Use of hydroxyrisperidone for the manufacture of a medicament for the treatment and prevention of psychoses, emesis and symptoms of withdrawal from alcohol and nicotine

Abstract

Methods and compositions utilizing compounds represented by Formula III, or a pharmaceutically acceptable salt thereof, for the treatment and prevention of psychoses in humans are disclosed. Compounds of the present invention exhibit fewer side effects than risperidone, a lessened liability toward drug-drug interactions than risperidone and a more predictable dosing regimen than risperidone. Compounds of the invention are also useful for the treatment and prevention of emesis and withdrawal syndromes.

What is claimed is:  
     
         1 . A method of treating psychoses while avoiding the concomitant liability of side effects associated with risperidone which comprises administering to a human an amount of a compound represented by Formula III,  
       
         
           
           
               
               
           
         
       
       wherein R is chosen from —OH, —P(O)(OH) 2  and —SO 3 H, or a pharmaceutically acceptable salt thereof sufficient to treat psychoses but insufficient to cause said side effects.  
     
     
         2 . A method of providing a predictable dosing regimen in the treatment of psychoses which comprises administering to a human a therapeutically effective amount of a compound represented by Formula III,  
       
         
           
           
               
               
           
         
       
       wherein R is chosen from —OH, —P(O)(OH) 2  and —SO 3 H, or a pharmaceutically acceptable salt thereof.  
     
     
         3 . A method of reducing potential for drug-drug interactions in the treatment of psychoses which comprises administering to a human a therapeutically effective amount of a compound represented by Formula III,  
       
         
           
           
               
               
           
         
       
       wherein R is chosen from —OH, —P(O)(OH) 2  and —SO 3 H, or a pharmaceutically acceptable salt thereof.  
     
     
         4 . A method of suppressing emesis which comprises administering to a human a therapeutically effective amount of a compound represented by Formula III,  
       
         
           
           
               
               
           
         
       
       wherein R is chosen from —OH, —P(O)(OH) 2 —SO 3 H, or a pharmaceutically acceptable salt thereof.  
     
     
         5 . A method of treating withdrawal from alcohol, nicotine or narcotic drugs which comprises administering to a human a therapeutically effective amount of a compound represented by Formula III,  
       
         
           
           
               
               
           
         
       
       wherein R is chosen from —OH, —P(O)(OH) 2  and —SO 3 H, or a pharmaceutically acceptable salt thereof.  
     
     
         6 . The method of any of claims  1 - 5  wherein R is —OH.  
     
     
         7 . The method of  claim 6  wherein the compound is administered orally.  
     
     
         8 . The method of  claim 7  wherein the amount of the compound, or a pharmaceutically acceptable salt thereof administered is from about 1 mg to about 20 mg per day.  
     
     
         9 . The method of any of claims  1 - 5  wherein R is —P(O)(OH) 2 .  
     
     
         10 . The method of  claim 9  wherein the pharmaceutically acceptable salt thereof is the N-methylglucamine salt.  
     
     
         11 . The method of  claim 10  wherein the compound is administered intravenously.  
     
     
         12 . A pharmaceutical composition for intravenous administration comprising the N-methylglucamine salt of a compound represented by Formula III′,  
       
         
           
           
               
               
           
         
       
       and a pharmaceutically acceptable carrier.