WO2001015697A1 - Use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament, and a method for treatment of obstructive lung diseases - Google Patents
Use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament, and a method for treatment of obstructive lung diseases Download PDFInfo
- Publication number
- WO2001015697A1 WO2001015697A1 PCT/SE2000/001683 SE0001683W WO0115697A1 WO 2001015697 A1 WO2001015697 A1 WO 2001015697A1 SE 0001683 W SE0001683 W SE 0001683W WO 0115697 A1 WO0115697 A1 WO 0115697A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- nicotine
- medicament
- substance
- intended
- use according
- Prior art date
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
- A61K31/465—Nicotine; 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.
Abstract
Description
Claims
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU70477/00A AU7047700A (en) | 1999-09-01 | 2000-09-01 | Use of at least one substance based on nicotine and/or a substance produced fromsaid one substance for the manufacture of a medicament, and a method for treatm ent of obstructive lung diseases |
EP00959096A EP1207883A1 (en) | 1999-09-01 | 2000-09-01 | Use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament, and a method for treatment of obstructive lung diseases |
CA002382567A CA2382567A1 (en) | 1999-09-01 | 2000-09-01 | Use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament, and a method for treatment of obstructive lung disease |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE9903085A SE516807C2 (en) | 1999-09-01 | 1999-09-01 | Use of nicotine based substances to treat obstructive lung diseases |
SE9903085-0 | 1999-09-01 | ||
SE0001075A SE0001075D0 (en) | 1999-09-01 | 2000-03-27 | Use of at least one nicotine-based substance and / or substance derived from this substance for the manufacture of a medicament and method for the treatment of obstructive pulmonary diseases |
SE0001075-1 | 2000-03-27 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2001015697A1 true WO2001015697A1 (en) | 2001-03-08 |
WO2001015697A8 WO2001015697A8 (en) | 2002-01-03 |
Family
ID=26655041
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/SE2000/001683 WO2001015697A1 (en) | 1999-09-01 | 2000-09-01 | Use of at least one substance based on nicotine and/or a substance produced from said one substance for the manufacture of a medicament, and a method for treatment of obstructive lung diseases |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP1207883A1 (en) |
AU (1) | AU7047700A (en) |
CA (1) | CA2382567A1 (en) |
SE (1) | SE0001075D0 (en) |
WO (1) | WO2001015697A1 (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002076434A2 (en) * | 2001-03-23 | 2002-10-03 | 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 |
US8557804B2 (en) | 2002-03-25 | 2013-10-15 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2005262174C1 (en) * | 2004-07-15 | 2010-05-06 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1998034615A1 (en) * | 1997-02-07 | 1998-08-13 | Synapse Pharmaceuticals International, Inc. | Pharmaceutical composition for treatment of synaptic dysfunction comprising an oxime |
-
2000
- 2000-03-27 SE SE0001075A patent/SE0001075D0/en unknown
- 2000-09-01 EP EP00959096A patent/EP1207883A1/en not_active Withdrawn
- 2000-09-01 CA CA002382567A patent/CA2382567A1/en not_active Abandoned
- 2000-09-01 AU AU70477/00A patent/AU7047700A/en not_active Abandoned
- 2000-09-01 WO PCT/SE2000/001683 patent/WO2001015697A1/en not_active Application Discontinuation
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1998034615A1 (en) * | 1997-02-07 | 1998-08-13 | Synapse Pharmaceuticals International, Inc. | Pharmaceutical composition for treatment of synaptic dysfunction comprising an oxime |
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002076434A2 (en) * | 2001-03-23 | 2002-10-03 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
WO2002076434A3 (en) * | 2001-03-23 | 2003-07-17 | Univ Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
AU2002249023B2 (en) * | 2001-03-23 | 2006-02-02 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
US7601720B2 (en) | 2001-03-23 | 2009-10-13 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
US8377936B2 (en) | 2001-03-23 | 2013-02-19 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
US8551983B2 (en) | 2002-03-25 | 2013-10-08 | Universite Laval | Nicotinic receptor agonists for the treatment of inflammatory diseases |
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 |
Also Published As
Publication number | Publication date |
---|---|
WO2001015697A8 (en) | 2002-01-03 |
AU7047700A (en) | 2001-03-26 |
CA2382567A1 (en) | 2001-03-08 |
SE0001075D0 (en) | 2000-03-27 |
EP1207883A1 (en) | 2002-05-29 |
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