naldemedine

Naldemedine is a peripherally acting mu-opioid receptor antagonist (PAMORA) used to treat opioid-induced constipation in adults with chronic non-cancer pain or in those with pain related to prior cancer or its treatment who do not require frequent opioid dose escalation. It is a derivative of naltrexone, structurally modified to limit its ability to cross the blood-brain barrier, thereby antagonizing peripheral opioid receptors without affecting central analgesia. Naldemedine binds and antagonizes mu-, delta-, and kappa-opioid receptors primarily in the gastrointestinal tract, counteracting the constipating effects of opioids while sparing their central nervous system actions[1][2][3][6][7].

Brand names

SymproicRizmoic

Other names

naldemedine tosilate