Pharm

Naldemedine

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Naldemedine, Symproic

  • Indications
  1. Opioid Induced Constipation (chronic non-Cancer Pain)
    1. Severe refractory Constipation due to Opioids
  • Contraindications
  1. Severe liver disease
  • Mechanism
  1. Block Opioid binding in the intestinal tract
  2. Decreases mu-Opioid receptor mediated bowel paralysis
  • Dosing
  1. General
    1. No renal dose adjustment needed
    2. May take with or without food
  2. Take 0.2 mg orally once daily while taking Opioid
  • Efficacy
  1. See Gastrointestinal Opioid Antagonist
  2. Best efficacy in those on Opioids for >4 weeks
  3. Refractory Opioid Induced Constipation in Cancer and Palliative Care
    1. Both oral Naldemedine (Symproic) and SQ Methylnaltrexone (Relistor) are effective with benefits outweighing harms
    2. Brown (2023) Am Fam Physician 107(2):131-2 [PubMed]
  • Safety
  1. Unknown safety in pregnancy
  2. Contraindicated in Lactation
  • Drug Interactions
  1. Strong CYP3A4 inducers
  2. Strong CYP3A4 Inhibitors
  3. P-Glycoprotein Inhibitors