Compositions and methods for ameliorating pain
This invention is directed to compositions, methods and kits that can be used for the treatment or amelioration of pain.
1. An analgesic composition of formula (I):
wherein R is selected from the group consisting of NH 2 , N(CH 3 ) 2 , NHCH 3 , N(CH 2 CH 3 ) 2 , N 2 (CH 2 ) 4 CH 2 C 6 H 5 , NH(CH 2 ) 2 C 6 H 5 , NHCH 2 C 6 H 5 , NO(CH 2 ) 4 , NHCH 2 CH 2 CH 2 CH 3 , NHCH 2 C 6 H 4 CH 3 O, NHCH 2 C 6 H 3 Cl 2 , NHCH 2 C 6 H 5 CH 3 , NHCH 2 C 6 H 4 Cl, NHCH 2 C 6 H 4 NO 2 , NHC 5 H 9 , NHCH 2 CH(CH 3 ) 2 , NHCH(CH 3 ) 2 , NHCH 2 CH 2 C 6 H 3 (OH) 2 , NHCH 2 C 5 H 4 N, NHC 5 H 3 NCH 3 , NHCH 2 CH 2 C 4 H 8 N, N(CH 3 )CH 2 CH 2 OH, NHCH 2 CH(OH)CH 2 NH 2 , NHR 1 , and NR 1 R 2 , wherein R 1 is selected from the group consisting of H, OH, CH 3 , CH 2 CH 3 , (CH 2 ) 2 C 6 H 5 , CH 2 C 6 H 5 , CH 2 CH 2 CH 2 CH 3 , CH 2 C 6 H 4 OH, CH 2 C 6 H 3 Cl 2 , CH 2 C 6 H 4 CH 3 , CH 2 C 6 H 4 Cl, CH 2 C 6 H 4 NO 2 , C 5 H 9 , CH 2 CH(CH 3 ) 2 , CH(CH 3 ) 2 , CH 2 CH 2 C 6 H 3 (OH) 2 , CH 2 C 5 H 4 N, CH 2 C 5 H 3 NCH 3 , CH 2 CH 2 C 4 H 8 N, CH 2 CH 2 OH, CH 2 CH(OH)CH 2 NH 2 , an alkyl group, a haloalkyl group, a halobenzyl group, a phenyl group, —O-(alkyl), —O-(haloalkyl), —O-(halobenzyl), —O-(phenyl), an alkyl phenyl, a haloalkyl-phenyl, an alkyl-halobenzene, an alkyl-nitrobenzene, —O-(alkyl phenyl), —O-(haloalkyl)-phenyl, and a cycloalkane group, and wherein R 2 is selected from the group consisting of H, CH 3 , and an alkyl group; wherein the alkyl group comprises C1-C10 carbons, the halo group comprises F, Br, or Cl, and wherein the cycloalkane group comprises a 5 or 6 membered ring; or a pharmaceutically acceptable salt thereof.
2. The analgesic composition of claim 1 having a chemical structure selected from the group consisting of:
3. The analgesic composition of claim 1 , wherein said composition has a reduced risk of hepatotoxicity when administered in vivo.
4. A method of alleviating pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
5. A method of preventing pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
6. A method of ameliorating pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
7. A method of reducing the incidence of pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
8. A method of delaying the development of pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
9. A method of preventing the development of pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
10. A method of palliating pain in a subject, the method comprising administering to said subject afflicted with pain a therapeutically effective amount of the analgesic composition of claim 1 .
11. The method of claim 4 , wherein pain comprises neuropathic pain, nociceptive pain, or a combination thereof.
12. The method of claim 11 , wherein the neuropathic pain comprises post-surgical pain, neuropathic pain, dental pain, ophthalmic pain, arthritic pain, post- and/or traumatic pain, or a combination thereof.
13. The method of claim 4 , wherein the therapeutically effective amount comprises a dose of about 10 μM to about 10 mM of the composition is administered to the subject.
14. The method of claim 4 , wherein the composition is administered in a single dose.
15. The method of claim 4 , wherein the composition is administered at intervals of about 4 hours, 12 hours, or 24 hours.
16. The method of claim 4 , wherein the composition is administered orally, parentally, transdermally, or nasally.
17. The method of claim 4 , wherein the composition is administered in the form of a pill, capsule, cream, spray, lotion, or aqueous solution.
18. The method of claim 4 , wherein the composition exhibits analgesia, antipyresis, or a combination thereof.
19. The method of claim 4 , wherein the composition reduces the risk of hepatotoxicity by at least about 20%.
20. The method of claim 4 , further comprising administering concurrently or subsequently a therapeutically effective amount of an opioid and/or NSAID to the subject.
21. The method of claim 4 , wherein the composition is not metabolized to NAPQI.
22. A medical kit for the treatment of pain, the kit comprising: printed instructions for administering the composition to the subject afflicted with pain; an analgesic composition of claim 1 .
23. A pharmaceutical composition comprising an analgesic composition of claim 1 .