Opioid antagonists containing compositions for enhancing...

A - Human Necessities – 61 – K

Patent

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A61K 31/485 (2006.01) A61K 31/135 (2006.01)

Patent

CA 2373348

The invention generally relates to compositions and methods with tramadol and an opioid antagonist to enhance analgesic potency and/or attenuate one or more adverse effects of tramadol, including adverse side effect(s) in humans such as nausea, vomiting, dizziness, headache, sedation (somnolence) or pruritis. This invention relates to compositions and methods for selectively enhancing the analgesic potency of tramadol and simultaneously attenuating anti- analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of tramadol. The methods of the present invention comprise administering to a subject an analgesic or subanalgesic amount of tramadol and an amount of excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of tramadol and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of tramadol.

La présente invention concerne des compositions et des procédés à base de tramadol et d'un antagoniste opioïde permettant d'améliorer la puissance analgésique et/ou d'atténuer un ou plusieurs effets défavorables du tramadal, y compris des effets secondaires négatifs chez l'homme, comme la nausée, les vomissements, les étourdissements, les maux de tête, la sédation (somnolence) ou le prurit. La présente invention traite de compositions et de procédés permettant d'améliorer, de manière sélective, la puissance analgésique du tramadol et d'atténuer en même temps les effets d'anti-analgésie, d'hyperalgésie, d'hyperexcitabilité, de dépendence physique et/ou de tolérance associés à l'administration du tramadol. Les procédés selon l'invention consistent à administrer à un sujet une quantité analgésique ou subanalgésique de tramadal et une quantité d'un antagoniste de récepteur opioïde excitant comme le naltrexone ou le nalméfène permettant d'améliorer la puissance analgésique du tramadol et d'atténuer les effets d'anti-analgésie, d'hyperalgésie, d'hyperexcitabilité, de dépendance physique et/ou de tolérance du tramadol.

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