GI Stimulant

  1. Metoclopramide (Reglan)-GI stimulant
    Indication: diabetic gastric delayed emptying, GERD, IV used for prevention of N/V due to chemotherapy, surgery, and post surgery

    MOA: GI uses: sensitizes GI tissues to effects of acetycholine leading to an increase in peristalis, N/V antidopaminergic agent

    drug induced parkinsons can occur
  2. Cisapride (Propulsid)-GI stimulant
    Indication: nocturnal heartburn due to GERD not responding to antacids or acid secretion reduction agents

    MOA: enhances the release of acetylcholine at the myenteric plexus 98% plasma protein bound, many serious drug interactions

    Available only as a compassionate useĀ  program drug

    Warning: serious cardiac arrhythmias (QT elongation)
  3. Alvimopan (ENTEREG)-GI stimulants for Ileus
    Indication: post-operative ileus following large/small bowel resection

    MOA: acting as a peripheral only mu-receptor opioid antagonst, it prevents the narcotic induced decrease in GI motility

    Does not cross BBB
  4. Methylnaltrexone Bromide (Relistor)-GI stimulants for Ileus
    Indication: restoration of bowel function in patients with late stage, advanced illness who receive opioids on a continuous basis for pain relief

    MOA: SQ injection: blocks mu-opiod receptors in GI cells thus allowing the bowels to continue to function normally

    Doesn't cross BBB
  5. Naloxegol oxalate (Movantik)-GI stimulants for Ileus
    Indication: an opiod antagonist for the treatment of opioid induced constipation in adult patients with chronic non-cancer pain

    MOA: a PEGylated derivative of naloxone, at the recommended dose levels, naloxegol functino as a peripherally-acting mu- opiod receptor antagonist in tissues such as the gastrointestinal tract, theraby decreasing the constipating effects of opiods

    Ex: pain pump due to shingles

    substrate for the _glycoprotein transporter
  6. Naldemedine (SYMPROIC)
    Indicaiton: an opioid antagonist indicated for the treatment of opiod induced constipation in adult patients with chronic non-cancer pain

    MOA: Naldemedine is a derivative of naltrexone to which a side chain has been added that increases the molecular weight and the polar surface area, thereby reducing its ability to cross the BBB

    CYP3A4 inducers and inhibitors. P-gp inhibitor
Author
Brook
ID
356465
Card Set
GI Stimulant
Description
Updated