US2002094947A1PendingUtilityA1

Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists

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Priority: Sep 21, 1992Filed: Jan 3, 2002Published: Jul 18, 2002
Est. expirySep 21, 2012(expired)· nominal 20-yr term from priority
Inventors:Stanley M. CrainKe-Fei Shen
G01N 33/94A61K 38/33G01N 33/9486G01N 2500/10A61K 31/485A61K 31/00
49
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Claims

Abstract

This invention relates to a method for selectively enhancing the analgesic potency of a bimodally-acting opioid agonist such as morphine and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of the bimodally-acting opioid agonist. The method of the present invention comprises administering to a subject an analgesic or sub-analgesic amount of a bimodally-acting opioid agonist such as morphine and an amount of an excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of the bimodally-acting opioid agonist and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of the bimodally-acting opioid agonist.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A method for selectively enhancing the analgesic potency of a bimodally-acting opioid agonist and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of the bimodally-acting opioid agonist, said method comprising administering to a subject an analgesic or sub-analgesic amount of a bimodally-acting opioid agonist and an amount of nalmefene effective to enhance the analgesic potency of the bimodally-acting opioid agonist and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of the bimodally-acting opioid agonist.  
     
     
         2 . The method of  claim 1  wherein the bimodally-acting opioid agonist is selected from the group consisting of morphine, codeine, fentanyl analogs, pentazocine, buprenorphine, methadone, enkephalins, dynorphins, endorphins and similarly acting opioid alkaloids and opioid peptides.  
     
     
         3 . The method of  claim 2  wherein the bimodally-acting opioid agonist is morphine.  
     
     
         4 . The method of  claim 2  wherein the bimodally-acting opioid agonist is codeine.  
     
     
         5 . The method of  claim 2  wherein the bimodally-acting opioid agonist is methadone.  
     
     
         6 . The method of  claim 1  wherein the amount of nalmefene administered is 1000-10,000,000 fold less than the amount of the bimodally-acting opioid agonist administered.  
     
     
         7 . The method of  claim 1  wherein the amount of nalmefene administered is 10,000-1,000,000 fold less than the amount of the bimodally-acting opioid agonist administered.  
     
     
         8 . The method of  claim 1  wherein the mode of administration is selected from the group consisting of oral, sublingual, intramuscular, subcutaneous, intravenous and transdermal.  
     
     
         9 . A method for treating pain in a subject comprising administering to the subject an analgesic or sub-analgesic amount of a bimodally-acting opioid agonist and an amount of nalmefene effective to enhance the analgesic potency of the bimodally-acting opioid agonist and attenuate anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of the bimodally-acting opioid agonist.  
     
     
         10 . The method of  claim 9  wherein the bimodally-acting opioid agonist is selected from the group consisting of morphine, codeine, fentanyl analogs, pentazocine, methadone, buprenorphine, enkephalins, dynorphins, endorphins and similarly acting opioid alkaloids and opioid peptides.  
     
     
         11 . The method of  claim 10  wherein the bimodally-acting opioid agonist is morphine.  
     
     
         12 . The method of  claim 10  wherein the bimodally-acting opioid agonist is codeine.  
     
     
         13 . The method of  claim 10  wherein the bimodally-acting opioid agonist is methadone.  
     
     
         14 . The method of  claim 9  wherein the amount of nalmefene administered is 1000-10,000,000 fold less than the amount of the bimodally-acting opioid agonist administered.  
     
     
         15 . The method of  claim 9  wherein the amount of nalmefene administered is 10,000-1,000,000 fold less than the amount of the bimodally-acting opioid agonist administered.  
     
     
         16 . The method of  claim 9  wherein the mode of administration is selected from the group consisting of oral, sublingual, intramuscular, subcutaneous, intravenous and transdermal.  
     
     
         17 . A method for treating an opiate addict comprising administering to the opiate addict an amount of nalmefene effective to attenuate physical dependence caused by a bimodally-acting opioid agonist and enhance the analgesic potency of a bimodally-acting opioid agonist.  
     
     
         18 . The method of  claim 17  wherein nalmefene is coadministered with an analgesic or sub-analgesic amount of a bimodally-acting opioid agonist.  
     
     
         19 . The method of  claim 18  wherein the bimodally-acting opioid agonist is selected from the group consisting of morphine, codeine, fentanyl analogs, pentazocine, buprenorphine, methadone, enkephalins, dynorphins, endorphins and similarly acting opioid alkaloids and opioid peptides.  
     
     
         20 . The method of  claim 19  wherein the bimodally-acting opioid agonist is methadone.  
     
     
         21 . The method of  claim 19  wherein the bimodally-acting opioid agonist is buprenorphine.  
     
     
         22 . The method of  claim 18  wherein the amount of nalmefene administered is 1000-10,000,000 fold less than the amount of the bimodally-acting opioid agonist administered.  
     
     
         23 . The method of  claim 18  wherein the amount of nalmefene administered is 10,000-1,000,000 fold less than the amount of the bimodally-acting opioid agonist administered.  
     
     
         24 . The method of  claim 17  wherein the mode of administration is selected from the group consisting of oral, sublingual, intramuscular, subcutaneous, intravenous and transdermal.  
     
     
         25 . A composition comprising an analgesic or sub-analgesic amount of a bimodally-acting opioid agonist and an amount of nalmefene effective to enhance the analgesic potency of the bimodally-acting opioid agonist and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of the bimodally-acting opioid agonist in a subject administered the composition.  
     
     
         26 . The composition of  claim 25  wherein the bimodally-acting opioid agonist is selected from the group consisting of morphine, codeine, fentanyl analogs, pentazocine, methadone, buprenorphine, enkephalins, dynorphins, endorphins and similarly acting opioid alkaloids and opioid peptides.  
     
     
         27 . The composition of  claim 26  wherein the bimodally-acting opioid agonist is morphine.  
     
     
         28 . The composition of  claim 26  wherein the bimodally-acting opioid agonist is codeine.  
     
     
         29 . The composition of  claim 26  wherein the bimodally-acting opioid agonist is methadone.

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