51 results about "OPIATE ANTAGONISTS" patented technology

Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.

Nicotine dependency is treated by administration of an opioid antagonist. In some embodiments, rapid or ultra rapid detoxification techniques include using a combination of an effective amount of an opioid antagonist such as nalmefene, naloxone or naltrexone or a mixture of any one of these, and either clonidine or related compounds either while awake, or while under sedation or anesthesia, followed by continued administration of an effective amount of an opioid antagonist with or without agents that enhance nicotine dependency treatment. Persons are also treated for nicotine dependency with more gradual detoxification methods using administration of a combination of an effective amount of an opioid antagonist such as nalmefene, naloxone, naltrexone, or a mixture of any of these, and an effective amount of agents used to treat nicotine withdrawal including nicotine, such as that delivered by a nicotine patch, nicotine chewing gum, nicotine inhaler or other methods for delivering nicotine, antidepressants and antianxiety agents, and / or clonidine and related compounds. Administration of an effective amount of an opioid antagonist to prevent relapse, attenuate craving, and reduce weight gain during and after treatment for nicotine dependency is continued in some embodiments.

Methods and compositions for treating subjects with pain, including neuropathic pain, using opioid antagonists or combinations of opioid antagonists and opioid agonists, including, for example, wherein the amount of an opioid antagonist enhances the neuropathic pain-alleviating potency of an opioid agonist.

This invention relates to a tamper-resistant transdermal dosage form comprising an active agent, such as an opioid, or a pharmaceutically acceptable salt thereof, a free base of an adverse agent, such as an opioid antagonist, and a pharmaceutically acceptable salt of an adverse agent, such as an opioid antagonist. The transdermal dosage form allows an effective amount of the active agent, or a pharmaceutically acceptable salt thereof, to be transdermally administered to an animal. The invention further relates to methods for treating or preventing pain in an animal comprising contacting the skin of an animal in need thereof with the transdermal dosage form of the invention for an amount of time sufficient to treat or prevent pain.

Methods and compositions for treating, managing or ameliorating pain in a subject (preferably, a mammal, and more preferably, a human) comprising administration of a centrally acting (i.e., crosses the blood brain barrier) agonist of a kappa-opioid receptor and a centrally acting opioid antagonist such that the analgesia achieved by this administration is greater than with administration of either the kappa-opioid receptor agonist or the opioid antagonist alone. Preferably the kappa-opioid receptor is nalbuphine or a salt or prodrug of nalbuphine and the opioid antagonist is naloxone or a salt or prodrug of naloxone. Preferred methods of administration include mucosal (e.g. intranasal or pulmonary) and intravenous. Other kappa-opioid receptors include pentazocine and butorphanol.

The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.

The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.

Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as an immediate release product as a single dose. The controlled release nature of the tablet prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.

Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.

Bone metabolic disorders are treated by administering to an individual a therapeutically effective amount of a peripheral opioid antagonist at one or more of the opioid receptors, including the various naloxone and naltrexone analogs or a pharmaceutically acceptable salt thereof. The invention is further embodied in the use of peripheral antagonists of the opioid receptors, such as the use of naltrexone and naloxone analogs, which can be opioid antagonist with peripheral selectivity at the μ opioid receptor, for the treatment of bone loss, osteoporosis, osteopenia and other bone disorders in individuals using opioid drugs, including patients using opioids for analgesia and in opioid drug-dependent individuals

The invention relates to formulations and methods for preventing and / or treating substance abuse, addiction, withdrawal symptoms, and anticipation associated with substance abuse. In particular the invention relates to formulations comprising at least one processed Morinda citrifolia L. product, and methods comprising the administration of at least one processed Morinda citrifolia L product to prevent and / or treat substance abuse, addiction, withdrawal symptoms, and anticipation associated with substance abuse in living organisms. Embodiments of the invention further comprise Morinda citrifolia based nutraceuticals and administration thereof to affect regulation of dopamine levels, inhibition of opioid receptors, inhibition of mu opioid receptors, inhibition of kappa opioid receptors, inhibition of delta opioid receptors, acting as NMDA antagonist, inhibition of sensitization of NMDA receptors, and / or acting as opiate antagonists.

Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

Methods of treating a human suffering from the Syndrome of Lipodystrophy or one or more HIV-related abnormalities included therein are provided. One method may include administering, by a pharmaceutically effective mode, a drug composition comprising an opioidergic agent, or alternatively, an opioidergic agent and an insulin secretagogue. The method may also include administering, by a pharmaceutically effective mode, a drug composition comprising an opiate agonist and opiate antagonist, or alternatively, an opiate agonist, opiate antagonist and an insulin secretagogue.

Medicament delivery devices for administration of opioid antagonists are described herein. In some embodiments, an apparatus includes a housing, a medicament container disposed within the housing and an energy storage member disposed within the housing. The medicament container is filled with a naloxone composition that includes naloxone or salts thereof, a tonicity-adjusting agent, and a pH-adjusting agent, whereby the osmolality of the naloxone composition ranges from about 250-350 mOsm and the pH ranges from about 3-5. The energy storage member is configured to produce a force to deliver the naloxone composition.

The present invention provides compositions comprising an opioid agonist and a water-soluble, non-peptidic polymer-opioid antagonist conjugate. Among other things, dosage forms and methods of administering the dosage forms are also provided.

The present invention provides accelerated detoxification methods for the treatment of a substance abuse-related condition in a subject. A method of the present invention may comprise administering to the subject an effective amount of at least one sedative (e.g, clonidine, diazepam, or olanzapine) and a micro-dose of an opioid antagonist (e.g., naltrexone or naloxone) for at least one day; optionally administering a small dose of an opiate, and administering to the subject a detoxifying amount of a second opioid antagonist (e.g., naloxone); and may further comprise administering to the subject a third opioid antagonist (such as, naltrexone) for an extended period of time (e.g., 12 months).

The present disclosure provides compositions, and their methods of use, where the compositions comprise a ketone-modified opioid drug, wherein the drug comprises a ketone-modified opioid and a substituent on the opioid that mediates retention of the drug in the peripheral nervous system as opposed to the central nervous system following ingestion by a subject.

The invention provides an improved method of treating a human suffering from one or more conditions included within the Coronary Heart Disease Risk Factor (CHDRF) syndrome. The method includes administering, by a pharmaceutically effective mode, a drug composition having an opioidergic agent including an opiate antagonist, opiate having μ-agonist activity or combination thereof, and an insulin secretagogue.

Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, purity, ease of preparation and / or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

The invention provides an improved method of treating a human suffering from one or more conditions included within the Coronary Heart Disease Risk Factor (CHDRF) syndrome. The method includes administering, by a pharmaceutically effective mode, a drug composition having an opioidergic agent including an opiate antagonist, opiate having μ-agonist activity or combination thereof, and an insulin secretagogue.

The present invention provides methods for reducing alcohol drinking behavior in humans and treating acute alcohol poisoning through the use of neutral or negative modulating agents of the neurosteroid sites on GABAA receptors. These agents avoid the unwanted side-effects of opiate antagonists and displays specificity toward the neurosteroid binding sites on GABAA receptors.

A process for general anesthesia assisted opiate detoxification comprises administering an opiod antagonist at at least a rate of 0.6 mg / kg / hr to an addicted patient.

Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and / or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

Embodiments of the invention provide methods of attenuating, e.g., inhibiting or reducing, cellular proliferation and migration, particularly endothelial cell proliferation and migration, including that associated with angiogenesis, as well as attenuating cancerous tumor growth and metastasis, using opioid antagonists, including, but not limited to, those that are peripherally restricted antagonists.