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
  • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
  • A61K31/415—1,2-Diazoles
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P11/00—Drugs for disorders of the respiratory system
  • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P19/00—Drugs for skeletal disorders
  • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
• • 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
  • A61P25/20—Hypnotics; Sedatives
• • 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]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/02—Nutrients, e.g. vitamins, minerals
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• the present invention relates to a new use for 5HT 3 receptor antagonists.
• CFS chronic fatigue syndrome
• chronic IV fatigue syndrome was defined as a diagnostic entity in the late 1980s and has been the subject of numerous studies and publications since then.
• CFS chronic mental and physical fatigue
• the object of the present invention is therefore to provide compounds which are suitable for the preparation of medicaments for the treatment of CFS.
• the present invention is based on the finding that the use of antidepressants which enhance the action of serotonin is not appropriate in CFS, as is also supported by the cited study relating to fluoxetine.
• this is a departure from the usual treatment methods, which have essentially focused on the presence of depressive states. It is therefore proposed to use substances that reduce the effect of serotonin, which are channeled through the subset of the so-called 5HT 3 receptors.
• the pharmacologically known class of highly specific 5HT 3 receptor antagonists which are used, for example, in the treatment of emesis in chemotherapy for cancer, is suitable for this purpose.
• the 5HT 3 receptor antagonists used are alosetron, tropisetron, ondansetron, granisetron, bemesetron or combinations of at least two of the above, very selectively active substances. It is preferred that the amount of active ingredient contained in a dose unit is 2 to 10 mg, an amount of active ingredient of 5 to 8 mg in a dose unit being particularly preferred.
• a daily dose generally comprises an amount of active ingredient from 2 to 20 mg, particularly preferably an amount of active ingredient from 5 to 16 mg. If necessary, however, the person skilled in the art is also familiar with varying the amount of active ingredient in a dose unit or the amount of the daily dose according to the requirements.
• the substances used according to the invention for the production of the medicament are preferably oral or intravenous
• Sore throat non-purulent pharyngitis
• the group of patients treated with tropisetron received the active ingredient in the form of a capsule with an active ingredient amount of 5 mg / dose unit, the daily dose also being 5 mg.
• the second group of patients received the active substance ondansetron in tablet form, one dose unit containing 8 mg of active substance and the daily dose consisting of two dose units twice, i.e. 16 mg daily.
• the 5HT 3 receptor antagonists were administered over a period of 15 days. During the study period, patients were tested for the following "listed parameters:
• Analog scales were recorded, which documented the extent of the abnormal fatigue / exhaustion and the reduction in performance.
• the subjectively invented state with regard to fatigue / fatigue or performance was marked on a one-dimensional scale, which covers a range from 0 to 100, where 0 stands for normal fatigue / fatigue or performance and 100 for the greatest fatigue / fatigue or for 100% reduction in performance.

Landscapes

• Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• General Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Rheumatology (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Epidemiology (AREA)
• Pulmonology (AREA)
• Neurology (AREA)
• Physical Education & Sports Medicine (AREA)
• Neurosurgery (AREA)
• Biomedical Technology (AREA)
• Hematology (AREA)
• Obesity (AREA)
• Nutrition Science (AREA)
• Pain & Pain Management (AREA)
• Otolaryngology (AREA)
• Diabetes (AREA)
• Immunology (AREA)
• Anesthesiology (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)
• Nitrogen Condensed Heterocyclic Rings (AREA)

Applications Claiming Priority (3)

Publications (1)

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Family Applications (1)

Country Status (9)

Families Citing this family (4)

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• 1999
  • 1999-12-22 BR BR9916495-7A patent/BR9916495A/pt not_active IP Right Cessation
  • 1999-12-22 JP JP2000589184A patent/JP2002532549A/ja not_active Withdrawn
  • 1999-12-22 CA CA002356246A patent/CA2356246A1/en not_active Abandoned
  • 1999-12-22 MX MXPA01006319A patent/MXPA01006319A/es unknown
  • 1999-12-22 AU AU24285/00A patent/AU759250B2/en not_active Ceased
  • 1999-12-22 EP EP99967889A patent/EP1140076A1/de not_active Withdrawn
  • 1999-12-22 CN CNB998158445A patent/CN1161118C/zh not_active Expired - Fee Related
  • 1999-12-22 US US09/868,972 patent/US6740672B1/en not_active Expired - Fee Related
  • 1999-12-22 WO PCT/DE1999/004071 patent/WO2000037073A1/de not_active Application Discontinuation
• 2004
  • 2004-04-30 US US10/837,370 patent/US20040204467A1/en not_active Abandoned

Non-Patent Citations (1)

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