N-DESMETHYL-DOXEPIN AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS
Desmethyldoxepin, isomers of desmethyldoxepin, and pharmaceutically acceptable salts and prodrugs of desmethyldoxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.
1 . A method for treating insomnia comprising administering to a patient desmethyldoxepin, a pharmaceutically acceptable salt thereof, or a prodrug thereof other than doxepin in a daily dosage ranging from about 0.01 to about 500 milligrams.
2 . The method of claim 1 , wherein the pharmaceutically acceptable salt of desmethyldoxepin is the hydrochloride salt thereof.
3 . The method of claim 1 , wherein the prodrug of desmethyldoxepin is a prodrug ester or amide.
4 . The method of claim 1 , wherein the daily dosage is about 20 to about 300 milligrams.
5 . The method of claim 1 , wherein the daily dosage is about 0.1 to about 20 milligrams.
6 . The method of claim 1 , wherein the insomnia is a chronic insomnia or a non-chronic insomnia.
7 . The method of claim 6 , wherein the non-chronic insomnia is a transient or a short term insomnia.
8 . The method of claim 1 , wherein the insomnia is selected from the group consisting of onset insomnia and maintenance insomnia.
9 . The method of claim 1 , wherein the desmethyldoxepin, the salt or the prodrug is administered in a cis-(Z) to trans-(E) isomer ratio of about 99:1, 98:2, 95:5, 90:10, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, 10:90, 5:95, 2:98 or 1:99.
10 . A composition comprising desmethyldoxepin, a pharmaceutically acceptable salt thereof, or a prodrug of desmethyldoxepin other than doxepin in an amount ranging from about 0.01 to about 500 milligrams.
11 . The composition of claim 10 , wherein the amount is about 20 to about 300 milligrams.
12 . The composition of claim 10 , wherein the amount is about 0.1 to about 20 milligrams.
13 . The composition of claim 10 , wherein the amount is about 0.1 to about 10 milligrams.
14 . The composition of claim 10 , wherein the amount is about 0.1 to about 5 milligrams.
15 . The composition of claim 10 , wherein the desmethyldoxepin, salt or prodrug is in a cis-(Z) to trans-(E) isomer ratio of about 99:1, 98:2, 95:5, 90:10, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, 10:90, 5:95, 2:98 or 1:99.
16 . A method for treating insomnia comprising administering to a patient an isomer of desmethyldoxepin, a pharmaceutically acceptable salt thereof, or a prodrug thereof other than doxepin in a daily dosage ranging from about 0.01 to about 500 milligrams.
17 . The method of claim 16 , wherein the isomer of desmethyldoxepin, the salt or the prodrug is administered in a cis-(Z) to trans-(E) isomer ratio of about 99:1, 98:2, 95:5, 90:10, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, 10:90, 5:95, 2:98 or 1:99.
18 . The method of claim 16 , wherein the insomnia is a chronic insomnia or a non-chronic insomnia.
19 . The method of claim 18 , wherein the non-chronic insomnia is a transient or a short term insomnia.
20 . The method of claim 16 , wherein the insomnia is selected from the group consisting of onset insomnia and maintenance insomnia.