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AssigneeMemorial Sloan Kettering Cancer Center
InventorsGavril Pasternak, Yuri Kolesnikov
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Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.
A pharmaceutical composition comprising at least two compounds, one effecting opioid analgesia and one effecting local anesthesia, in amounts sufficient to potentiate an antinociceptive response when both compounds are topically administered in a physiologically acceptable topical excipient.
3 The topical pharmaceutical composition according to claim 2, wherein the opioid is selected from the group consisting of ethylmorphine, hydromorphine, morphine, oxymorphone, codeine, levorphanol, oxycodone, pentazocine, propoxyphene, fentanyl, sufentanil, lofentanil, morphine-6-glucuronide and buprenorphine, methadone, etorphine, [D-Ala2,MePhe4,Gly(ol)5]enkephalin (DAMGO), butorphanol, nalorphine, nalbuphine, naloxone benzoylhydrazone, bremazocine, ethylketocyclazocine, U50,488, U69,593, spiradoline, naltrindole, [D-Pen2,D-Pen5]enkephalin (DPDPE), [D-Ala2,Glu4]deltorphin, and [D-Ser2,Leu5]enkephalin-Thr6 (DSLET).
A method of providing topical analgesia to a subject comprising topical administration of a pharmaceutical composition comprising at least two compounds, one effecting opioid analgesia and one effecting local anesthesia, wherein the pharmaceutical composition is administered in a physiologically acceptable topical excipient and in an amount and a duration sufficient to potentiate an antinociceptive response.
The method wherein topical administration of the pharmaceutical compositions is directed to cutaneous, mucosal, vaginal, rectal, ocular, or nasal surfaces.
Dependencies are inferred from the claim text.