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Details for Patent: 6,274,591

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Details for Patent: 6,274,591

Title: Use of methylnaltrexone and related compounds
Abstract:A method for preventing or treating the opioid induced side effect, inhibition of gastrointestinal motility is disclosed. 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 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:
Filing Date:Jul 22, 1998
Application Number:09/120,703
Claims:1. A method for preventing opioid induced inhibition of gastrointestinal motility comprising orally administering an enterically coated quaternary derivative of noroxymorphone to a patient prior to administration of an opioid, wherein substantially no quaternary derivative is released in the stomach.

2. The method of claim 1 wherein the quaternary derivative is methylnaltrexone.

3. The method of claim 2 wherein the methylnaltrexone is administered at a dosage a 0.1 to 40.0 mg of active drug per kg body weight.

4. The method of claim 3 wherein the methylnaltrexone is administered orally at a dosage of about 0.1 to about 10 mg/kg body weight.

5. The method of claim 2 wherein the methylnaltrexone is administered as an enterically coated tablet or capsule, or as enterically coated granules.

6. The method of claim 2 wherein the patient's plasma level of methylnaltrexone remains below 25 ng/ml.

7. The method of claim 2 wherein the enteric coating provides time release of the methylnaltrexone.

8. The method of claim 1 wherein the inhibition of gastrointestinal motility is manifested as constipation.

9. The method of claim 1 wherein the patient's peak and sustained plasma levels of the quaternary derivative are below about 50 ng/ml.

10. The method of claim 1, wherein the patient's peak blood plasma levels are lower than they would be if 10% or more of the same dose of quaternary derivative were released in the stomach and the rest was released enterically.

11. A method for treating opioid induced inhibition of gastrointestinal motility comprising orally administering an enterically coated quaternary derivative of noroxymorphone to a patient subsequent to administration of an opioid, wherein substantially no quaternary derivative is released in the stomach.

12. The method of claim 11 wherein the quaternary derivative is methlynaltrexone.

13. The method of claim 12 wherein the patient's plasma level of methylnaltrexone remains below 25 ng/ml.

14. The method of claim 12 wherein the methylnaltrexone is administered at a dosage 0.1 to 40.0 mg of active drug per kg body weight.

15. The method of claim 14 wherein the methylnaltrexone is administered orally at a dosage of about 0.1 to about 10 mg/kg body weight.

16. The method of claim 12 wherein the methylnaltrexone is administered as an enterically coated tablet or capsule, or as enterically coated granules.

17. The method of claime 12 wherein the enteric coating provides time release of the methylnaltrexone.

18. The method of claim 11 wherein the inhibition of gastrointestinal motility is manifested as constipation.

19. The method of claim 11 wherein the patient's peak and sustained plasma levels of the quaternary derivative are below about 50 ng/ml.

20. The method of claim 11, wherein the patient's blood plasma levels are lower than they would be if 10% or more of the same dose of quaternary derivative were released in the stomach and the rest was released enterically.

21. A method for treating opioid induced inhibition of gastrointestinal motility comprising orally administering an enterically coated quaternary derivative of noroxymorphone to a patient wherein the inhibition of gastrointestinal motility is induced by endogenous opioids.

22. A composition for preventing or treating opioid induced inhibition of gastrointestinal motility comprising an enterically coated quaternary derivative of noroxymorphone, which is substantially free of non-enterically coated quaternary derivative of noroxymorphone.

23. A composition as claimed in claim 22 in the form of a pill, tablet, capsule or granules.

24. A composition as claimed in claim 22 where the quaternary derivative of noroxymorphone is methylnaltrexone.

25. A method of treating or preventing opioid induced inhibition of gastrointestinal motility comprising orally administering an enterically coated quaternary derivative of noroxymorphone to a patient wherein the patient's peak plasma levels of the quaternary derivative do not exceed about 50 ng/ml.

26. The method of claim 25 wherein the patient's peak plasma levels of the quaternary derivative do not exceed about 40 ng/ml.

27. The method of claim 25 wherein the patient's peak plasma levels of the quaternary derivative do not exceed about 30 ng/ml.

28. The method of claim 25 wherein the patient's peak plasma levels of the quaternary derivative do not exceed about 20 ng/ml.

29. The method of claim 25 wherein the patient's peak plasma levels of the quaternary derivative do not exceed about 10 ng/ml.

30. The method of claim 25 wherein the patient's peak plasma levels of the quaternary derivative do not exceed about 2 ng/ml.
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