Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Epidural method of producing analgesia|
|Abstract:||A improved method of treating pain is disclosed. The method includes administering to a subject an N-type voltage-sensitive calcium channel blocking omega conopeptide which is characterized by its ability to (a) inhibit electrically stimulated contraction of the guinea pig ileum, and (b) bind selectively to omega conopeptide MVIIA binding sites present in neuronal tissue. The method includes administering the omega conopeptide epidurally, preferably so that the compound is in prolonged or sustained contact with the epidural region.|
|Inventor(s):||Bowersox; S. Scott (Menlo Park, CA), Gadbois; Theresa (Menlo Park, CA), Pettus; Mark Raymond (San Jose, CA), Luther; Robert R. (Los Altos Hills, CA)|
|Assignee:||Elan Pharmaceuticals, Inc. (South San Francisco, CA)|
|Filing Date:||Mar 08, 1996|
|Claims:||1. In a method of producing analgesia in a mammalian subject by administering to the subject, an omega conopeptide composition which is effective (a) to inhibit electrically stimulated contraction of the guinea pig ileum, and (b) to bind selectively to omega conopeptide MVIIA binding sites present in neuronal tissue, wherein the activities of the omega conopeptide in inhibition of guinea pig ileum and in binding to the MVIIA binding site are within the ranges of such activities of omega-conotoxins MVIIA and TVIA, the improvement comprising |
administering said omega conopeptide composition via a spinal epidural route over a period of time such that said conopeptide is in prolonged contact with the epidural region, at a dosage that is in the range of an effective intrathecal analgesic dose administered over an equivalent period of time.
2. The method of claim 1, wherein said epidural administering is via continuous infusion.
3. The method of claim 2, wherein said dosage is measured over a twenty-four hour time period.
4. The method of claim 1, wherein said prolonged contact is effected by administering said conopeptide in a sustained release formulation.
5. The method of claim 1, wherein said administering is carried out in the absence in said composition of an agent for enhancing permeation of the conopeptide through meningeal membranes.
6. The method of claim 5, wherein said analgesia is produced in a patient experiencing neuropathic pain, and said administering is effective to prevent further progression of a neuropathic condition underlying said pain.
7. The method of claim 1, wherein said conopeptide is selected from the group consisting of conopeptides identified by SEQ ID NO: 1 (MVIIA/SNX-111), SEQ ID NO: 7 (TVIA/SNX-185), SEQ ID NO: 30 (SNX-236), SEQ ID NO: 2 (SNX-159), SEQ ID NO: 32 (SNX-239), SEQ ID NO: 33 (SNX-199), SEQ ID NO: 35 (SNX-273), SEQ ID NO: 36 (SNX-279), and derivatives thereof.
8. The method of claim 7, wherein said conopeptide is identified by SEQ ID NO: 1 (MVIIA/SNX-111).
9. The method of claim 1, wherein said activity to bind selectively to omega conopeptide MVIIA binding sites is further evidenced by a selectivity ratio of binding at said MVIIA binding site to binding at a site 2 omega conopeptide binding site which is within the range of selectivity ratios determined for omega conopeptides MVIIA/SNX-111, SNX-199, SNX-236, SNX-239 and TVIA/SNX-185.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.