg/24h, 14mg/24h or 21 mg/24h. These doses refer to a medicament with nicotine in substantially pure form.
  • Such a dose may for instance be obtained by means of tablets of the type called "slow release".
  • Such tablets may contain a binding agent permitting a slow release of the active nicotine substance.
  • the tablets are suitably designed in such a way that the patient may take one or two tablets per 24h.
  • the dose may also be obtained by the plasters mentioned above or chewable tablets which also may contain flavouring substances, consistency agents and/or any binding agent having an ability to bind nicotine and permit the release thereof at a suitable speed.
  • the nicotine may be present in a substantially free form in such a binding agent, be chemically bounded to any substance or any nicotine compound or as a nicotine derivative.

Landscapes

  • 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)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne l'utilisation d'au moins une substance à base de nicotine et/ou d'une substance produite à partir de la substance précitée et destinée à la préparation d'un médicament à administrer à une personne ou à un animal afin de neutraliser, de manière prophylactique ou thérapeutique, des maladies pulmonaires obstructives, en particulier l'emphysème pulmonaire. Le médicament est conçu pour être libéré dans le sang et administré par le tube digestif, par voie transdermique, intravasculaire, intranasale ou intravaginale. L'invention concerne également une méthode de traitement prophylactique ou thérapeutique de maladies pulmonaires obstructives chez une personne ou un animal, selon laquelle on administre à cette personne une substance à base de nicotine.
EP00959096A 1999-09-01 2000-09-01 Utilisation d'au moins une substance a base de nicotine et/ou d'une substance produite a partir de la substance precitee et destinee a la preparation d'un medicament et methode de traitement de maladies pulmonaires obstructives Withdrawn EP1207883A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
SE9903085 1999-09-01
SE9903085A SE516807C2 (sv) 1999-09-01 1999-09-01 Användning av åtminstone ett nikotinbaserat ämne och/eller ett ur detta ämne framställt ämne för tillverkning av ett medikament
SE0001075 2000-03-27
SE0001075A SE0001075D0 (sv) 1999-09-01 2000-03-27 Användning av åtminstone ett nikotinbaserat ämne och/eller ett ur detta ämne framställt ämne för tillverkning av ett medikament samt förfarande för behandling av obstruktiva lungsjukdomar
PCT/SE2000/001683 WO2001015697A1 (fr) 1999-09-01 2000-09-01 Utilisation d'au moins une substance a base de nicotine et/ou d'une substance produite a partir de la substance precitee et destinee a la preparation d'un medicament et methode de traitement de maladies pulmonaires obstructives

Publications (1)

Publication Number Publication Date
EP1207883A1 true EP1207883A1 (fr) 2002-05-29

Family

ID=26655041

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00959096A Withdrawn EP1207883A1 (fr) 1999-09-01 2000-09-01 Utilisation d'au moins une substance a base de nicotine et/ou d'une substance produite a partir de la substance precitee et destinee a la preparation d'un medicament et methode de traitement de maladies pulmonaires obstructives

Country Status (5)

Country Link
EP (1) EP1207883A1 (fr)
AU (1) AU7047700A (fr)
CA (1) CA2382567A1 (fr)
SE (1) SE0001075D0 (fr)
WO (1) WO2001015697A1 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2341952A1 (fr) 2001-03-23 2002-09-23 Universite Laval Agonistes du recepteur de la nicotine pour le traitement des maladies pulmonaires inflammatoires
US8557804B2 (en) 2002-03-25 2013-10-15 Universite Laval Nicotinic receptor agonists for the treatment of inflammatory diseases
US8039459B2 (en) 2004-07-15 2011-10-18 Universite Laval Nicotinic receptor agonists for the treatment of inflammatory diseases
CA2573977C (fr) * 2004-07-15 2012-04-10 Universite Laval Agonistes du recepteur de nicotine pour le traitement de maladies inflammatoires

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1014981A1 (fr) * 1997-02-07 2000-07-05 Synapse Pharmaceuticals International, Inc. Composition pharmaceutique contenant de l'oxime, pour le traitement de dysfonctionnement synaptique

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0115697A1 *

Also Published As

Publication number Publication date
SE0001075D0 (sv) 2000-03-27
WO2001015697A8 (fr) 2002-01-03
WO2001015697A1 (fr) 2001-03-08
CA2382567A1 (fr) 2001-03-08
AU7047700A (en) 2001-03-26

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