Injectable Capsaicin

Abstract

The present invention provides compositions and methods for relieving pain at a site in a human or animal in need thereof by administering at a discrete site in a human or animal in need thereof a dose of capsaicin in an amount effective to denervate a discrete site without eliciting an effect outside the discrete location, the dose of capsaicin ranging from 1 μg to 3000 μg.

1 . A method for attenuating pain at a site in a human or animal in need thereof, comprising:
 administering at a discrete painful site in a human or animal in need thereof a single injectable or implantable dose of a capsaicinoid in an. amount effective to denervate said discrete site without eliciting an effect outside the discrete location and to attenuate pain emanating from said site, said effective dose being from about 1 μg to about 5000 μg of capsaicin or a therapeutically equivalent dose of a capsaicinoid other than capsaicin.   
     
     
         2 - 4 . (canceled) 
     
     
         5 . The method of  claim 1 , wherein said dose of capsaicinoid is administered in a pharmaceutically acceptableyehicle for injection or implantation. 
     
     
         6 . (canceled) 
     
     
         7 . The method of  claim 5 , wherein said pharmaceutically acceptable vehicle comprises an agent selected from the group consisting of antimicrobial agents, isotonic agents, buffers, antioxidants, local anesthetics, suspending and dispersing agents, emulsifying agents, sequestering, chelating agents and any combinations thereof. 
     
     
         8 . (canceled) 
     
     
         9 . The method of  claim 1 , wherein said dose of capsaicinoid is injected or implanted into a site selected from the group consisting of subcutaneous, intramuscular, intrathecal, epidural, intraperitoneal, caudal, intradermal, or intracutaneous, intercostal at a single nerve, intra-articular, intrasynovial, intraspinal, intra-arterial, at a laparoscopic, surgical site, and a body space. 
     
     
         10 . The method of  claim 7 , wherein said intra-articular administration comprises administration into a joint selected from the group consisting of knee, elbow, hip, sternoclavicular, temporomandibular, carpal, tarsal, wrist, ankle, intervertebral disk, ligamentum flavum and any other joint subject to pain. 
     
     
         11 . The method of  claim 1 , wherein said dose of capsaicinoid is administered in the form of injectable or implantable microparticles selected from the group consisting of microcapsules and microspheres. 
     
     
         12 . The method of  claim 1 , further comprising administering a local anesthetic prior to or concurrently with said dose of capsaicinoid in an amount and location effective to attenuate an initial hyperalgesic effect of said administered dose of capsaicinoid. 
     
     
         13 . The method of  claim 12 , wherein said local anesthetic is selected from the group consisting of dibucaine, bupivacaine, ropivacaine, etidocaine, tetracaine, procaine, chlorocaine, prilocalne, mepivacaine, lidocaine, xylocalne, 2-chloroprocaine, and acid addition salts or mixtures thereof. 
     
     
         14 . (canceled) 
     
     
         15 . The method of  claim 13 , wherein said local anesthetic is administered to said site as a regional nerve block. 
     
     
         16 - 19 . (canceled) 
     
     
         20 . The method of claim  19 , wherein said capsaicinoid is selected from the group consisting of resiniferatoxin, N-vanillylnonanamides, N-vanillylsulfonamides, N-vanillylureas, N-vanillylcarbamates, N[(substituted phenyl)methyl]alkylamides, methylene substituted N[(substituted phenyl)methyl]alkanamides, N[(substituted phenyl)methyl]-cis-monosaturated alkenamides, N[(substituted phenyl)methyl]diunsaturated amides, 3-hydroxyacetanilide, hydroxyphenylacetamides, pseudocapsaicin, dihydrocapsaicin, nordihydrocapsaicin anandamide, piperine, zingerone, warburganal, polygodial, afntmodial, cinnamodial, cinnamosmolide, cinnamolide, isovelleral, scalaradial, ancistrodial, β-acaridial, merulidial, scutigeral, and any combinations thereof. 
     
     
         21 . (canceled) 
     
     
         22 . The method of claim  18 , wherein said capsaicin consists essentially of trans-capsaicin. 
     
     
         23 - 26 . (canceled) 
     
     
         27 . The method of  claim 1 , wherein said pain is associated with Morton's Neuroma, and the method further comprises administering to a digital nerve in a human or animal in need thereof a single injectable or implantable dose of a capsaicin in an amount effective to denervate said digital nerve without eliciting an effect outside the digital nerve, said dose of capsaicin ranging from about 1 μg to about 3000 μg. 
     
     
         28 - 31 . (canceled) 
     
     
         32 . The method of  claim 1 , wherein said pain is associated with a condition selected from the group consisting of tendonitis, bursitis, osteoarthritis, and rheumatoid arthritis. 
     
     
         33 . The method of  claim 1 , wherein said pain is associated with an orthopedic disorder of the foot selected from the group consisting of heel spurs, corns, bunions, Morton's neuroma, hammertoes, ankle sprain, fractures of the ankle or metatarsals or sesamoid bone or toes, plantar fascitis and injuries to the achilles tendon. 
     
     
         34 . The method of  claim 1 , wherein said pain is associated with an orthopedic disorder of the hand selected from the group consisting, of arthritis, carpal tunnel syndrome, and ganglion cysts. 
     
     
         35 - 37 . (canceled) 
     
     
         38 . The method of  claim 1 , wherein said pain is associated an injury selected from the group consisting of a tear of the anterior cruciate ligament, a tear of the posterior cruciate ligament, a tear of the medial collateral ligament, a tear of the lateral collateral ligament; a meniscal cartilage tear; a cartilage defect of the knee; and combinations of any of the foregoing. 
     
     
         39 - 43 . (canceled) 
     
     
         44 . The method of  claim 1 , wherein said pain at said site is associated with cancer pain. 
     
     
         45 - 49 . (canceled) 
     
     
         50 . The method of  claim 1 , wherein said pain at said site is post-surgical pain, and a single unit dose capsaicinoid injection or implantation attenuates pain at the site for at least about one week. 
     
     
         51 - 66 . (canceled)