Use of methylnaltrexone and related compounds

Abstract

A method for preventing or treating opioid induced side effects including 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 orally in an enterically coated form.

What is claimed is:  
     
         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 the administration of an opioid.  
     
     
         2 . The method of  claim 1  wherein the quaternary derivative is methylnaltrexone.  
     
     
         3 . The method of  claim 1  wherein the inhibition of gastrointestinal motility is manifested as constipation.  
     
     
         4 . The method of  claim 2  wherein the methylnaltrexone is administered at a dosage 0.1 to 40.0 mg of active drug per kg body weight.  
     
     
         5 . The method of  claim 4  wherein the methylnaltrexone is administered orally at a dosage of about 0.1 to about 10 mg/kg body weight.  
     
     
         6 . The method of  claim 2  wherein the methylnaltrexone is administered as an enterically coated tablet or capsule.  
     
     
         7 . The method of  claim 2  wherein the patient's plasma level of methylnaltrexone remains below 25 ng/ml.  
     
     
         8 . 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 the administration of an opioid.  
     
     
         9 . The method of  claim 8  wherein the quaternary derivative is methlynaltrexone.  
     
     
         10 . The method of  claim 8  wherein the inhibition of gastrointestinal motility is manifested as constipation.  
     
     
         11 . The method of  claim 9  wherein the patient's plasma level of methylnaltrexone remains below 25 ng/ml.  
     
     
         12 . The method of  claim 9  wherein the methylnaltrexone is administered at a dosage 0.1 to 40.0 mg of active drug per kg body weight.  
     
     
         13 . The method of  claim 12  wherein the methylnaltrexone is administered orally at a dosage of about 0.1 to about 10 mg/kg body weight.  
     
     
         14 . The method of  claim 9  wherein the methylnaltrexone is administered as an enterically coated tablet or capsule.  
     
     
         15 . The method of  claim 8  wherein the constipation is induced by endogenous opioids.  
     
     
         16 . The method of  claim 2  wherein the enteric coating provides time release of the methylnaltrexone.  
     
     
         17 . The method of  claim 9  wherein the enteric coating provides time release of the methylnaltrexone.