Methods for treating allergic disorders using optically pure (-) cetirizine

• US 5,698,558 A
• Filed: 01/27/1997
• Issued: 12/16/1997
• Est. Priority Date: 09/24/1992
• Status: Expired due to Term

• Current Assignee: Sunovion Pharmaceuticals Inc. (Sumitomo Chemical Company Limited)
• Original Assignee: Sepracor Incorporated
• Inventors: Gray, Nancy M.
• Primary Examiner(s): Jarvis, William R.A.
• Application Number:
  US08/789,502
• Time in Patent Office: 323 Days
• Field of Search: 514/255
• US Class Current: 514/255.04
• CPC Class Codes: A61K 31/495 having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazinesA61K31/48 takes precedence ; with three nitrogen atoms A61K31/53
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

Methods are disclosed utilizing optically pure (-) cetirizine for the treatment of seasonal and perennial allergic rhinitis in humans while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cetirizine. The optically pure (-) isomer is also useful for the treatment of allergic asthma.

Claims

1. A method of treating the symptoms of seasonal and perennial allergic rhinitis in a human which comprises administering to a human in need of such symptomatic relief therapy an amount of (-) cetirizine, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer, said amount being sufficient to alleviate or palliate said allergic rhinitis.

2. A method of treating the symptoms of seasonal and perennial allergic rhinitis in a human, while avoiding the concomitant liability of sedation associated with racemic cetirizine, which comprises administering to a human in need of such symptomatic relief therapy an amount of (-) cetirizine, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer, said amount being sufficient to alleviate or palliate said allergic rhinitis but insufficient to cause said sedation.

3. The method of claim 2 wherein (-) cetirizine is administered by intravenous infusion or orally as a tablet or a capsule.

4. The method of claim 3 wherein the amount of (-) cetirizine or a pharmaceutically acceptable salt thereof administered is from about 1 mg to about 25 mg per day.

5. The method of claim 4 wherein the amount administered is from about 2 mg to about 20 mg per day.

6. The method of claim 5 wherein the amount administered is from about 5 mg to about 10 mg per day.

7. The method of claim 2 wherein the amount of (-) cetirizine or a pharmaceutically acceptable salt thereof is greater than approximately 90% by weight of the total weight of cetirizine.

8. The method of claim 2 wherein the amount of said (-) cetirizine 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 2, wherein (-) cetirizine is administered as a hydrochloride salt.

10. A method of treating allergic asthma in a human which comprises administering to a human in need of such therapy an amount of (-) cetirizine, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer, said amount being sufficient to alleviate symptoms of allergic asthma.

11. A method of treating allergic asthma in a human, while avoiding the concomitant liability of sedation associated with racemic cetirizine, which comprises administering to a human in need of such therapy an amount of (-) cetirizine, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer, said amount being sufficient to alleviate symptoms of allergic asthma but insufficient to cause said sedation.

12. The method of claim 11 wherein (-) cetirizine is administered by intravenous infusion or orally as a tablet or a capsule.

13. The method of claim 12 wherein the amount of (-) cetirizine or a pharmaceutically acceptable salt thereof administered is from about 1 mg to about 25 mg per day.

14. The method of claim 13 wherein the amount administered is from about 2 mg to about 20 mg per day.

15. The method of claim 14 wherein the amount administered is from about 5 mg to about 10 mg per day.

16. The method of claim 11 wherein the amount of (-) cetirizine or a pharmaceutically acceptable salt thereof is greater than approximately 90% by weight of the total weight of cetirizine.

17. The method of claim 11 wherein the amount of said (-) cetirizine or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer, is administered together with a pharmaceutically acceptable carrier.

18. The method according to claim 11, wherein (-) cetirizine is administered as a hydrochloride salt.