Details for Patent: 5,972,954

Title:	Use of methylnaltrexone and related compounds
Abstract:	A method for preventing or treating opioid induced side effects including dysphoria, pruritus and urinary retention and non-opioid induced changes in gastrointestinal motility. The method comprises administering methylnaltrexone or another quaternary derivative of noroxymorphone to a patient prior to the administration of an opioid or after the onset of side effects induced by the administration of an opioid, wherein the methylnaltrexone or quaternary derivative is administered by the route selected from the group consisting of intravenous, intramuscular, transmucosal, transdermal, and oral administration, preferably administered orally in an enterically coated form.
Inventor(s):	Foss; Joseph F. (Chicago, IL), Roizen; Michael F. (Chicago, IL), Moss; Jonathan (Chicago, IL), Yuan; Chun-Su (Chicago, IL), Drell; William (San Diego, CA)
Assignee:	Arch Development Corporation (Chicago, IL) UR Labs, Inc. (Reno, NV)
Filing Date:	Nov 03, 1997
Application Number:	08/962,742
Claims:	1. A method for preventing opioid induced side effects comprising administering a quaternary derivative of noroxymorphone to a patient prior to the administration of an opioid, the side effect selected from the group consisting of dysphoria, pruritus, and urinary retention. 2. The method as recited in claim 1 wherein the quaternary derivative is methylnaltrexone. 3. The method as recited in claim 2 wherein the methylnaltrexone is administered by the route selected from the group consisting of intravenous, intramuscular, transmucosal, transdermal, and oral administration. 4. The method as recited in claim 3 wherein the methylnaltrexone is formulated with saline for administration by the route selected from the group comprising intravenous and intramuscular administration. 5. The method as recited in claim 3 wherein the methylnaltrexone is formulated with a sugar and cellulose mix for transmucosal administration. 6. The method as recited in claim 3 wherein the methylnaltrexone is formulated with binders to make a tablet for oral administration. 7. The method as recited in claim 6 wherein the tablet is coated with an enteric coating. 8. The method as recited in claim 6 wherein the methylnaltrexone is administered orally as an enterically coated tablet at a dosage of about 1.0 to about 80 mg/kg body weight. 9. The method as recited in claim 3 wherein the methylnaltrexone is administered at a dosage of about 0.03 to about 1.0 mg/kg body weight through a route selected from the group consisting of intravenous or intramuscular administration. 10. The method as recited in claim 3 wherein the methylnaltrexone is administered transmucosally at a dosage of about 0.03 to about 1.0 mg/kg body weight. 11. The method of claim 3 wherein the methylnaltrexone is administered transdermally at a dosage of about 1.0 to about 10.0 mg/kg body weight. 12. The method as recited in claim 3 wherein the methylnaltrexone is administered orally at a dosage of about 1.0 to about 40 mg/kg body weight. 13. The method as recited in claim 2 wherein the methylnaltrexone is formulated with a pharmacologically acceptable carrier. 14. The method as recited in claim 2 wherein the methylnaltrexone is administered at a dosage 0.03 to 1.0 mg/kg body weight for intravenous or intramuscular administration; 1.0 to 10.0 mg/kg for transdermal administration; 1.0 to 40.0 mg/kg body weight for administration of a methylnaltrexone tablet; and 1.0 to 80.0 mg/kg body weight for oral administration of an enterically coated methylnaltrexone tablet. 15. The method as recited in claim 1 wherein the side effect is dysphoria. 16. The method as recited in claim 1 wherein the side effect is pruritus. 17. The method as recited in claim 1 wherein the side effect is urinary retention. 18. A method for treating opioid induced side effects comprising administering a quaternary derivative of noroxymorphone to a patient subsequent to the administration of an opioid, the side effect selected from the group consisting of dysphoria, pruritus, and urinary retention. 19. The method of claim 18 wherein the quaternary derivative is methylnaltrexone. 20. The method as recited in claim 18 wherein the methylnaltrexone is administered by the route selected from the group consisting of intravenous, intramuscular, transmucosal, transdermal, and oral administration. 21. The method as recited in claim 20 wherein the methylnaltrexone is formulated with saline for administration by the route selected from the group comprising intravenous and intramuscular administration. 22. The method as recited in claim 20 wherein the methylnaltrexone is formulated with a sugar and cellulose mix for transmucosal administration. 23. The method as recited in claim 20 wherein the methylnaltrexone is formulated with binders to make a tablet for oral administration. 24. The method as recited in claim 23 wherein the tablet is coated with an enteric coating. 25. The method as recited in claim 23 wherein the methylnaltrexone is administered orally at a dosage of about 1.0 to about 40 mg/kg body weight. 26. The method as recited in claim 20 wherein the methylnaltrexone is administered at a dosage of about 0.03 to about 1.0 mg/kg body weight through a route selected from the group consisting of intravenous or intramuscular administration. 27. The method as recited in claim 20 wherein the methylnaltrexone is administered transmucosally at a dosage of about 0.03 to about 1.0 mg/kg body weight. 28. The method as recited in claim 20 wherein the methylnaltrexone is administered transdermally at a dosage of about 1.0 to about 10.0 mg/kg body weight. 29. The method as recited in claim 18 wherein the methylnaltrexone is formulated with a pharmacologically acceptable carrier. 30. The method as recited in claim 18 wherein the side effect is dysphoria. 31. The method as recited in claim 18 wherein the side effect is pruritus. 32. The method as recited in claim 18 wherein the side effect is urinary retention. 33. A method for preventing nonopioid induced gastrointestinal dysfunction comprising administering a quaternary derivative of noroxymorphone to a patient prior to the onset of the gastrointestinal dysfunction. 34. The method of claim 33 wherein the quaternary derivative is methylnaltrexone. 35. The method as recited in claim 34 wherein the methylnaltrexone is administered by the route selected from the group consisting of intravenous, intramuscular, transmucosal, transdermal, and oral administration. 36. The method as recited in claim 34 wherein the methylnaltrexone is formulated with binders to make a tablet, said tablet being coated with an enteric coating. 37. The method as recited in claim 34 wherein the methylnaltrexone is administered orally at a dosage of 1.0 to 80 mg/kg body weight. 38. The method as recited in claim 33 wherein the gastrointestinal dysfunction is selected from the group consisting of inhibition of gastric emptying and constipation. 39. A method for treating nonopioid induced gastrointestinal dysfunction comprising administering a quaternary derivative of noroxymorphone to a patient after the onset of the gastrointestinal dysfunction. 40. The method of claim 38 wherein the quaternary derivative is methylnaltrexone. 41. The method as recited in claim 40 wherein the methylnaltrexone is administered by the route selected from the group consisting of intravenous, intramuscular, transmucosal, transdermal, and oral administration. 42. The method as recited in claim 40 wherein the methylnaltrexone is formulated with binders to make a tablet said tablet being coated with an enteric coating. 43. The method as recited in claim 40 wherein the methylnaltrexone is administered orally at a dosage of 1.0 to 40 mg/kg body weight. 44. The method as recited in claim 39 wherein the gastrointestinal dysfunction is selected from the group consisting of inhibition of gastric emptying and constipation. 45. A method for preventing opioid induced dysphoria comprising administering a quaternary derivative of noroxymorphone to a patient prior to the administration of an opioid. 46. A method for treating opioid induced dysphoria comprising administering a quaternary derivative of noroxymorphone to a patient subsequent to the administration of an opioid.