Therapeutic agent

Abstract

The use of (+)-sibutramine in the treatment of depression, obesity, Parkinson's disease, cerebral function disorders and diabetes is described.

1 . A method of treating depression in a human which comprises administering to a human in need of antidepressant therapy, an amount of (+)-sibutramine, or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate depression.  
     
     
         2 . A method of treating depression in a human according to  Claim 1  in which said amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, is sufficient to alleviate depression but insufficient to cause adverse effects associated with the administration of racemic sibutramine.  
     
     
         3 . The method of claims  1  or  2  wherein (+)-sibutramine is administered by intravenous infusion, transdermal delivery, or orally as a tablet or a capsule.  
     
     
         4 . The method of  claim 3  wherein the amount administered is from about 1 mg to about 60 mg per day.  
     
     
         5 . The method of  claim 4  wherein the amount administered is from about 2 mg to about 50 mg per day.  
     
     
         6 . The method of  claim 5  wherein the amount administered is from about 5 mg to about 45 mg per day.  
     
     
         7 . The method of  claim 3  wherein the amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof is greater than approximately 90% by weight of the total amount of sibutramine.  
     
     
         8 . The method of  claim 3  wherein the (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, is administered together with a pharmaceutically acceptable carrier.  
     
     
         9 . The method according to  claim 3  wherein (+)-sibutramine is administered as a hydrochloride salt.  
     
     
         10 . A composition for the treatment of depression in a human which comprises an amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate depression.  
     
     
         11 . A composition for the treatment of depression in a human according to  claim 10  wherein said amount of (+)-sibutramine, or a pharmaceutically acceptable salt thereof, is sufficient to treat depression but insufficient to cause adverse effects-associated with the administration of racemic sibutramine.  
     
     
         12 . A composition according to  claim 10  or  11  wherein said amount is from about 1 mg to about 60 mg.  
     
     
         13 . A composition according to claims  10  or  11  wherein (+)-sibutramine is in the form of hydrochloride salt.  
     
     
         14 . A composition according to  claim 12  wherein said composition is adapted for oral administration.  
     
     
         15 . A composition according to  claim 12  adapted for intravenous delivery.  
     
     
         16 . A composition according to  claim 12  adapted for use in a transdermal patch.  
     
     
         17 . The composition according to  claim 12  which comprises (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, and a pharmaceutically acceptable carrier.  
     
     
         18 . A method for treating obesity or weight gain in a human which comprises administering to a human in need of a reduction in weight, an amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate obesity or weight gain.  
     
     
         19 . A method for treating obesity or weight gain in a human according to  claim 18  wherein said amount is sufficient to alleviate obesity or weight gain but insufficient to cause the adverse effects associated with administration of racemic sibutramine.  
     
     
         20 . The method of claims  18  or  19  wherein (+)-sibutramine is administered by intravenous infusion, transdermal delivery, or orally as a tablet or a capsule.  
     
     
         21 . The method of  claim 20  wherein the amount administered is from about 1 mg to about 60 mg per day.  
     
     
         22 . The method of  claim 21  wherein the amount administered is from about 2 mg to about 50 mg per day.  
     
     
         23 . The method of  claim 22  wherein the amount administered is from about 5 mg to about 45 mg per day.  
     
     
         24 . The method of  claim 23  wherein the amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof is greater than approximately 90% by weight of the total amount of sibutramine.  
     
     
         25 . The method of  claim 20  wherein the (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, is administered together with a pharmaceutically acceptable carrier.  
     
     
         26 . The method according to claims  18  or  19  wherein (+)-sibutramine is administered as a hydrochloride salt.  
     
     
         27 . A composition for treating obesity or weight gain in a human which comprises an amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate obesity or weight gain.  
     
     
         28 . A composition for treating weight disorders in a human according to  claim 27  wherein said amount is sufficient to alleviate obesity or weight gain in a human but insufficient to cause adverse effects associated with administration of racemic sibutramine.  
     
     
         29 . A composition according to claims  27  or  28  wherein the amount is about 1 mg to about 60 mg.  
     
     
         30 . A composition according to  claim 27  or wherein (+)-sibutramine is in the form of hydrochloride salt.  
     
     
         31 . A composition according to  claim 29  wherein said composition is adapted for oral administration.  
     
     
         32 . A composition according to  claim 29  adapted for intravenous delivery.  
     
     
         33 . A composition according to  claim 29  adapted for use in transdermal patch.  
     
     
         34 . The composition according to  claim 29  which comprises (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, and a pharmaceutically acceptable carrier.  
     
     
         35 . A method of treating disorders ameliorated by inhibition of neuronal monoamine reuptake in a human which comprises administering to a human in need of such treatment an amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate said disorders.  
     
     
         36 . A method of treating disorders ameliorated by inhibition of neuronal monoamine reuptake in a human according to  claim 35  in which said amount is sufficcient to alleviate said disorders but insufficient to cause adverse effects associated with administration of racemic sibutramine.  
     
     
         37 . A method of treating disorders ameliorated by inhibition of neuronal monoamine reuptake in a human according to claims  35  or  36  wherein said monoamine is dopamine.  
     
     
         38 . A method of treating disorders ameliorated by inhibition of neuronal monoamine reuptake in a human according to claims  35  or  36  wherein said disorder is Parkinson's disease.  
     
     
         39 . The method of claims  35  or  36  wherein (+)-sibutramine is administered by intravenous infusion, transdermal delivery, or orally as a tablet or a capsule.  
     
     
         40 . The method of  claim 39  wherein the amount administered is from about 1 mg to about 60 mg per day.  
     
     
         41 . The method of  claim 40  wherein the amount administered is from about 2 mg to about 50 mg per day.  
     
     
         42 . The method of  claim 41  wherein the amount administered is from about 5 mg to about 45 mg per day.  
     
     
         43 . The method of  claim 39  wherein the amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof is greater than approximately 90% by weight of the total amount of sibutramine.  
     
     
         44 . The method of  claim 39  wherein (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer is administered together with a pharmaceutically acceptable carrier.  
     
     
         45 . The method according to  claim 39  wherein (+)-sibutramine is administered as a hydrochloride salt.  
     
     
         46 . A composition for the treatment of disorders ameliorated by inhibition of neuronal monoamine reuptake in a human which comprises an amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate said disorders.  
     
     
         47 . A composition for the treatment of disorders ameliorated by inhibition of neuronal monoamine reuptake in a human according to  claim 46  wherein said amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, is sufficient to treat said disorders but insufficient to cause adverse effects associated with the administration of racemic sibutramine.  
     
     
         48 . A composition according to claims  46  or  47  wherein the amount is about 1 mg to about 60 mg.  
     
     
         49 . A composition according to claims  46  or  47  wherein (+)-sibutramine is in the form of a hydrochloride salt.  
     
     
         50 . A composition according to  claim 48  wherein said composition is adapted for oral administration.  
     
     
         51 . A composition according to  claim 48  adapted for intravenous delivery.  
     
     
         52 . A composition according to  claim 48  adapted for use in a transdermal patch.  
     
     
         53 . The composition according to  claim 48  which comprises (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, and a pharmaceutically acceptable carrier.  
     
     
         54 . A method for treating cerebral function disorders in humans which comprises administering to a human an amount of (+)-sibutramine, or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate cerebral function disorders.  
     
     
         55 . A method for treating cerebral function disorders in a human according to  claim 54  wherein said amount of (+)-sibutramine or a pharmaceutically acceptable thereof, substantially free of its (−)-stereoisomer, is sufficient to alleviate cerebral function disorders but insufficient to cause adverse effects associated with administration of racemic sibutramine.  
     
     
         56 . A method for treating cerebral function disorders in a human according to claims  54  or  55  wherein said disorder is caused by a cerebrovascular disease.  
     
     
         57 . A method for treating cerebral function disorders in a human according to claims  54  or  55  wherein said cerebral function disorder is selected from the group consisting of senile dementia, Alzheimer's type dementia, memory loss and amnesia/amnestic syndrome.  
     
     
         58 . A method for treating cerebral function disorders in a human according to  claim 56  wherein said cerebrovascular disease is selected from the group consisting of cerebral infarction, cerebral bleeding, cerebral arteriosclerosis, cerebral venous thrombosis and head injuries  
     
     
         59 . The method of claims  54  or  55  wherein (+)-sibutramine is adminstered by intravenous infusion, transdermal delivery, or orally as a tablet or a capsule.  
     
     
         60 . The method of  claim 59  wherein the amount administered is from about 1 mg to about 60 mg per day.  
     
     
         61 . The method of  claim 60  wherein the amount administered is from about 2 mg to about 50 mg per day.  
     
     
         62 . The method of  claim 61  wherein the amount administered is from about 5 mg to about 45 mg per day.  
     
     
         63 . The method of  claim 59  wherein the amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof is greater than approximately 90% by weight of the total amount of sibutramine.  
     
     
         64 . The method of  claim 59  wherein the (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, is administered together with a pharmaceutically acceptable carrier.  
     
     
         65 . The method according to  claim 59  wherein (+)-sibutramine is administered as a hydrochloride salt.  
     
     
         66 . A composition for treating cerebral function disorders, which comprises an amount of (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, said amount being sufficient to alleviate cerebral function disorders.  
     
     
         67 . A composition for treating cerebral function disorders according to  claim 66  wherein said amount of (+)-sibutramine or a pharmaceutically salt thereof, substantially free of its (−)-stereoisomer, is sufficient to treat cerebral function disorders but insufficient to cause the adverse effects associated with the administration of racemic sibutramine.  
     
     
         68 . A composition according to claims  66  or  67  wherein the amount is about 1 mg to about 60 mg.  
     
     
         69 . A composition according to claims  66  or  67  wherein (+)-sibutramine is in the form of a hydrochloride salt.  
     
     
         70 . A composition according to  claim 68  wherein said composition is adapted for oral administration.  
     
     
         71 . A composition according to  claim 68  adapted for intravenous delivery.  
     
     
         72 . A composition according to  claim 68  adapted for use in a transdermal patch.  
     
     
         73 . The composition according to  claim 68  which comprises (+)-sibutramine or a pharmaceutically acceptable salt thereof, substantially free of its (−)-stereoisomer, and a pharmaceutically acceptable carrier.