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 saltR.sup.1 means amino-, hydroxyl-, --NH-phenyl or --NH--CO--NH.sub.2 groups,R.sup.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.

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 saltR.sup.1 means amino--, hydroxyl--, --NH--phenyl or --NH--CO--NH.sub.2 groups,R.sup.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.