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
• • 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
• • 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
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/34—Tobacco-abuse

Definitions

• This invention relates to a method to aid smoking cessation. More
• the method relates to treating a patient who wishes to stop smoking
• the method relates to preventing weight
• the present invention relates to compositions containing agents which
• compositions in order to take advantage of a noradrenergic agent's effect on
• the present invention more
• sibutramine is administered to individuals who are attempting to quit smoking in a quantity sufficient to ameliorate or prevent the mood disturbances and/or to suppress the weight gain frequently evident in individuals trying to give up smoking, as well as to reduce recidivism.
• sibutramine is administered in conjunction with the patient's participation in a behavior modification program.
• administration of sibutramine is carried out in conjunction with the use of a nicotine patch and the patient's participation in a behavior modification program.
• Administration of a noradrenergic compound according to the method of the present invention can be of great benefit to persons who experience withdrawal symptoms and increased appetite associated with giving up smoking because the compounds act to alleviate or prevent such adverse symptoms. While the biochemistry of nicotine habituation and of cigarette withdrawal is not completely understood, a theoretical basis for treatment has been established. The abstinence syndrome produced by withdrawal or addictive substances is associated with an abrupt increase in sympathetic outflow from the brain stem. In particular, noradrenergic neurones in the locus coeruleus (containing half the noradrenergic neurons in the mammalian brain) show a marked increase in firing rate during withdrawal (Amaral and Sinnamon, 1978).
• the present invention relates to a method of aiding
• R 2 are independently H or methyl, is administered in conjunction with a
• a preferred compound of formula I is N,N-dimethy 1- 1 - [ 1 -(4-)
• a particularly preferred form of this compound is N,N-dimethyl-l-[l-(4-)
• the present invention includes the use of the
• the enantiomers may be
• reaction of one enantiomer with an enantiomer-specific reagent for example
• Preferred compounds of formula I are N,N-dimethy 1- 1 - [ 1 -(4-)
• the compound of formula I may be administered in any of the known
• the dosage of the compound to be administered will be in the range 0. 1 to 50 mg,
• Oral dosage forms are the preferred compositions for use in the present invention and these are the known pharmaceutical forms or such administration, for example tablets, capsules, granules, syrups and aqueous or oil suspensions.
• the excipients used in the preparation of these compositions are the excipients known in the pharmacist's art.
• Tablets may be prepared from a mixture of the active compound with fillers, for example calcium phosphate; disintegrating agents, for example maize starch; lubricating agents, for example magnesium stearate; binders, for example microcrystalline cellulose or polyvinylpyrrolidone and other optional ingredients known in the art to permit tableting the mixture by known methods.
• the tablets may, if desired, be coated using known methods and excipients which may include enteric coating using for example hydroxypropylmethylcellulose phthalate.
• the tablets may be formulated in a manner known to those skilled in the
• Such tablets may, if desired, be provided with enteric coatings by known methods,
• capsules for example by the use of cellulose acetate phthalate.
• capsules for example by the use of cellulose acetate phthalate.
• hard or soft gelatin capsules containing the active compound with or
• the tablets and capsules may conveniently each contain 1 to 50
• dosage forms for oral administration include, for example, aqueous
• a non-toxic suspending agent such as sodium carboxy-methycellulose
• the active compound may be formulated
• the granules may be ingested
• the granules may contain disintegrants, eg an
• effervescent couple formed from an acid and a carbonate or bicarbonate salt to
• the therapeutically active compounds of formula I may be formulated into
• cocoa butter or polyethylene glycol bases cocoa butter or polyethylene glycol bases.
• Dosage forms for topical administration may comprise a matrix in which
• the pharmacologically active compounds of the present invention are dispersed so
• a suitable transdermal composition may be prepared
• a topical vehicle such as a
• mineral oil petrolatum and/or a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax, e.g. paraffin wax or beeswax, together with a wax,
• transdermal accelerant such as dimethyl sulphoxide or propylene glycol.
• the active compounds may be dispersed in a pharmaceutically
• topical formulation is intended to be on the skin.
• the therapeutically active compound of formula I may be formulated into
• composition which is dispersed as an aerosol into the patients oral or nasal
• Such aerosols may be administered from a pump pack or from a
• pressurized pack containing a volatile propellant containing a volatile propellant
• the present invention may also be administered by continuous infusion either from
• an external source for example by intravenous infusion or from a source of the
• containing the compound to be infused which is continuously released for example by osmosis and implants which may be (a) liquid such as an oily
• suspension of the compound to be infused for example in the form of a very
• waxy material for the compound or a series of several bodies each containing part
• present invention in the form of particles of very small size, for example as
• program may also be offered to the patient who is attempting to quit smoking.
• the programs include self-help programs and programs that are taught by others
• the invention will be used by patients who desire to quit smoking and
• Sibutramine will be continued at this daily dose until six months after the planned
• sibutramine This program may consist of individual counseling sessions or
• the invention will be used by patients who desire to quit smoking and
• This program may consist of individual counseling sessions or group counseling sessions. Beginning on the planned quit date, a
• the invention was used by patients who desired to quit smoking and who have
• the invention was used by patients who desire to quit smoking and who have
• abstinence e.g. abstinence form alcohol, other smoker in the household

Landscapes

• Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Addiction (AREA)
• Epidemiology (AREA)
• Neurology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Neurosurgery (AREA)
• Biomedical Technology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Psychiatry (AREA)
• Emergency Medicine (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Priority Applications (12)

Applications Claiming Priority (4)

Publications (1)

Family

ID=26814491

Family Applications (1)

Country Status (19)

Cited By (1)

Citations (2)

• 2000
  • 2000-01-19 EP EP00905659A patent/EP1150672A1/en not_active Withdrawn
  • 2000-01-19 IL IL14439000A patent/IL144390A0/xx unknown
  • 2000-01-19 CZ CZ20012662A patent/CZ20012662A3/cs unknown
  • 2000-01-19 PL PL00349002A patent/PL349002A1/xx not_active Application Discontinuation
  • 2000-01-19 BR BR0007633-3A patent/BR0007633A/pt not_active Application Discontinuation
  • 2000-01-19 TR TR2001/02999T patent/TR200102999T2/xx unknown
  • 2000-01-19 MX MXPA01007388A patent/MXPA01007388A/es unknown
  • 2000-01-19 JP JP2000594459A patent/JP2002535273A/ja not_active Withdrawn
  • 2000-01-19 HU HU0105431A patent/HUP0105431A3/hu unknown
  • 2000-01-19 ID IDW00200101605A patent/ID30432A/id unknown
  • 2000-01-19 SK SK1031-2001A patent/SK10312001A3/sk unknown
  • 2000-01-19 AU AU27308/00A patent/AU2730800A/en not_active Abandoned
  • 2000-01-19 CA CA002359564A patent/CA2359564A1/en not_active Abandoned
  • 2000-01-19 KR KR1020017009174A patent/KR20010111254A/ko not_active Application Discontinuation
  • 2000-01-19 CN CN00804941A patent/CN1355696A/zh active Pending
  • 2000-01-19 NZ NZ513638A patent/NZ513638A/xx not_active Application Discontinuation
  • 2000-01-19 TR TR2001/02786T patent/TR200102786T2/xx unknown
  • 2000-01-19 WO PCT/US2000/001217 patent/WO2000043002A1/en not_active Application Discontinuation
• 2001
  • 2001-07-19 NO NO20013575A patent/NO20013575L/no not_active Application Discontinuation
  • 2001-08-15 BG BG105820A patent/BG105820A/xx unknown

Patent Citations (2)

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