Patent ReferencesOximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists Treatment for cocaine abuse Pharmaceutical composition and use Inhibiting the development of tolerance to and/or dependence on a narcotic addictive substance Delta opioid receptor antagonists to block opioid agonist tolerance and dependence Patent #: 5352680 InventorsAssigneeApplicationNo. 276966 filed on 07/19/1994US Classes:514/282, One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)514/811, Alcohol514/812NarcoticExaminersPrimary: Reamer, James H.Attorney, Agent or FirmForeign Patent References
International ClassA61K 031/14AbstractThis invention relates to a method of selectively enhancing the analgesic potency of morphine and other clinically used bimodally-acting opioid agonists and simultaneously attenuating development of physical dependence, tolerance and other undesirable side effects caused by the chronic administration of said bimodally-acting opioid agonists comprising the co-administration of a bimodally-acting opioid agonist which activates both inhibitory and excitatory opioid receptor-mediated functions of neurons in the nociceptive (pain) pathways of the nervous system and an opioid receptor antagonist which selectively inactivates excitatory opioid receptor-mediated side effects. This invention also relates to a method of using excitatory opioid receptor antagonists alone to block the undesirable excitatory side effects of endogenous bimodally-acting opioid agonists which may be markedly elevated during chronic pain. This invention further relates to a method of long-term treatment of previously detoxified opiate, cocaine and alcohol addicts utilizing said excitatory opioid receptor antagonists, either alone or in combination with low-dose methadone, to prevent protracted physical dependence, and to compositions comprising an excitatory opioid receptor antagonist of the invention and a bimodally-acting opioid agonist. | |