Use of substances with oxytocin activity against climacteric disorders

Abstract

The present invention relates to the use of substances with oxytocin activity against climacteric disorders or similar symptoms due to dysfunction in the ovaries. It also relates to a pharmacetucial composition comprising at least one substance with oxytocin activity against climacteric disorders.

1 . Use of a substance with oxytocin activity for the preparation of a pharmaceutical composition against climacteric disorders, such as weight changes, mood swings, hot flushes, dry and ulcerous membranes, fissures, and bone loss.  
     
     
         2 . Use according to  claim 1 , characterised in that the substance is selected from the group consisting of the following compounds:  
       
         
           
                 
                 
                 
               
                     
                 
                   {overscore (|     )}S-R-S{overscore (      |)} 
                     
                     
                 
                   X 1 -X 2 -X 3 -X 4 -Asn- Cys-X 5 -X 6 -X 7 -NH 2   
                   (SEQ ID NO: 2) 
                 
                     
                 
             
                
                
                
                
               
            
           
         
       
       wherein 
 X 1  is selected from the group consisting of Cys and nothing,  
 X 2  is selected from the group consisting of Tyr, Phe, and nothing,  
 X 3  is selected from the group consisting of Ile, Val, Hoph, Phe, Cha, and nothing,  
 X 4  is selected from the group consisting of Gln, Ser, Thr, Cit, Arg, and Daba,  
 X 5  is selected from the group consisting of Pro, and nothing.  
 X 6  is selected from the group consisting of Ile, Leu, nothing, Val, Hos, Daba, Thr, and Cit,  
 X 7  is selected from the group consisting of Gly, nothing, and Ala,  
 R is a chemical bond or, in the case neither of X 1 , X 2 , X 3  and X 4  represents Cys, represents nothing.  
 
     
     
         3 . Use according to claim  1 - 2 , characterised in that the substance is selected from the group consisting of the following compounds: SEQ ID NO: 1, SEQ D NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO: 11, SEQ ID NO: 12, SEQ ID NO: 13, SEQ ID NO: 14, SEQ ID NO: 15, SEQ ID NO: 16, SEQ ID NO: 17, SEQ ID NO: 18, and SEQ ID NO: 19.  
     
     
         4 . Use according to claim  1 - 3 , characterised that the pharmaceutical composition comprises substances that increase the release of oxytocin and/or the number or affinity of oxytocin receptors, such as oestrogen, or drugs having an α 2 -agonistic effect, such as clonidine.  
     
     
         5 . Use according to claim  1 - 4 , characterised in that the substance is administered in amount of 0.01-100 ng/g body weight of the patient.  
     
     
         6 . Use according to claim  1 - 5 , characterised in that the substance is administered in amount of 0.1-10 ng/kg body weight of the patient.  
     
     
         7 . Pharmaceutical composition against climacteric disorders, characterised in that it comprises an effective concentration of at least one substance with oxytocin activity in mixture or otherwise together with at least one pharmaceutically acceptable carrier or excipient, wherein the substance is selected from the group consisting of the following compounds:  
       
         
           
                 
                 
                 
               
                     
                 
                   {overscore (|     )}S-R-S{overscore (      |)} 
                     
                     
                 
                   X 1 -X 2 -X 3 -X 4 -Asn- Cys-X 5 -X 6 -X 7 -NH 2   
                   (SEQ ID NO: 2) 
                 
                     
                 
             
                
                
                
                
               
            
           
         
       
       wherein 
 X 1  is selected from the group consisting of Cys and nothing,  
 X 2  is selected from the group consisting of Tyr, Phe, and nothing,  
 X 3  is selected from the group consisting of Ile, Val, Hoph, Phe, Cha, and nothing,  
 X 4  is selected from the group consisting of Gln, Ser, Thr, Cit, Arg, and Daba,  
 X 5  is selected from the group consisting of Pro, and nothing,  
 X 6  is selected from the group consisting of Ile, Leu, nothing, Val, Hos, Daba, Thr, and Cit,  
 X 7  is selected from the group consisting of Gly, nothing, and Ala,  
 R is B chemical bond or, in the case neither of X 1 , X 2 , X 3  and X 4  represents Cys, represents nothing.  
 
     
     
         8 . Pharmaceutical composition according to  claim 7 , characterised in that the substance is selected from the group consisting of the following compounds: SEQ ID NO: 1, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ED NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO. 11, SEQ ID NO: 12, SEQ ID NO: 13, SEQ ID NO: 14, SEQ ID NO: 15, SEQ ID NO: 16, SEQ ID NO: 17, SEQ ID NO: 18, and SEQ ID NO: 19.  
     
     
         9 . Pharmaceutical composition according to claims  7 - 8 , characterised in that it comprises substrates that increase the release of oxytocin and/or the number or affinity of oxytocin receptors, such as oestrogen, or drugs having an α 2 -agonistic effect, such as clonidine.  
     
     
         10 . Pharmaceutical composition according to claims  7 - 9 , characterised in that the effective concentration is 4-70% by weight, preferably 0.1-50% by weight.