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Oncology NEWS International. Vol. 16 No. 8
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Focus on Pain 

Methylnaltrexone reduces opioid-induced constipation

August 1, 2007

Progenics also announced positive preliminary results of a phase I clinical study of a new oral formulation of methylnaltrexone, conducted by Wyeth. The trial is a double-blind, randomized single-dose crossover pharmacokinetic/pharmacodynamic study in subjects receiving methadone(Drug information on methadone), an opioid used to treat addiction.According to the companies, a substantial majority of patients experienced a bowel movement after receiving the higher of two doses of oral methylnaltrexone. The formulation was generally well tolerated. Based on these findings, the companies plan to conduct further clinical testing of new oral formulations.

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The Science Behind the Study

Opioids provide pain relief by interacting with specific opioid receptors located in the central nervous system. Opioids also interact with the receptors outside the CNS, such as those affecting the GI tract, altering intestinal motility and resulting in constipation that can be debilitating. Methylnaltrexone, a peripherally acting muopioid receptor antagonist, is designed to mitigate the effect of opioids on peripheral receptors without interfering with CNS pain relief.






 
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