Therapeutic method with capsaicin and capsaicin analogues

{
  "publication_number": "US5962532A",
  "country": "US",
  "kind": "A",
  "title": "Therapeutic method with capsaicin and capsaicin analogues",
  "abstract": "Methods and compositions for treating pain at a specific site with an effective concentration of capsaicin or analogues thereof are described. The methods involve providing anesthesia to the site where the capsaicin or analogues thereof is to be administered, and then administering an effective concentration of capsaicin to the joint. The anesthesia can be provided directly to the site, or at remote site that causes anesthesia at the site where the capsaicin is to be administered. For example, epidural regional anesthesia can be provided to patients to which the capsaicin is to be administered at a site located from the waist down. By pretreating the site with the anesthetic, a significantly higher concentration of capsaicin can be used. Effective concentrations of capsaicin or analogues thereof range from between 0.01 and 10% by weight, preferably between 1 and 7.5% by weight, and more preferably, about 5% by weight. This provides for greater and more prolonged pain relief, for periods of time ranging from one week to several weeks. In some cases the pain relief may be more sustained because the disease that underlies the pain may improve due to a variety of factors including enhancement of physical therapy due to less pain in the soft tissues which may foster enhanced mobilization of soft tissues, tendons, and joints.",
  "claims": [
    "1. A method for providing relief from pain at a specific site in a patient in need of treatment thereof comprising: a) administering to the patient an effective amount of an anesthetic to alleviate the pain associated with injection of capsaicin to the painful site which results from the intense nociceptor discharge occurring during the excitatory phase following injection of the capsaicin, and b) injecting into the site capsaicin or capsaicin analogue in a dosage formulation having a concentration between about 0.01 and 10% by weight capsaicin, wherein the dosage is effective to prevent pain at the site.",
    "2. The method of claim 1, wherein the concentration of the capsaicin is between 1 and 7.5% by weight.",
    "3. The method of claim 2, wherein the concentration of the capsaicin is about 5% by weight.",
    "4. The method of claim 1, wherein the pain results from nerve injury or neuropathies.",
    "5. The method of claim 1 wherein the pain results from tendonitis, myalgias (pain originating from disease and/or inflammation of muscle), or bone or joint pain associated with inflammation or caused by injury or arritis associated with degenerative diseases, rheumatoid arthritis, or other arthritic conditions.",
    "6. The method of claim 1 wherein the pain is associated with painful trigger points.",
    "7. The method of claim 1 wherein the pain is from tumors in soft tissues.",
    "8. The method of claim 1, wherein the anesthetic is administered as a proximal, regional, somatic, or neuraxial block.",
    "9. The method of claim 1, wherein the anesthetic is administered directly to the site.",
    "10. The method of claim 1, further comprising administering a narcotic analgesic to further inhibit the irritant effects of the capsaicin.",
    "11. A kit for treatment of pain comprising: a) capsaicin or capsaicin analogues in a pharmaceutically acceptable formulation for injection in a patient at a painful site, in a dosage amount effective to alleviate the pain; b) an anesthetic in a pharmaceutically acceptable carrier for administration to a patient in an amount effective to alleviate the pain resulting from the intense nociceptor discharge occurring as a result of the injection of the capsaicin; and c) means for injection of the capsaicin into the painful site.",
    "12. The kit of claim 11 wherein the anesthetic is a local anesthetic.",
    "13. The kit of claim 11 wherein the anesthetic is a general anesthetic.",
    "14. The kit of claim 11 further comprising delivery means for the anesthetic wherein the anesthetic is formulated to effect a proximal, regional, somatic, or neuraxial block.",
    "15. The kit of claim 11 wherein the anesthetic and capsaicin are formulated together.",
    "16. The kit of claim 11 wherein the anesthetic is provided in a controlled release formulation.",
    "17. The method of claim 1 wherein the anesthetic is a narcotic anesthetic.",
    "18. The method of claim 1 wherein the capsaicin analogue is reinsiferatoxin.",
    "19. The method of claim 1 wherein the anesthetic is administered as a local anesthetic.",
    "20. The method of claim 1 wherein the anesthetic is administered as a general anesthetic.",
    "21. The method of claim 1 wherein the anesthetic is administered as a spinal block.",
    "22. The method of claim 1 wherein the anesthetic is administered as an epidural block.",
    "23. The method of claim 1 wherein the anesthetic is administered as a nerve block.",
    "24. The kit of claim 11 wherein the anesthetic is a narcotic anesthetic.",
    "25. The kit of claim 11 wherein the capsaicin analogue is reinsiferatoxin."
  ],
  "description_excerpt": "This application claims priority to U.S. Ser. No. 60/040,697 entitled \"Therapeutic Method with Capsaicin and Capsaicin Analogues\" filed Mar. 13, 1997 by James N. Campbell.\n\nThis application is directed to compositions and methods for relieving pain at a specific site, for example, associated with inflammation of joints, tendons, nerves, muscle, and other soft tissues, nerve injury and neuropathies, and pain from tumors in soft tissues or bone.\n\nCapsaicin, a pungent substance derived from the plants of the solanaceae family (hot chili peppers) has long been used as an experimental tool because of its selective action on the small diameter afferent nerve fibers (C fibers and A-delta fibers) that are believed to signal pain. From studies in animals, capsaicin appears to trigger C fiber membrane depolarization by opening cation channels permeable to calcium and sodium. Recently one of the receptors for capsaicin effects has been cloned.\n\nAlthough detailed mechanisms are not yet known, capsaicin mediated effects include: (i) activation of nociceptors in peripheral tissues; (ii) eventual desensitization of peripheral nociceptors to one or more stimulus modalities; (iii) cellular degeneration of sensitive A-delta and C fiber afferents; (iv) activation of neuronal proteases; (v) blockage of axonal transport; and (vi) the decrease of the absolute number of nociceptive fibers without affecting the number of non-nociceptive fibers.\n\nBecause of capsaicin's ability to desensitize nociceptors in peripheral tissues, its potential analgesic effects have been assessed in various clinical trials.",
  "cpc": [
    "A61K 31/245",
    "A61K 31/00",
    "A61K 31/165",
    "A61K 31/445",
    "A61K 31/47",
    "A61P 19/02",
    "A61P 21/00",
    "A61P 23/00",
    "A61P 23/02",
    "A61P 25/02",
    "A61P 29/00"
  ],
  "ipc": [
    "A61K 31/00",
    "A61K 31/165",
    "A61K 31/167",
    "A61K 31/245",
    "A61K 31/445",
    "A61K 31/47",
    "A61K 45/00",
    "A61P 19/02",
    "A61P 21/00",
    "A61P 23/02",
    "A61P 25/02",
    "A61P 29/00"
  ],
  "inventors": [
    "James N. Campbell",
    "Marco Pappagallo",
    "Richard A. Meyer"
  ],
  "filing_date": "1998-03-12",
  "publication_date": "1999-10-05",
  "grant_date": "1999-10-05",
  "priority_date": "1997-03-13",
  "application_number": "US-4129498-A",
  "family_id": "21912426",
  "cited_by_count": 178,
  "citations": [
    "US4424205A",
    "US4812446A",
    "US5290816A",
    "US4997853A",
    "US5008289A",
    "US5188837A",
    "WO1996040079A1",
    "US5762963A"
  ]
}