Quaternary derivatives of noroxymorphone which relieve nausea and emesis
AssigneeThe University of Chicago
InventorLeon I. Goldberg
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Abstract
Quaternary derivatives of noroxymorphone are used to prevent or relieve nausea and emesis associated with the use of narcotic analgesics without interfering with the analgesic activity of the drugs. A particularly preferred compound is methylnaltrexone. The compound is administered in a concentration between 0.25 mg/kg and 1.0 mg/kg prior to or concurrently with the administration of the narcotic analgesic.
Claims11
A method for preventing or relieving nausea and emesis associated with the use of narcotic analgesics in warm-blooded animals, which comprises administering to an animal prone towards nausea or emesis on receiving narcotic analgesics, an effective amount of at least one nausea and emesis relieving compound of the formula:
- ##STR3## wherein R is allyl or a related radical such as chloroallyl, cyclopropyl-methyl or propargyl, and
- X is the anion of an acid, especially a chloride, bromide, iodide or methylsulfate anion, prior to or simultaneously with administration of the narcotic analgesic.
A method for preventing or relieving nausea and emesis associated with the use of narcotic analgesics in warm-blooded animals, which comprises administering to an animal prone to exhibit nausea or emesis on administration of narcotic analgesics, methylnaltrexone in the amount of between about 0.25 mg/kg and about 1.0 mg/kg simultaneous with or up to about two hours prior to the time of administration of the narcotic analgesic.
Dependencies are inferred from the claim text.