Methods of food intake management

Abstract

Methods for regulating food intake in a human subject; for improving a compliance of a human subject to caloric restriction; and for reducing a desire of a human subject to consume fats, utilizing H1-receptor agonists that have a pharmacological half-life that allows an efficient treatment regime thereof are disclosed. The methods can be efficiently used for treating conditions such as overeating, overweight, obesity, binge eating disorder, night eating syndrome, obsessive eating, compulsive eating and bulimia, as well as conditions associated with metabolic derangement such as dyslipidemia.

1 . A method of treating a condition associated with adverse imbalance of a level of a metabolite in a human subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an H 1  agonist, said metabolite being selected from the group consisting of total cholesterol, high density lipoprotein-cholesterol, low-density lipoprotein-cholesterol and a triglyceride.  
     
     
         2 . The method of  claim 1 , wherein said condition is associated with high fat consumption.  
     
     
         3 . The method of  claim 2 , wherein said condition is dyslipidemia.  
     
     
         4 . The method of  claim 2 , wherein said condition is hypercholesterolemia.  
     
     
         5 . The method of  claim 1 , further comprising administering to the subject a therapeutically effective amount of an additional active agent selected from the group consisting of a fibrate, an HMG-CoA reductase inhibitor, a bile acid sequestrant, a cholesterol absorption inhibitor, nicotinic acid, a derivative, analog and metabolite thereof, and any mixture thereof.  
     
     
         6 . The method of  claim 1 , wherein said H 1  agonist is betahistine or a pharmaceutically acceptable salt thereof.  
     
     
         7 . The method of  claim 1 , wherein said H 1  agonist is a betahistine metabolite.  
     
     
         8 . The method of  claim 7 , wherein said betahistine metabolite is 2-(2-aminoethyl)-pyridine.  
     
     
         9 . The method of  claim 6 , wherein said betahistine salt is selected from the group consisting of betahistine dihydrochloride, betahistine mesilate, and betahistine trimebutine maleate.  
     
     
         10 . The method of  claim 1 , wherein said H 1  agonist is a betahistine derivative.  
     
     
         11 . The method of  claim 10 , wherein said betahistine derivative is selected from the group of compounds represented by formula I:  
       
         
           
           
               
               
           
         
         wherein each of R 1 -R 12  is independently selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl.  
       
     
     
         12 . The method of  claim 1 , wherein said therapeutically effective amount ranges from about 2 mg per unit dosage to about 96 mg per unit dosage.  
     
     
         13 . The method of  claim 12 , wherein said therapeutically effective amount ranges from about 10 mg per day to about 50 mg per day.  
     
     
         14 . The method of  claim 1 , wherein said administering is effected from about 1 to about 4 times per day.  
     
     
         15 . The method of  claim 1 , wherein said H 1  agonist forms a part of a pharmaceutical composition, said pharmaceutical composition further comprising a pharmaceutically acceptable carrier.  
     
     
         16 . A method of reducing total cholesterol level in a human subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an H 1  agonist.  
     
     
         17 . The method of  claim 16 , wherein said H 1  agonist is betahistine or a pharmaceutically acceptable salt thereof.  
     
     
         18 . The method of  claim 16 , wherein said H 1  agonist is a betahistine metabolite.  
     
     
         19 . The method of  claim 18 , wherein said betahistine metabolite is 2-(2-aminoethyl)-pyridine.  
     
     
         20 . The method of  claim 17 , wherein said betahistine salt is selected from the group consisting of betahistine dihydrochloride, betahistine mesilate, and betahistine trimebutine maleate.  
     
     
         21 . The method of  claim 16 , wherein said H 1  agonist is a betahistine derivative.  
     
     
         22 . The method of  claim 21 , wherein said betahistine derivative is selected from the group of compounds represented by formula I:  
       
         
           
           
               
               
           
         
         wherein each of R 1 -R 12  is independently selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl.  
       
     
     
         23 . The method of  claim 16 , wherein said H 1  agonist forms a part of a pharmaceutical composition, said pharmaceutical composition further comprising a pharmaceutically acceptable carrier.  
     
     
         24 . A method of reducing low-density lipoprotein cholesterol and increasing high-density lipoprotein cholesterol levels in a human subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an H 1  agonist.  
     
     
         25 . The method of  claim 24 , wherein said H 1  agonist is betahistine or a pharmaceutically acceptable salt thereof.  
     
     
         26 . The method of  claim 24 , wherein said H 1  agonist is a betahistine metabolite.  
     
     
         27 . The method of  claim 26 , wherein said betahistine metabolite is 2-(2-aminoethyl)-pyridine.  
     
     
         28 . The method of  claim 25 , wherein said betahistine salt is selected from the group consisting of betahistine dihydrochloride, betahistine mesilate, and betahistine trimebutine maleate.  
     
     
         29 . The method of  claim 24 , wherein said H 1  agonist is a betahistine derivative.  
     
     
         30 . The method of  claim 29 , wherein said betahistine derivative is selected from the group of compounds represented by formula I:  
       
         
           
           
               
               
           
         
         wherein each of R 1 -R 12  is independently selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl.  
       
     
     
         31 . The method of  claim 24 , wherein said H 1  agonist forms a part of a pharmaceutical composition, said pharmaceutical composition further comprising a pharmaceutically acceptable carrier.  
     
     
         32 . A method of reducing triglyceride level in a human subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an H 1  agonist.  
     
     
         33 . The method of  claim 32 , wherein said H 1  agonist is betahistine or a pharmaceutically acceptable salt thereof.  
     
     
         34 . The method of  claim 32 , wherein said H 1  agonist is a betahistine metabolite.  
     
     
         35 . The method of  claim 34 , wherein said betahistine metabolite is 2-(2-aminoethyl)-pyridine.  
     
     
         36 . The method of  claim 33 , wherein said betahistine salt is selected from the group consisting of betahistine dihydrochloride, betahistine mesilate, and betahistine trimebutine maleate.  
     
     
         37 . The method of  claim 32 , wherein said H 1  agonist is a betahistine derivative.  
     
     
         38 . The method of  claim 37 , wherein said betahistine derivative is selected from the group of compounds represented by formula I:  
       
         
           
           
               
               
           
         
         wherein each of R 1 -R 12  is independently selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl.  
       
     
     
         39 . The method of  claim 32 , wherein said H 1  agonist forms a part of a pharmaceutical composition, said pharmaceutical composition further comprising a pharmaceutically acceptable carrier.