Compositions and use of varenicline for treating dry eye
Described herein are methods and pharmaceutical formulations for treating dry eye disease.
1. A method of activating a trigeminal nerve in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is local administration of a spray of a liquid pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, into a nasal cavity of the individual, wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms.
2. The method of claim 1 , wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors.
3. The method of claim 1 , wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms.
4. The method of claim 1 , wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms.
5. The method of claim 1 , wherein the amount of varenicline so administered into the nasal cavity is between 5 micrograms and 500 micrograms.
6. The method of claim 1 , wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects.
7. The method of claim 1 , wherein the amount of varenicline so administered does not result in clinically significant vomiting.
8. The method of claim 1 , wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer.
9. The method of claim 1 , wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4.
10. The method of claim 9 , wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4.
11. A method of activating an anterior ethmoidal nerve in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is local administration of a spray of a liquid pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, into a nasal cavity of the individual, wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms.
12. The method of claim 11 , wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors.
13. The method of claim 11 , wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms.
14. The method of claim 11 , wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms.
15. The method of claim 11 , wherein the amount of varenicline so administered into the nasal cavity is between 5 micrograms and 500 micrograms.
16. The method of claim 11 , wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects.
17. The method of claim 11 , wherein the amount of varenicline so administered does not result in clinically significant vomiting.
18. The method of claim 11 , wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer.
19. The method of claim 11 , wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4.
20. The method of claim 19 , wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4.
21. A method of activating a nasolacrimal reflex in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is local administration of a spray of a pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, into a nasal cavity of the individual, wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms.
22. The method of claim 21 , wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors.
23. The method of claim 21 , wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms.
24. The method of claim 21 , wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms.
25. The method of claim 21 , wherein the amount of varenicline so administered into the nasal cavity is between 5 micrograms and 500 micrograms.
26. The method of claim 21 , wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects.
27. The method of claim 21 , wherein the amount of varenicline so administered does not result in clinically significant vomiting.
28. The method of claim 21 , wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer.
29. The method of claim 21 , wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4.
30. The method of claim 29 , wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4.