Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-12-16
2000-07-18
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 314406, A61K 314436, A61K 314439
Patent
active
060908297
DESCRIPTION:
BRIEF SUMMARY
This invention provides a method for using 3-(4-hexyloxy-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine, (hereinafter referred as "xanomeline"), for the treatment of excessive aggression.
Excessive agression can be a problem for institutionalized patients and may be associated with violent suicides. Extreme aggressiveness can be harmful to the individual prone to extreme aggressivenes, may be detrimental to relationships and family members interacting with the individual, and may complicate the management of patients or prisoners in the institutional setting.
Studies of animals and human beings suggest that 5-HT serves a critical role in aggression and impulsivity. Several human studies report a correlation between low cerebrospinal fluid 5-HIAA and violent suicides. Therefore, extreme aggression appears to be associated with abnormalities in 5-HT. Goodman and Gillman, The Pharmacololgical Basis of Therapeutics, 257 (9th Ed. McGraw-Hill, New York, 1996).
However, there is a need for new treatments that can manage extreme aggression in a safe and ethical manner. Applicants have discovered that xanomeline can be useful for the treatment of extreme aggression. More specifically, the invention provides a method of treating extreme aggression in a mammal using 3-(4-hexyloxy-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine.
As noted hereinbefore, the compounds employed in the method of the present invention are known. Methods of preparing the compounds, as well as pharmaceutical formulations containing the compounds, are taught by Sauerberg in U.S. Pat. No. 5,043,345 (hereinafter refered to as the "'345 patent") herein incorporated by reference. The '345 patent teaches that xanomeline can be useful for treating Alzheimer's Disease and as stimulants of the cognitive function of the forebrain and hippocampus of mammals. Applicants have discovered that xanomeline can be useful for the treatment of extreme aggression. Xanomeline may address the long felt need for treatments which provide a favorable safety profile and effectively provides relief for the patient or individual suffering from extreme aggression.
The presently claimed invention provides a method for treating extreme aggression, comprising administering an effective amount of a compound of Formula I: ##STR2## or a pharmaceutically acceptable salt or solvate thereof to a patient in need of such treatment.
A preferred embodiment of the present invention is for use in the treatment of Conduct Disorder as characterized by the DSM-IV as catagory 312.8.
An especially preferred embodiment of the present invention is administering the effective amount transdermally using a patch.
The term "effective amount", as used herein, represents an amount of compound necessary to prevent or treat a mammal susceptible to or suffering from excessive aggression following administration to such mammal. The active compound is effective over a wide dosage range. For example, dosages per day will normally fall within the range of about 0.005 to about 500 mg/kg of body weight. In the treatment of adult humans, the range of about 0.05 to about 100 mg/kg, in single or divided doses, is preferred. However, it will be understood that the amount of the compound actually administered will be determined by a physician, in the light of the relevant circumstances including the condition to be treated, the choice of compound to be administered, the age, weight, and response of the individual patient, the severity of the patient's symptoms, and the chosen route of administration, and therefore the above dosage ranges are not intended to limit the scope of the invention in any way. While the present compound may be administered orally to humans susceptible to or suffering from extreme aggression, the compound is particularly well suited to be administered transdermally. When the compound is delivered transdermally, it is preferred that the effective amount is from about 10 mg to about 100 mg per day delivery of base compound. It is especially preferred that such patch de
REFERENCES:
patent: 5041455 (1991-08-01), Sauerberg et al.
patent: 5043345 (1991-08-01), Sauerberg et al.
patent: 5328923 (1994-07-01), Sauerberg et al.
patent: 5328924 (1994-07-01), Sauerberg et al.
patent: 5488056 (1996-01-01), Bodick et al.
patent: 5708014 (1998-01-01), Bodick et al.
Rapaport, et al., Biol. Psychiatry, 29, 658-664 (1991).
Katzung, B.G., Basic & Clinical Pharmacology, (Appleton & Lange, Norwald), 90-94 (1995).
Sauerberg, et al., J. Med. Chem., 35, 2274-2283 (1992).
Bodick Neil C
Bymaster Franklin P
Shannon Harlan E
Eli Lilly and Company
Spivack Phyllis G.
Stemerick David M.
Vorndran-Jones MaCharri
LandOfFree
Method for treating excessive aggression does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Method for treating excessive aggression, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Method for treating excessive aggression will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2037487