abstract |
The present invention provides a homo-dimer compound of naloxone or naltrexone and pharmaceutical compositions including the homo-dimer compound, wherein the two naloxone or naltrexone monomers are covalently ether-linked through phenolic hydroxyl groups of the two monomers by an ethylene residue. Accordingly, a naloxone dimer compound is represented by the formula: The homo-dimer compounds are particularly resistant to metabolism while preserving their receptor phamiacology of the corresponding monomer, therefore are useful for treating opioid bowel disorders, in particular opioid-induced constipation. |