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Development of Peripheral Opioid Antagonists: New Insights Into Opioid Effects

The recent approval by the US Food and Drag Administration of 2 medications-methylnaltrexone and alvimopan-introduces a new class of therapeutic entitles to clinicians. These peripherally acting µ-opioid receptor antagonists selectively reverse opioid actions mediated by receptors outside the ce ntral nervous system, while preserving centrally mediated analgesia. Methylnaltrexone, administered subcutaneously, has been approved in the United States, Europe, and Canada. In the United States, It is indicated for the treatment of opioid-induced constipation in patients with advanced Illness (eg, cancer, AIDS) who are receiving palliative care, when response to laxative therapy has not been ...

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