| abstract |
A biologically active preparation for human or veterinary use for the selective blockade of opioid binding sites of the brain responsible for respiratory depression containing in a biologically active quantity the codeinone derivative of general formula (I) or its salt; R1 means amino-, hydroxyl-, -NH-phenyl or -NH-CO-NH¿2? groups, R?2¿ means a hydrogen atom or a hydroxyl group. The invention also covers a process for selective blocking the opioid binding sites of the brain responsible for respiratory depression by administering to a patient in need of an analgetic a preparation containing a codeinone derivative of general formula (I) or its salt preferably three times per day in doses of 2.5 - 5 mg. A preferred feature of the invention is an analgetic composition containing a codeinone derivative of general formula (I) and in a mass ratio of 1 : 2-3 morphine of formula (IV) or an other, biologically equipotent agonist type opiate or opioid compound and optionally inert, pharmaceutically acceptable accompanying materials. |